Ee 2012

www.phannacyprep.
com Evaluating Exam Review Guide

,
Pharmacy Prep
,/
Evaluating Exam
Review
.
Misbah 13iabani, Ph.D

Toronto InstiNle of PhannaceuticaI Sciences (f[PS) Inc.
Toron'o, ON M2N 6K7
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2012 .
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Pharmacy. Prep
Professional Exams Preparation Center
5460 Yong SI. Suites # 209 and 210, Toronto, ON, M2N 6K7
WWW.PHARMACYPREP.COM .
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Toronto 1Jlslitute of Pharmaceutical Sciences Inc.
02000 to 2012 Inc. All Rights Reserved.
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Disclaimer
Evaluating Exam Review Guide
Your use and review of this information constitutes acceptance of the following tenns and
conditions:
The infonnation contained in the notes intended as an educational aid only. It is not intended
as medical advice for individual conditions or treatment. It is not a substitute for a medical
exam, nor does it replace the need for services provided by medical professionals. Talk to your
doctor or pharmacist before taking any prescription or over the counter drugs (including any
herbal medicines or supplements) or following any treatment or regimen. Only your doctor or
phannacist can provide you with advice on what is safe and effective for you. Pharmacy prep
make no representation or warranty as to the accuracy, reliability, timeliness, usefulness or
. .
completeness of any ofthe information contained in the pr:oducts. Additionally, Pharmacy prep
does not assume any responsibility or risk for your use of the phannacy preparation manuals or
review classes.
In our teaching strategies, we utilize lecture-discussion, small group discussion,
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Our preparation classes and books are not intended as substitute for the advise of
NABPLEX. Every effort has been made to ensure that the information provided herein is not
directly or indirectly obtained from PEBCprevious exams or copyright material. These
references are not intended to serve as content of exam nor should it be assumed that they are
the source of previous examination questions.
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Foreword by
/Misbah BiabaiIi, Ph.D
Coordinator, Pharmacy Prep
Toronto Institute ofPharmaceutical Sciences (TIPS) Inc
5460 Yonge St. Suites 209 and 210
Toronto ON M2N 6K7, Canada
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Content
Abbreviations
Part 1: Biomedical Sciences
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Human Anatomy
Gastrointestinal System
Nervous System
Cardiovascular System
Endocrine System ../"
Renal System
Liver Function and Pathophysiology
8. Respiratory System
9. Urinary System
10. The Eve and Ear
11. Blood and Anemia
2. Biochemistry
13 Clinical Biochemistry
14 Nutrition
.. Microbiology
16. Cell and Molecular Biologv
17. Pharmacogenetics
18. Immunology
19. Immunizations
20. Biotechnology
21. Toxicology
Part 2: Pharmaceutical Sciences (35 '/)
/ _ sl-uvv1' $'10 ~
22. Pharmacy Calculations; RatiQ and Proportions
23. Pharmacy Calculations; Dilutions and Allegations
24. Pharmacy Calculations: Dose Calculations
25. Pharmacokinetics
26. Rates and Orders ofReactions
27. Pharmacodynamics
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~ Basics of Medicinal Chemistry
'29. Medicinal Chemistry and Pharmacology of Autonomic Nervous System Drugs.
. 30. Medicinal Chemistry and Pharmacology ofHistamines. Serotonin, Prostaglandin and
Non-Steroidal Anti-inflammatory Drugs
31. Medicinal Chemistry and Pharmacology ofCardiovascular Drugs
32. Medicinal Chemistry and Pharmacology of Psychiatric & Neurological Drugs
33. Medicinal Chemistry and Pharmacology Endocrine Drugs
34. Medicinal Chemistry and Pharmacology of Respiratory Drugs
35. Medicinal Chemistry and Pharmacology of Musculoskeletal Drugs
- 36. Medicinal Chemistry and Phamlacology of Antimicrobial Drugs
37. Drug Metabolism
38, Biopharrnaceutics
39. Physical Phannacy
40. Phannaceutical Excipient
41. Rheology
42. Phannaceutical Dosage FanTIS
43. Drug Delivery Systems
44. Sterile Preparations
45. Extemporaneous Compounding
6'. Pharmaceutical A"nalysis
Part III: SociallBehaviouraIlAdministrative Sciences
47. Bioethics and Professional Ethics
48. Canadian Healthcare System
49. Canadian Pharmacy Regulations and Administration
50. Social and Behavioural Aspects of Pharmacy Profession
51. Pharmacy Operations Management
52. Phannacoeconomics
53. Drug Infonnation Resources
54. The New Drug Approval Process
55. Basics ofClinical Research and Epidemiology
56. Biostatistics
57. Hospital Phannacy
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5
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Part IV: Pharmacy Practice, Therapeutics and OTe Drugs pc:J 1-
J58. Brand and Generic Name Indexes _ n
59. Prescription Processing and Medication Dispensing ''o
60. Pharmaceutical Care and Drug Related Problems __--=:j.:;::1(::===
61. Adverse Drug Reactions and Management
62. Drug Interactions
63. Therapeutic Drug Monitoring
'/64. Safety ofMedications in Special Populations
65. Identification and Prevention orDwg Toxicity
66. Professional Pharmacy Communication Skills
67. Medication Errors
68. Pharmaceutical Preparation Storage Conditions
. 69. aTe and Prescription Drugs for Dermatological and Foot Conditions
70. aTe and Prescription Drugs for Ophthalmic. Ear and Mouth Disorders
71. OTe Drugs Antihistamine. Qecongestants, Antitussives. Expectorants
/72. GTC Drugs for Nausea, Constipation. Diarrhea.
Analgesics. and Topical Pain Relievers
74. Asthma and Chronic Obstructive Pulmonary Disease (COPD)
'" 75. Smoking Cessation
76. Insomnia
,,77. Eating Disorders
78. GERD, Ulcers. Inflammatory Bowel Disease (lED) and Bowel Syndrome (mS)
" 79. Diabetes Mellitus Type I and Type 2
80. Thyroid Disorders
tWContraception
@ Gvnaecologic and Genitourinary Disorders
'( 83. Rheumatoid Arthritis, Osteoarthritis and Gout arthritis
1.84. Osteoporosis
85. Hypertension
86. Coronary Artery Diseases
l87bStroke
's1'( Congestive Heart Failure
89. Cardiac Arrhytlunias
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I90l Peripheral Vascular diseases
)1. Anticoagulants
92. Anxiety Disorder
93. Depression
94. Psychosis and Schizophrenia
95. Dementia
96. Seizures and Epilepsy
97. Parkinson's Disease
9&. AlilimiclOblal Agents
99. Anticancer Drugs and Chemotherapy
100. Pharmacognosy and Natural Products
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Abbreviations
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Abbreviation Meanine. Latin Phrase Abbreviation Meaninp Latin Phrase
,
Before Ant< b.i.d. Twice a day
"
Before meals Ante cibum la m I nuanuc
1po After meal Post eiburn f a.a.m. EvelY mornin
0 with D dexter 1a,d Everyday I ( uaauc die
"
With food S""sinister "a.a.d. Every other day
tAUl .. _I . . _'N
1 nj.d. Four times a day I ( uartcr in die
g
,
bis in die
- ' ,,1
..
"
. -,I
"i , "m
I 0.0. B mouth Per os
,< , .. 10'
Per rectum
_ ." Both "es I D.r.n. As needed Pro re nala
dr Dram 101 Pint
dx Diagnosis
I. Gram 02h Every two hours
I", Grain
101 I ouart
1 ett Drop n, Rx I nrescrilltion
h Hour 5 without sine
h, Hour 55 One halr(Jn , I,,:>
2-
h.s. At bed lime Horn sOffini stat immediately
hx History ,"DO 5U osito
ID Intradennal
"
symptoms
1M Intramuscular T, Tbsp or tbs tablespoon
IV International
ioV/I.;ts
I, tsp leaspoon
unit
IV Inlravenous I.i.d. 3X aday N\ ter in die "-Iet..l'
IVPB IV pil!vback T.O. Teleohone order
"
Kiloeram I, tincture
L Liter Ix treatment
Ib Pound
"0'
ointment
,... m, MicroQram WV VO Verbal order
mEq Milliequivalent aalaaa Of eacbl apply
ICPJa"'l>e

affected area
m'
Millil.!.ram Ad lib As desired Ad libitum
ml Milliliter
' I.
A, Ai/.J.;::
a, Ounce
1p I post 051
, ..... v-H
- .. 3-1>"", '/
102 =

"
I9'2>H
Prefix Meanin,g Prefix Meanine.
a 'an-'ana No' nol' without micro Small
ab- Away from Multi many
ante Before; fonvard o,a New
anti- ae.ainst oap Nal
auto-
"If
olil.!.o Few; less
bi Two- double- both 1 All
brady Slow Ina,., Near; beside
carein cancerous 1Dec ThrOUl!:h
contra A2ainst; ormosite I neri Around
Copyright" 2000-2011 TIPS Inc. Unauthorized reproduction or this manual is strictly prohibited and
it is illegal 10 reproduce without permission. This manual is. being used during review sessions
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Dys- Difficult; painful poly Many
Ect- Outside; out post After
en Within; in pre Before; in front of
endo within primi First
epi Above; upon retro Behind; back;..upward
ex OUl semi Half
Gynec/o woman sub Below; under
hemi half super Above; over; excess
hyper Above; excess supra Above; on top of
hypo Below; deficient sym With
infra Below; inferior syn Together; with
inter between tachy Fast
intra within tri Three
iso Same; equal uni One
macro large xero Dry
mal Bad; poor; abnormal aa\ Apply affected area
meta Change; after; beyond
--
Suffix Meaning SuffIX Meaning
ac; al; ar; ary Pertaining to otomy Incision into
algia pain ous Pertaining to
..
cele Hernia, herniation paresis Paralysis
centesis Surgical puncture pathy Disease
crine To secrete
_""nibe,,,,,,,.,,,,,,,'
crit To separate .. ,.
cytc Cell f.. :. t ".:i
cytosis Condition of cells
..

' .
desis Binding together - phonia Voice; sound
ectomy Surgical removal; excision plasty Surgical repair
emesis.
- '.
-,..-- ."". ......
S'Qwiting .. _ plegia Paralysis
.:.: .r,;.
.. J ..:..
."
,., .
":'B.'l0R.Q ' : ... tpnea'
.-. , .. .;...,
, ,-
genesis, genic, gen Producing; forming - poiesis Formation
globin; globulin protein r/rhage; r/rhagia Bursting forth
gram Record rrhea Flow; discharge
graph Instrument for recording rhesis Rupture
graphy Process of recording sclerosis Hardening
ia; iac; ic Pertaining to scope Instrument for viewing
ism CQrrqjtion scopy Process of viewing
rltis
....... J:
"
.. ,.,':'-'
somnia Sleep ";'1"
lYlysis; Iytic''-
"
.... :.:-::-
spasm Twitch
. malacia Softening stasis Control; stop
lifuegaly' '1, .. -,.. -

stenosis narrowing
oid Resembling; like therapy Treatment
(o)logist Specialist thorax Chest; pleural cavity
(o)logy Study of tocia Labor; birth
oma tumor tripsy Crushing
osis Abnormal condition trophy Growth; development
ostomy Creation of an opening tropin Nourish; development;
stimulate
Root Meaning Root Meaning
abdomin/o abdomen CystJo Bladder, sac, urinary bladder
Aden/o Gland CytJo Cell
Adip/o Fat Dacry/o Tears
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aminio amnion
De"
Tooth
AndrIa Male; man Dermlo Skin
An i/o Vessel Dennatlo Skin
Aauelo Walerv DinVo Two. double
Artcrilo
Dioslo Thirst
ArterioVo arteriole Duodenlo Duodenum
Arthr/o "oint Dur/a Dura mater
Ather/o Fat;
-
Electr/o Electricirv
Audila sound Embrv/o Embrvo
Aurlo
'"
EncenhaVo Brain
bili Bile;;;;11 Enter/a Intestines
BlcDhar/o evelid Eosinlo Red
Bronchfa bronchus Eoisli Vulva
BronchioVo bronchiliole EMhr/o Red
Bucclo ,heek sonhat>lo Esonhaftu$
Burslo riOiDI Fascilo Fascia
Caldi calcium Femor/o Femur
ca nia Carbon dioxide Fetla; felli Fetus
Carcinfo Cancer Fibul/o Fibula
Cardilo heart fundlo Fibula
C, 0 Wrist bone Gastr/o Fundus
Ce haVo head Gastr/o Stomach
Cerebrlo cerebrum Ginl!.iv/o Gums
ChoVe Bile; gall Glaudo Silver/l!rav
CholaOl'iJo Bile duct Gli/o Nerve cell
Cholecvsl/o I llallbladder Glomerul/o Glomerulus
Chondr/o cartilape Glosslo Tonpue
Coapul/o clottinp Gludo Glucose supar
CochleJo cochlea Gonadlo Sex plands
Collo Colon Gravid/alo Pre nanc
Con'uncliv/o conunctiva G nlo of< woman
CorIo heart G ncdo Woman
Cornelo cornea Hem/o Blood
Coronlo heart Heman io/o BloOd vcssel
Costlo rib Hcmatlo Blood
Crani/o cranium Heoatlo Liver
C 10 cold Hidr/o Sweat
Cutlo cuti skin Humcrlo Humerus
Cutanelo skin Hvdrlo Water; fluid
Cvanlo blue Hvster/o uterus
Root Meanin
p
Rool Meaninp:
ilelo ileum Orthlo Straip:ht
ililo ilium Ostelo Bone
Immunelo Protection OUo
E"
islo &ual Ovarilo
r ieunlo I ieiunum
oxi Oxv"en
Kalli ium Pachvlo Thick
Kinesi/o
- I"" Pancreatlo Pancreas .-
'-'cUo Milk Parlo Bear; labor; childbirth
Abdominal wall Patellolo Knee ca

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Pector/o Chest
li"amcnt
I """
Children
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linS!.ua TOnl!Ue Pelvli Children
Liolo
r"
Perinelo Pelvis
Lith/o stone Pcritonelo Perineum
Lumblo lvmnh Pcritonelo Peritoneum
Mammlo b=1 Pha!?/o Eal
Mastfo b",ast Phalan 0 and loe bones
Melanlo black Pharyn!?/o PIwy",
Mento Menses menstruation Phleb/o Vein
Melacarp!o Hand bones Photfo Lieht
Melatars/o Foot bone Phrcn/o Diaohrap:rn
Momh/o Form shaoe Pilla Hair
mucus
,
Pneum/o -
-
,
do
. -
podi Foot ..
-
. ...
-
, eVo:- __
.
?Bone malTO\v;.spinal oord...... Proctfo Rectum
.,
Mirin 0 ""drum
Psych/o, psychli Mind or soul
..Narclo;';
. .
,sleCp t
_ ..
Pub/o Pubis: pubic bone
- - ... - - -
Nos/o nose Pulmonfo Lunl!S
r,a.ratfo .n.atal Birth delivery
,
Py/o
p"
Neohr/o kidney pyello
Renaloclvis
Neur/o nerve
-
I Ouadrli Four
Nocllo nip:ht Radilo Radius
Nvctallo nip:ht R<etlo Rectum
Ocullo oe Renlo Kidney
On chlo nail Relin!o Retina
Oophor/o ovary Rhabdomy/o Skeletal muscle; striated
muscle
o thalm/o oe Rheum Wate dischar e
o tio
, ,
Rhinlo Nose
Or/o mouth SalpinWo Fallopian LUbes
Orchlo Testis' testicle S='o Flesh
Orchidlo Testis; testicle Seminlo semen
Rool Meanine. Root Meanine:
scoti bacleria Ten/o; tendlo lendon
Siallo saliva Tendon/o lendinlo tendon
Sinuslo sinus Tcstlo Testis/testicle
Somatfo bod Testicullo Testis/tesl ide
S ennau'o sperm Thoraclo chest
S here/o round Thromblo Ciol
Sphye.mlo I pulse Th rIo Thyroid 21and
Soir/o Breathe- breath Trachelo Tmcl>ea
Soleen/o soleen Tymoanlo Eardrum
Spondyllo Vertebra; vertebral Urelhralo U",thr.t
column
Steth/o Chest Ur/o Urinary lract
Stoma stomat/o mouth Vos/o Vessel
S novilo 'oint Venlo Vein
Tarslo Ankle bones Xanthlo yellow
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it is ilJegalto reproduce withoul permission. This manual is being used during review sessions
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Human Anatomy -=
h-hiS chapter reviews essenti(lls Clod definitions of systemic human anatomy terrt1inology and provide'a basic
of how the human b6dy is structured with emphasis on clinical applications. This chapter also
reviews cellular mechanism in human physiology. A special emphasis is on drug-induced diseases and effects of
adverse drug reactions on various organs.
Questions Alerts!
Common questions in pharmacy exam is to ask!
Anatomy of body movements like: abduction, adductions
Anatomical Planes: Sagittal and midsagittal plane
jointl: Patella (kneecap), hip jqints or bowl and socket (ilium, ischium, pubis), skull
, > . ,._-
bones, knee joints have poplietalspaces,
Muscles: Flexor and Extensor muscles, myocin for muscle contraction, messetEjr muscles are attached
to mandibles .
Body movements (F;,1.11
Abduction: Movement away from the midline of the body
Adduction: Movement toward the midline of the body
,Ex:tension-..,Lengtheningor straightening-of a flexed limb
Flexion; 'Bending of a b7J'dV
Dorsi'flexion: Backward of the foot
Plantar flexion: Bending of the sale of the foot downward toward the ground
Pronation: Act of turning the hand 50 that the palm faces downward
Supination: Act of turning the hand 50 that the palm is uppermost.
Eversion: Outward turning.
Fascia: Fibrous membrane separating and enveloping muscles
Anterior (ventral): Front side of the body (Example: Abdomen is anterior to the spinal
cord)
Posterior (dorsal): Back of the body (Example: Spinal cord is posterior to the stomach)
Deep: Away from the surface
Superficial: On the surface (Example: superficial veins can be viewed through skin)
Proximal: near the point of attachment to the trunk or near the beginning of a structure
(Example; The proximal end of the stomach is at the esophagus or the proximal end of the
upper bone joins with shoulder bone)
I-I
PhannacyPrep.com Human An<;itomy
Far fn;>m the point of attachment to the trunk or the beginning of a structure
(Example: The distal end of the stomach is at the small intestine)
Inferior: Below another structure. Caudal (pertaining means in' ..,
human. (Example: The urinary bladder lies inferior to the kidney)
Fig 1.1
Orcumduction
nrerior
Anato.mical Planes and
Directions
Dorsiflexion/plantar flexion
Abd'uction
Ankle Extensionlflexion
Inversion/eversion
Pronation/supination
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Pharmacyprep.com Human Anatomy
1.2)
Shoulder joint consists of humerus, scapula, synovial membrane, articular cartilage,
articular capsule, articular liquid, and ligament.
Knee joint consists of: Femur (longest bone), tibia, patella, meniscus, articular cavity,
Serous bag, and articular capsule &cartilage
Patella knee cap bone is present in knee joint -, pAoJe-f 4-4 1<'\lZ...J f).( .......r
Hip joint (socket and ball) consists of: ileum, ischium, and pubis
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Sagittal plane: Plane created by an imaginary line that is parallel to the median
Separates the body into right and left portions
Midsagittal plane (median plane): Plane created by an imaginary line that divides the body
into right and left halves_ Separates the body/body part into equal right/left portions
Parasagittal plane: Divides the body into unequal right and left portions.
Coronal plane/frontal: Divides the body/body part into anterior and posterior portions.
Transverse plane/horizontal: Divides the body/body part into superior and inferior
portions.
Oblique plane: Passes through the body/body part at an angle
Postural: Positional
Orthostatic: Standing upright
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The major skull bones include: frontal,
parietal, sphenoid, temporal, nasal, maxilla,
occipital, zygomatic, and mandible Skull have
bones, of which
Cranial bones (8)
Facial bones (14)
Ossicles (ear bones) 3
Muscles
Trapezius-7 neck
... Triceps bronchi-7 shoulder (anterior) HJoid
Biceps bronchi-7 upper arm (biceps
femorus is present in back of thigh and leg)
Quadriceps > thighs
Gluteus medium-7 hip
Psoas muscle-7 hip
largest maximusr (which forms part of the buttock)
Fastest muscle is-7 eyelid elevator

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Phannacyprep.com Human AnatQmy
Longest single sartorius muscle (which stretches from the pelvis to below the
knee. (more than 15 inches or 40 cm long)
Smallest muscle stapedius (found inside the middle' ear'(less t1i<'in 0.04 inch"(lmm)
long).
Strongest muscle.-7 masseter muscle (which elevates during mastication. It can exert a
force equivalent in 100 kg (220 Ibs).
Muscles account for 40% of total body weight.
Triceps are in arms and thighs
Cranium
Mandible
v-S
temum
0JV Costal cartilage
ItI' (,\J/ Vertebral column
Sacrum
Patella------.jB!

Calcanells
Clavicle

\,;r-----Humerus

Radius
UJna
Carpals
Metacarpals
Phalanges,
Phalanges
Human Skeleton
Knee SideView

joint capsule

Fig 1.2
1-4
Tips
Types of tissues and functions: Four basic types of tissues: Epithelial (covering), Connective
(support), Muscle (movement), nervous (control/integration)
Epithelium -7 It's functions include: Covering, Secretion, absorption, and sensitivity,
Connective -7 Support (cartilage, bone, blood, fibrous tissue of ligament (chondrocytes)
Muscle-7 (Movement) Muscle tissue, skeletal muscle tissue, cardiac musCle tissue,
smooth muscle tissues.
Nervous-7 control and integration
Fig 1.3
Human Anatomy
Smooth muscle cell
Skeletal muscle cell
Pharmacyprep.com
Tissue functions: Protection, absorption, filtration, excretion, secretion, sensory reception
Epithelial tissue: Covering/lining or glandular. Glandular: 2 basic types: Endocrine
"ductless" produce hormones, exocrine have ducts; sweat, oil, saliva, bile enzymes, mucin
(mucus).
Connective Tissue: support protection, insulation, transportation. Characteristics: large
extra cellular matrix
Four basic classes of connective tissue:
Connective Tissue Proper: Loose: adipose, areolar storage, support organs or vessels,
Dense: regular, elastic (tendons and ligaments)
Cartilage: Cushion, structure, support, and laid down before bone
Osseous (bone): Bring in beef bone, compact - rigid, spongy - marrow
Blood: RBCs, WBCs, and platelets, and plasma matrix
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1 Su'pination 2. flexion 3. Abduction
4 Extension 5. adduction 6. Parasagittaf plane
7 Sagittal plane 8. Midsagittal plane 9. Kneecap
1-5
Phannacyprep.com Human Anatomy
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plwd or fLe--- bJ

Abduct'o,4 ( )25 """ ..,....r "0.<>&)- t<.<>- ..AJ JWI--
5"''''pl,,,>41 )27 J ....+ "',l:Id1a-l,...... -4 crSl'CI':1'II(fl)i Mr
Para sagltal plane 7( ) 2-
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Transverseplane7( ISO tlL"lI<U-- flL%t-levt-o
Hip joints have 7 I )/i,f'3)2
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Flexor muscles are present in7 ( J h,p. th,Wl,. JD'.J:j
Extensor muscles are present in7 ( ) I 0 ..JO 1....t.oS
Epithelialtissueispresentin7( 22 I 15
Endothelial tissues is present in 7 ItS'J hlo
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t, /r,v-!JfJ:'d
Skull bones are 7??? (Nt/) ,os s' (
Movement away from the midline of the body (.1 I
Act of turning the hand so that the palm is uppermost I i.- I
bending part ofthe body (t)
movement toward the midline of the body (5 1
lengthening or straightening of the flexed limb
found in arms and thighs (10) ,II
Found in arms only(., I II
Separates the body into unequal right and left portions (, I
Separates the body into equal right and left portions ('lS)
Separates the body into right and left portions 0 "1
It protects the front of the joint ( l.9 /t( kJUt C-P-f
Difficulty in breathing ( l 'H...
Difficulty in swallowing ( l,2-
Difficultv in urination ( ) 3 ,
Found in limbs, foot, arms ( ) r ry) 10
Hipjoints have ( ) ;11''''''''1 f'uJ,d
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Which one is a part of the shoulder?( )
Popliteal space is present knee { , Lj
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,
10 Biceos bronchi 11- Triceps bronchi 12. dvsohagea

13 Joints 14. Hormone I!:lands 15. Blood vessels
,.
Extensor muscles 17. Flexor muscles 18. Pubis
"
Ilium 20. Ischium 21. transverse plane
22 Endocrine-..iands 23. Arteries 24. Skull bones
2S Mavin;away from body 2. closer to body 27. slicir;-vertically
28 slicing vertically from 2. Slicing vertically from 30. Slicing horizontal
middle line side lines
31 dysurea 32. Dyspnea
Adduction 7 ( ) 26

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I r PharmacyPrep.com Gastrointestinal System
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Gastrointestinal
This chapter review anatomy, physiology and pathophysiology of the gastrointestinal system, common disease
that occurs in gastrointestinal tract.
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Questions Alerts!
Stomach secretions (intrinsic factor, HCL, gastrin)
Large intestine (colon) bacteria and excessive absorption of water that cause constipation
Disease of GI system like Crohn's disease, ulcerative colitis and IBS symptoms
Food allergens like gluten (celiac), lactose and milk proteins '. I . A._
f\o\"'-' t1r S,.,.,tJ.L tV\ at I
Anus
Esophagus
Stomach
Diaphragm
Spleen
Pancreas
Transverse colon
Descending colon
Sigmoid colon
Rectum
Uver
Gallbladder
Trachea
Duodenum--t-
(of smaIIlntestlneJ
Common bile duct
Small Intestine
Ascending colon
Cecum__
Appendix
Parotid:3
SalivarY
glands.
Submandibular '
Pha&'nx
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Gastrointestinal Systeip
Mouth
Tongue has bony attachments (styloid process, hyoid bone) attached to the floor of the
mouth by frenulum.
Posterior exit from mouth guarded by a ring of palatine/lingual tonsils.
Ducted salivary glands open at various points into the mouth. This process involves teeth
(muscles of mastic.ation move jaws) and tongue (extrinsic and intrinsic muscles).
Mechanical breakdown, plus some chemical (ptyalin, enzyme in saliva) secretion.
Saliva amylase does hydrolysis of starch and glycogen into maltose.
Esophagus
The esophagus is about 10" long.
Food moves through by peristalsis.
Stomach
Esophagus
lower esophageal
sphincter
Lesser
curvature -- _
Gastric ---:::;
ulcer
Duodenal
ulcer
Duodenum
The Stomach and Duodenum
80&
Stomach
Fig 2.2
Cardioesophageal sphincter guarding entrance from esophagus.
Pyloric sphincter guarding the outlet is much better defined.
Fundus, body and pylorus recognised as distinct regions.
Stomach sec::retes both acid and mucus (for self protection).
Surface area increased by rugae; serves as temporary store for food.
Stomach secretions
Secretions Purp?se Source
Mucus Lubricant, protects surface from acid Mucus Cell
,/
Intrinsic factor Vitamin B
u
absorption (in small intestine: ilium) Parietal cell
Acid (H+) Kills bacteria, breaks down food, converts Parietal cell
pepsinogen
Pepsinogen Broken down to pepsin (a protease) Chief Cell
Gastrin Stimulates acid secretion GCell
Deficiency of intrinsic factors gives pernicious_anemia
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Gastric acid secretion mechanism: In the parietal cells CO
2
and H
2
0 are converted H+ and
HC03- catalyzed by carbonic anhydrase. The parietal cells secrete HCI into the lumen of the
stomach and concurrently absorb He0
3
- into the blood stream.
Gastric acid stimulations: Gastric acid production is stimulated by three mechanisms.
Vagal stimulation: Vagal nerve inne.rvates parietal cells and stimulates H+ secretion directly.
Histamine release: Histamine is released from mast cells in the gastric mucosa and diffuses to
nearby parietal cells.
.Gastrin: It is released in response to eating a meal, thus stimulates parietal cells to secrete H+,
.
Pathophysiology of gastric acid secretions causes gastric ulcer, duodenal ulcers and Zollinger-
E!!!.:'on syndromEL
Small intestine. Consist of duodenum, jejunum, and ileum C c:::D:T::I.... )
[Duodenum:} f'r--ja>o-'--P-Iv--,
First part of the small intestine.
C-shaped 10" (inch) long and curves around the head of pancreas and the entry of
common bile duct.
Highest drug absorption in the body takes place here.
Pancrease is a large glandular organ attached near the stomach.
Pancreas secretes intestinal enzymes, and these helps in the digestion of
carbohydrates
1Jejunum] It is 8 tolD feet long
Secretion;
Secretin -7 Stimulates pancreas to produce watery fluid, high in
concentration.
Pancreozymin -7 Stimulates pancreas to produce a viscous fluid low in bicarbonate
concentration.
The majority of food absorption takes place in the jejunum.
Ileum: It is 12 feet long. Towards the end of the small intestine, accumulations of lymphoid
tissue (Peyer's patches) are more common here.
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large Intestines: It is also known as colon
Jejunum terminates at caecufD.

Animals digest cellulose in colon
.- The large intestine reabsorbs water then eliminates drier residues as feces.
Its primary purpose is to extract (absorbed) water from feces.
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PharmacyPrep.com Gastrointestinal
Colon consists of higher flora and fauna in GI tract: 90 to 99% bacte
. ."" . t
Example: B. jragilis and C. di/ficle anaerobic and aerobic E. coli
-

Diseases of the Mouth and Jaw:
[
.:
Inflammatory disorders
Herpes labialis; also known as fever blisters or cold sores and caused by and HSV2
Mouth ulcers; caused oral thrush is caused by Candida albicans, and mon1liasis
Gingivitis; caused by Fusobacterium sp.
Disease of the Salivary Glands:
Sjogren syndrome (dry mouth, dry eyes); autoimmune disease, it is associated with
rheumatoid arthritis.
.....
Diseases of the Esophagus:
Gastro esophageal reflux disease (GERD): Reflux of acid contents into esophagus
Diseases of the Stomach: 9-.
Gastritis (inflammation of gastric lining): Caused by NSAIDs, cigarette smoking, and heavy
alcohol
Peptic ulcer: There are two main causes of Helicobacter pylori infections or drug induced
Diseases of the Small Intestine:
Duodenal ulcers: mainly caused by Helicobacter pylori and the second most common
reason is medications like NSAIDs.
Zollinger Ellison syndrome: excessive secretion of HCI
Crohn's disease (small intestine or colon), chronic inflammatory of ilium, and colon, this
can lead to fistula
Celiac disease; caused by sensiti':!.tx to gluten in cereals. This is e.M.e iqabjlity gf ab,sor..e.tion
gluten (it '!.'ainly. on Upl',l,e.uarrt9!..
Diseases of the Colon
Inflammatory bowel disease (IBD): Consist of two conditions, Crohn's disease and
ulcerative colitis.
Ulcerative colitis occurs"mainly'in colon and Crohn's diseaseioccurs'from esophageal to
I rectum.
(0./ Irritable bowel syndrome (IBS): this can cause severe chronic diarrhea, constipation,
V"' .bloating and <;Lamps, nausea and vomiting.
Pseudomembranous colitis: Clostridium difficile over growth (produce exotoxin).
symptoms indude diarrhea
Amebic colitis is caused by Entamoeba histolytica
Cholera is caused by Vibrio cholera
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PharmacyPrep.com Gastrointestinal System
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Hernia: a perturbation of GI tract at the junction of esophagus and stomach (osteomy care)
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Normal Sliding hiatal hernia
Paraesophageat hiatal hernia
Fig 2.3
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Digestion and Absorption
Only monosaccharide's such as glucose, fructose, and galactose are absorbed. Most common
site of carbohydrate absorption is small intestine.
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Carbohydrate Absorption:
Disorder of Carbohydrate Absorption: Lactose intolerance results from absence of brush
border lactase... Thus nonabsorbed lactose -
Milk intolerance can results from 2 reasons
Digestive Enzymes: Proteins that speed of biochemical reaction in digestion.
Amylase-7Hydrolyse starch and glycogen into maltose. There are amylase in saliva and
stomach
Converts maltose into glucose + glucose M oJ +o.se > 6rlu Gille -+ G
sucrose into glucose + fructose oucAiue &IXf.R-5e. '> U1ll (A)Jle. + FMC oJ'- ,
l..o ( 1'_, GUS. + (J a C--f1)! .(
- Lactase -7Converts lactose (milk) into glucose +' Lac. we ) u: U
.J:!) Trehalase degrades carbohydrate to glucose .
0./ Glucosidase breakdown sucrose and starch to glucose
\../"
J'- released mainly from the pancreases into the GI track to help breakdown fat
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-/1-lactose intolerance
/2-Milk prote.in allergies
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lipid Absorption: Bile acids emulsify lipids in the small intestine, increase surface for
digestion. . .
/ Pancreatic lipases -7 liPi, to fatty acids, monoglycerides, cholesterol and
lysolecithin. Cpl1o:sph.iLJ0Pld
lipid absorption disorders: Malabsorption of lipids thus causing fatty stools, this also referred
as Stethorrhea. Stethorrhea can cause by:
Pancreatic diseases such as pancreatitis, and cystic fibrosis.
Hyper secretion of gastrin '. E.,+ehk, b .'-fpSf't1
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I ea resection . J l-' ) I J Ii';yt....
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Bactenalovergrowth /--- -? 0 (J'
Absorption of and chymotrypsin are secreted by pancreas, which helps in
digestion of proteins
Trypsin: It secretes in the inactive form as trypsinogen and is converted to trypsin by
enzyme enterokinase.
Chymotrypsin: Secretes in the inactive form as chymotrypsinogen and converted to
chymotrypsin by trypsin.
Absorption of nucleic acid:
Nuclease--7 Nucleic acid into nucleotide.
Ribonuclease -7 Hydrolyses RNA
Deoxyribonuclease --7 Hydrolyses DNA
Absorption of water (HzO): It is isosmotic in the small intestine and gallbladder.
Absorption of Vitamins and Nutrients: Fat soluble vitamins (ADEK) are absorbed in small
intestine alon,g with other lipids. Vitamin B
12
is absorbed in the ileum and intrinsic
factor. Pernicious anemia is a result of loss of..&astric parietal cells. This is treated by vitamin
-
B
12
injection. Q"'0h\C,.\!) Yf<t:
, Absorption of Calcium: Mainly occurs in small intestine, which assisted by active form of
; vitamin D3, 1, 25-dihydroxycholecalciferol, which is produced .
-../ vit.amin D in. inadequate intestinal Ca
z
+
causmg In and
--> (J;a-J) gL
:!{W) SC-
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Absorption of. Iron: bound to hemoglobin or myoglobin) or as
In intestinal cells, 'heme iron is degra'ded to Fe
2
+ and released. :!' .I
a'p'(f>,fet:rjtimand is transported into the blood.. -
....':'r
Fr.ee Fe
2
+ circulates binds transferring and transports it from small intestine to its
storage sites in the liver and from the' liver to, the ?one marrow for the synthesis of
hemoglobin...
Cystic fibrosis , .,
It is multi organ disease but it is mainly associated with secretion.
It results from a in Cr.chanllels that is by a mutation in the cystic
transl.!lembrane cqnductance regulator (GFTm gene..
Associated with a deficienc,y.of resulting in malabsorpti,on and
steatorrhea.
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Autonomic innervations
Cholinergic
It is usually excita'tory on functions of GI tract
It is carried via the vagus and pelvic nerves
Vagus nerve innervates the esophagus, stomach, pancreases and upper large intestine
v. Pelvic nerve innervates the lower large intestine and and
Adrenergic
It usually inhibitory on the functions of GI tract
Direct post ganglion adrenergic innervations of bloOd vessels and some smooth
muscles
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Basic Tissue Layers of the GI tract.
Mucosa - innermost, moist lining membrane. Epithelium (friction resistant stratified
squamous in esophagus, simple beyond) plus a little connective tissue and smooth.muscle.
Submucosa - soft connective tissue layer, blood vessels, nerves, lymphatics
Muscularis externa - typically circular inner layer, longitudinal outer layer of smooth
muscle
Serosal Fluid Producing Single layer:
Tips
Practice answering tips from table'
1. diarrhea 2. constipation 3. Bloating
4. cramps 5. Proteases 6. nuclease
7. 2 glucose 8. colon 9. gluten present in cereal
10.. Alpha glucosidase 11 95-100% anaerobic bacteria 12 Fructose + glucose
13 Peptidase
;'.;:
14 Enterokinase 15 Chymotrypsin
16 Trypsin 17 Vit D3 18 Deficiency of intrinsic factors
19 Parenteral vit B12 20 Alcohol dehydrogenase 21 wheat
22 rye 23 oats
\ :
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PharrnacyPrep.com Gastrointestinal System
/.
The most basic part of the GI tract ( 'i J Colo V\./ l> wh hl&-h'ro
Irritable bowel disease symptoms (1,2.,:)4 P 4 I ,
The proteins are digested by ('5 ) IA'
What converts nucleic acid into nucleotides (6 ) 4- \J, I- 13,
The pernicious anemia is caused by ( ) \"6 1" I 0-- - 'L
What digest peptides into amino acids ({)) fer+t )
pernicious anemia is treated by v,I- 13r'L C -:it'(), .5c.....
What converts inactive trypsinogen into trypsin t
What enzyme oxidizes alcohol to aldehyde and acids 0') M Co L-I
What are the major bacteria present in colon (I \) q)_ lO'Or/. a
Breakdown sucrose & starch topluCQs" ( ) 0< (mu.-W 5 1-- 0"1CE
Gluten is present in ('! ) to R"'J:L 1 1"-
4- Mi',k.
Celiac is caused by
Soya milk allergies due to Mit k
A patient with chronic renal failure have deficiency of vitamin? (\1) I
Pernicious anemia is caused by -7 "V It- rl,,-
'V'}. (i/?.... i'nJ.e..<J-' .....
Maltase breakdowns maltose to -7 (i) &r (l.( U:{- -r- Cd u.
Sucrase breakdowns sucrose to -7 (\'V) OrI t{ -f'
Alcohol dehydrogenase: ethanol -7 acetaldehyde -7 acetic acid
Irritable bowel symptoms (IBS) include -7 h 1"') dr I '1, kl /
. . . 1. &levl-J'e I...
Alpha glucosidase IS -7 ( ) q Y') VY) > b.J.-P./ti- . ...
Active Vitamin D is -7 ((\) V,'t '/.2.6 d j
What is allergic component in milk?-7( ) M i (k P , .....
Bacteria in colon makes _> ( V t..\. 1< I U c,..>.eJ.,.L.
.
Cysticfibrosis is --> ( tJ\.J...h , ..z:,.h(.,Vj /If (1ft
l
PClMv<uJ-<.4
4- 15
PharmacyPrep.
PhannacyPrep.com Nervous System
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Nervous Systel11
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Questions Alerts!
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Sciatica pain site is buttocks and back of thighs
Serotonin and GABA physiological actions
Causes of multiple sclerosis
Nervous sYstem
Cerebrum
Spinal cord
Fig 3.2
Corpus
callosum
The Brain into
nervous
and peripheral nervous system. The
nervous system consist of brain and spine.
Vertebral
column
Nervous
system divided
central
system
central
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PhannacyPrep.com Nervous System
SOAnCA
Brain
- voluntary and involuntary movements. Think and decide
what to say.
- Brain stem-7ls the posterior part of the brain consist of pons and medulla oblongata and
mid brain.
- Cerebellum-7 controls balance and modifies body movements. Maintain body
coordination and balance. L'dh+-
- Spinal cord: vertebral column, epidural space, meninges, spinal cord, dorsal vertebra, and
spinal nerve
Thalamus: affects sensory levels, awareness and alertness
Meninges
The meninges are three concentric membranes that surround and protect brain and spinal
cord.
The dura mater-7outer most membrane
/- The arachnoid-7middle layer, transparent, flexible
.../. The pia mater-7 inner layer, is fine, and delicate
Cerebro Spinal Fluid (CSF); The CSF is outside of the brain and circulates through the cavities
inside the brain called ventricles.
Blood brain barrier (BBB): tM'oarrier between cerebral capilla:,W blo09 aDd cerebrospinal,.
. .fhJ.lO and the spate'.' Three functions of BBB'
/- Protects brain or exogenous toxins
v4 It prevents escape of from CNS into blood circulations
Lipids soluble drugs cross faster than water soluble drugs
All nerves of the body residing outside of the brain and spinal cord comprise the
peripheral nervous system.
Peripheral Nervous System: Periphery can be divided into sensory
(somatic) and autonomic.
Ulnar nerve-7Passes through the shoulder to wrist
- :SCiatic Runs thrwgh buttock and thigh's'down to
,: - Intercostal nerve.-?Are that anterior divisions of the thoracic
spinal nerves,
nerve --;> Runs through wrist to finger tips.
The branch of the autonomic nervous system that induces the
"flight or fight" response is the sympathetic.
Ependymal cells are specialized epithelial cells in the CNS that
produce cerebrospinal fluid. In general, positively charged ions are termed cation. On the
inner cell membrane surface of a resting neuron, there is an accumulation of negative
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(anionic) charge.
Nervous System
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In electrical terms, "potential" is synonymous with" voltage ".
An "excitable" cell is one that can quickly and dramatically change 'its resting membrane
potential. Two types of examples of excitable cells include muscle fibers and neuronal cells.
The typical neuronal resting membrane potential measures approximately -70mV. A neuronal
,impulse is- also referred to:as an action potential ,which indicates that it is a "moving" region
of v ~ l t g e change" that migrates along the neuronal cell membrane. Movement of CI- into a .
neuronal cell would make a neuron less likely to fire an action potential._
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Nerve Cell: Nerve cell consists of: Dendrite, Cell body, Axon, Myelio sheath, Synapse
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Fig 3.2
Motor
End
Plate
Skeletal Muscle Aber
1I,l'!---M'elin
L __-Axion of Motor
Neuron
Neurotransmitter Receptors
Fig 3.3
l. Sciatic nerve Blood brain Adrenal
2 barrier 3 medulla
4 Tardive dyskinesia Protects brain from 6 bradykinesia
5 endogenous &exogenous
toxins
7 Nissl substance 8 Multiple sclerosis 9 cerebrum
3-3
PharrnacyPrep:com Nervous System
10 it prevents escape of 11 lipid soluble drugs cross faster
neurotransmitter from eNS than H20 soluble drugs
into blood circulations
It is the barrier between cerebral capillary blood and cerebrospinal fluid (CSF) the CSF fills
the ventricles & the subarachnoid space )
A eNS disease where the myelin sheath of motor neurons is degenerating or being
destroyed, which interferes with neuronal impulses ( 1J )
The nerve that pass through buttocks, thighs down to foot (, )
What part of brain voluntary and involuntary movements (.:r )
Inappropriate posture of neck, face and limbs is referred as (-1) -rtU.J..J VfL dJ.f k Iv
Epinephrine is released from ( ) rVl.aJd..1P..-
Functions of blood brain barrier ,( 10) S ,II
Slow movement ( &)
The dark granular inside'neuronal cell bodies (cj ) ....... I Y)
GABAis-7( ) is
Enkephalin are -7 ( ) pepth'k +p-e,. <1r typlO rei IvI
Serotonin consist of -7 ( ) (hcJ.-.6Vi ....0
Sciatica is -7 ( ) 5 C I oJ" c.. ..s
Nor epinephrine becomes epinephrine, this reaction is catalyzed by -7 ( ) p'ntVlf e.:l..J.,o
The longest and largest nerve is --> ( 1- ) ifh ,f1 J _ 1_' . L.. N - M.J..#tj 1p.v-f i
Delirium is --> ( ) Ac..u.h.., I .,
Serotonin physiological actions include --> ( ) et

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8radlIocephl.lIc alUd
lefI common aorotld arteolY
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Aortlcarch
Pulmonarr mmk
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lnkorlorvena Qlva
Heart and Great Vessels (fig 4.2)
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Questions Alerts!
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Definitions of embolus, aneurism, dyspnea, atherosclerosis, plaques
Definitions of depolarization and repolarization
Electrode potential curve (P wave is atrial depolarization, mechanical contractions
of ventricles is QT waves)
Fig 4.4
muscle wall
of the heart
right ventricle
right atrium
ventricle
lttl---'!,ll-'"- left atrium
sinoatrial node---=--ff---'
(SAN)
atrioventricular
(AVN)
atrioventricular bundl
(AV bundle)
Conduction System of the Heart (fig 4.4)
The heart's conductive !:I stem
-
Cooductkln #Jtemof the 1'>Nr1"
laplace's law: laplace's law describes how tension in the vessel wall increases with
transmural pressure. According to laplace's Jaw, the pressure gradient across the vessel wall.
Types of pacemakers
Natural (main) pacemaker of heart
SA node
Fig 4.5
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"'\0' -;;l U ~ - \ - . - .
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latent pacemaker of heart
AV node
Bundles of His
Purkinje fibres "
Pulse direction: SA node -7 AV node -7 Bundles His -7 Purkinje fibres
Depolarization; carrying positive charge (influx of sodium ion into cell)
Repolarisation; carrying negative charge (efflux of potassium ion out of the cell)
Extracellular ions: Na, CI, Ca
Intracellular ions: K, Phosphates, Mg
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Myocardial action potential curve: Myocardial action potential curve reflects action potential,
which describe electrical activity of five phases. ThiS occurs in atrial and ventricular myocytes
and purkinje fibers
3
4
2
1
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---1
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Myocardial action Ilotentiill curye
mV
Phase 0: Rapid depolarization:
Nat enters the cell
Phase 1: Early rapid
repolarisation: K' leaves the cell
Phase 2: Plateau: cit enters the
cell
Phase 3: Final rapid
repolarisation: K' pumped out of
the cell
Phase 4: Slow depolarization: K
t
inside the cell and Nat, Ca
2t
outside the cell
Phase 1 to starting phase 3 is absolute
refractor period or effective refractory
period -7 The cell cannot respond to any
stimuli
During Phase 3 is relative refractory period -7 The cell ability to respond stimuli increases or
cell can respond to strong stimuli
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Depolarization (inwar.d current): Brings +ve charge into cell
Increase Nat influx into cell
Decrease K
t
efflux out to cell
Repolarization (outward current or hyper polarization), take +ve charge out of cell
Increase K" efflux otlt to cell
Increase cr influx into cell
Copyright 0 2000-2012 TIPS Inc. Unauthori7.ed reproduction of this manual is strictly prohibited and it is 4.3
PhannacyPrep.
PhannacyPrep.Com Cardiovascular y s t ~
Electrocardiograph Wave Forms: The electrical activity occurred during depolarization and
repolarization transmitted through electrodes attached to the body and transformed by an
electrocardiograph (ECG) in to series of waveforms;
R
o
Pwave: indicated atrial depolarization
PR interval: indicates the spread of the impulse from the
atria through purkenje fibres.
QR5 complex: indicates ventricular depolarization
5T segment: indicates phase 2 of the action potential the
absolute refractory period.
T wave: shows phase 3 of the action potential-ventricular
repolarization.
Q-T interval-7 mechanical contraction -of the ventricles (Torse de pointes)
U wave -7 caused by hypokalemia
T<?rsad,e de pointes: This is also called the Q-T interval. A problem in one of the ion channels
can prolong the Q-T interval. A prolonged Q-T interval can increase risk for a type of
arrhythmia called torsade de pointes.
Thrombus (blood dot)
Normal aorta
Thrombus is -7blood clot
Embolus is -7moving blood clot
Aneurysm is -7 abnormal dilatation of arteries
Stenosis -7 constriction or narrowing of opening
Fig 4.6
Aortawtth
abdominal aneulYsm
Ag45
Tips
Find answers from the table' ,
1. Absolute refractory 2. Repolarization 3 arrhythmia
period
4. Phase 0 5. Phase 1 to starting 6 Relative refractory
phase 3 period
7. Phase 3 8. +ve inotropic 9 -ve inotropic
10 Digoxin 11 ACE inhibitors 12 Dihydropyridine CCBs
13 Beta blockers 14 stroke 15 brain attack
16 cerebral embolism
Copyright CO 2000-2012 TIPS Inc. Unauthorized reproduction of this manual is strictly prohibited and it is 4-4
PhannacyPrep.
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Absence of rhythm ( ) !tM..,}/, ro".... .
Drugs that cause +ve inotropic eaect ( ) V'v
Rapid depolarization ( ) 'P 0
Increase in force of contraction ( ) -t VL J C
The cell cannotrespond to any stimuli ( ) phC4U.. i -+0 pt,c-Le.3
The cell ability to respond stimuli increases or cell can respond to strong stimuli (
Decrease in force of contraction ( I - Ve,. \OV\.Orf'bO pI (J
Excessive negative charge in cell occurs ( )
,rJMIL J..a., f01>J-.s bf-.... _..., ....
Select True/False Statements . U
-ro,w.. cJ..;.., po,...J4j trl.AJ 1{.J,o..,
A brain attack that occurs when a wandering clot (embolus) or some other partic:le forms
in a blood vessel away from the brain-usually in the heart (Cerebral embolism)
Drugs that cause -ve chronotropic effect (digoxin, beta blockers) 1j:dejFalse
Stroke or brain attack happens when brain cells <;fie because of inadequate blood flow to
the brainJJ!"e/False)
Copyright C 200Q.2012 TIPS Inc. Unauthorized reproduction oflhis manual is strictly prohibited and it is 4-5
iJlegallo reproduce without pennission. This manual is being used during review sessions conducted by
PhannacyPrep.
PharmacyPrep.Com Endocrine System
Endocrine System
Questions.Alerts!
Hormone of anterior and posterior pituitary gland
Hypothyroid and hyperthyroidism symptoms
Hypoglycemia and. hyperglycemia symptoms
Pathophysiology of diabetes and diabetic ketoacidosis
Hypo corticosteroids (Addison diseases) and hyper corticosteroids (Cushing s disease)
Definitions
surgical puncture of the amniotic sac
.process of viewing the urinary bladder
DysmenQ,,ithea: Painful periods
Embryology: study of the growth and development of the human organism
Gynecologist: specialist in the diseases of the female reproductive system
HydrocelXi,accumulation in the scrotum;
Menorrhagia: Excessive bleeding during menstruation
Nephritis: Inflammation of the kidney
Primigravida: first pregnancy
Spermatogenesis: creation of new sperm
Urology: studr of urinary tract /
yf-o-p I
Endocrine system
Consists ofa group of organs that have NO DUCTS and therefore are also known as
DUCTLESS GLANDS that secrete hormones directly into the blood stream..
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Endocrine System
Fig 5.1
Female
"'""
""'- (tt'popIf'sis)
...........
.......,
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Endocrine glands Male
Major endocrine glands: Pituitary .Gland (present under hypothalamus), the master
endocrine gland. Testes, Ovaries, Thyroid Gland (neck), Adrenal Gland (on kidney), Pancreas
Gland (endocrine and exocrine)
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Parathyroid Gland (neck)
Thymus Gland (chest)
Pineal Gland (brain)
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Pituitary Gland
Located at the base of the brain.
Consists of two parts: anterior lobe and posterior lobe.
It is sometimes known as the master gland.
It controls the functions of other endocrine glands and is in turn controlled by the
hypothalamus.
Endocrine Tvpes of hormone Target tissue PhVsiologic actions
Gland
Hvpothalam Houses releasing and Anterior pituitary Controls release of anterior pituitary
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inhibitine. hormones hormone
Anterior
,
ThVroid-sti mulating ThVroid Production of thyroid hormone (T4 and TJ,
Pituitary hormone (TSH) and calcitonin) -
-
gland -
Adrenocorticotropic (ACTH) Adrenal cortex Secretion of cortisol
5-2
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Endocrine System
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Growth hormone (GH) Bones; soft Stimulates growth of bones and soft tissues
. tissues
Follicle-stimulating Females; ovary Promotes growth of ovarian follicle;
.
hormone (FSH) Stimulates estrogen secretion
-
Males: Testes Stimuiates sperm production .
luteinizing hotffiofle (lH) Females: ovary ovulation
:Stimula,tes orOl!esterone secretion
.
Males: Testes
,
:Stimul,fi'es testosterone secretion
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Prolactin Females: breast breast development; stimulates
-
. milk secretion
Posterior
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Kidney Causes Y/ater retention
Pituitary . mon oJ.
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Uterus causes contraction fW./'-VJ
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Breasts Gauses o(milk
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Pineal iMelatonin Brain; anterior Sets the bocfy's "'time clock"
,
pituitary; Causes sleep in response to darkness
reproductive

organs; possibly
other sites
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Thyroid Thyroid hormone (T,and Most cells Increases the metabolic necessary for
,
T '____. normal growth and development.
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Parathyroid Parathyroid hormone Bone; kidney; Increase amount of calcium in the

intestine bloodstream. Decreases amount of
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phosphate in the bloodstream
ca :lI: Bones? Blood
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Thymus Thymosin T IvtpphOeytes Enhances the production ofT Iymphoeytes
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Insulin Most cells use and storage of nutrients
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Secreted frorr(beta
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partic1,llarty glucose, after eating
..
Glucagon Most cells MaiRt9ins glucos.e le.vets in the bloodstream

Secreted from alpha cells during periods of 00 food
Somastatin Digestive system Inhibits digestion and absorption of nutrients
Secreted from delta cells
Adrenal Epinephrine Kidnev Increases Na' retention and K' excretion
Medulla
Adrenal Lona Aloosterone Kidney Increases Na' retention and K' secretion
cortex glomerul -
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, Most cells ln.creases glucose in the blo/'dstre9m... ,
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Z. Androgens Females:-bone Puberty growth spurt and sex drive in
and brain females -
Testes Testosterone Male sex organs; Stimulates production of sperm; resporfsible
(malel body as a whole for development of sex characteristics;
.
promotes sex drive
Ovaries Estrogen Female sex
.
Stimulate ulll!!ine and breast growth;
(female) organs; bod.,. as a responsible for se;characteristics
wtlole
Progesterone Uterus Prepares for pregnancy
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(.: effects of some pituitary hormones ., d
, ;. Somatostatin: opposes the, effects ofGrowth Hormone-Releasing Honnone (GHRH)
; Prolactin: It is synthesizec'fand secretea" by cen"s in the anterior pituitary gland, breast (J
'. . and th,tj..,deciduas.
( :..1 Effects
t . Cstlur Stimulates the mammary glands to produce milk (lactation).
Provides the body withsexmfl gratification after sexual acts
\. j immune tolerance of'the fetus by the: maternal organism during pregnancy.
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() Stimulate proliferation ofoligodendrocyte precursor cells which differentiate into
oligodendrocytes, the cells responsible for the formation of myelin coatings on
axons in the central nervous system
Thyroid Gland (Fig 5.3): Secretes thyroid hormones, which in tum control the body's
mclabol ic ratc.
Types ofthyroid hormones
Thyroxin (T.)
Naturally occurs in leve (L) isomer
Foml produced in the thyroid gland
,Gol1verted:in the liverJand-other organs to T)
Controls the of metabolism in the body
T. -? T,
5-5
Triiodothyronine (T3)
MetaboJically active form
Calcitonin (a peptide) .--,:-;c---,,--;;-::;:;--;:-:,
Secreted brlparafollicular cells (C- cells) 1
Reduces blood calcium IOn concentration by moving Ca from blood to
bones
Hypocalcemic honnone
Indicated in treatment of osteoporosis associated vertebral fracture.
Hypercalcemia stimulates calcitonin production.
Functions of thyroid honnones:
Growth
Development
Proper function of all body system
Maintenance of all body tissues
carbohydrate, fat, protein, and vitamin metabolism (Basal Metabolic Rate)
Affects the secretion of other hormones (insulin, NE, Epi, cortisol, estrogen and
testosterones.
Mechanism of action
At the target cell, proteases split protein carrier ofT from the thyroid hormone and most
ofT4 is deiodinated to T).
T) (and probably some T4) enter the cell through membrane transport proteins and bind
to a specific nuclear receptor.
The T)-T receptor complex moves into the nucleus, where it binds to specific
sequences of DNA in the promoters of responsive genes.
The effect of the hormone-receptor complex binding to DNA is to modulate gene
expression, either by stimulating or inhibiting transcription of specific genes.
Hypothyroidism: Thyroid gland is under active and produces insufficient thyroid hormone.
Deficiency of thyroid hormones I I J
Dwarfism M 'J) t+ k.-. I. It1
Mental retardation (J _
Myxedema
Hashimoto
Causes
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Sensitive TSH assay
o Commonly used in patient receiving replacement therapy to con'trol treatment
o Replacement therapy indicated in hypothyroidism or healthy adult with
levothyroxine
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Endocrine System
Auto immune reaction (Hashimoto's thyroiditis)
o Most common cause of hypothyroidism
o Common in elderly women _
ii) Treatment of hyperthyroidism (surgical removal) )"'"
Symj5fofus;" , Y\
Sensitivity to@)
Dry flaky skin
Coarse hair
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Slowed speech
Puffy face, hands, feet
Hearing ldss
J Decreased libido
Slow return of deep tendon reflexes
If untreated myxedema and coma may
develop.
--./' Weight gain , , I. _I
J Constipation -:3.> Ncr lGO-'e.L
1m aired memory
Hypertensio bradycardia
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o Th,is is not separate test but estimation mathematical
interpretation of relationship ofRT3U and serum T4 levels.
Hypothyroidism and pregnancy
Hypothyroid females during child bearing period have ovulation -
infertile _ ; ."
Hypothyroid pregnant woman should receive an adequate dose thyroxine, necessary
for development of the fetal brain.
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Hyperthyroidism
Ove roid gland causing an abundance of thyroid hormone.
hyrotoxicosis the general term for over activity ofthe thyroid gland
Common forms 0 ype yroidism
Graves disease (diffuse toxic goiter)
Plummer's disease (toxic nodular goiter)
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Symptoms
Diffusely enlarged non tender goiter
Nervousness, irritability, anxiety and insomnia
Heat intolerance and profuse sweating
Weigh loss in spite of increased appetite
Tremor and muscle weakness
Tachycardia
Diarrhea
Grave's disease (diffuse toxic goiter)
Most common form of hyperthyroidism
disorder, antibodies (long-acting thyroid stimulators) bind to and I _J. e,.,.!C1U1A
activate TSH receptors .2S C)'\-OU- r'
Plummer's disease (toxie nodular goiter) . 1:<> 1,25 d ecJc1to-<rl
Less common than Grave's dIsease eAch.... (..... o-d(,(.v-Ai Vd-::b )
Less common Cenns
Jodbasedow phenomenon: Over production of thyroid hormone following
sudden increase in iodine ingestion
Factitious hyperthyroidism: Occurs with abusive ingestion of thyroid
replacement agents, in a misguided effort to lose weight.
Methods of controlling hyperthyroidism:
Antithyroid drug therapy
Surgical thyroidectomy
Destruction ofthe gland by radioiodine isotopes
(
Hyperthyroidism test
Serum lotal thyroxine (Free T.,)
o Elevated T4 indicates hyperthyroidism
o Decreased T4 indicates hypothyroidism
Serum total triiodothyronine (1T3)
4-kJh 111..11.'6/5 c:a-r ,,., 101"
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L, pTH
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o Disproportionate rise indicated hyperthyroidism '!'.
o Useful In early detection and rule out of hyperthyroidism Ieet Ylu'mloM. q.,ach'( '1-1> \
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Parathyroid Glands: 4 tiny glands in the posterior surface of the thyroid land, whiCh is I
positioned on the esophagus, produce parathyroid honnone (PTH), whio regulates the
calcium metabolism in the body I' less bo W!.-
Hypoparathyroidism h'DJA.,
Decrease production of PTH \..-...- A..eSlQ.I..{J
Decrease blood calcium \-ltJL6': j f'TH .., eWal<4-
lncrease blood phosphate levels , t4 .
Causes convulsions or ec.JOU/,M.--' 0 -
Causes hypokalemia '. AM, tJA _
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Causes neuromuscular irritability i I i"l I-Lc.... 1.u>N..- )
Hyperparathyroidism { C B6
Increase production of PTH L-
Increase blood calcium levels tk wv.L /
PTH tht. /ltcJ,1tnJf!i0V'v '1 f1., r'
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Glycogenesis: increased glycogen storage (liver, muscle)
Gluconeogenesis: synthesis ofglucose from non-carbohydrate source ('J:/Jr1' ?"1' ....
Lipogenesis: fatltriglyceride storage (adipose tissue)
t Glucose uptake into cell
--
Decrease blood phosphate lev,e1s
Causes muscle weakness
Causes muscle atrophy
Causes fatigue
Endocrine System
,
,
Has the acini which produces digestive enzymes f' .J v..P'('i'"
Islets produce 3 types of harmones; r b \jl. \ ..
o lnsulinproducedhybetacells jl-\YI' I _WA t 0\1"';.-, f'h"
o Glucagon produced bya-cells / l)O- _. U
o Somatostatin prodnced delta cells 0
Insulin
Pancreas
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Insulin requirement
Increase:
_ heavy meals
__ stress
infections
__ pregnancy
Insulin requiremenl
decrease:
Physical activity
Exercise
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Insulin acts on liver, adipose tissue and muscles.
Produced by beta cells of islets of langerhans.
Insulin is peptide
Stored in vesicles in combination with zinc
51 amino acid chain
Half life insulin is 3 to 5 min Controls blood glucose concentration
Decrease insulin secretion
Carbohydrate metabolism
Increase glucose uptake
Decrease glycogenolysis
Decrease ketogenesis
Decrease glucogenesis
Increase lipogenesis
,
Protein metabolism:
5-8
PhannacyPrep.Com
Increase RNA and DNA synthesis
protein synthesis
Increased cell growth
Increased amino acid
Fat metabolism:
Increase storage of fatty acid in adipose tissue
Increase lipogenesis
Decrease lipolysis
Endocrine System.
Glucagon
breakdown of glycogen to glucose (glycogenolysis) in the liver
Increase blood glucose levels
DIABETES MELLITUS
This is a primary disorder of carbohydrate metabolism that exhibits the following
characteristics: A defective or deficient insulin secretory response, Glucose
and Hyperglycemia
Types of diabetes:
Insulin-Dependentn'ype I (IDDM)
Non-Insulin DependentfType 2 (NIDDM)
econdary Diabetes (e.g. pancreatic disease)
Impaired Glucose tolerance
Gestational Diabetes (i.e. glucose intolerance w/onset during pregnancy)
Diabetic Patient
Insulin or resistance
* Polyphagia (increased appetite)
tGlucose in blood (hyperglycemia)
Osmotic diuresis
Glucose in urine (glycosuria)
* Polyuria (profound loss of water and electrolytes)
* Polydipsia (intense thirst)
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PhamiacyPrep.Com Endocrine System

Late Complications:
Diabetic microangiopathy; Atherosclerosis: myocardial infarction, cerebral stroke,
gangrene of the lower extremities
Diabetic nephropathy; Progressive proteinuria and chronic rena', failure (eRF)
Diabetic retinopathy; cataract [annalion or glaucoma
Diabetic Neuropathy pain (numbness, tingling, pin feeling and burning)
Symmetric peripheral neuropathy- affects molor and sensory nerves oflhe lower
ex.tremities: Schwann cell injury. myelin degeneration, axonal damage
Autonomic neuropathy- sexual impotence, bowel and bladder dysfunction
Prevention:
Routine screening for diabetes
Modification ofCV risk factors; weight, BP, cholesterol, and smoking
Home health aids
Diabetes Insipidus (DI)
Anti diuretic nonnone (vasopressin) deficiency causes diabetes insipidus
Insufficient ADH due to dysfunction of hypothalamic nuclei (eg. tumors,
hydrocephalus. histiocytosis, trauma)
Passage of large volumes of dilute urine
Decrease in ADH causes:
Large volume of dilute urine, Polyurea, Polydipsea, Polyphagea
Treatment: Anti diuretic honnone
THYMUS GLAND
Regulates the development ofT-lymPhocytes in immune system)
PINEAL GLAND
Small cone shaped gland
Smallest of all glands located in mid brain
Large in children and begins toshrink at pubeI1Y
Only brain structure that does not come in a pair
Produces melatonin and dimethyl tryptamine in the dark
Functions
rnnuences circadian rhythms e.g. sleep and temperature
Sexual development
mcmbolism
Regulates the mating behavior
Regulates day and night cycle
Adrenal Gland (fig 5.4): Two adrenal glands one on top ofeach kidney
Inner part (medulla)
Secretes epinephrine (adrenalin)
Epinephrine increases BP, HR. vasoconstriction and blood supply to skeletal muscle
5-10
PhannacyPrep.Com. Endocrine System
Norepinephrine increases effects ofepinephrine
Outer part (cortex)
Secretes corticosteroids, androgens and mineralcorticoids
AC1B regulates the secretion of mineral corticoids. e.g.
Aldosterone: Helps regulate salt and water balance by retaining salt and water
and excreting potassium
Glucocorticoids
Control glucose metabolism and protein synthesis.
The principle glucocorticoids are cortisol and cortisone
Androgens are male sex honnones mainly testosterone.

Functions of ACTH
ACTH stimiltatesthe:cortex ,
corticosteroids, mainly.glucocorticoids but also mrneralcorlicoids and sex steroids
.. . . ... ;.,.. .'.: . '::;::t:'iH':'i:;if'( ll{
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ACTH IS also related to
The half-life of ACTH in human blood is about 10 minutes.
Hypo corticosteroids::A:ddison's disease.(chronic insuffici,ency, .or
hypocortisolism) '. r' : i:
Causes: Auto immune reaction, HIV and IB
Signs and symptoms
Chronic fatigue that gradually worsens
Muscle weakness
Weight loss amI loss of appetite
Nausea, diarrhea, or vomiting
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Treatment t/@
Replacement of missing cortisol and fludrocortisones f.-) tJe4--L &w .
Hypercorticosteroids: Cushing's syndr.ome or
caused by high levels of cortisoJ in the blood. '.I I'
Signs arid symptoms:
Rapid weight gain'
Moon face
Buffalo ijump .
Reduced libido
Easy bruising"
Treatment
5- I I
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PhannacyPrep.Com Endocrine System
Removal of adrenals
Post operative steriod replacement. (hydrocortisone or prednisolone)
Menopause
Ovaries: Produces two honnones estrogen and progesterone;
Estl'"ogcn: ConlrOls the development of female sex characteristics and reproductive system
Progesterone: Prepares the lining of the uterus for implantation of a fertilized egg
Readies the mammary glands to secrete milk
Pregnancy test: Human chodonic gonadotropin (heG) honnone levels are elevated in first 3
months of pregnancy ( the first trimester). Progestin's in pregnancy is produced by: Ovaries, corpus
luteum and placenta.
Dysmenorrhea ., dJoc c 4c,c.!
Menstrual pains are referred as dysmenorrhea.
- It is most common from age 20 to 25
Primary when no underlying cause is found
Secondary when a cause is idenlified as a gynecological disorder
Cessation of menstrual periods is referred to as menopause
Occurs when the ovaries slap producing estrogen
Ovarian follicles are depleted at approximately 51 year of age.
Most common symptoms: Hot flushes, Night sweat, Mood swings,
Sleeplessness, Lethargy, and Depression
Urogenital atropy (this leads to: dryness oflhe vagina, dyspareunia; painful
intercourse)
Ovulation cycle and menstrualion
During the menstrual cycle estrogen is prodUCed by the ovarian follicles
After ovulation estrogen is produced by the corpus luteum.
During pregnancy ovulation does nol occur.
It is suppressed by high levels ofestrogen and progesterone's.
/
.' Dehydroepiandrosterone (DHEA).
Androstenedione (Andro)
Androstenediol: Androsterone
Dihydrotestosterone (OHT)
Androsterone
Other androgens are
Endometriosis
Common cause of secondary dysmenorrhea tV
Endometriosis gives:
Pelvic pain
Spotting before normal periods
May cause infertility
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Endocrine System
Menstroal cycle
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Luteum C. Luteum
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1 3 5 7 9 11 1 1 17
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2 4 6 8 10 12 14 16 18 20 22 24 26
Day of Menstrual Cycle
{Average values. Durations and val .
differentfemales or different cycles.yes may differ between

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Endocrine System
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1. adrenal medulla 2, pituitary gland 3. posterior pituitary gla.nd
4. diabetes insipidus 5. glucose 6. H20 + CO2
7. excessive urination 8. outer adrenal cortex 9. sensitivi.ty to cold
10. bradycardia 11. Weight gain 12. Glycogen
13. constipation 14. dry skin 15. weight loss
16. tachycardia 17. diarrhea 18. sensitivity to heat
19. sweating 20. palpitation 21. fatigue
22. polyhagia 23. polyurea 24. Blurred vision
25. polydipsea
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Gluconeogenesis: fats & proteins-7( ) ..f tJ Gr f
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What hormones are released from posterior pituitary gland? ( ) AeY).4 0 Y"4 Of< I Vv
Hypothyroidism laboratory investigation include ( ) 'r") 4- 1'1 1
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Aldosterone is released from? ( ) , ., ...J
Testosterone to 5-hydroxy testosterone is catalyzed by? ( ) S;-,?f
Diabetes mellitus symptoms? ( ).3 pO(;j (t.(}..RA.-) ch..pllc......J
Hypoglycemia symptoms? ( ) J pe-.{,pI.J-J-.
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Addison disease is -7 ( ) J
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5-14
PhannacyPrep.Com
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Renal System
Questions Alerts!
Filtration, Secretion and Reabsorption process \
Symptoms of renal disease ct- acvJ::i:
Creatinine clearance in renal di.seases
Types and causes of acute renal failure
Metabolic and
I'
,
,
Ureter
Fig 6.1
Rltration
Blood Flow
Urine
Fig 6.2
Nephron: A nephron is the basic unit of renal function; there are millions of nephron present
in each kidney. Nephron has three major functions:
Filtration
The filtration occurs at glomerular or bowman capsules.
6-1
PharmacyPrep.Com
Renal System
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Creatinin clearance is the measure of glomerular filtration rate.
Normal creatinin clearance is 80 to 120 mL/min
Reabsorption
Transportation of ions or drugs back into blood from nephron is referred as
reabsorption.
Secretion
Secretion of ions or small molecular drugs into nephron from nephron walls.
Acute Renal Failure
Three types of ARF
Prerenal ARF (occurs due to problems in organs liver, heart and blood circulations)
IntrinsicARF (occurs due to problems in kidney)
Post renal ARF (occurs due to problems in organs after kidney like ureter or bladder)
Prerenal ARF is characterized by inadequate blood circulation (perfusion) to the kidneys,
which leaves them unable to filter the blood properly. Many patients with prerenal ARF are
critically ill and experience shock (very low blood pressure). There is often poor perfusion
within many organs, which may lead to multiple organ failure.
Causes: Some of the most important causes of prerenal ARF are dehydration, heart failure,
sepsis (severe infection), and severe blood loss.
Prerenal ARF is associated with a number of pre-existing medical conditions, such as
atherosclerosis ("hardening" of the arteries with fatty deposits), which reduces blood flow.
Dehydration caused by drastically reduced fluid intake or excessive use of diuretics (water
pills) is a major cause of prerenal ARF. Many people with severe heart conditions are kept
slightly dehydrated by the diuretics they take to prevent fluid build up in their lungs, and they
often have reduced blood flow (under perfusion) to the kidneys.
Risk Factors
Atherosclerosis
Blood loss
Chronic liver disease
Heart disease
Blood sugar
Symptoms of prerenal ARF include the following: Dizziness, Dry mouth, Low blood pressure
(hypotension), Rapid heart rate, Slack skin, Thirst, Weight loss
Urine output is usually low in people with prerenal ARF. The patient also may have
symptoms of heart or liver disease,
6-2
PharmacyPrep.Com
Electrolytes and Disordets
IElectrolytes
I
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Extracellular (interstitial)
Intracellular
Na+, Cl-, Ca
2
+ .
K+, Mg
2
+, Phosphate
n ~ l System
Calcium (Ca
2
+): In normal adults, there are approximately 1,400 g of calcium in the body, of
which 99% in bones. The total of 0.1% calcium is present in blood (plasma). The most common
source of calcium is dairy products.
Calcium Plays an important role in propagation of neuromuscular activity and regulation of
endocrine functions.
Parathyroid hormone (PTH) helps to dissolve calcium ion from bones and moves calcium to
blood, thereby hyper PTH can cause hypercalcemia. Helps in calcium reabsorption in kidney
Calcitonin: is secreted from thyroid gland. It helps in movement of calcium ion from the blood
to bone formation. Thereby hypercalcemia stimulates secretion of calcitonin from thyroid
gland.
Vitamin D: The active form of vitamin 'D is 1, 25-dihydroxy vitamin 0
3
(chole-calciferol) . It
enhances absorption of calcium when calcium is low in the blood. Calcium is primarily
absorbed by carrier-mediated diffusion at small intestine Uijenum, and duodenum).
* Blood coagulation
* Bone and tooth structural integrity
* Normal values: 8.8 to 10.3 mg/dl or 2.20 to 2.56 mmol/l
Hypercalcemia
Causes:
'. Malignancy or metastatic bone disease
Hyperparathyroidism: Excessive parathyroid hormone (PTH) secretion.
Drugs that cause hypercalcemia are: Thiazide diuretics.
Vitamin D intoxication: Cholecalciferol (Calcinol) -7active (due excessive absorption.of Cal
Treatment: Hypercalcemia can be treated with drugs such as: calcitonin, bisphosphonates,
zolindranoic acid, corticosteroids, and prednisone.
6-3
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PhalmacyPrep.Com
Renal System
Regulation of calcium and phosphate metabolism
Phosphorus
Phosphorus is an intracellular ion. Phosphorus is found primarily in bone (85%) and soft
tissues (14%).
DietalY ca, P
fig 6.3
1,2S(OHhD stimulates
absorption. of ca and P
from gut
Ca,P
ActivttY of
paratt-f roids
regulated it level
afserumCa
Parathormone
increases resorption of Ca
and decreases resorption of P
Bone
Caldtonln suppresses
Ca release it suppression
of osteoclast
I
Hypocalcemia
Causes: Due to deficiency of vitamin D.
Hypoparathyroidism (due to decrease in PTH secretion)
Drugs that can cause hypocalcemia are: e.g. corticosteroids: corticosteroids counteract the
effects of Vitamin D and loop diuretics (Loops loose calcium). Excess of phosphate in total
parenteral nutrition (TPN) .
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Hypophosphatemia
Hyperparathyroidism (excessive PTH) causes hypophosphetemia
6-4
PhannacyPrep.Com
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Renal System
Hypophosphatemia (seen mostly in primary hyperparathyroidism and malignancy-
associated hypercalcemia). Exacerbates by increasing renal synthesis of
l,2S-dihydroxycholecalciferol, reducing bone formation and Increasing bone resorption.
Hyperphosphatemia
Occurs due to hypoparathyroidism (low PTH)
Drugs that prevent bone resorption (death) are referred as antiresorptive agents.
Antiresorptive agents are: Bisphosphonates, c1odronate disodium, pamidronate disodium
and zoledronic acid.
Potassium (K+): Potassium distributed primarily in intracellular (98%) and extracellular (2%) in
muscle tissues.
Major cation in intracellular space
Maintenance of proper electrical conduction in cardiac and skeletal muscles (muscle and
nerve excitability)
Plays a role in acid-base equilibrium acidosis
Range of normal value: 3.5 to 5 mEqjL
regulated by:
Kidneys (renal function)
Aldosterone
Arterial pH
Insulin
Ksupplement intake
Sodium delivery to distal tubule
Hyperkalemia
Causes: Renal insufficiency and drugs
Drugs that cause hyperkalemia include: K+ sparing diuretics (Spironolactone, Triamterene,
Amiloride), and ACE inhibitors, and ARBs etc.
Adrenal insufficiency (aldosterone hormones)
During vigorous exercise
Cellular breakdown (tissue damage, hemolysis, burns, infections)
'. Metabolic acidosis, and cardiac arrest.
Hypokalemia
Malaise (feeling NOT well)
Confusion
Dizziness
ECG changes
Muscle weakness
Pain
6-5
PharmacyPrep.Com Renal System
Causes:
Excessive mineral corticoid activity
Vomiting
Diarrhea
Drugs that cause hypokalemia: Diuretic use (Thiazide, loop diuretics, and acetazolamide),
corticosteroids, penicillins (piparicillin, ticaracillin), beta2 agonist, and amphotericin.
Glucosuria
Alkalemia
Administration of insulin and glucose
Chloride (Cn
The most abundant extracellular anion is cr (Na is the most abundant extracellular
cation)
Maintenance of acid base balance relationship between Na, and CJ.
Hyperchloremia (er excess) and hypernatremia ( Na excess in the blood)
Caused by:
Renal insufficiency when chloride intake exceeds excretion
Dehydration
Excessive salt intake
Hypochloremia
Caused by:
Excess loss of GI fluids
Diuretic therapy: Thiazide, and loop diuretics. Hypochloremic alkalosis is caused by:
thiazides.
Fasting
Adrenal insufficiency
Sodium (Nat)
Sodium is the predominant cation of the extra cellular fluid (ECF).
Norma sodium levels (135 to 147 mEq!l or mmol/l).
Sodium is essential in establishing osmotic pressure relation between intracellular and
extra cellular fluid.
Hyponatremia $' "-"4-1 /{'J ..-} h<tY
0
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1
0
Caused by: Cirrhosis, CHF, nephrosis or the administration of osmotic active solutes such
as albumin or mannitol (osmotic diuretic).

Hypernatremia
Caused by:
loss of free water (Hot body fluid)
loss of hypotonic fluid
Excessive Sodium intake
6-6
PharmacyPrep.Com Renal System
Drugs that contain (beta lactam: ticaracillin, antacids such as sodium carbonate)
Acid BaseDisorders
Metabolic acidosis
j Bicarhonates (HCO,') in blood
t CO, in blood
pH of blood is reduced in metabolic acidosis (acidic)
pH of urine is increased (alkaline).
Drugs that cause metabolic acidosis are: AClDazolarnide (carbonic anhydrase inhibitors),
amiloride, triamterene (potassium sparing), and aldosterone antagonist (spiranolactonc) and
overdose of ASA.
Treatment: Sodium bicarbonate (NaHC0
3
)
Metabolic alkalosis
1 Bicarhonatcs (HCO,) in blood
j Co, in blood
Drugs and disease that cause metabolic alkalosis: Thiazide and loop diuretics, hypercalcemia,
High concentration ofalkali administration, and vomiting.
Treatment: Ammonium chloride (NHtCI) or ascorbic acid (vitamin C).
Rcspi ....atory Acidosis
This occurs due inadequate ventilation orco
l
by lungs.
Predisposing factor for respiratory acidosis: astluna, beta-blockers, sleep apnea, eNS
depressants, pulmonary edema or embolism, cardiac arrest.
Respiratory Alkalosis
Due to increase secretion of COl
Not very common
lips
I. Hypokalemia 2. in kidnells 3. Creatinine clearance
4. J"HCOS'tCO
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S. 'tHCO J" CO 6. Azotemia
7. Renal perfusion 8. Ureter
Bladder or prostate
10 Flow rate 11 pH 12 Tonicity
13 Metabolism 14 Hllpocalcemia IS Hypercalcemia
Excessive blood urea nitrogen in blood ( ) It;...

The most common cause of pre-renal acute renal failure is due to (
What happens in metabolic acidosis? ( ) I (:;,7,.
What happens in metabolic alkalosis? ( ) Co 2-
Intrinsic acute renal failure occurs in? ( ) 1<\, . -JY
Post renal failure can occur in? ( ) I I
Factors that affect reabsorpt;on( I e,IP.cL fsb"'/
Glomerularfiltration (GFR) measures... ( ) e.te-J-,'N....... cofe.<.ut..q, .-ftHv '7-
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Reabsorption of H
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Pre-renal ARF is due to (
Chronic renal disease may cause... ( ) o-iJ..a-d
Adrenal gland cancer (pheochromacytoma) may cause... { ) wvJ.I-
DuetodeficiencyofVitD( ) c.c.
Stimulates secretion of calcitonin from thyroid gland ( ) h,jftA.-{
albumneurea is __> ( ) , "1
Albumneurea is indicator of --> { l
The most common extra cellular cation i5--> ( ) Nc,,-'
The most common extra cellular anion is--> ( ) Ceo.
What happens in metabolic acidosis? ( ) j, H-(0.J i CO?",
What happens in metabolic alkalosis? ( t J. (.oL..-
Write the examples of drugs that cause metabolic acidosis? ( ) Itf<...- I f<. ..spc.A.!::J
Write the examples of drugs that cause metabolic alkalosis? ( ) -, 4-. dJ I.o..t.
Normal serum potassium levels ( .2" - -IS:. 0 h
If it is defect in renal filtration, CrCI ( )
Normal erCi is I ) SO - 120 w-I / "" ,
In renal disease CrCI is ( ) <::... S- 0 l>"'t"") ( Jh"'J t'..... d/t....
) ?-"1 (UA-'vt- aOH
Potassium sparing diuretics gives -7 ( ) I rtJ.}...... '..
Pyuria and dysuria is symptoms of (
lactic acidosis is SE of -7 ( )
Select True or False statements
Summary of electrolytes action in kidney {True! False}
Early proximal convoluted tubule =Reabsorbs Na+, cr, Ca
2
+(True/ False}
Early distal convoluted tubule = Reabsorbs Na', cr, Ca
2
+(True/ False}
Thin descending loop of Henle =Reabsorbs H20 (True/ False)
Thick ascending loop of Henle = Reabsorbs: Na, K', cr, Mg
2
+, Ca
2
' {True}
Collecting tubule: Reabsorbs Nat in exchange of K' or H+ (regulated by aldosterone).
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www.phannacyprep.com Liver function and Pathophysiology
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Liver Functions and Chronic
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Liver Diseases
Questions Alerts!
Causes of chronic liver diseases like ascitis
Hepatitis A, B, Cinfections causes of infections
Hepatitis A and Bvaccines and treatment
Mechanism drugs induced hepatotoxicity like acetaminophen
LIVER FUNCTIONS
Detoxification
Blood
glucose
regulation
Bile
drainage
SYnthesis
and storage of
amino adds, proteins,
vitamins and fats
Blood \\
drculatlon
and filtration fig 7.1
Definitions
Necrosis cellular breakdown example: Acetaminophen
Steatosis: Hepatocytes filled with small droplet of lipid: Example: Tetracycline's
Drugs transportation into the bile from the liver
There ~ transporters fqr anions, bile salts, cations, and neutral organic
compounds.
Release small intestine.
7-1
www.phimnacyprep.com Liver function and Pathophysiology
Oral drugs passage to liver: mesenteric veins -7 portal veins -7 liver -7 hepatic vein
-7 systemic circulation
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Enterohepatic re circulation
This term refers to drugs emptied via bile into the small intestine and then
reabsorbed from the intestinal lumen into the systemic circulation.
It can allow the body to conserve endogenous substances such as bile acids, vitamins
o and B12, estrogen etc. It may be responsible for some of the long half-lives of
drugs.
Antibiotic therapy interferes with the process of enterohepatic recirculation by
drugs, which have been conjugated can be hydrolyzed by gut enzymes such as
glucuronidase and then reabsorbed as the active drug or as a metabolite. A decrease
in bacterial flqra as a consequence of antibiotic therapy can decrease the amount of
sulfatase and glucuronidase-containing bacteria. This could then lead to an
increased rate of elimination of the drug.
f
.
Chronic liver disease: Ascites, hepatic encephalopathy, cholestatic
disease, Wilson's disease, alcoholic liver disease and viral hepatitis.
I Chronic Liver Disease
Ascites Or Hydroperitoneum
The accumulation offluid in peritoneal cavity is referred to as ascites. Symptoms
include abdominal distention. Ascites is caused due to infections such as
tuberculosis, heart failure, cirrhosis, and portal hypertension, and various cancers.
Drug of choice is spiranolactone is inhibitor of aldosterone, because aldosterone
hormone increases Na!H20 retention. Alternate furosemide can be added to
enhance diuresis.
Chronic Cholestasis
Cholestasis is a condition in which obstruction of bile from liver to intestine, it is also
referred to as obstructive jaundice. Symptoms are pruritus (itching) and is due to
hyperbilirubinemia associated with liver diseases. Cholestyramine removes excess of
,/ bilirubin from the body. Antihistamines can be used for non-specific pruritus.
I
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Spontaneous
Ascites Hepatic
Bacterial Chronic cho1estasis
Peritonitis (SSP) Treatment
encephalopathy
Treatment: Antihistamine or
Treatment: Treatment:
Antibiotics cholestyrmine
Diuretics Lactulose
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Hepatic Encephalopath'y:' (Porto Systemic Encephalopathy)
Condition in which brain function is impaired by
presence of toxic substances, absorbed
from colon, wliich is no'rmally -detoxify and
removed by liver. This condition occurs in
severe liver damage such as liver
cirrhosis.
Symptoms.include: Drowsiness,
confusion, difficulty in performing task
(e.g writing) and coma.
Drug of choice is lactulose to achieve 2 to
3 bowel movement a day. If no
improvement in 1 to 2 days add
metronidazole.
Wilsons Disease
Excessive copper can cause Wilsons disease. Drug of is the penicillamine and
treatment is lifelong. Pyridoxine (vitamin B
6
) 25mg daily should be given with
penicillamine to counteract its antipyridoxine effect.
Avoid food that has high copper content: Peanuts, chocolate, Shellfish, Mushrooms,
and liver.
Viral Hepatitis: There are 5 types of hepatitis viral infection, hepatitis A, B,C,D,
and E. However the common infections are hepatitis A, Band C.
Hepatitis A
Hepatitis A is acute infection
Transmits through fQQd..contaminations such as or orofecal
Vaccine available
Hepatitis A vaccine is recommended to travelers.
Hepatitis Band C
Hepatitis Band Care chronic
The most common hepatitis B
Hep-B is DNA type of virus, where as other hepatitis are RNA type.
Transmission through body fluids, such as blood transfusion, sexual contact and
drug abuse and spa.
Hepatitis Bis 90% in ch"ndren and 5% in adults.
Hepatitis Cis often chronic in adults (acute hepatitis C, is 80% becomes chronic
likely within first year of infection).
Hepatitis Chas va,ccine.
Hepatitis Bvaccine also protects hepatitis 0 infections.
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Interferon alfa (IFN alfa) is the r ~ g of choice to treat acute viral hepatitis and
chronic hepatitis
Causes of ascietes include ~ infections, TB, cancer, GJ surgeries, chronic liver
disease
lactulose is used in what type of chronic liver disorder ~ hepatic encephalopathy
(decrease NH3)
What type of hepatitis is chronic -7 Band C
What is treatment of hepatitis -7 interferon's
Hepatitis A transmits by ~ water and orofecal
Hepatitis Band Ctransmits by -7 sexual contact
Ascitis is caused by -7 infections, cancer, GI ulcer, TB
If takes Hep Bvaccine, this also protects -7 HepD
Drugs that can cause hepatotoxicity include:
Acetaminophen (> 4g daily)
Tetracycline (>2g daily)
Methotrexate (>25mgJwk)
Vitamin A (chronic use over 40,000 U daily)
Salicylates (chronic use >2g daily)
Iron (single dose >lg)
Cyclophosphamide
6-Mercaptopurines
Cholestatitis
Retention of bile acids because of the obstruction of bile ducts.
Example: Penicillins (isoxazole type)
Cholestatitis can lead to hyperbilirubinemia
Example: Rifampin
Bacterial peritonitis: Chronic liver disease, history of fever, abdominal pain.
/ TIpS
l. Penicillamine 2. Ascites 3. Wilsons disease
4. Cholestatitis 5. hepatic 6. Hepatitis B
enceohalopathy
7. Hepatitis C 8. Infections
Tuberculosis
10 cancer 11 GI sUrlzeries 12 Chronic liver disease
13 Se){ual contact 14 water 15 Orofe<:aJ
16 Interferon alfa 17 Portal hypertension 18 Spironolactone
7-4
www.phannac.Yprep.com Liver function and Pathophysiology
, .
What type of hepatitis is chronic? ( ),I 7
What is the treatment of hepatitis? ( ) / ("
Hepatitis A transmits by? ( ) IS_ .
Hepatitis Band Ctransmits by? ( +- f>/l;(J I b
Ascites is caused by? ( I ea. 4-
What is a DNA type of virus ( 6)
Accumulation of fluid in peritoneal cavity ( 2.)
It is caused by excessive copper ( 3 )
Drug of choice to treat Wilsons disease ( ,)
Retention of bile acids because of obstruction of bile ducts (
A type of hepatitis that has no vaccine (7)
The drug of choice to treat ascites ( ) -I
Lactulose is used in what type of chronic liver disorder? (
What type of hepatitis is chronic ( ) f3 +C-
What is treatment of hepatitis ( ) IJv.-/JeJ-6",-,J
Hepatitis A transmits by -7 ( ) 10 J@'1/ 0
. Hepatitis.B and Ctransmits by -7 ( ) G t...+
Ascitis is caused by ( )
Iftakes Hep Bvaccine, this also protects ) J Crl J Ue-fat J "C.fl
Select True or False statements:
Cholestatitis: Retention of bile acids because of the obstruction of bile ducts.
Example: Penicillins (isoxazole type) (True/False)
Cholestatitis can lead to hyperbilirubinemia example: Rifampin (True/False)
Bacterial peritonitis: Chronic liver disease, history of fever, abdominal pain.
(True/False)
Causes of ascites include -7 infections, TB, cancer, GI surgeries, chronic liver disease
(True/False)
Lactulose is used.in what type of chronic liver disorder -7 hepatic encephalopathy
(decrease NH
3
) (True/False)
7-5
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.2'ie.c.1l0 C1
Respiratory System
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Respiratory System
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Questions Alerts!
Asthma triggers
Definition of emphysema ;-
Differences between COPO (terminal bronchioles) and Asthma (bronchus)
(
Copyright 02000-2012 TIPS Inc. Unauthorized reproduction or this manual is strictly prohibited and 8-1
conducted by PharmacyPrep.
Definitions:
Sialorrhea: drooling (excessive saliva).
Rhinorrhea: Runny nose
Hypoxia!Hyperapnea, and acidosis.
Dyspnea: difficulty in breathing
Emphysema: Permanent enlargement of alveoli
COPD: Emphysema or chronic bronchitis
Emphysema isCOPD
cough is symptoms Asthma
Allergens that triggers asthma smoke, dust, aoimal dander, viruses, mold, cold air, (warm
air is NOT a trigger), humidity (recommended <50%), emotional stress, and exercise.
Smoking is risk factor for..;) COPD, CVD, Cancer, Ulcer and stroke
Fig8,1
Esophagus

laO' ngeal philO' nx
,__ Sphenoidal sinus
Trachea --=7"0::::._-
Frontal sinus ----+-8
EpiglottiS --!,!!--...
Nassal cavitY -----I
larYm: and vocal cords _--1''\
Right rung

Right bronchus
Horizontal
MediaSlinum cross-section
......... __ of lungs
\ Diaphragm
Tenninal bronchiole
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Re<piralory
Physiology Ventilation
Respiration
Ventilation
.
Air moves from URT-)lRT-)aJveoJi
Respiration
Gaseous exchange occurs at alveoli capillary membrane.
Factors that

Increased in resistance to air flow
decrease the

Decrease ventilation
respiration
Decrease diffusion
Mucosal edema
Increased branchial secretion
Bronchospasm
Arrangement of

Tracheobronchial tubes have smooth muscle fibers arranged on
Bronchiole a spiral around the tube.
smooth muscles
Disease Asthma
COPD
Emphysema
Bronchitis
iii
'{ r!f y' lower Respiratory Tract
Upper respiratory tract

Tips
Anatomy Nasal cavity
Pharynx
Larynx
Trachea
Disorders Acute rhinitis
Acute pharyngitis
Acute tonsillitis
Acute laryngitis
Common cold
Treatment Antihistamine-7 Runny nose
Decongestants (Sympathomimetics)-7nasal congestion
Antitussive-7 Cough
Antibiotics-7 Infections
Expectorants-7Bring up mucus
.
1 asthma 2 emphysema 3 dyspnea
4 COPD 5 rhinorrhea 6 sialorrhea
Difficulty In breathing
Copyright 0 2000-2012 TIPS Jne. Unauthorized reproduction of this manual is strictly prohibited and 8-2
conducted by PharmacyPrcp.
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Urinilry System
9
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Questions Alerts!
.. Urinary tract infection symptoms
.. Benign prostatic hyperplasia symptoms
.. Types of urinary incontinence
Urinary System
The urinary system includes two kidneys, two ureters, the bladder, two sphincter muscles, and
the urethra. Urinalysis is a test that studies the content of urine for abnormal substances such
as protein or signs of infection. Urodynamic tests evaluate the storage of urine in the bladder
and the flow of urine from the bladder through the urethra.
U
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Copyright 0 2000-2012 TIPS Inc. Unauthoriled reproduction of this manual is strictly prohibited and it is illegal
to reproduce without permission. This manual is being used during review sessions conducted by Pharmacy-
Prep.
9-1
www.pharmacyprep.com Urinary System
Benign prostatic hyperplasia (BPH) is a condition in men that affects the prostate gland, which
is part of the male reproductive system. The prostate is located at the bottom of the bladder
and surrounds the urethra. BPH is an enlargement of the prostate gland that can interfere with
urinary ~ u n t o n in older men. It causes blockage by squeezing the urethra, which can make it
difficult to urinate. Men with BPH frequently have other bladder symptoms including an in-
crease in frequency of bladder emptying both during the day and at night. Most men over age
60 have some BPH, but not all have problems with blockage. There are many different treat-
ment options for BPH.
Symptoms: urine obstructions symptoms include: frequent urine, drop by drop, incomplete
voiding; nocturea and also include irritation symptoms. NOT a symptom; jet urination
Painful bladder syndrome/Interstitial cystitis (PBS/IC) is a chronic bladder disorder also known
as frequency-urgency-dysuria syndrome. In this disorder, the bladder wall can become inflamed
and irritated. The inflammation can lead to scarring and stiffening of the bladder, decreased
bladder capacity, pinpoint bleeding, and, in rare cases, ulcers in the bladder lining. The cause of
IC is unknown at this time.
Kidney stones is the term commonly used to refer to stones, or calculi, in the urinary system.
Stones form in the kidneys and may be found anywhere in the urinary system. They vary in size.
Some stones cause great pain while others cause very little. The aim of treatment is to remove
the stones, prevent infection, and prevent recurrence. Both nonsurgical and surgical treatments
are used. Kidney stones affect men more often than women.
Prostatitis is inflammation of the prostate gland that results in urinary frequency and urgency,
burning or painful urination, a condition called dysuria, and pain in the lower back and genital
area, among other symptoms. In some cases, prostatitis is caused by bacterial infection and can
be treated with antibiotics. But the more common forms of prostatitis are not associated with
any known infecting organism. Antibiotics are often ineffective in treating the nonbacterial
forms of prostatitis.
r
. Proteinuria is the presence of abnormal amounts of protein in the urine. Healthy kidneys take
wastes out ofthe blood but leave in protein. Protein in the urine does not cause a problem by
itself. But it may be a sign that your kidneys are not working properly.
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9-2
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www.pharmacvprep.com . Urinary System
Urinary retention, or bladder-emptying problems, is a common problem with many possible causes.
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Urinary incontinence, loss of bladder control, is the involuntary passage of urine. There are
many causes and types of incontinence, and many treatment options. Treatments range from
simple exercises to surgery. Women are affected by urinary incontinence more often than men.
Avoid use of diuretics. To treat incontinence, anticholinergic drugs like oxybutinin is the drug of
choice.
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Urinary incontinence symptoms -7 "1 0 () v\. f,.,la d &.vI.- /JA.
Drugs that are used for treatment of urinary incontinence-7 (J'f. j '/'"II.,

Drugs that are avoided in patient with urinary incontinence -)
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EnureSIs (bed wetting) drug of chOice -7 A\D1+ lie....! 6rrv<-'J' .... -' :lc
Benign prostatic hyperplasia (BPHj is -7 orr- h: "
Benign prostatic hyperplasia symptoms are __ > d!fit.J}.QG , (tf... "'-t:JJ, ,LiA. q
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Saw palmetto is used for --> EPH
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9-3
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~ E;yc o n ~ [or
Questions .Alerts!
The Eye and Ear
Photoreceptors rods and cones
Sensitivity to day light and colors
Cornea is upper layer of eye is rate determine step in ophthalmic drops
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Dental anatomy and physiology
102
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to r e p r o u ~ without permission. This manual is being used during review sessions conducted by Pharmacy-
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These rods are responsible for night vision, our most sensitive motion detection, and our
peripheral vision.
The rods are more numerous, some 120 million, and are more sensitive than the cones.
However, they are not sensitive to color.
The 6 to 7 million cones provide the eye's color sensitivity and they are much more concen-
trated in the central yellow spot known as the macula.
Where does image forms in eye -7 retina
Ophthalmic drug rate limiting step ~ cornea
There are 20 primary teeth and 28-32 permanent teeth. The last 4 is being wisdom teeth.
In adult, there are 16 teeth in maxilla and 16 in the jaw.
Wisdom teeth mayor may not grow in.
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Incisors 8, canine 4, premolar 8, molar8 ,wisdom(third molar)4 =32.
Baby teeth start to grow during intrauterine first trimester (8 weeks).
Teeth are made of enamel, dentin, and cement.
Dentin composes most of the root.
Crown is covered by the enamel.
The root embedded inside the maxilla and jaw bones has a bulb canal.
The Eye and Ear
-
Terminology
Cornea: In the front of the eyeball is a transparent opening known as the cornea.
Pupil: After light passes through the cornea, a portion of it passes through an opening
known as the pupil
Iris: pupil opening can be adjusted by the dilation of the iris
Ciliary muscles: The lens is attached to the ciliary muscles
Retina: The inner surface of the eye is known as the retina
Macula: Small central area of retina
Optic nerve: The network of nerve cells is bundled together to form the optic nerve on the
very back of the eyeball.
Optic disk :The nerve cells is bundled at very back of eyeball, is also known as blind spot.
Myopia: If the incoming light from a far away object focuses before it gets to the bad: of the
eye, that eye's refractive error is called "myopia" (nearsightedness).
Hyperopia: If incoming light from something far away has not focused by the time it reaches
the back of the eye, that eye's refractive error is "hyperopia" (farsightedness)".
The retina contains two types of photoreceptors, rods and cones.
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The bulb canal,conta!ns b!ood supply and nerve terminals.

The root teeth may be single in number or multiple.
Gingival or gums consist of mucosal tissue lies over the alveolar bone.
Oral hygiene is practice of keepi"ng mouth and teeth clean, to prevent bad breath, and den-
tal problems.
Plaque is yellow-sticky films-that form on the teeth and gums.
Bacteria in plaque release acid that harm the enamel.
Brushing and flossing daily the teeth will prevent tartar forming.
Fluorides are a primary protector against dental cavities.
Fluorides make teeth surface more resistant to acids.
Drinking water contains enough fluorides.
Sugar free gum increases salivation and help to clean teeth surface.
Good food items for teeth; green tea, milk and yogurt, cheese, apples, onion.
Smoking and chewing tobacco causes multiple dental diseases.
Bulimia nervosa and repeated vomiting causes significant damage to enamel.
Bad dental hygiene show direct link to systemic diseases;
I-Cardiovascular disease.
2- Bacterial pneumonia.
3- Low birth weight.
4- Complication of diabetes.
5- Osteoporosis.
Tips
Blind spot is
Age related macular degeneration cause due to-7
Glaucoma occurs due to -7
Drugs that are used to treat glaucoma are -7
,
Select True/False Statements
The retina contains two types of rods and cones. (True/False)
10-3
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to rep"roduce without permission."This manual is being used" during review sessions cOhducted by Pharmacy-
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The Eye and Ear
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These rods are responsible ~ o r nignfvision; our most sensitive rJ.10tion detection, and our periph.eraJ
vision. (True/False)
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The rods are more numerous, some 120 million, and are more sensitive that) the c o n ~ However,
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they are NOT sensitive to color. (True/False)
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the central yellow spot known as the macula. (True/False)
Cones are sensitive to color vision(True/False)
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10-4
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Blood a
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Questions Alerts!
Blood cells platelets, red blood cells, and white blood ceils
Hemostasis
Morphological changes of anemia
Iron deficient microcytic anemia
Megaloblastic anemia
Elemental iron supplements (ferrous fumerate > dried ferrous sulfate> ferrous
sulfate> ferrus gluconate)
Iron supplement drug interactions: thyroid hormone, tetracycline and quinolones,
colestyramine
This chapter reviews blood cells and functions. Types of anemia and their morphological changes.
Terminology
Agranulocytosis: Decrease in number of granulated white blood cells such as neutrophils, basophils, and
eosinophils.
Neutropenia: Decrease in neutrophils
Neutrophilia: Increase in neutrophils
Esinophilia: Increase in esinophils
Thrombocytopenia: reduced.platelets to less than 150 x 10
9
/L
Function of blood include transportation of gases, nutrients, hormones, metabolic wastes
regulates body temperature, pH, electrolyte balance, fluid volume protects: prevents
blood loss (clotting), and prevents infection (WBC and antibodies).
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Blood and Anemia
fi 11 1
Multlpotent stemcells
From Stem Cell to Blood Cell
ED'throblasr
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Edthrodtes
(red blood cells)
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Blood
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55% Fluid r 45% Cells
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Water containing salts Erythrocytes 5-6 mil/mL (44%)
Proteins Leukocytes + Platelets = (1%)
Antibodies
Hormones
Electrolytes
Fats and lipids
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Sugar (carbohydrates)
Erythrocytes II Leukocytes I I Platelets I
Mineral
Vitamins
Megaca(foblasts
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Blood constitute 55% fluid and 45% cells.
Blood and Anomin
1. Blood proteins:
Blood Proteins; (albumin, .glycoprotein, and fibrinogen)
From the liver blood carries:
Albumin: This is the most common blood proteins (55%) in blood. Which is carrier of,
buffer, osmotic pressure, transport lipids, fatty acids and acidic drugs.
Globulins: carry ions, hormones, steroids and bind base drugs
Fibrinogen changes to fibrin, helps in blood clotting
2. Electrolytes
Electrolytes present in blood = (Na", K", ca
2
", Mg
2
', cr and C0
3
)
Extracellular = Na', cr and Ca
2
"
The most common extra cellular cation is Sodium (Na)
The most common extra cellular anion is Chloride (Cl)
Intracellular = K', Mg
2
", and phosphate
Antibodies (Immunoglobulin) =IgG, IgM, IgE, IgA, and IgD
Erythrocytes (Red blood cells)
RBC is composed of: Globin (protein), iron (metal), phospholipid (lipids), potassium
phosphate (salt), hemoglobin (contain porphyrin ring system) bind loosely to oxygen
and carbon dioxide. In the overdose of carbon monoxide, the hemoglobin binds with
carbon monoxide.
RBC synthesis: Pre-erythrocyte is the first step in the synthesis of RBe series.
The normal value of the RBC in adult men would be 4.7 million.
Erythrocytes are originated in the following sequence of celis: Hemocytoblast-7
Megaloblast-7 Erythroblast (Normoblast) --> Reticulocytes-7 Erythrocytes
Erythropoietin, a glycoprotein, is a key hormone for the production of RBC. In the
absence of erythropoietin, hypoxia is unable to stimulate the production of Rae. The
kidney is a principal organ for the synthesis of erythropoietin; therefore, kidney
failure would result in severe anemia. Il"i.-/tIi '<.AdJ (l.cI Hio
RBC destruction: Life span of RBC is 120 days (4 months). CHhA1C-::l .g(] r<::t- "/.
RBCs are destroyed in the spleen (spleen also referred to as grave yard of RBe)
Hemoglobin (Hgb): Blood protein-containing iron metal, carries oxygen in blood.
Hemoglobin content 14.5 gm/lOOml: Carries oxygen in blood. Hemoglobin consists of
porphyrin ring. Oxygen binds with porphyrin ring. Porphyrin ring present in
haemoglobin is tetramer.
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Hemoglobin Myoglobin Cytochrome oxidase
Transport oxygen in blood Transport oxygen in tissue Catalyzes phase I metabolism
Porphyrin tetramer Porphyrin monomer Porphyrin
Has affinity and binds with Has affinity and binds with Has affinity and binds with O
2
,
O
2
, CO, CO
2
and (N. Oz, CO, CO
2
and eN co, CO
2
and eN.
Ferrous ion (Fe
2
+) Ferrous ion (FeJ:f) Ferrous ion {FeJ:+j
Myoglobin: protein present in tissues which is essential for oxygen transport in
tissues. Carries oxygen in tissue. The porphyrin ring present in myoglobin is monomer.
Methemoglobin: Nitrite ions react with hemoglobin and produce methemoglobin,
which has a low affinity for oxygen and a high affinity for cyanide ions. This forms
iron eN complex it is referred as cyanomethemoglobin
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Platelets (Thrombocytes): Platelets are referred to as thrombocytes. Platelets help in the
process of blood clotting. Platelets lack nudei and platelets are produced in bone marrow.
Platelet life span: 7 to 10 days, range in blood: 150,000 to 300,000 mm
3
.
Deficiency of platelets is referred as thrombocytopenia.
leukocytes (WBC)
leukocytes: Produced in bone marrow like RBC's
About 30% are lymphocytes and about 60% are neutrophils and 8% are monocytes
Normal range of WBC's (white count) in blood is 4000 to 1l000/mm
3
(4000 to 11000 I
cmm)
leukocyte's consist of clearly defined nuclei
Neutrophils: About 60% of white blood cells are neutrophils.
Monocytes: About 8% of white blood cells are monocytes
B lymphocytes and T lymphocytes are primary cell of specific immune response.
Neutrophils: Responsible for immune defence phagocytosis
Basophils: Responsible for inflammatory response
Eosinophils: 'Defence against parasites" ','J
Monocytes: Immune defence (precursor of tissue macrophage) ~ i eaters
a-lymphocytes: Antibody production (precursor of plasma cells)
T-Iymphocytes: Cellular immune response.
/ Granulocytes: the blood cells that contain granules, example: neutrophils, basophils,
esinophils, and mast cells.

Granulocytes are: Neutrophils, eosinophils, and basophils, cells that stain
Neutrophils gives -7 stain with acidic or basic dyes
Eosinophils gives? stain with acidic dye
Basophils gives -7 stain with basic dye
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illegal to reprOduce without pcnnission. This manual is being used during review sessions conducted by
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f..

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Agranulocytes
. Cells that do not stain are agranulocytes
There are 2 types
Lymphocytes
Monocytes
Bluuu (1I1U Allcmla
Agglutinogens in human' RBCs are known as: The Rh factor blood with this factor is
described as Rh without this factor is described as Rh (-)
negative. In Rh-negative mother, Rh-positive antigens may transfer from Rh-positive fetuses
to the mother via placenta. This may lead to production of Rh-positive antibodies in the
mother's blood. These same antibodies may transfer back from the mother's blood into fetus
via the placenta, and produce antigen-antibody reactions. This leads to lysis of red blood cells
in the fetus, and miscarriage. gram prevents the formation of anti-Rh antibodies in a
mother who bears Rh positive fetus.
Blood Groups
Blood groups: surface of RBC's have antigen
A RBC has A antigen, plasma has Bantibodies
B: has Bantigen, A antibodies
AB: has A and Bantigens, no antibodies
0: (universal donor) has no antigens, has antibodies against A and B, transfusion reaction
can lead to kidney failure.
Rh (rhesus monkey) + have antigens, lacks antigens, antibodies only form after exposure.
Rh- women who have + babies get a Rhogam shot.
DONOR
0 A B lAB
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Qualities of Blood
Temperature: 38C (lOO.4F); warfarin (anticoagulant) added in blood storage
Viscosity: 5xH20-sticky, cohesive, resistant to flow. pH: 7.35 - 7.45
volume: 4-6 litres (7% body weight in kg) (2.2 Ib/kg) ,
Transport O
2
and C02 2% of cells in whole blood males: 40-54 (androgens stimulate
production) females: 37-47 (estrogens inhibit production).
Hemoglobin (Hb): binds transports O
2
and CO
2
(280 million/RBC) Hemoglobin - Fe+
2
males: 14-18 g/100ml; females: 12-16 g/dl, fetal hemoglobin has a higher affinity for
O
2
.
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Blood and Anemia
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Anemia
Anemia has categorized based on morphological changes of Rae.
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Mean cell volume (MCV): The MCV detects changes in cell size. Decrease in {.J,l MCV
indicates a microcytic cell anemia, which is due to iron deficiency. Increase in (1') MCV
indicates: macrocytic anemia (megaloblastic anemia), which is due to deficiency of vitamin
B
12
and folic acid.
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Mean Cell Hemoglobin Concentration (MCHC): Weight of hemoglobin in average red cell.
VAncrease in (4tl MCHC -7 Microcytic anemia ~
DaGreasQ iR ('l UCHC ~ Megelel3lastic aAef:Ri:a ) 2. ct,..
Mean Corpuscular Hemoglobin (MCH) = Average weight of hemoglobin in red cells
( l.
Serum ferritin: Iron stores are measured by serum ferritin
Anemia is characterized as deficiency of red blood cells and this can occurs in three forms:
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Anemia
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Microcytic Macrocytic Normocytic
(Hypochromic) (Megaloblastic) (Normochromic)
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Microcytic (hypochromic) anaemia: Symptoms: Fatigue or dyspnea on exertion may occur
during pregnancy and in infants. Mainly occurs due to iron deficiency. This is could be due to:
Low mean cell volume (MCV)
Impaired heme (protein) synthesis
Deficiency of serum iron
; Increased total iron binding capacity.
Decreased serum ferritin
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Iron storage is measured by serum ferritin C-rk .Co L-L 11w k.. ~ )..() (.A..-
Folate storage is measured by red cell folate rather than serum folate
Response to oral and parenteral iron occurs at the same rate in normal circumstances.
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Blood and
Good reticulocyte response indicates active red cell production
Enteric-coated and time-released iron preparation is intended to reduce s/e but may be
ineffective because of failure to release iron in the gastric environment.
Iron supplements:
The most common side effect of iron supplement is constipation.
Take with food to decrease GI side effects. However absorption is better on empty
stomach.
Separate antacids from iron supplement, because antacids decrease absorption of iron.
Antidote for iron overdose is: Deferoxamine.
Megaloblastic Anemia (Macrocytic anemia): Due to deficiency of vitamin B
12
a.':ld folic acid
Mean cell volume (MeV) is increased.
Deficiency of vitamin 8
12
or folate due to decreased of DNA synthesis. Megaloblastic
anemia (large abnormal form or precursors to RBC). Impaired DNA synthesis usually due
to folate or vitamin B
12
deficiency.
B12 deficiency only:
Pernicious anemia is a type of autoimmune disorder. This occurs due to deficiency of
intrinsic factor. The intrinsic factor helps in absorption of vitamin B
12
in stomach.
Treatment: Parenteral vitamin B
1
2 supplement. Oral vitamin B
12
supplements are NOT
effective in pernicious anemia due to deficiency of intrinsic factor. .i:;z)
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Folate Deficiency: oLt' .' c::i.Lb1 efk. y,
Most often occu,rs in chronic alcoholics, pre nancy and drug induced folic acid deficiency
by drugs such as phenytoin, sulfonamides, methotrexate, dapsone, and oral - ("
contraceptives. d.
Intestinal malabsorption caused by Giardia lamblia infection. V,." !l,Z
Folic acid supplements: CL.c. L kat, wf?ri
In pregnancy prophylaxis folic acids 1 mg supplements should begin 1 month before ; fel f..l#tI
conception. a
Folic acid suppleme'nts in pregnancy reduce the risk of neuro tu.bule defect (NTD) .
, Major causes of megaloblastic anemia include folate/vitamin B
12
deficiency this is due to,
chemotherapy and alCoholism and seniors.
Drugs that cause megaloblastic anemia: Acyclovir, alcohol, antiepileptics (carbamazepine,
valproic acid), methotrexate (dose dependent), nitrofurantoin, oral contraceptives,
proguanil, sulfasalazine, trimethoprim (usually due to worsening of pre existing folate ..
deficiency).
11-7
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Blood and Anemia
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Normocytic (Normochromic):
In normocytic anemia MCV is normal.
Due to acute hemorrhagic or RBe hemolysis due to immune or non-immune mediated.
Examples of normocytic anemia include: Sickle cell anemia, and thalassemia
Hemolytic anemia
Sickle cell anemia disease is an inherited disorder caused by a defect in the gene for
hemoglobin. Sickle cell anemia and thalassemia are hemolytic anemias associated with
abnormal hemoglobins. Due to poor solubility of such abnormal hemoglobins in a reduced
state, semicrystalline bodies are formed inside of RBe. These crystalline bodies are pointed
and elongated inside of the cell, and rupture the red blood cells.
Glucose-6-phosphate dehydrogenase (G6PD) anemia:The enzyme G6PD
necessary to maintain the reduce glutathione level (GSHj in red blood cells. This enzyme is
necessary to prevent the hemolysis. The deficiency of this enzyme may cause severe
hemolytic anemia in patients with the use of certain oxidant drugs such as primaquine,
sulfonamide, nitrofuran, nalidixic acid, probenecid, chloroquine, and dimercaprol. Glutathione
is an antioxidant, which prevents the oxidation of hemoglobin to methemoglobin.
The Coombs test
The coombs test is used to distinguish immune mechanism or glucose 6-phospho
dehydrogenase (G6PD) deficiency anemia. In autoimmune hemolytic anemia, coombs test
is positive.
Example of drugs that cause false positive coombs test: penicillins, cephalosporins and
methyldopa.
Aplastic anemia (Total or partial destruction of the bone marrow); Reduced red blood cell and
white blood and plate.lets (thrombocytopenia) counts is decreased. Aplastic anemia is due
to inadequate production or release of myeloid stem cells.
Drugs that cause cell aplasia: Azathioprine, phenytoin, isoniazid, penicillamine,
Chlorpropamide, chloramphenicol, erythropoietin, cephalosporins, penicillins, tetracyclines,
insulin, Methotrexate, isoniazid, quinidine, quinine, rifampicin, sulphonylureas, methyldopa,
mefenamic acid, drugs with oxidant effect on cell membrane (particularly in G6PD deficiency)
Agranulocytosis
Agranulocytosis is profound reduction of agranulocytes such as lymphocytes and monocytes
than normal.
Recovery usually 2 to 3 weeks after the drug is withdrawn. Repeat exposure to causative drug
is not recommended due to sensitization.
11-8
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:Rlood Anem;!l
Drugs that can cause agranulocytosis: Antibiotics (p'enicillins, cephalosporins, cotrimoxazole,
chloramphenicol, sulphonamides), antidepressants (imipramine, domipramine, desipramine,
mianserin), antiepileptics (carbamazepine, phenytoin), anti-inflammatory (gold, penicillamine,
lefunomide, sulfasalazine, NSAIDs), Antipsychotics (chlorpromazine, thioridazine, c1ozapine),
antithyroid (carbimazole, propylthiouracil), captopril, and ticlopidine.
Thrombocytopenia (reduced platelets to less than 150 x 10
9
/L). May as easy bleeding,
bruising or purpura. Prolong bleeding time but INR remains normal. Usually occurs 7-10days
after drug administered.
Tips
l. Vit C& E 2. Anemia associated chronic renal 3. Parietal cells in
. .
disease stomach
4. Vit B12 5. Intrinsic factor 6. Skin cell cancer
7. Neurotubule defect 8. thrombocytopenia 9. pernicious anemia
10 megaloblastic anemia 11. iron 12 proximal convoluted
tubule (PCT)
13 Methotrexate 14 Sulfa drugs 15 OCP
16 Phenytoin 17 Ferrous gluconate 18 Breathlessness
when lying down
19 Microcytic anemia 20 Sickle cell anemia 21 Folic acid
22 Empty stomach 23 constipation 24 ferrous gluconate
25 diarrhea 26 melena 27 vomiting
28 bronze disease, excessive 29 Deferoxamine 30 Penicillins
absorption and storage of
iron
31 Primaquin 32 Use straw

Anemia due to deficiency of iron ( 11' v'-V L1T "-
Vitamin supplements recommended in elderly ( ) V,+4..-- 1312-
Intrinsic factors secreted from.. ( cdJ..J
Deficiency of intrinsic factors cause.. ( ) . a
Megaloblastic anemia is due to ( ) d..LIJ' cJ 'lr V,,J- (j ,2, +- L a
Oprelvekin (interleukin 11) is approved for ( ) 'I--
Epoietin alpha are used to ( .) fUlL I 14.., -f-I..e,uJ.fJ WIf(D
Deficiency of folic acid supplements in pregnancy can cause ( )
What is the meaning of melanoma? ( ) U Ht1?l- ;f
that gives folic acid deficiency ( ) )
Vitamin that decrease oxidative degradation ( ) <\111- L e- <r-
Anemia in pregnancy is due to ( ) 'J tyr6.e. #
- - I 11-9
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Blood and Anemia
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The most abundant metal in the body ( /AoVV
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Site of calcium reabsorptIon ( i t'\ r.... -
Characteristic of both vitamin 8
12
and folic acid deficiency ( J /OwN.
Which component is required for vitamin B12 absorption ( )
What is orthopnea? ( ) "'r 0"'-
What iron salts have higher Gl absorption? ( ......
A patient deficiency, sulfa drug can cause... ( )
Moon shaped RBCare seen in.. ( ) $/c..k.tzJcdJ. c.et1- a
The highest elemental iron present in... ( )
Apatient taking methotrexate for cancer treatment, to treat bucal ulcers give... (
How do you take iron supplement? ( ) 4e.J<'JI;
Common side effect of iron supplement ( J 0"d:hpeJA.......,;,
Overdose symptoms of iron ( )
Iron supplement antidote ( ) a w,JV'\.I.I -h:J
liquid iron is taken by using.. ( ) sJ..I.A.......,....h. "void oS "'V9
What type of anemia can cause G6PD deficiency? ( .. ) 0
Drugs that induce hemolytic anemia? ( )
What is hemochromatosis? ( l..<..d........,.l
Excessive bleeding like menorrhea cause the type of anemia --> (
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11-10
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Biochemistry

Bioch'emistry
Questions Alerts!
Common questions ilJ pharmacy exam is to ask!
Primary metabolism of glucose ( glycolysis, glycogenesis, gluconeogenesis)
Essential aminoacids (PVT TIM HALL)
Essential fatty acids (Omega 3, 6 and 9)
This chapter reviews basic and essentials of biochemistry topics such as, intermediary metabolism,
carbohydrates, lipids, amino acids, proteins, enzyme kinetics and porphyrins.
Catabolism: This pathway convert pyruvate (glycolysis), acetyl Co-A (fatty acid degradation),
and amino acid to carbon dioxide and water with release of energy. This cycle is strictly
oxygen dependent (aerobic).
Anabolism: This pathway forms amino acid such as aspartate and glutamate from cycle
intermediates; also the porphyrin ring of the heme (hemoglobin, myoglobin and .cytochrome)
is formed from intermediates cycle.
Fermentation: The formation of ethanol and lactate from glucose are examples of
fermentation.
Carbohydrate classification
Monosaccharides; C6H1206 = Examples: Glucose, Fructose
'. Disaccharides =C
12
H
24
0
12
=Examples: Sucrose, lactose, and maltose .
Polysaccharides ='More than two mon'osaccharides = Examples: starch, cellulose
Oligosaccharides =2 tolD monomers
12-1
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12-2
Carbohydrate metabolism
Glycolysis: Glucose -7 CO
2
+ H
2
0
Under anaerobic conditions (absence of O
2
). Glycolysis involves the conversion of glucose to
lactate (lactic acid). This can occurs in ce.JIs without mitochondria.
Biochemistry
www.PharmacyPrep.Com
..
Glycolysis is breakdown of glucose to water and carbon dioxide. Glycolysis occurs in the
cytosol and mitochondria in most organs of the body.
Glycogenolysis (glycogen breakdown): Glycogen -7 Glucose (Glycogenolysis is break down of
glycogen to glucose.)
Under aerobic conditions (presence of 0
2
1. Glycolysis involves the conversion of glucose to
pyruvate (pyruvic acid), this occurs in mitochondria.
Carbohydrate digestion and absorption; Dietary carbohydrate is digested in the mouth and
intestine and absorbed from the small intestine.
Disaccharides (e.g" sucrose, lactose). oligosaccharides (e.g., dextrins), and polysaccharides
(e.g., starch) are cleaved into monosaccharides (e.g., glucose, fructose).
Glycogenesis (glycogen synthesis): Glucose Glycogen (Glycogenesis is synthesis of
glycogen from glucose. This glycogen is stored in liver and muscle.)
Mature RBC lack mitochondria, hence there is no Krebs cycle activity. In bacteria use
glyoxylate cycle in place of Krebs cycle.
Citric acid cycle (Krebs cycle): This citric acid cycle pathway is also known as the Krebs cycle,
which serves both breakdown and synthetic purposes, and occurs in mitochondrial
compartment.
Gluconeogenesis
Gluconeogenesis is the synthesis of glucose from non carbohydrate sources.
This process, which occurs primarily in the liver and kidney is the synthesis of glucose from
small noncarbohydrate precursors such as lactate and alanine.
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GLYCOLYSIS
Glycogenolysis
[GLUCOSE < .. 'I GLYCOGEN I
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Glycogenesis
Gluconeogenesis
IFAT & PROTEId
Amino Acids
Essential amino acids (EMs) are the components of proteins that make them essential in the
diet, of the 20 amino acids in proteins, 10 are essential, i. e, 1'equired
cannqt.be synthesizedin the body;. All humans require eight EAAs. Infants require histadine
- ...::-,.;'&.... _.,........ - ........ ..
Only essential amino acids taken through diet because they are not synthesized in body in
sufficient amounts. Essential amino acids are PVT TIMHAU: Phenylalanine, Valine,
Tryptophan, Threonine, Isoleucine, Methionine, Histidine (in infants), Arginine (in infants), --
leucine and Lysine .\

,
Tyrosin -? Thyroxine
Dopa -? Melanin
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Tryptophan -? Niacin ,""t 8.s .
Tryptophan -? Melatonin
Histadine -? Histamine
Glycine -? Porphyrine ring -? Heme
Arginin -? Nitric oxide (NOj-? vasodilator
Arginin -? Urea
Arginin -? Creatinin
;Glutamate -? Gamma aminobutyric acid (GABA)
ACID Base properties of amino acids:
12-3
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Biochemistry
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At all physiological pH all amino acids have both negative and positive charge.
When pH =pKa, there is 50% ionized and 50% unionized.
Amino acids can act either as an acid or base and are defjned as a'mphoteric or ampholytes.
Zwitter Ion: Amino acids are ionisable +ve ions as amines, -ve ions as acid. (no net charge)
pKa values indicate the pH at which the group (acid or amine) is 50% dissociated
All amino acids have two titration curves.
H,N(+)-CH,-COO(-I
rsoelectric Point: (pi) The pH at which there is no net charge on the structure.
At a pH > pi the structure has net negative charge
At a pH < pi the structure has net positive charge.
Every structure has one isoelectric point but can be many pKa values.
Proteins
There are 20 amino acids commonly found in proteins, they are linked together by peptide
bonds. Protein is generally classified into three different categories:
I Simple protein
II Conjugated protein
III Derived protein
Simple protein are naturally occurring proteins, which upon hydrolysis yield only alpha-amino
acids such as albumins, globulins, prolamines, glutelins, and albuminoids.
Conjugated protein: Conjugated proteins are further classified on the nature of their
prosthetic groups
Derived proteins: They are formed from primary or conjugated proteins by the actions of the
acid, alkali, heat, water, enzyme or alcohol. They generally differ in physical and chemical
properties from the protein they are derived from. They are subdivided into primary derived
protein (Denatured protein) or secondary derived protein
\
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Phosphoprotein
Nucleoprotein
Glycoprotein
Chromoprotein
lipoprotein
Metalloprotein
Prosthetic Group
Phosphoric acid
Nucleic acid
Carbohydrate
Colored group
lipids
Metals
Example
Casein ovovitellin
nuclein
mucins
hemoglobin
lecithin, lOl, HDl
tyrosinase
Arginase
Xanthine oxidase
12-4
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Biochemi try
, .
Denaturation of proteins: p'rotein denaturation r.esults in the unfolding and of
the protein structure, which does not occurs by hydrolysis.
. . - .
Denaturising agents include: heat, organic solvents, mechanical mixing, strong acids or base,
detergents and ions of heavy metals such as lead or mercury. Denatured proteins are
insoluble and precipitate. Denaturation process is often irreversible.
Globular and Fibrous proteins:
Globular hemeproteins: Hemeproteins are groups of specialized proteins that contain heme
as tightly bound prothetic groups. The most common heme proteins in human are:
haemoglobin and myglobin. These proteins bind oxygen reversible. These proteins have high
affinity to carbon monoxide.
Hemoglobin: complex of porphyrin ring and ion (Fe
2
+). Transport oxygen in blood only.
Carbon dioxides and carbon monoxide also binds with haemoglobin reversible.
Myoglobin: complex of porphyrin ring and ferrous ion (Fe
2
+). Transport oxygen in tissues.
Myoglobin present in heart and skeletal muscles.
Hemoglobinopathies: Example of hemoglobinopathies: Sickle cells anemia, (HbS),
haemoglobin Cdisease (HbC) and the thalassemia syndrome.
Fats and Lipids
Fatty Acid Synthesis Palmitate is an end product. Associated with Hexose
Monophosphate Shunt.
=:
Lipids can be divided into five classes according to their chemical structure.
Glycolipids: Also known as cerebrosid.es. They are isolated from the brain. Upon hydrolysis,
they yield fatty acid, galactose and sphingosine. They are also known as galactolipids due to
the presence of galactose, such as phrenosin, and kerasin.
Phospholipids: Known as phosphatides. They are esters that consist of fatty acid, phosphoric
acids and nitrogenous compounds, such as lecithin.
Sterols: The sterols are alcohols structurally related to steroids. They are obtained from
plants and animals such as cholesterol and ergosterol. Steroid structures have 3 cyclohexane
rings and 1 cyclopentane ring.
Waxes: Waxes are defined as high molecular weight esters. They consist of monohydric
alcohol and high molecular weight of fatty acids, such as spermaceti.
12-5
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Biochemistry
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Fixed oils and fats: They are esters of and fatty aCid's, as olive .oil. Fixed oils, such
as hard, which are solid at room are as fat. c..
Iron
Zinc
Iodine
Selenium
Chromium
Molybdenum
Copper Wilson's disease (excess), leucopenia, neutropenia (deficiency),
Minks' (defect of Cu+).
Penicillamine is used for treatment of Wilson's disease.
Copper present in: Cytochrome oxidase
The most abundant metal in body
Deficiency of iro'n microcytic anemia, and hypochromic anemia
Hemochromatosis {excess of iron)
Enzyme or proteins contain iron: Hemoglobin, myoglobin,
Cytochrome oxidase, myeloperoxidase.
Children: poor growth, impaired sexual development (deficiency)
Adults: dermatitis (alcoholics)
Selenium deficiency can cause cardiomyopathy..
Impaired glucose tolerance
Present in xanthine oxidase enzyme which catalyzes conversion of
purine to uric acid
Deficiency of iodine may cause goiter disease

Trace element Complication associated with deficiencies
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The serotonin is produced by? ( \ )
Phenylketonuria (PKU) is? ( l3
Carbon monoxide-has affinity to? ( 10
Carboxyhemoglobin is? ( "5"
l. linolenic (Omega 3) 2. linoleic (omega 6) 3. Arachidonic

4. Arginin S. Oxidized hemoglobin 6 HMG Co- Reductase
7. Methylated 8. Prostaglandin 9. Ferrous
hemoglobin
10 Hemoglobin 11 Myoglobin 12 Cytochrome
oxidase
13 Excessive 14 Tryptophan
phenylalanine in the
urine
Nitric oxide (NO) is a derivative of what amino acid? (
)
!
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12-6
Ilioehemistry
Methemoglobin is? ( 7 )
Iron in hemoglobin is normally what state? (el )
Cholesterol synthesis rate limiting step is cata1Y1'ed by... (
Essential fatty acids ( I, 2- )
Ecosanoids synthesis are dependent on? ( q
The most basic amino acid (J1) L A -'2 A. l-
Zwitterion-7 A-wd (;.pH., v.(...
All amino acids have two titra.tion curve lAS>
Isoelectric point (pl)-7 pH d"f5 IV\;
At pH>pl the structure has net negative charge
At pH<pl the structure. has net positive I
Energy storage form in body is? & lr .. n S' L J
Starch is composed of? I..pi <A t.., ro Je-
Lecithins-7 b-r l;prebtl q L"pufW'o
Sphingofipids are-7 Crt lJ to Wp"-,
End product of anaerobic glycolysis -7
End product of aerobic glycolysis -7 .
End product of amino acid (proteips) synthesis -7
Krebs cycle occurs in -7 /t'V"l )ro ()...-"-
End product of purine cycle -7 LA#"l.:.. <::::"'A.,..- r .
Glycolysis occurs in? pi i-1 f--ULl-
..
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/-
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Clinical Biochemistry
Renal Function Tests BUN
Liver Function Tests AST, ALT, ALP, bilirubin
Cardiac Enzymes Troponins I, Creatinine kinase (CK)
Urine Analysis Ketone bodies, pH, specific gravity
Blood works CBC
Anticoagulants INR (International normalized ratio), warfarin (INR 2 to 3), heparin (aPTI), and
LMWH (no monitoring)
Thyroids Tests -:> Serum TSH (0.5 to 5 mUlL), TI4, FT4, TI3 and FT3
Questions Alerts!
{
This chapter reviews basics of clinical biochemistry such as liver function tests, renal function tests, haematology,
acid base disorders, anemia and its application in laboratory tests to monitor diseases and monitor drug adverse
reactions.
Common tests: renal function test, liver function test (LFT), urinalysis, common enzyme serum
test, and hematological test (blood works).
( I
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Renal Function Tests (RFT)-7CrCI, BUN
Liver Function Tests (LFT)-7LDH, AST, ALP
Cardiac Enzymes -7 Troponins I, Creatinin Kinase (CK)
Urine Analysis -7 Ketone bodies, pH, specific gravity
Blood works (hematological)-7 CBC
Anticoagulants -7 INR (International normalized ratio), warfarin (INR 2 to 3),
I (aPTI), and LMWH (no monitoring)
,
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Renal Function Test. Can be measured by blood urea nitrogen (BUN), serum
creatinin, and creatinin clearance (Crel).
Blood urea nitrogen (BUN): Urea: an end product ofprotein metabolism. It is produced in liver
and excreted by the kidneys. In normal conditions, urea clearance is equal 60 % GFR. BUN
increase indicates renal disease.
PhannacyPrep.
13-1
Clinical Biqchemistrv
Normal values for BUN: range 8 mg/dL to 18 mg/dL (3 to 6.5 mmol!q. The concentration of
BUN reflects renal function, because the urea nitrogen in blood is filtered completely at the
glomeruli of the kidney, then reabsorbed and tubular secreted within nephron.
Increase in BUN indicates an acute renal failure. The BUN decrease may indicate terminal
stages of liver disease, because liver produces solely BUN. Increase BUN indicator of azotemia
or uremia
Serum Creatinine: The creatinine is a metabolic product of muscle creatinin phosphate. More
sensitive indicator for renal damage than BUN levels.
Normal values for serum creatinine range from 0.6 to 1.2 mg/dL (50 to 120 mmoI!L).
Generally serum creatinine values doubles with each 50% decrease in GER. If a patient normal
serum creatinin is 1mg/dL represents 100% renal function, 2mg/dL represents 50% function
and 4mg/dL represents 25% function. Serum creatinin solely filtered by glomerular filtration
(GFR). Thereby decrease GFR, may lead to increase in serum creatinine (SrCr). This indicates
renal disease.
.-- Le.--Y:S ~ c- ~ ~
Serum creatinine decreased in elderly; As a person gets older muscle mass represents a small
proportion of total weight and creatinine production is decreased.
Females: Serum creatinine concentration in females patient is generally 0.2 to OAmg/dL less
than males, because females have relatively small kidneys.
Creatinine Clearance: The rate at which creatinine is removed from the blood by the kidney,
roughly equal to GFR. Normal values for men range from 80 mL/min to 120 mL/min. If it is less
than < 50 ml/min, it is categorised as renal disease. Creatinine clearance reflects the GFR.
<.2>OH ~ ~ a N 2 ~ ~
Calculation for creatinine clearance (Cl
cr
): Cl
cr
= CuV/ C
Cr
C
u
= concentration of creatinin in urine
V =urine volume (millilitres per minute or urine formed over collection period).
C
cr
serum creatinin concentration.
CI cr = (140 - age) (body wt in Kg)
g (C
cr
in mg/dl)
. To measure creatinine clearance use: Cockcroft and Gault formula
for males (mL/min) = (l40-Age)/{Body weight in Kg)
(SrCr)/72
for female, the above formula must be multiplied by 85%
PharmacyPrep. .
13-2
Aspartate aminotransferase {AST): Previously known as serum glutamic oxalocacetic
transaminase (SGOT), primarily. found in heart, liver tissues, and lesser extent is found in
skeletal !21uscles, renal tissues, and pancreatic tissues. AST is sensitive to damage to heart,
such as MI, CHF, and acute hepatitis.
13-3
Alkaline phosphate (ALP): It is produced from the liver and bones. This is sensitive to mild
or partial biliary obstruction.
]

. are 4 liver enzymes which are indicators of liver
dysfunction. levelsof LDH, ALP, AST and AlT increase with liver dysfunction. Increase levels of
these enzymes indicate liver has been damaged.
lDH = lactate dehydrogenase; ALP = Alkaline phosphate; AST = Aspartate aminotransferase;
ALI =Alanin aminotransferase .
lactate dehydrogenase (lDH): The glycolytic enzyme LD (100 to 190 units!L) catalyzes the
interconversion of lactate and pyruvate and present in most tissues. LDH is present in high
concentration in the heart, kidney, liver, lungs, and skeletal muscles.
The liver will liberate LDH quickly when damaged by physical trauma, infection or
ischemia.
lDH therefore useful in diagnosing myocardial infarction, hepatic disease and lung disease
LDH"& LDH,
LDH, LDf4, and LDH,
(Heart) (Lungs) (Liver, skeletal muscle)
Cardiac Troponins (Tn):

Troponins T, Cand I are complex of proteins that mediate the calcium mediated _,
interactions of actin and myosin with muscles.
Troponin T is in: Cardiac and skeletal muscle cells.
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Alanin aminotransferase (ALT): It is previously known as serum glutamic pyruvic
(SGPT). It is primarily found in liver, and lesser amount in heart, skeletal
.. ;'" muscles, and kidney. AlT is sensitive to cell damage, less sensitive than AST.
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Troponin I is present only in cardiac muscle. (TI for MI)
Troponin Cis present in two distinct isoforms that are present in skefetal arid'-cardiac "---"
muscles: '.'
Troponin T and I are more specifi.c and sensitive indicator of myocardial injury.
Troponins are a relatively new method to identify myocardial cell injury and thus assist in
the diagnosis of acute MI
The use of troponin as primary diagnostic tests for acute MI is widely accepted.
Serum Bilirubin (Bile):
It is primary breakdown product of haemoglobin and is formed in reticulosites into stream
blood. Where it is almost completely b.ound to serum.albumin. When bilrubin arrives at
the liver at sinosidal surface of liver cells, the free fraction is rapidly taken up by liver and
converted to bilrubin diglucorinide and monoglucorinide, referred to as conjugated
bilirubin. The conjugated biliruhin then secrete into bile, appears in intestine, where
bacterial converts bilirubin to urobilinogen. Most of urobilinogen is destroyed in feces, but
some fraction reabsorbed in blood and liver.
Effective bilirubin conjugation and excretion depends on RBC turnover and hepatobilary
function. Normal values of total bilirubin are: 0.1 to 1 mg/dL (2 to 18 mmol/L)
Direct bilirubin: 0.0 to 0.2 mg/dL (0 to 4 mmol/L).
Increase of bilirubin indicates jaundice.
Causes of increased bilirubin: Hepatocellular damage, cholestasis (post hepatic), hemolysis
(prehepatic). There are 3 major reasons for increase bilirubin:
Increase hemolysis (urine color not changed)
Biliary obstruction (biliary stones), dark urine and bile in urine, chlorpromazine gives intra
hepatic cholestasis)
Liver cell necrosis (viral hepatitis), dark urine color and bile in urine..
Serum Protein (blood proteins)
Primary serum proteins: Albumin and globulins (alpha, beta, gamma). Albur:nin is the
major protein of the blood, it constitutes 55% of serum proteins. Acidic drugs bind to
albumin. It is primarily produced from liver. Albumin: (40 to 60 giL) liver disease decrease
albumin.
Albumin is produced by the liver and contributes approximately 80% of serum colloid
osmotic pressure. Therefore hypoalbuminemia associated with edema and transudation
of extracellular fluid (ECF).
Hypoalbuminemia
Decrease in essential amino acids due to malnutrition can lead to hypoalbuminemia.
Albumin can be lost directly from blood because of hemorrhage, and burns.
Hyperalbuminemia
Increase in albumin can cause shock or volume depletion.
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13-4
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Plasma Proteins Concentration that chanRes with some conditions
Conditions Albumin Alpha -1- acid glycOPr6tein
Renal failure
t
Hepatic failure
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Arthritis - t
Burns
-
Pregnancy
-
Stress/Trauma
t
Globulins: There are several types of globulins such as alpha, beta, gamma, etc.
The gamma globulins are the same as immunoglobulin (Ig).
Globulins: 2.3 to 35g!L: A decrease in albumin levels results in compensatory increase of
globulins.
Uri nalysis: Provides basic information regarding renal function, urinary tract disease, and
presence of certain systemic diseases.
Urine colors: Normal urine color is clear, pale yellow, and deep gold.
Red color may be blood, drugs such as pyruvinium pamoate. phenolphthalein (used as
laxative)
Brownish-yellow -7 conjugated bilirubin, jaundice
Orange red -7 rifampin
Dark urine -7 metronidazole. metformin
Blue color -7 Triamterene
Pyuria and baeturia is symptoms of -7urinary tract infection
pH: Urine pH is around 5 to 9
Specific gravity (SG): Normal SG is 1.003 to 1.035
Increase SG indicates -7 excessive blood sugars or proteins in urine
Decreased SG indicates -7 diabetes insipidus.
Fixed SG at 1.003 indicates -7 kidney lost its ability to concentrate or dilute urine
Proteins in urine: Normal values SO to 80 mg/24 hours. Excessive proteins in urine
(proteinuria) -7 caused by UTI (bladder infection), renal disease. fever, and venous
congestion.
Albuminuria indicates glomerular permeability
Microalbuminuria presence of albumin in urine at the level of higher than normal but
lower than the limits that are detected by standard test. Microalbuminuria indicates
nephropathy
Glucose: Glucose does not normally appear in urine. Glycosu'ria indicates diabetes
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illegal (0 reproduce wilhou( permission. This manual is being used during review sessions conducted by
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13-5
Ketones: Ketones does NOT normally appear in urine. If there is No glucose stores, fats stores
begins to metabolize to ketones. Ketonuria indicates uncontrolled OM, or starvation, and zero
or low carbohydrate diets.
Three types of ketone bodies:
Betahydroxy butyric acid (80%) I kL+O
Acetoacetic acid (20%)
Acetone (trace amounts)
Components of urinalysis:
pH----------4.S to 9.0
Specific gravity------l.OlO to 1.025
Protein levels-----------SO to 80 mg/24hours
Glucose levels-------------180 mg/dL
Ketone levels----------(type 2 DM)-----do not appear in urine
Common Serum Enzymes: Creatin kinase (CK), previously known as creatin
. -
phosphokinase (CPK). It is primarily found in heart muscle, skeletal muscle and brain tissue.
Creatin kinase catalyzes the transfer of high energy phosphate group in tissues that consume
large amount of energy. Therefore total CK can increase in exercise, 1M injections of drugs
that are irritating to tissue (diazepam, phenytoin, statins), acute psychosis episodes, and
myocardial injury.
CK
I I
CK-MM CK-BB CK-I\I!B V"
In muscle
In
\;-
cp+cJ, j/\./
.
CK isoenzyme: Creatin kinase helps to diagnose myocardial (acute) (CK-MB) or skeletal muscle
(CK-MM) damage diagnostic tests. Deep intramuscularly injection can CK levels.
CK-MM is found in skeletal muscle
CK-BB is found in brain tissue
CK-MB is found in heart muscle
Hematological laboratory Tests (Blood work): Complete blood counts (CBe): The CBt is one
of the most commonly ordered clinical laboratory test. It is package of the following
laboratory tests: CBC measures:
Hemoglobin (Hgb)
Hematocrit (Hct) or Packed cell volume (PCV)
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13-6
(
('.:
Total white blood cells (WBC)
Red blood cells (RBe)
Mean Cell Volume (MCV)
Mean Cell hemoglobin concentration (MCHC)
Some CBe mayor may not include:
Platelets count
Reticulocytes counts
Leukocyte differential count
Hematocrit (Het): The percentage of red blood cells to the blood volume is the Het. (Packed
cell volume). The decrease in {.J,HctJ result from anemia, bleeding, bone marrow depression
by drugs, chronic diseases, genetic anemia (sickle cell anemia), and hemolysis. An increase in
Het may result from: polycythemia (this means increase RBe)
WBCs (leukocytes): also referred to white cell count.
Normal levels of WBC: 4,000 to 11,000 WBC/mm
3
.
WBC signals infection (leukocytosis) and inflammation.
WBC indicates bone marrow depression this indicates (Ieukopenial
,... 14 Jtz: I "4"d!r'-

55%- 75%
20% to 40%
0% to 7%
0% t05%
0% to 1%
Neutrophils
lymphocytes
Monocytes
Eosinophils
Basophils
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Measuring blood coagulation
Warfarin Heparin low Molecular Weight Heparins (lMWH)
Oral anticoagulant ivor S(
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INR and PT .PTT Not monitored because predictable response
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Bacterial infections generally increase neutrophils to 80% and decrease lymphocytes to

10%.
Viral infections increase lymphocytes (lymphocytosis)
Allergic reactions, such as asthma, allergic rhinitis, parasite infections, and drug allergies
Increase eosinophils f:l r 1 -r cBJA . .
COPO Increase neutrophils ..,..
Immunodeficiency, AIDS or WBCs (lymphopenia), or duster
differential ((0
4
count)
Tuberculosis Increase monocytes (monocytosis)
(
Warfarin monitoring: International normalized ratIo (INR) (2 to 3), and prothrombin time
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PharmacyPrcp.
13-7
Heparin monitoring: Activated partial thromboplastin time (aPTI), heparin assay, and PT
Prothrombin Time (PT): Prothrombin is synthesized in the liver and is converted to thrombin
during blood clotting process.
Thrombin formation is the critical event in the hemostatic process because thrombin
creates fibrin monomers that form a network of clot and thrombin activates platelets.
Clotting time
Measures deficiencies in factor II, VII, IX, X (2, 7, 9 and 10)
Not specific for liver diseases
Normal values: 10 to 13 seconds
+
Increase in PT (INR) .
Can occur due to inadequate vitamin K in the diet or drugs that i.ncrease PT; warfarin,
low molecula( weight heparins (LMWH), high dose.of salicylates, and antibiotics.
The higher the PT, the greater the risk of bleeding.
Decrease in PT (INR)
Increase in vitamin K supplements or diet that contains vitamin Ksuch as dark green
vegetables, broccoli, avocado, spinach, and lettuce. Thereby increase in risk of blood clot.
Activated Partial Thromboplastin Time (aPTI):
The aPTI measures the intrinsic clotting system, which depends on factors.
Measures intrinsic clotting system factors VIII, IX, XI, XII and XIII as well as common
pathway factors II, V, and X.
Monitored for heparin therapy
Normal values: 21 to 45 sec
Increase in aPTT
Causes:
Severe liver dysfunction
Inadequate vitamin Kintake (deficienCy of vitamin K)
Poor or inadequate nutrition
Increase in aPTI increase the risk of bleeding
. International normalized ratio (INR): The INR is the PT ratio that would result if world health
organizations (WHO) international reference thromboplastin were used to test the patient
sample. NormallNR is 2 to 3 in patient using warfarin. Increase in INR is an indication of
blood thinning where as decrease in INR is an indication of b,lood thickening.
Increase in INR (>3): Indicate blood thinning: Warfarin, Heparins, LMWH, ASA/NSAID,
Acetaminophen> 2g
PharmacyPrep.
13-8
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Decrease in INR 2): Indicate blood thickening
Vitamin Ksupplements
Green vegetable (avocado, broccoli and spinach)
Oral contraceptives
Normal lipoproteins levels
low density (LDL) cholesterol (serum) <2.2 mmol/l or <125 mgjdL
Triglycerides <3.6 mmol/L or <160 mgJdl
High density (HOL) cholesterol (serum) >0.9 mmol/l >35 mg/dl
Cholesterol/HDl ratio is 5 mmol/l
Thyroid function tests (serum)
Normal Hypothyroidism Hyperthyroidism
TSH: 0.5 mUll to 5 mUll > SmUll <0.5 mU/l
Serum TSH Sensitive TSH
Free T and TJ
Thyroid stimulating hormone (TSH)-70.5 to 5.0 mUjL, 0.5-5.0 jlU/ml
Free thyroxine (free T4)-710 to 36 pmoljl, 0.8-2.8 ngjdl
Total serum thyroxine (T
4
)-7 51-142 nmol/L, 4-11 ,ug/dL
Total serum triiodothyroxine (T3)-71.2-3.0 nmol/L 78-195 ng/dL
Thyroid disease diagnosis tests-7 Free T4 and Sensitive T5H
Replacement therapy for Sensitive TSH assay, Free thyroxin index (FTI),
resin triiodothyronine uptake RT3U, Total thyroxin TT
4
FreeT
3
and T4 :
The FT4 is the most reliable diagnostic test for evaluation of hypothyroidism and
hyperthyroidism when thyroid hormone binding abnormality exists. In contrast
measurement of
FT3 is expensive.
Total T
3
and T4 (TT3and IT4):
The IT3and IT4 measures both free and bound (total serum T3and T4)'
/
IT3 is particularly helpful in diagnosis of Graves's disease.
TT3 is not good indicator of hypothyroidism.
Thyroid stimulating hormone (TSH):
The secum TSH is the most sensitive test to evaluate thyroid function.
The TSH is elevated in hypothyroidism
. .
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In dehydration:
Mild: normal BUN/Creatinine
Moderate: t BUN/Creatinine
Severe: t BUN/Creatinine, t Hb, low sucrose
Tips
1. 80-120 ml/min 2. bleeding 3. bilirubin
4. does not change 5. parathyroid hormone (PTH) 6. 3.5 to 5 meq/L
7. 2 to 3 8. troponin 9. aPTI
10 AST>ALT 11 Creatinine kinase CK-MB 12. Stop Warfarin, monitor INR
and give oral Vit K
13 No monitoring
required
----::;)
Normal range of serum potassium levels? (6) -;sH
Hypothyroidism can be monitored by? (
What is normallNR level in patient taking warfarin? (2-1&1.
Increase INR indicated the risk of? ( & 't"
Normal levels range of creatinine clearance l. 0 I J.,.. . h I .....
What substance levels are increased in jaundice? ( ) I;l $ i >- p..l-..,. A-
What enzyme ration increases in alcoholic hepatitis? ( . ) A j 1 >A-.!.-..,.
What is monitored in patient taking LMWH? ( ) M(.1 ,......,0 Y'l - TDJ.J< '1b dt\. 5
If INR is more than 5 indicates ( ) ).J4.>- 0& b ,
What is monitored by heparin? ( a 1'71) ....-
Name the enzyme most likely to increase in levels suggesting a myocardial infarction? ( C k - M (3
What cardiac enzyme exclusively elevated after MI? ( ) -r,.<AJ pO tn J"'t - \
Osteoporosis can change calcium level by? ( ) cl 0eA IAcH- ....,...Cll.
Calcitonin opposes action of? ( ) poJ...PJ{.., JkH J
b6VVL

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PharmacyPrep.
13-10
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Alerts!
Vitamin A, D, E, K and Vitamin B deficiency symptoms
Active vitamin OJ
Essential fatty acids (omega 3 and omega 6)
Nutrition
14
Nutrition
(r--
This chapter review the important feature of the vitamins is that they generally cannot be synthesized by
mammalian cells and, therefore, must be supplied in the diet.
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Balanced diet
Carbohydrate 55%
Proteins 30%
Fats <5%
Fibre 30 g/day (vegetables, cereals etc)
Minerals/Vitamins
Water 8 to 10 glass/day
Salt <2 g jday
,/ Nutrition Allergens
Gluten Wheat, rye, oat, soy, cereal
Milk -7l!aaose or
Peanut -7 ,
Tartrazine 7yellow coloring agent
iO. i 'o!. hOI, H0 Orl uJ<! Yl.-
The vitamins are of two distinct types:
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Vitamins
I
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Water soluble Fat soluble
Thiamine (E,), Riboflavin (B,), Niacin (E)), Vitamin A
Pantothenic Acid (B
5
), Pyridoxal, Pyridoxamine, Vitamin D
Pyridoxime (B6), Biotin, Cobalamin (B12) Vitamin E
Folic acid, Ascorbic Acid (C) Vitamin K
o i 11 -thL. bl 1'>-'-1 kf Il I'\.b.JdP>v-o
...; Thiamine (Vitamin BIl
.\'

Derived from a substituted pyrimidine and thiazole which are
, ,-
coupled by a methylene bridge
p
(
It is rapidly converted to its active form: Thiamine

pyrophosphate (TPP), and thiamine diphosphotransferase
f
Dietary
t.!!e arbhy,drate ..E0rl.!ent. of ...!he .J!if1-is then
requirements thiamine intake should be required.
Deficiency

Severely reduced capacity of cells to generate energy
Beriberi (result from a diet of carbohydrate rich and thiamine
- deficiency) /'" (b,<p.J" c.. .......<L- tcJ, rh/y""""
v
Wernicke-Korsaskoff syndrome (Thiamine related disease

I
,
mostly found in chronic alcoholics due to their poor dietary
lifestyle)
Deficient in chronic alcoholic thereby take vitamin B
1
supplement.
Riboflavin (Vitamin B
2
1
It is a precursor for coenzyme flavin rnononucteotide (FMN) and

Flavin adenine dinucleotide (FAD)\The enzyme'that requires
FMN or FAD as cofactor are termed f1avoproteins
Riboflavin decomposes when,exposed to visible light. This

characteristics tan to .. ncies in newborns
treated fOLQj"yperblirubinemia bv phototherapv
Source

Eggs, milk, meat, and cereals "10.,.,0.&." rfW{.po"', tr( ""oNt, d. fW
Dietary
1.2 to 1.7mgfday for normal adults

requirements
Deficiency

It is often seen in chronic alcoholics due to their poor dietetic
habits . , .
sIs

Glossitis, angular stoma'titis, cheilosis and
photophobia .../
.
Niacin {Vitamin B31
Both nicotinic acid and nicotinamide can serve as the dietary

source of vitamin B
3
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Niacin is required for the synthesis of the active forms of Vitamin
B
3
, nicotinamide adenine dinucleotide (NAD+), and nicotinamide
adenine dinucleotide phosphate (NADP).
Both NAO+ and NADP' function as cofactors for numerous
dehydrogenases. Eg. lactate and malate dehydrogenases
Niacin is NOT a true vitamin in the strictest definition since it can
be deriyed from amino acid tryptophan
Dietary
Nicotinic acid (but not nicotinamide) when administered in
requirement pharmacological doses of 2 to 4g/day lowers plasma cholesterol
s levels and has been shown to be useful therapeutic for
hypercholesterolemia.
Nicotinic acid therapy is not recommended for diabetics or

persons who suffer from gout.
Deficiency

Diet deficiency in niacin (as well as tryptophan) leads to glossitis
of the tongue, dermatitis, weight loss, diarrhea, depression and
dementia
Severe symptoms: Depression, dermatitis and diarrhea, are
associated with the condition known as PElLAGRA
Several physiological conditions (E.g. Hartnup disease and

malignant carcinoid syndrome)
In Hartnup disease tryptophan absorption is impaired and in
malignant carcinoid syndrome tryptophan metabolism is altered
resulting in excess serotonin synthesis
Drug (-l- ) Isoniazid therapy (for TB) may lead to niacin deficiency
Niacin
Pantothenic acid (Vitamin 8
s
)
,.
It is formed from Dlanine and pantoic acid.
Source

Whole grain cereals, legumes, and meat
Deficiency

Extremely rare for it is readily available food sources
Vitamin B;o;vri oxine, Pyridoxal, and Pyridoxamine)

-; -r
"""- I'
Biologically active form of vitamin B6, pyridoxal phosphate
Dietary

During pregnancy and lactation the requirement for vitamin
B6 increases approximately O.6mgfday. Therefore vitamin 8
6
used for nausea & vomiting in pregnancy.
Drug (-l-)

Isoniazid (for TB), and penicilla.mine (for rheumatoid arthritis
pyridoxal, and cystinurias)
Diclectin (vitamin B
6
+doxylamine) is the drug of choice for the
treatment of nausea & vomiting in pregnancy (morning sickness).
y

Avoid vitamin B
6
with levodopa because, vitamin 86 increases
the peripheral conversion of levodopa to dopamine thereby it
gives nausea and vomiting.
(
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14-3
www.PhannacyPrep.Com Nutritioll
Biotin ( \" f>'+- ')
Biotin is the cofactofrequired;by enzymes that are involved in
carboxylation reactions, ego acetyl CoA carboxylase and pyruvate
carboxylase
Source Found in numerous foods and also is synthesized by intestinal bacteria
Deficiency Excessive consumption of raw eggs due to affinity of egg white protein,
AVIDIN, for biotin preventing intestinal absorption of the biotin
Drug Antibiotics (long therapy)
,

Cyano cobalamin (Vitamin B
n
)
6 PI' '<J 1"
c.o
Is composed of a comple>(tetrapyrrgDfing structure (corrin ring)
and a cobalt ion in the center.
It must be hydrolyzed from protein in order to be active.

, .
+--
Hydrolysis occurs in the stomach, and carried to the ileum where
it is absorbed
.
--
8
12
as cofactor during these reactions: Catabolism of fatty acids
with an odd number of carbon atoms and the amino acids valine,
isoleucine and threonine
Following absorption the vitamin is transported to the liver in the

blood bound to transcobalamin II
Deficiency

Pernicious anemia is a megaloblastic anemia resulting from
vitamin 8
1
2 deficiency that develops as a result of lack of intrinsic
factor in the stomach leading to malabsorption of the vitamin B
12
.
Treatment of pernicious anemia: Use vitamin 8n parenteral (im or

sc), however do not use oral supplements.
Drug Vitamin 812 malabsorption has been reported with aminosalicylic
acid, slow-release potassium iodide, colchicine, trifluoperazine,
ethanol, metformin and oral contraceptives.
All persons over SO and elderly should get vitamin 8n

supplements of:approximately 2mcg daily.
Elderly are achlorhydric, thereby have decreased vitamin B

12
absorption.
. Folic Acid Ylt ij'j
A conjugated molecule consisting of a pteridine ring structure

linked to para-aminobenzoic acid (PABA) that forms pteroic acid
Animal cannot synthesize PABA nor attach glutamate residues to

pteroic acid, thus requiring folate intake in the diet.
Source

Yeast and leafy vegetables
Anfffial liver
Dietary

An .increase in the daily intake of folate during pregnancy is
requirements A

t-
1
JNH

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4-4
Nutrition
needed, and doubled by the third trimester of pregnancy
Deficiency
Megaloblastic anemia. (macrocytic anemia). in pregnancy can
cause neuro tubule defect.
SiS

Drug
Anticonvulsants, oral contraceptives, methotrexate, S-flurouracil

(S-FU) 5ulfonamides, trimethoprin, sulfasalazine and dapsone.
Ascorbic acid (Vitamin C)
Ascorbic acid is derived from glucose via the uronic acid pathway.
It is required for maintenance of normal connective tissue as well as
wound healing.
Hydroxylation of proline residues in collagen is the most important

reaction that requires as cofactor
Source
Fruits
Deficiency
Scurvy
Cause of vitamin Cdeficiency is poor diet and increased

requirements, esp during severe stress or trauma (Vitamin Cis
readily absorbed)
SIS

Easily bruised skin, muscle fatigue, soft swollen gums, decreases
wound healin!!: and hemorrhaging, osteoporosis, and anemia
-'
Ascorbic acid is a good water-soluble antioxidantD
An acidifying agent used to treat overdose of base drugs
Vitamin Cis deficient in smokers, thereby vitamin C

supplements.
Vitamin A
With 3 active molecules:
.d
B-carotene retinol '7 retinal '7 retinoic acid

Retinol, retinal (retinaJdehyde), and Retinoic acid

B-carotene is a precursor of vitamin A.
Ad.
Rhodopsin is active form of vitamin A in vision
B-carotene consist of 2 molecules of retinal linked at their

aldehyde ends, also referred as provitamin A
Very effective as antioxidant
Overdose of vitamin A can cause toxicity.
Excessive accumulation of vitamin A in the liver can lead to

toxicity, which manifest as bone pain, hepatosplenomegaly,
nausea and diarrhea.
Deficiency

Xerophthalmia
Signs and

Night blindness
symptoms
Early symptoms: Follicular hyperkeratinosis (increased
susceptibility to infection, cancer, and anemia equivalent to iron
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deficient anemia.
Prolonged lack of vitamin A: leads to deterioration of the eye
.tissue through progressive keratinization of the cornea, known as
xerophthalmia
(
Isotretinoin (Accutane) is 13-cis retinok acid and this is oral only

Tretinoin (Retin-A) is 13-trans retinoic acid and this is topical only

(ITT)
.
yr/
v.
Recommended vitamin A dose 2500 IU (over dose can cause
toxicity)
Vitamin 0
It is a steroid hormone.
Active form is: 1, (Vit 011 is derived

from ergosterol and from 7-dehydrocholesterol (produced in the
skin)
Chronic renal failure can cause deficiency of vitamin 0

3
Ergocalciferol (02) is formed by UV irradiation or ergosterol
In the skin 7-dehydrocholesterol is converted to cholecalciferol

following UV irradiation
Source

I liter milk fluid/day 400 IU vitamin 0
3
Person with risk for osteoporosis and taking bisphosphonates should
take 800 to 1200 IU vitamin D
3
/day
Dietary

Found fish liver oil and eggs. Also produced from skin
requirements
Deficiency

Rickets in children and osteomalacia in adult
S/5

Rickets is characterized by improper mineralization during
development of the bones resulting in soft bones
Osteomalacia is characterized by demineralization of previously

formed bone leading to increased softness and susceptibility to
fracture.
Drug
Vitamin 0 supplement 800 IU
Newborn (infant) on breast-feeding should get vitamin 0 drops.

Skin (ultraviolet)
i
Cholecalciferol
,j, 1c.,,} L".,
t PTH 0l)
,j, I ,I>,,,ph.,,, .. L:::--...

\
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1, 2S(OHI1chole<:alciferol
(Active)D]

24,25-(OHh-eholecalciferol
(Inactive)
14-6
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Nutrition
I
eOOH
9 12
Essential fatty acids (EFAs)
Essential fatty acids (EFAs) are required in amounts equalling 6 to 10%of fat intake
(equivalent to 5 to 10 glday).
15
5 3
) .
Alpha-Linolenic Acid (omega-3)

They include@6 (n-6) fatty acids are linoleic acid (cis-9, 12-octadecadienoic acid) and d ,..--
arachidonic acid (cis-5, 8,l1,14-eicosatetraenoic acid) and '6>-3 (n-3) fatty acids are
linolenic acid (Ci59, 12, lS-octadecatrienoic acid), acid
(EPA), and cis-4, 7,10,13,16,19-docosahexaenoic acid (DHA).
EFAs must be provided by the diet: Vegetable oils provide linoleic acid and linolenic acid,
and marine fish oils provide eicosapentaenoic acid and docosahexaenoic acid. However,
some HAs can be made from others. For example, the body can make arachidonic acid
from linoleic acid, and eicosapentaenoic acid (EPA) and docosahexaenoic (DHA) acid can
be partially synthesized from linolenic acid, although fish oil is a more efficient source.
Tips
i}rocopheral (vitamin E)

Act as a natural by sC3ven.ging free radicals and

molecular oxygen
Storage site of vitamin Eis in adipose tissue (fatty tissues).
Alpha tocopheral;s the strongest antioxidant among all
tocopherals.
Dietary
Increased intake of vitamin Eis recommended in premature
requirements
infants fed formulas that are low in vitamin as well as in persons
consuming a diet high in poly saturated fatty acids
SIS Increase in red blood cell fragility
Vitamin K
Vitamin K
1
(Phylloquinone) is derived from green vegetables
Vitamin K2 (Menaquinonej is produced by intestinal bacteria
Vitamin K] is a synthetic menadione. When vito K] is

administered, it will be alkylated to one of the vito K
z
forms of
menaquinone.
Dietary

It maintains normal levels of blood clotting protein factors 2, 7, 9,
requirements 10, and protein C, and protein S
'1H"- 6ke0bN1
Deficiency

Hemorrhagic syndrome (for infants)

Drug (t) Antidote of warfarin

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14-7
Nutrition
1. Vitamin D
:
2 Vit 812 Trans I, 3 retinoic acid (Vit A) 3
4. Vitamin D3 5 ileum 6 folic acid
7. neurotubule defect 8 Vitamin A 9 1,25 dihydrocholecalciferol
Vit D3
10 25 hydroxycholecalciferol
Vitamin D2 in liver
Chronic renal disease patient should receive vitamin -7 (
What vitamin is found only in animal products? (
The most common vitamin deficiency in United States and Canada (
What is precursor acid? ( ) -PJ:H3- It
Active form of vitamin Dis? ( r;)3 )
Storage form vitamin Dis? (cP2J r f u ~ ~
Supplement of folic acid in early pregnancy reduces? ( ) n.e..U/Ul
Sun exposed skin forms the type of vitamin Dis? ( ) ~ f L ~ ~
Retin A is topical used for wrinkles and acne is isomer of? ( ) rf",(Av::f 1J /Uli V',..tT1 vOClcl
Vitamin A, D, E, Kabsorption takes place in what part of gastrointestinal tract? ( ) @ty.aJ..( I ~ \-
All B-complex vitamin washouts from body except? ( (3" t2--)
what vitamin is essential for the synthesis of nitrogenous bases in DNA and RNA? ( ~ (J.e..t4
People who do not eat from animal sources have deficiency of? (\/(1- ) 1.3,2.-
what vitamin overdose causes toxicity? ( ) Vtl- P
Chronic alcoholics have deficiency of? ( ) '\/,.+- B1)-$2.-
Select True/False Statement

. -----
Deficiencies in newborns treated for hyperbilirubinemia by photo therapy; Riboflavin
Niacin is not a true vitamin. (True/False)
Niacin; derived from the amino acid tryptophan. (True/False)
Pellagra is due to deficiency of vitamin B
3
(niacin) (True/False)
Pernicious anemia is due to vitamin B
12
deficiency. (True/False)
i. Pteridine ring structure is present in folic acid (True/False)
Scurvy is due to deficiency in vitamin C. (True/False)
[J:arotenoids is precursor of vitamin A. (True/False)
Vitamin Ddeficiency in children is rickets and in adl:Jlts is osteomalacia.. (True/False)
Vitamin D supplements are recommended in newborn that are on breast-feeding.
(True/False)
14-8
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tube defects (spina bifida) in their children. (True/False)
Omega 6 is Lenore!c acid. (True/False)
Omega 3 is lenolenic acid -7 act like aspirin ~ Antiplatelets. (True/False)
lenolenic acid mainly present in fish and walnut. (True/False)
Vitamin Etoxicity ~ More than 1100 units (average capsule is 400 units) ~ Prevent the
synthesis vitamin Kcoagulant factors (act as anticoagulant). (True/False)
Severe Vitamin 8
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thiamine deficiency; Beriberi and WernickeKorsaskoff syndrome.
(True/False)
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Microbiology
Questions Alerts!
Endotoxin (pyrogen) of gram negative and exotoxins gives positive organism
Infective organism of common. infections like pneumonia, traveler's diarrhea, toxic shock syndrome,
endocarditis, cellulites, meningitis I 6;ifhi 1 .
VIA.tA!:J: Hsv 1, 2 I Vz.. V I "psfei M V
co '. A I B, c ct ViM.<.&)
Bacterral Structure
Bacteria =Contain cell membrane and cell organs
Bacterial shapes = Round (coccus), rod like (bacillus), and spiral (spirochete)
Bacterial nucleus = Not surrounded by cell membrane
Bacterial ribosome =305, 50S, and 70S
Cell membrane = consist of cytochrome and lipids and enzymes
Mesosomes =convoluted invagination of mitochondria.
_. Plasmid (bacterial resistant): Closed circular extra chromosomal DNA
Endospore = Metabolically inactive cell. Contain calcium dipicolinate to seyer
environmental conditions)
External layer =Capsule (resistant to phagocytosis)
Cell wall =Portion external to cell membrane, Osmotic protection
Peptidoglycan =Present in cell membrane of Gram ':"'ve & +ve
Mucopeptide = (protein + carbohydra,te)" is a peptidoglycan
Techoic acid =Water-soluble polymer, Present In gram +ve only
Periplasmic space = Found in gram +ve cell, between cell membrane and outer cell
membrane contains proteins
Outer membrane;; Present in Gram -ve, Phospholipid layer, embedded proteins/porins
Lipopolysaccharide =Present in Gram -ve, consist of lipid A, also known as endotoxin.
Glycocalyx = Present in Slime layer, Adhesive
Appendages =Flagella, Pili/Fimbr:iae, ordinary pili or sex pili.
Bacterial growth curve lag 7 increase in individual size (many nutrient)
Exponential or log 7increase in population ._
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Stationary -7 division = death (accumulate toxin, decrease in nutrient)
15-1
Fungi
Cell membrane contain ergosterol layer
Protozoa
Protozoa are unicellular or single cell organisms and classified based on flagellates
;' Atypical'bacte.ria
I
Mycoplasma: Have no cell wall
Rickettsia: Can be transmitted by ticks, mites etc.
Chlamydia: lack ATP synthesis
. Mycobacteria
Cell membrane contain mycolic acid layer.,)/
Acid-fast test detect mycobacteria

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www.PhannacyPrep.com Microbiology

H2GZ, act as bactericidal
Superoxide dismutase: Enzyme to neutralizes peroxide like hydrogen peroxide (H
Z
0
2
).
Obligate anaerobe: has no superoxide dismutase
J'Facu"lta1ive.anaer.obe;,Most pathogenic bacteria, can shift from fermentative to
respiratory metabolism
Aerotolerant anaerobes; Similar to facultative, remains fermentative
Capnophilic anaerobes: Require CO
2
example: bocteroidjragilis (gram -ve anaerobe)
Oxygen requirement
Obligate aerobe: Generate H
2
0
Z
, it is bactericidal. Super oxide dismutase enzyme
neutralizes HzO
z
Obligate anaerobe: No super oxide dismutase, killed by Oz-
Facultative anaerobe: Most pathogenic bacteria, can shift from fermentative to
respiratory metabolism
Aerotolerant anaerobe; Similar to facultative to remains fermentative
No cell membrane and consist of DNA or RNA and proteins
Some viruses have single strand of DNA
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Gram -ve
CapSllle
..
,oOteT membrane
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Grai'n+ve
Techoic acid
Virus

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Gram +ve
Stain blue or purple Stain red or rose pink
Gram -ve
Microhiology
Techoic acid (LPS) in outer membrane
Peptidoglycan layer is thick . layer is thin
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. ...".pr"""o=-:a"u'tt.,....: '''''''---:-',,,-;-'---:--------1
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Exoto,xin is (heat sensitive) Endotoxin is more toxic than exotoxin, destroyed at higher
destroyed at'a temper.ature over 60C temperatures.
Exotoxin is a high molecular weight protein. Endotoxin a complex structure made up of phospholipid,
polysaccharides and protein
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GRAM +ve and aerobiC bacteria
Gram +
Streptococcus (in short Strep)
S. pyogenes (Group,AJ
S. agalactiae (Group B)
S. bovis (Group D)
S. pneumoniae )
S. vjrida1;ls l Te.dt I -$ ""11
Staphylococcus (in short Staph)
S. aureus
S. saprophyticus
S. epidermidis
Enterococcus
Gram +ve bacilli
Cyanobacteria diphtheriae
Listeria monocytogenes
Bacillus cereus
Nocardia
GRAM +VE and Anaerobic bacteria
Clostridium
C. pe!fringens , I on '-'
C. tetani >
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C. difficile I
C. botulinum 1.0_
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GRAM -ve and aerobic bacteria
Grall) -ve cocci
NISSERJA
W{.:.'
'.i-"H'I
lV. meningitis
Moraxella catarhaUs
Gram -ve bacilli (rods)
;z:;. , , .1,. .' '. "f'" k ' l;l
'r..SCl}etl' 'nw'cv' rIL."cv I;
Klebsiella pneumoniae
Enterobacter spp.
Shigella
Proteus mirabilis
Salmonella
S. typhi
S. enteritidis
Vibrio..c;hoIerqe
aeruginosa
Paste-Jrella milltocida
H. influenza
H duceryl
Legio;,-ella pneumophila
Yersinia
Y. enterococolitica
Y. pestis
GRAM-VE and Anaerobic bacteria
Fusbbacterium

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15-3

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Bacteria
Gram we Cocci
Found on the skin and in the nose
Boils,
Staphylococcus oureus Septicaemiae
Penicillin G and Penicillin V
Catalase and coagulase positive Food poisoning
Wound infections
Toxic shock syndrome (TSS)
Beta-hemolytic streptococci eg
Tonsillitis. darithromycin
Strep pyogenes (Group A Strep:
Cellulite!>, scarlet fever, Erythromycin
SeP.ticaemiae may cause immunemediated Azithromycin
GAS)
disease le.1! rheumatic fever) Penicillin G
Amoxicillin acute otitis
Alpha-hemolytic
Pneumonia {CAPI. media
Otitis media, Penjcillin G
Streptococcus pneumoniae
Meningitis Clarithromycin
AZithromycin
Alphahemolytic Endocarditis,
Amoxicillin, Penicillin G
Streptococci viridons Dental caries
Instrument contamination
S. epidermidis Catheter infections
UTI
Gram +ve bacilli
Diphtheria (disease due to toxin
Erythromycin or penicillins
Corynebacterium diphtherioe (to eliminate carrier state)
production)
Tetracvcline
Clostridia sp.
a. reroni,
Metronidazole, or
a. perfn'ngens,
,
Gas-gangrene,
vancomycin
CI. botulinum Botulism
,
CI. difficile Pseudomembranous coliris
Gram coed ,
Neisseria meningirides
Meningococcal meningitis +/- shock
Penicillin G
commensal of unper resniratory tract
Gonorrhea (S1O)
Cephalosporins 2 and 3
Neisseria gonorrheae generations or
Always pathogenic
Ciprofloxacin
:Gram!.ve bacilli
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Urinary tract infections (90%),
E. coli (UTI); sulfa drugs ,
,
E. coli
.
diarrhea
-
(cotrimoxazo]e)
Proteus sp. Wound infection,
E. coli (diarrhea)-
Klebsiella sp sepsis
Ciprofloxacin
Normal inhabitants of the gut
Enteric fever (typhoid), food poisoning
S. typhi Most sp. are animal pathogens (eg; eggs Chloramphenicol (typhoid)
Salmonella sp etc)
.
Ciprofloxacin
S. typhi infects man only, causes typhoid
S"hinellas;:;, . D"sentery (blood" diarrhea or shipellosis) CihrolJoxacin
Pseudomonas aeruginosa
Nosocomial (hospital acquired) and Aminoglycosides Ampicillin,
opportunist infections (most common S. Ceftazidime
)
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aureus)
Clarithromycin
Haemophilus influenzae
Pneumonia, meningitis, Azithromycin
Otitis media Ampicillin, amoxicillin
Tetracycline
Acid-fast bacilli
Isoniazid
Tuberculosis Rifampicin
Mycobacterium tuberculosis The most common cause of infectious Streptomycin
death world-wide Ethambutol
Pyrazinamide
Mycobacterium leprae Leprosy
Dapsone
Rifampicin
Spirochaetes
Treponema pa/lidum Syphilis
Penicillin G
Doxycycline

Borrelia burgdorferi TIck born infection causing, rash, arthralgia Tetracycline
,
and neurological signs. (Bull eye rash)
Have thick, ergosterol containing cell walls
Fungi and grow in humans as budding yeast cells
and slender tubes (hyphae).
Thrush, mucocutaneous infection,
Nystatin
Candida albicans (yeast)
vulvovaginitis
Clotrimazole
Miconazole
Clotrimazole
Tinea pedis Athlete's foot Tolnaftate (topical)
Sporotrichosis or granulomas Abscesses (puss)
Skin, nail and hair
Dermatophytes Ringworm infections, sometimes
acquired from animals.
Aspergillus sp. Allergic reactions, opportunistic infections
Ubiquitous airborne
filamentous fungus
Cryptococcus neoformans Meningitis in immunocompromised
Present in soil and pigeon
droppings
Protozoa
Malaria
Chloroquine
Plasmodia sp Four sp. infect man via biting female
Mefloquine
Primaquine
anaphlex mosquito
Doxycycline
Giardia lamblia
Low grade gastrointestinal disease:
Metronidazole
giardiasis
Entamoeba histolytica Amoebic dysentery
Metronidazole
and (are infective when swallowed; travelers
Ciprofloxacin
Giardia lamblia (intestinal diarrhea) Severe, may invade and spread to
Cotrirnoxazole
protozoa)" the liver
Viruses
DNA viruses
Adenoviruses
Conjunctivitis,
Sore throat
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HSV-l and HSV-2 can cause oral and genital
Herpesviruses
lesions.
H5V-l causes cold sores and
Acyclovir
Herpes simplex virus
Keratoconjunctivitis.
Famcidovir
Herpes zoster Foscarnet
Cytomegalovirus (CMV)
VZV can cause (Varicella: chickenpox,
Ganciclovir
Epstein.Bar IEB virus) (HHV-6)
zoster: Shingles),
Glandular fever,
Roseola infantum (sixth disease)
Hepatitis B
Hepadnavirus: Hepatitis 8 Transmitted via blood and body fluids and Interferon alpha
sexual contact
Parvovirus: parvovirus B
I
,
Slapped cheek disease, (fifth disease,
Can cause crises
erythema infectious)
Implicated in cancer of the
cervix
Papovaviruses: papillomavirus,
W.'"
Ubiquitous viruses'may
Polvomavirus Hemorrhagic cystitis cause disease in transplant
patients.
Gardasil
Poxviruses: Molluscum contal1:iosum. Smallpox
RNA viruses
Amantadine. Ribavirin,
Orthomyxoviruses:
Rimantadine {influenza Al
Influenza (flu) Neuroaminidase inhibitors:
Influenza A and B
Oseltamavir (A and BJ
Zanamavir (A and B)
Flaviviruses: Yellow fever, Hepatitis Yellow fever, chronic hepatitis
C
Paramyxoviruses: parainfluenza, Respiratory infections: Croup
RSV Measles, May be se....ere in infants
Measles Mumps Mumps
Picomaviruses: Enteroviruses (eg Meningitis.
-
poliovirus), rhinoviruses. Common cold- (rhinovirusesl Rhino has runny nose
Hepatitis A Hepatitis
Reoviruses: rotavirus Gastroenteritis
AIDS NRTl
Retroviruses: HIV-l. 2
T-eellleukemia, NNRTI
HTlV I, II
Spastic paraparesis Protease in hibitors
Rhabdoviruses: rabies Rabies Zoonotic infection
Togaviruses: Rubella, German measles (Rubella).
Alpha viruses Encephalitis
.
Eye infections
I Eye Infections
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Blepharitis Hordeola
I
IConjunctivitis
I
IKetatitis
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15-6
Microbiology
Hordeola (External hordeolu 'stye') or (Internal hordeolum "acute meibomianitis)
,.
Causative agent S. aureus
" .
Site of infection At the edge ofthe eyelid or underneath it. Head and it ruptures
spontaneously within days
Treatment Warm compresses + oral antistaphylococcal agent
E.g. cloxacillin or flucloxacillin.
Comments Incision and !irainage indicated and patient should be referred to
an ophthalmologist if the patient does not respond to the treatment
above.
Conjunctivitis (pink eye or red eye)
Causative agent (Viral, bacterial, chlamydial) & (noninfectious: allergy, foreign
body).
Treatment Chlamydial disease in adults:
Oral tetracycline (Doxycycline 100mg 12 hourly) or
Erythromycin (Safe in pregnancy) (500mg 6 hourly) for 7 days, or
Azithromycin (safe in pregnancy) Ig PO as a single dose
Amoxicillin (safe in pregnancy)
Gonococcal conjunctivitis in adults:
Ceftriaxone Ig 1M as a single dose
Comments Purulent or mucopurulent discharge suggest a bacterial or
chlamydial cause
SIS Watery discharge may be associated with upper respiratory
inflection or adenovirus
Hallmarks of viral conjunctivitis are follicular.reaction and
preauricular lymphadenopathy
Viral conjunctivitis ("pink-eye")
Treatment Treatment is supportive
Topical corticosteroid therapy is controversial.
Comments Children are generally kept out of school for up to 2 weeks after the
onset of the infection
Bacterial Conjunctivitis
Causative agent Staphylococcus and/or Streptococcus for
Haemophilus influenza more common in children
Treatment Alternative agents include or Tobramycin eye drops
(adults), and ointment (for children), or Fusidic acid eyedrops
Conjunctivitis in newborn (Ophthalmic neonatum)
Causative agent Chlamydia trachomatis or Nisseria
Treatment Chlamydia trachomatis: Erythromycin syrup (40 to "50 mg/kg/day)
in 3 divided doses for 14 days. If needed treat parents for genital
15-7
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Microbiology'
infection
Nisseria gonorrheae: Ceftriaxone 25 to 50mglkg.lM as a single
dose. If needed treat oarenls for 2cnital infection
Comments The best fonn of prophylaxis is 2.5% aqueous povidone.iodine
solution.
Canaliculitis
Causative agent Actinomyces, and rarely propiobacterium, nocardia or bacteroids
Treatment Mechanical expression orlhe exudative or granular material from
canaliculi, combined with probing and irrigation ofthe
nasolacrimal system with penicillin G (100,000 V/ml) eye drop
solution.
Comments Patients should be referred to an ophthalmologist for definitive
treatment
15-8
Ear Nose and Throat Infections'
Dacrocystitis
Causative agent Streptococci including S pneumoniae or S. aureus hut culture
should vuide definitive theraov
Site of infection Infection of nasolacrimal sac
Treatment Acute infection:
Oral amoxicillinc1avulanate or cefuroxime
Chronic infections:
Irrigate the outflow tract with an antibiotic solution such as
penicillin G (100,000 Vlml) as a temporary measure.
Definitive surgical decompression ultimately rests with the
ophlhalmologist
Keratitis
Causative aRent Bacteria, u n ~ i Hernes simnlex virus, acanthamoeba
Site of infection Infection of the cornea
Comments It is a sight-threatening ocular emergency and requires prompt
recolmition and immediately referral to an oohthalmoloe.ist
, ,
-
Causative aRent
Common cold Viruses: E.g. Rhinoviruses
I (acute rhinitis)
Herpes simplex keratitis (Viral)
Causative ae.ent Heroes simolex IHSY-Il
Treatment Epithelial disease: Topical antiviral agents E.g. acyclovir ointment
.
applied t6 eye 5x/day, continued for at least 3 days after healing.
trifluridine (viroptic) and idoxuridine (Hcrplex-D) ophthalmic
drops
Stromal disease: Complex-combination ofantiviral therapy and
tonical corticosteroids
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Sinusitis Bacteria: E.g. Streptococcus pneumoniae
.
Pharyngitis Viruses: Eg. Adenovirus
(sore throat) Bacteria: S. pyOf!enes
.
Acute bronchitis Viruses:, E.g. Myxovirus'es
Chronic bronchitis Bacteria: E.g. H influenza
Pneumonia Bacteria: E.g. S. pneumoniae
Otitis media Bacteria: S. pneumoniae, H influenza, M catarrhalis
(middle ear int)
Skin and SoB: Tissue Infections
Bacterial skin infections
Erysipelas
Normal skin
flora
Gram (-) ve and Staphylococcus viridans, Streptococcus diphteroid
Propionobacterium, actinobacter and yeast.
Normal person carry 10
12
bacteria on the skin, including
Staphylococcus epidermidis and Propionibacterium acnes
Cellulitis
An acute spreading infection ofthe dermis, Lesion is hOI, usually
red and swollen.
Causative agent Strep. and/or Staphylococcus aureus
Site of infection Dermis, " .
Treatment. A combination of penicillin and Flucloxacilllin
Impetigo
agent/s Streptococcus pyogenes (hemolytic group A Strep) and/or Staph
aureus andpresents as bullous, crusted or pustular eruption ofthe
skin
Site of infection Epidermis layer due to local invasion of causative agent
Treatment PenicillinlAmoxicillin with or without Flucloxacillin
Follculitis, boil (funincles) and carbuncles
Causative agent S. aureus
Site of infection Invasion'ofS. aureus in the hair follicles causing, minor abscess
Treatment Penicillins or Amoxicillin
elas
the skin (dermis
15-9
, ,
Microbiology
fSk" b VIRUSES
I "
It has weeI-defined spreading erythematous inflammation, usually
accomoanied bv fever and other sYstemic manifestatiori
Causative 3QCntls Strentococcus PYOl?,encs. Occasionally S. aureus
Site of infection Dennis of the face
Treatment Penicillin or Amoxil, wilh or without Flucoxacillin as S. aureus
may occasionallv be the causative agent
Necrolising fasciitis
Is an inflammatory response to in/eelion a/the tissue below the
dermis, spreading with alarming rapidity along the facial planes
causing disruption a/the blood supply hence necrosis and
I flOnf!rene
"
Causative agent/s Streptococcus pyogenes (B-haemolytic group A Strep)
Micro aerophilic Streptococci with anaerobic bacteria
Site of infection Soft tissue below the dermis
Treatment Benzyl penicillin, and c1indamycin with or without Metronidazole,
in addition to 'tissue debridment
Foumier's gangrene
A form ofnecrotisingfascUtis occurring around the groin area
Diabetes and local trauma are the main oredisDOsing factors
Causative ae:ent/s Colifonn (E. coli), Strentococci (GrouD A Stren)
Treatment Penicillin and Cephalosporins if allergic, beta lactams Quinolones
I (ciDronoxacin)
Comments Pain, fever, and systemic toxicity are usually prominent factor of
the disease
Signs ofgas formation and gangrene may also be seen
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Causative Of!ent Disease and Characteristics
Panilloma virus Common wart
Molluscum contagiosum Fleshy papule
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Pox virus from sheep, goats Paplovascular lesions, or skin lesions with systemic spread
such as heroes simplex (vesicular lesions)
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Dermatophyte (keratin- Ring wonn or skin lesions can be part ofsystemic
loving fungi) manifestation of the disease such as Cryptococcus
neoformans and Blastomyces dermatitidis
Tinea pedis Athlete's foot treatment: Clotrimazole. miconolole,
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IBaclerial Meningitis IDisease and characteristics
15-10
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www.PharmacyPrep.com Microbiology
(Neonatal- 6 weeks) Group B Strep Empirical treatment: Ampicillin+ Gentamicin or
E..coli; and other
."
Ampicilin +Cefatriaxone "
Children (>3 months) and adults:
Empirical treatment: Cefatriaxone or ampicillin or
S. pneumonia, N. meningitis vancomycm
H. influenza type B (can be
prevented by vaccmation)
..
Elderly (>50 yrs), alcoholics,
Empirical treatment: Cefatriaxone or ampicilin or
irnmunocompromised, head vancomycin
injuries: E. coli, S. pneumonia, L.

Meningococcal Infection: Spread by respiratory route, pharyngeal
Neisseria colonization in 5-10% of population
Haemophilus influenza type B
Affects 6months - 5year old children (can be
prevented by Rib vaccine).
Spread respiratory route'
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Pneumococcus
Elderly patients: - pneumonia, immunosuppressed,
haematological malignancy .
Very young 3 months): Head injury with skull
fracture. mortality (up to 30%)
Encephalitis
Virus infection of brain and CNS cells.
HSV-I (most common), CMV, rabies, mumps,
measles, eschovirus, coxsackievirus
Polio
Enterovirus, faecal-oral spread; 90-95% well; 5%
viral 1% paralytic polio destroys motor
neurons of anterior lumen
Brain abscess
. Streptococcus; Staphyl9coccus;
Haematogenous
Direct"spread from middle ear, sinuses or mastoid
Usually mixed infection = anaerobes +
streptococcus + haemophilus, coliform
TB
Causative MeninJ!ococcus; Pneumococcus; H irifluefl?ae
Site of infection CNS
Treatment Meningococcus: benzyl penicillin
Pneumococcus: benzyl penicilliri/cefotaxime or vancomycin if
resistant
H influenzae - cefotaxime (start with penicillin and cefotaxime)
Prophylaxis: meningococcus - Rifampicin or ciprofloxacin (whole
familyJclose contacts)
.Respiratory mfections:
Community acquired pneumonia
Causative agent Is. pneumonia (most common)
15-11
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Bronchitis
Viral Bronchitis f.rio1ogy based on age group
(95%) <I year: RSV (respiratory Syncytial Virus), Parainfluenza, Corona
ViruS
1-IOyo: Parainnuenza, Enelrovirus RSY
>10 years: lnnuenza. RSV, Adenovirus
Bacterial Chlamydia pneumoniae, Mycoplasma pneumoniae
Bronchitis
Treatment: Routine antibiotic treatment is not recommended
Antipyretidanalgesic: Acetaminophen
Antitussives: Dextromethorphan
Beta-aRonist: Salbutamol
Ambulatory patients 18 to 40 YT Requirin,g hospital admission
Mycoplasma pneumonia (2;4%) S. (17%)
S. pneumonia (5%) Mycoplasma pneumonia (14%).
Chlamydia pneumonia t2%) Chlamydia pneumonia (10%)
H. influenza (1%) H influenza (7%)
Lepionella Dneumophilia (I %) L. oneumoDhilia (1 %)
Treatment Emergency treatment for pneumonia: Pencillin V
S. pneumonia: Penicillin G, Amoxicillin or Macrolide
High level resistant: Cefotaxime, ceftriaxone, po or iv
fluoroquinolones
H influenza: 2"" and 3
ru
generation cephalosporins or amoxicillin +
c1avalunate
Staphylococcus aureus: .
Methicillin susceptible - - - Cloxacillin
Methicillin resistant - - - - - Vancomycin
M pneumonia & C. pneumonia: Doxycycline or Macrolide
LegioneUa sp.: Fluoroquinolones. macrolide +rifampin
E. coli (aerobic gram -ve bacilli) and proteous sp.: 2
00
and 3
fU
Gen
cephalosporins (initial therapy should he with Cefoxitin or
I oioeracillin + tazobactam)
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I Lower UTI I Upper UTI I
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Urrnary Tract lnfectlon
15-12
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1 1 Pyelonephritis
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Urinary Tract Infection
Causative agent
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The most common E. coli
~ y t t Cotrimoxazole, or amoxicillin. !fineffective or allergic use
Ciprbf]oxacin
Urethritis Acute urethral syndrome (urea plaSma and chlamydia infection):
DoxycyClin; During pregnancy used Erythromycin
Pyelonephritis Bacterial infection of kidney substances
Ampicillin, cephalosporins, cotrimoxazole or aminoglycosides '
Sexually Transmitted Infections
Causative agents Nisseria gonorrhea
Syphilis
Chlamydia
Lymphogranuloma
Trichomoniasis: vaginitis (colored discharge)
.
Bacterial vagiriosis: vaginitis (fishy smell)
AIDS
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Condylomata acuminate
Hepatitis B and C
Chancroid
Genital herpes
Genital warts
Candida or yeast (NOT STIs)
Comments Candida infections (vuTvo vaginitis) is not STI thereby sexual
partner does not require treatment.
Symptoms of candida infections are: white-curdy discharge.
If reoccur within 2 months, partner need treatment
Infections of the joint and bones
....-------------,
Joint and bones infections
Lyme disease
Infectious arthritis
Male/female The gonococcus bacteria may cause different'symptoms in women
differences than in men. Women may develop red sores on the hand feet, in
"
addition to severe pain in the wrist and ankles. In men, the
gonococcus will frequently attack only a single joint, most often the
knee.
Treatment Arthritis due to gonococcus can be treated with oral ampicillin.
Surgery is generally not necessary or particularly helpful
15-13
: }
Osteomyelitis
It is a bacterial infection of the bone and bone marrow
Causative Agent SwphylocOCCllS allrellS
Microbiology
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Food
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1'10 answers or tle tiPS rom t e 0 owmg ta e,
1. S. pneumonia 2. Chlamydia 3. Pselldomonas aeruginosa
/rachomalis
4. S. aureus 5. Treoonema vallidum 6. Corynebacterium
Lvme disease
A tick-borne infection can cause arthritis and, in severe cases, heart
and/or CNS complications.
Causative agent Spirochete (Borelia burgdorfen) is transmitted to humans via deer
tick (3 tiny insect found not only in deer but in squirrels, rabbits,
other rodents, birds, and household vets)
Comment Prevalent durinR July to August
Gastroinlestinallnfection
Nonnal person carry 10 bacteria in his GI tract, 95 to 100010 of
which are anaerobic. The gut has a resident bacterial population -
nonnal
Stomach Infection with Helicobacter pylori is common and is associated
with DCotic ulcer disease and eastric cancer.
The large intestine These are predominantly anaerobes (99.9%) and an apparent
nee:lie:ible 0.1 %l ofaerobes.
Anaerobes Bacteriosides, Bifidobacterium, Clostridium, anaerobic cocci
Aerobes Enterobacteriaceae, E. coli, Klebsiella, Proteus, Enterococci.
.
IOOlsonlng
Bacteria Poisoning
Shigella Dvsenterv (traveler's diarrheal
Campvlobaeter ieiuni Traveler's diarrhea
Salmonella Eggs, ooultrv. meat
,
ClostridiulIl difficile Pseudomembranous colitis
E.scherichia coli Meat food ooisonine: and traveler's diarrhea
S. aurells Meat, mayonnaise. custard
Clostridium oerfrinpells Acute gastroenteritis, reheated dishes
Non',lalk virus Diarrhea in hosoitalized oatient
Entomoeba Amoebiasis
Bacillus cereus rB. cereus) Reheated rice (Be Seriolls!!!)
Vibrio parahaemolyticus Contaminated sea food
Listeria Meat
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7. E.coli 8. H pylori 9. Borrelia
10. Haemophilus 11 M catarhalis 12. Group BStrep
influenza
13. Herpes simplex 14. Cytomegalovirus 15. Rubella
virus
16. Heroes zoster 17 Influenza A& B 18. N. meninJ!iLis
19. Eptein barr 20 21. Compylobacter !eiuni
E. coli is classified as? -7 -Ve. C A A/J2. )
Beta hemolytic bacteria example is? -7 sJM-f' f
. Toxic shock syndrome is caused by? -7.$. (. U.Ii! 1" f6rJ)
Lyme disease is caused? -7
Techoic acid is present in? -7
Encephalitis is? -7 bf'U ,+fi' -- 4J IJ{ -
Chlamydia neonatrum (c. trachomatis) is? -7
Non gonococcal infections that cause UTI are?
Diphtheria is caused by? -7
Syphilis is caused by? -7
Antrax is caused by? -7 S. a WIU.tA./
What bacteria catalase degrades H
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Examples of live attenuated vaccines? ('f) f"/\ .J !5t!.&/ffP.
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Viral diarrhea is caused by -7
The most common cause of community acquired pneumonia ( S
The most common cause of subacute endocarditis (
The causative organism of syphilis (
The causative organism of Iyme disease (
Tick born infection (Iyme disease)
The causative organism of bacterial diarrhea (
The causative organism of otitis externa ( )
The most common pathogen isolated from middle ear (
Infection when aspiration of ear is performed. ( rn I v-.b-
The most common cause of bacterial meningitis ( H
The most common cause of encephalifis ( mV )
J'. Example of gram +ve bacilli ( c
The causative organism of sinusitis ( 5
The causative organism of nosocomial (hospital) infections (
A types of herpes virus include,( H:!V j I rlJ V2) '" )
Causative organism of shingles ( 1r!v..-p.(.A,.- zk.:!)gI'v
Causative organism of seasonal flu ( IJ. )(.l1.
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15-15
Cell and Molecular Biology
C'O I" . (
Questions Alerts!
Nucleic acids DNA and RNA bases, nucleotide (phosphate, sugar and base)
Complimentary pair (A - T and C- G)
Transcription and translation in protein synthesis
DNA recombination methods and plasmid
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ThIS chapter reviews basics of chromosomes. gene, nucleic acids, DNA structure and functions, replication,
mutations and recombination. RNA structure and functions, transcription from DNA and translation to
synthesize proteins. Also review topics such as recent development of gene cloning and genetic engineering.
Fig 16.1
16-1
www.PhannacyPrep.Com Cell and Molecular Biology,
Prokaryotic Eukaryotic
Primitive nucleus (no nuclear membrane) Have nucleus
large single DNA molecule Animal: no cell wall but cell membrane
Contain cell waif (rigid): covalently bonded short chains of No chloroplast
amino acids. mitochondria
cell wall contain murein (polysaccharide chain) yes cell wall
Yes chloroplast
NO-7 mitochondria (cell membrane)
Present in bacteria Present in: Animal, plant, fungi, parasites, algae,
and orotOloa
Bacteria are reproduced by type of cell division called
binary fission.
Cell organs composes of a number of tissues, and each tissue composes of cells of the same
type. The individual cell is the minimal self-reproducing unit in all living species. It performs
two type of functions, l.Performs chemical reactions necessary to maintain our life
2.Passes the information for maintaining life to the next generation.
Since the cell is the vehicle for transmission of the genetic information in all living species, it
needs to store the genetic information in the form of double-stranded DNA.
The cell replicates its information by separating the paired DNA strands and using each as a
template for polymerization to make a new DNA strand with a complementary sequence of
nucleot/des. The same strategy is used to transcribe portions of the information from DNA
into molecules of the closely related polymer, RNA. The RNA is the intermediate between
DNA and protein and it guides the synthesis of protein molecules by the complex machinery
of translation, i.e. the ribosome. The resultant proteins are the main catalysts for almost all
the chemical reactions in the cell. In addition to catalyst, proteins are performing also building
block, transportation, signalling, etc.
Cell Organs
Endoplasmic reticulum (ERJ: It is a series of membranes extending throughout the cytoplasm
of eukaryotic cells.
Cytochrome P4S0 present in ER
Rough endoplasmic in protein synthesis
Smooth endoplasmic Helps in lipid synthesis
Does not contain ribosome.
Golgi body (Goigi apparatus): Series of flattened sacs.
Synthesize the cell's proteins and lipids.
lysosomes: Drop like sac of enzymes in the cytoplasm. Help digestion within cells.
Mitochondria: (power house of the cell).
It releases energy in the form of ATP.
16-2
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Chromosomes
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Ceil and Molecular Biology-
Human Chromosomes
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16.-3
Chloroplast (chlorophyll): It is normally present in green plants.. Its principal function is to
absorb energy from the sun.
Vacuoles:
They are big, fluid like structures, and may occupy more than 75% of the plant cells.
Store nutrients as well as toxic wastes.
Flagella: It exists as single and it helps bacteria to move.
Cilia: It exists as numerous and it helps bacteria to move.
Genome, Chromosome, and Gene
Genome: The genome of an organism is its complete set of DNA. All the" genetic
information in an organism is referred colleetiv.ely as a "genome".
Chromosome Structure
Chromosome: The 3 billion bases of the human genome are not all in one continuous strand
of
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a
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Diploid
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Haploid
chromosome
DNA. Rather, the human genome is divided into 23 separate pairs of DNA, called
chromosomes. Chromosomes are structures within the
cell nucleus that carries genes. A chromosome contains
continuous molecule of DNA which is wrapped around
histones. Human has 22 pairs of autosomes and 1 pair of
chromosome, hence make up to 23 pairs of
chromosomes. Autosomes are non-sex determining
chromosomes, while sex chromosomes are Xand Y
chromosome. Male will have XY sex chromosomes,
whereas female will carry XX sex chromosomes. The
collection of chromosomes in an individual is called karyotype. For example, the typical male
karyotype has 22 pairs of autosomes, Xand ..

Gene Expression. O' -
A gene is a DNA sequence that encodes a protein or an RNA molecule. Each
chromosome contains many genes, i.e. the basic physical and functional units of
heredity. Each gene exist in the particular position of particular chromosome. In
human genome, it is expected that there are 30,000 to 35,000 genes. In prokary-
otic genome, one gene is corresponding to one protein. Whereas, in eukaryotic
genome, one gene can corresponds to more than one protein because of the process
called as "alternative splicing".
Plasmid: extrachromosal substance of DNA. Plasmids are often used for DNA recombination
and cloning.
Nucleotide structure: Consist of 3 units that is base, sugar and phosphate
Nucleic acid (DNA and RNA): Nucleotides are the building blocks of all nucleic acid molecules
(such as DNA and RNA). These structural units consist of three essential components, i.e.
A pentose sugar; deoxyribose (in DNA) and ribose (in RNA)
Phosphate (bound to the 5' carbon)
Base (bound to the l' carbon); nitrogenous base
For the structure of nucleotides (in DNA),
, Forms of Nucleotides
Nucleotides can have 1, 2, or 3 phosphate groups. Monophosphate nucleotides
have only 1 phosphate, which are the building blocks of ':!u-:
nucleotides have 2 phosphate groups and triphosphate have 3 phosphate
groups, which are used to transport energy in the cell.
There are two chemically different nucleic acids: Deoxyribosenucleic acid (DNA) and
Ribonucleic acid (RNA).
16-4
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What are incorrect
complimentary pair?
Ribose
Nitrogen Bases I
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Purine Bases
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IPyrimidine Bases
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Adenine (A) Cytosine (C)
CUTPy
Guanine (G) Uracil (U)
Thymine (T)
RNA
Adenine (A)
Question Alert!
Cytosine (C)
Guanine (G)
,
What bases are not
Uracil (U)
present in DNA?
Single stranded
Purine can form 2 hydrogen bonds
Pyrimidine can form 1 hydrogen bond
DNA
Pure As Gold
Adenine (A)
Cytosine (C)
Guanine (G)
Thymine (T)
Double stranded
2Deoxyribose
Pairs of purine with pyrimidines formed by hydrogen bonds. When strands base pair, they are
said to be complementary.
A pairs with T (2 hydrogen bonds)
G pairs with C(3 hydrogen bonds)
A pairs with U(DNA - RNA hybrid)
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Mutations: If complimentary pair incorrectly compliments other than A to T and Gto Ccan
result into mutations. There are 3 possible mutations like purine to purine, pyrimidin.e to
pyrimidine and purine to pyrimidine.
Deoxyribonucleic acid (DNA): The molecule that carries the genetic information for most living
systems. DNA is present in chromosomes of eukaryotic organisms, mitochondria, chloroplast
of plants. Prokaryotes are single-celled organisms with no nuclei (e.g. bacteria). They have no
distinct
nuclear compartment to house their DNA and therefore the DNA swims within
the cells. Eukaryotes, on the other hand, are organisms whose cells contain a
nucleus surrounded by cytoplasm which is contained within a plasma membrane.
The DNA locates within the nucleus. Eukaryotes are organisms with single or
multiple cells, for example, plant and animal.
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Prokaryotic organism, which does not have nucleus but contain single chromosome. The DNA
is present in single chromosome of prokaryotic organism.
Structure of DNA: Double helix; A term often used to describe the configuration of the DNA
molecule. The helix consists of two spiralling strands of nucleotides (a sugar, phosphate and
base) joined crosswise by specific paring of the bases and 3,S-phosphodiester bonds.
Some viruses contain single stranded DNA.
There are proteins associated with DNA present in eukaryotic nucleus, these proteins referred
as nudeoproteins. In prokaryotic this protein present in DNA complex present in neucleoid
The DNA molecule consists; Four bases: Adenine (A), Cytosine (C), Guanine (G), Thymine (T)
A sugar-phosphate backbone, arranged in two connected strands to form a double helix.
Complementary DNA (eDNA): DNA synthesized from a messenger RNA rather than from a
DNA template. This-type of DNA is used for cloning or as a DNA probes for locating specific
genes in DNA hybridization studies.
Ribonucleic acid R N A ~ Nucleotide structure for RNA. Similar to the n.ucleotide of DNA, the
nucleotide for RNA also has Phosphate and Base. The only difference is that the nucleotide
here has Ribose Sugar, instead of deoxyribose in the DNA nucleotide. The Ribose has an extra
OH group at 2', which is different from the Hgroup at the same place of deoxyribose. That's
why we call these two different things "ribonucleic Acid" and "deoxyribonucleicAcid" one is
with the OH group, which contains the "0" molecule, yet the other one without.
RNA Polymerases: Theses enzyme helps in synthesis of: rRNA, tRNA and mRNA
There are 3 types of types of RNA based on their functions:
rRNA: (Ribosomal RNA), normally synthesize ribosome 80% of total RNA. The rRNA is
present in ribosome in cell.
tRNA: (Transfer RNA), 15% of total RNA. Each tRNA amino acid carries the specific amino
acid to the site of protein synthesis. Each tRNA molecule contain anticodon that generally
recognizes all the codons on mRNA
mRNA: (Messenger RNA), 5% of total RNA. mRNA carries the genetic information from
DNA to cytosol for protein synthesis
Codon
The codon are present in the messenger RNA (mRNA): They are: Adenine (At Guanine (G),
Cytosine (C), Uracil (U). These four nucleotide bases produce three base codons. There are
64 different combinations of these bases. Sixty one of 64 codons normally produce 20
common amino acids. However, there are 3 codons UAG, UGA and UAA, do not produce
amino acids.
The follOWing codons do not code for amino acids, they are known as stop, nonsense or
termination codons. When one of the codons appears the synthesis of peptide chain is
stopped.
16-6
-
16-7
Post-translational Modificati()ll
; (including g1ywsylation,
pllosphOlylation, and
sulfatalion.
Protein
What comes first?
is present on? t '-R
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e -7 Protein synthesis
Important concept!
Translation
Occurs in the cytoplasm at
the ribosome and involves
rRNA and !RNA
Transcription
DNA ----------------------7 mRNA
Step 1: Transcription -) DNA -7 mRNA
Step 2: Translation -7 mRNA -7 tRNA
Important concept!
DNA recombinant technology!
Gene transcription and translation process:
Transcription: This is first step in cell protein synthesis, during this process information from
DNA copied to m-RNA.
Translation: This is second step in cell protein synthesis. The protein synthesis occurs in
ribosome's. During translation information from m-RNA is brought to ribosome's by t-RNA.
This will determine the sequence of amino acids and protein synthesis.
lntrans and exons
The coding region of an eukaryote's gene is different from that of a prokaryote.
For Eukaryotes, each gene contains introns and exons. Intron is a segment of gene situated
between exons. It is not responsible for the coding of protein. So the introns will be ultimately
spliced out of the mRNA. And exon is a nucleotide sequence in DNA that carries the code for
the final mRNA molecule and thus defines the amino acid sequence during protein synthesis.
The process of removing the introns for the mRNA sequence is called RNA splicing. This
process is done with the help of spliceosomes. Though the Intrans seem "useless", it is quite
amazing that in eukaryotes, each gene can have many introns, and each intron may have
thousands of bases. Introns in eukaryotic genes normally satisfies the GT-AG rule, that is
intron begins with GT and ends with AG. Intrans can be very long.
Restriction Endonuclease Enzymes: Restriction enzymes or restriction endonuclease is a class
of enzymes. They are DNA-cutting enzymes, which recognize certain pojot:, called
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restriction site, in the double-stranded DNA with a specific pattern and break the
phosphodiester bonds between the nucleotides. Such process is called digestion". Naturally,
restriction enzymes are found and isolated from various bacterial species; which are used to
break foreign DNA to avoid infection or disable the function of the foreign DNA
There are two types of restrictive enzymes lyase and Iygase;
lyase; split the DNA on specific site
lygase; join the DNA on specific site
Plasmid
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Inserting a DNA Sample into a Plasmid
16-8
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Into Plasmid
Plasmid calTies the
DNA into the cellv
2. Insert the recombinant into the host cell (usually, E. coli). This makes use of a chemical
based transformed method, where the bacterial cells are made "competent" to take up
foreign DNA by treating with calcium ions. After the recombinant DNA molecules are mixed
with the bacteria cells, a brief heat shock is applied to facilitate uptake of DNA.
Cloning: Given'a piece of DNA X, the process of duplicating itjnto many pieces is
cloning. The basic steps involve:
1. Insert Xinto a p . vector ith antibiotic-resistance gene and a recombinant DNA
molecule is formed. Plasm and DNA fragments must have compatible RE ends for ligation
by T4 DNA ligase. A linear product of DNA and the linearized plasmid is firstly formed,
followed by the joining of the opposite ends to form a circular product.
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3. Grow the host cells in the presence of antibiotic. Note that only cells with antibiotic-
resistance gene can grow. Note that when we duplicate the host cell, X is also duplicated.
4. Select those cells contain both the antibiotic-resistance genes and the foreign DNA X. Some
cells only contains plasmid vector but without the foreign DNA due to unsuccessful ligation in
step 1. The cells with foreign DNA X can be correctly selected by the complementation of
beta-galactosidase, in which the correct colony will show blue colour.
5. Kill them and extract X.
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Genetic diseases: Hemophilia: ur--....... I.A...-l1 ' ..... -=q lJ
Hemophilia: This is a genetic disease often associated with X chromosome only;'Thus men
can hemophilic or no hemophilic, however there is no carrier in men.
Hemophilia causes slow blood dot formation.
There are two types of hemophilia, that is type A and B
16-9
www.PhannacyPrep.Com .Cell and Biology
Hemophilia type A is due to deficiency of clotting factor 8 (antihemophilic factor)
Hemophilia type Bis due to of clotting factor 9 ('Christmas factor)
lips
Select answers from the following table:
1. plasmid 2. Iygase 3. lyase
4. gene 5. transcri ption 6. nucleotides
7. Uracil 8. adenine 9. guanine
10. hemophilia 11. genome 12. Intron
13 A DNA sequence of
specific organism.
How many type of nucleic acid?
Building blocks of all nucleic acid molecules are the (
Purine bases ( )
Pyrimidine bases (
Base found only in RNA ( )
All the genetic information in an organism is referred collectively as...(
DNA sequence that encodes a protein or an RNA molecule is a (
This is the first step in cell protein synthesis ( ;-..."...
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A segment of gene situated between exons is ( I bI
Split the DNA on specific site (
Join the DNA on specific site ( I 'A
Small circular, extra chromosomal DNA molecule called....( r(4v-n\r .
This is a genetic disease often associated with Xchromosome only. ( I
Genome (DNA library), complete genetic information of one species
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What is plasmid, except? .s rncJ,L c IN . ...
What is genome? -7 fr'$)M P. or-
Select True/False Statements .sfa+
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,. Prokaryotes -7 Have cell membrane. (True/False)
Eukaryotic -7 animal cell have no cell wall (True/False)
Nucleotide -7 base + sugar + phosphate (True/False)
DNA bases -7 A, C, G and T (True/False)
RNA bases -7 A, C, G and U (True/False)
Complimentary bases -7 A-T, G-C or A-U (True/False)
Transcription is -7 DNA to mRNA (True/False)
Translation is -7 mRNA to tRNA (True/False)
cDNA is -7 complementary DNA that produced from mRNA (True/False)
16-10
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Anticodons present on tRNA (True/False)
The largest type of RNA? r-RNA (80%) (True/False)
The Smallest type of RNA? m-RNA (5%) (True/False)
Single strand DNA is present in? Some virus (True/False)
RNA polymerase I make? m-RNA (True/False)
Haploid -7 single chromosome (True/False)
Daploid -7 double chromosome (True/False)
DNA transferase catalyzes the transfer of various groups such as phosphate and
amino groups. (True/False)
DNA hydrolase's = hydrolyses various substances. (True/False)
DNA lyase =catalyzes the removal of various functional groups other than the process of
hydrolysis. (True/False)
DNA isomerase's = catalyzes various isomerisation's (True/False)
Reverse transcriptase found in some viruses, they are referred as retrovirus, is an RNA
dependent DNA polymerase. This enzyme requires an RNA template to direct the
synthesis of new DNA. Example: NRTI-Nucleoside reverse transcriptase inhibitors. NNRTI-
Non nucleoside reverse transcriptase inhibitors.
DNA synthesis by reverse transcriptase can be inhibited by AZT (zidovudine). (Anti HIV)
Retrovirus: Virus that contain reverse transcrjptase enzyme. Example. HIV utilizes this
enzyme to replicate their RNA genome. (True/False)
Hapten is a low molecular weight compounds that act as immunogens after chemically
complexing to a larger molecule or cell surface. (True/False)
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17
Pharmacogenetics
The pharmacogenomics is integration of pharmacology and genetics. The study of
pharmacogenomics allows to design and develop drugs that are customized to each person's
genetic mark up. The pharmacogenomics also utilized to study cytochrome enzymes that are
responsible for drug interactions.
To perform pharmacogenetics, the first step is detailed analysis of patient list of single
nucleotide polymorphism.
Single nucleotide polymorphism (SNP): occurs when one base pair of nucleotide replaces
another. A single base differences that exist between individual. This is the most common
genetic variation in DNA
Defective splicing: In which an internal polypeptide segment is abnormally removed, and the
ends of the remaining polypeptide are joined.
Biological drugs
I. Trastuzumab 2. use for breast cancer
3. Hirceptin 4. Used for breast cancer HER2 receptor
.
Tips
What is phannacogenetics -7 r ~
Phannacogenetics ~ ~ <f/i oLuo ~ H .fo ~ VGtLt .
Herceptin is used for -7
Trastuzumab >
The study which allows to design and develop drugs that are customized to each person's
genetic mark up ( )
References: Made especially for you: phannacogenomics and phannacy practice, CPJ. Jan
2008 vol. 14I,No.!
Copyright C 2000-2012 TlPS Inc. Unauthorized reproduction of this manual is strictly prohibited and it is 17-1
PharmaeyPrep.
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Immunology
Questions Alerts!
Immune cells response (B cell and TCellsJ
Immunoglobulin's (lgE asthma and anaphylactic reaction)
Mechanism of inflammation (bacterial infections neutrophil ~ viral infections
lymphocytes)
Types of hypersensitive reactions ( poison ivy, Hashimoto, Montaux test,
anaphylactic reactions)
Autoimmune diseases (ruce 10M. RA. SlE)
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THE ORGANS OF THE IMMUNE SYSTEM
The organs of the immune system are stationed throughout the body. They are known
as lymphoid organs because they are concerned with the growth, development, and
deployment of lymphocytes, white blood cells (WBC) that are key operatives of the
immune system.
LYMPH NODE: lymph nodes are small, bean-shaped structures that are laced
throughout the body along the lymphatic routes. lymph nodes contain specialized
compartments where immune cells congregate, and where they can encounter
antigens.
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CELLS OF THE IMMUNE SYSTEM
Question Alert!
,cey
Killer Cell
Precursor of RBC,
platelets?
Erythrocytes
(Red blood cells)
MonQcytes
Neutrophils
Basophils
Eosinophils
Antibody or (Ig)
Cytotoxic T'
Cell
Cells involved in the immune system
White blood cells (wEC) or leukocytes
a) polymorphonuclear leukocytes (granulocytes)
Neutrl?Phils
Eosinophils
Basophils.
b) Mononuclear leukocytes without granules in their cytoplasm
i) Monocyte
ii) Lymphocyte
i. T-lymphocyte
Helper T-cell
Cytotoxic T-cells
Suppressor T-cells
ii. B-Iymphocytes
iii. Natural killer cells
18-2
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Ncutrophils:
Most abundant WBC
Not only phagocytes but also granulocytes
Uses its prepackaged chemicals to degrade the microbes it ingest
Eosinophils:
Named for the way they stain in the laboratory
Playa role in defending against parasitic wanTIs. They secrete their granule
contents onto WOnTIS, which helps kill them
Basophils:
Smallest circulating granulocytes
Discharge the contents of their granules, releasing a variety of mediators such as
histamine, serotonin, prostaglandins, and-Ieukotrienes, which leads to
inflammation and other symptoms assodated allergic reactions and
infections
Question Alert!
e:
Mast cells and basophiles
-
produce histamines!
What cells are not
distinguishable?
White blood cells
Nonnal range of while blood cells are 4000 to 11000 Icmm
Lymphocytes: About 30% of white blood cells are lymphocytes.
Neutrophils: About 60% of white blood cells are neutrophils.
Monocytes: About 8% of white blood cells are monocytes
B lymphocytes and T lymphocytes are primary cell of specific immune response.
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LYMPHOCYTES
LYMPHOCYTES are a type of white blood cells found in the blood and many other
parts of the body. TYPES OF LYMPHOCYTES INCLUDE B cells, T cells, Natural
killer cells
B CELLS: B CELLS have thousands of identical antibodies in their membranes that allows
them to bind chemically to a small group of chemically related antigen.'
VIRGIN B CELLS: never respond to an antigen since they release into the circulation
from bone marrow. Their membrane antibodies are of the immunoglobulin M and D (Ig
M and Ig D).
MEMORY B CELLS: are derived from cell division fonn another cell that has
responded to an'antig.en! Thekmembrane antibodies ate Ig A, Ig E, Ig G' ,
. .
B CELLS (B lymphocytes) mature into plasma cell that secrete antibodies
(immunoglobulins), the proteins. that recognize and attach to foreign substances known as
antigens. Each type ofB cell makes one specific antibody, which recognizes one specific
antigen.
CELLS IN THE IMMUNE SYSTEM SECRETE TWO TYPES OF PROTEINS:
ANTffiODIES and CYTOKINES
ANTIBODIES (Immunoglobulins, Ig): Antibodies respond to antigens by latching on
to, or binding with, the antigens. Specific antibodies match specific antigens, fitting
together much the way a key fits a lock.
.
.
Question Alert!
Types of immunoglobulin's
and functions?
Ig A 10%, Ig Ai and Ig A2; Present in saliva, tears, urine! and external body fluids.
19D Less than 1%; Functions not well understood.
Ig E 1%; located on the cell surface of blood basophils and on connective tissue mast cells
to trigger the secretion of inflammatory mediators fro.m these cells in the presence of
specific antigen. IgE mediates allergic reactions (asthma).
Serum half is 2-3 aays. When this bound mast cells, the serum half life could be
18-4
[8-5
[,--_Ig_E_J
This accounts for ..... 1%.
This binds to Ig Ereceptors located on the cell surface of blood basophils and on
connective tissue mast cells to trigger the secretion of inflammatory mediators from
these cells in the presence of specific antigen. rgE mediates allergic reactions (asthma).
SERUM HALF IS 2-3 DAYS.
When this bound mast cells, the serum haff life could be several months.
)
IgA
[
IgG
Ig G is the predominant immunoglobulin, (- 70%). This is secreted at the end of primary
immune response and during memory responses. .
It diffuses from blood into other extra cellular fluids, particularly in inflamed
vasculatures, and it crosses the placenta to enter the fetal circulation.
SERUM HALF LIFE IS 25-35 DAYS.
Subclass: [gGI - IgG4
Ig A is secreted during memory response, this accounts for 10%of serum
immunoglobulins. \ It is secreted across mucosal surfaces into gastrointestinal,
respiratory, lachrymal. mammary, and gen!tourina.rv secretions. this protects
mucosa from of and other microorganisms.
SERUM HALF LIFE IS - 5 DAYS,
Subclass: IgAl and IgA2
IgM
It does not leave the blood in significant amount because of it PENTAMERIC STRUCTURE
(molecular size 900,000 daltons)
This accounts for ..... 20%. Serum half life 9 11 days
IgM is the most potent activator of"all immunoglobulins.
Subclass: IgMl and IgM2
several months. Ig Elevels increased in allergic reactions_
IgG 70%, most common of alllg's. This is secreted at the end of primary immune
response and during memory responses. IgGt-lgG., and can cross placenta
IgM 20%; IgM is the most potent activator of all immunoglobulins.
IgMl-lgM2. First immunoglobulin"produced in body.
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Accounts for less than 1%. Has no o ~ function.
T CELLS
T cells contribute to the immune defenses in two major ways. Some help regulate the
complex workings of the immune system, while others are cytotoxic and directly contact
infected cells and destroy them. Chief among the regulatory t cells are "helper/inducer"
t cells. They are needed to activate many immune cells, including b cells and other t
cells. Another subset of regulatory t cells acts to turn off or suppress immune cells.
Cytotoxic t cells help rid the body of cells that have been infected by viruses as well as
cells that have been transformed by cancer. They are also responsible for the rejection
of tissue and organ grafts.
THYMUS GLAND: T cell do not enter the circulation directly from bone marrow. But
first enter the thymus gland to mature. Most developing T cells die in thymu gland.
Vffi.GIN T CELLS: Release from thymus to circulation are virgin T cells.
MEMORY T CELLS: Originate through cell division and responses of other T cells.
T Cell receptors (T antigen receptors)
T Cell have two membrane proteins (alpha and beta or gamma or delta). These proteins
define specificity of each T. Cell, and several other membrane proteins know as CD)
complex. Cell mediate immune response
T cells: Helper T Cells, Cytotoxic T Cells, Natural Killer Cells
The helper T cells: Glycoproteins; The most T cells can be classified by the presence of
membrane glycoproteins:
The helper T cells (TH cells)--------------- CD4
Cytotoxic T Cells (CTL) or Tc Cells ---------- CDg
The helper T cells (THcells): These can be divided two type THI and TH2.
18-6
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These cells produce Iymphokines, are small proteins that act on other cells in autocrine,
paracrine, endocrine manner.
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I: Activate other cells, inhibit antibody production by inhibiting the fonnation ofTH2.
T
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2: activate B cells to divide and produce antibody.
T Cytotoxic Cells (Tc): T Cytotoxic Cells (Tc) Are Able Jo Kill Cells ThatInfected By
Virus. This is done direct binding to the infected cells or through release cylotoxins.
Most ofT cytoloxic cells are C04+: All ofthese cells suppress i m m u ~ responses
through the secretion of IL-IO and TGF-heta and cells designated CD4+ C025+ are also
inhibit through direct cell contact. Cytotoxic cytokines are released by a type ofT cell
called a cytotoxic T cell. These cytokines attack cancer cells directly.
Immunodeficiency's and Immunopathology
A. Primary
Either hereditary or congenital and at least one basic element to the Immune
system does not function properly or is absent
I. X-linked aggamaglobinemia (hypogammaglobulinemia)
inherited deficiency in antibody production in which T cell function is relatively
nonnal but B-cells do not fully mature
Symptoms: pneumonia, sinusitis, meningitis and septicemia
2. SCIDS
Heterogenous group of inherited disorders with deficiencies ofT cells, B cells and
serum Ig
Infections with opportunistic organisms occur in the lSI few postnatal and survival
for longer than one year is rare without successful bone marrow transplantation
B. Secondary Immunodeficiency
invoke decreased immunologic responsiveness
AIDS
Acquired deficiency syndrome is a serious and most fatal condition in which the
immune system breaks down and does not respond normally to infection.
How is HIV transmitted?
Sexual transmission
Transfusion of infected blood and blood products
Maternal transmission
I-IlV contam inated instruments
Tests that are used to diagnose HIV infection:
ELISA
Western blot
Polymerase chain reaction (PCR assays)
Stages of HIV reproduction
I. HIV enlers a CD4 cell (helper T cell)
18-7
2. HIV is a retrovirus that its genetic infonnation is stored on single stranded RNA
instead of double stranded DNA found in most organisms. To replicate, HIV uses an
enzyme known as reverse transcriptase to convert its RNA into DNA
3. HN DNA enters the nucleus of the CD4 cell and inserts itself into the cell's DNA then
instructs the cell to make many copies of the original virus
4. With the help of the protease enzyme, new virus particles are assembled. These newly
fonned viruse,s have the cell ready to infect other CD4 cells
5. Shortly after HIV infection, the CD4 cell count'falls'sharply in the early'stages of fIIV
infection because the virus targets and destroys CD4 cells. When the body starts to cope
with the infection, the CD4 cell count rises again. In the advance stage, the rate at which
the virus reproduces or rate at which the virus reproduces or "replicates" surpasses the
rate of CD4 cell turnover, making the body more susceptible to a variety of AIDS-
defining illnesses such as Pneumocystis carinii pneumonia (PCP), as the viral load
rapidly increases unchecked and the CD4 cell counts decline these illnesses that signal
late stage infection eventually'lead to death
Common opportunistic infections:
1. Tuberculosis, both pulmonary as well as extra pulmonary. This is the one the
commonest presentations. Atypical mycobacteria such as Mycobacterium avium
complex (MAC) may also cause infection
2. Oral candidiasis
3. Eosophageal candidiasis
4. Herpes zoster
5. Diarrhea, which may be due to a variety of pathogens ,
Protozoal - amoeba, Giardia, isospora belli, cryptosporidium
Helmints - strongyloids
Viral - cytomegalovirus
6. Bacterial pneumonia and Pneumocystis carinii pneumonia
7. Toxoplasma encephalitis
8. Cytomegalovirus renitis
Cancers such as Kaposi's sarcoma and non-Hodgkin's lymphoma are also seen in these
patients .
CD4/mm
350
275
200
100
50
Type of opportunistic infections
M. tuberculosis
Kaposis sarcoma
lymphoma
P.carinii pneumonia
Cytomegalovirus and M avium intracellular
18-8
Interferon
CYTOKINES
18-9
Question Alert!
Interleukins, interferon's and
(SF applications!
Substances produced by some immune system cells to communicate with other cells
Types ofcytokines include
Lymphokines
Interferons
lnterleukins
Colony-stimulating factors (CSF).
Natural Killer Cells
/
At least two types of lymphocytes are killer l l s ~ cytotoxic T cells and natural killer
cells. Can increase the number of red blood cells 3lid reduce the need for red blood cel1
transfusions in patients receiving chemotherapy; and Oprelvckin can reduce the need for
platelet transfusions in patients receiving chemotherapy.
MONOCYTES are white blood cells that can swallow and digest microscopic organisms
and particles in a process known as phagocytosis. Monocytes can also travel into tissue
and become MACROPHAGES, or "big eaters."
A class of lymphokine proteins important in the immune response. Proteins that are
secreted by cells when they become infected with virus
Bind to nearby infected cells and prevent viral infection
This increased resistance of cells to viral infection and slows the spread of disease
There are three major types of interferon:
Alpha (leukocyte)
Bela (fibroblast)
Gamma (immune)
lnterferon's inhibit viral infections and may have anticancer properties. Interferons are
indicated in hepatitis infections.
lnterleukin
A type oflymphokine that regulates the growth and development of white blood cells.
Twelve interleukins (IL-I through IL-12) have been identified to date.
Example: Interieukin-3 (hematopoietic growth factor), Oprelvekin (interieukin-l I) is a
polypeptide growth factor obtained by recombinant DNA technology. Increases platelet
production via stimulation of hematopoietic stem cells.
Therapeutic use: Chemotherapy related thrombocytopenia
Side effects: Fluid retention, peripheral edema and dyspnea
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COLONY-STIMULATING FACTORS (CSF)
Colony-stimulating factors (CSFs) (sometimes called hematopoietic growth factors)
usually do not directly affect tumor cells; rather, they encourage bone marrow stem
cells to divide and develop into white blood cells, platelets, and red blood cells. Bone
marrow is critical to the body's immune system because it is the sO'urce of all blood cells.
The CSFs' stimulation of the immune system may benefit patients undergoing cancer
treatment. Som.e examples of CSFs and their use in cancer therapy: Erythropoietin,
Epoetin alpha, Epoetin beta.
Therapeutic use: Treatment of anemia resulting from chronic renal failure
Side effects: Increase BP, Monitor: Blood pressure
Produced by recombinant DNA technology: Filgrastin and Pegfilgrastin and
Sargramostim: These glycoprotein's produced via recombinant DNA technology
Therapeutic use: Treatment of chronic and chemotherapy induced neutropenia
Sargramostim is approved for myeloid reconstitution (in bone marrow transplantation)
Side effects: Skin allergies, respiratory allergies, cardiovascular allergies
Filgrastin and pegfilgrastin are contraindicated in patient with allergic to E. coli derived
proteins.
MAJOR HISTOCOMPATIBILITY COMPLEX (MHC) proteins:
Recognize peptide epitopes (fragment of antigens), combined with chemical an.d MHC
proteins to produce two major classes of MHC proteins.
Class 1 proteins: Present on all surfaces of body cells.
Class" proteins: Present on specific antigen presenting cell (APC's). .
Lymphokines are part of larger network of regulatory cytokines. This network includes
secretion of other cell types in addition to those Iymphocytes. .
Hypersensitivity Reactions
Excess, inappropriate and prolonged immune responses that cause damage to normal
tissue.
Causes Symptoms
IgE mediated type I hypersensitivity reaction Inflammation of upper and lower
Respiratory allergies-grass, animal fur, carpet mites respiratory tract (asthma), GI and skin.
- GI allergies---Dairy products, shellfish, peanut. Atopic dermatitis, pruritis, rhinitis,
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Skin allergies-7topical drugs (procaine)
c.
asthma, food allergies.
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Intravenous allergies7insect venoms Approximately 50% of patient with
Non IgE mediated type I: Anaphylactic asthma secret IgE
.. reactions7epipen
Transfusion mismatches, hemolytic anemia, Hemolytic anemia and thrombocytopenia
-
Rh disease, Specific autoimmune diseases Hashimoto - are more common.
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thyroiditis, myasthenia gravis. Hyperacute graft rejection
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Non specific Autoimmune disorders-? lupus Iympoadenopathy, fever, and rash- first
= erythematous, rheumatoid arthritis. symptoms
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Hepatitis infections, local respiratory form of fungal More serious: glomerulonephritis,
~ reactions. vasculitis and lupus. arthralgia and
Penicillin and sulfonamides arthritis
Prolong action of protozoa: Mycobacterium Symptoms of type IV: Contact dermatitis;
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Tuberculin test and poison ivy microvesicle formation,
Spongiosis
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Autoimmune Disease
When the immune system mistakes self tissues for non selfand mounts an inappropriate
t t c ~ the result is an autoimmune disease. There are many different autoimmune
diseases. Some examples are:
Organ specific autoimmune disorders:
Rheumatic fever
Anlithyroid autoimmunities
Myxedema (hypo)
Hashimoto thyroiditis (hypothyroidism)
Graves disease (hyperthyroidism)
Myasthenia gravis (weakening of muscles)
Autoimmune pernicious anemia
Goodpasture's syndrome
Autoimmune hemolytic anemia, thrombocytopenia, neutropenia, lymphopenia
lnsulin dependent diabetes mellitus (IDDM)-typel
Multiple scelorosis
Non organ specific autoimmune disorder: Sjogren syndrome, lupus erythromatus
Drugs that provoke lupus-like syndrome: Procainamide, hydralazine, quinidine,
methyldopa, isoniazid, phenytoin and chlorpromazine, penicilamine (HLPPP MCQ)
Treatment: Mild diseases (low fever, arthritis) - NSAlDs Severe symptoms - oral
methyl prednisone
Tips
Monocytes are white blood cells that can swallow and digest microscopic organisms and
particles in a process known as ->
18-11
Questions Alerts!
Immunizations or Vaccines

.
Immunizations
Common questions in pharmacy exam is
Influenza (flu) viral infections: high risk groups, flu seasOn contraindications
Hepatitis vaccinations: Hepatitis A and B, travelers
Immunization is the means of providing specific protection against common and damaging
pathogens.
'i:)tt;fiVE:lmmunity
Antigen enter the body and the body responds by making its own antibodies and B-
,
memory cells;
longer lives
Naturallmmunitv:
occurs when the person is exposed to a live pathogen, develops the disease, and
becomes immune as a result of the primary immune response
Artificial Immunity:
Can be induced by vaccine, a substance that contains the antigen. A vaccine stimulates
a primary response against the antigen without causing symptoms of the disease
a) live (attenuated) organism --> 1'10+ +>
MMR vaccine (measles, mumps, rubella) ---
TOPV (Trivalent oral polio vaccine)
b) Killed (inactivated) organism
IPV (inactivated Poliomyelitis Vaccine)
Rabies vaccine
Influenza vaccine -> .
i) Vaccines with fragments of microorganisms
immunization for meningococcal meningitis
pneumococcal pneumonia
Hib (Haemophilus influenza type B) or secreted toxins (detoxified)

Diphtheria and tetanus component of the DtaP and Td vaccines
Immunizations or Vaccines
B) PASSIVE IMMUNI,{ hv" ,4vJ L,oelo F
Antibodies made in another person or animal enter the body
Short-lived
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Artificial Immunity
Injection of antibody-containing serum or immune globulin, from another person or
animal or the injection of monoclonal antibodies
The use of pooled adult human immune globulin (lG) to prevent infections in people
with certain immunodeficiency diseases
Human NBIG to prevent hepa B in those not actively immunized with hepa Bvaccine
There are two categories of immunizations
Active Passive
Slow acting, is used for prophylaxis Fast acting.
long duration of action. Short duration of action. Require booster dose.
Administered im or iv, or sc. -
Example: Flu.shot; Takes 2 wk to be Example: Hepatitis B immune globulins (HBIG).
effective and taken annually. Prophylaxis and therapy.
"' ......
vacdhi:!;jTakes 2 wks to Vericella zoaster immune globulins (VZJG).
be effective. High risk patient can take Rho (D) immune globulin (RhoGAM): Prophylaxis
every 5 to 10 years. for Rh +ve fetus by Rh -',Ie mother receives
Tetanus vaccine effective for 10 years. RhoGAM). Prophylaxis given during pregnancy and
after labor (delivery).
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There are two methods of vaccines preparations'
live (attenuated) vaccine
-
Killed (inactive) vaccines
Measles; Mumps; Rubella Influenza A and B
Chicken pox (varicella) Polio (inje'cted)--t Salk
Polio (oral)--t Sabine; Typhoid (oral) Pertusis; Plague; Hepatitis A and B;
Tuberculosis, yellow fever; small pox Rabies; Typhoid (injected); Cholera
live vaccines are contraindicated in Killed vaccine are can be given in pregnancy and
pregnancy and HIV patients immunocompramized.
live vaccines are made from live viruses Inactivated vaccines consist of whole microbes
and bacteria. that have been killed by heat or chemicals.
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Important to vaccines: Influenza A&B vaccine (seasonal flu)
Given annual
Flu season in
Flu immunization season:.Otrtb mid-Nov
High risk group: seniors (>65yo), asthma, COPD, CVD, diabetics, children >6mo to 2yo,
healthcare workers, and pregnancy..
CI: children < 6mo, egg allergies, and with flu symptoms
19-2
www.phannacyprep.com Immunizations or Vaccines
Hepatitis vaccine
Hepatitis A and B have vaccine
Hep A is given anyone over I yr age
Hep A transmits by food or oral fecal
Hep B& C are chronic, transmit by sexual, blood, drugs abuse, spa
Hep B vaccine protects hep D
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Who is high-risk group for seasonal flu? ( P1 t'lo: ,C!. 1 0-)- c.opdl ,C-Vd,
Who should nollake flu vaccine? l'"'N , 4- rtu- t).-
The type of acquired immunity whereby resistance to a disease is built by either having
the disease or receiving a vaccine to it. ( AcJwe. I hh".,v)o't JJ..a
Who should not get live vaccines? ( NJv'!-4- ) I rr'j'h'lu"""-l) v-...o.,..,.
Flu vaccine effective against which type of viruses? ( I 4-.../1 J J.-u.. ..
Dukoral oral vaccine is used against ( -rklAveb-c.- C- 4- c.r---
Travelers are recommended to take ( LJe.p:J,.Jtd po""'" .
Rota vaccine is to prevent to prevent rota virus is used against (
Gardasil vaccine is used against ( V
1. In pregnancy 2. Immuno compromised 3. Egg allergies
4. Influenza A& B 5. Seniors over >65 6. asthma
7. COPO 8. CVO 9. diabetes
10 children from the age 11 Egg allergies 12 flu symptoms
of 6 months to 2 years
13 under 6 months of age 14 Active immunity
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Biotechnology
Questions Alerts!
Biotechnology methods for manufacturing pharmaceuticals
Examples of biological medicines
This chapter is focused on pharmaceutical products that are developed using recent biotechnological methods
and their storage conditions, role of pharmacist.
Clotting Factors: Recombinant antihemophilic factor (rAHF): Indicated for treatment of
classical hemophilia A. The dry concentrate of rAHF should be storea1>etween 2 to gO C and
protect from freezing.
Hemophilia is a genetic disease. It is categorized as hemophilia A and B.
Hemophilia A is due to deficiency of clotting factor 8.
Hemophilia B is due to deficiency of clotting factor 9 (Christmas factor)
Cytokines: Cytokines functions as the messengers of the immune system. They are secreted
by cells of immune system in response to stimulations.
Colony stimulating factors (CSF): Glycoprotein cytokines that promote proliferation,
differentiation and activation of immune cells.
/" ~ ~ Ylw}/-<>pe.N"'- O I M ~ SIJ.L.-<Wdr"
Granulocyte CSF (Fitgrastim): This drug stimulates the production of neutrophils wyhin bone
marrow. It is approved for chemotherapy related neutropenia. It does not contain
preservatives it should be stored between 2 to 8 .c. It is not frozen.
Granulocyte Macrophage CSF (GM-CSF; Sargramostim): This drug is indicated for acceleration
of bone marrow in patient with non Hodgins lymphoma, acute lymphoblastic leukemia.
Erythropoietins
Erythropoietlns.is sialic acid containing proteins secreted by kidney In response to hypoxemia
and transported to the bone marrow through the plasma. It resembles an endocrine hormone
more any other cytokines.
20-1
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Biotechnology
Erythropoietins enhance erythropoiesis by stimulating the formation of proerythroblasts and
release of reticulocytes from bone marrow. Erytopoietins are indicated in anemia, associated
with cancer chemotherapy. It is also used to chronic renal disease associated anemia.
Epoietin alpha (Eprex, epogen, procrit): once week. It is approved for anemia related to
.cancer chemotherapy, chronic dialysis, and AZT therapy.
Darbopoietin alpha (Aranesp): every 3 week
Human growth hormone (hGH)
The pituitary gland secretes human growth hormones (hGH), which stimulates an
individual growth.
Systemic growth hormone; Humatrope, protropin, and somatrem
Interferon's
Interferon's inhibits viral multiplications, thus indicated for viral infections.
Interferon's are classified into two types; type I interferon's (alpha and beta), which share
the same molecular receptors, and type II (gamma or immune), which has different
receptors.
Interferon beta Ib-Betaseron, Interferon-beta Ib (IFNB) is effective in the treatment of
relapsing remitting types of multiple sclerosis.
Interferon alpha la; drug is used in the treatment of hepatitis viral infections.
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Interferon Beta -7 used for the treatment multiple sclerosis
Interleukins: synthesized by monocytes, macrophages, and lymphocytes. Interleukins are
soluble messengers between leukocytes.
IL-l- intensify the production of collagen, prostaglandin and antibodies
IL-2 - Fusion protein
IL-3 - Hematopoietic growth factor
IL 11 - Operlaveukin; Indicated for thrombocytopenia associated with cancer
chemotherapy. A type of Iymphokines that regulates the growth and development of
Platelets
Monoclonal antibodies: Monoclonal antibodies are ultra sensitive, hybrid, immune system
derived proteins designed to recognise a specific antibodies.
f" :-, .. \1- .'," - \. j-"
, ;'Muromonalj (Orthbrtlohe OKT3)
Indicated in acute graft rejection in renal, cardiac and hepatic transplant patients.
free reduces binding to cells.(mast.cells,
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Tissue plasminogen activators (t-PA): These are substances produced in small quantities by
the inner lining of blood vessels and by the muscular wall of uterus. Tissue plasminogen IJfY'- .
activator prevents abnormal blood clotting by converting plasminogen, a component of blood, /JW u.-uJ
the enzyme plasmin. The plasmin is breakdowns fibrin, the main constituent of blood clot.

20-2
Recombinant alteplase (activase): This drug is indicate.d in management myocardial
infarction (STEMI). ".
Tumor Necrosis Factor (TNF): It is produced mainly by activated mononuclear phagocytes,
have both beneficial and potentially harmful effects, mediating cytotoxic and inflammatory
reactions. Two anti-TNF alpha monoclonal antibodies are approved for the treatment of
rheumatoid arthritis and ehron's disease
Infliximab (Remicade); is chimeric IgG antibody directed against TNF alpha (selectively binds
with alpha), it is approved for Crohn's disease and for the treatment of rheumatoid arthritis.
Administered i.v. 3mg/kg, at 0, Z, and 6 weeks and then every 8 weeks after. Inf,Ux.iii1ab"'Shdtild"'.
.
be-admin-istere,d with methotrexate to prev.ennhe formation of antibddies t6 infliximab.
Biotechnology
Blood
Plasminogen
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Prothrombin (II) Thrombin Ua
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Pl'T Fibdnt::::
Fibrin degradation prOduc,... (- blMx! C) 04-
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Etanercept: binds with both TNF alpha and beta. The greater risk of etanercept therapy is
immuno suppression and subsequent serious infections.
Tips
;' Find answer from the table:
L Infliximab 2. Etanercept 3. Megakaryoblast
4. Hemophilia A S. Muromonab-CD3 6. Erythropoietin's
Orthoclone OKT3
7. Filgastrim 8. Epoetin alpha
Indicated for anemia, associated with cancer chemotherapy; also used for chronic renal
disease associated anemia (
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What is the treatment of neutropenia associated to chemotherapy (
p'recursor of platelets ( 10 t 0
What drug binds with both TNFalpha and beta ( E1-a VlesLc--l1r---
What drug is used to treat acute graft rejection in renal, cardiac and hepatic transplant
patients (
What it is approved for Crohn's disease and the treatment of rheumatoid arthritis ( I
Due to deficiency of clotting factor 8 cause fl-
Inflix'imab is indicated for? IJ(Pr J U-o h i-ly . I uG
InfJiximab is given as? I'. V
What drugs attacks CD/ T cells? -7 V1w..o w..o CoklJ)) 4- fY)A-5.s
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Poison prevention strategy: Child proof containers, Constant vigilance, Labelling
Formulation
Toxicology
r:r.
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Toxicology
www.PhannacYDrep.com
This chapter focuses in methods of treatment associated with overdose of drugs and
overdose symptoms, chemicals toxicity. Drugs and chemicals that commonly ca use toxicities,
and the role of the pharmacist. Antidotes and treatment are presented for specific drug
toxicities.
Questions Alerts!
Overdose symptoms of overdose of benzodiazepines, opioids, acetaminophen,
tricyclic antidepressants and iron.
Antidotes of overdoses of benzodiazepines, opioids, acetaminophen, tricyclic
antidepressants and iron.
General management of toxici.ty:
Supportive care (ABCs)
Gathering information of toxicity
Evaluating toxic symptoms and refer to doctor or emergencies
Documentation
Gastric lavage or gastric gabage: This procedure can be used:
Good for patient if unconscious
Depression
Seizures
Coma and convulsion
GI Decontamination procedures
Decontamination consists of removal of any unabsorbed poison from the patient's body.
I Commonly used methods include gastric lavage or gastric gabage, emesis, ipecac, adsorbent
agent - charcoal.
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Toxicology
Contraindicated in patients who have ingested Acids, Alkali, Hydrocarbons, Risk of GI
perforation
Emesis (vomiting): This method is used to evacuate GI tract.
Emesis procedure is contraindicated in
Children less than 6 month
>
Strong acid and base
Depression
Unconsciousness
Seizures
Coma and convulsion
Extremely rapid onset of action
Emesis following ingestion
Sharp objects
Hydrocarbons, petroleum products
Ipecac induced emesis and gastric lavage primarily removes substances from the stomach and
their efficacy is affected by time and quantity of ingestions.
These procedures are more effective if they are implemented within 1 hour of ingestion.
Syrup of Ipecac is admi,:,istered within 60 min toxic dose ingestion (later has no benefit)
Onset of emesis: 30 min
Effect could last 2 hours
3 episodes of emesis in 60 min
Dose of Ipecac for adults and children
For emesis Adult 1S to 30 ml po with 1 to 2 glass of water
For emesis .child 10 to 15 ml po with 1 to 2 glass of water
For expectoration Adult 1 to 2 ml po
For expectoration child 0.25 to 0.5 ml po
Decontamination
Activated Charcoal
This method is preferable method of decontamination.
Higher the surface area of charcoal higher the adsorption.
Heating charcoal increase adsorption?
Adsorbent agent: Charcoal is good for drug and chemicals
NOT for: (not adsorbed): Methanol, ethanol, iron, cyanide, ethylene glycol, mer:cury, organic
solvents, potassium, strong acids and bases. Do not use if patient is vomiting
Dosage: Adults ZS to 100 g; Children 1 to 12 years 25 to 50 g; 0 to 1 years; 19/kg
Charcoal available as colloidal dispersion form.
21-2
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Question Alert!
ASA overdose is treated by
NaHC03 alkaline diuresis
Bowel Irrigation Method: Osmotic solution of polyethylene glycol (PEG) is used (l-2Iiter /hr
orally).
21-3
NaHCO) side effects: Metabolic alkalosis, hypernatremia, hyperosmolarity, and fluid overload
Enhancement of elimination: Enhancement of elimination is possible for a number of toxins,
including manipulation of urine pH to accelerate renal excretion of weak acids and bases.
,
Diuresis: Promotes elimination acids and bases. This can be alkaline and acid diuresis.
Alkaline Diuresis: Promotes the ionization of weak acids therefore prevents re-absorption by
the kidney, facilitate excretion of weak acids.
Example: Salicylic acids, ASA, phenobarbital, and barbitura
Dosage: NaHC03 (sodium bicarbonate) 50 to 100 mEq of
pH 7.3 to 8.5 (urine)
Urine output: 5 to 7 ml/kglhr
Acid Diuresis: Used to promote elimination of weak bases.
Example: Amphetamines, phencyclidines, quinidine derivative, and alkaloid drugs.
Dosage: Ascorbic acid (SOD mg to 19l, and ammonium chloride (4 g) every 2 hours
Serum electrolyte and pH should be monitored.
Important characteristics of the toxicology of arsenic iron lead and mercury

Metal From Entering Body Route of Target Organs for Treatment
Absorption Toxicity
lead Inorganic lead oxides Gastrointestinal Hematpoietic Dimercaprol, Edentate (EOTAI,
and salts tract, respiratory, system, eNS, penicillamine, succimer.
skin (minor) kidneys
Tetraethyllead Skin (major), CNS Seizure control, supportive
Gastrointestinal
Arsenic Inorganic: arsenic All mucosal capillaries, Dimercaprol succimer,
salts sunaces gastrointestinal penicillamine
tract,
I
hematopoietic
system
Arsine gas Inhalation Erythrocytes Supportive
Mercury Elemental Inhalation CNS, kidney Dimercaprol
Inorganic salts Gastrointestinal Kidneys, Penicillamine, dimercaprol
-
tract gastrointestinal .
tract
Organic mercurials Gastrointestinal CNS Supportive
tract
Iron Ferrous sulfate Gastrointestinal Gastrointestinal Deferoxamine
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Toxicology
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Toxic features of specific agents
Agent Toxic Features
.
Acetaminophen M!ld anorexia. nausea. vomiting. delayed jaundice. hepatic and renal failure
Max dose 4 g/day:Max dose 2 gjday for chronic alcoholic, and hepatic disease
Antidote is acetylcysteine. should be administered within.8 hours of overdose.
Antifreeze (ethylene Toxic oxidized product of ethylene glycol is oxaiic acid.
glycol) Renal failure. crystals in urine, anion and osmolar gap. initial CNS excitation;
eye examination normal.
Botulism Dysphagia. dysarthria. ptosis, opthalomoplegia, muscle weakness; incubation
period 12 to 36 hours
Carbon monoxide Coma. metabolic acidosis. retinal hemorrhages
Cyanide Bitter almond odor. seizures. coma. and abnormal ECG
Gasoline Distinctive odor, coughing, pulmonary infiltrates on xray.
Iron Bloody diarrhea. coma. radiopaque material in gut (seen on x-ray), high
leukocyte count. and hyperglycemia.
Lead Abdominal pain. hypertension, seizures. muscle weakness, Metallic taste,
anorexia, encephalopathy. delayed motor neuropathy. changes in renal and
reprodu.ctive function..
Gray mouth
LSD Hallucinations. dilated pupils. and hypertension
Mercury Acute renal failure, tremor, salivation. gingivitis. colitis, Erethism (fits of crying,
irrational behaviour). nephritic syndrome
Methanol Rapid respiration, visual symptoms, osmolar gap, severe metabolic acidosis.
Methanol toxicity gives blindness due to formic acid.
Mushrooms (Amanita Severe nausea and vomiting 8 hours after ingestion; delayed hepatic and renal
phalloides type) failure
Paraquat Oropharyngeal burning. headache. vomiting, delayed pulmonary fibrosis. and
death
Phencyclidine (PCP) Coma with eyes open, horizontal and vertical nystagmus. hyperacusis,
myoclonic jerks, violent behaviour
..
Plants Nightshade Hallucinations. mydriasis, seizures (these plants contain atropine-like alkaloids)
family, jimsonweed
Oleander and foxglove Digitalis poisoning
Predatory bean (rosary Delayed severe gastrointestinal distress, seizures, hemolytic anemia, death
pea)
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Antidote Poisons
Acetylcysteine Acetaminophen; best given within 8 to 10 hours after overdose
Antivenin Snakes. black widow spiders
Atropine Cholinesterase inhibitors. organophosphates, carbamates
Bicarbonate. sodium Membrane-depressant cardiotoxic drugs, ego Quinidine, tricyclic
antidepressants, and ASA
Deferoxamine Iron salts
Digoxin-specific Fab antibodies Digoxin and related cardiac glycosides
(digifab)
Esmolol Caffeine, theophylline, metaproterenol
Ethanol Methanol, and ethylene glycol
Flumazenil Benzodiazepines, zolpidem
21-4
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1. Flumazenil 2 N-acetylcysteine 3 Glucagon
4. latanoprost 5 NaHC0
3
6 Amiodarone
7. Myopathies 8 elevated CK MM 9 Rhabdomyolysis
10 Hydrochloroquine
Glucagon Insulin, beta-blockers,
EDTA Lead
Dimercaprol Lead, 2old, arsenic, and mercury
Hvdroxocobalamine Cyanide
Penicillamine Copoer, lead, arsenic, 20ld and Wilson's disease
Naloxone Opioid analgesics
Oxve.en "carbon moooxide
Physostigmine Atropin (muscarinic antagonist). not tricyclics
Pralidoxime Organophosphate cholinesterase inhibitors
Sodium thiosulfite Cyanide (nitroprusside)
Protamine sulfate Heparin
Vitamin K Warfarin
Phvtanodione
Fomepizol (alcohol Methanol, ethanol, and ethylene glycol
dehydrogenase enzyme
inhibitors)
21-5
.5
Tips
Find answers from the table"
,
,
Insulin antagonist is? { ;3

Benzodiazepine antagonist is? (1. )
Salicylates overdose may be treated by? (
Acetaminophen antagonist is? (2 )
Naloxone is antidote against overdose of (e f fer rc4
Vitamin Kis antidote against overdose of ( <-
Protamine sulfate is antidote against overdose of ( f,...a-f4.JJ I
Aminophylline is an antidote against overdose of ( Sa..J.,
Glucagon is used in emergencies to treat symptoms of (JeNe'l...-
Which glaucoma medication causes iris pigmentation? ( ,) f.t;..,!-.rJJ
latanoprost side effect ( e;v>- cl-) 4"'7'-
Which antiarrhythmic drug cause pulmonary toxicity? ( 4".,..., Co
Amiodarone{'L..f5' bVblJl'
Which antimalarial drug causes retinopathy side effect? ( I ) J I . , _ 1.::J
"Jdw
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Phannaceutical sciences
Part II:
Phannaceutical Sciences
(3
5
1)
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Phannacy Calculations
Questions Alerts!
Conversions
Ratios and Proportions and Concentration
Active drug quantity
Conversion of dosage forms
Dose Tapering
IV Rate of infusion
Units
tn Metric System
Weight
1 Kilogram", 1000 grams
1 Gram", 1000 milligrams
1 Milligram c 1000 micrograms
1 Microgram = 0.001 milligrams
1 Milligrams E 0.001 grams
1 Microgram" 10 -4 grams
1 Nanogram II: 10.
9
grams
1 Grai9- =6S milligrams
J(1)
Volume
1 pint = 473 ml '" 16 fluid ounces
1 fluid ounce" 29.6 mt "approximately 2 tablespoonfuls ;:.3 0 v4
1 fluidram = 3.7Sml
1 teaspoonful:. Sml
1 tablespoonful = 15m!
One wine glassful'" 60 ml
Copyright 0 2000-2012 TIPS Inc. Unauthorized reproduction or this manual is strictly prohibited and it is 22-2
PhannacyPrep.
One tea cupful = 120 ml
One full glass = 240 ml
4 cups =1 pint
8 pints =1 gallon
1 gallon =3.8 L
An "official" dropper contains 20 drops/ml (of water)
Body Surface Area
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"BSA" stands for "body surface area." units are m
2
. BSA is sometimes used in dosing of medications (more on
this later). A universal equation for calculating BSA of both kids and adults is:
BSA in m
2
:= (Ho.
3964
) (WO.S378) (0.024265) H c w--

AY15 -cD
lJ",I<6 0il :::.
\-1= 15"M
8M!.
. Where height is in centimetres and weight in kilograms.
BSA in m
2
: VHxW / 3600
Body Mass Index (BMI)
BMI = weight in Kg/height m
2
or Weight in Kg/height m x height m
BMI :"""1i'drm'i,i171-8:9 to' 24.9
t . . '.'.. .'
BMI := overweight >25 to 27
BMI := obese >30
BMI := morbid obese> 35
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Q A person body weight is 180 Ibs and height is l.S m? What is right BMI?
A-normal B-over weight C-obese @-norbid obese
Density =Weight / volume (D =WIV)
Volume = Weight / Density
Weight = Volume x Density
@A doctor want to prescribe orlistat (xenical) to patient to I I

treat weight loss. Patient weight is 140lbs and height is 1.6 m. However, clinical practice guidelines suggest to ' 'J-
use orlistat in patient 8MI is gre,ter than 30. Is this patient is eligible to receive orlistat} _I. bola- + ).LCfY'.e.. , _____
A -:f BMI -::. 63."3 l'S' -:::. 2-4 . " pcJ>eva t5 Tl 0'1 e.-uo: o. elL GY'IU
nj eu 'Pe/1- 2JU-A .,
Density (specific gravity) ..,-,

Examples:
Water 1000 ml, its density is 1, what is weight water in grams? -;> I 000
Glycerine 1000 ml, its density is 1.2, what is weight in g of glycerine?-1 1C)...()(Jrr"-
Weight = Volume x Density; 1000 x1.2 = 1200g
A winter green oil density is 0.9, what is the weight of 1000 ml oil? -7 900
A topical preparation density is 1.1 and its volume is 720 ml. What is weight in kilograms.
C19.0X!' 1Qi.QM
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PhannacyPrep.
Decimal to mixed number
To convert decimal to mixed number
Mixed numbers to decimal number
A newborn child weighs 10 Ibs. What is weight in kg? -J It 54 Ij-
Pharmaceutical sciences www.pharmacypreo.com
Fractions to decimal numbers
35/10 = 7/2 = 3 Y,
Example: 1.25 = 125/100 = 5/4
Pounds and Kilograms or Kilograms (Kg) and Pounds (Ibs)
Example: 3.5 =3 Yz
Step 1 -7 Write the decimal number over one, dividing with one =3.5/1
Step 2 -7 Move the decimal point in the top as many places as to right as necessary to
form a whole number.
Move the same in bottom. 35/10
To convert mixed numbers to decimal number
Example: 2 % = 11/4 = 2.75 or 11 % = 11.75
Step 1-7 multiple bottom number by whole number and add with top number.
Step 2 -7 divide top number by bottom number
To convert fractions to decimal numbers -7 divide top number by bottom number
Example: Yz =0.5
Example: 3/10 =0.3
Example: 10/3 =3.3 ;
To convert Ibs into Kg =divide by 2.2
To convert Kg to Ibs =multiply by 2.2:
Example: 35 kg =7.7 Ibs or 5 Kg =llibs 10.3 =103/10 =10.3/10
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/
1. On admission to the hospital your patient weighed 1581b and was placed on a diuretic.
Two days later the patient's weight was 70.9 kg.
This patient has lost kg or 2.:0l-lb of body weight in response to this medication.
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Pharmaceutical sciences
Teaspoons (tsp) and Tablespoons (Tbsp)
2. The physician has ordered 50 mg.of a medication to be administer daily. The drug
reference states that you should administer no more than 1 mg/ kg of body weight daily. This
client weighs 164 lb. '
The largest dose that this patient could safely receive is mg.
3. The physician has ordered injectable versed for your patient who 135 lb. Your drug
reference states that the maximum dose is 0.06 mg/kg of body weight;.,/" b
The largest dose that can safely be administered to this patient is2:>' mg. .6 , ..) (x d a

1. The physician has prescribed 1 Tbsp of Riopan. The unit dose container available contains
30 ml of this medication.
The correct dose is ml.
2. The client has been taking 20 ml of a medication in the hospital. In preparing him to
administer this medication in the home setting, you would teach him to tak,e -4- tsp of this
drug.
3. The client is to take Yz Tbsp of medication. The most accurate method for measuring this
dose is to pour ml of this drug.
Milligrams and Grains
1. You are to administer phenobarbitol gr %. There are scored 60 mg tablets available in floor
stock.
You would administer Ml?mg or __- _ tablet(s).
2. Morphine sulfate gr 1/8 1M is to be prepared from a solution containing 10 mg/1 ml.
The volume to be given is tlml. 65 K Yg;; I 25
Ans: I vv-4. I cJ I '2..b
L'lJ
3. Ferrous sulfate gr 5 po q AM is ordered for your Pharmacy has provided 325 mg
tablets. 'S '(. S" "- 32J; /V-i1..-4,uA btL-
You will administer tablet(s) ,...\ h " ui. 1 tc.b
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Millilitres and Ounces 'i &: '/2. ;. 1 l)
l.The physician has ordere@unces of a The correct dose is A.s- ml.
2. You are to administer 5 ml of ferrous gluconate that must be diluted in water to protect the
client's teeth and gastrointestinal track. The directions in your drug reference state that each
ml of this medication must be diluted in 20 ml of water.
Once diluted, the total volume to be administered is 105 ml.
--,----
PhannacyPrep.
Percentage: To convert percent to fractions
3/4 . 100 = 75%
Ratios: Relation between two quantities
W/W 1 gram in 100 grams =19:100g
W/V 1 gram in 100 ml = 19:100ml
V!W 1 ml in 100 grams =Iml:l00g
VjV 1 ml in 100 ml = Iml:lOOml
25%=25/100 =X
0.25 . 100% = 25%
50%=50/100 =Yz
200%= 200/100 =2
To convert fraction to percentage: multiply by 100
Pharmaceutical sciences www.phannacvorep.com
3. Your client is to drink 64 oz of Golytely over a 3-hour period. How many milliliters must this
person consume each hour to comply with the physician's order? / k....--
Administer 640 ml each hour. 64 ><30 '" I 2.0 M 3
-. (;40/ Jv"..
Calculations involving percentage, ratios, proportions
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Ratio percent: W/W%
Example: 5 grams of glucose in 50 ml water, what is ratio percent? 100/0W/V
Examples: 50 g of glucose in a 1 kg glycerine, what is ratio percent7 5% W{W
Example: If 2% of glucose in water, what is ratio? 2g/l00ml = 1/50 = 1:50
12.5 grams glucose in 100 ml Water, what is ratio percent?= 12.5%w{v
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1.5%glucose in water = 1.5g!lOOml
2.5% glucose in 80 ml of water? Glucose? 2 'am
2.5g ------------- 100mI
?--------------80ml
Example: if 10%of dextrose in water, what is ratio? 19 :10ml W/V
if 50g/l glucose, what is ratio percent? 5%W/V
Example: 100g/1l water, what is ratio percent? 10%
= 5g/50 ml = 5:50 or 1:10
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Pharmaceutical sciences
50 grams of glucose in 1 L
= 50g/1L =50:1000 = 5:100 = 1:20
Example: Convert 5 grams of glucose. in 100 mL into percent?
5g/100mL. 100 = 5 W/V%
5 grams of in 1l water, what is ratio percent?
5/1000.100 = 0.5 W/V%
50 gram of glucose in 500 ml of water, what is ratio percent?
50/500.100 = 10 W/V%
5 grams of glucose in 500 mL water, what is ratio percent?
5/500 .100 = 1 W/V%
Convert 1O.grams of glucose in 10 ml into percent?
109/10mL = 100/1 = 100 w/v%
Two ratios with the same value are equivalent.
1/3 x 2/2 = 2/6 = 1/3
If two ratios are equal, then their reciprocal are equal:
If 1/3 = 2/6 then 3/1 = 6/2
Percent Calculations
Weight / weight Weight / Volume Volume / Volume
W/W% W/V% V/V%
Number of grams of Number of grams of Number of milliliters of
substance in 100 grams of constituent per 100 ml of a substance in 100 ml of
solvent or mixture. solvent. the solvent
1-How much drug should be added to 30 ml of water to w!;>solutiOn?
Solution:
22-7
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The mass of the final solution in this case in unknown, we only have the mass of solvent
(water) as 30 ml will weight 30 grams.
So know we need a solution which contains 10 grams (10%) of drug in 100 grams of the
solution (solvent + drug) r.G, _
In this case the solvent will represent 100 -10 = 90%
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So i(90% ~ 3 0 grams, how much is 10 %7
The weight of the drug is =10 30/90 = 3.33
Copyright 0 20002012 TIPS Inc. Unauthorized reproduction of this manual is strictly prohibited and it is 22-8
PhannacyPrcp.
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50 "'d
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1000
0
6'050 G-a
-jM)<.1
250 mL
O.02%w/v
o 02
11m
x 2S ml = 125 mg
x 100 =5%wjv
1.
Potassium permanganate
Purified water ad
1.
1,000 mg
x 1.000 mg
Solution:
0.02-7100 ml
SOmg x
1 mL
0.5
100 mL
2-What is the percentage strength of an injection that contains 50 mg of pentobarbital
sodium in each millilitre of solution?
Solution:
3-lf an injection contains 0.5% w/v of diltiazem hydrochloride; calculate the number of
milligrams of the drug in 25 ml of injection. \ ero y.rj -----;J 0, S ~
o . 0 D'S )( .2J;" = 6 . 1 'P" .v;- ----) L? J
Solution: :. I ~ S \IV'(j-
4-How many grams of potassium permanganate should be used in compounding the following
prescription?
Rx
Solution:
0.02. x 250 mL =0.05. =SO mg =SO, 000 ~
100 ml
Ratio Strength
I-Express 0.02% as ratio strength
For solids in liquids (w/v) For liquids in liquids For solids in solids (w/w)
I
(v/v)
Grams /1000 ml of mixture ml/lOOO ml of liquid Grams /1000 grams of Mixture
Or
Grains/lOOO grains of mixture
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20issolving 4.8 g of NaCI in water can make how many millilitres of a 1:1500 solution?
Solution:
_
tP
We have 1 gram for every 1500 ml of solution
So for 4.8 we will give x ml of solution
X ml =4.8 1500 /1=7200 ml
I 06..15 'fW1.-
M
. is an 85% wjv solution of sucrose in water. It has a density of 1.313 g/ml. How many
of water should be used to make 125 ml of syrup? (0 = W/V) . J
Working: (: inc.! $6/ vii = It<f .1.25
Density of solution =mass j volume
Density of solution = Weight of solution /125
Therefore the weight of the solution will be 164.125 g
Now we have 85 grams of sucrose in 100 ml of solution
Therefore for 125 ml of solution we need: (125 *85)/100=106.25 grams the weight of
water in this solution =164.125 -106.25 = 57.875
Proportions: (two ratios): relation of two ratios is the proportion
Parts Per Million (ppm)
Example: How many mg (?) of glucose in 500 ml if this is a equal to 1 g in lOOOml of water
j 't" (P U" k..-o-
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o' 5 t"" =so-o "1
Occasionally, you will see a number followed by the term "ppm." This stands for "parts per
million" and is most often used to indicate the amount of trace substances in water. The
standard dilution for fluoride added to a municipal water source, for example, is 1ppm. In
every 1,000IOOO.JTl1 of water, therefore, there is 1 g of fluoride.
, I-Express 5 ppm of iron in water as ratio strength and in percentage strength
Solution: 5 ppm = 5 parts in 1,000,000 parts
Ratio strength: 5: 1
1
000,000 = 1: 200,000
Percent strength: 5 x 100 = 0.0005%
1,000,000
Express 10 ppm, in percent strength? 0.001%
10:1,000,000 = 0.001%
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illegal to reproduce without pcnnission. This maJiual is being used during review sessions conducted by
PhannacyPrcp.
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ftelu.. = lin>
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_'Oil ;:. /O''1g /
"l J0
0.0005 x 1000000 =5:1000000
100
D=W/V
900 mL x 0.9 g/mL =810 g
81Og+100g =910g
100g/910g .100 = 10.9%
Express 0.0001% in how many ppm? Ippm
www.pharmacypreoocom
Express 0.023% of iron in water as ppm? B-
2-lf 500 ml of a 1$% v/v solution is diluted to 1,500 ml, what is the resultant percentage
strength?
Ql (quantity) x (1 (concentration) = Q2 (quantity) x C2 (concentration)
51rtlf. 6tS - ,,/S
"15' XI0-0;: 5' /- "/V
/5!JO
500 (mL) x 15 (%) = 1,500 (mL) x1 (%)
1,500 x = 7,500 I c.l =itt 6L.-.-
x = 7,500 /1,500
x=: S%v/v
Q1 X(1 =: Q2 X(2"
100 (mL) x 65% = x X(%)
85x =6,500
Copyright 0 2000-2012 TIPS Inc. Unauthorized reproduction of this manual is strictly prohibited and it is 22) 0
PhannacyPrep.
2-Express 0.0005% of iron in water as parts per million (ppm)? 5 y '(r
f----,-:----,------,------,--------,-----,--,-----:c-,-------
containing 65% w/v of sucrose is evaporated to 85% of its volume, what percent of
V sucrose will it contain? Note: any convenient volume of may be selected, say 100 ml.
Then, 85% x 100 ml =: 85 ml (Q2)
o fi-A parenteral solutions used in TIPS pharmacy. If g.of parenteral solution dissolved in
fV 900 mL of petrolatum (Density of petrolatum is 0.9 gfml), the concentration of parenteral
solution is:
Solution:
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x= 76.47% wjv
{cD

Qlx (1 =Q2 XC2
3,785 (mL) x 30 (%) = x (mL) x 50(%)
4-lf 1 gallon of a 30% wjv solution is evaporated so that the solution has strength of 50% w/v,
what is its volume in milliliters? "I 0,311"
Solution: -
,
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x =2,271 mL
pharmacist mixed 100 ml of 37% wjw concentrated hydrochloric acid (specific gravity,
t> 1.20) with enough purified water to make 360 mL of diluted acid. Calculate the percentage
strength (wjv) of the diluted acid.
100 ml x 1.20 (specific gravity) =120 g of concentrated acid
120 g x 37% w/w = 44.4 g HCI
44.4 g x 100 =12.33% w/v
360 mL
Drug Strength Expressions
Units (International units):
Some examples of drug measured in international inits (IU)
Insulin, Penicillin G, Vitamin K, Vitamin E, Vitamin A, Vitamin D, Heparin, LMWH (Fragmin),
interferon alpha, Nystatin, Polymixin, and Bacitracin.
U-100 insulin contains 100 unitsjmL
Rx
Insulin 40units
For 60 days and bid.
, How many ml of insulin you dispense?
Solution:
1 ml x 40 units = 0.4 ml
100 units
For 60 days and two times a day = 48 mL
2-How many milfilitres of a heparin sodium injection containing 200,000 heparin units in 10
ml should be used to obtain 5,000 heparin units?
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illegal to reproduce wilhout permission. This manual is being used during review sessions conducted by
PharmncyPrep.
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S-A 20-ml vial of biologic solution is labeled "2.0 megaunits." How many units of drug are
present in eve'):.ml of solution? 21-lOb
A-2ooo8-1DOqyJ-00,OOD D-lO,ooo iii 0 - 100,00'-'
I 6-A prescription calls for 10 units of a drug to be taken 3 times a day. How much will the
patient have taken after 7 days?
A-21.0 units B-0.21 units C-2.10 units @210units
How many grams of
(/?
-
500
@give }S tablet C-give 1 tablet
How much is to be administered if the dose on
Practice calculations
solution:
10 ml x 5,000 units = 0.25 ml
200,000 units
2-An elixir is to contain me of an alkaloid in each teaspoonful dose.
the alkaloid will be required to prepare 5 liters of the elixir? O. 50
A-D.25g 8-5g @2SDgD-2.5g ?
3-A pediatric product contains loomg of erythromycin ethylsuccinate in each dropperful
(2.5ml) of the product. How many kilograms of erythromycin ethylsuccinate would be
required to prepare 5000 bottles? O.ldlJa" (1 j
A-74.6 kg 8-84.6 kg C-99.5 kg kg 01." 2 3( ,.00
I-In dosing the drug gentamicin in pediatric patients, for every 1 mg/kg of gentamicin
administered, serum drug concentrations are expected to increase by 2.$ ll&/mL What would
be the expected serum drug concentration following an administration of a 2.5 mg/kg dose of
gentamicin?
A-S 06.25 C-lO D-2.5
,
4-A physician places a patient on a daily dose of 48 units of U 80 insulin (80units/mL). How
many ml should the patient inject each day? t..<{
@
'dOll , _
A-OA mL B-O.5 mL 0.6 mL 0-0.25 mL - 19. J
.:1...,
7-A physician orders Meprobamarp.o.2 g.
hand is 400 mg. in each tablet?
A-do not dispense Bgive 2 tablets
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PharmacyPrep.
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70 X ().

8-The usual initial dose of chlorambucil is ug per kg of body weight once a day.
many milligrams should be administered to a person weighing 154Ibs.?
010.5 mg B-18 mg (-15 mg D-8 mg
How
D-21.2 ml
."-
9-An initial heparin dose of not less than 150 units/kg of body weight has been recommended
of open heart surgery. How many ml of anTnjection containing 5000 heparin units per
milliliter should be administered to a 300 pound patient?
A-5.11l1 B-4.1111 (-5.1 ml @1--.1 ml
lO-The pediatric dose of cefadroxil is 30 mg/kg/day. If a child is given a daily dose of 2
teaspoonful of a suspension containing 125 mg of cefadroxil per 5 ml, what is the weight in lb.
of the child?
A-19.5lbs. B-18.8Ibs. @18.3 Ibs. D-18.1Ibs.
ll-If the loading dose of Kanamycin is 7 mg/kg of body weight, how many grams should be
administered to a patient weighing 130 Ibs.?
A-0.492 g @-0.414 g (-414 g D-0.485 g
12-The adult dose of a liquid medication is 0.1 ml/kg of body weight as single dose. How
many teaspoonfuls should be given to a patient weighing 220 Ibs.?
02 tsp. B-2.5 tsp. (-2 tbsp. D-2.5 tbsp.
13-lf a prescription order requires 25 g of concentrated HCI (Density 1.18g/m1L what volume
should the pharmacist measure?
G29.50 ml B-0.0212 ml C-23.0 ml
14-lf the dose of a drug is O.5mg/kg body weight/day, how many mg will a 351b infant receive
per 24hours?
@7.9 mg B-7.1 mg C-7.2 mg D-7.4 mg
15-What is the weight of 60 ml of oil whose density is 0.9624 g/ml?
A-5.770g @57.7g C-6.0gD-0.577g
16-A prescription calls for 0.3 g of phosphoric acid with a specific gravity of 1.71.
milliliters should be used in compounding the prescription? .
,A-0.5 B-0.7 @0.18 D-O.3 -=
How many
17-How many ml of 0.9% (wjv) NaCI solution should be prepared from 250 ml of 25% (wjv)
solution? y '2. r!1,
A-3750 B-25006944.4 D-9 .
18-A patient is determined to have 0.8 mg of glucose in each milliliter of blood. Express the
concentration of glucose in the blood as
A-800 mg% B-0.8 mg% C-8 mg% mg%
PharmacyPrep.
28-Calcium Hydroxide Topical Solution contains 170 mg of calcium hydroxide per 100 mL at
1$2 C. Express this as a ratio strength. ",.'!1-/o."... tcr6/" 101\:>
A-I: 688 Bl: 888 C- : 588 0-1: 788 ._-_.-
/61>/"_1':10
29-How many mg of isofluorophate are contained in 15 g of a 1: 10,000 ophthalmic solution
of isoflurophate in peanut oil?
A-1.7 mg B-1.9 mg C-1.8 mg @1.5mg
27-How many grams of a drug are required to make 120 mL of a 25% solution?
830g BlO g C-12.0 g 0-12 g
/0
O. fDo'\.
0 2
2
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-
0'0
-/ .. 0
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24-Change to percent the number 1/300.
A-3% 833%
23-How many grams of dextrose are required to prepare 4 liters of a 5% solution?
A-0.2g 0)200g C-2g D-20g
26-How many grams of potaRum citrate are needed to prepare lliter of 10%7
AlOoo g B50 g g 0-10 g
3D-Express 0.2 % in a ratio
A-I: 5000 B-1:50 191: 500 0-1:5
21-Strong Iodine Solution U$P contains 5% w/v iodine. How many mg of iodine are consumed
daily if the usual {:Jose is 0.3 ml t.i.d.?
A-IS B-90 C-22.5
19-How many ml of a 1;400 (w/v) stock solution should be used to make 4 liters of a 1:2000
(w/v) solution? I.' 4u: C.2 S -t kJ/v I
A-lOOOml B-200ml @SOOml D-l600mL I 2000" 0,0)'+ ""/1/
22-Express in percentage the fluoride concentration in drinking given in 0.6 ppm.
A-0.06% (9.00006% C-0.0006% D' , I< I""
I 00l> 0 l6'"
25-A Pharmacy tech adds 75 ml of strong iodine solution USP (5.0% w{v) to 1 liter of sterile
water for irrigation. What is the % w{v of iodine present? D' ..-_
B-0.375% C-0.53% D-0.60%
a patient is determined to have 100 mg % of blood glucose, what is the eqUiValen

y
,
(). concentration in terms of mg/dl? \ 0-0 IN1j = 10-0 ttv1 1 d L
A-I B-I0 C-40 (9100 !()1)
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31-How much of a substance is needed to prepare 1l of a 1: 10,000 solution?

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'j I, #.

c-omg 0-1.0 g
32-A,i:upric chlorid
r
injection (0.4 mg Cu/ml) is used as an additive to IV solution for TPN.
w/'ff)t is ttie final ration strength of copper in the TPN solution if 2.5 ml of the injection is
to enough of the IV solution to prepare 500 ml?
A-i;600 .. B-1:SDOO 0: 500,000 0-1: 50,000
. , V
t.. oJ> 3- ow many milliliters of a 23.5% (w/v) concentrate of Sodium Chloride solution should be
"J;l;"ol!d in a stock solution such that 30 ml diluted toSwill yield a 1: d .1"'-'"
5dQO solution?' (J. 6 '1c /- 3 !".
A-0.2ml B-4.33ml (0.8.44ml 0-1l.75ml .. 0.1 ....,
'n..... J....... 'SO
34-You have a stock solution of 50% Sodium citrate and you were asked to prepare 300 ml of
a 10%solution. How ml is needed? "";>_0
A-20 8-15 C-30 (9160 70.... +']., q0
/"' .... ,
0-642.86 g (-50,400 g
38-The only source of Sodium Chloride is in the form of each containing 5.0 g. How
many tablets should be used in preparing 3000 litres of a solution of such strength that 20 ml
diluted to 100 ml with water will yield a 0.9% (w/v) solution? 0'" _,
A-GO,ODD tablets {!)-7,OOO tablets C-12,OOO tablets 0-9,000 tablets i>
- 39-How many grams of 10%(w/w) ammonia solution can be made from 1800 g of 28% (w{w)
strong ammonia solution?
A-6428.57 g @040g
_ ?7-HOw many milliliters of 24% (w/v) concentrate of saline solution should be used in
V 600 ml of a solution such that 10@ilutedtoaliterwill
Y
ieldao.09%SOlutiOn?
A-300 ml B-150 ml (-50.0 ml 0- 25 ml , A "- 6
.J v..... "1) 'b_
35-How many milliliters of 1:16 solution of sodium hypochlorite should be used in preparing
5,000 ml of a 5% solution of sodium hypochlorite for irrigation?
A-800 ml B-2500 ml <?;}4000 ml 0-300 ml \15-"
o 6'''.1 ,i _ () ,
3G-Prepare 1000 ml of KMn04 1:.12,000 compresses out of KMn04 1: 8,000.
.,4' A-Add 333.3 ml water to' 1000 ml KMn04 1: 8,000
B-Add 666.6 ml water to 333.3 ml KMn04 1: 8,()(X)
333.3 ml KMn04 1: 8,000 and enough water to make final volume 1000 mL
333.3 ml water to 666.6 ml KMnO" 1: 8,()(X)
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Dilution, Concentrations
23
,.
Dexamethasone is available as 47g/mL preparation; in infant is to receive mg.
Prepare a dilution so that the frna concentration is Img/mL. How much diruent will y.ou
need if the o'riginal product is in a ImL vial and you""USe'The full vial?
A-4ml ,-:: 'Irl>'j', - (]:) )(
'" ,-' -
C-I mI["" f:-. <r-J>..1. diJ>I' J,.",
D-O.35ml -'-----. _
Stepl: detennine the volume of final product. Since dexamethasone is 4mglmL, a I ml
vial have 4mg of drug
Imlllmg
JI1
/3.f.
1
It M ;

C,Q,
so 0.25% x 30g = 0.1 % x g?
g? = 0.25% x 30g1 0.1% = 75 W
bu't the added tube contains 30 gm
so the used base = 75-30 = 45 gm'
Questions Alerts!
"
Common questions in pharmacy exam is to ask]
Dilution from Stock
Using Allegation methods to prepare ointments
Most commonly dilution and concentration can be solved by -inverse proportion method
and by detemlination or ratio strength. The reliowing fannula can be used
to calculate dilutions and conc(ntrations:
Ql (quantity) X C
1
(concentration) = Q2 (quantity) X C
2

Or
We can use the equatiol1 =C,* V1= C2 .. V2
, / A prescription for hydrocrotisone cream 0.1 %: phannacy have 0.25% available in 30 g
../ tube. How many grams diluents base (vanishing cream) should be
A-30g B-45g C-50gD-75g E-25g
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Step2: substract the volume of concentrate from the total volume to determine the amount
of diluent needed.
4ml-Iml = 3rnL
I-If a 600 ml of a 15% (v/v) solution of methyl salicylates in alcohol are diluted to 1500
ml what will be the percentage strength.
QI * C1=Q2 * C2
C
2
=Q2/QI *C.
I500mL = 15% = 6%
600 mL X%
2-If a potassium chloride elixir contained 20 mEq of potassium ion ineach 15 mL of
elixir, how many milliliters will provide 25 mEq of potassium ion to the patient?
Solution!Answer:
20 mEg 25 mEg
15 mL x mL
. x= 15 x25 x= 18.75 mL
20
3-How many grams of dextrose are required to prepare 4,000 mL of a 5% w/v solution?
Equivalent factor: a 5% w/v solution =5 gin 100 mL of solution. ~
~ 0-00;>< 0, oS ~ (j..)J'/r.7
SoIution!Answer -=::::::::.--
~ x 4000 mL = 200 g -------=--
100 mL
-
.,..
~ tt ~ Q, Ct.-
400
0
)(.()'O)
~
1000 mL
Solution!Answer: 1:500 = 0.2%
4 liters = 4000mL
1:2000 = 0.05%
0.2% = 4000 mL
0.05% x mL
Calculations involving dilution and concentration of Stock solutions
A solution of known concentration that is prepared in the most concentrated form is
referred as stock solutions. Sometimes a stock solution will be pure drug in powder or
crystalline form. At other times it will be a liquid or a solid paste or cream.
er 'l-+
I-How many mL of a 1:500 (w/v) stock solution should be used to make 4 liters of
1:2000 (w/v) solution?
bd)
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Allegation medial: a method for calculating the average concentration of a mixnlre of
t\VO or morc substances.
I"
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e-........-

}'\c1.
M-DxV
M 1.25 x 1000 mL 1250 g
250 g+1250 g 1500 g (total volume)
250gl1500 g 100 16%
Allegation Method
Then
2-A parenteral solutions used in hospital phannacy.lf250 g ofparenlcraJ solution
dissolved in 1000 mL of glycerin (density of glycerin is 1.25 g1mL), the concentration of
parenteral solution is:
Solution/Answer: D = MN
Allegation alternate: a method of calculation of the number of parts oftwo or morc
components of known concentration to be mixed when the final desired concentration is
known.
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Therefore the percentage is 35/350=10%
Ointment mixture of 15 g of 70%. 5g 0[90%. 109 of40%, 5g of 10%, what is final

36

Qo +10-t:)
35D
I-What is the final percenlage of ZIlO ointment made by mixing ZIlO ointment of the
strengths?
200gof10% +50gof20%+100gof5%
Solution:
+20010%=20+
+50 20%=10+
+1005% = 5+
Therefore we have 350 gram ohhe ointment which contain 35 gram of ZnO
concentration ofthis mixture?
Ans: 55%
, 15g+5g+lOg+5g 35g
70%+90%+40%+10% =
10.5+4.5+4+0.5 19.5/3 g x 100 - 55%
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2-Which proportion of95% alcohol and 50% alcohol should a solutIon
of500 mL of70% alcohol? e.V:> 1.
Solution: .
95%
----........
50% ---
the final proportion is 20:25
20 parts of 95
70%----........
25 parts of50%
-
Constituted solutions, and intravenous admixture
Constitution of dry powder to oral solutions or oral suspensions
Type 1: concentration after constitution:
The label for a dry powder package penicillin V potassium for oral solution directs. The
phannacist to dissolve the powder in the container with sufficient purified water to make
200mL solution. If the package contains 5 g of penicillin V potassium. How many
milligrams ofthe penicillin V potassium is present in each teaspoonful dose ofthe
resultant solution? D. 02.(,1"11--1'" R..S ""1
Type 2: volume of dry powder and total drug content:
Label for an ampicillin antibiotic states that the addition of78 mL of water to make
IOOmL of constituted suspension such that each 5 mL contain 125 mg ofAmpicillin?
What is the volume of dry powder? 2
What is the total Ampicillin present? 62EO'O
Type 3: Modifying Label instruction to obtain desired concentration
From the previous calculation a physician, 'wants Ampicillin concentration of IOOmg/5
mL (ralher than 125mU5mL), how many millilitres of water should be added to the dry
powder? Iaa..-l <4 -; or 01Tll , ,
5"00 "'1 occ."-P"J -> 2.2.."'" ,",I' lN1 <f. AiM '.
II ""'1 t,...\0 I b -D "'-<J'r
T pc 4: onstitutiorJIbased on dosage calculation ofweigbt
o . The label ofa dry powder for oral suspension states that when lJ J mL of water are added
to the powder 150 !TIL of a suspension containing 250mg/5mL ampicillin are prepared.
How many mL should be used to prepare a suspension, which would contain a dose of8
mg/kg per 5 mL. to be given to a child weighing 60 Ibs. 'l 'l Ii.. <it I ._i
-P"/ Solurion: 2./ . I .' (j S ....)
<a) Evaluate data l, 3'b) If..tiJj H
Child weight 60 Ibs 27.7 kgs.
Dose (per 5mL) required for this child is 8 x 27.27 = 218.2 mg/5mL ( =43.64mg/mL)
Unreconstiluted bottle contains(250/5) x 150 = 7,500 mg ampicillin
-
234
23-5
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From the data given, 111 mL of water are required 10 produce 150 mL of suspension.
This means that the dry powder occupies (150-111) = 39 mL
(b) Calculate
For a dose of43.64 mglmL, the bottlc must be diluted to a volume of (7,500/43.64) =
171.8 mL
But from (iv) we know that the dry powder occupies a volume of39 m!
Therefore, the volume of water required is 171.8 - 39 = 132.8
Dry powder for parenteral usc
Type 5: Solvent needed to produce desired concentration when dry powder docs NOT
contribute to final volume?
13. Using a vial containing 200,000 units of penicillin G potassium how many mL of
solvent should be added to the dry powder to prepare a solution having a concentration of
25,000 units per mL.
Solution:
vial contains 200,000 units of penicillin G
Each mL of reconstituted solution will contain 25,000 units. Therefore, you will need
(ln5,000) x 200,000 "" 8mL to produce a solution containing 25,000 units / mL
Type 6: Solvent nceded to produce desired concentration when dry powder does
contribute to final volume?
l1le package inronnation enclosed with a vial containing 5,000,000 units penigllin G I
P ssium specifies that when 23mL ofa sterile solvent are added to dry powder the
sultant concentration is 200,000 unitsimL. On the basis of this information, how many
mL of sterile water injection should be used to prepare a solution containing penicillin G
potassium 500,000 unitslmL?
Solution:
vial contains 5,000,000 units of penicillin G
23 mL are used to prepare a solution ofconcentration 0[200,000 unitslmL. Since no
drug is removed from the vial (and it therefore still contains a total of5,OOO,000 units),
the total volume inside the vial is 5,000,000/200,000"" 25 mL This means that the
volume of powder occupies 25-23 "" 2 mL
to dilute the vial to produce a solution whose concentrations is 500,000 unitslmL J need
[0 be diluted to 5,000,000/500,000 ~ 10 mL
From (ii) we know that the powder occupies 2 mL of volume. Therefore the amount of
sterile solvent requested is 10-2"" 8 mL
Intravenous admixtures
A medication order for a patient weighing 154 Ib calls for 0.25 mg of amphotericin B per
kg of body weight to be added to 500 mL ~ dextrose injection. If the amphotericin B
is to be obtained from a reconstituted injectibiJ that contains 50 mg per 10 mL, how many
milliliters should be added to the dextrose injection?
q 5" ~ -7 ')t>O 11 '1 ':)f ~
Solution:
I kg::: 2.2 Ibs
154(lb) = 70 kg
2.2 (lb)
0.25 mg x 70 = 17.5 mg
Reconstituted solution contains 50 mg per 10 mL
"
50 (rog) =
17.5 (mg)
10 (mL)
x (mL) x = 3.5 mL, answer
An intravenous infusion is to contain 15 mEq of potassium ion and 20 mEq of sodium ion
in 500 mL of 5% dextrose injection. lJ'Sifffan injection of potassium chloride containing
6 g per 30 mL and 0.9% injection of sodium chloride, how many milliliters ofeach
should be used to supply the required ions? .
Solution:
15 mEq ofK+ ion will be supplied by 15 mEq ofKCI
and
20 mEq ofNa+ ion will be supplied by 20 mEg ofNaCI
I mEg ofKCl = 74.5 mg
15 mEg ofKCI = 1117.5 mg or 1.118 g
6 (g)
1.118 (g)
= 30 (mL)
x (mL) x =5.59 or 5.6 mL, and
1 mEg ofNaCI =58.5 mg
20 mEq ofNaCI = 1170 mg or 1.170 g
0.9 (g) = 100 (mL)
1.17 (g) x (mL) x = 130 mL, answers.
Amedication order for a child weighing 441h calls for a polymyxin B sulfate to be
administered by the intravenous drip method in a dosage of7500 units per kg of body
weight in 500 mL of 5% dextrose injection. Using a vial containing 500,000 units of
polymyxin B sulfate and sodium chloride injection as the solvent, explain how you would
obtain the polymyxin B sulfate needed in preparing the infusion.
I kg = 2.2 Ib
23-6
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2.2
7500 units x20 = 150,000 units
Step I: Dissolve contents of vial (500,000 units) in 10 mL ofsodium chloride injection.
Slep 2: Add 3 mL of reconstituted solution to 500 mL of 5% dextrose injection, answer.
Pa.renteral nutrition's
The following is a fannula for a desired hypcralimentation solution. Using the source of
each drug as indicated; calculate the amount of each component required in preparing the
solution.
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Hyperalimentation Solution
Formula
(a) Sodium Chloride 35 mEq
(b) Potassium Acetate 35 mEq
(e) Magnesium Sulfate 8 mEq
(d) Calcium Gluconate 9.6 mEq
(e) Potassium Chloride 5 mEq
(I) Folic Acid 1.7 mg
(g) Multiple Vitamin Infusion 10 mL
To be added to:
Amino Acids [nfusion (8.5%)
Dextrose Injection (50%)
5 (mEg) - 2 (mL)
35 (mEq) x(mL) x ~ 14mL,and
Component
Vial. 5 mEq per 2 mL
Vial, 10 mEq per 5 mL
Vial, 4 mEq per mL
Vial, 4.7 mEq per 10 mL
Vial, 40 mEq per 20 mL
Ampul, 5 mg per mL
AmpullOmL
500mL
500mL
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35 (mEq) x (mL) x ~ 175 mL, and
4 (mEg) - I (mL)
8 (mEq) x (mL) x ~ 2 mL, and
4.7 (mEg) - 10 (mL)
9.6 (mEq) x (mL) x ~ 20.4 mL, and
40 (mEg) - 20 (mLl
5 (mEq) x (mL) x ~ 25 mL, and
23-7
1.49 (g) x (mL)
15 (g) = 100 (mL)
198/20 =9.9 mL, and
5 (mg) = 1 (mU
1.7 (mg) x (mL) x =0.34 mL, and
10 mL, answers.
The fonnula for a TPN solution calls for the addition of 2.7 mEq of Ca++ and 20 mEq of
K+ per liter. How many milliliters ofan injection containing 20 mg of calcium chloride
per mL and how many milliliters of a 15% (w/v) potassium chloride should be L
used to provide the desired additives? MAL lJ'1
Co---CI.,( 2. -;- V-'Z
, ,. L l -) l / " -CJ).5 ;}-
Solution: <-- e"l v {,J-1 /2-
1 mEq ofCa++ =20 mg
2.7mEqofCa++=20mgx2.7=54mg <. I -= '135
++ looe C73 ,5 'Jt.lL..
54 mg ofCa are furnished by 198.45 or 198 mg of calcium chloride ::. I ..
Since the injection contains 20 mg of calcium chloride per mL, then
, . l M-lI<y 'Zo -5
.2. 7 YtI(4-" = /q-g .
'. f
I mEqofK+=39mg IGf<l.4S' Wj.1) Cacli have- -) 27
fn
C=$ c.qt"
20 mEq ofK+ =39 mg X 20 =780 mg N.a.
. 27 mc"\. C I
780 mg ofK+ are furnished chloride 15% (w/v) solution contains
15 g of potassium chloride then 'to"',w l<cl '-t S
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P2tassium phosphate injection contains a mixture monobasic potassium

,C) phosphate (Kl-hP0
4
) dibasic potassium p osphate (K2HP0
4
) per mL. If
10 mL of the injection are added to 500 mL ofD
5
W (5% dextrose in water for injection),
(a) how many milliequivalents ofK+ and (b) how many millimoles of total phosphate are
represented in the prepared solution?
Formula weight of KlhP0
4
= 136
1 millimole (mmol) ofK.H
2
P0
4
= 136 mg
10 mL of injection contain 2240 mg ofKlhP0
4
and thus provide 2240 /136 = 16.4 or 16 mmol ofKH
2
P0
4
or 16 mmol ofK+ and 16'mmol ofH
2
P0
4
Formula weight ofK
2
HP0
4
= 174
1 millimole (mmol) ofK
2
HP0
4
= 174 mg
10 mL of injection contain 2360 mg ofK
2
HP04
and thus provide 2360 /174 = 13.6 or 14 mmol ofK
2
HP0
4
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= active ingredient (to be administered)
solution (needed)
mEq = Molecular Wcight
Valence
Mole = molecular weight in grams
One mole ofNaCI = 58.5 g
One mole ofKCI = 74.5 g
One mole of HCI = 36.0 g
One mole ofNa
2
C0
3
= 106.0 g
or 14 (mmel) x 2 (KJ;= 28 mmel arK+, and 14 mmol thus 10 ml of injection
-0 2.'" 't.-
provide a total of: I M '1 z.",Sllt, 1Jlz.
44 mmo! arK+ or {since the valence orK+ is I) 44 mEq arK+ and e..q V-' I/"J. ....., I ",g 0,; 5
30 mmol or total phosphate, answers. , .1 :. 1 w:d-
Calculating active drug moiety :.-, J.. 'fJ" I \J." ;: r3q2 .17
Type I: Calculating weight of constituent given weight of
1. A prescription calls for 220 mg ydroU5 sui fat . However your phannacy have
ZinC sulfate he tally rate:fo reCClV t e eqUlva ent amount of elemental zinc, how many
illigrams of zinc SU 'ale heptahydratc (.71-1
2
0) would be patient need to take? (MW:
zinc 65, ZnSO, 161, H,O 18). _ 3'11. '17 "'(l-
2-Recommend equivalent alternate dose of oral iron to provide all equivalent amount of
elemental iron as FeS04.7H20 300 mg lid. Your pharmacy haye Ferrous gluconate and 271 9 r---
Ferrous Sulpahte heptahydrate. -.., 1t:r1t:J . I 7I-ho "" 13.g.Q.s-
Solution: ' f'(\(-ev :.. \3 g. 5
Molecular wt or atomic wt are: t9 ) ;110 e.-v;
V" Ferrous gluconate (FeC12H"O,,) = 446 4'0 'f"><l""'"
Ferrous Sulpah!e heptahydrate (FeS04.7H20) = 277.9 (,. M "}
Iron (Fe) = 55.8
The equivalent iron dosage to be administered daily as the giliconate salt would be
approximately what?A /4 L,';: 0 4
pr
Calculation involving electrolyte solutions
Reference atomic weights: Na = 23, C = 12, 0 = 16, K = 39, CI = 35, Ca = 40
I-The amount of solution needed can be detcnnined by setting the two ratios equal:
active ingredient (available)
Solution (available)
2-

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3-Converting between milligrams (mg) and milliequivalent (mEq)
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Number of rnEq = Weight of substance in mg
mEq weight
4-
Molarity
Molarity is the expression of the number of moles of solute is dissolved in litre of
solution. Molarity can be calculated by diving the moles of solute by the volume of
solution in litres.
One mole dissolved in 1liter solution is 1M.
1M HCl = 36.5g ofHCI dissolved in IL
1M NaCI = 58.5g ofNaCI dissolved in lL
One mole of substance dissolved in a liter solution
Molarity = molecular weight in grams
Litres
Imolar NaCI = 58 grams in litre
/
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I-To prepare 100 mL of 1M NaCI, how many grams ofNaCI (Mol. wt ofNaCI = 58.5g)
needed?
Solution:
58.5 x 100 = 5.85g
1000
2-To prepare 28 mL ofO.5M NaCI, how many grams ofNaCI needed? (M. Wt ofNa =
58.5) 58 .5 fr"> /1 --;) M NO cl
2. q9. 5 / L 1\.--1 6 S- 1"1 l'f 4 C./
Solution: 58.5/2 = 29g
29/1 000 x 28 mL = 0.8g

23-10
D-33.2 mEq E-66.6 (96.6mEq
I-How many mEq of magnesium sulphate are represented in 1 g anhydrous magnesium
sulfate? (M. wt ofMgS0
4
=120)
A-120 mEq B-166 mEq
mEq
Ans:B
Tips:
I g = 1000mg
mEq = (weight) (valence)
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Molecular weight
(1000 mg) (21 - 16.6 mEq
120
2-A solution contain 10 mg% ofCa
2
-+-, describe this concentration
weight = 40 and valence = 2 Q. l........
j M \-Iv" "'tI0 G;
10 mg% is = 10 mgllOO ml Il-
10 mg% for IL is 100 mgiL l./ / (11)'0
_
mEq/L = (mgIL)(valencel
atomic weight
MglL=1..lL-147= 294mg= 0.294g/L=0.002g1mL
2
3-What is the concentration in g per ml of a solution containing 4mEq of calcium
chloride (CaCI, x 2H20) M. wI = 147
ImM 24g11 000 0.024 g = 24 mg
(J 00 mgIL)(2) = 5 mEqlL
40mg
Magnesium has an atomic weight of24', whal is weight of I mmol?
Millimole (mmol) I L = molecular wi in milligrams
Litres
Immol afNael solution contain how many milligram of sodium chloride? 58.5 mg IL
I mmol of 100 mL NaCI contain how many milligram afNae!? 5. 8 mg
0.5 mmol afNael contain how many milligram afNael? 29 mg
Normality
Equivalent wt dissolved in J L
A method ofdealing with acids, bases, and electrolytes which involves the use of
equivalents. One equivalent of acid is the quantity oflhat acid that supplies or donates of
mole ofH" ions. One equivalent of base is quantity that gives off one mole of01-1- ions.
One equivalent ofacid (I-(-+-) reacts with one equivalent of base (OHl
Equivalent can be calculated for atoms or molecules.
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Equivalent wt = M. wt in g
Valence
IN HCI = 36.0 g ofHCI dissolved in lL
The salts with valence 1 have the same molarity and nonnality. The valence in salts is
referring to metal ions.
The salts with valence 1: .NaCI, HCI, KCl, LhC03, Na2C03, NaHC03
Thesaltswit:h. valence 2: CaC03, CaCI
2
, MgCb, Mg (OHh, ZnCb
The salts with valence 3: AI, citrate
One mole ofNaCI contain one equivalent ofNa+ (Na mol. weight 23 g)
One mole ofNaCI contain one equivalent ofCr (Cl mol. Weight 35 g)
0.9 % NaCI contain 0.9g ofNaCI in every 100 mL
0.9% NaCI contain 9 g ofNaCI in every Hiter
MilliEquivalent: The amount, in mg, of a solute equal to 1/1000 of its gram equivalent
weight per unit volume;'
mEq = molecular weight
valence
Converting rnilliequivalents per unit volume to weight per unit volume
mEq = [mg x valence]/(mol.wt)
mg = [mEq x (mol.wt)]/valence
Sodium atomic weight is 23 and valence is 1. How many milli equivalents are in 92 mg
ofNa?
Number of mEq =weight of substance in mg
mEq weight
92/23 =4mEq
1-What is the concentration in mglml of a solution containing 2 mEq of KCI per
milliliters?
m. wt. OfKCI = 74.5 g
Eq. wt. ofKCI= 74.5 g
lmEq. ofKCI = (1/1000) * 74.5 = 0.0745 g =74.5 mg
2mEq. OfKC1= 74.5 mg * 2 = 149 mglml
OR
mglml =2 (mEq/ml) * 74.5 = 149 mglml
2- What is the concentration, in grams per milliliter of a solution containing 4 mEg. Of
CaCh.2H
2
0 per milliliter?
Fonnula weight ofCaCh.2H20 = 147
Eqo wt. OfCaCl
2
.2H
2
0 = 147/2 = 73.5
1 mEq. CaCl
2
.2H
2
0 = (1/1000) * 73.5 g = .0735 g
4 mEq. Of CaCh.2H
2
0 = 0.0735 g * 4 =0.294 glml
23-12
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OR
by mg/ml: [4' (mEq/ml)' 147] / 2: 294 mg/ml: 0.294 g/ml
Converting Milligram % to mEqlL
I-A solution contains 10 % mg% ofK+ions .Express the cone. In terms ofmEqlL?
Solution:
Atomic weight ofK+ = 39
Equivalent weight of K+- = 39
I mEq. OrK: 111000' 39 g: 0.039 g: 39 mg
10 mg%ofK += 10 mg K'" per 100 ml
= 100 mg per liter
100 mg , 39 : 2.56 mEq/L
Or
MEq/L: [100 mgIL' 1J /39: 2.56 mEqlL
3-A solution contains 10 mg % orCa ++ ions .Express this concentration in tenns of
mEqlLiter
mEq/Liter = [100 rng IL *2 ] 140 (atomic weight orCa ")
Converting weight to milliequivalcnts
I-How many mEq. Of KCL are represented in a 15 ml dose of 10% w/v KCL elixir?
Malec.weight KCI ~ 74.S g
Solution:
Equivalent weight = 74.5 g
I mEq ofKCL = 0.0745 grams =74.5 mg
15 ml dose of 10 % w/v elixir = 1.5 gor 1500mg KCL
74.S mg - - ~ I mEq
1500 mg - - ~ x x = 20.1 mEq
/MilliosmOle
It is the unit of measuring the osmotic concentration. Osmotic pressure is directly
proportional to the number of particles in the solulion.
smotlc pressure ce urn r 0 Particles in solution
OsmoVL = wt. Ofsubstance in giL X number of species
Molecular weight in g
23-13
mOsmollL = WI. Ofsubstance in gil x number of species x 1000
Solutes, which dissociate exert osmotic pressure based on the number of particles present
in the solution after they have dissociated.
Some Example salts:
For NaCl, the number of species =2
NaCI Na+ +cr
For CaCl
z
. the number of species = 3
CaCI2 -7 Ca
2
+ + 2Cr
For LjzCO
J
the number of species = 3
LjzCO
J
2Li + +CO
J
2-
For MgS0
4
the number of species = 2
For Solutes which do not dissociate, the milliosmole = millimole
I-solution contains 5% anhydrous dextrose in water injection. How many miIliOsmoles
per litre are present in this concentration? (M. wt = 180 g).
Solution:
mOsmollL 2Qu..1 x 1000 278 mOsmollL
180
Note: dextrose, gluconate are examples of substances that do not dissociates. However
salts dissociates into ions.
2-How many milliosmoles per litre are present in 0.9% NaCI solution.
Solution:
0.9% NaCI is 0.9g in 100ml, however, solution in one litres, thereby NaCI concentration
is 9g
9 x 2 x I000 307 mOsmol1L
58.5
Isotonic solutions preparations
Isotonic "Nonnal saline" and is 0.9% NaCI concentration
Hypotonic7 Less than 0.9% NaCI concentration
Hypertonic More than 0.9% NaCI concentration
23-14
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Tonicity is affected by number of particles in solution.
Substances that dissociate have greater Ionic effect than non-dissociated substances.
Greater the dissociation greater the osmotic pressure and greater the tonic effect.
The dissociation factor is the measure of the number of particles resulted in when a
subslanceis placed in aqueous solution.
Non-electrolyte substances have low dissociation factor.
Dissociation factor for non-electrolytes substances are assigned a value of I.
Substance dissociate into two ions dissociation factor (I) = 1.8
For three ions (I) = 2.6
For fOUf ions (I) = 3.4
For five ions (I) = 4.2
Salts that dissociate into two ions: Nael. KCI, Liel, NaHCO)
Salts lhat dissociate into three ions: LbCO] Na2CO} ZnCh CaCho Mg(OH)2
Sodium chloride equivalent
the sodium chloride equivalent for fluorescein sodium, which dissociates into
three ions and has a molecular weight of376.
i factor for sodium chloride:::: 1.8
i factor for fluorescein sodium = 2.6
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Mol. wt ofsodium chloride
i factor ofsodium chloride
x i factor of substance
Mol. WI of substance
= sodium chloride equivalent
58.5 x 2.6 0.22
376
Nael equivalent (E) - 0.22
much NaCi must be added to the following Rx to make it isotonie? NaCI -::::-
@ equivalent NaCI Equivalent '!YIbtt,.e----
0-" Rx "Y 0.1' > O'OIL I r'
9
ZnS04 ..----.. -1/4 % 0 ,
'\)"i
;.., f'\ Phenylephrinc.. I/8 % d ,o3'f)'Y ','
.JcP NaCI---......-..----Q.s. 0 . 02 2.. -
,
-rl '" p.f1.t-1r/J' h , v/op',p-J ",...!::J 6, 02L"...,
Aq.Distilledadto30mL '''J r /V"T' JlJl'-"-f.
you have to follow the steps as follows: I nJ hf.,jv.,. -/4 (fIJI')
First step: (J'!l 'f. W/v f-.lAC! - )
C I I h f h
ed' . I' ''''< "'''-'fuAJ><l a. ;" Jo--l --h:> ......
a cu ale t e amount 0 eae mgr lent In t le prescnptlon O . .$'" i.,so.fce.-iC-
SO if we look at the prescription you will find that the final volume is 30 mi.
so for ZnS04, we need 0.25 for each 100 ml so for 30 ml we need 30' 0.25/100"'0.075
grams. now for phenylephrine do the same so we will need 30 * 0.125/100 = 0.0375
grams. . J-,..-I-
It, '.J' {,l>{Jhov\' AftfAP-e-04 O 0 2l- '(i"V N c I "'l' v
v .. .27 """ Na" TO n,c.kc-- ":!S,+oN '-
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By using the NaCI equivalent of each of them calculate the contribution of these salts to
the isotonicity of the solution.
now for ZnS04: 1 gram ofZnS04 is equivalent to 0.16 grams ofNaCl, but in ,?ur
prescription we have only 0.075 so this makes the solution as if it contains
1 gram ------> 0.16 NaCI
0.075 gram -------> x NaCI
x 0.075 0.012 NaCI
Applying the samc for phenylephrinc: 0.0375 *0.29/1 = 0.0108 NaCI
therefore total contribution of the salts =0.012 + 0.0 I08 = 0.022875 NaCI
Third step:
Find the amount ofNaCI needed to make 30 ml- which is the volume of the final
solution - isotonic.
so wc need 0.9 grams NaCI for every 100 ml ...so for 30 ml we need:
0.9 g --------100 ml
x g m--m-30 ml 30' 0.9/100 0.27g NaCI
therefore the amount ofNaCI needcd = 0.27 - 0.022875 =0.247 grams = 247 mg NaCI_
c' /2-You are given ZnCh 0.7%, phenylephrine 0.1 % and boric acid with E values
J 0.16,0.32 and 0.5 respectively. This be:
A-Hypotonic B-Hypertonic C-Isotonic D) Non isotonic.
Solution:
0.7xO.16
100
+ QJ. x 0.32
100
+ Ux 0.5
100
0.00112 + 0.00032 + 0.0055 0.00694
NaCI 0.9/100 0.009 > 0.007 Hypotonic
How much NaCI required making isotonic solution? O. 6Cl'L '3'1'1 Htl c I
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sociation factors ,. 6 .
Q I-Zinc sulfate is a electrolyte, dissociating 70% in weak solutions.' Calculate its
dissociation factor.
ZnSO, ? Zn + SO, + ZnSO,
Solution:
On the basis of70% dissociation, 100 particles ofzine sulphate (21150
4
) yield:
23-16
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70 sulphate ions
30 undissociated particles
170 total particles
Because 170 particles represent 1.7 times 35 many particles as were present before
dissociation, the dissociation h1ctor is 1.7.
Calculations involving Balance sensitivity
J-What is the minimum quantity lhal can be weight on a balance with sensitivity
requirements of ISmg of a 5% error is pennissible?
Sensitivity Requirement = Weight x Error
15 = weight x L = 300 mg
100
2- What is the sensitivity of a balance that can weight 120mg ofa substance and has a
permissible error of 5%?
SR Weigh. x Error
SR = 120mg x .L = 6mg
100
Error = sensitivity requirement/weight
Weight = sensitivity requirement/error
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What is the sensitivity of a balance that can weight 120 of substance and has accuracy of
98%?
Sensitivity requirement::: weightxerror
120X2J100=2.4
Tips Practice format 002; Electrolyte Solutions
'./ Molarity - molecular weight in grams
V Litres
C,/ Millimole (mmol) I L - molecular wt in milligrams
Litres
Converting milliequivalcnts per unit volume to weight per unit volume
mEq [mg x valenceJ/(Mol.wt)
23-17
mg = [mEq x (mol.wt)]/valence
mOsmollL = Wt. Of substance in gIL x number of species x 1000
Sensitivity Requirement =Weight x Error
Error = sensitivity requirement/weight
Weight = sensitivity requirement lerror
I-A solution contains 10 % mg% ofK+ ions .Express the cone. In terms ofmEqfL?
10
0
1'>"1 _. :I 1(-1': w.::l 2.'S{, WJ i/l--
/001'-1 llfOOV1 1 l. rUt'
t. 1.-7'
2-How many mEq. OfKCL are represented in a 15 ml dose of 10 % wlv KCL elixir?
Molecular.weightKCl=74.5g '5t< OID -:;. -;
'" of ':. /'1 I 17

l
d 2../1 . 1.1
3- 0{J many per litre are present in 0.9% N<iCI J!
:. 307 . , 9 rY) (:J:JfYJOL t--
I-In dosing the drug gentamicin in patients, for every I mg/kg of gentamicin
administered, serum drug concentrations are expected to increase by 2.5 J.1g/ml. What
would be the expected serum drug concentration following .an administration of a 2.5
mg/kg dose of gentamicin?
A-5 llg/ml
@6.25 Ilg/ml
C-IO Ilg/ml
D-2.5 Ilg/mJ
Ans:B
I mg/kg = 2.5 mg/kg
2.5 Ilg I ml X Ilg Iml
X = 6.25 Jlg Iml
Ans: C
Xg 0.25 g
5000 ml 5 ml
X= 250 g
2-An elixir is to contain 250 mg of an alkaloid in each teaspoonful dose. How many
grams of the alkaloid will be required to prepare 5 litres of the elixir?
A-0.25g lJV-II.! tvi
. ,.. JU1J . 0
, \ 7:\
D-2.5g Jv '.---
COOt>M
J
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X 94.6 kg 0.0001 kg X
2.5 ml 2,365,000 ml
3-A pediatric product contains IOOmg oferythromycin ethylsuccinate in each dropper
(25ml) of the product. How many kilograms oferythromycin ethylsuccinate would
be required to prepare 5000 pint-size bottles? 6 /
A-74.6 kg I '''':l t5 M
B-84.6 kg
C-99.5 kg
0-94.6 kg
Ans: 0
I pint = 473 ml
480 ml x 5000 2, 365,000 ml
4A physician places a patient on a daily dose of 48 units ofU 80 insulin (80unitslmL).
How many ml should the patient inject each day?
A-O.4
8-0.5
C-0.6
0-0.25
Ans: C
U- 80 INSULIN
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Iml X
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I Megaunil 1000,000 U
20 ml ---7 2000000 units
I
X=2x 1000 x 1000 = 100,000 units
20
1000,000 units
5-A 20-ml vial of biologic solution is labelled "2.0 megaunits." How many units of drug
are present in every ml ofsolution?
A-2000
B-IOOO
C-IOO,OOO
0-10,000
Ans: C
IMegauni. 1000KU
I KU = 1000 units
2.0 Munits x 1000 KU x 1000 units
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8-The usual initial dose ofchlorambucil is 150 j..lg per kg of body weight once a'day.
How many milligrams should be to a person weighing 154Ibs.?

A 10.5 mg /54 ,:- 2..t '10
-18 mg
C-15mg O./)1JX1-O IO'5"'d
D-8 mg
Ans: A
= 70 kg 1541bs x I kg
2.21bs
150 llg =.-X...
-Ifck!"g'-""'- 70 kg
X = 10, 500
= 10.5 mg
4.
09
150 units
I kg
5000 u
1m/
X=4.1 ml
9-An initial heparin dose of not less than 150 unitslkg of body weight has been
reconunended ofopen-heart surgery. How many ml of an injection containing 5000
heparin units per milliliter should be administered to a 300-pound patient?
A-5.1 300 -'- 2..2 , /36. 3b 1't1
8-4.1
C-5.lml 18!.J(y If> 0. 2
0
4S!t."4
D-4.1 m/ --_.__.... "-
Ans: 0 -"'" 0
300lbs x...l.!9L = 136.36 kg =
2.21bs
X = 20, 454.54 units
136.36 kg
20454.54 u
X
lO-The pediatric dose of cefadroxil is 30 mglkglday. Ira child is given a daily dose of2
teaspoonful of a suspension containing 125 mg of cefadroxil per 5 ml, what is the
weight in lb. of the child?
A-19.5Ibs.
B-18.8Ibs.
C-i 8.3 Ibs.
D-18.1 Ibs.
Ans: C
125 mg x 2 = 250 mg
5 ml 5 ml
250 mg = 30mg
X I kg
'6. gg \<fl
23-20
23-21
220 Ibs x l...kR.. = 100 kg
2.21bs
0.1 mL=...x..-
I kg 100 kg
X= 10mi
= 2 tsp
12-The adult dose ofa liquid medication is 0.1 mllkg of body weight as single dose.
teaspoonfuls should be given 10 a patient weighing 220 Ibs.?
0'2 tsp. 100 '''''0 >< 0 I I 0 I'J1
82.5 lSp. <:)
C-2.bsp.
0-2.5 tbsp.
Ans:A
ww,.... phannacyprep.com
x = 8.33 kg
8.33 kg x 2.2 Ibs = 18.33 Ibs
I kg
11lflhc loading dose of Kanamycin is 7 mglkg of body weight, how many grams should
be administered to a patient weighing 130 Ibs.?
A-0.492 g
':>'1'Oj 1.<,s,xO,OO'(,,-
C-414 g
D-0.485 g
Ans: B
130 Ibs x .lk!L = 59.09 kg
2.21bs
7mg = X
I kg 59.90 kg
X= 413.63 mg
=0.414g
13-lfa prescription order requires 25 g ofconcentrated HeI (density 1.18g1ml), what
volume should the phannacisl measure?
A-29.50 ml
B-0.0212 ml

(71.2 ml
AilS: D
W=25g
D= 1.18 g/ml
V=...M.. =..1.L = 21.2 ml
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dose ofa drug is 0.5mglkg body weight/day, how many mg will a 351b infant
receive per 24hours?
@y.9mg '15'Q;< (j
B-7.1 mg
C-7.2 mg
D-7.4 mg
Ans:A
351bs x I kg = 15.9kg
2.21bs
0.5 mg = X
I kg 15.9 kg
X= 7.9 mg
15- What is the weight of 60 ml of oil whose density is 0.9624 g/1ll1?
A-5.770g r,>,6'op\ _
(8,57.7 g C S " 1'vo,
'C-6.0 g
D-0.577 g
Ans: B
v= 60 ml
D = 0.9624 gfml
D=J;L
V
M=DxV
= 0.9624 x 60
= 57.7
16-A prescription calls for OJ g of phosphoric acid with a specific gravity of 1.71. How
many milliliters should be used in compounding the prescription?
A-0.5
!

Ans: C
D=J;L =....!:...
V ml
V= J;L = 0.3 g
D 1.71 glml
X=0.18ml
23-22
o /,?,-How many mL of a syrup having a specific gravity of 1.350 should be mixed with
V 3000 mLofa syrup having a specific gravity of 1.250 to obtain a product having a
specific gravity of 1.31 O?
A-3500 mL 1,9..00 /. 361" ,
D-4500 mL , " /
" .
C-4600 mL I . 3/
D-5500 mL "-....A
Ans: -"",
0.06 = 0.04 0 0 '0(,
X 3000 ml I
X=4500ml
Express patient is detennincd to have 0.8 mg of glucose in each milliliter of blood.
the concentration of glucose in the blood as mg%.
A-SOO mg%
8-0.8 mg%
,-8 mg%

Ans:D
Mmg =..--1L
I ml 100m!
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19-1-Iow many mL of a 1:400 (w/v) stock solution should be used to make 4 litres ofa
4""' )( 0
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X=80mg%
IdL = 100mL
XmL = 400mL
2g Ig =800mL
20-lra patient is detennined to have 100 mg % of blood glucose, what is the equivalent
concentration in tenns ofmgldL?
A-I mgldL ,dr..-- '10
D-IOmgldL -, /oo"''''!
s:.'i'0 mgldL
Q) 00 mgldL IaD J.Vl} _ I
I co"'" ?idf-
6'0'; 1:2000 (w/v) solution?
A-IOOOmL
B-200 mL
C-800 mL
D-1600mL
Ans:C
.-L!L= X = 2g
2000mI 4000mL
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JD.L = mg
dL 100 mL
=100mg/dL
2I-Strong Iodine Solution USP contains 5% w/v iodine. How many mg of iodine are
consumed daily if the usual dose is 0.3 mL ti.d.?
A-15mg - o.e lw"/ )(i}'<lr' ;
B-90 mg
C-22.5 mg
QJ45mg
Ans:D
_5_=l
100 0.9
X = 0.045 g x 1000
=45 mg
22-Express in percentage the fluoride concentration in drinking given in 0.6 ppm.
A-0.06%
B-0.00006% _.Q_ ~ __ ~ f ~ ": 0 0. ~ (', < /.
C-0.0006% 1,6 ()o. ~
D-O.006%
Ans: B
O.6g =L
1 000,000 100
X=0.00006%
23-How many grams of dextrose are required to prepare 4 litres of a 5% solution?
A-0.2g
B-200g
C-2g
d-20g
Ans-B
x
4000mL
5g
100mL
24-Change to percent the number 1/300.
A-3%
B-33%
C-3.3%
D-l/3%
Ans: D
_1_= .L-
300 100
..J1L=0.33%
6J]-/-
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X ~ 100
=
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250 mg X
X ~ 1000g
26-How many grams of potassium citrate are needed to prepare 1 litre of 10%7
A-1000 g
~ g
/;tIOOg
0-10 g
Ans:C
100
,.....,. rowmany grams of petrolatum should be added to 2S0g of a 25% sulphur ointment
V 10 make a 5% ointment?
A-IOOO g 0 &:i (Zb' ~ )
B-1250 g ,,------./
C-500 g .
O-IOOg /6,
Ans: ../ "'-..
." .........
Given: 250 g of25 % ~ ...5
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27-How many grams ora drug are required to make 120 mL ora 25% solution?
A-30 g
B-IOg ,,Q.odl-C c ~ o ~
C-12.0 g
0-12 g
AilS: A
L ~ 25
120 100
X ~ 30
~ .QJ2.g ~ L
100 ml X
X ~ 588 ~ 1:588
28-Calcium Hydroxide Topical Solution contains 170 mg of calcium hydroxide per 100.
mL at 15 C. Express this concentration as ratio strength.
A-I: 688
fl<!: 888
(01: 588
0-1:788
Ans:C
170 mg
100 ml
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29-How many mg of isofluorophate are contained in 15 g of a 1: 10,000 ophthalmic
solution of isoflurophate in peanut oil?
A-I.7 mg
B-l.9 mg
r"1.8 mg
(!Vl.5 mg
Ans:D
1 g = X
10,000mg 15g
X = 1.5 mg
3D-Express 0.2 % in ratio strength.
A-I: 5000
B-l:50
y:500
D-l:5
Ans: C
02-
--
I lrT>
--
/Cl'"
.JLL =_1_
100 15 g
0.2X= 100
X= 500
ofa substance is needed to prepare lL ofa 1: 10,000 solution?
A- .1 g
-lOg I b I _.') t
C-O.OI g !.
D-l.O g
Ans: A
-2L
10,000 1000
X =0.1 g
32-A cupric chloride injection (0.4 mg Cu/mL) is used as an additive to IV solution for
TPN. What is the final ratio strength of copper in the TPN solution if 2.5 mL of the
injection is added to enough of the IV solution to prepare 500 mL?
A-I: 500 0
0
1
@
:5000 -=,__ ._ . -
C- : 500,000 SDo 5.01), ....
-1.50,000
Ans:C
0.4 mg
1 inl
= X
2.5 mJ
X = 1 mg ::::Q.OO1 g
0.001 g = ..L
500 mJ X
X = 500,000
1: 500,000
23-26.
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x 0.2 g
X 4.33 g
B-15
X = 18.44 ml
J..
5000
23.5 = 4.33 g
100 X
!UJL X
30 Inl 650 ml
33-How many millilitres ofa 23.5% (wtv) concentrate of Sodium Chloride solution
should be used in preparing 650 mL ofa stock solution such that 30 mL diluted to
litre will yield a 1: 5000 solution?
A-0.2 mL
B-4.33 mL
C-18.44 mL
0-11.75 mL
Ans:C
A-20
Ans: D
Q,C, = Q,C,
X (50) = 300( I0)
X =60
..-L
100
Q,C, =Q,C,
(X) 6.25% = (5000)(5%)
X = 5% x 5000mL
6.25%
X=4000 ml
34-You have a stock solution 050% Sodium citrate and you were asked to prepare 300
mL ofa 10% solution. How many mL is needed?
6
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35-How many millilitrcs of 1:16 solution of sodium hypochlorite should be used in
preparing 5,000 roL ofa 5% solution of sodium hypochlorite for irrigation?
A-800 ml 500' , '5 4,,"_A 0.
B-2500 ml vv
C-4000 ml ' ,,,-,
0-300 ml
Ans:C
36-Prepare 1000 ml ofKMnO, I :12,000 compresses out ofKMnO, I: 8,000.
A-Add 333.3 mL waler '0 1000 mL KMnO, I: 8,000
BAdd 666.6 mL water to 333.3 mL KMn0
4
1: 8,000
CAdd 333.3 mL KMn04 I: 8,000 and enough water to make final volume 1000 mL
O-Add 333.3 mL waler to 666.6 mL KMnO, I: 8,000
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Ans-D
1000 xl/12000 = 1/8000 x V
2
V2 = 666.6 mL of Kmn04
. .
37-How many milliliters of24% (w/v) concentrate of saline solution should be used in
preparing 600 mL of a solution such that 10mL diluted to a litre will yield a 0.09%
solution?
A-300 ml B-150 ml C-50.0 ml D-225 ml
Ans:D

>eboa::
0.09
--LL
X = 0.9 g
fa
100 1000

st.,
X X=54 g
..
-
10 ml 600 ml
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=

X=225 ml

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38-The only source of Sodium Chloride is in the form of tablets, each containing 5.0 g.
How many tablets should be used in preparing 3000 litres of a solution of such
strength that 20 mL diluted to 100 mL with water will yield a 0.9% (w/v) solution?
A-60,000 tablets
B-27,000 tablets
C-12,000 tablets
D-9,000 tablets
Ans: B
0.9
100
--LL
100
X =0.9 g
M1t.. = X
20 ml 3,000,000 ml
X = 135,000 g
135.000 g = 27,000 tabs
5g
\
39-How many grams of 10% (w/w) ammonia solution can be made from 1800 g of28%
(w/w) strong ammonia solution?
A-6428.57 g
@-5040 g
C-50,400 g
23-28
Ans:
Ans:
2000 ml x 0.5 1000
500 ml x 0.7 = 350
2500 ml x 0.95 = 2375
5000 ml 3725
3725
5000 100
X = 74.5
23-29
900 ml x I.I 898 1070.82
700 ml x 0.975 682.5
I 150 ml x 1.240 1426
3 I79.32
D-642.86 g
Am:B
17-How many ml of 0.9% (w/v) Nael solution should be prepared from 250 ml of25%
(w/v) solution? /?'\
A-3750 ml B-2500 ml (5;6944.4 ml D-9 ml
Ans:C
9-Delennine the specific gravity ofa mixture 0900 mL of syrup with a sp. Gr. of
1.1898,700 mL of elixir with asp. Gr. 00.975 and 1150 mL ofglycerin with asp.
Gc. or 1.240.
a) 1.1349 b) 1.1486 c) 1.1486 d) 1.1561
Q,C, Q,C,
(10) X (1800)(28)

Q,C,
250(25)
X 6944.4 ml
1.1561
2750
10-Whal is the percentage alcohol in a mixture 02000 mL 050% (v/v) alcohol. 500 mL
070% (v/v) alcohol and 2.5 L of95% (v/v) alcohol?
0)71.67% b)73.25% c) 72.50% d) 74.5%
25-A Pham13cy tech adds 75 mL ofstrong iodine solution USP (5.0% w/v) to I litre of
1'1sterile water for irrigation. What is the % w/v of iodine present?
04'.35% B-D.475cro C-O.53% 0-0.60%
Ans:A
Q,C, Q,C,
75(5) (l075)X
X =0.35%
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II-li800 g of5% coal tar ointment is-mixed with 1200 g ofa 10% coal tar ointment.
What is the concentration of coal tar in the fmished product?
a) 8.5 % b) 9.5% c) 8% d) 9%
Ans:C
800 x 0.05 = 40
1200xO.l = 120
160
~
2000 100
X=8%
23-30
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Dosage Calculations
Questions Alerts!
Common Questions in pharmacy exam is to ask!
Electrolyte solutions milliequivalent to milligram
a Electrolyte solutions milligram to milliequivalent
mEq = mg x valence
M.wt (mg)
mg = mEg x M.w! (mg)
valence
2-A physician orders Meprobamate 0.2 g. How much is to be administered if the dose on
hand is 400 mg. in each tablet?
A-do not dispense B-give 2 tablets C-give I tablet D-give Y2
tablet
Ans: 0
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I-A prescription calls for 10 units ofa drug to be taken 3 times a day. How much will
the patient have taken after 7 days?
A-21.0 units 8-0.21 units C-2.! 0 units @).IO units
Ans: 0
10 units x 3 x 7 = 210 units
200 mg _1_ tab
400mg 2
each tablet containing 5mg. Start 35 mg and then taper by 5mg every
other day. How many tablets are needed? (3
A-20 lab B, 6 tab
,
Ans:B
7+7+6+6+5+5+4+4+3+3+2+2+1+1 = 56 tabs
C-14 tab D-:
inhaler 120 doses. How many days the patient will take to finish the entire
with this signature: "Use 2 inhalers in each nostril every morning and at bedtime
a) 7 days b) 10 days c) 20 days d) 15 days e) 30 days
Ans-D ''Two inhalers in each nostril every morning and at bedtime'
2 x 2 nostril x 2 (morning + night) = 8 doses daily
120 doses..;. 8 doses daily = 15 days supply
Stock Solutions
I-The amount of solution needed can be determined by setting the two ratios equal:
active ingredient (available)
Solution (available)
= active ingredient (to be administered)
solution (needed)
2-
mEq =Molecular Weight
Valence
3-Converting between milligrams (mg) and milliequivalent (mEq)
NumberofmEq =Weight of substance in mg
mEq weight
4-
lOx mL = 20 mL
I-You have a stock solution that contains 10 mg of active ingredient per 5 ml of solution.
The physician orders a dose of 4 mg. how many millilitres of the stock solution will have
to be administered?
Using the information provided, set up a proportion:
x mL = 5 mL
4 mg 10 mg
xmL = 2mL
Thus 2 ml of solution are to provide the dose.
2-The molecular weight of magnesium sulphate (Mg 2+ S04 2-) is 120 mg and its valence
is 2. How many milligrams does 1 mEq of magnesium sulphate weigh?
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1 mEq = 120 mg = 60 mg
2
. /3- You are to reconstitute 1 g of dry powder. The label states that you are to add 9.3 mL
V of diluents to make a final solution of 100 mg/m\. What is the powder volume?
24-2
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The final solution will have a strength of 100 mglmL. Then, since you start with 1
g = 1,000 mg of powder, for a final volume x of the solution. it will have.strength 1,000
mgtx mL.
x mL = I mL
I,OOOmg 100mg
x mL = (1,000 mgl x I mL
100 mg
x mL = 10 mL
10-9.3 =0.7ml
4-lf a 600 ml of a 15% (v/v) solution of methyl salicylates in alcohol are diluted to 1500
Illi what will be the percentage strength.
C, Q,IQ,'C,
1500mL = 15% = 6%
600 mL X %
5-How many mL of a 1:500 (w/v) stock solution should be used to make 4 liters of
1:2000 (w/v) solution?
Working: 1:500 = 0.2%
4 liters - 4000 mL
I:2000 0.05%
0.2% 4000mL 1000mL
0.05% x mL
6) Ifa 600 ml ora 15% (v/v) solution of methyl salicylates in alcohol are diluted to 1500
ml what will be the percentage strength.
C,
1500mL = 15% = 6%
600 mL X%
I-How many tablets each containing 25J.1g, will provide the equivalent orO.5 mg of
sodium Liothyronine?
Working:
0.5
:. Number or lablets = 500 tablets
2-Rx
Codeine P0
4
200 mg
24-3
Dimetapp qs 120 ml
Sig. 1 tsp tid and HS
How many mg Codeine received by the patient daily?
Working
4 tsp means 4 x 5 = 20 ml/day
if 120 ml contain 200 mg
so daily =200 x 20/120 =33.3 mg/day
Pounds and Kilograms or Kilograms (Kg) and Pounds (Ibs)
To convert Ibs into Kg =divide by 2.2
Example: 10 Ibs =4.5 kg or 7 Ibs =3.1 kg
To convert Kg to lbs = multiply by 2.2:
Example: 3.5 kg = 7.71bs or 5 Kg = II Ibs 10.3 = 103/10 = 10.3/10
1. On admission to the hospital your patient weighted 158 Ib and was placed on a
diuretic. Two days later the patient's weight was 70.9 kg.
This patient has lost ~ kg or 201-- lb of body weight in response to this medication.
2. The physician has ordered 50 mg of a medication to be administer daily. The drug
reference states that you should administer no more than I mg/ kg of body weight daily.
This client weighs 164 lb.
The largest dose that this patient could safely receive is t'I ~ ,S-t, mg.
3. The physician has ordered injectable versed for your patient who weighs 135 lb. Your
drug reference states that the maximum dose is 0.06 mglkg of body weight.
The largest dose that can safely be administered to thi patient i l.J...( mg.
Teaspoons (tsp) and Tablespoons (Tbsp)
The physician has prescribed 1 Tbsp of Riopan. The unit dose container available
contains 30 ml of this medication.
The correct dose is ~ ml.
2. The client has been taking 20 ml of a medication in the hospital. In p r p r i n ~ him to
administer this medication in the home setting, you would teach him to take tsp of
this drug.
.
3. The client is to take Y2 Tbsp of medication. The most accurate method for measuring
this dose is to pour /.5' m) of this drug.
24-4
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Milligrams and Grains
2. Morphine sulfate gr 1/8 [M is to be prepared from a solution containing 10 mg / 1 ml.
The volume to be given is d ml.
Ans: 0.81 ml
Phannacy has provided 325 3. Ferrous sulfate gr v po q AM is ordered for your patient.
mg tablets.
You will administer __tablet(s)
Ans: I tablet
3. Your client is to drink 64 oz ofGolytely over a 3-hour period. How many milliliters
must this person consume each hour to comply with the physician's order?
Administer ml each hour. \
Ans: 640 ml. ;----:;-
?
I-How many tablets each containing 25/lg, will provide the equivalent of 0.5 mg of
sodium
Liothyronine?
Working:
0.5 mg=500 Ilg
Number of tablets .::;: 500 /25=20 tablets
Milliliters and Ounces
The physician has ordered iss ounces ora laxative. The correct dose is m!.
Ans: 45 ml.
2. You are to administer 5 011 of ferrous gluconate that must be diluted in water to protect
the client's teeth and gastrointestinal track. The directions in your drug reference state
that each ml of this medication must be diluted in 20 ml of water.
Once diluted, the total volume to be administered is.J.6- Ill!.
Ans: 105m!.
I. You are to administer phenobarbitol gr %. There are scored 60 mg tablets available in
floor stock.
You would administer __mg or __tablet(s).
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Codeine P04 200 mg
Dimetapp qs 120 ml
Sig. I tsp tid and HS
How many mg Codeine received by the patient daily?
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24-5
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Working
4 tsp means 4 x 5 = 20 ml/day
if 120 mt contain 200 mg
so daily 200 x 20/120 33.3 mglday
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3. Prednisolone each tablet containing Smg. Start 35 mg and then taper by Smg every
day. How
many tablets are needed?
Rtab

D 8tab
./ --8 tab
\r -I -r
I::' -l Co
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4-Ifthree tablets contain 975 mg of ASA, how many grams of ASA would be contained
in J2 tablets?
A-4g
B-325g
(93.9g
D-39g
E-390g
5-How many milliliters ofa heparin sodium injection containing 200,000 heparin units in
10 mL should be used to obtain 5,000 heparin units?
A-0.50mL
""-
'-.-S-O.25mL
l::-O.lOmL
D-0.75mL
E-250mL
)<; physician asks the pharmacist to compound codeine sulfate tablet triturates
,!,v'b \ f} 'ontaining 10 mg of codeine. The patient needs a S-day supply and may take 1-2 q4-6h
pm. How much codeine is nceded to filllhis prescription?
'7/ A-300 mg
B-400 mg
C-600 mg
D-J200 mg
E-just dispense one dose because it is pm
6. Prednisolone each tablet containing 5mg. Start 35 mg and then taper by 5mg every 2
day. How many tablets are needed?

(b56 tab
C-14tab
D-28 tab
E-84 tab
24-6
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I Pharmacokinetics
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Pharmacokinetics
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Questions Alerts!
Absorption, DE1Jibution, Metabolism and Elimination (ADME)
Volume of distribution V
Renal or hepatic elimination
Steady state concentrations
Phannacokinetics desccibes the absorption, distribution, metabolism, and excretion of drugs in
patients receiving a drug therapy.
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D
M
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Absorptjon
Distribution
Metabolism
Elimination
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required to contain the entire drug administered so that the concentration will be the same as
that found in the blood. d...v-j @e..:H-<""
V
d
=A
b
(amount of drug in the body)jC (concentration of drug in plasma)
Some important formula involving volume of distribution; To calculate volume of distribution Jt.c. b
/ _ Vd::: J+mow.4 dt 1"-' 0,
Vd-D
C, P Io.s h') "'- -c;"-'..t..J-1JI'
To calculate iniliaJ plasma drug concentration
Cp=D
Y,
To calculate dose
25-1
Pharmacyprep.com
To calculate loading dose
Dl=CssXV
d
C
ss
= steady state concentration
D
L
= loading dose
To calculate renal clearance:
CLR=kx V
d
Factors affecting drug distribution
Pharmacokinetics
Rate of distribution (speed of distribution) Extent of distribution (amount of distribution)
Membrane permeability Lipid Solubility
Blood perfusion pH - pKa

-
Plasma protein binding
-
Intracellular binding

Plasma Protein Binding
Plasma proteins refer to the proteins present in the plasma binding to drugs. There two major
types of proteins in the plasma; these are albumin and glycoproteins.
Drug undergoes protein binding with three types of proteins; Acid drugs-?Albumin (55%-
major proteins): albumin has strong affinity to for anionic drugs (weak acids) and hydrophobic
drugs.
Base drugs binds to alpha acid glycoproteins, and Important concept!
lipoproteins Albumin is the major protein that binds
, steroid etc binds globulins. with acidic drug
Conce.-f+' '--------------'
Extensive plasma protein binding will cause more drugs to stay in the central blood
compartment. Therefore drugs that-bin'd -strclngly to plasma protein
volumes of distribution. Dru'gs that have high plasma protein binding, 'less volume of
diStrioution and v'kettversa':" .' , .-
, .-t....."
.' Tissue Binding: Generally, high degree of tissue binding implies large Vd, ego Digoxin.
Questions Alert! Clinical importance ofwug displacement.
If patient is using class 1 drug tolbutamide, is give class 2 drug sulfonamide
antibiotics administered. It displaces tolbutamide and increase rapid
concentration of tolbutamide.
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% protein binding (fotal - Unbound) x 100
Total
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Drugcffcclal
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Protein Dound
Drug
Phenytoin
Vancomycin
Warfarin
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Plasma Proteins Concentration that changes with some conditions
Conditions Albumin Alpha 1 acid glycoprotein
Renal Failure J. (hvpoalbuminemia) f
Hepatic Failure f
Arthritis
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f
Burns
.
Pregnancy
.
Stress/Trauma 4- f
Elimination: Removal of drug from the body may occur via a number of routes. The most
important routes of elimination are: Kidney into urine. Other routes of elimination: bile,
intestine, lung or milk in nursing mothers. Second most important organ for elimination; liver
Drug Elimiulton
(
! Renal Clearance
Total clearance (CL
T
) CL. + CL
NIl
CLT Plasma drug concentration Cp
CLr= F x D lAUe F= bioavailability, D= dose rale
CLT =Vd X lcel where Vd =volume ofdistribution and keJ is the elimination rate constant
V
d
= CLTlK
ei
Md>bol"'"
[g
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''''''1 , uerCI;oa I .. Urine (rcn::r.1 ur kl<iney)

BIC3S1 milk
Exbaledair
The rate of elimination (disappearance of the active molecule from the blood stream or body)
determines the duration ofaction for most drugs.
Rate of elimination Drug elimination
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Pharmacokinetics
tll2 = 0.693 IKel
CL
r
= V
d
x (0.693/tll2) where 0.693 = ln
2
and tl/2 is the drug elimination half-life
Factors that affect renal clearance: As clearance is decreased half-life increases, changes in
Vd cause proportional changes in half-life.
Half life = 0.693 x Vd / Ch
Steady-State Drug Plasma Concentration (C
ss
)
C
ss
= l/(ke*Vd) * (F*D)ff
Hepatic Clearance: The volume of drug containing plasma that is cleared by liver per unit
time. Measured indirectly as difference between total body clearance and renal clearance
Cl
H
= Hepatic clearance
Or ClH=QER
Q = product of blood flow
ER = Ca - Cv
Ca
Ca = arterial plasma drug concentration liver
Cv = venous plasma drug concentration in liver
Values for ER range from 0 tol, if the ER is 0 then no drug removed by liver, if 0.8 then 80%
of incoming drug is removed by the plasma profuse in liver.
Hepatic clearance depends '?": Blood flow: Blood flow to the liver is approximately 1.5
L/min. Exercise, disease or drugs may alter Blood flow.
SAfter oral drug administration the drug is absorbed fonn GI into mesenteric vessels -7 hepatic
V0rtal vein -7 liver -7 systemic circulation.
Intrinsic clearance (Cl
iot
)
.' The ability of the liver to remove the of the blood
oxidase enzymes biotransfonn drugs). IntrinSiCCearance pnmarily occurs because of ability of
metabolizing enzymes (mixed function oxidase) as they metabolize the drugs they enter in
liver.
Relationship between pharmacokinetics factors and eliminations:
The relationship between steady state plasma concentration and volume of distribution can be
obtained by:
25-4
The relationship between AUC and volume ofdistribution can be obtained by: lJllravenous F is
=1
The relation between steady state plasma concentration and volume of distribution can be
obtained by: C
ss
= R/Vd X K
R = rate of infusion
K = elimination constant
Vd = volume of distribution
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R = rate of infusion
K= elimination constant
V
d
= volume of distribution
The relationship between loading dose and volume of distribution:
DL.=CssxVd
0L = loading dose
The relationship between body clearance and average plasma concentration:
C..v=FxD
g
CLT x t
t "" dosing interval
Cay = average plasma conc.
Cl.:r=tolal clearance
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The relation between loading dose and volume of distribution: DL - C
ss
x Vd
D
L
= loading dose
Steady state concentrations C
ss
/ Plasma concentration at steady state <Ca). Under the steady state conditions; the fraction of
. drug absorbed equals to the fraction ofdrug eliminated in the body
25-5
Phannacyprep.com
200
Phannacokinetics
C
max
SS (peak)
180
C
55
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30
c .55
24 20
Important concept!
Rate in :::: Rate out means rate of
absorption is equal to rate of
eliminations
16 12
ko :::: rate of infusTJw
e
CL:::: total body clearance
DL:::: loading dose
DM:::: maintenance dose
Vd:::: volume of distribution
"'[ =dosing intervals
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20
40
c
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DM :::: C
SS
x CL x T
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R-me i __...1..-_---L.__L-_
E
'-"'
/C
ss
:::: CL
Css=
Plateau Principle
Time to reach steady state depends only upon the tll2 of the drug and is independent of the
size of the dose and the frequency of dosing.
The zig-zag and graph represents the same data.
It takes>7t 112 to reach mathematical steady state
Steady state is reached when either rate in :::: rate out or when the values associated with a
dosing interval are the same in the succeeding interval.
Aminoglycosides given at intervals that are much longer than one half-life.
Phenobarbital intervals that are smaller than one half life are slowly cleared 'from body,
therefore their peak concentration are relatively smaller.
The time to reach C
ss
:
The concentration of drug rises from zero to C
ss
by first order process
To reach 90% of the final steady state concentration takes 3.3 $""" -t> 4, 9 I "=" ".J"
The sole detenninant of the rate that a drug reached C
ss
is the half-life or Ke and rate is
influenced by only those factors that effects half-life.
25-6
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25-7
Pharmacokinetics Phannacyprep.com
Shelf life -
T9Oo/c,orTIO%= 0.105
k
Formulas
t
'
/2 = 0.693 V,/CI,
Dosage Regimens
The number of doses to be given per day is usually detennined by the half-life of the drug and
the difference between the minimum therapeutic and toxic concentrations.
CL = rate of e1imination/C
CL = Vd x lcel where Vd= volume of and lcel is the elimination rate constant
CL = Vd . (0.693/1112) where 0.693 = In 2 and tin is the drug elimination half-life nOle that
plasma clearance CLp inciude renal (eLf) and metabolic (elm) components
Clearance
If volume ofdistribution increases (drug displacement from protein binding, heart failure,
cadiogenic shock). How this effect on half life?
Half life increase because it is directly proportional to Vd
What if clearance decreased (renal diseases, hepatic cirrhosis)?
Halflife increase
What ifmelabolism decrease? half life increase
What if dose is increase, how the half life effects? dose does not affect half I ire
From the above formula:
e55 time-does NOT influenced by rate of infusion. C
ss
concentration rises with infusion.
I SI order:
C = Co x 10 -Wl.303
Log C = log Co -1..'"I!2.303
C=Coxe-l..,
InC=lnCo-
kt
Halflife
0.693/k
C.,I2k
Shelf life
190 O.105/k
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Clearance
Distribution
Vd A,Ie.
Tips
X I (yO
x,--::--
BLow)
F
1 albumin 2 IlZlvcoorotein 3 aloha & beta lioovrotein
4 loadilU! dose 5 AUe 6 Nonionized lioid forms ofdruQ"s
7 More hydrophilic
compounds and drugs
, ' , ..
the [mllal dose used to initIate so as tq Yield therapeutic concentrations that wIll result In
clinical effectiveness. ( )
which plasma proteins do acidic drugs bind to? ( Al 6U rnJ V'\....-" )
What types of drugs are excreted by way of the sweat and saliva? ( )
-
25-8
Halflife calculations
Questions Alerts!
First order elimination
Rates and orders of Reactions
www.Pharmacvorep.com
Rate: speed (velocity)
Order: the way in which concentration effects rate
Reaction orders: There is four orders of reactions are described below. Zero order reactions, lSI
order reactions, 2
nd
order reactions, 3
rd
order reactions, and pseudo order reactions.

Rates and Orders of Reactions
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Independent of concentration
Time dependent
-dc/dt Ko
Slope
Example: Photochemical degradations
-Zero order constant expressed in units ofconcentration ego milligrams pcr millilitre per hour.
Or gramIU hour
/ Linear equation:::: C ::: -Kot +Co
K
o
is slope ofthe line = zero order constant (conc.ltime)
Co is initial concentration
T= time
C = drug concentration
Slope of the line is not equal to the rate constant because it includes minus sign.
The negative indicates that slope is decreasing. Rate ofelimination is independent of the
amount of drug to be eliminated. TIle zero order elimination rate constant is K
o
and has the
units of amount/time. A eonslant amount of drug is eliminated per unit of time.
26-1
'.
www.Pharmacyprep.com Rates and orders of Reactions
A constant fraction (percent) of drug is eliminated
4hr 4 hr 4 hr 4 hr
Most drugs do Dot follow zero order processes.In zero-order equations, a constant amount is
removed for each unit oftime. This kinetics fit the following equation.
Zero order elimination: alcohol toxic doses of aspirin, and high doses of phenytoin, amino
glycosides.
80 mg -7 70 mg -7 60 mg -7 50 mg -7 40 mg
time
First order reactions
Rate of reaction is proportional to the first en ratIOn.
Concentration and time dependent r- 2.JU) W
Log ColC = K\/2.303 I< ?- . d -
Where _---1::..-- C-_-I
'---" -
Co =concentration at to
K =rate constant
A plot of log of concentration against time produces a straight line with a slope:
Slope -k/2.303
Half-life 0.693/k
A constant fraction (percent) of drug is eliminate' half of the starting amount ofdrug is a
. constant and is known as the half-life t1/2- .1" c........
4hr 4hr 4hr 4hr C;S:i
80 mg -7 40mg -7 20 mg -7 10 mg -7 5 mg - :;=-
First order rate constant: DCldt == -kC time-I (llhr or h(l)
k = first order rate constant
C =Coe-
kl
In C =-kt + In Co
26-2
Examples of second order: Saponification of esters
CH,COOC,H, + OH ~ (double arrows) CH,COO- + C,H,OH
Second order equation: Rate of reaelion proportional to the each ofthe two reactant
concentration and time
Dx/dt = k (a-x) (b-x)
where
a = concentration of reactant A at time t
b = concentration of reactant B at time t
dxldt = rate of reaction
x= number of moles ofreactant A and B at time t
k = reaction constant
If concentration orreaetant A and B are equal:
dx/dt = k(a-x)(a-x)
dx/dt = k(a-x)'
Second order tIn = Ilka
When there is concentration of A and B 110t equal, secondary order equation will be:
k =2.303/t(a-b) = log bra-xl/arb-x)
time
Rates and orders of Reactions
log C = - kt/2.303 +Iog C,
www.Phannacyorep.com
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Rate of reaelion is proportional to concentration ofeach of the three reactions
Dx / dt = k (a-x) (b-x) (c-x)
When a = b = c
Dx/dt = k (a_x)'
Pseudo order: Rate of reaction is proportional to the concentration ofonly one reactant, in
nvo-reactant reaction, if a reactant present in high concentrations.
Example: Saponification ofesters in presence of high concentration of bases (Gloor) or acids
CH,COOC,H, + OH (excess) ~ (double arrows) CH,COO' + C,H,OH
Half-life fl/
2
26-3
www.Phannacyprep.com Rates and orders of Reactions
Half-life: (tll2) -7 time required to-decrease the amount ofdrug in o ~ by 1/2 during
elimination (or during a constant infusion). Plasma t 12 is The time it takes for the plasma drug
concentration to fall to half its initial value.
First order reaction
0.693
k
No. Of half-lives 1 2 3 3.3
., .. -
Concentration 50% 75% 87.5% 90%
Tips
What is the plasma t 12 of a drug?
The time it takes for the plasma drug concentration to fall to half its initial value.
What is the difference between first order and zero order rate of elimination of a drug?
With zero order elimination the rate of elimination is constant and independent of drug
concentration. The t Y2 depends on the amount of drug given and is longer when more of
the drug has been administered. With fITst order elimination the t 12 is constant and the rate
of elimination depends upon how much drug is present, being higher at higher plasma drug
concentration. A constant fraction of the drug is being eliminated in unit time. Most drugs
are eliminated with first-order kinetics.
Zero order reactions7
Independent of concentration
Time dependent
-dc/dt = Ko
Slope -ko
Example: Photochemical degradations
Zero order constant expressed in units of concentration ego milligrams per millilitre per hour.
Or gram/U hour
Linear equation =C =-Kot +Co
Ko is slope of the line = zero order constant (conc./time)
Co is initial concentration
T = time
26-4
Where
Half-life 0.693/k
Rates and orders of Reactions www.Phannacvorep.com
C = drug concentration
Slope of the line is not equal to the rate constant because it includes minus sign.
The negative indicates that slope is decreasing.
Rate ofelimination is independent oftne amount of drug to be eliminated.
(.
C
c=Coc
to
In C = ~ k t + In Co
log C = - kt/2.303 +Iog Co
The zero order elimination rate constant is K
o
and has the units ofamount/time
A constant amount ofdrug is eliminated per unit of time
First order reactions
Rate of reaclion is proportional to Ihe first power of concentration.
Concentration and time dependent
Log ColC =K,I2.303
Co = concentration at to
K = rate constant
A plot of log of concentration against lime produces a straight line with a slope:
Slope -kJ2.303
Half-life t
ll2
First order reaction
0.693
t
ll2
=
k
k<
~ 3 3
ka
Co
~
-
CA, --
t
c
Blood or plasma considered in equilibrium with total volume of distribution.
t,n = (0.693 X Vd) I CL
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PharmacodynalTlics
Questions Alerts!
Agonist and antagonist relations
Pharmacodynamics is the relationship between the concentration of a drug and the response
obtained in a patient.
Drug/Receptor Interactions (Fig 27.1)
Affinity: measure of ability of drug to bind to receptor
Efficacy: measure of how well the drug/receptor complex produces a physiological
response
is comparative measure. It compares the amounts of two drugs necessary to
produce the same size effect in the body
Agonist: and efficacy
Antagonist (blocker): has affinity and zero efficacy
Partial agonist: is the only class of drug that can be used either as an antagonist or as an
agonist.
When only partial agonist present, it will give the response until its ceiling effect
When a full agonist is already present in the body, administration of partial agonist reduce
the effect full agonist, thus act as antagonist.
antagonism
L7" two drugs act on different receptor; cancelling effect
,. Neutralizing antagonism/Chemical antagonism
does not need receptor;
chemicals act on the body (Ex. antacids, digoxin)
27-1
272
Competitive
(reve"ible)
Log clo,e of drug
Drug B-> Full agonist
Drug A. C-+ Partial agonl'I
C
B
. Antagonism
(
log dose of drug
Potentian
. v ,
wr!'t Antagonl,m & Potentiation
control '
Efficacy & Potency of Full and Partial Agonist
Log dose of d",g
Incompetitive . -I I I
(irrev.,lbl.)
LL---,---L?-77--'C---- ...----_.. __..- ....
Log do,. of drug
100
100
Fig 27.1 .
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Type of drug interactions; Matbematical model
Addition 1+1 = 2 (same effect)
_______ Synergism 1+1 = 3 (gives. greater effect)
/ Potentiation 0+1 =2
Antagonism 1+1=0
-f Quantal response: CcvJ:,1dArCf -f- I
ED
so
: Effective dose in 50% oftest population
'----' U LD
so
: Lethal dose in 50% of test population
TD
so
: Toxic dose in 50% of test population
TI: Therapeutic index, a measure of safety of a drug measure by LDsolEDso or TDsolEDso.
Therapeutic Window
The therapeutic window is the useful "opening" between the minimum tberapeutic
concentration and the minimum toxic concentration of a drug.
The minimum effective concentration usually = trough levels of a drug
The minimum toxic concentration determines the permissible peak plasma concentration.
Narrow therapeutic index drugs that require routine plasma drug monitoring.
Therapeutic range of select medications
Procainamide 4 - 10 mglL
Quinidine 2 - 6 mgIL
Disopyramide 2 - 6 mgIL
Lidocaine 2 - 5 mg/L
Valproic acid 50 - 100 mgIL
Carbamazepine 4 - 12 mgIL
Phenobarbital 15 - 40 mglL
Lithium 0.4 - 1.2 mEq/L
Quantal Dose-Response Curve:
=Guassian (bell-shaped) distribution
Graded Dose-Response Curve
=Efficacy =maximum effect
= Potency = different doses, same effect
Log Dose-Response Curve:
= Efficacy: height of log dose-response curve (Emax)
= Potency: ED50
=Competitive antagonist: curve shifts t90 the RIGHT, and the shift is parallel
=Non competitive antagonist: curve shifts to the RlGHT, but the shift is nonparallel
E
max
Mechanism Of Drug Action
27-3
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I. Interaction with receptors
2. Interaction with enzymes
a. Enzyme induction
= Barbiturates, phenytoin, other anti-epileptics, rifampicin, antihistamines,
griseofulvin, oral contraceptives.
b. Enzyme inhibition
= Chloramphenicol
3. Replenishers
= Replace/fill-in endogenous substances or Ouids
= TV fluids, vitamin supplements, HRT
4. Diagnostic agents: . ".
= functional macromolecular component of a specific stereo chemical
configuration with which a ligand interacts in a lock-and-key fashion
a) Regulatory proteins
b) Structural proteins
c) Enzymes
d) Transport proteins
Enzyme Kinetics (Enzyme Inhibitors): Enzymes arc calalyst.ln biochemical reactions, reactants
are commonly known as substrates (S), enzymes (E), ES = Enzyme and substrate complex, P =
product
In the following reaction
E +S <--> ES <--> ES* <---> EP <---> E + P
Enzyme substrate (ES) complex
Enzyme product complex (EP)
The transition state (ES*)
Enzyme inhibition classified in two categories:
Reversible enzyme inhibition
Irreversible enzyme inhibition
Reversible enzyme inhibitors:
This can be categorized into competitive and non-competitive.
Competitive (Reversible) competes with the substrate for binding to the enzyme at
active site, this binding is mutually exclusive. Inhibition can be reversed in the presence of
saturating substrate, since in this case all enzyme active sites will be occupied by substrate
Non-competitive (irreversible) It is independent binding, both substrate and drug bind to the
enzyme at different site. This cannot be reversed by increasing concentration substrate.
The Michaclis-McntcD cquation: By using Michaelis-Menten equation, rate and order of
reaction can be determined.
VI Vm" ISI/{Km+(SJ)
27-4
Pharmacodynamics
>
- --
.r)
The reaction rate [v Jl, maximum reaction rate (Vmax), substrate concentration [S] and the
Michaelis-Menten constant (K
m
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of<={
.-.---.....

V
- -- -- -----. -- -- i--
. 1/2 V
A :'.
:Km.
[S]
The Michaelis-Menten equation first order, when the substrate concentration is much smaller
than K
m
.
The Michaelis-Menten equation how the rate of the reaction (v) depends on the
concentration of both the enzyme [E] and substrate [S],
The only way to increase Vmax is by increasing [E] enzyme concentration.
The Michaelis-Menten equation has the same form as the equation for a rectangular hyperbola;
graphical analysis ofreaction rate (v) versus substrate concentration [S] produces a hyperbolic
rate plot.
Zero order7
Substrate concentration is same as K
m
K
m
=V
max
Substrate concentration do not effect rate
First order7
Substrate concentration is much lower than K
m
Km is lower than Vmax
Substrate concentration directly proportional to rate of reaction.
K
m
Km is the measure of the affinity of the enzyme for it substrate.
Km is the intrinsic property of the enzyme substrate system and cannot be altered by
changing enzyme and substrate concentration.
K
m
lower than Vmax indicates first order reaction.
Km and Vma;< approxiJ.nately same at zero order reaction.
27-5
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IS\ order ratc linear relation with substrate concentration [S]
) receptors may result in opposite effects? (
Effects that arc greater than additIve ( 1"1
The effect whereby two drugs acting on the same tissue or organ through independent
A graphic representation ofa quantitative response between the amount of drug given and
the response of the drug ( _ ,Iv26 f" v-:sL- f!-.
The amount of drug necessary to produce an effect. T.he concentration or dose ofthe drug
required producing 50% of the drugs maximum effect. (.!j ) 6e. SO j I
The maximal response produced by a drug 11...,..VV"" q-
The drug concentration required producing 50% of the maximum response ) SU
An agonist, whieh at even higher concentrations, gives less than 100% response ( 9f(' ) faA10 OCr
A drug which compete reversibly with agonists for the same receptor site and produces no
response ( f'e-ve61 J,1c.) 01-, - '7
It is called an irreversible antagonist thal binds to the receptor sile or another site which D
inhibits the response to the agonist (True/false) No V\- C,.orr:>fW<Pv.J Y"""h"

Vmax depends on [E] and [5] concentration in 1st order equation.
Vmax is the maximum ratc possible to achieve with given amount o[enzymc.
TIpS
I I ohvsiolol!ical antal!onism 2 I ootency ofdrug 3 efficacy of drug

4 dose-resDonse curve 5 svncrQistic effects 6 nOl1-comoclitive inhibitor
7 comnetitive inhibitor 8 I nartiaI 3Ponist - 9 EC
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-
Medicinal Chemistry
Questions Alerts!
Functional groups
Optical isomerism, calculating optitalisomers 2
n
Active chemical rings in drugs structures: Dihydropyridine, indole, piperidine,
pyridine. thiazolidine. dihydrothiazine. pteridine.
Basics of Organic Chemistry
Organic is the, study that contain carbon, hydrogen, oxygen, nitrogen,
sulphur etc. However carbon is the essential'element in organic chemicals.
Atomic number of carbon is 6. Valence of carbon is 4. Carbon can form only 4 bonds (not less
or more than 4). Carbon can form chains and rings and can bind to the functional groups.
Carbon can form covalent bonds (sharing of electron between two elements).
Electronic configurations of carbon are: 1S
2
2S
2
SP2
Hybridization:
v SP
3
=Alkanes =107 =Tetrahedral
\/",SP
2
=Alkenes =120 =Trigonal
'-""SP = Alkynes = 180 =linear
Functional groups
Alcohol (-OH); or hydroxyl group
'. Primary alcohol: PIimary alcohol oxidation produces an aldehyde
Secondary alcohol: Secondary alcohol oxidation produce ketone
Tertiary alcohol: Does not undergo oxidation
Alcohols
OH
H+H
I'i
Primary (1)
un )
, ,

OH OH
R1+R2 R
1
+R
3
I'i R
2
Secondary (.2") Tertiary (30)
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28-1
Amines (NH
2
): Amines are basic
Categorized as: Primary, secondary and tertiary
-, Tertiary amines are more basic than secondary.
Base strength of amines: Tertiary amine> secondary> primary> aromatic
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Chair
Conrormalion
More: Slrain
-
More: slbale:
less Slrain

Boal
Conrorm3fion
More: Stable:
Lc:ss

Tautomerism Planar
;;&
. Amines:
R,
I
NH, R -NH R -N
I
1 I 2 [
R,
R, R
3
PrimaI)' (1 ') Secondary (2') Tertiary (3)
Wbich is more stable

Carboxvlic acid (-eDOH): Pharmaceuticals that contain carboxylic acid group are acidic.
Amide (-CONH
z
): Amides undergo hydrolysis, however amides hydrolysis are. slower than
ester hydrolysis. Amides upon hydrolysis produce acid + amine. Amides bonds are commonly
exist in proteins.
Stability of compounds:
00
/
Esters (-COOCH3): Pharmaceutical that contain ester functional group, are acid or
sensitive, due to hydrolysis.
Hydrolysis of ester produce -7 acid + alcohol.
# AExampJe: acid sensitive beta lactams antibiotics, undergoes hydrolysis when taken orally.
V I(penicillin G!)
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..' . .
Isomerism
Compounds that have the same molecular formula but different chemical structures are isomers
or isomeric.
Do the compounds
have the same molecular
fb"rrmiiae? .
NO
Not isomers
--..-
NO
Do the compounds have
the same connectivity?
NO
YES
Stereoisomers I
I
YES
1\10
I Co nfiguratio nal I
I
Is the isomerism at a
tetrahedral center?
YES
~
Are the compOUndSj
non-superimposable
mirror images?
YES
Optical isomerism
Optical isomers: Contain at least one asymmetric or chiral carbon atom. Asymmetric centre
or chiral centre -7 a carbon atom attached to four different groups. Using number stereogenic
~ or chiral centres or a;;.:2--:..oy .... m......... m.;.:e:.;t;;..r";.:lc;....c:.:a:.:.r..::.bon, one can redict the number optical isomers
p ~ To calculate possible of optical isomers with given chiral centres use
formula =2"
...
~ n = number of chiral centres
28-3
D(+) or L(-) orre<:emic (dL) or ()
Medicinal Chemistry
o-
9f\'JH-CH
J
/; C-C-CH
3
1-/
nly Antitussive
Dextrophanol
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Same physical and chemical properties except in rotation of plane polarized light.
Enantiomers can have large differences in potency, receptor fit, biologic activity, transport
and metabolism.
levorphanol
L ( - I
Narcotic analgesic and Antitussive
lead structure: Chemical substance with therapeutic use.
Pharmacophore: The pharmacophore of drug molecule is that portion of the molecule
containing the essential organic functional group that directly interact with receptor active
site thereby it shows biological activity of interest.
Diastereoisomers: Two asymmetric carbon atoms. They are not 5uperimposable and are!!2.t
mirror images.
Oiastereomers
Analog: Molecule with same skeletal structure with different functional groups attached.
Some examples of analogs: HI-antihistamines (0- missing).
.../Enatiomer are mirror image with one asymmetric center and non superimposable
./Geometrical isomers Trans isomers: To form trans isomers, it is essential to have .... 1.. A.-.I L
double bond. Examples of geometrical isomers include 2-butene, diethyl stilbes.terol (NO", 'f'1 v l>7' cl91
(synthetic estrogens).
Structure Activity Relationship (SAR)
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Phenothiazines
Homolog: Difference of-CHz- in an identical molecules. Example: phenothiazines
(antipsychotic), a chlorpromazine is a dopamine antagonist and used as antipsychotic drug
and tricyclic antidepressants.

/
[1illCH
2
N H
3
h ICH
2
CHtCH
2
N(CH
3
h
.
.. ..... CJ
Bioisosters: The functional groups <'tr atoms that impact similar physical and chemical
properties on a molecule. Examplel methyl, ethyl, bromine, and chlorine
"" . I, '"

vNM h-
I CI r CI
CH
2
CH
2
C(CH
3
h CH
2
CH
2
C(CH
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h
Some examples of bioisosters: phenothiazines, and synthetic estrogens
Important concept! fundamental pharmacophores for drugs used to
treat disease
Pyridine ring Nicotinic acid is vitamin B
3
. This metabolizes
Nicotinic Acid
(]
to nicotinamide.
Nicotinamide
Nicotine
N
Isoniazid
Pyridine
Dihydropyridine ring Dihydropyridines are molecules based upon
Amlodipine
0
pyridine that have been semi-saturated with
Nifedipine two substituent's replacing one double bond
Felodipine
N
Particularly well known in pharmacology
Nicaradipine
H
type calcium channel. blockers
Dihydropyridine
\

28-5
Piperidine ring Present in numerous natural alkaloids such as
Morphine
0
piperidine and qUlriine. and is the main active
Codeine chemical agent in black pepper and relatives,
Heroin hence the name. Piperidine is also-a
Meperidine
H structural element of many pharmaceutical
Thioridazine drugs such as raloxifene. minoxidil,
Haloperidol
Piperidine
thioridazine and mesoridazine
Risperidone
-
"
Muscarinic blockers
Atropine
Ipratropiurn
Bromotropin
Scopolamine
Pvrrolidine ring is a cycfic amine
Muscarinic blockers H
0
Pyrrolidine is found naturally in the leaves of

0
tobacco and carrot
rpratropium
"
Pyrrolidine ring is the central structure of the
Bromotropin amino acids proline and hydroxyproline
Scopolamine
Pyrrolidine
lmidazoline ring

0
Imidazoline is a nitrogen containing
Clonidine
LJ
heterocycle derived from imidazole
...
Imidazoline
Isoxazole: Sulfonamide Isoxazole is an azole with an oxygen atom to
""-t'" '"
8
the nitrogen
Isoxazole also form the basis for the CQX-2
O,N
inhibitor
ISox3zoie
8actams H Penicillin nucleus. Beta lactam is the square
Penicillin's

at the centre
Cephalosporin Cephalosporin's -7 Beta lactam and
o 0 N
thiazolidine ring??
;:;.
O:"Jro.OH
..
"
Beta Lactam .
Amino penicillin's
--
NH2'
Beta lactam antibiotics
Amoxicillin
/
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Ampicillin
JGJCH
.. '"
(
Jr6;.) 1<c;%1
(' I ... , ,R
'HO "
.
.
.
Amino Penicillin's
Pyrazole Pyrazoles are used for their analgesic, anti-
COX II inhibitors H inflammatory, antipyretic, antia arhythmic,
0
\lj
tranquilizing, muscle relaxing,
\ N
psychoanaleptic, anticonvulsant,
"
Monoamineoxidase inhibiting, antidiabetic
Pyrazole
and antibacterial activities.
Indole ring is an aromatic heterocyclic compound
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28-6
www.Phannacyprep.com Medicinal
,
Serotonin
Indole is solid at room temperature. It occurs

(Neurotransmitters, present naturally in human feces and has an Intense
in eNS). fecal odor. At very low concentrations,
H however, it has a flowery smell, and is a
ttL
constituent of many flower scents (such as

orange blossoms) and perfumes. It also
occurs in coal tar
Quinolone ..

Quinoline or benzopyridine, is a heterocyclic
Quinine, hydroxyl quinine

aromatic organic compound
and It is toxic: short-term exposure to the vapour
Quinidine
" I,.
causes irritation of the nose, eyes, and throat
N
H
as and nausea. Longer-term
effects are uncertain, but quinoline has been
Quinoline
linked to liver damage
Sulfhydril group Captopril is an ACE I consist of sulfhydril
Captopril 0 group that gives rash and metallic taste.

-
-
CH
3
2
H
Captopril
GABA derivatives Gabapentin was initially synthesized to mimic
Gabapentin, Pregabalin and
H2NoCOOH
the chemical structure of the
vigabatrin neurotransmitter gamma-aminobutyric acid
L...
(GABA), but is not believed to act on the
same brain receptors. Its exact mechanism of
GABA Group
action is unknown, but its therapeutic action
on neuropathic pain is thought to involve
voltage-gated N-type calcium ion channels.
Originally was developed for treatment of
epilepsy
Imidazole
HistamiDe, histadine and

,
azole antifungars
-
N
H
\
28-7
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1 Amlodipine,Felodipine, 2. Muscarinic blockers, 3. nicotinic acid,
Nifedipine. Nicardipine Atropine, nicotinamide,
Bromotropine, nicotine,
Scopolamine isoniazid
4 Penicillins, Cephaloshorin 5. Pteridyl ring 6. Morphine, Codeine,
7. Clo
..
8. Ranitidine 9. Sulfonamide
10 vnistamine, histadine &

Indole ring 12 quinolone ring
azole antifungals, ARB's
.
13 I of 14 3 rings of cyclohexane cox II
& pyrrOllolne and 1 ring 15 inhibitors
cyclopentane
28-8
Tips
Essential functional groups in the Structure activity of drugs
Pyridine ring ( 2> ,p oV rhaAev-)
Dihydropyridine ring ( i C0><CI21'1" V 'I-r 0.
Piperidine ring ( 2 J b )
Pyrrofidine ring ( 2 I
Imidazoline ring (7 ) * J..
Isoxazole! 9 I
Beta laetam (..y )
Amino penicillins ( mPlc..,II,/.-t..
Pyrazole (IS" I Ccu/.Q-Cd<rb
Steroids (I L1 ),.f, G-r C<:I
". Folic acid ! S . \' rovd.< Pft'A- I I Cf
Imidazole { 10 - A-..-h'" Y:s.. +u ..... y.."t,..
Imidazole ring (I D Ct
Serotonin ( I I l
Quasi ring ( ,,,.,1)...- ) lit _
Vitamin K ( \ z... ) . Jt
Ciprofloxacin (11.-- ) >-<.- Jv... v vc.-
'. Quinidine & Quinine (\'l.-- I.IL oJ Je.-v-,e-L
Isomers ( .$0 l'>oLu:..J.x- t-t... I fQJ.N1 r , h..h.
example of geometrical isomers ( LJ,..... t
1'''1 C "if)
u-I CLOI.UWJ4N:0
'1,+ f+. i.5 .,!'/,I.N./.Ju.,,, ao CC!.ft;L.8+fk-6'cUJ
GAL Ce=c.o..sqnrJa..s)
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Medicinal Chemistry and Pharmacology of
Autonomic Nervous System
Questions Alerts!
.."... Biosynthesis of catecholamine's (Tyrosine --> L-dopa --> dopamine -->
norepinephrine --> epinephrine) _ -,
Structures of direct acting acetylcholine agonist
Structure of atropine and muscarinic blockers Q tt,
Pharmacology and structure of sympathomimetics like pseudoephedrine,
ephedrine.
Pharmacological actions of sympathetic receptors alphal& 2 and beta 1 and 2.
Parasympathetic receptors like muscarinic and nicotinic.
Nervous System
__--Jl .
I
I
I
Central Nervous System (CNS)
Peripheral Nervous System (PNS)
Spinal cord and brain
I
I
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,
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Sensory somatic nervous
System
12 pairs of cranial nerves
I
31 pairs of spinal nerves

29-1
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Functions of ANS
Ganglia is spinal cord Ganglia is near organs
Parasympathetic (cholinergic)
Neurotransmitters
ACh
Receptors
ACh-7M>, M" M], M, and MS, NI
and N2
Neurotransmitters
Norepinephrine (Nf)
Epinephrine (epi)
Dopamine CD)
ACh
Receptors:
Norepinephrine (NE)-7 aJ,(tl.1l1 (Not on
p,)
Epinephrine ct.!> ct.l.lll.
> > ct.
ACh -7 N,
Sympathetic (adrenergic)
The autonomic nervous system CANS) controls involuntary body functions.
The ANS is composed of two divisions:
Sympathetic (adregcnic) system
Parasympatbetic (cholinergic) system.
Types ofNcurolls in ANS . 1.kJ"': .
Gy.r'-jo\v
Efferent neurons (motor neurons) -) deliver message from brain to organs
Afferent neurons -) Collects message from organs to the brain
Efferent neurons divided into the
Sympathetic (adrenergic) nervous system
Parasympathetic (cholinergic) nervous
system
ANS is responsible for regulation of
Internal metabolic activity
Myocardium
Smooth muscle of the viscera
Glandular activity
Hormonal activity
Ensure thallbe body operates in optimum range
Originate in the thoracic and lumbar region Originate in sacral and cranial region
y"- 1.n- p,
..-{:---I-I Post ganglionic nerve fibre very long Post ganglionic nerve fibre very short .()-
Preganglionic nerve fibre very short Preganglionic nerve fibre very long
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Drug receptors
Generally pharmacological receptors can be categorized into 4 types
Seven transmembrane proteins
Ion channels
Transcriptional regulators
1-Transmembrane proteins

Seven transmembrane proteins:
The G protein coupled receptors are the largest types of pharmacological receptors, which
almost 200 human receptors are known to date.
The G proteins coupled receptors are the major therapeutic significance with well-established
therapeutics studies.
Examples of Gproteins coupled receptors as therapeutic targets are:
Transcription regulators: There are over 150 receptors of this family, which acts as
transcriptional receptors. This is second major class of receptors, which include steroid
hormones including estrogens, androgens, the glucocorticoids such as corticosteroids, vitamin
0, retinoic acid, and thyroxin.
norephinephrin{beta-receptoyangiotensin AT
l
, dopamine
serotonin, histamines, and
Gll.!tamic acid (glutamate); excitatory
GABA inhibitory; Benzodiazepine, barbiturates, and antiseizure drugs
Dopamoine (01, O
2
, 03, 0
4
, and 05); inhibitory: G protein linked cAMP: Antiparkinson drugs
and antipsychotics
Norepinephrine excitatory; antidepressants, and antianxiety.
:
/
f-/()4__--'"
Ion channels: There are two types of ion channels
Voltage gated: Na+ channe!, channel, K+ channel
Transmitter gated: neurotransmitter interact with specific receptors
5H1
,One transmembrane proteins: These receptors include several growth factors such as tumor
necrosis factor, serine/threonin kinase, neurotropins, and cytokines.
Most neurotransmitters interact primarily with postsynaptic receptors, but some receptors
are located on presynaptic neurons, providing fine control of neurotransmitter release.
in Autonomic nervous system
Cholinergic receptors are classified as nicotinic N
l
(in the adrenal medulla and autonomic
ganglia) or N
2
(in skeletal muscle) or muscarinic M
l
(in the autonomic nervous system,
29-3
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striatum, cortex, and hippocampus) or M

2
(in the autonomic nervous..sYstem, heart, intestinal
smooth muscle. hindbrain, and cerebellum). '
,
Neurotransmitt Chemical structures Characteristics
ers
Acetylcholine
eH,
Is a neurotransmitter of peripheral
1.----.......... CHJ
(ACh)
HJC-, 'I
nervous system IPNS) neuromuscular
junction. parasympathetic system, visceral
CHJ 0
motor nuclei in the brain stem, and basal
ACCf)'Id>vI",c (ACllI
nucleus of Meynert.
Epinephrine

Uses al. a. 1 or PI, Ph th-adrenergic
receptors, which are G-protein linked
receptors; Plays insignificant role in CNC; is
-
found in the adrenal medulla

Uses aJ, a lor Pl.o Jh.lh-adrenergic
Norepinephrine
receptors, which are G-protein linked
receptors; is the transmitter of
HO postgangfianic sympathetic neurons and
ON
Norcpi_qWl'"
eNS (locus ceruleus); plays role in anxiety
states, panic, attacks, depression
Dopamine

Uses 01 and 02 dopamine receptor, which
are G-protein-linked reception;'is depleted
in Parkinson disease; is increased[;;
scliizophrenia.
.
OH
-
,..
Serotonin {s-

Uses S-HT receptor, which is a transmitter-
hydroxy-
HO I "" '\ \
gated ion channel that is permeable to Na'
tryptamine: SHTj and K' ions; is neurotransmitter of the
d N
raphe nuclei of the brainstem whose
H
'HT
neurons project to widespread areas of
the eNS.
y-Aminobutyric
/'...../COOH Uses the GABA receptor, which is a
acid (GABA)
H,N
transmitter-gated ion channel that
Gama-Aminobutyric Acid (GAB
permeable to cr ions; Uses the GABA
receptor, which is G-protein-Iinked
receptor; is a major inhibitory
neurotransmitter in the CNS.
29-4
Glycine COOH Uses the glycine re.ceptor, which is
H2N+H
transmitter-gated ion channel that is
permeable to cr ion; is the major
ff
inhibitory neurotransmitter in the spinal
cord.
Glycine
Glutamate COOH Uses the N-methyl-O-aparate (NMOA),
H
2
NYCOOH
kainite, gUisqualate Areceptors, all of
which are transmitter-gated ion channels
ff
that are permeable to Na+, K+ and Ca
2
+
ions.
Glutamate
Adrenergic receptors are classified as <Xl (postsynaptic in the sympathetic system), (X2
(presynaptic in the sympathetic system and postsynaptic in the brain), P1 (in the heart), or
(in other sympathetically innervated structures).
Oopaminergic receptors are classified as 0
1
, O
2
, 0
3
, 0
4
, and 05. The 0
3
and 0
4
playa role in
. --
.thought cootrol (limit negative symptoms of schizophrenic processes), whereas O
2
receptor
activation controls the extra pyramidal system. ,-"'...
, v' Mc6f
GABA receptors are classified as GABA
A
(activating chloride
,r The GABAA receptor consists of several distinct polypeptides
and is the site of action for several neuroactive drugs, including benzodiazepines, newer
anticonvulsants (eg, lamotrigine), barbiturates, picrotoxin, and muscimol.
Serotonergic (S-HT) receptors (with at least 15 subtypes) are classified as 5-HT
1
(with four
subtypes), 5-HT
2
, and 5-HT
3
5-HT1A receptors; which occur presynaptically in the raphe
nucleus (inhibiting presynaptic uptake of 5-HT) and' postsynaptically in the hippocampus,
modulate adenyl ate cyclase. 5-HT
2
receptors, located in the fourth layer of the cortex, are
involved in phosphoinositide hydrolysis. S-HT
3
receptors occur presynaptically in the nucleus
tractus solitarius.
Glutamate receptors are classified as ionotrophic NMOA (N-methyl-O-aspartate) receptors,
which bind NMOA, glycine, zinc, Mg
2
+, and phencyclidine (PCP, also known as angel dust) and
affect the influx of Na+, K+, Ca
2
+, and non-NMOA receptors, which bind quisqualate and
, kainate. Non-NMOA channels are permeable to Na+ and K+ but not to Ca
2
+. These excitatory
receptors mediate important toxic effects by increasing calcium, free radicals, and proteinase.
In synthesis of nitric oxide (NO) involving NO synthase increases in response to
glutamate.
Endorphin-enkephalin'(opioid) receptors are classified as J.l1 and J.l2 (affecting sensor motor
integration and analgesia), <)1 and 02 (affecting motor integration, cognitive function, and
analgesia), and leI, le2, and 1(3 (affecting water balance and food intake).
.J .
...../
Sigma receptors, currently classified as nonopioid and mostly localized in the hippocampus,
bind drugs. Opioid receptors and neurotransmitters are peptide type:
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Effector Ore.an
Adipose
Arterioles
Skin and mucosa
Skeletal Muscle
Bladder
Detrusor
Sphincter
Eye
Radial Muscle, iris
Sphincter muscle, iris
Ciliary muscle
Heart
Sinoatrial node
Atrioventricular node
Atria
Ventricles
Kidnev
Lacrimal
Liver
Lung (bronchialmusclc)
Male sex organs
Nasopharyngeal g.lands
Pancreas
Saliyary Glands
Stomach & intestine
Motility
Sphincters
Secretion
Sweat l!lands
Uterus
Veins (svstemic)
SDleen
SvmD3thetic
I Lipolysis
Metabolisc fatty acids
Constriction (cr.,)
Usually relaxation (132. M)
Relaxation (132)
Contraction (cr.,)
Mydriasis (contraction. a,)
Accommodation
(Relaxation.
THeart ratc (13,)-7Chronotropic
i Conduction (13,)-7Dromotropic
t Contractility (131)4 Inotropic
?
Renin secretion (13,)
Glvcogen breakdown ((32)
Ejaculation ((X2)
i Insulin secretion (32)
Viscous secretion (al)
Decrease (32) 4 Peristalisis
Contraction (ttl)4Spincter
T Secretion (M)
i Contraction Relaxes
detrusor
Relaxation Ui.,)
i Dilation
Contraction (a,)
Medicinal Chem'istry
Parasvrnoathetic
Some relaxation (M)b
Some relaxation (M)b
Contraction (M)
Relaxation (M).
Miosis (M)
Contraction. for near vision
(M)
! Heart rate (M,)
! Conduction (M)
! Contractility (M)
?
t Tear secretion (M)
Glycogen synthesis (M)
Contraction fM2)
Erection (M)
Mucus secretion
i Fluid secretion (M)"
Marked water secretion (M)
Increase (M)
Relaxation (M)
Stimulation (M)
T Secretion (M)
29-6
Medicinal Chemistry
. .
Autonomic Innervations and Primary Effects
Receptor type shown in parentheses "Co. alpha, Pbeta, M=cholinergic-muscarinic). Note that
preganglionic synapses for both systems are cholinergic-nicotinic.
Indicate absence of direct innervations. However, receptors are present and may be stimulated
by agonists.
Classification of adrenergic agonist (Sympathomimetics)
Tyrosine
Norepinephrine
Noncatecholamines

."
HO
OH

'"
HO eOOH
.. 0 NH
z
'"
HO
* Dopamine
* Epinephrine
* Isoproterenol
* Norepinephrine
* Albuterol (Salbutamol)
* Terbutaline
* Salmeterol
* Metaproterenol
* Amphetamine
* Ephedrine
* Methylphenidate
Catechol amine type of neurotransmitters Cflvi

Epinephrine
29-7
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'. .
Medicinal Chemistry
Prazocin
Add ocm groups
Note: phenylethallolamine
Alpha2 agonist
CH
3
HO 1:1- NH,

Alpha Blockers
1\ on
CH''r()lOyN'--.JN-C-",d'

NH,
Prazosin
Melllyl Norepinephrine
o

OJ IN
; Guanidine group
NH, DNA & RNA basic
H

HN..J>'-- lmidazofine ring
Propanolol
Methyl dopa - a prodrug
Sympathetic antagonists
Beta Blockers

)) COOH
Decarboxylation
Clonidine

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Medicinal Chemistry
Classification of Cholinergic Agonists
Choli.netgic
...-
DU<ct
cholinergic
a .ust
IndireCI
cholinergic
agonislS
"Ecbothiopbate:
"Malathion
"Parathion
"Sarin
'Somao
"Physostig:mooe
'Nc:osligminc
'Demecarium
"Pyridostigminc
Antixcl)"lcbol iocslcrascs
"Edropbonium
'TacriDc:
"Oooepezi\
Pilocarpine
Cevimeline
ACClylchol'
agooists
Ikthanecbol
'Carbachol
_ activity of direct actmg cholinergic drugs
CH3
I A ,OVCH3
Acetylcholine H3C;r v II
CH
3
a-
CH
3
./ CH3

\ CH3
CH
'Methyl
Carbamate
CH /
1
3
Q

. I QlII
CH
3
Methanocholine
Correction: acetyl group
Carbacholine Bethanacholine
Indirect acting sympathomimetics amine: Example: Hydroxyamphetamine, ephedrine or
, pseudoephedrine, methyl amphetamine, and tyramine.
Indirect acting sympathomimetics amines may have one, two, or no hydroxyl groups. The less_
the hydroxy! group the higher the lipophylic and the greater the absprption and
duration of activity after oral administration. Alkyl substitution at the alpha carbon next to
amino group reduces the destruction of phenol ina-phenyl compounds and increases
-
lipophylic characters methcrystal structure
o 1-1
, I

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J-
29-10
Medicinal Chemistry
Important concept!
Structure activity of muscarinic
blockers
Quaternary amine
Ipratropium
Tiotropium
Glvcopvrrolate
Ester group
Epinephrine act on? ( :;,") 7, '(
Norepinephrine act on? ( 5,1', -, )
Enzyme that catalyzes norepinephrine to epinephrine ( 10 )
Muscarinic drugs essential group for anticholinergic action is?
Muscarinic blockers structure contain? 2-, J I &
Acetylcholine, methanchol, carbachol and bethanechol differs in? ( it
competitive muscarinic blocker, that act on vestibular system and the eNS (
Choose 3 examples of direct acting acetylcholine agonist? , ,
Scopolamine mechanism is -7 (13 )
Methanachot is structurally similar to acetylcholine, however differs in -7 t1
Write three examples direct acting acetylcholine agonist? h, 2-,j )
Organophosphate antidote is? ( vV
Atropine overdose is treated by { can get into brain
Myasthenia gravis is treated by (
Structure activity of anti-cholinergic drugs
.-----.:::..-_-----------
I Muscarinic <Jntae:onist I
f0w-"> 'Ir

Pyrrolldin"----.... N / H OHJ alcohol
o )
I '" ) fromatic hydrocarbon
o /' .
. y
Atroplrre- Scopolamine
QUASI RING IS PRESENT IN MUSCARINIC ANTAGONIST; IT IS COMBINATION OF Piperidine +
Pyrrolidine. longer the chain on nitrogen of quasi ring, lower antimuscarinic activity
lips
l
1. Meth.nol 2. carbachol 3. Bethanechol
,.
One methyl group 5 Alpha 1 6. Alpha 2
7. Beta 1 8. Beta 2 9. Scopolamine
10 phenylethanolamine N- 11 Quasi ring 12 Piperidine & pyrrolidine ring
methyl transferase
13 Competitive muscarinic blockers, it act
on vestibular system and the eNS.
Tertiary amines
Atropine
ScopoJamine- JV1lJjl,.,.,sl{ ...u..
Benztropine -
Tnhexyphenidyl
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Medicinal Chemistry,
Medicinal Chemistry and Pharmacology of
Histamines, Serotonin, Prostaglandin and Non-
SterJidal Anti-inflammatory Drugs
. 0"
Questions Alerts!
Chemical structure of diphenhydramine (lipid soluble) as sedative.
Serotonin synthesis from -7 .. ...,
pharmacological actions of agonist (tri!l.tans) and antagonist I. /" c,UJUl
-LlAAA bt't ,tVI"1ift.. wt.cu""'-(j
Structure prostaglandin analogues PGEl (misoprostol) and PGF2alpha
(Iatanoprost)
Pharmacology of and zafirlukast.
Acetaminophen and metabolism that explains hepatotoxicity.
Autocoids (local hormones): Chemical mediators that the body releases as a response to
pathogens or noxious substances. Produced in the body and has profound pharmacological
effects.
Autocoids or chemical mediators ,.
I
Amine types
Histamines
Serotonin
Endogenous type
Ecosonides
Prostaglandins
Prostacyclin
Thromboxane
Leukotrienes
Bradykinin
Amines: No real clinical application in the treatment of diseases however antihistamines are
of great importance. Amine types of autocoids include: Histamines and serotonin
30-1
Chemistry of Hi-antihistamine: Usually lipid soluble. and similar in terms of absorption and
distribution.
Good absorption after oral administration distribution with peak plasma concentration of
1 to 2 hours.
Allows some to go to the blood-brain-barrier especially structural resemblance to
histamine
Endogenous Peptides
Site of production for endogenous peptides are Gil, kidneys, lungs, pancreas and uterus.
Physiological actions of endogenous peptides are:
Prostaglandin's; Pain sensation, development of inflammation
Thromboxane: Aggregation of platelets
Prostacyclin: Inhibition of platelet aggregation
leukotrienes: Inflammation, chemotactic properties (PLlII substances to them)
Histamines
Histamine is produced from '!last cells. Histamines act on three receptors, of these HI, Hz
receptors are excitatory and H3 receptors. ,.r."-')- (;):J &
{IJJ
Physiological functions of HI receptor typical; () 0 0
Allergic and anaphylactic response to histamines. J
Gives bronchoconstriction, and vasodilatation. c;=:::,
'!I
Increase capillary permeability. (1'J
Spasmodic contractions of smooth muscle ( j..,,)( . h...,.l
AI/..fv...... .... "I-l'
iJ'
.
-CO, '.Jt
Histadine Histamine _1.1 _ ..... INion
!.-. er""'"
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HI antihistamine chemical classification
Ethylene diamines: Pyrilamine. and triplennamine
Alkylamines: Brompheniramine, chlorpheniramine, and
acrivastine.
Ethanolamines: Diphenhydramine. dimenhydrinate, and
doxylamine
Piperazines: Meclizine, cyclizine, hydroxyzine, and cetrizine
PhenotRiazine: Promethazine
Dibenzocycloheptenes: Cycloheptadienes
Pthalazinone: Azelastine
Medicinal Chemistry
Important
Concept!
Structure activity
relation of
antihistamines
"{. ..... J-.-p'.J
.<JI,.J,!l, l' }y).& 3'
Co uu. (j edJ,.ov..,
30-2
www.Phannacyprep.com Medicinal Chemi.stry
Cyclizine
'--
Diphenhydramine
Piperidine: Terfenadine, astemizole, levocabastine, loratadine, and fexofenadine.

Tertiary amine t},)C-4
L)p\d sdJ,J' '7

Mechanism: Competitive antagonist of histamine receptors. H
1
receptors are located in the
brain, heart, bronchi, GI tract and vascular smooth muscle. Mast cells and basophiles are
principle histamine containing cells
HI - Antihistamine
I
r()oJv1'l
1
1/.DtI\
I
1
st
Generation 3
rd
Generation
Ethanol amines
2
nd
Generation
Piperadine Derivatives
Diphenhydraminj I'YJvtfJl'v
Piperazine derivatives
Desloratadine (Aerius)
Dimenhydrinate
Cetrizine (Reactine)
Doxylamine
Piperidine Derivatives
Alkyl amines
Fexofenadine (Allegra)
Chlorpheniramine
Loratadine (Claritin)
Piperidine Derivatives
Azatadine, Cyproheptadine
Piperizines
Meclizine, Cyclizine
hydroxyzine
Side effects: Sedation, dizziness, nausea, constipation, diarrhea, loss of appetite and
anticholinergic
Metabolism of antihistamines: Some examples of metabolites of antihistamine, that are used
as drugs.
loratadine -7 Desloratadine
Hydroxyzine -7 Cetrizine
30-3
N-H
OH
Medicinal Chemistry
Fexofenadine
Desloratadine
N-COOCH
2
CH
3
~
J CHJ
I CH
J
N '"
OH
Terfinadine
Loratadine
Terfinadine -7 Fexofenadine
Pharmacology HI-antihistamines
Hj-antihistamine therapeutic uses: Antihistamine may bring relief to cold symptoms, runny
nose, red and itchy eyes. Allergic rhinitis symptoms such as nasal allergies. Antihistamine
Histamine H)-receptor blockers
I
-
Particularly Particularly Particularly I All H1- antihistamines
I
Diphenhydramine, promethazine cyproheptadine
promethazine
Anti Alpha
Dopamine
Serotonin Histamine HI Histamine H
2
Cholinergic
f--
Adrenergic
receptor
receptor receptor receptor
(muscarinic) receptor
HI antihistamine pharmacological actions (drugs action) takes place by blocking blocks H
t
-
histamine receptor effect. This results in beneficial effect on, Allergic symptoms, seasonal
rhinitis, conjunctivitis, rhino viral infections (common cold) and urticaria.
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Medicinal Chemistry
sedative properties are utilized to treat temporary relief of insomnia. Antihistamines are
effective to treat nausea and vomiting.
Used for;
Allergies-7 2
nd
gen
Runny nose-'7 Diphenhydramine
Insomnia -7 Diphenhydramine,
Nausea and vomiting -'7 Dimenhydrinate, doxylamine
Motion sickness -7 Meclazine & 2
nd
gen or scopolamine
Side effects:
Anticholinergic-'7Dry mouth, constipation, tachycardia, and difficulty voiding urine.
eNS: Dizziness, drowsiness, performance impairment (memory, work performance, visual
motor coordination) .
GI: Constipation
Contraindications with mainly first generation anti histamines:
Narrow angle glaucoma,' bladder neck obstruction, hyperthyroidism, cardiovascular disease,
and benign prostate hyperplasia (BPH).
Comparison of 1
st
and 2
nd
generation of HI antagonist
First generation Second generation
Higher sedation and anticholinergic Less sedation due to less lipid soluble and do
Tertiary amine (cause sedation) not penetrate the BBB.
Lipids soluble, and can cross blood brain NO anticholinergic effect
barrier Drug interaction
More central anticholinergic side effect Terfenadine/astemizole: cardiac arrhythmias
Anti-serotonin characterized by prolong QT interval (torse
Antibradykinin de pointes)
Usually OlD Grapefruit juice (apple, orange) reduces oral
bioavailability of fexofenadine.
Dimenhydrinate, Meclizine, cyclizine and Cetrizine have high fatigue and somnolence
promethazine are useful for the prophylaxis (10%)
of motion sickness and vertigo. Loratidine have low fatigue and somnoJence
Promethazine is the most potent
antihistamine, and limits its use due to
sedation
Pregnancy: Bromopheniramine can cause teratogenicity. All 1
st
gen and 2nd generation
antihistamine are used in pregnancy except: Bromopheniramine due to its teratogenicity. 1
st
generation commonly used due to its wide experience.
30-5
I
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30-6
H
1
antagonist side effects: Cimetidine can cause gynecomastia
Mild diarrhea, or constipation, headache, myalgia, confusion, hallucination, and excitement.
.. 1
Medicinal Chemistry
Ranitidine
H
1
receptor
','
. PPls
Muscarinic receplor
_t-_Atropine
N-CN
C"'I' I CH,SCt+,CtJ,NH-C-NHCH,

In children (less sedative) antihistamines such as: Loratidine or use sodium chromoglycate.
First generation impairs academic and learning abilities in children. Most antihistamine and
nasal cromoJyn considered safe in children over 2 years of age. There is limited information
about fexofenadine in under 12-year-old age.
Hz receptor antagonist (H2RA); present on parietal cell, and help to produce secretions, H
2
receptors mediated functions; H
2
receptors responses to histamine such as: increased
secretion of gastric acid, increase pepsin and intrinsic factor (Castle's factor).
C-PNVe!<J c.""' v
Ach Histamine Gastrin
Topical antihistamines: Olopatadine (Pantanol), Levocabastine (Livastin), Emedastine
(EmadineJ, Azelastine (AsteJin, Optivar), and Kitotifen (Zaditor)
Topical applications of H
1
receptor antagonist to the eye relieves itching, congestion of
conjunctiva and erythema. The density of mast cells are high conjunctiva and tear film.
H
2
antagonist chemistry
Cimetidine, an Hzreceptor antagonist
Classification of H
2
antagonist (H
2
RA): Ranitidine, Cimetidine, Famotidine and
Nizatidine (end with "tidine")
Hz antagonist pharmacology: Hz receptor antagonist competitively blocks'H
z
receptors thus
blocking the effect of histamines on gastric secretions.
Hz antagonist therapeutic use: To treat heartburn, dyspepsia GERD, Gr ulcers, Stress-induced
gastritis,
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Medicinal Chemistry
Administration: all H
2
RA are available oral and cimetidine, famotidine and ranitidine are also
parenteral. Oral have rapid absorption.
SerotOnin (5i-fydroxytrypfamine; 5KT)
Serotonin
Melatonin
Niacin
Tryptophan
Serotonin (5HT)
Indole ring
Tryptophan (amino acid) -7 5-bydroxy tryptophan -7 Serotonin (neurotransmitter).
Conversion of tryptophan to serotonin takes place in two reaction, first hydroxylation and
decarboxylation catalyzed by tryptophan hydroxylase and L-amino acid decarboxylase
respectively. Serotonin contain indole ring.
NH
2
.
NH2
'?' . HWH2CH2NH2
o ./ I N I COOH '?' I I COOH I I 0 I
V H -------1.-_ . 0
Hydroxylase Decarboxylase MAD
Tryptophan Hydroxy tryptophan .. Serotonin (5HT)
I Vlcltr1tt a u.h<..
c:ll CAcf
Physiological functions of serotonin receptors: Serotonin group has several subtypes of
receptors: SHT
1
, SHT
2
, and SHT
3
-70eficiency of SHT
1
, SHT
2
and SHT
3
gives anxiety,
depression, aggression, impulsive and appetite.
SHT
lD
-7Auto receptors inhiDit presynaptic activitY in both serotoninergic and adrenergic
neurons in the eNS.
SHT2-7Vasoconstriction, and platelet aggregation
SHT
3
-) Excessive of SHT3gives nausea/vomiting
SHT4-) Release of acetylcholine in the enteric region.
Subtype location Drug Clinical Use
S-HT
1
CNS Buspirone Antianxiety
, I"S-HTIb/ld CNS, vasoconstriction Triptan attacks
5-HT
lc
CNS
Platelets, smooth muscles, Ergotamine (cafergot) Antimigraine (acute)
CNS Cyproheptadine
S-HT
3
eNS, gastrointestinal Ondansetron Antiemetic in chemotherapy
S-HT
4
CNS, gastrointestinal
30-7
(
.,
,
SHT 10/18 receptor agonist therapeutic uses: Triptans are used to treat migraine headache
attacks.
Medicinal Chemistry
Serotonin
SHT
1
receptor class of drugs
SHT
1B
/
1D
receptor agonist
Mechanism: contraction of arterial smooth muscles, especially in carotid and cranial
circulations
Triptans (all are indole derivatives): Sumatriptan, Rizatriptan, Naratriptan, Zolmitriptan,
Almotriptan, and Frovatrrptan
SHT 10/18 receptors pharmacological actions: Cause constriction
SHTID receptor agonist side effects: Feeling of warmth, dizziness, tightness or heaviness in the
chest, rarely patient may experience chest pain.
t
I 5HT,.
I
]5HTlblld
II
5HT,
I
I
5HT,
I
I 5HT.
I
Ergotamine (DIIE)
+
Agonist Antagonist
Agonist
Agonist Partial agonist of 5HT1a Cisapride
Buspirone
Triptans and 5HT
1d
Ondanselron
..
Sumatriptan Antagonist of 5HTza:
Alosctron
Rizatriptan atypical antipsychotic
Fabesetron
Zolmitriptan Olanzapine, clozapine,
Ramosetron
Naratriptan
and risperidone
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4
agonist
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Cisapride (a benzamide), and tagaseride (indole derivative). Ergotamine-serotonin partial
agonist: Ergot alkaloids have agonist and antagonist properties
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Medicinal Chemistry
Ergot alkaloids and derivatives with antagonist/partial agonist activity include: ergonovine,
dihydroergotamine (DHE), methysergide and
CI

OCH
3
CH30
bromocriptine. Cisapride
Serotonin antagonist: SHT
3
receptor antagonist; Ondansetron (indole derivatives) and
Granisetron (benzimidazole derivative)
Indole ring
Ondansetron
GOOH
SHT3 receptor antagonist pharmacology Act on SHT
3
mixed receptors and can effect on
nausea and vomiting.
SHT
3
receptor therapeutic use: Ondansetron and granisetron are used to treat chemotherapy
induced or vagal stimulation and surgery nausea and vomiting
SHT
3
receptor antagonist side effects: Ondansetron side effects: Constipation, headache,
dizziness and granisetron: diarrhea
Prostaglandins, throboxanes, prostacyclins and leukotrienes are synthesized from arachidonic
acid. These four are naturally occurring 20-carbon cyclopentanofatty acids
derivative.
Ecosonides
Ecosonides are metabolites of arachidonic acid (a fatty acid). Examples of ecosonides are:
prostaglandin analogs, thromboxanes, and prostacyclins.
Arachidonic is derived from linoleic acid or taken from diet and esterified to phospholipids
(phosphatidylethanolamine) $.'tc..1) p .... at pe..phclL
Prostaglandin (XI. '1, K ,d I pa nc4M/l4 4-
Prostaglandin has been classified based presence and absence of keto or hydroxyl groups at 9
and 11. Subscripts relate to the number of double bond present in aliphatic chains.
9
30-9
Medicinal Chemistry
Cyclooxygenase
- NSAlD. ASA. coxon
Leukotrienes
tL;poxygenase
Arachidonic acid
PGE,& PGF,
t Uterine tone
t Vascular tone
..
Phospholipase A
z
Prostaglandins G
Hydroperox;dase
PGH
2
&- Thromboxane A
z
1 I t Paltelet aggregation
, +Vascular tone
Dipyridamole
Prostacyclin (PGI
2
)
I
Platelet aggregation
Vascular tone
Bronchial tone
Uterine tone
!
Membrane phospholoipids 0 ..
t
Corticosteroids
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PHYSIOLOGICAL FUNCTIONS: GJ ,smQ9th .
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I PGE,
I PGE; I PGF",
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Protects gastric
Pyrogen
Bronchoconstricti
Decrease
Increase Platelets
IlJucosa
elevate PGE
2
on contraction of
platelets
aggregation
contraction of
uterus aggregation
..
uterus
Misoprostol
I
! Tbrombox3ne A
2
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Alprostadil
Epoprostenol
Dinoprostone
Bronchial & ASA
Bronchial & smooth
Blood vessels
Dipyridamol
smooth muscle
Dronchial &
muscle
dilatation
inhibits
dilatation
smooth
constriction Platelet aggregation
muscle
Inhibit
dilatation
Cr ,QMp"'"
aggregation
30-10
PGE analogs
PGE
1
analogs classification: Misoprostol, and alprostadil
PGE
1
analogs medicinal chemistry: Misoprostol is chemically belongs to ecosonides.
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PGE
1
analogs pharmacology: PGE
1
and PGH
1
can be used to produce relatively local
vasodilatation.
PGE
1
analogs therapeutic uses:
Misoprostol (Cytotec): is used for prevention of NSAID induced GI ulcers.
Combination products: Naproxen + misoprostol, and diclophenac + misoprostol
(Arthrotec)
Alprostadil (Caverject): In adults it useful for the treatment of impotence due to erectile
dysfunction.
Alprostadil (Prostin VR pediatric) is used for temporary maintenance of a patent ductus
arteriosus when awaiting corrective surgery for congenital heart defects.
PGE
1
analogs side effects:
Misoprostol: Abortificient side effect
PGE
z
analogs classification
Dinoprostone derivatives: Dinoprostone
PGE
z
analogs therapeutic uses:
Dinoprostone are used for their abortificient effects and to induce cervical ripening in
pregnancy.
.' PGF
2
]analogs classification
Latanoprost (Xalatan), Travoprost (Travatan), Bimatoprost (Lumigan), Unoprostone (Rescula)
and Carboprost (Hemabate)
PGFzcJanalogs pharmacology
PGFzdJanalogs therapeutic uses
30-11
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latanoprost (XalatanJ-7 Used topically to lower intra ocular pressure in OAG, combination
products latanoprost + TImolol indicated for open and dose angle glaucoma.
Travoprost (Travatan) -7 topical ophthalmic drug
Bimatoprost (lumigan) -7 topical ophthalmic drug
Unoprostone (Rescula) -7 topical ophthalmic drug
Carboprost (Hemabate) -7 abortificient (withdrawn)
PGFillaoalogs side effectsEye pigmentation, lengthening and thickening eye lashes.
PGI analogs (Prostacylcin): Epoprostenol (Prostcyclin, Flolan)
PGI analogs (prostacylcin) chemistry
PGI analogs (prostacylcin) pharmacology
PGI analogs (prostacylcin) therapeutic use
Epoprostenol : Used in the treatment of emergency pulmonary hypertension.
Thromboxanes (TxA
z
)
Increase platelet aggregation
Potent vasoconstrictors
l.eukotrienes
leukotrienes are produced from arachidonic acid; this reaction is catalyzed by Iipoxygenase
enzyme. Play important rore in numerous physiological functions;
Slow reacting substance of anaphylaxis.
Heart; Negative inotropic, smooth muscles chemotaxis
GI tract; Neutrophils chemotaxis
Pulmonary (major); Bronchoconstriction, increase permeability, and increase mucus
secretion.
Blood; chemotactic agent for neutrophils, eosinophils, and modify lymphocyte
proliferation and differentiation.
leukotriene antagonists chemistry: Zafirlukast (Accolate) and montelukast (Singulair) have
peptidomimetic structure and inhibit LT4 and LTD" receptors. ~ 1'1 c t ~ t!J"ItJ.., 2-"JPlUSOo
leukotrienes antagonists therapeutic uses:
Zafirlukast: For the prophylaXis and chronic treatment of asthma in adults and children
12 years of age and older. Take empty stomach to enhance it absorption
30-12
www.Phannacyprep.com Medicinal Chemistry
Montelukast: Can be used in children over 2 year age, montelukast may be taken without
regard of food. Available as chewable tablet (once daily in the evening) and granules.
Administer granules directly into mouth or mix 'with teaspoon of cold or room temperature
applesauce, carrot, rice or ice cream. Do not take aspirin or NSAIDs while on this medication.
Leukotriene inhibitors are drug of choice for the treatment of aspirin induced asthma.
Side effects: GI upset, abdominal pain, diarrhea, liver dysfunction, and headache.
Drug interactions: Terfenadine significantly reduces the plasma concentration of zafirlukast.
NonSteroidal Anti-inflammatory Drugs (NSAID)
S!\w
salicylates derivatives
.L
. . .
Acetyl salicylic acid (ASA)
-"'.s p/Iii"'"
and antl-
.'t........
lnflarrlmatOf)'
Salicylic acid
Methyl salicylates Wintergreen oil-topical agent) counter irritant
Salsalate, sodium thiosalicylate injectable
Choline salicylate oral liquid
Mesalamine
Olsalazine
Sulphasalazine
Diflunisal Diflurophenyl derivCltive of salicylic acid
p-Aminophenol derivatives

Acetaminophen Analgesic, and antipyretics
Pyrazolone derivatives
Sulfinpyrazone
Phenylbutazone
Propionic acid derivatives
Ibuprofen
Ketoprofen
Naproxen
Garprofen
Fenoprofen
Acetic acid derivatives
Indomethacin Indocin: high renal side effects, have high
antinAammatorv
Didofenac Voltaren
Ketorolac Teradol
Sulindac Clinoril
Etodolac
Anthranilic add derivatives
d:wJJ10 ......
.
t Ace1fcfa.tt
c
4<,1 31>.TIY

1iY)(l 4) II c.eta
M

-
)
Only lumerocoxib has no sulfa allergy, where all other Cox II inhibitors have sulfa allergy.
Medicinal Chemistry
r,:::;y-OH

Methyl salicylate (Winte.rgreen oil)
Diflunisal (Dolobid)
r(YCOOH

}-CH,
o
Acetyl Salicylate
Mefenamic acid
Medofenate
Oxicams derivatives
PiroKicam Feldene
Meloxicam
PyTazoJe derivatives: caxlI inhibitors
celecoxib Celebrex
.
Chemistry of Salicylates derivatives
Acetyl salicylic acid (ASA)
Pharmacological actions: ASA exhibits analgesics, antipyretics, anti-inflammatory 3fld
antiplatelet actions. ASA irreversibly inactivates both COX-. & COX-II, where as all
other NSAIDs inactive reversible COXI &COX. 4feU-
h9W '. P"" wJ1a"- .,wu.""

Analgesic action 9. V pl,-J lI\ f
,.... /-
Antiplatelets
Irreversible platelet inhibition and inhibition ofCox-l& Cox-!! action gives antiplatelcts
aClion. 60 to 80 mg (81 mg).-. ct<Jd (p.v--f'-<. u..vJeA-) )l Lt>.v
I- ew"",-,
Anti-inflammatory action t1d e....t-..J
F C-<Jh.
(,j f4- cLu- at Mil o.J- Cd
Prostaglandin (PGE2) thought to sensitize the nerve en 0 e action of bradykinin,
histamines and other chemical mediators, thus inflammatory process may cause analgesic
action. Decrease ofPGE2 synthesis represses the sensation of pain. ASA analgesic dose:
325 mg every 4 to 6 h
, "n .",,' .. wh.f iA "vJ.,,).._ ?
l " . I
Prostaglandm PGE2 stimulatIOn occurs producmg
agents such as cytokines is released from the'wllire"oloOd cells that are activated by
infection, hypersensitivity, malignancy or inflammation. Salicylates lower temperature by
I decreasing PGE2 synthesis. ASA antipyretics dose 325 to 650 mg q 4 to 6 h PRN
Reye syndrome -7 Children with flu and viral infection should avoid using ASA, because it
may cause Reye's syndrome
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Cox-I, Cox-II and prostaglandin inhibition. The anti-inflammatory dose of ASA 650 mg
Mechanism of action of ASA
ASA
COX I &11
(
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II
O-C-CH
3
(inactive)
COOH
(Y0H
Problems associated with NSAID and acetyl salicylic +- M aCJ c&s "S
Respiratory depression: Toxicity respiratory (increase CO
2
and decrease pH)
GI effects: due to inhibition of pro taglandin PGEs. Prostacyclin PGh inhibit gastric
secretion. The most common side effects of salicylate are GI disturbances like nausea,
vomiting, epigastric discomfort, peptic ulcers (dyspepsia, heart bum).
PGE
2
and PGF2a stimulate synthesis of protective mucosa in stomach and small intestine.
Indomethacin has the highest incidence of (35 to 50%) of GI ulcers
Renal problems: PGE2 and PGh are responsible for renal blood flow. It can cause acute
renal failure
Reye's syndrome: is an acute syndrome that may follow influenza and chicken pox infections in
children. It is characterized by symptoms of sudden vomiting, violent headache, and unusual
behavior.
Sulfasalazine chemistry
Contains azo bond. Sulfasalazine contains a sulfonamide group, may cause allergy
patients with sulfa allergy.
In metabolism undergoes azo reduction (phase I). Metabolism produces 5-amino salicylic
acid. Sulfasalazioc, olsalazine, balsalazine are metabolized in the colon by gut flora to
yield 5ASA. Avoid in ASA allergic patients.
Sulfasalazine therapeutic use: Drug of choice for ulcerative colitis.
Sulfasalazine side effects: can cause megaloblastic anemia, and infertility (in men).
Azo bond
Sulfasalazine
Azoreductase
at Gu1
NH
20
CO,H
,""
h
OH
S-aminosalicylic add
(Mesalamine)
Azoredudion in colon
30-15
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DiOurophenyl derivative of salicylic acid
No salicylate toxicities (docs not produce salicylic acid)
No antipyretic action
Propionic acid derivatives: Ibuprofen, Kctoprofen (Orudis, Oruvail), Naproxcn (Naprosyn,
Naprelan), Carprofen and Fenoprofen
Propionic acid
Jr(;.C ~
I Q, ~ H C O O H
Ibuprofen
Acetic acid derivatives: lndomethacin (lndocin), Diclofenac (Voltaren), KetoroJac (Toradal),
Sulindac (Clinoril) and Etodolac.
Acetic acid
H 3 C O ~ C O O H =
tQ.l.,JLCH
1.
0
N
,O '
~ 'ndome'hacln
Acidic acid derivative therapeutic uses
Indomethacin (indocin)-7 used for acute gout attacks treatment. more eNS effect, aplastic
anemia and contraindicated in elderly
DicJofenac (Voltaren)-? ophthalmic drops
Ketorolac (Toradol)-? short-tenn use only
Sulindac (Clinoril)-7 safest in renal failure
Anthranilic acid (fenamates) derivatives
Mefenamic and Meclofenale acid
AnthraJnic acid
~ H ~ C H
<Q{-NH\Q;
eOOH
Mefenamic acid
Mefenamic acid is associated with severe diarrhea and associated with inflammation of bowel.
30-16
Anthranilic acid (fcnamates) derivatives fhcrnpeutic usc:
Preferred in dysmenorrhea TC, 4
th
Ed. Page 758
Oxicams derivatives
Piroxicam (fcldene), Mcloxicam (?vfobic) and Tenoxicam.

.. N'CH
0, '
Piroxicam
Oxicams derivatives side effects
Chemistry
Piroxicam (Feldene)-7 Its mean half life is 50 hours, thus this can be used once daily dose,
more bleeding, contraindicated in elderly.
p-Aminophenol derivatives
Acetaminophen chemistry: Phenacetin or acetanilid-7 Acetaminophen
Acetaminophen is an active metabolite ofphenacctin and acetanilide.
hfffil / H,COCHN
0 0 Dealkylation
r '-'!' '" J.,AJ CH,CONH j OCH,CH,
'3' '''1 CI r .eJa'",.-,) I
(?\-U p"_ . OH
W+ a Phenacetin Acetaminophen
Acetaminophen undergoes phase I metabolism and glucuronidation. sulphate conjugation, and
glutathione conjugation. Toxic intennediate of phase I metabolism is Nbenzoquinoneimine,
which is catalyzed by glutathione conjugation leading meracaptopurine.
Acetaminophen therapeutic uses: [t is used as antipyretic and analgesic.
Acetaminophen phannacology: Have antipyretic and analgesic action.
Inhibits central prostaglandin synthesis (eNS). Less effective in blocking peripheral
prostaglandin synthesis, acetaminophen has no anti-inflammatory activity and does not
effect on platelet function.
. Antipyretic action dose is 325 to 650 mg q 4 to 6 h PRN
Acetaminophen does not have Rye syndrome and may safely be able to be used in patient
(child) with varicella or an influenza type viral infection.
Advantages: Stable in liquid thus available in various solutions.
in ASA or patierits._Can be in children because

Acetaminophen side effects:
30-17
Medicimii Chemistry
lutalhione conjugation
1
"
Cytochrome CYP 450 ? '"
U9"
N-benzoquinoneimine
o

Acetaminophen Metabolism
Acetaminophen

S Glucoronidation
Sulfate conjugation
Mercaptopurine C
OHS
i

"NH2 0
Glut3ti_
Structure of N-acetylcysteine:
r. -'
Skin rash, hemolytic anemia (long term phenacetin use) renal dysfunction and tubular
necrosis hepatotoxicity if it used more than 4 gfday. With excessive alcohol max dose 2
g/day.
NAPB: N-acetyl p-benzoquinoneimine
UDP-GT = Uridinyl diphosphate glucuronidase transferase
Glutathione is consist of cysteine, glycine, and glutamic acid
Aritl 0 e'bf acetaminophen is N-acetylcysteine --; \.s
cjWv
,):-
Cyclooxygenase inhibitors
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COX-I functions
Daily synthesis of prostaglandin that contribute to normal homeostatic (arrest of.
bleeding).
Protection of the gastric mucosa through prostaglandin
Hemostasis through the synthesis of thromboxane.
COX-II functions
30-18
Expressed only in response of inflammation of injury. E.g. Celecoxib (Celebrex), Veldecoxib
(Bextra)
Pyrazole derivatives
COXII inhibitors: Celecoxib (Celebrex), and veldecoxib (Bextra)
Side effects: Arrhythmias, GI upset, Diarrhea Back pain, Respiratory problems,
nephrotoxicity. Celebrex contain sulfa group, therefore celecoxib has sulfallergy.
Celecoxib and veldecoxib have functional group.
OpioidAnalgesics
Chemical classification of opioids
Benzomorphan derivatives
Pentazocine hydrochloride
Pentazocine lactate
Diphenylpropylamine derivatives
Propoxyphene hydrochloride
Propoxyphene napsylate
Morphinan Derivatives
Butorphanol tartrate
Nalbuphine hydrochloride
Natural opium alkaloids
Codeine phosphate
Hydromorphone hydrochloride
Morphine hydrochloride
Morphine sulfate
Oxycodone hydrochloride
Oxymorphone hydrochloride
30-19
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3
'1

Medicinal Che ' mlstry
Butorphanol (Stadol)
Codeine

N CH3
}-J-...J--cH
3
H H
3
Pentazocine (Talwin)

a
HO
CH
3
0
o 0
Oxycodone (percodan)
Naloxone (Narean)

Hydromorphone
H
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Phenylethylamine De, . Ivatlves
Methadone
Phenyl p. . lpendine De . nvatives
Alfentanil hydrochl .
Fentanyl citrate onde
Meperidine hydroch .
Sufentanil citrate londe (pethidine)
loperamide
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Medicinal Chemistry
1
Reactive metabolite of morphine ~ morphine 6-glucuronide
Phenolic hydroxyl is important for activity. Analgesic activity is depends on p-phenyl-N-
alkylpiperidine moiety (4-phenylpiperidine). Piperidine ring is chair-form conformation
and perpendicular aromatic ring. It has tertiary amine group (methyl).
Codeine, heroin, morphine, meperidine, hydramarphone is structurally same class and
have cross allergy. Hydrocodone is derivatives of codeine hydromorphone is derivative of
morphine
Methadone is chemical structure of propoxyphene.
Meperidine is piperidine analgesics, meperidine metabolizes to toxic metabolite
(seizures): normeperidine
Partial agonist/antagonist characteristics: replacement of methyl moiety on the nitrogen
atom with larger substituent's.
Allyl substitution7 nalorphine and naloxone
Substitutions at the (3 and 4 morphine hydroxyl group's pharmacokinetic properties
altered
Methyl substitution at C
3
reduces first-pass hepatic metabolism by glucuronide
conjugation: as a consequence codeine and oxyccidone have a higher oral: parenteral
potency
Acetylation of both morphine hydroxyls = heroin {more rapid access across the blood-
brain barrier compared morphine}; in the brain heroin is rapidly hydrolysed to
monoacetylmorphine and morphine
Opioids as analgesics: this activity is due to p-phenyl n- methyl piperidine
Opioids as antidiarrheal drugs:
Loperamide (Imodium): Has low abuse potential. Used as antidiarrheal. Maximum dose 16
mg/day
Diphenoxylate + Atropine = Lomoti!
Opioids as antitussives drugs:
Codeine is used extensively as cough suppressants.
Hydro codeine bitartrate is 3 times more effective as antitussive.
. Dextromethorphan HBr is the (+) isomer of the 3-methoxy form of the synthetic opiaids
levorphanol.
lips
1. PGF2a analog 2. Ecosonide PGEl analog 3. Tryptophan
4. histadine 5. LTC
4
and lTD
4
6. N-acetyl-p-
benzoquinoneimine
30-21
7. Mercapturic acid 8. proton pump inhibitor 9. Pyroxicam
10. Misoprostol 11- Tertiary amine 12. lipid soluble
B. Crosses BBB 14. GI bleeding 15. Renal diseases
16. 5HT3 antagonist 17. SHTlB/lD agonist 18. peptide opioid
neurotransmitter
19. Diacetyl morphine 20. cysteine 21- glycine
22. glutamic acid 23. pinpoint pupil 24. respiratory depression
25. constipation 26. Type 1 PG analog 27. steroid sparing agents
28. analgesic 29. antidiarrheal 30. antitussive
Medicinal Chemistry www.Phannacyprep.com
Histamine precursor is? (4 )
Serotonin precursor of? ( 3)
Misoprostol is? ( J
1
st
generation antihistamines often cause sedation, this is due to? (II, )12..
Ondansetron is classified as? ( \' )
Triptans is classified as? (17 )
latanoprost is classified as? ( , )
Montelukast and zafirlukast act on? ( S )
Endorphins are? (I 16 J
Acetaminophen hepatotoxicity is due to? ( , )
Glutathione conjugation produce? ( 7)
The most common side effects associated with N5AIDs ( ) t 4, I)'"
What NSAID has highest GI bleeding? ('9)
Drug of choice to treat NSAID induced GI ulcer ( 81
Drug of choice to prevent NSAID induced GI ulcer? ( '0)
Glutathione consist of? ( I Q. d I 2..1, Ll.-
Ibuprofen, indomethacin, mefenamic acid are? c.2.-' )
leukotriene antagonist also referred as? U. ry )
Opioids can be used as? ( ) 2A t 1 '
Heroin structure ( l').b &- ) va
Morphine overdose symptoms; ( '1 ,
Gluathione ( (jeSt'" I is a tripeptide that contain unusual tripeptide linkage between
aminoacids of l-Glutamaic acid, l-Cysteine and Glycine
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Chemi,stry

Medicinal Chemistry and
Pharmacology of
Cardiovascular Dru s
Questions Alerts!
Mechanism of diuretics and site of actions. Hydrochlorothiazide chemical
structure.
ACE Inh. structure activity relation and captopril structure
ARBs Structure activity relation.
Statins or HMG Co-A reductase inh. structure activity relation
Calcium channel blocker (CCBs) structure activity relation
Thiazide Loop diuretics K+ Sparing CA inhibitors Osmotic
Chlorthalidone Ethacrynate Na Arniloride Acetazolamide Mannitol
Hydrochlorothiazide Ethacrynic acid Spironolactone Urea
lndapamide Furosemide Triamterene
Metolazone (K+ STAys)
Distal convoluted Ascending loop Collect duct Proximal tubule Proximal
tubule tubule
Hyper GLUe
OHDANG HyperKalemia
,
Loops loose Ca
Metabolic
Metabolic Metabolic Metabolic
alkalosis
alkalosis acidosis and acidosis
intracellular
alkalosis
31-1
, ,
In general. the opposite findings of serum electrolytes are seen in urine
Thiazide diul'"etics: ChlorthaJidone, Hydrochlorothiazide,lndapamide hemihydrate, and
metolazone
Type of Ca Mg Na K Uric Blood Lipids Metabolic Disturbances
diuretic acid sugar
Thiazide t t t t
Hypokalemic metabolic
alkalosis
Loop .t t
-
Hypokalemic metabolic
alkalosis
K-
t t t
Hypcrchloremic
-
- -
sparing metabolic acidosis
(TC02)
Intracellular alkalosis
CAl
- - -
t t
-
Heperchloremic metabolic
acidosis
Osmotic t
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Diuretics
Medicinal
Thiazide diuretics chemistry: Benzene ring with sulfonamide in position 7, and halogen
or trifluoro methyl group in position 6. Saturation of 3,4 double bond (increases potency
with hydrochlorothiazide)
Methyl group at position 2, or lipophylic substituent's at position 3, enhance the potency
and prolong the activity. Replacement of sulfonyl in position I by a carbonyl group
prolongs the activity.
Diazoxide (Hyperstat)
ClyYN'1
A)l.S... NH
NH2S02 02
Chlorothiazide
H t:;::? No Doble bond
N
i
on position 3 - 4
S,NH
0,
Hydrochlorothiazide
Indapamide (Lozol)
CI r
CI1'61 "p

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Essential
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Thiazide diuretics pharmacology
Thiazide act on distal tubule of nephron and i H20, Na, CI, K, excretions (! levels in
body), hyperu.-icemia and retain calcium (Ca)
May cause alkaline urinary pH by effecting on carbonic anhydrase
Metabolic alkalosis (Hypochloremic alkalosis)
Thiazide diuretics therapeutic uses
Thiazides are the drug of choice for uncomplicated hypertension
Especially useful in elderly and African populations and with chronic renal diseases.
Not effective in patient renal clearance less than 50mVmin.
Not preferable in diabetic and hyperlipidemic patient.
Counteract Na/H20 retention caused by other antihypertensives such as hydralazine
and 1BP in both the supine and standing position, except in elderly
Thiazides diuretics side effects (Hyper GLUe)
Hypokalemia, hypomagnesia, hyponatremia, Hypercalcemia, hyperuricemia,
Hyperglycemia, Metabolic alkalosis Photosensitivity rashes, acute pancreatitis
Libido, difficulty with erection and ejaculation (long term).
Loop Diuretics: Furosemide, ethacrynate sodium, and ethacrynic acid.
Loop Diuretics chemistry: Anthranilic acid derivatives with sulphonamide substituent, or
aryloxyacetic acids without sulphonamide substituent.
I
o 0
NH
2
S 2 OOH R
/ Furosemide (Lasix) Ethacrynic acid (Edricin)
Loop diuretics pharmacology
Increase H
2
0, Na, CI, K, Ca excretion (decrease levels in body) and increase Ca
2
+ion
excretion (Loops Lose Calcium)
No change in urinary pH; Metabolic alkalosis (hypochloremic alkalosis)
act in the thick ascending loop of henIe and inhibit the sodium/potassium dichloride
co-transport system. Potent agent can excrete up to 25% of filtered Na+. No ions
come into the cell therefore the sodium pump and Na/Cl symport do not work.
Loop diuretics therapeutic use
Furosemide is the drug of choice in renal disease (CrCl is less than 50mVmin), acute
pulmonary edema, Hypercalcemia.
31-3
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Osmotic diuretics
Osmotic diuretics = Mannitol (Osmitrol), and Urea
Carbonic anhydrase inhibitor pharmacology: Increase water, sodium, potassium and
bicarbonate excretion. Cause alkaline urinary pH, and gives metabolic acidosis.
Carbonic anhydrase inhibitor therapeutics
Used in treatment of Glaucoma (not chronically)
Acute mountain sickness (respiratory alkalosis) High altitude sickness (mountain
sickness).
Because of the alkaline diuresis it produces, acetazolamide has been used for the
treatment of overdoses of acidic drugs .
Medicinal Chemistry
Acetazolamide
Loop diuretics side effects: OH DANG
Ototoxicity
Hypokalemia
Dehydration
Allergy (sulfa), except ethacrinic acid
Nephritis (intestinal)
Gout arthritis
Sequence of ototoxicity (ethacrynic acid> furosemide> bumetanide)
Carbonic anhydrase inbibitors: Acetazolamide (Diamox):
Carbonic anhydrase inhibitor chemistry
Acetazolamide: Aromatic or heterocyclic sulfonamides with a thiadiazole ring.
Carbonic anbydrase side effects
Because of the alkaline Electrolytes -7 Hyperchloremic metabolic acidosis (loss of
HCO,), hypokalemia
Formation of renal stones (phosphaturia & hypercalciuria).
eNS -7 depression, drowsiness, sedation, fatigue, and disorientation.
GI Nausea, Vomiting, and Constipation
Blood related -7 Bone marrow depression, thrombocytopenia (reduction of number of
platelets in blood), hemolytic anemia, leucopenia (reduction in number ofWBC),
agranulocytosis (acute deficiency of neutrophils). Sulfa drugs antibiotics type
allergies
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Osmotic diuretics chemistry
Water-soluble with low renal threshold, and highly polar.
They limit tubular reabsorption of water
Promote diuresis
Increase in urinary pH
Mannitol (monosaccharide-) a carbohydrate)
Medicinal
Mannitol (Osmitrol)
Urea (Ureaphil)
Osmotic diuretics
This drugs limit tubular reabsorption of water and promote diuresis.
Increase excretion of H
2
0, Na, Cl and HC0
3
(decrease levels in body), Increase
alkaline urinary pH-) Increase excretion ofHC03
Osmotic diuretics tberapeutic use
This limit tubular reabsorption of water and promote diuresis.
Mannitol used in treatment of shock, to treat drug overdose and to decrease
intracranial or intraocular pressure.
Prophylaxis of acute renal failure.
Osmotic diuretics side effects: Pulmonary edema, dehydration and contraindicated in
CHF, and anuria (renal failure)
Potassium sparing diuretics
Spirolactone, amiloride hydrochloride. and triamterene
Potassium sparing diuretics cbemistry
binds at the receptors at the late distal tubule and collecting tubules
thus prevents the reabsorption ofNa+ and cr ions.
Pteridine or pyrazine derivatives or steroid analogue antagonist of aldosterone
Triamterene, amiloride contain pteridine or pyrazine derivatives.
Spironolactone: Contain sterol structure + lactones
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Medicinal 'Chemistry
triamtcrene{Dyrcnium)
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Potassium Sl)aring diuretics pharmacology
Act in the early collecting duct to inhibit the electrogenic reabsorption ofNa+ by
blocking the Na channels and hence the exchange of sodium for potassium.
After administration: i Na+, cr elimination, !K+, Ca
2
+(amiloride).
Increase Na, H
2
0, HeO
J
excretion (decrease levels in body),
Decrease K+, J---( excretion
Alkaline urinary pH-7 Increase excretion ofHe03
Potassium sparing diuretics gives the intracellular alkalosis.
Potassium sparing diuretics therapeutic use
Amiloride, spironolactone and triamterene act as competitive antagonists of
aldosterone in the kidney. Because they are weak diuretics when given alone, they
are often used in combination with hydrochlorthiazide.
Spiranolactone is the drug of choice for the treatment of ascites
Spironolactone is antiandrogenic and has been used to treat hirsutisms in doses of
200 mg/day
Amiloride used in nephrogenic diabetic insipidus
Spiranolactone is the drug of choice for the treatment of ascites,
Potassium sparing diuretics side effects
A side effect may be hyperkalemia., an increase in potassium levels, so-that potassium
supplements are usually not taken with these drugs. If they are needed, the dose of
potassium is frequently administered three times a week instead of daily.
Side effects of spiranolactone include endocrine -7 Gynecomastia., menstrual
irregularities, Electrolytes -7 Hyperkalemia, irregularities, eNS -7 mental confusion
Amiloride, spironolactone a sulfa drug like allergy.
Vasodilators
31-;;
www.Phannacyprep.com Medicinal Chemistry
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ACE Inhibitors
Captopril, benazepril, cilazapril, enalapril, fosinopril, lisinopril, perindopril, quinapril, ramipril,
and trandolapril.
Important Concept!
Structure activity relation of ACE
Inhibitors and ARBs.
Vasodiiation
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BradYlcini: J r
[t Na & H
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Renin
. (kidney)
Angiotensin I
ACE Inhibitors chemistry: Captopril
The sulfhydryl groupof captopril is proved to responsible for excellent activity of captopril,
and this also responsible of its two most common side effects skin rashes and taste disturbances
(example: metallic taste and loss oftaste). The sulfhydryl group also present in another drug
penicillamine, which attributes to its metallic taste.
0yO-CH
2
-CH
3
..
Esterase rOH
o
CH -
H0
2
C CH3
Bioactivation
Captopril and fosinopril are acidic drugs while all other ACE inhibitors are amphoteric. -"
ACE Inhibitors are Captopril and fosinopril
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Angiotensinogen ( t Sympathetic
(alpha globulin in blood)
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ACE Inhibitors pharmacology
1 sympathetic oulput
Increase vasodilatation of smooth muscles
i levels ofbradykinin-7causes dry cough
By reducing circulating angiotensin U levels ACE! the secretion ofaldosterone, resulting 1
retention ofNa and H
2
0 retention leads to decrease in cardiac output (CO)..-
1 in preload and after load
Dilation of venous blood vessels leads to decrease in cardiac preload by 1 venous
capacitance.
Arterial dilator reduces systemic arteriolar resistance and 1 after load.
Lower BP by reducing peripheral vascular resistance with reflex increasing cardiac output
ratc.
Little change in HR., or GFR.
ACE Inhibitors therapeutic use
ACE inhibitors are used to treat uncomplicated hypertension and pre-hypertensive patient.
However, if Angiotensin is not the contributing factor for the hypertension, the chances of
ACE inhibitors working are diminished.
These drugs represent a major advance in hypertensive treatment and have most displaced
digoxin as the drug of choice in congestive heart failure. IS1 line treatment for: Heart
failure.
ACE inhibitors also tcnd to protect the kidneys ofdiabetics from developing renal failure
when used in the early stages ofdiabetic nephropathy. Diabetes nephropathy, post ML
LVH (Left ventricular Heart failure)
Pri.or CVAffIA (Cardiovascular Attacks! Transient Ischemic attacks) & in renal disease
ACE Inhibitors side cffects
Profound low pressure (hypotension), taste abnormalities, dry cough (5 to 15%), blood cell
abnonnalitics, and kidney problems such as proteinuria (presence of protein in urine). They
are contraindicated in pregnancy. A persistent dry cough may necessitate discontinuing the
drug. These drugs can cause Hyperkalemia Use of potassium supplements and ACE
inhibitors increase the risk of hyperkalemia. Allergic reactions angioedema (rare).
Reversible neutropenia and fatigue.
Angiotensin Receptor Blockers (ARBs)
Losartan, telmisartan, valsartan, irbesartan, and candesartan
Analogs of imidiazolc ring group
31-9

Medicinal Chemistry
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Imidazole ring
Tetrazole ring OH
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II
N"
N
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These drugs block the effects of angiotensin II, a naturally occurring substance that cause.s
blood vessels to narrow (constrict). When these drugs are administered, blood vessels dilate,
thereby lowering blood pressure and decreasing the workload of the heart.
These drugs appear to have the same benefits as ACE inhibitors, without or less producing the
common side effect of a dry cough.
Pharmacological actions:
Angiotensin binds to its own receptors are found on vascular muscle and in the adrenals.
Stimulation leads to vasoconstriction and release ofaldosterone in the adrenal gland.
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Side effects
Less dry cough (cough associated with ACE inhibitors does appear with these drugs),
Bradykinin causes vasodilation of arterioles and venules results 1TPR, less dry cough.
DiZZiness, hypotension/syncope, renal dysfunction. renal failure),.hyperkalemia
and angioedema
Contraindications
Pregnancy' (renal fetal toxicity), and bilateral renal artery stenosis (stenosis; abnormal
narrowing of passage or opening, such blood vessels or heart valve.
Pharmacokinetics: Losartan may increaSe the effects of potassium supplements, potassium-
sparing diuretics and cyclosporine, leading to raise of potassiwn in the blood
Antihyperlipidemic Drugs
Classification of drugs
Fibrates Bezafibrate BEZALIP
Fenofibrate LIPIDIL
Gemfibrozil LOPID
31-10
Fibrates I
Triglycerides
Adipose tissue
Medicinal Chemistry
VWL
!
IDL
!
WL
Blood
Niacin inhibit
breakdown of
cholesterol to LDL
Statins inhibit
HMG-CoA
reductase
Ezetimibe inhibit
intestinal absorption
of Cholesterol
Acetyl-CoA
CIT
Resins bind to BAs and excrete
in stools thus 1 BAs absorption
into liver
Cholester
01
Bile
aeids
Antihyperlipidemic drug chemistry: Categorized into non-absorbable agents and absorbable
agents.
Nonabsorbable agents
Resins (Polystyrene resins)
Anion-exchange resins bind with the enzymes in intestine and prevent the synthesis of
cholesterol. It Decrease LDL 15 10 30%, increase I-IDL 3 to 10%, however no change or
increase in TG (disadvantage).
Pharmacological actions
Clofibrate
3-Hydroxy-3- Atorvastatin calcium LlPITOR
Methylgluteryl (l-IMG)- Fluvastatin sodium LESCOL
CoA Reductase
Lovastatin MEVACOR
lnhibitors
Pravastatin sodium PRAVACHOL
Rosuvastatin CRESTOR
Simvastatin ZOCOR
Niacin Derivatives Niacin
Resins (Bile Acid Cholestyramine resin QUESTRAN
Sequestrants) Colestiool hvdrochloride COLES
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Cholestyramine chloride
Medicinal Chemistry
A basic anion-exchange resin made of trimethylbenzylammonium groups in a large
copolymer of styrene and divinylbenzene.
Act on small intestine.
Available as powder only
Mixed with juice, water or non carbonated beverages
Colestipol hydrochloride
A copolymer of diethylpentamine and epichlorodrin
Available as granules or tablets (lg)
Do not crush, chew or cut and should be taken with plenty of water.
Hygroscopics
Water insoluble
Do not absorb orally
Do not metabolized and excreted in feces
All resins do not change triglycerides or may increase TG.
Avoid in cholelithiasis or complete biliary obstruction due to impaired secretion of bile acids
caused by these conditions.
All oral medication should be administered 1 hour before and 4 to 6 hour after resins.
Absorbable agents
Niacin: Nicotinic acid (Niacin or vitamin B3)
Fibrates = Clofibrate and Fenofibrate (aryloxyisobutyric acid derivatives)
Probucol (sulfur containing bis-phenol)
Statins =lovastatin (3-hydroxy-3methylglutaryl-coenzyme A)
Fatty fish oil = Eicosapentaenoic acid (EPA) and Docosahexaenoic acid (DHA)
Nicotinic acid
orally, it converted in body to nicotinamide, NAD+ and NADP+. The later two
are coenzymes essential for biochemical oxidation/reduction reactions. Participation in tissue
. ' respiration oxidation -reduction reactions, which decreases hepatic lDl and VlOl production.
At high doses lowers lOl, VlDl and raises HDL. Strongly inhibits lipolysis in adipose tissues.
Inhibits tubular secretion of uric acid, causes gout or hyperuricemia
31-12
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Niacin
Medicinal Chert'iisfry
Statins
LDL VLDL --
. In Liver
Fatty acids Triacylglycerol
Adipose tissue
Triglycerides
The most common side effect and often dose limiting is cutaneous vasodilatation that gives
flushing and pruritus. The flushing can be managed by taking ASA 325 mg and take with food.
Hepatic dysfunction (elevate LDH, AST, and ALl) is another serious side effect of niacin at
higher doses and avoids alcohol. Gl side effects as nausea, vomiting, and diarrhea can be
minimized be taking with meals.
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Structure Activity Relationship:
HMG-CoA reductase inhibitors: Statins are chemical component is a prodrug lactone.ring. and
activates to 3,5 dihydroxy acid. The 3,5 dihydroxycarboxylate is essential for inhibiting HMGCo
reductase action. Lovastatin and simvastatins are prodrugs have lactone structure, it require
in vivo hydrolysis. Statins may increase blood transaminase and creatinine kinase activity
associated with myopathy. especially when combined with fibrates or cyclosporine. lovastatin
and simvastatin are prodrugs. It has lactone structure and it becomes active liver.
Lactone
CH
3

I
CH
3
CH
2
CH-C-O
Blocks the action of enzyme HMG eoA reductas.e, this enzyme needed for the synthesis of
cholesterol, mainly in the liver. Decrease LDl receptors (18 to 55%), and lower cholesterol
synthesis (cholesterol pills).
HMG-CoA reductase -7 Mevalonic acid
Lovastatin
HMG CoA Reductase inhibitors Pharmacokinetics -
Statin
Atorvastatin I Fluvastatin I Lovastatin I Pravastatin I Rosuvastatin ISimv3Statin
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FLS =Take at bed time (mght): ALS =AVOId grape:trultJUlce (because grape frUltJUlce mhlblt
CYP 3A4); FL = Take with Food;HMG =3-hydroxy, 3-methyl glutaric acid
Metabolizing CVP3A4 CYP2C9 CP3A4 Not Known CYP2C9 CYP3A4
Enzyme (s)
Grapefruit Avoid Avoid " Avoid
iuice
Take At night At night At night
Food With or With or With or With or With or With or
without after after without without without
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Lovastatin should be always administered with food to increase Bioavailability, otherwise it
can decrease 30% bioavailability.
Atorvastatin can be taken anytime of the day; because has long half.life.
The best agent for renal disease patient is atorvastatin, because it has minimal renal
elimination, thus do not require dose adjustments.
Fibrates
Clofibrate and Fenofibrate (aryloxyisobutyric acid derivatives
Decrease TG levels, increase fIDL levels (moderately), decrease LDL levels
inhibit cholesterol synthesis.
Antianginal agents
Chemistry of Nitrates
Nitrates: Nitroglycerin and isosorbide nitrates are organic esters of nitric acid
Nitrites: Amyl nitrites are organic esters of nitrous acid
Pharmacology of nitrates
Nitrites and Nitrates (faSt acting antianginal agents): Directly relax vascular smooth muscle
by formation of free radical 'nitric oxide. Nitric oxide (NO) activates guanylyl cyclase to
increase synthesis of cGMP within smooth muscle: .
Vascular effects: Peripheral pooling ofthe blood, reduced preload decreased systemic
vascular resistance, reduced after load. (Reduce myocardial oxygen demand; redistribution
of coronary flow.
Nitrates H'-t-N-i-tr-it-es--4 1t Nitric oxide (NO) 1-.. Vascular smooth
. J . muscle relaxation
Nitrates therapeutic use
Relieve acute anginal attacks, as prophylaxis, for long-term management of recurrent angina
pectoris
31-14
Calcium Channel Blockers
Nitrate tolerance; this associated with nitroglycerin transdennal patch. This can be
minimized by "nitrate free period"
Calcium channel blockers can be characterized in two types non-dihydropyridine and
dihydropyridines.
Nitroglycerin (sublingual): Headache (usually resolves if patient persists with therapy),
hypotension, tachycardia, flushing, and edema.
Medicinal Chemistry
ICalcium Channel Blocker
Nitrates side effects
Nitroglycerine (transdennal) NitTo-Dur, Transdenn-Nitro, and Minitran: contact dermatitis.
Nitrate drug interactions: Avoid concomitant use ofPDE
5
inhibitors such sildcnafil,
vcrdanefil, and tadanafil within use of 5 days, because can cause severe hypotension.
Nitroglycerin (topical) Nitrol: Patients should have a 10 to 20 h nitrate-free period each day
to prevent tolerance.
Nitroglycerin SL storage
Store at room temp
Store original tightly closed container
It is hygroscopic, keep tightly closed
Dihvdroovridine rnHP\ Non-DihvdroDHidines fNDHP\
Benzothiazcoines
Nifedipine Verapamil hydrochloride Diltiazem hydrochloride
Amlodipine
I' Nicardipine
Feladioine
J. Vascular resistance J. Myocardial oxygen Have both cardiac depress
thus vasodilatation and demand and reverse and vasodilator.
hypotension may lead to coronary vasospasm Bradycardia
reOex tachycardia
Bradvcardia
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Dihydropyridine type calcium channel blockers
R,
Co,nco,.,
CH
3
6 1 CH3
General slrUeture of 1,4 dihydropyridines
1,4-dibydropyridioe ring
CH,
Nifedipioe
(active)
Medic,inal
CH,
CO,CH3
NO,
Oxidized analog
(inactive)
Calcium blockers pharmacology. These agents are used to treat hypertension and are
effective in treating angina as well. All muscles, including the smooth muscle of the blood
vessels, require calcium inorder to contract. If the CCB block the entrance of the calcium
into the muscle, the muscle will not contract.This will allow the muscle to relax and
subsequently reduce the blood pressure. Other therapeutic uses: angina, migraine,
antiarrhythmic.
Non-dihydropyridine
Verapamil is similar to beta-blockers in effect, verapamil can cause bradycardia. The effect on
Heart is graded from higher to lower: verapamil >diltiazem > nifedipine.
Verapamil-"7 avoid using in CHF (cause -ve inotropic effect) and constipation.
Dihydropyridine
These agents are similar to Nitrate in effect: Peripheral decrease after/oad (good for
vasospastic angina), dihydropyridine can cause tachycardia. Dihydropyridines relax and
dilating arteries. The effect on vascular smooth muscies is high with dihydropyridine:
, nifedipine > diltiazem > verapamil.
Calcium channel blo<;kers therapeutic uses
These. agents are used to treat hypertension and are effective in treating angina as well. All
muscles, including the smooth muscle of the blood vessels, require calcium in order to
contract. If the calcium-channel blocking agents block the entrance of calcium into the
muscle, the muscle will not contract. This will allow the muscle to relax and subsequently
reduce the blood pressure. Other therapeutic uses: angina, migraine, and antiarrhythmic.
31-16
Dihydropyridine side effects. Blood pressure will fall too low and sometimes causes heart
rhythm. Tachycardia, flushing, headache, dizziness, orthostatic hypotension, and edema.
Non-dihydropyridine side effects
Flushing, profound low blood pressure, swelling of legs and feet, constipation and stomach
upset. If edema (swelling) of the legs and feet occur, a diuretic may be added to the regimen.
31-17
Anticoagulants chemistry
Heparin large, highly acidic mucopolysaccharide made up of sulfated
D-glucosamine and D-glucuronic acid molecules
lMWH low-molecular weight heparin fragments (1-10 kDA),
enoxaparin, dalteparin, tinzaparin, and ardeparin. are being
produced through controlled depolymerization of Heparin
Danaparoid A low-molecular weight heparinoids that are
glycosaminoglycans extracted from porcine mucosa.
l lepirudin A recombinant DNA-derives 65 amino acid polypeptide (nearly
identical to hirudin)
Coumarin derivatives Warfarin, and dicumarol chemically related to vitamin K, are
water-insoluble, weakly acidic 4-hydroxycoumarin lactones
Phenindione are indanedione derivatives
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Antiroagulants
Anticoagulants classification
Heparin Catalyzes the inhibition
of thrombin
low molecular
weight Heparin
(lMWH)
Heparinoids
Vitamin KAntagonists
Various
Anticoagulants
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Medicinal Chemistry
Heparin sodium
Dalteparin sodium (Fragmin)
Enoxaparin sodium (loveno.x)
Nadroparin calcium (Fraxiparine)
Tinzaparin sodium (innohep)
warfarin sodium
Nicoumalone
Antithrombin III (human)
lepirudin
Medicinal Chemistry
Coumarin ring
Structural formula of coumadin derivative oral anticoagulants (Warfarirr)
Anticoagulant pharmacology
lMWH: These agents are not interchangeable with heparin in their actions and use.
Because these highly acidic. These administered parenteral as sodium salt. Because poorly
absorbed from GI tract.
Heparin: Enhances the serum protease antithrombin III results in inactivation of factors
2a, 9a, lOa, lla, 12a, and 13a. Maximum effect occurs within minutes. Heparin stops the
expansion of thrombi by preventing fibrin formation. Antidote of heparin is Protamine
sulfate: Works by acid base neutralization. Heparin act In vitro and In vivo. It has faster
onset of action
Warfarin: Inhibits the hepatic synthesis of vitamin Kdependent factors 2, 7, 9 and 10.
Warfarin antidote is Vitamin K. This agent act only in vivo (in liver). Onset of action is
slower (8-10h). Warfarin is contraindicated in pregnancy.
Anticoagulant therapeutic use
lMWH: Used in prevention of deep vein thrombosis (DVT) or pulmonary embolism (PE).
J:feparin: Major antithrombotic drug for DVT and pulmonary embolism. To prevent
postoperative venous thrombosis in-patient undergoing surgery.
Warfarin: used to prevent blood clots, mainly in areas where blood flow is slowest,
particularly in the leg and pelvic veins.
Anticoagulant side effects
lMWH: Hypersensitivity reaction (chills, fever, urticaria etc), Bleeding, Heparin induce
Thrombocytopenia (HIT), Osteoporosis.
Heparin: Hypersensitivity reaction (chills, fever, urticaria etc), Bleeding and heparin induce
Thrombocytopenia (HIT).
Warfarin: Bleeding; hair loss; Skin necrosis (rare), Blue fingers and toes (uncommon) this
also referred as purple toe syndrome
Add table of comparison of
Cardiac glycosides
31-18
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Digoxin has an additional hydroxyl group at position 12. Duration of action is inversely
proportional to the number of hydroxyl groups, which increase polarity.
Cardiac glycosides Chemistry
Consist of one or more sugars (glydne portion) and a steroidal nucleus (aglycone or genin
portion) bonded through an ether (glycosilic) linkage. Have an unsaturated lactose
substituent (cyclic ester) on the genin portion.
Medicinal Chernislry
o
o
DIGOXIN --.....
CH OH H C

OH CH3 OH
CH OH H C

OH OH
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Digoxin mechanisms of action
Cardiac glycosides Pharmacology
Cardiac glycoside at therapeutic doses produce:
Positive inotropic effect (+ve inotropic). negative chronotropic effect (-ve chronotropic),
and increased vagal tone of the sinoatrial (SA) node (vegomimetic).
DIGITOXIN
.L Heart Rate
(Desired)
Increased Vagal tone
(Mechanism)
Brady arrhythmias
(Side effect)
Tachyarrhythmias
(Side effect)
Electrolyte' rearrangement'
(Mechanism)
t Inotropic
(Desired)
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Inhibit the membrane bound activated ATPase increase intracellular sodium.
concentration, reduce calcium transport form cell, and facilitate calcium entry via voltage
gated membrane channel.
Cardiac glycosides Therapeutic use
Cardiac glycoside at therapeutic doses produce: Myocardial contra.ctility and efficiency,
improve systemic circulation, improve renal perfusion and reduce edema thereby it
indicated in treatment of:
Congestive heart failure, atrial fibrillation, atrial flutter, paroxysmal atrial tachycardia
Contraindications:
Digoxin is contraindicated in ventricular arrhythmias.
t-pa
(tissue type
plasminogen activator)
Alteplase (activase)
Reteplase (Retevase)
very high affinity to
plasminogen, bound to
throm.b!JS
uJ.kinase
CAbbtinase)
Directly degrade
fibrin and
fibrinogen
Thrombolytic Drugs.
I
Anistriptas. (Aminase)
Prodrug of streptokinase
I
Streptokinase
(Strepto protein from
Group C-B-hemplytic
steptococci bacteria
Thrombolytic chemistry
Alteplase, Recombinant DNA-derived plasminogen activators (t-PA) with 527
reteplase, and and 355 amino acids.
Tenecteplase
Streptokinase Nonenzymatic 47-kDa. Derived from [Jlemolytic streptococci
cultures
Anistreplase (APSAC) is a complex of human Iys-plasminogen and
streptokinase with an anisoyl group blocking the catalytic site
Urokinase A two-chain serine protease obtained form human kidney cell
culture.
Thrombolytic pharmacology
Facilitate conversion of plasminogen to plasmin that subsequently hydrolyzes fibrin to
dissolve clots.
31-20
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Thrombolytic therapeutic use
Acute MI (STEMI), stroke and acute massive pulmonary embolism (PE), and deep vein
thrombosis (DVT).
Thrombolytic side effects
Hypersensitivity reactions, Internal GI bleeding, retroperitoneal bleeding, superficial
bleeding at catheter injection site. nausea and vomiting.
Antiarrhythmicagents
Antiarrhythmic drugs are classified as follows:
Class IA: Procainamide, quinidine, disopyramide
Class IB: Phenytoin, lidocaine, mexiletin, tocainide
Class IC: Propafenone, Ftecainide, Moricizine
Class II: All the beta-blockers
Class III: 50talol, Bretyljum, Amiodarone
Class IV: All the calcium channel blockers
Antiarrhythmic drugs Chemistry
Cinchona alkaloids, natural products (Example: quinidine, it is an optical isomer of quinine)
Amides type of local anesthetics (Example: procainamide, flecainide, disopyramide)
Xylyl derivatives (lidocaine (xylocaine), MexiHtine)
Quaternary ammonium salts (bretylium)
Diiodobenzyl oxyethylamines (amiodarone)
[3Jlockers (nadolol, propranolol, esmolol)
Non-dihydropyridine type calcium antagonist (diltiazem, verapamil)
Hydantoins (phenytoin)
Antiarrhythmic drugs pharmacology
Class la: Quinidine (Biquin durules), and Procainamide (Procaine SRJ, Disopyramide (Norpace
CR): Slow the phase 0 (slow entry of Sodium ion), Prolonged re-polarization, Prolonged
effective refractory period
/ Class Ib: lidocaine, Toeainamide, and Mexiletine: Minimal effect on Phase 0 Slow phase -III
, repolarization (decrease Kpump out).
Class Ie: Eneainide (Enkaid), Propafenone (Rhythmol), and Fleeainide (Tamboeor); Very
effective on slowing phase 0 depolarization, little effect on repolarization.
Class II: Beta blockers: Propranolol, Atenolol, and TImolol: Competitively block catecholamine
induced stimulation of Beta receptor thereby suppressing phase IV depolarization
Class III K' channel blockers: Amiodarone, Bretylium, Sotalol: Prolong Phase III repolarization
(Prolong QT de pointes
Class IV Ca
2
' channel blockers: Verapamil, Djltiazem, Nifedipine: Shortens action potential
31-21
I' .:
Medicinal Chemistry
, " " t
Digoxin: affects vagotonic response (vegomimetic) thereby increasing AV nodal refractoriness.
It is contraindicated in ventricular fibrillation. Ventricular tachycardia may result from digitalis
toxicities
Antiarrhythmic drugs therapeutic use
Class fa: Quinidine (Biquin durules), Procainamide (Procaine SR), Disopyramide (Norpace CR):
indicated to treat SVT, VT
Class Ib: Lidocaine, Tocainamide, and Mexiletine: indicated in the treatment of VT, VA
Class Ie: Encainide (Enkaid), Propafenone (Rhythmol), and Flecainide (Tambocor); Indicated in
the treatment of VA
Class II: Beta bJockers:'Propranolol, Atenolol, and Timolol: Indicated to treat AT, SVT, VT, VA
Class III K+ channel blockers: Amiodarone, Bretylium, Sotalol: Prolong Phase III repolarization
(Prolonged QT interval)-7Torose de pointes.
Class IV Ca
2
+ chinnel blockers: Verapamil, Diltiazem, Nifedipine: Indicated in the treatment of
SVA,VA
Digoxin: Effects vagotonic response (vegomimetic) thereby increases AV nodal refractoriness.
It is contraindicated in ventricular fibrillation. Ventricular tachycardia may result from digitalis
toxicities
Antiarrhythmic drugs side effects
Class fa: Quinidine (Biquin durules), procainamide (Procaine SR), disopyramide (Norpace CR):
Torsales de pointes
Amiodarone -7 blue skin, photosensitivity, photophobia; Respiratory: Pulmonary toxicity
which including interstitial pneumonitis; Respiratory muscle impairment, pigmentation; GI:
nausea, anorexia, constipation; hepatitis and cirrhosis; hypothyroidism; hyperthyroidism;"
Blue skin color, corneal deposits, hepatic toxicity, optic neuritis, erectile dysfunction,
photophobia
Antiplatelet drugs
31-22
-'
ADP inhibitors: Tidopidine and c1opidogrel
Change chart
Fab fragments of human monoclonal antibody to the glycoproteine (GPllbjllla) receptors
(Abciximab, tirofiban, eptifibatide).
ASA (Aspirin, Entropen), c1opidogrel (Plavix), ticlopidine (Ticlid),
dipiperdino-dinitro pyrimidine and theonopyridine.
Medicinal Chemistry
Monoclonal antibodies act against the glycoprotein lib/ilia-receptor
thus prevent platelet-platelet aggregation.
Reversible antagonist of fibrinogen, von WiJlebrand's factor
www.PharmacYorep.com
Antiplatelet drugs pharmacology
ASA Inhibits platelet cyclooxygenase production of thromboxane A
21
thus
preventing platelet aggregation or clumping.
ASA act as antiplatelet action at dose =60 to 80 mg
Interfere ADP-induced membrane-mediated platelet-fibrinogen binding.
Antiplatelet Drugs
1-1-1-,------1
ASA Dipyridamole Ticlopidine Glycoprotein Prostaglandin
& inhibitors analOr
Clopidogrel 1
Eptifibatide tpOprosteno!
Tirrofiban
Tiddpidine &
Clopidogrel
Fab
fragments
GPlib/llla-
receptor
antagonist
I Antiplatelet drugs therapeutic use
Platelets, of the elements of blood cells, tend to clump together. The antiplatelet drugs
interfere with the coagulation by inhibiting platelet aggregation. Heart attacks and
strokes occur when a blood clot that forms in a narrowed portion of an artery blood flow
and cuts off the supply of oxygen and nutrients to the tissue that lies beyond the site of
the clot.
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Antiplatelet drugs side effects
ASA (Aspirin, entropen): Bleeding (epistaxis to major GI bleeds), Serious GI bleeding less
common with lower doses (80-325mg/day)
Clopidogrel (Plavix): Bleeding, diarrhea, rash, and thrombocytopenia.
Ticlopidine (Ticlid): Neutropenia, bleeding, diarrhea, rash, thrombocytopenia (2.5%) that is
generally reversible with drug discontinuation. Monitor neutrophils every 2 wk for 1
st
3
months .,
Antianemicagents
Iron .
preparations
Cyanocobalamin
(Vitamin B
1
2)
Folic acid
Epoetin and
Darbepoetin
Oprelvekin
(interleukin 11)
Filgrastim
Consist of complex ferric hydroxide and low-molecular weight
dextrans.
A nucleotide macromolecule with corrin ring containing a trivalent
cobalt atom.
Cyanide with the cobalt atom, as benzimidazone
Benzimidazole is bonded to Oiboso! phosphate.
Pteridine nucleus is bonded to nitrogen of p-amino benzoic acid, and
p-amino benzoic acid is bonded to glutamic acid through eJn amide
linkage.
Are glycoprotein produced through recombinant DNA technology.
Epoetin is same with natural erythropoietin
A recombinant DNA produced non glycosylated polypeptide growth
factor.
Are glycoprotein produced through recombinant DNA technology
HN N N
2 ,r'y _ 0 COOH
L/ -0-.N---{1--Jf
Ji."..r N H Glutamyl moity
p-amino benzyl
group (PABA)
Folic acid
Erothropoetins
Therapeutic use: anemia associated with cancer chemotherapy and renal disease
Oprelvekin
Therapeutic use: Thrombocytopenia
31-24
Therapeutic: neutropenia associated with cancer chemotherapy.
Medicinal-chemistry
Filgrastim
Find answers from the table".
1. Nitroglycerin 2. AL5 3. APR
4. Fluvastatin and lovastatin 5. Contain sulfhydryl 6. CYP3A4
group
7. increase HDl 8. decrease lDL 9. decrease TG
10. act on distal collecting 11 intracellular alkalosis 12 Sulfonamide and
tubules halogen at position 6 & 7
13 angina 14 MI 15 CHF
16 Nitrates
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Dihydropyridine are used for the treatment of? ( 4Y\1'))I, "'1 j J=
Essential functional group that are present in thiazide diuretics? ( .s c..J ",J ,
What diuretics cause intracellular alkalosis? (
Nitric oxide (NO) is a neurotransmitter that acts on? ( vt:...JocLhJ....L.)
Drugs that cause venous pooling? ( Nl'h.,/Jf.......
Nitroglycerin is classified as? ( N )
Fibrates? ( 7, h .5 )
Statins that should be avoided with grapefruit juice J
Statins that should be taken with meals ( FL I
Statins that can be taken anytime of the day ( 1>f>t2. )
Dihydropyridine oxidized to pyridine by enzyme? ( t. t}
Drug that contain sulfhydryl group ( Ce.,1-0"..-o
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Norepinephrine f s /l P <l- 1 <5>$1'
Epinephrine t s (J P .t. J 5>Bf
Dopamine f sf]" 4-- '1 1'.:v81"
Dobutamine, isoproterenol 1 10 (]P ..,t.. 5)ap
Reserpine -7 J" '+'""f.J)1!.f
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Non selective Beta blocker
et sJ-. pf'i,L",
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31-25
Medicinal Chemistry ofCNS Drugs
32
MedJCinal Chemisby and Pharmacology of Psychiatric
and NewoIogical DisorderAgent
Questions Alerts!
Phenothiazine structures activity relation
Pharmacological actions of SSRls and dual acting antidepressants and serotonin
syndrome
Structure of phenytoin, gabapentin
Structure activity of benzodiazepine and half lives.
Classification of Antidepressants
32-1
5HTonly
Selective serotonin
reuptake inhibitors (SSRI's)
Fluoxetine, Fluvoxamine
Paroxetine, Sertraline
Citalopram, Escitalopram
I
Monoamine Oxidase
Amine reupla
(MAO) Inhibitors
inhibitors dru
Lrreversible MAOI
I
Phenelzine
Isocarboxazid
I
Clorgyline
Tranylcypromine Non-selective
Reversible MAO! (RIMA) 5HT, NE, D
Moclobemide
I
I
5HT, NE
Dual action
Tertiary amine type
(5HT> NE)
SNRJ
Amitriptyline
VenJafaxine
Imipramine
Duloxetine
Secondary amine type
NDRI
5 H T ~ N E
Bupropion
Desipramine
Nortriptyline
ke
gs
(12 receptor blockers
Mirtazapine
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32-2
Secondary amine type
Monoamine oxidase inhibitors (MAOls) side effects
Reversible MAO inhibitor (RIMA): Moclobemide
Monoamine oxidase inhibitors (MAOls) pharmacology
These drugs inhibit the destruction of these brain chemicals, which leads to increased
concentrations of these neurotransmitters, which may account for their antidepressant
activity.
Monoamine oxidase inhibitors (MAOls) chemistry
Irreversible MAO inhibitors: Phenelzine (Nardil), Tranylcypromine (Parnate), Isocarboxazid,
Clorgyline (MAO-A selective), Selegiline (MAO-B selective)
Abbreviations: 5HT = S-hydroxy tryptamine (Serotonin), NE = Norepinephrine; SNRI = Serotonin Norepinephrine
Reuptake Inhibitors, NORI = Norepinephrine Dopamine Reuptake Inhibitor; RIMAs = reversible inhibitors of
monoamine oxidase. TCA = Tricyclic
Monoamine oxidase inhibitors (MAOls) therapeutics
The r:nonoamine oxidase inhibitors (MAOls) were the first class of compounds used to treat
depression. They are also used as anti-anxiety and narcolepsy. Selegiline ~ used for the
treatment of Parkinson's disease.
Antidepressants
Classes of antidepressant drugs include: tricyclic compounds (TCAs), monoamine oxidase
inhibitors (MAOls), selective serotonin fe-uptake inhibitors (SSRls) and reversible inhibitors of
monoamine oxidase (RIMAs).
Patients, taking these drugs, must monitor their diet for tyramine, an amino acid present
in many foods that are fermented, aged or smoked e.g. cheese. There are a number of
foods containing tyramine and such' drugs must be avoided. Monoamine oxidase is an
enzyme, which inactivates the neurotransmitters, epinephrine, nor epinephrine and
dopamine. CVS affects ~ Orthostatic Hypotension, Tachycardia, Arrhythmias, Stroke.
CNS effects ~ Sleep disturbances, CNS stimulations. Weight Gain, Sexual Dysfunction
Anticholinergic ~ e s s than TeAs.
Tricyclic antidepressants (TCA) chemistry
Dibenzocycloheptadine (Example: Nortriptyline) and dibenzapines (Example: Desipramine)
Tertiary amine type
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Dibenzocycloheptadine: (Example: Amitriptyline and Dibenzapines (Example: Imipramine)
Dibenzocyclohepatadiene Derivatives
Amitriptyline
Nortriptyline
Dibenzapine Derivatives
Imipramine (tofranil)
QQJ
tH
2
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2
CH
2
NHCH
3
Desipramine (Norpramin)
Tricyclic antidepressants (TCA) pharmacology
These drugs inhibit reuptake of NE and SHT at receptor site, which leads to increased
concentrations of these neurotransmitters, which may account for their antidepressant
activity.
Tricyclic antidepressants (TCA) therapeutic use
These drugs are used for the treatment of major depression. Clomipramine is the drug of
choice for anxiety disorder (OeD). Amitriptyline also used in migraine prophylaxis and
treatment of Neuropathic pain. Imipramine was used to treat enuresis in children
(Bedwetting)
Tricyclic antidepressants (TCA) side effects
'. CVD effects: Orthostatic Hypotension, Tachycardia (AV blockade); CNS-7
Confusion/Delirium. Weight Gain, Sexual Dysfunction, and Bone marrow depression
Anticholinergic side effects (Constipation, Blurred vision, Urinary retention, Dry mouth).
Selective Serotonin Reuptake Inhibitors Chemistry
32-3
r l
Serotonin syndrome?
Antipsychotic drugs
Selective Serotonin Reuptake Inhibitors (SSRIS) side effects
Sexual dysfunction (orgasmic delay), G[-7 nausea (most common), headache, insomnia,
nervousness, and fatigue.
Selective Serotonin Reuptake Inhibitors (SSRJ) therapeutic use
This c1.ass of antidepressants has fewer side effects than MAOI's or TeA'5. They are also used
for bulimia, obsessive-compulsivc disorder and panic attacks.
Medicinal ChemisuyofCNS Drugs
Ipiperidine Dibenzox pine Dihydro ndolone
Loxapine Molindone
Trazodone (Desyrel)
Fluoxetine (Prozac)
www.pharrnacvorep.com
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Selective Serotonin Reuptake Inhibitors (SSRlS) pharmacology
The SSRJs are selective in blocking the reabsorption of serotonin by nerve cells by acting at the
5-HT receptors, and therefore, increasing the amount ofscrotonill available in the brain.
Typical
Pheno iarine Thi01G!Jl nes Butyro hcnones Diphcnylbut
Cblol"promu.ioc Chlorprothixcne Haloperidol Pimozidc
Fluphenazine Thiothixene Droperidol
Trinuopcrazine
Thioridazine
Phenothiazincs: Chlorpromazine, thioridazine, and prochlorperazine,
Must contain nitrogen containing side chain substituents on nitrogen for antipsychotic activity
drug. The ring and nitrogen must be separated by chain such as chlorpromazine
(Thorazine).
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Medicinal Chemistry of CNS Drugs
. . . . ..'
Pbenothiazines: such as (Mellaril) in which the ring and side chain nitrogen are
separated by a two-carbon chain has only antihistaminic or sedative activity.
Difference of one -CHr in side chain referred as homologs
Side chain containing piperazine derivatives have the greater potency and highest
pharmacological activity. .
Butyrophenones: Haloperidol
Butyrophenones are chemically not related to phenothiazines but have similar activity.
Thioxantbines: Thiothixine, chlorp.rothixine: lack rin.g nitrogen and side chain is attached
through double bond.
Side chain
R =CH
2
CH
2
CH
2
N(CH
3
h
Phenothiazine skeleton
Phenothiazines
Chlorpromazine (aliphatic)
Thioridazine, mesoridazine (piperidine ring)
Fluphenazine, perphenazine, prochloperazine
Trifluoperazine (piperazine rings)
Antipsychotic drugs pharmacology
1
51
generation antipsychotic mainly bind to D
2
thereby block dopamine receptors in cortical
and limbic areas of brain. Blockade in dopamine at basal ganglia leads to side effects such
as Parkinson's (Extra pyramidal side effects).
2
nd
generation antipsychotics bind and inhibit serotonin (5HT) receptors and dopamine
receptors. Some examples: Clozapine 5HT2, D
1
and D
2
, D
4
, muscarinic, and alpha-
adrenergic receptors. Risperidone Blocks 5HT2 greater than D2 receptors.
Least effect on doparnine
Antipsychotic drugs therapeutic use
The antipsychotic agents are as major tranquilizers and are used to help people with
schizophrenia and other psychoses (major mental disorders). The individual is
.out of touch with reality, hallucinates, hears voices and exhibits bizarre behaviour. These
symptoms are only one aspect of schizophrenia. Other symptoms are: social and
an inability to communicate or to concentrate.
32-5
32-6
Medicinal Chemistry ofCNSUrugs
R,; OH
Lorazepam
Oxazepam
Temazepam
R,
R,

""'......
I'"
.&
Ist Generation aniipsychotics are preferred to treat positive sch.izophreniasymptoms. 2
nd
Generation antipsychotics prererably used to treat negative schizophrenia symptoms
Antipsychotic drugs side effect: Exira pyramidal Symptoms (EPS), Parkinsonism. sexual
dysfunction, anticholinergic side effeclS, tardive dyskinesias, sedation. The first generation
antipsychotics have high extrapyramidal side elTecrs, and second generation have high weight
gain side effects.
eNS stimulants
Methylation
Amphetamine --> Methyl amphetamine (street name: meth, crystals, glass, ice)
Dehydroxylation
Ephedrine or pseudoephedrine --> Methyl amphetamine
QHr OHr r

tH3 tH3 tH3
Ephedme
C
A B
Benzcx:fiazepines
Neurotransmitters that play important role in sleep or hypnotic actions are: GABA, histamine.
acetylcholine catecholamine and adenosine
Benzodiazepine chemistry:
Dcalkylalion:
Structure correction: benzene connect 7 member ring
Short acting Intennediatc acting Long acting

Midazolam Alprazolam Diazepam
Estazolam Lorazcpam Flurazcpam
Triazolam Oxazepam Clonazepam
Temazepam Chlordiazepoxide
Nitrazepam
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diazepam and chlordiazepoxide metabolized to dcsmethyl diazepam or desmethyl
chlordiazepoxide have long half life (>SOhr)
Flurazepam metabolized to desalkyl flurazepam
Oxidation
Alprazolam and triazolam -7 oxidized to short and intermediate acting
Rapid conjugation
Oxazepam and lorazepam -7 metabolite with no intrinsic activity
Benzodiazepines (LOn with OH group at position 3 easily undergo phase II
glucuronidation conjugation, and have short half-life.
Benzodiazepine without OH group at position 3. must undergo phase I hydroxylation
reaction, and have long half life (long acting).
Diazepam forms the intermediate metabolite desmethyldiazepam, which has a very long
half-life.
Benzodiazep'ine pharmacokinetics
Long acting benzodiazepines include: Diazepam (longest half life), flurazepam, c1onazepam,
chlordiazepoxide
Intermediate acting: Alprazolam, Lorazepam, Oxazepam, temazepam and nitrazepam .
Short acting: Triazolam, midazolam (shortest half life). Short acing benzodiazepine have no
phase 1metabolism, or extra hepatic metabolism
Benzodiazepine pharmacology
Benzodiazepine receptors BZ\ and BZ
z
are found in brain, bind to BZ
I

BZ
z
that are parallel to GABA receptors.
Benzodiazepine therapeutic use
Benzodiazepine are minor tranquilizers are used to treat insomnia, anxiety and seizure. Xanax
is used to help panic attacks. When used for insomnia, benzodiazepines should be
administered for short-term use only as they become ineffective and cause memory loss.
Continuous R.E.M. sleep deprivation makes people more irritable and less able to concentrate.
Beuzodiazepine side effects: The benzodiapines in some patients, especially with long-term
use, experience drowsiness; tolerance dependency and withdrawal symptoms can be
problematic. Even with short-term use, some patients experience tolerance and dependency.
Barbiturates
I I I
Ultra-short action Short acting Lortg action
Thiopental Amobarbital Phenobarbital
Secobarbital
Pentobarbital
32-7
( l
Barbiturates Side effects
Barbiturates pharmacology
Barbiturates interfere with Na+ and Ki- transport across membrane potentiates GABA
A
action
on cr entry. These drugs do not bind to BZ. and BZz benzodiazepine receptors.
Barbiturates Thc.-apcutic Use
They are effective only for a few weeks since they alter the length of time spent in R.E.M.
sleep. They should only be used for short-tenn therapy as sedative or hypnotics: Tuinal (a
combination of secobarbital and amobarbital), and secobarbital are reportable controlled drugs.
Phenobarbital is used to control seizure disorders, often in combination with primidone and/or
phenytoin.
Buspirone (Buspar)
General Barbiturate Structure
5, 5-<:1isubstituted derivatives of barbituric acid, a saturated diketopyramidine.
Two side chains in position 5 are essential for sedative hypnotic activity and long acting
has a phenyl and an ethyl group in position 5.
Barbiturates have structural similarity with hydantoins (phenytoin), however, hydantoins
have five membered ring structure.
Primedone is prodrug, and active metabolite is phenobarbital.
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HNrNH
Barbiturates chemistry
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Drowsiness the next morning, tolerance, and dependence.
/
NOD benzodiazcpinc GABA-A agonist
Act at GABAA receptors and have high affinity than bcnzodiazepines.
Short acting
No rebound effect on withdrawal
Low physical dependence
Imidazopyridines
Zopiclone
Zolpidem (ambien)
32-8
. '.
Medicinal Chemistry ofeNS Drugs
Pyrazolopyridine
Zeloplon (Sonata)
Anti-Parkinson's Drugs
Drugs to treat Parkinson's disease
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Dopamine .COMT Dopamine MAOB
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Anticholinergic
precursor inhibitors agonist ,inhibitor
Anti-viral drug
Peripheral -
Amantadine
dopa
decarboxylase Entacapone Selegiline Ben<.tropine
inhibitor
I
* L-d a * Carbidopa * Pramipexole
* Ropinirole I Ergot alkaloids
I
* Bromocriptine
* Pergolide
* Sinemet
COMT = Catecholamine O-Methyltransferase Inhibitors: DA= Dopamine
Anti-Parkinson's drugs chemistry
Levodopa
Benztropine
Ethopropazi ne
32-9
t ;
Direct acting dopamine agonist: (Bromocriptine. Pergolide, Pramipexole, and Ropinirole),
Direct acting Oz agonist. Inhibiting the secretion of the hormone prolactin from pituitary
gland.
Brain
eral tissues
ctnyldopa
J-Q-Methyldopa
COMT
Tolcaponc
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v:x:lopa
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Ldopa
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Dopamine
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D
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and D
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DOPfuninc
receptors
Sefegilinc
MAO
Rest:gJine
Dihydroxyphenylacclic
Acid (DOrAC) + 1-1
1
0
1
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Anti-Parkinson's drugs phannacology
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agonist. Efficacious and longer effective than bromocriptine.
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Dopamine precursors (Ievodopa): High protein content meals interfere with transport of
levodopa into the eNS. Levodopa should be taken on an empty stomach,!tvpicaJly 45min
before a meat. I
Dopamine precursors and decarboxylase inhibitors: levodopa (l-dopa)/carbidopa - the single
most effective anti-Parkinson drug; it is changed into dopamine in the brain.
Antiviral agent with antiparkinsonian properties (Amantadine). Indicated in drug induced
Parkinson's Disease because levodopa will reverse the beneficial effect of the drug.
Anti-Parkinson's drugs therapeutic use
Anti-Parkinson's drugs side effects
32-10
www.pharmacyprep.com Medicinal of eNS Drugs

Levodopa (L-dopa)/carbidopa: Nausea, Vomiting, Orthostatic hypotension, dyskinesia,
hallucinations, confusion Long term use of L-dopa/carbidopa therapy can produce:
Mydriasis & precipitation of glaucoma, Melanoma
Amantadine: anticholinergic side effects, hallucinations, edema of feet &ankles.
Anticholinergic drugs: avoid in elderly. It aggravates glaucoma, memory impairment
COMT inhibitors: dyskinesias, nausea, sleep disorders, anorexia, hallucinations.
Direct acting dopamine agonist: (Bromocriptine, Pergolide, Pramipexole, Ropinirole)
na.usea, vomiting, orthostatic hypotension, psychosis, pleural fibrosis (chest x ray before
initiating therapy).
Non selective dopamine agonist:
Bromocriptine and pergolide are ergot alkaloids that have effects on partial dopamine (D
1
)
and full on D
2
receptors and other receptors.
Selective (Full) dopamine agonist: Pramipexole, and Ropinirole selective full agonist on D
2
and D
3
receptors. These drugs do not have effect on non-dopamenergic receptors; thereby
there are no peripheral effects associated with these drugs.
Anti-epileptics chemistry
Anti seizure drugs (Antiepileptics, anticonvulsants)
Phenytoin (Dilantin}-) Hydantoins
Carbamazepine (Tegretol}-) Iminostilbenes
Valproic acid (Depakene}-) Dialkylacetate: divalproex and valproic acid are related
chemicals. Divalproex is a mixture of valproic acid and sodium valproate. In the body they
are metabolized to separate compounds, and both exert anticonvulsant effects.
Primidone (Mysoline): Phenobarbital and primidone are chemically related. Primidone is
metabolized to phenobarbital and another compound in the body, both of which have
an'ticonvulsants properties:
Ethosuccimiae (Zarontin) -) Succinamides
, GABA analogs: Gabapentin, vigabatrin, pregabalin and baclofen: muscle relaxant
Gabapentin (structurally similar to GABA neurotransmitter) GABA analog
Lamotrigine -7 Phenyltriazine derivative
32-11
Ethosuximide (Zarontin)
GABA
Gabapentin (Primary amine)
o
Phenytoin (Dilantinl
Carbamazepine (Tegretol)
Anti-epileptics pharmacology
Anticonvulsants are eNS acting drugs that are used to treat seizures. Epilepsy is a disorder of
electrical conduction in the brain and results in loss of consciousness, seizures and
convulsions. The electrical activity causes nerve cells to become hyper-excitable and to
discharge uncontrollably. Phenytoin decreases the sodium content of nerve in the brain and
thereby decreases the hyper excitability of the cells that are involved in initiating seizures.
Carbamazepine blocks Na channels thereby reducing abnormal impulses in brainr
side effects
32-12
Phenytoin: can cause overgrowth of the gums (gingival hyperplasia) and proper mouth
hygiene is necessary for people taking this drug. Encephalopathy, blood dyscrasias,
Nystagmus, Hirsutism. Birth defects cleft palate, and Stevens Johnson syndrome.
Phenytoin structure has hydantoins. Thus it give hydantoins syndrome. This can give
congenital defect in children as cleft palate.
Carbamazepine: Rash, l' liver enzymes, neutropenia, aplastic anemia
Chronic: drowsiness, vertigo (The sensation of dizziness and a confused, disoriented state of
mind). Aplastic anemia, Stevens Johnson syndrome (skin hypersensitivity reactions), Acute
intoxication: Coma, hyperirritability, convulsions and respiratory depression.
Topiramate: Cognitive dysfunction, headache, kidney stones, and weight loss.
Clobazam: Tolerance to therapeutic effects, insomnia, depression, drowsiness,
light headedness, ataxia.
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Local anaesthetics chemistry: Most local anesthetics are structurally similar to the alkaloid
cocaine, however these structures consist of a hydrophilic amino group through ester or amide
functional groups.
Ester Type: Cocaine, procaine, chloroprocaine, benzocain, aDd butamben.
Short acting due to rapid hydrolysis. Ester type of local anesthetic hydrolysis produces para
amino benzoic acid (pABA) ,
Amide Type: Lidocaine, dibucaine, prilocaine, mepivacaine, bupivacaine, and etidocaine. Long
acting, and metabolized in liver. Procainamide is long acting amide type local anesthetic than
procaine an ester type, because isosteric replacement of ester oxygen with a nitrogen atom
Lidocaine (tertiary amine)
Amide Type
Procaine (aromatic amine)
Ester Type
Local anesthetics pharmacology
Inhibit sensory nerves that carry stimuli to CNS, block nerve fibre conduction, Blockade is
reversible, must continue administration of the drug for effects to continue
Local anesthetics therapeutic use
Procainamide -7 Antiarrhythmic drug (Na+ channel blocker)
Lidocaine is used for -7 antiarrhythmic drug and amide type local anesthetic
, General anesthetics
Add classification from phannacology
General anesthetics chemistry
32-13
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General anaesthetics sidc cffects
Tips
Ketamine Hydrochloride Thiopental Sodium
*
HNyN
~ N a
General anesthetics pharmacology I
Ketamine: Short acting Iton-barbiturate anesthetic induces a dissociated state in which the
patient appears awake but is unconscious and does nol feci pain., . .
Propafol: Sedative or hypnotic action, used in induction and maintenance of.anes"lhesia. Fast
onset (40 seconds of administration).
Ketamine: Causes sedation, immobility, amnesia, and nightmares.
Halothane is associated with malignant hyperthermia.
Thiopental is rapid acting barbiturates
General anaesthetics therapeutic use
Halothane (Fluothane) is used in pediatric anaesthesia; it is infrequently used in adults.
IsoOurane (Forane), coOuraue (Ethrane), sevonurane (Sevorane, Uhane) and desflurane
(Suprane) are frequenlly used in adults.
Enflurane is used as an inhalation agent for adults; but is not widely used for pediatric
cases.
Isoflurane may be Ihe most widely used inhalation agent.
Fentanyl: is a narcotic, available as transderrnal patch (Duragesic). Good analgesic property
SSRJ onset ofaction is ~
Fluoxetine washout period -)
Depression with sexual dysfunction ~
To treat depression in insomnia patient ~
Depression with diabetes ~
Venlafaxine at higher dose act on ~
Higher dose of venlafaxine (225mglday) have effect on -7
Patient on antidepressants and shows with dilated pupil, may be due t o ~
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A substance found commonly in fermented foods, which can be toxic when MAO
inhibitors are,
MAo is classified as
Avoid taking cheese with
St. JOMS wort is
Selegiline and Resegiline
Venlafaxine is classified as
Drug of choice against bipolar disorders and manic depression
Lithium toxicity symptoms -->
CNS-->
Thiopental-7
Lithium blood levels in adults -7
Serotoninergic syndrome -7
Fast or quick acting benzodiazepine is
GABA analogs are
Antiseizure drugs that gives Stevenson Johnson syndrome -7
What anti seizure drugs that is also used as weight loss therapy?
Nystagmus-7
Select TRUE OR FALSE Statements
concentration varies with Na+ions (T/F)
Lt conc. increases with decrease Na+(TIF)
Lt conc. decreases with increase in Na+( TIF)
ACEI decrease Na+ and increase Li+( T/F)
NSAID decrease Na+ renal perfusion is Jess (TIF)
Thiazide deplete Na+( TIF)
Fluoxetine (SSRl) increase Li+ toxicity (TIF)
Renal dysfunction -7 Li+ increase( T/F)
32-15
Other Antidiabetic:
Insulin and incretin hormones functions
33-'
General SUlfonylurea srtucture
33
. .
Medicinal Chemistry"
First generation: Tolbutamide, Chl9rpropamide, Tolazamide, and Acetphexamide
Second generation: Glyburide, Glypizide, and Glimepride
Antidiabetic drug chemistry
Oral hypoglycemic drugs: Sulfonylureas
Questions Alerts!
Chemical structures of estrogen, progesterone and testosterones
Pharmacology of Endocrine
Drugs
Thyroid hormones T4 and 13
Classification hypoglycemic drugs like 1st & 2nd geo sulfonylureas
Second generation agents have larger R
1
substituent's; because of large substituent's these
are more lipids soluble and more potent compared to first generation. Sulfonylureas areas
acidic compounds attached to aromatic ring.
o H H
R ~ "_N_,,.._N,
1 II" R
- 0 0 2
Metformin: basic compound. Meglitinides; acidic compounds. RosigiitalOne and pioglitazone;
acidic compounds
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Medicinal C.hemistry
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Hypoglycemic drugs Antihyperglycemics
Increase insulin secretion
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Biguanide: Metformin
Sulfonylureas Meglitinides
Increase sensitivity of insulin
Netiglinide
Decrease resis,tance of insulin (increase glucose
Repaglinide
uptake)
Decrease glycongenolysis (breakdown of glycogen to
I
1
st
Generati<;m II 2
nd
Generation I,
.glucose), . " :
Tolbutamide Glyburide
Decrease gluconeogenesis (decrease formation of
Tolazamide Glipizide
glucose from proteins and fats)
Chlorpropamide Glimepiride
Glicalizide
SITAGLIPTfN (JANUVlA): Inhibitor of
dipeptidyl peptidase enzyme '(DPP-4).
Liraglutide (Victoza): Incretin honnone analog
Thiazolidinedione (Increase insulin sensitivity)
Rosiglitazone (Avandia)
Pioglitazone (Actos)
a-Glucosidase inhibitor (Prevents breakdown of
starch and sucrose to glucose)
,',
Antidiabetic drugs pharmacology
Sulfonylureas (Chlorpropamide, Gliclazide, Glimepiride, Tolbutamide): increasE7d
secretion of insulin by action on of pancreas. Glyburide may produce a mild diuresis by
enhancing renal free water clearance, Chlorpropamide has antidiuretic activity possibly due to
potentiating of antidiuretic hormone (ADH) in the renal tubules
Meglitinides (Nateglinide, Repaglinide): Increased secretion of insulin by action on of
pancreas.
I Alpha-glucosidase Inhibitors (Acarbose)
Inhibits alpha glucosidase in intestinal.
border thus decreasing the absorption of
starch and disaccharides.
Important Concept!
Acarbose do not decrease glucose
absorption.
Biguanides (Metformin hydrochloride)
Increased peripheral utilization of glucose by decreased gluconeogenesis. Do not cause
hypoglycemia in monotherapy.
33-2
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Decreases insulin resistance in the periphery and liver. Improves glycemic.control while
reducing circulating insulin levels.
Orlistat: Blocks the action of stomach and pancreatic enzymes (lipases) that digest fats, so fats
and other fat soluble vitamins ADEK are not absorbed in the body but pass through and
excreted in the feces
Antidiabetic drug Therapeutic uses
Sulfonylureas (Chlorpropamide, Gliclazide, Glimepiride, Glyburide, Tolbutamide)
Disulfiram like reaction is caused by which type of antidiabetic drugs, when taken with
alcohol.
Chlorpropamide has antidiuretic activity possibly due to potentiating of ADH in the renal
tubules; there is some evidence that chlorpropamide may actually stimulate ADH secretion.
Meglitinides (Nateglinide, Repaglinide): Nateglinide used for type 2 diabetes. It is imperative
that there be rigid attention to diet and careful adjustment of dosage. When metformin is
combined with a sulfonylurea, instruct the patient on hypoglycemic reactions and their .
control. If vomiting occurs, withdraw drug temporarily, exclude lactic acidosis, then resume
dosage cautiously.
Biguanides (Metformin): Metformin can be of value for the treatment of obese diabetic
patients. May cause hypoglycaemia when combined with sulfonylureas (glyburide).
Alpha-glucosidase Inhibitors (Acarbose): For type II Diabetes Mellitus in combination with
other antidiabetic drugs. In combination oral hypoglycemic therapy, always use agents from
different class of oral hypoglycemics.
Thiazolidinediones (Pioglitazone, Rosiglitazone): These agents depend on the presence of
insulin for its mechanism of action. Contraindicated in patients with serious hepatic
impairment, acute heart failure. Increasing insulin sensitivity in type 2 diabetes. It improves
sensitivity to insulin in muscle and adipose tissue and inhibits hepatic gluconeogenesis.
Rosiglitazone + Metformin: Indicated for use when diet, exercise, and metformin or
rosiglitazone alone do not result in adequate glycemic control. Rosiglitazone+metformin is the
combination used in Case of insulin resistance.
Rosiglitazone + Metformin (Avandamet): If acidosis of any kind develops, Avandamet should
be discontinued immediately. The use of rosiglitazone in combination therapy with insulin is
not indicated due to its side effects; therefore, avandamet is not indicated for use in
combination with insulin.
33-3

Orlistat (Xenical): Reduces fats stores and produce _-
inhibitor.
Medicinal C.hemistry .
Antidiabetic drugs Side effects
Sulfonylureas (Chlorpropamide, Gliclazide, Glimepiride, Glyburide, Tolbutamide):
GIT disturbance (metallic taste), hypoglycemia, weight gain, hepatic x renal insufficiency.
(Jaundice), tachycardia, headache, rash, increased ADH.
Biguanides (Metformin hydrochloride)
GI (Diarrhea, nausea, vomiting, abdominal bloating, flatulence, and anorexia) are the most
common reactions to metformin and are approximately 30% more frequent in
patients70ccasionally, temporary dose reduction may be helpful.
Decreased vitamin B
12
absorption "cyanocobalamine7 megaloblastic
Unpleasant or metallic taste, which usually resolves spontaneously
A rare and serious side effect is lactic acidosis.
Alpha-gluc<?sidase Inhibitors (Acarbose): GI: Flatulence, diarrhea, abdominal pain, cramps,
nausea.
Thiazolidinediones (Pioglitazone, Rosiglitazone): Weight gain, fluid retention, and
hemodilution, varying effects on lipids: increase HOL, increase LOL, pioglitazone decrease TG.
As a consequence of their improved insulin sensitivity, these patients may be at risk of
pregnancy if adequate contraception is not used.
Orlistat: stetorrhea (oily leakage), and
abdominal discomfort
Thyroid disorders
Important Concept!
Orlistat intestinal lipase inhibitor
Thyroid gland secretes Levothyroxine, Liothyronine or triiodothyronine and calcitonin
33-4
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Medicina1 Chemistry
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Deionidation
NH2
~ CONa
I
Sodium Liothyronine (T3)
r
:>
~ H 2
...
GONa
Sodium Levolhyroxine (T4)
Important Concept!
Deiodination reaction is catalyzed by deiodinase enzyme takes place in peripheral
tissues and liver.
Medicinal chemistry of thyroid disorders
Drugs U s ~ ~ n Thyroid Disease
I
I J-1ypothyroids
I
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Thyroxine (1'4)
I Triidothyronine (T3) I
Synthroid
Eltroxin
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Iodide
1
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Methimazole
Lugol solution:
Propylthiouracil
(1<1+1)
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liothyronine and thyroid, desiccated
Thyroid hormones therapeutic use: Levothyroxine (Eltroxin, Synthroid), liothyronine, thyroid,
desiccated is used for the treatment of Goiter and thyroid cancer
Thyroid hormones Side effects: Levothyroxine (Eltroxin, Synthroid): Rare side effects such as
anxiety, diarrhea, weight Joss, sweating, insomnia, and muscle cramps.
33-5
1
Medicina}
Thyroid hormones Drug interactions
Levothyroxine may increase the effects of warfarin. Thyroid hormones increase catabolism of
vitamin Kdependent clotting factors. Glycemic,control may decline with initiation of 4,
potentially necessment of antihyperglycemic agents. antiepileptic, cholestyramine, and
sucralfate may reduce the absorption of Levothyroxine because these agents binds with T4.
Drug and Food interactions: Levothyroxine: May
decrease absorption of levothyroxine by: Iron salts,
Cholestyramine, Colestipol and sucralfate
Thyroid hormones monitoring
Question Alert!
Thyroxine taken empty
stomach.
Levothyroxin: Periodic tests of thyroid function, Monitor TSH levels to adjust initial
dosage after 6 to 8 weeks then as required or annually adrenal insufficiency may adrenal
insufficiency may have to be increased during pregnancy to maintain TSH in desired range;
check TSH each trimester and 4 to 6 wk after any dosage adjustment.
Treatment of hyperthyroidism
Antithyroid drugs Chemistry: Thioamides: .methimazole, and propylthiouracil, and iodides,
Lugol solution (KI+I) and radioactive iodine.
Antithyroid drugs Pharmacology
Methimazole:
Do not prevent the uptake of I by the gland they inhibit the synthesis of T3 and T4 by
inhibiting the iodination of tyrosine in the thyroglobulin
. Blocks the coupling ofthe iodo thyroxin.
Inhibits the conversion of T4 to T3 thereby thyroid hormone synthesis is decreased.
Obvious effects are very slow since it takes 3-4 weeks before the hormone levels show a
decrease
Propylthiouracil: Manage the overactive thyroid gland
Iodides: (Lugol's solution)
'. Lugol solution is KI+I
Inhibits the uptake of 1
2
by a tyrosine.
Inhibit hormone release by inhibiting thyroglobulin degradation..
Decrease the size of the gland, decrease blood supply to the enlarged gland therefore it is
used in preparation for surgery
Radioactive iodine:
Effects of iodide on the thyroid gland.
33-6
\ ,
Therapeutic uses
Radioactive iodide: induced genetic damage, leukemi.a, Cannot be aQmlnistered to
pregnant and nursing mothers cross placental barrier secreted into the breast milk
Emission of Brays.
Gets incorporated into the storage facility
Very effective as it concentrates in the thyroid destroys the gland within a few weeks
Medicinal Chemistry

Iodides: Uncommon, reverses when the drug is discontinued, outbreak of acne
Swollen salivary gland, ulceration of the mucous mer:nbranes, conjunctivitis, rhinorrhea, and
metallic taste, bleeding disorder, anaphylactic reaction.
Antithyroid drugs side effects
Antithyroid drugs (Methimazole and propylthiouracil): Reduction in white blood cells leading
to the risk of infection, nausea and vomiting, joint pain, headache, rashes and itching,
Jaundice, fever.
Antithyroid drugs (Methimazole Propylthiouracil)
Methimazole: used to treat hyperthyroidism
Propylthiouracil: used to treat hyperthyroidism
Iodides: Used in the treatment of thyroid storm
Radioactive iodine: 1
131
isomer of is used in the treatment of thyrotoxicosis
Antithyroid drugs Contraindications I Precautions
Propylthiouracil: Prescribed with caution in pregnant-women. There is a risk of goiter and
hypothyroidism in the newborn infant if too high dose is used. Reduce dose to infant and
children
Iodides: Should be avoided in pregnancy as it crosses the placental barrier thus causing
fetal goiter.
Antithyroid drugs Pharmacokinetics
Methimazole: WeJl-absorbed, Slow excretion, tl/
2
is 6 hours
Propylthiouracil
Propylthiouracil- rapid absorption after oral administration
Peak serum levels seen after 1 hour, and tl/2 is only 2 hours
Extensive first pass metabolism
Excreted by the kidneys as glucuronide (inactive)
Preferred jn pregnancy for it does not cross the placental barrier
Strongly protein bound. Secreted in breast milk less than methimazole
Radioactive iodine: Sodium 1
131
given orally and well absorbed from the GIT, tl/2 is 5 days
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Medicinal Chemistry
Medicinal Chemistry Steroid Hormones: The hormones that consist of fused 17-carbon atom
ring system are classified as steroids. Examples of hormones that have steroidal structure:
Vitamin D, adrenocorticoids or corticosteroids, and gonadal o r o n ~ s or sex hormones
(estrogen, progesterone, and testosterones). Chemically these are derivatives of
cyclohepanoperhydrophenanthrene, which also similar to aromatic phenanthrene ring
structure. Steroid skeleton consist of three 6 member cyclohexane rings and 1 cyclopentane
ring.
17
3
4
6
16
Question Alert!
All steroid hormones like estrogen,
progesterone, testasterone and vitamin
'D have 3 cylohexane rings, and 1
cyclopentane ring
Adrenocorticosteroids: Derived from C-21 pregnane
steroidal nucleu's
Cortisone and hydrocortisone
Question Alert!
Oxygen atom at C-li is,
essential for glucocorticoid
activity.
Steroid Skeleton
Formed and seereted from the middle layer of
adrenal cortex.
17-Q<eto-side chain ((O(H
2
0H), the 4-ene, and the 3-ketone structures.
Oxygen atom at (-11 is essential for glucocorticoid activity.
Double bond between (-1 and (-2 increases glucocorticoid activity wlo increasing mineral
corticoid activity.
Fluorination at (-9 increases both mineral corticoid and glucocorticoid activity
Fluorination at (-6 increases glucocorticoid activity and less on mineral corticoid activity.
Hydroxyl group at (-17 and methyl group at (-16 enhances glucocorticoid activity and
abolishes mineral corticoid activity.
An acetate ester at (-21 or 16a.-, 17a.-isopropylidenedioxy groups enhances topical
absorption.
Aldosterone
Desoxycorticosterone acetate and fludrocortisone acetate. Formed in the outer layer of
the adrenal cortex, a prototypical mineral corticoid (aldosterone) and middle layer gives
cortisones.
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Hydrocortisone
33-8
www.Phamacyprep.com Medicin'al Chemist:ry
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Desoxycorticosterone
o
Ac
Fludrocortisone
Gonadal Hormones
Testosterone
I
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Testosterone Testosterone
Anabolic steroids Antagonist
Finasteride
Dutasteride
Cyproterone ac.etate
Nonsteroidal
nist
Flutamide
6)
Bicalutamide
nilutamide
Norethidrone
Norgestrel
Norethynodrel
Norgestimate
Desogestrel
Medroxy p r o ~
Progesterone antago
Mifepristone (RU-48
Gonadal Hormones
,--------1-------
8
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I
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I Estrogen
Estradiol
Ethinyl estradiol
Mestranol (prodrug)
Estrogen antagonist
Tamoxifen
Clomiphene
Estrogen agonist +
antagonist (SERM)
Raloxifine
/
Estrogen Progesterone Testosterone
Although there is a new chiral group at C
7
. It is considered antiestrogen since there is no
functional group at carbon 7
33-9
Estrogens
Medicinal
Estrogen chemistry: Ovaries produce 1713 estradiol and estrone. These hormone have 18
carbons for four rings. Three 6 membered rings and one 5 member ring. Estrogen exist as
estradiol in body in equilibrium with oxidized form of estrone and further biochemically
modifies water soluble of estriol that let excrete estrogen. Estrogen A ring is phenolic ring
(aromatic), basic nucleus is known as estrane with methyl group designated as C-18 on
position C-13 cyclopentano-perhydrophenanthrene.
Ethinyl estradiol 17 alpha estradiol
Diethylstilbestrol Non steroidal synthetic estrogen (stilbene derivatives)
H 0
Estradiol Estrone
Estriol
Estrogen Pharmacology
Estrogens are female sex hormones that are used primarily to decrease bone loss and to treat
the symptoms of menopause. Estrogen is used to reduce or prevent osteoporosis in
susceptible women. Estrogens decrease the frequency and severity of hot flashes as well as
the dryness in the vagina that many post-menopausal women experience.
Estrogen therapeutic uses
Estrogen is the component of all brands of oral contraceptive pills. Estradiol and conjugated
estrogens are available in tablet form; estradiol is available in a patch and injection.
Conjugated estrogens are available in a vaginal cream. Estrogen is component of Diane 3S and
, Alesse oral contraceptive that are used for the treatment of acne.
Estrogen side effects: Feminization (Breast tenderness), Gl: Nausea, stomach upset,
depression, weight gain, CVS: increased blood clotting (Increased risk of thromboembolism
diseases), edema, hypertension, stroke, and MI. The most frequent adverse effect is nausea.
Prolonged used of estrogens (estrogen given without progesterone) in
postmenstrual women increases the risk of endometrial cancer.
33-10
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Raloxifene therapeutic use: Used in prevention of osteoporosis.
Raloxifene side effects: Hot flushes
OH
Raloxifen
(EVISTA)
HO
CI
Clomiphene
Tamoxifen
(NOLVADEX)
Antiestrogen pharmacology
Tamoxifen competes for binding to the estrogen receptors thereby inhibits the action of
estrogen.
Clomiphene Interferes with negative feedback of estrogen on hypothalamus and pituitary
thereby increases the secretion of gonadotropin releasing hormone (GnRH) and causes
stimulation of ovulation.
The two-drug tamoxifen and clomiphene are categorized as full antiestrogens. Ratoxifene is a
Selective Estrogen Receptor Modulator (SERM) has partial antiestrogen and estrogenic
actions.
Antiestrogen chemist.rv: These drugs are non-steroidal antiestrogenic compounds equally
effective in oral or injection forms.
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Antiestrogen therapeutic use: Tamoxifen is indicated in advanced breast cancer in
postmenopausal women. Clomiphene is used to treat infertility associated with anovulatory
cycles.
Raloxifene Pharmacology: Reduces bone resorption thereby decrease bone turnover. Exhibit
estrogen like (agonist) effect on bones and lipid metabolism. Exhibit estrogen antagonist
action on uterine and breast tissues.
Antiestrogen side effects: Tamoxifen: hot flashes, vaginal bleeding, menstrual irregularities,
risk of endometrial cancer, nausea, least nauseating anticancer drugs.
Clomiphene: ovarian enlargement, vasomotor flushes, visual disturbances.
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Medicinal Chemistry
Question Alert!
17-alphaethinylandrogen are
potent progesterone
Progesterone chemistry: Progesterone is a C-21 steroid, its basic nucleus is known as
pregnane.
Two types of progesterone
17-alpha hydroxyprogesterone: Medroxyprogesterone acetate and Megestrol acetate
17-alpha ethinylandrogens (more potent):
Norethindrone and Norethynodrel: Commonly used
in OCs, because potent oral activity, more lipids
soluble and less first pass metabolism.
(no aromatic ring
and ketone at position 3
Progesterone Medroxy Progesyterone Acetate
HO ,C C-H
\\\\\
Noethindrone
Progesterone therapeutic use
Progesterone are used alone for the treatment of amenorrhea, abnormal uterine bleeding,
and endometriosis. Levonorgestrel is progesterone, which is available as a sub-dermal
implant for long-term contraception. Six capsules are implanted on the inside of the upper
arm. Contraception begins within 24 hours and may last up to 5 years. Side effects: nausea,
depression, liver failure, cancer and high blood cholesterol. Medroxyprogesterone acetate
(Depo-Provera) is used to treat amenorrhea (cessation of menstrual periods) and abnormal
uterine bleeding. It is also used as a contraceptive. As a contraceptive, 150 mg is injected
once every three months.
33-12
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Progesterone side effects
Medroxyprogesterone acetate (Depo-Provera): unexpected or increased flow of breast milk,
depression, loss or changes in speech, coordination, stomach pain, swelling of face, ankles or
feet, headaches, mood changes, unusual fatigue.
Anti Prq;estiI ti
Anti Progesterone: Mifepristone (RU - 486)
Anti Progesterone pharmacology
Progestin antagonist with partial agonist activity. Mifepristone also has anti glucocorticoid
property. Causes abortion if administered in early pregnancy (85%) due to interference with
progesterone and decrease in production of human Chorionic Gonadotropin (heG).
Anti Progesterone therapeutics use
Abortifacient: Administration of mifepristone used as contraceptive given once a month
when progestin levels are high (Prostaglandin E
1
and misoprostol orally aher single dose of
mifepristone effectively terminates the gestation.
Androgens
Danazol. Nandrolone, Stanozolol, and Fluoxymesterone
Testosterone: (-19 steroid
Androgenic effect: Testosterone 17-enantahne; resemble estradiol esters that increases
duration of action when given I.M. Agents with 17-methyl groups are orally active
Androgen Teslosterone enalllhalC
TestOSlcronc (no ester or cthinyl group)
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Dromostanolone Anliandrogtn
33-13

Androgen pharmacology
Medicinal
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Testosterone is the androgen that leads to the development of male'secondary sexual
characteristics and maintains the male reproductive system.
Androgen therapeutic use
Testosterone is commonly prescribed in the treatment of female breast cancer, androgen
deficiency, and for stimulation of growth, weight gain, and red blood cell production.
Commonly known as "anabolic steroids" because they promote muscle growth. They are also
commonly used to help patients recover from a surgery and cancer treatment that resulted in
damage to muscle tissue. Androgens orally ineffective.
Danazol: indicated in endometriosis (ectopic growth of the endometrium)
Androgen side effects
In males: Priapism (continuous erection), impotency, and
In females; masculinization, acne, hirsutism, deepening of voice, menstrual irregularities.
Contra indicated in pregnancy.
Increase LOL, decrease HDL levels, and increase coronary artery disease (CAD), fluid
retention (edema).
Finasteride (Proscar, Propecia), Dutaste'ride, Flutamide, and Cyprote'rone acetate
Antiandrogen nonsteroidal in nature (example: Flutamide, bicalutamide, and nilutamide)
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Antiandrogen
Testosterone (no ester or ethinyl'group) Finasteride (presence of Heterocyclic ring)
Anti androgens pharmacology: Inhibit the syntnesis of androgen
Finasteride: Competitively inhibits 5-alpha reductase this alpha reductase catalyses
testosterone to dihydrotestosterone (DHT). Because growth is dependent on
DHT, rather than testosterone. This drug is used for BPH.
33-14
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Insulin is stored at >
Insulin antagonist-7
Insulin has pharmacodynamic effect on
Chlorpropamide + alcohol can cause -7
Medicinal Chern istty
Metformin + glyburide may cause7
Meglitinides - Nateglinide (Star:lix), repagliriide (GrucoNorm)
Biguanides - metformin (Glucophage)
Dose adjustment in renal impairment, SE: lactic acidosis, diarrhea (most), VB
12
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ONLY oral, NO Wtl" -7 good for obese Pt, NO hypoglycaemia on its own
01: alcohol (potentiates hypoglycemic effect)
CI: hepatic impairment, renal impairment, CHF, hypoxemic states Pts
Glucagon cause-7
DKA mainly occurs in -7
Sulfonylureas: Chlorpropamide, Gliclazide (Diamicron), gliclazide long-acting
(Diamicron MR) glimepiride (Amaryl),glyburide (Oiabeta),tobutamide
What drug shows it action by acting on cell surface?
Thiazolidinediones (TZOs) - pioglitazone (Actos), rosiglitazone (Avandia)
rosigritazone / glimepiride (Avandaryl), metformin (Avandamet)
SE: Wtl'(most), fluid retention, l' HOl, NO hypoglycaemia on its own
01: gemifibrozH (l'repagrinide conc. avoid), C1: CHF pts, can use renal impairment
pts
,
Anti androgens therapeutic: Finasteride: steroid like drug approved for benign prostate
hyperplasia (BPH) treatment.
Antiandrogen side effects
Sexual dysfunction: Decrease libido, testicular pain breast tenderness and hirsutism
Hypersensitive reactions like rashes, pruritus, swollen face and lips
Contraindications: Pregnancy
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www.Phannacvprep.com Medicinal Chemistry
Alpha-glucosidase Inhibitors: (GI.ucobay)
With meal, NO use as monotherapy, SE: flatulence, diarrhea
Incretin hormone (Dipeptidyl peptidase-4) Inhibitors (DPP-4s) (Januvia)
SE: Nasopharyngitis, Dr : low (NO inhibit CYP P450),
Take with metformin, with or without food, NO potentiates hypoglycaemia
Intestinal Lipase Inhibitors - orlistat (Xenical)
SE: Diarrhea, Stethorrhea, abdominal discomfort, and oily leakage.
Take with food; impair absorption of fat-soluble vitamins (A, D, E, K)
Thyroid Hormones-Ievothyroxine (Eltroxin, Euthyrox, Synthroid): T4
Dosage: 1.6 I1g/kg/day (adults), 12.5-25 Jlg/day (pts with coronary artery disease or
elderly)
Example of antithyroid drugs -7
Myxedema is malfunction of -7
Antithyroid Agents - methimazole: MMI (Tapazole), propylthiouracil: PTU (Propyl-
Thyracil).
SE: agranulocytosis, monitor WBC or CBC
Stop about Sdays prior to a thyroid scan, RAIU or treatment with 131,
Increase in cortisone cause (Hypercorticoids) -7
Decrease in cortisone cause (Hypocorticoids) -7
Glutathione is -7
During ovulation increase of -7
Corpus luteum is stimulated by -7
What steroidal hormone structure have phenolic ring -7
Finaseride is -7
Vitamin D
3
acts as -7
The effect of vasopressin on kidney -7
Deficiency (absence) of ADH cause -7
Glutathione protects-7
The endocrine gland plays important rule in calcium metabolism -7
33-16
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Steroid structures are common in hormones, such estrogen, progesterone, and
111 postmenopausal therapy, which drugs have, risk of endometrial cancer ~
Example of antiandrogenic drug -)
Finasteride mechanism of action -7
The major factor that controls Na excretion in kidneY7
The e i f e ~ t of the antidiuretic hormone is to -)
Medicinal Chemistry
testosterones. Steroid contain how many cydohexane and cyc!opentane respectively
in it skeleton.
Oral contraceptives completely contraindicated in7
Oxytosin is used -7
Calcium reabsorption of distal convoluted tubule due to-7
Testosterone to 5-hydroxy testosterone is catalyzed bY?-7
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Pharl11acology of
Respiratory Drugs
Questions" Alerts!
Common questions in"pharmacy exam is to ask!
Pharrnacol?gy ofbeta2. agonist
Side effects of oral steroids like prednisone
AS rna
Chronic inflammatory disorder of the airways, l' airways responsiveness, causes
reversible obstruction. In asthma esinophils, mast cells and T lymphocytes plays
significant role.
l' sensitivity, <;Ind hypersensitivity of airways to specific and non-specific stimuli, such as
air, odour, allergens, and virus etc.
Asthma COPD
Airway (Bronchus) .ir.ermmal alveolf
"Inflammatory disease .'E1rf'p'llysenia'(>p'ermanent Bl'Onchitis
ofaTVe61i)
Esinophilic Neutrophilic
Coughing with wheezing during SOB (dyspnea) SOB (dyspnea) +
breath, SOB sputum
DOC for acute asthma attacks is DOC bronchodilator
salbutamol, Inhaled ipratropium, LABA
corticosteroids (ICS)
Beta2 Adrenergic Agonist
MOA: beta2 stimulation causes increase camp in smooth muscle leading to
bronchodilation
34-1
.-----
34-2
Oral Beta2 agonist: Albuterol (Salbutamol), Orciprenaline, and Terbutaline
More SE, and less bronchodilation effect than inhaled preparations
Corticosteroids
Inhaled corticosteroids (ICS): Benefit l' lung function, "
.J,. symptoms of exacerbations. Max clinical effects in 2 to 4 wks. Fluticasone in few
days, given 2 to 4 pf BID
Oral corticosteroids (Po CST)
Therapeutic use: Severe asthma with intensive airway inflammation.
SEs: hyperglycemias, osteoporosis, hypothyroidism, hypertension, weight gain,
susceptible to infections.
Question Alert!
SEs of inhaled corticosteroids (ICS) like oral
thrush management
TIotropium a long acting anticholinergic
bronchodilator.
Question Alert!
Anticholinergic: Ipratropium bromide: useful as
alternative for patients who are already
susceptible to tremors or tachycardia from B2
agonist. Tiotropium is long acting anticholinergic
taken once daily, it is administered by handihaler
Long acting beta2 agonist (lABA):
Inhaled: Formoterol (full 8
2
agonist), salmeterol (partial agonist)
Onset: 14 min arid duration up to 24 hours. Regular BID'treatment
Therapeutic use: Maintenance therapy and EIA NOT for acute. Used in patients
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already taking corticosteroids. Fnqnoterol can 'be used for atute andl11a.in:tf'iiarice"
Short acting beta2 agonist (SABA).
Inhaled: Albuterol (salbutamolJ. terbutaline, isoproterenol
Onset: within 5 min
Therapeutic use: relieve bronchoconstriction, the acute symptoms of cough,
wheezing and chest tightness, asthma emergencies and exercise induced asthma
SE: Tremors, nervousness, weakness, flushing of face or skin, nausea and vomiting.
Regular use can lead to decline in lung function.
leukotriene antagonist: Montelukast and zafirlukast
Therapeutic use: Asthma maintenance (steroid sparinG acentsl, and drug of choice
for ASA induced and beta-blockers induced asthma
Montelukast: used in children> 2 yr age, available as granules and chewable tablets
$1;:'Ofa'lphara-ngeal candidiasis (oral thrush),
from-vocarcdrd
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Zafirlukast: used in over >12 yr age, only oral available
Chronic Obstructive PUlmon'ary Diseases
COPO: Chronic Obstructive Pulmonary Diseases; capo is due to chronic obstruction of
airway passage. COPD is two types:
Emphysema (high altitude sickness)
Chronic bronchitis.
Emphysema is a disease in which the small air exchange sacs (alveoli) in the" lungs
become permanently enlarged and damaged (alveoli walls destroyed) decreasing
oxygen absorption and resulting in shortness of breath.
Chronic bronchitis is an inflammation of the airways in the lungs that causes lungs to
produce excessive amounts of mucus (phlegm), associated with chronic productive
cough. This reduces the flow of air to the lungs.
Drug used for the treatment of capo
Anticholinergics:.lpratropium (Atrovent) and
tiotropium (Spiriva): It is muscarinic blocker
and act as bronchodilator
Beta adrenergic agonists
Corticosteroids
Theophylline
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capo is I"
Asthma symptoms 3 ' C2- ,s
Asthma triggers include, ca f I \', "J Il .13 J t
A young patient having asthma and allergic to air conditioners. What will be the _I 1.. .
pharmacist recommend? -7 VJe.. I 4
What is the drug of choice in allergy induced bronchospasm? -7 ep' .1
What action of adrenergic agonist action is selected treatment of asthma? -7 f1t U(
Formeterol is can be best described as-7 kh::; A.. M H.(f t:-.4
Theophylline clearance is increased by -7 OJ..e. f...J... j' h,aho/&I &
What are the drugs that cause bronchodilation and bronchospasm?
Drugs that cause bronchodilation
Beta2 agonist
Mixed alpha & beta
Muscarinic antagonists-7
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Mixed betal and beta2 blockers, partial agonist & antagonist
Salbutamol is? beta2 agonist (sympathomimetics)
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receptor 2. cough 3. wheezing
4. en"largement 5. Salbutamol 6. Ell)physema
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7. chronic bronchitis 8, emotional stress 9, cold air
10. dust pollen 11, ASA 12. Animal dander
13, mold 14, humid>SO% 15. exercise
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asthma symptoms(
asthma triggers include? ( J
The drug of choice to treat allergen induced bronchospasm ( I
what action of adrenergic agonist action is selected treatment-of asthma? (
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34-4
Pharl11acology of
Musculoskeletal .Drugs
Questions Alerts!
Osteoarthritis symptoms (pain in weight bearing joints)
Acetaminophen and NSAIDs side effects (renal), ulcers
Rheumatoid arthritis: Methotrexate dose and infliximab
Acute gout attack therapy: indomethacin, colchicine and prednisone
Rheumatoid Arthritis
IgRF
complex
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Production of
autoimmune
antibodies
Activation of
Bcells
Glucocorticoids
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Stiffness Moming or after inactivity (last 30 min) In the morning (last 1 hour)
limited affected joints.
localized Worsens with activity or Not localized
Pain after prolong use, (weight bearing activity) Worsened with prolonged inactivity. (usually
Generally weight bearing joints improves with activity).
Affects on weight bearing and non weight
bearing joints
Inflammation Uncommon Common
Risk factor :> 6S years Autoimmune
Osteoarthritis
A degenerative joint disease caused by a breakdown of the cartilage of the bones.
Degradation of articular cartilage in synovial joints
Osteoarthritis fOAl is a degenerative joint disease caused by a breakdown of the
cartilage between bones.
Question Alert!
Initial therapy to treat osteoarthritis;
acetaminophen 650 mg q4-6h
Rheumatoid arthritis (RA): Inflammation of joints with frequent acute attacks.
Rheumatoid arthritis occurs when body's immune system attacks the tissue
lining and results in the joints causing cartilage to erode.
Causes:
RA; autoimmune
OA; aging of cartilage and trauma
Sex distribution:
RA; more common in females
OA; equal in both sex
Symptoms:
RA; Joint stiffness in the morning, painful and swollen joints
OA; Painful joints, restricted joint movements
Diagnosis:
RA; Rheumatoid factor, erythrocyte sedimentation rate, x-ray, antinuclear
antibody
OA; X-ray only
Treatment
Rheumatoid arthritis -7 NSAIO's, and OMARO's
Osteoarthritis -7 NSAIO's
Non-prescription:
Acetaminophen is initial drug of choice for
symptom relief. Maximum therapeutic dose
should be tried for 2 to 3 weeks
Acetaminophen 650 mg 4 to 6 times a day
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lab investigations of RA.
Question Alert!
Question Alert!
Methotrexate dose. weeki.-
lab tests before initiating methotrexate
ASA/NSAIDs/lbuprofen is 2
nd
line therapy
Acetaminophen + caffeine + codeine
Glucosamine/Chondroitin
Topical counter-irritants (Methyl salicylate/Menthol/Capsaicin)
Prescription Medication:
COX-2 inhibitors (Celecoxib) as effective as NSAIDs but lower incidence of GI side
effects.
Intraarticular corticosteroids ( 3 to 4 injections year)
Hyalunon injections only for those who failed other therapies
Narcotic analgesics
Rheumatoid.arthritis
A chronic systemic, autoimmune inflammatory condition. Symmetric synovitis affecting
similar joints bilaterally.
It is non organ specific autoimmune disease
Type III hypersensitive. reaction
Blood contain rheumatoid factor
Stiffness occurs in the morning
Large of areas of joints are effects
Not associated with frequent of use of
joints
It effects on weight bearing and non-weight bearing joints.
Pharmacological Choices:
Disease modifying anti-rheumatic drugs (DMARDs)
Methotrexate is the gold standard for the treatment of RA
Should be started within 3 months of disease onset (max effect in 3 to 6 months)
Initial dose of 20 to 25 mg po/wk, do not exceed> 25 mg/wk
Minor SEs oral ulcers can be reduced by concurrent use of folic acid
Should be avoided in patients with hepatitis Band C, renal insufficiency, or lung
disease, serious SEs are cytopenia, and hepatic
toxicity.
Hydroxychloroquine; SE corneal and retinal
deposition
Sulfasalazine
Leflunomide
Can be used in combination with methotrexate (Cl in pregnancy) or in place of it for
patients who have failed have contraih'dications to methotrexate.
Should be stopped in both males and females at least 3 months before attempting
conception (patient must undergo drug elimination by taking cholestyramine 8 g TID
for 11 days.
35-3
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Glucocorticoids; Prednisone/Triamcinolone - safest therapy during
pregnancy and lactation
Biological response modifier: Inflixim.b, el.nereept, .d.Jimumab
Formation or uric acid, urea and glyoxylic acid from purines
Gout is a disease in which monosodium urate monohydrate (M5U) crystal deposit in
joints, soft tissues such as cartilage, tendon and bursa or renal tissues such as glomeruli,
interstitium tubules.
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Xanthine
Adenin....
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Allantoin
Adenine
Azathioprine a purine analog immunosuppressive agent
Cyclosporine
Minocycline
Penicillamine
Gold sodium thiomalate
NSAIDs
InfJiximab
Biological response modifier act as TNF a inhibitor. It is monoclonal antibody
Only available as i v. Store in refrigerator
Approved for ulcer.live eolilis Question Alert!
It is always used with methotrexate. Infliximab mechanism, SEs and monitoring
SEs: The most common SEs are headache,
fever, chills, fatigue, diarrhea, pharyngitis
upper respiratory tract and UTJs.
Gout Arth ritis
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Gout is associated with increased body stores of uric acid. Acute attacks involve joint
inflammation caused by precipitation of uric acid crystals.
Hyperuricemia Urate crystal in joints inflammatory response
Acute gout arthritis
Abrupt onset of excruciating pain and inflammation of joint during the night or early
morning. Patient cannot tolerate even light pressure such as a bed sheet on the affected
joint. Attacks often resolve spontaneously over 3 to 10 days.
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Colchicine
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line treatment is indomethacine, jf contraindicated then colchicines and if
contraindicated then corticosteroids
Indomethacin
It is prostaglandin type I NSAID
It has the highest anti inflammatory action in all NSAIDs
It has high GI irritation SE
It do not decrease uric acid
Colchicine
It produce an anti-inflammatory and analgesic effect
It not used as analgesic action
The most common SE is GI irritation
CI: in severe renal diseases (CrCI <50 ml/min)
Corticosteroids
Given intraarticular injections for monoarticular pain
Given oral for polyarticular pain
Antihyperuricemic agents
Allopurinol
Inhibit xanthine oxidase (XO)
Allopurinol and azathioprine drug interactions is due to which enzyme: XO
SE: can form urate crystal in kidney and take with plenty of fluids
35-5
35-6
l. Anti hyperuricemia 2. GI irritation 3 Allopurinol
drugs
4. Sulfinpyrazone s. Probenecid 6 Alloxanthine or
oxypurinol
7. Acetaminophen 8. Renal failure
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Increase uric acid excretion
SE: can from kidney stones
Drink plenty of fluids
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A1loxanthinc:
Allopurinol (ox)'purinol)
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Probenecid
Increase uric add excretion
SE: can form kidney stones
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Drink plenty of fluids while taking... (3, t
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What analgesic is not used in gout arthritis? ('- )
Example of drug that decrease uric acid production (3
Example of drug that increase uric acid secretion H, r )
What drug is not used for acute gout attack? (g,,() 1
The major metabolite of allopurinol (II l I'
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Pharmacology of
Antimicrobial Drugs
".
Questions Alerts!
Quinolones mechanism of action
Structure activity of p n i i l l i n ~ and cephalosporin's
Mechanism of penicillin resistance
Tetracycline epimerization gives 4-epitetracyclin
Macrolides side effects explain by structure activity
Antibiotics classifications
Cell Wall synthesis Penicillins, Cephalosporins, Vancomycin
inhibitors
Protein Synthesis Aminoglycosides, Macrolides, Tetracycline's, lincosamide
inhibitors
DNA Synthesis QuinolonesjFluoroquinolones, Metronidazole
inhibitors
Folate Inhibitors Sulfonamides, Trimethoprin
36-1
k.- I
f3 cl .....
/oJ'1 9 'P"1S
111 reploJ.r.rp&
eaOH
R
H

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/ COOR
Dihydrothiazinc
Thiawlidine
R
eOOH
6-Aminopenicillanic acid

13-lactarn ring
o
Penicillins
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D=Susceptible to hydrolysis
Penicillins
Cephalosponns
Protein Synthesis Inhibitors
,
ChloramphenIcol, are bactereostatl(.
Macrolides: Erythromycin, c1arithromycin and azithromycin
Mechanism: Protein synthesis inhibitors
Structure: Large lactones ring of 12 or 14 or 16 atoms; attached to a
& neutral sugar by glycosidic link
Erythromycin
lactone ring + desoamine (amino5ugar) + c1adinose (neutral sugar)
Common SE: Gastric upset, is due to conversion of erythromycin to ketal
The macrolide are generally unstable to acids, bases & high temperature
Azithromycin
Stable to acids, bases & high temj), thus less gastric upset
long half-life, greater and longer tissue penetration
covers H. influenza
I 50 S Antibacterial Agents
I
I 30 S Antibacterial Agents I
Macrolidcs Chlorampbcnicol
Aminoglycosidcs Tetracycline's
Gental1lycin Demeclocycline
Erythromyein Lincosamides
Streptomycin Doxycycline
Azithromycin Clindamycin
Clarithromycin Lincomycin
.
Kanamycin Minocycline
TEST CC: T" E= 5 _ Sulfadrugs, T" trimethoprin, C= C =
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Important Concept!
Tetracycline must take empty stomach
due to chelation with metal ions.
Clarithromycin
The enhanced Iipophylic allows for lower or less
frequent doses
Tetracycline's: Tetracycline, doxycycline, and
minocycline
Tclracyclinc
4 Epi- Tetracycline
M
Epimeriuu.ion of Tetracyclines
m
HOQwH
M= di or trivalent metal ion
Metal chelation with the tetracyclines
Quinolones &Fluoroquinolones
Mechanism of action: DNA gyrase inhibitor (topoisomerase II) and topoisomerase IV
Quinolones
Fluoroquinolones
Nalidixic acid (disinfectant)
1
st
gen: Nalidixic acid, Norfloxacin .
2
nd
gen: Ciprofloxacin, Oflaxacin
3
rd
gen: Gatifloxacin, Moxifloxacin Levofloxacin (respiratory)
4
th
Travofloxacin
/
I
Question Alert!
Quinolone mechanism of action! by DNA
gyrase (topoisomerase II) and
topoisomerase IV .
Folate antagonist Sulfa drugs
Dihydroteroate diphosphate + PABA -7
.. dihydroteroic acid -7 tetrahydrofolic acid -7
thymidine -7 DNA
Question Alert!
Sulfonamides are dihydroteroate
synthase inhibitors
36-3
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Oxazolidinones: Linezolid (po, parenteral I
Mechanism: binds to bacterial ribosome's to inhibit protein synthesis.
SE: reversible thrombocytopenia.
Tips
36-4
)3

The chemical ring present In peniCillin s (
The chemical ring present in cephalosporin's (

Tetracycline at 4 position undergoes... ( ) 4
Tetracycline chelate with.. antacids, Ca and Iron ( )
Sulpha drugs act on? ( ) ,
Sulpha drugs action prevent formation of? ( ) t
Quinolone antibiotic are bactericidal act by inhibiting... ( )
What is an example of urinary tract disinfectant? () c.
loOl-<J C<M"""::1 -I-<cd
Tips
IS commonly causes dose-related 61 tract disturbances, Includmg nausea, vomiting,

and diarrhea( 1 )
raises blood levels of theophylline and potentiates terfenadine in producing
ventricular arrhythmias_ (7 )
have enhanced activity against Haemophifus influenza (.,) )
Inhibit the activity of DNA gyrase ( II "n
are effective in bacterial prostatitis and bacterial diarrhea except that caused by C.
difficile(
as competitive inhibitors of p-aminobenzoic acid in the folic acid metabolism cycle( !.
)
It is used primarily for the treatment of Trichomoniasis, Amebiasis, Giardiasis (14)
1. Folate antagonist 2. Nalidixic acid 3. Thiazolidine
4. epimerization S. DNAgyrase & 6. Antacids
topoisomerase II
7. ea (bi and trivalent) 8. Dihydroteroic acid 9. Dihydrothiazine
10. Tetrahydrfolic acid
... ,
1 AmoxicilJin 3 Penicillin Gand V 5 Tetracycline
2 Cephalexin 4 Cefuroxime
Ceftriaxone
7 Erythromycin 8 Clarithromycin 9 Azithromycin
10 Ciprofloxacin 11 Ofloxacin 12 Oindamycin
13 Trimethoprim- 14 Metronidazole 15 Vancomycin
sulfamethoxazoJe
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Stevens-Johnson Syndrome is a severe form of erythema multiforme (
characterized by bullae on the oral mucosa, pharynx, anogenital region, and
conjunctiva; target-like lesions; and fever
Antacids containing Mg or aluminum interfere with absorption if taken within 4 h ( )
Tips practice format 02: Find answers from the table:
1. Folate antagonist 2. Nalidixic acid 3. Thiazolidine
4. epimerization S. DNAgyrase & 6. Antacids
topoisomerase IV
7. ea (bi and trivalent) 8. 9. Dihydrothiazine
10. Tetrahydrfolic acid 1I. 12.
the chemical 'ring present in penicillin's ( -r11
1
4Jo
11
r
the' chemical ring present in cephalosporin's ( cJ,J l; /' )
tetracycline's at 4 position undergoes...( )
Tetracycline chelate with.. ( )
S.ulpha drugs act on? ( )
Sulpha drugs action prevent formation of? ( )
Quinolones antibiotic are bactericidal act by inhibiting.:.(
what is an example of urinary tract disinfectant? (
36-5
I Phase I metabolism (Functional group metabolism or mixed function oxidase metabolism)
Reactions that convert the parent drug into: More polar (water-soluble) molecules by
introducing a polar functional group, such as -OH, or-NH
z
, COOH, SH
Phase 1 Metabolism
Definitions
Biotransformation: Biochemical reactions that are catalyzed by enzymes.
Bioactivations: Metabolic reactions that produce active metabolite.
Metabolism
Questions Alerts!
functional group metabolism major
Phase II or conjugation metabolism like glucuronidation, glutathione conjugation,
acetylation.-
Alcohol metabolizing enzymes
Phase 1 Phase II
Functional groups metabolism (OH, NH
2
, COOH, SH etc) Conjugation metabolism
Oxidation, reduction, hydroxylation, deamination, Glucuronidalion, glutathione conjugation,
dealkylations, demethylation sulfonation, acetylation, and methylation
Cytochrome oxidations (0YP"4S0j, rei:lt1ct<!se, aminase.
After metabolism of drugs: Drugs become more water soluble, excreted faster and toxicity
can increase or decrease.
Breakdown to other active or toxic metabolites.
Phase I metabolism mainly occurs in liver, kidney, GI tract and othertissues. These reactions
are catalyzed by cytochrome (CYP 450). Cytochrome is mainly found in ribosomes, specifically
endoplasmic reticulum.

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Metabolism
Drugs in ,1 undergoes the following reactions: Oxidation (most common
phase 1 reactidnL h:tdroxylation, dealkylation, deamination, reductions, hydrolysis, and de-
I \ ".
sulfuration '
Oxidative metabolism
The most common phase I reaction is oxidation. Oxidation metabolism most commonly occurs
in live;; Less in intestine, lungs and kidney catalyzed CYP4S0 with different routes 3A4:2C9,
2C6 and others oxidizing enzymes. Example: substrate, enzyme inducers and enzyme inhibitor
Alcohol oxidations
Primary alcohol oxidation -7 aldehyde -7 acid
Secondary alcohol oxidation -7 ketone
Tertiary alcohol -7 no oxidation
Question Alert!
Et.hylene glycol C\S antifreeze. L,d
m<2.1"o-h&lfsec/ L K:.
Alkyl -7alcohol -7 aldehyde -7 carboxylic acid . C-k>1<:iJy
CH
4
-7 CH
3
0H (methanol) -7HCHO (formaldehyde) (formic
acid is toxic-7 . ." ,
CH3CH3 -7 CH3CH20H (ethanol)-7 CH
3
CHO (acetaldehyde) -7 CH
3
COOH
Ethylene glycol oxaldehyde -7
Ethanol
Alcohol dehydrogenase
Acetaldehyde
<
Nausea and vomiting

headache
Hypotension
Thiamine decrease
bioavailability
Question Alert!
What vitamin deficiency can occur
in chrol\ic .alcoho!iim?

Acetaldehyde dehydrogenase
Acetic acid
Methyl group to Carboxylic
acid (Oxidation) 0
-0-
0 ..
- II .Jl"
H
3
C \ I S-N N-C
4
H
g
IJ II H H
o
Reduction Reactions
Common metabolic reactions are azoreduction, nitro reduction and carbonyl reductions.
37-2
. ---
, ,
Hydrolysis:
)7,)
Metabolism
+
o 1)' .. 1

NH
2
Sulfapyridine
Question Alert!
Site of hydrolysis in penicillin's and
cephalosporin's.
at Gut
Azoreductase
o
, \ .1
c.-On +
Sulfasalazine
Azoreduction in colon
Nitro reduction: Nitro (NO
z
) group upon reduction produce -7 Amine (NH
2
) group. Drugs that
undergo nitro reductions: eg; nitro reduction takes places in the metabolism of
chloramphenicol and c1ona2epam. Carboxylic acid upon reduction produces -7 Aldehydes and
then -7 Alcohol
Carbonyl (ketone or aldehyde) reduction: alcohols. example; acetohexamide.
acetohexamide undergoes carbonyl reductions.
Hydrolysis is a metabolic reactions that most commonly occurs in gastrointestinal tract.
I Hydrolysis is catalyzed by enzyme called esterase's. There are two functional groups
commonly undergo hydrolysis: Esters and amides.
Esters (esterases): present in plasma and various
tissues.
Ester (hydrolysis) produce -7 acid +alcohol,
Amide hydrolysis products -7 acid + amine.
Amide hydrolysis is catalyzed by amidases.
Fixed oils consist of functional groups, metabolized by ester hydrolysis, and produce
glycerol + fatty acid .....
H.01+
c--orllo\- :'9
...
C 0Ei:11 .. ..."'__
. - M __ "
r./..i-. r'-1!l _ C, \.h r) /">'.&.._11 ..
Reduction
Reduction - Bacteria resident in the Gl tract afe known to be involved in aw and nitro
reductions. Reactions catalyzed by reductase. Both mechanism of oxidation and reduction is
to create a polar substrate to be excreted.
Azoreduction: as in sulfasalazine and olsalazine
Reducing.enzymes caUed reductase, such as azoreduction is catalyzed by azoreductase
enzyme, which catalyzes reduc;tion reaction. Example of azo (-N=N-) reduction: Sulfasahine
undergoes azoreduction in gut (colon) and produces 5-aminosalicylic acid and sulfpyridine
NH'QC0
2
H
I'"
Azo bond '" OH
Saminosalicylic acid
(Mesalamine)
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Metabolism
phenacitin de ethylation
(dealkylation) give acetaminophen
A'
Meperidine
Hydroxylation
Hydroxylation
-
(SCOCH' 6
COCH
'
.
Acetanilid \ / Acetaminophen
Deamination: Examples of deamination include amphetamine and dopamine
Oxidative Deamination
O
H H
II C+NH2
CH
3
+
Aliphatic Hydroxylation
(Phenobarbital, meprobamate)
Aromatic hydroxylation
Phynetoin, phenylbutazone
R-Q
R-oOH
Olefinic Hydroxylation
(carbamazepine, cyproheptadine)

R

Benzylic Hydroxylation
(Tolbutamide, imipramine)

Allylic Hydroxylation
(Pentazocine, hexobarbital)

Dehalogenation: (Halothane, Chloramphenicol)
37-4
/
. Genetic factors: Acetylation rate by N-acetyltransferase. which may result in fast acety
dators or slow acctylators.
Nutritional status: Low protein diet decreases oxidative drug metabolism, Vitamin C deficiency
decreases oxidative pathways. Vitamin E deficiency retards dealkylation and hydroxylation
-
"
Sulfonamides, isoniazid, cJonazepam,
mescaline, and dapsone (Primary
amines undergo acetylation)
Drugs
Acetaminophen, morphine, diazepam,
sulfathiazole, and digoxin
Salicylic acid, nicotinic acid (niacin),
deoxycholic acid
Acetaminophen, methyldopa, est,,,/vCrf'>t
Epinephrine, norepinephrin.v \v\"
_ . histamine............... cJv.
Ethacrynic acid, reactive phase 1
metabolite of acetaminophen.
acid is pr6duced
Enzymes
N-acetyl transferase
Uridenyl Diphosphate
Glucuronyl Transferase (UDP
GT)
Acetyl transferase
Glutathione Stransferase
(GST)
O-Methyltransferase
Sulfotransferase
. in phase 11 reaction
Acetylation
(NH"OHI
Phase 2 reaction
Glucuronidation
Methylation
Factors affecting Drug Metabolism
Glycine conjugation
(Amino acid
conjugation)
Sulfate conjugation
I ,II':> \r-
1-1-6 " J \,./"CP>I\.-
Chemical structure (functional group), ""' \ .
Speclcs differences: Quantitative (presence 0
cl,:==-
Physiological or disease state; liver disease, CHF. renal disease, Hypo & hyperthyroidism.
Also alteration in albumin production as in elderly
'GTUmKfone
(tysteine+
'glycihe+gltitarflic acid)
"
f'4!l'\ , II 14
- e.-
D

rfl.r-J -
Cft2.. sH

Ir
t
t
H - c.H-z.-- 1SOOiF C?
Phase 2 metabolism reactions are referred as conjugation reactions; parent drug or its
metabolite with certain natural constituents such as glucuronic acid, glycine, glutamine,
sulfate, and glutathione. There are 6 major conjugation pathways:
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Metabolism
Circadian rhythms-'nocturnal plasma levels oftheophylline and diazepam are lower than the
diurnal plasma levels. . .
Drug administration route (first by pass) for oralpnly, sublingual no first bypass.
Cytochrome classification
Cytochrome P450s enzymes are located in the endoplasmic reticulum and are highly
concentrated in the liver and small intestine. Additionally. CYP P450s are also found in the
mitochondria membrane. CYP 450s encompass a highly diverse "superfamily" of hemoproteins
and one of their most relevant functions is that of metabolizing drugs in humans.
Cytochron:ac P450 into subtypes:
CVP = Cytochrome
I or 2 or 3 number = family
A, B, C. indicate subfamily
1,2.3 indicate individual genes
CVPIAI CVP2D6
CVPIB2
CVPIC3
CVP2C9
CVP2CI9
CVP3A4
CVP3AS
Drug metabolism (secondary): CVPI, CYP 2. CVP3, and CVP4 subtype of enzyme catalyze
drugs, or exogenous chemicals. CVP3A is the most common enzyme thaI catalyze phase I
oxidative reactions.
Steroid and bile acid metabolism (primary): CYP 7. CYril, CYP 17, CYPI9, CYP21 and
CYP27 enzymes metabolize steroids, and bile acids, is referred to as primary metabolism.
Cytochrome P450s are a laige group of monooxygenase enzymes responsible for the
metabolism of toxic hydrocarbons. NADPH is required as a coenzyme and O
2
is used as
a substrate.
C"''' 3.1'1'" .siLl!Jltj..c.h ,I')'''''
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Enzyme Substrate nhibitor Inducers IExamoles
IrYP3A4 lBenzodiazeoines lNefazodone henobarbital IQenerally all anticonvulsants
ihvdronvridine CCBs /o:;:l:;;RJs henvtoin k. .... inducers + Rifamnin
arbamazenine IA7nle antifunoals arbamazenine
thvnilesu-adiol imelidine rednisone lrVPJA is tbe mosl.abuod.aol
, latins (AL$l lMacrolides lE C) !TO(!litazone VP3A4 is most next CVP3A5
erfenadine rotease inhibitors IRifamoin
heonhvlline eranamil Ritonavir . isapriCfe ahd terfe-mfdil)e can
Protease inhibitors Iomenl'llzo[e - 51. Johns Wort

riazolarn Saouinavir ,zbles,an Clarith(orovtin,
I\mitriotvline
idocaine
Icvclosoorin
li"oxin

r '" "'- M"W- I
Pathway
tential D-D interaction as
drtJ S from 1 thera utic class
-F interaction
s chothcra euties
Fatal 0-0 intuaction
_" D-C interaction
ine
hen loin
me Ie
henobarbital
ifarn in
efazodone
luoxetine
uinolones
d ronox.acin
.a fruit;'. '"
eta blockers
enlafaxine
Narcotics
YPIA2
www.
They have porphyrin ring so susceptible with CO,
C02,CN
CVPs in Endoplasmic reticulim in liver and small intestine and also mitochondrial membrane
are monoexygenase Catalizors (oxidizing) need NADPH as co-enz. to use 02
lheir naming is CVP # Alphabet # (I.e., CVP3A2) genetic family/genetic subfamily/specific gene baha.
CVP 1.2,3,4, isofonns involved in drugs and xenobiotics - A-t I ".jJ.A.t9.. 1O.eA;\'O I _
CYP 7,11,17,19,21,27 involved in steroids and bile acids .... - <t"
/til ..........
1- 'CA and SSIU as well as other
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NHR
Amphetamines
Metabolism
Deamination (followed by oxidation and reduction of
the ketone fonned)
N-oxidation
N-dealkylation
Hydroxylation of the aromatic ring
Hydroxylation of the l3-carbon atom
Conjugation with glucoronic acid of the phenol
products from the ketone formed by deamination
o o
Oxidation and complete removal of substituents at
carbon 5. ' \
N-dealkylation at N
1
and N
3
Desulfuration at carbon 2 (thiobarbiturates)
Scission of the barbiturate ring at 1:6 bond to give
substituted malonylureas
R
1
N
y
"NR
3
1 II 3
a
Barbitunites
Phenothiazines
NH
2
Sulfonamides
N-dealkylation in the N side chain
N-oxidation in the N'o side chain
Oxidation of the heterocyclic S atom to sulfoxide or .
sulfone
Hydroxyaltion of one or both aromatic rings
Conjugation of phenolic metabolites with glucuronic
acid or sulfate
Scission of the N
10
side chain
Acetylation at the N
4
amino group
Conjugation with glucoronic acid or sulfate at the
amino group
Acetylation or conjugation with glucoronic acid at N
1
amino group
Hydroxylation and conjugation in the heterocyclic ring,
R
IHydroxylation of one aromatic ring
37-9
Oxidation to lactam
Aromatic hydroxylation
N-oxidation
Conjugation of ohenolic nroducts
Hydrolysis of ester to acid

Hydroxylatin of aromatic ring
N-oxidation
Both N-dealkylation and hydrolysis
Con"u ation of henolic raduels
Metabolism
Hydroxylation of tenninal methyl groups of
alkenyl side chain to give cis and trans
(major) alcohols
Oxidation of hydromethyl product of the
alkenyl side chain to carboxylic acids
Reduction of alkenyl side chain and
oxidation oftenninal methyl group
Conjugation of phenolic products with
glucuronic acid or sulfate
Hydrolytic scission oCthe hydantoin ring at
the bond between carbon 3 and 4 to give
5,5-diphenylhydantoic acid
Hydrolysis of methyl ester
Hydrolysis of benzoate ester
N-dealkylation
Both hydrolysis and N-dealkylation
Cocaine
Meperidine
HO
Pentazocine
Phen om
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Phernnetrazine
OH
E hedrine
CH
3
A
CH3
OH
4'
Pro ranolol
Metabolism
N-dealkylation
Oxidative deamination
Oxidation of deaminated product fo benzoic
acid
Reduction of deaminated product to 1,2-diol
Aromatic hydroxylation at C-4'
N-dealkylation
Oxidative deamination
Oxidation of deaminated product to
naphthoxylactic acid
Conjugation with glucoronic acid
O-dealkylation
CI
Indomethacin
Tips
o
O-demethylation
N-deacylation of p-chlorobenzoyl group
Both O-dealkylation and
Conjugation of phenolic products with
glucuronic acid
Other conjugation products
Tips practice format 02: Find answers from the table:
IT] UDP-gluconyltransferase ---IlD UDPGT
37-11
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Co,." "'" '1 Oyf' 2:i> {, Sc....b,W4 J-,-J.,I, ,./- -7 Ca Au....rL. 4 :;ti 1st WJY-cl
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4. formic acid 5. alcohol 6. oxidation
dehydrogenase
7. inhibit metabolism and 8 in the liver 9. drug metabolism is
increase concentration impaired by protein
deficiency
10. levels of some cytochrome 11. Phenobarbital, 12. Codeine & Fluoxetine
P450 isoenzymes will vary Phenytoin,
between individuals Carbamazepine,
Rifampin, St. Jolm's
wort
13. CYP 450 14. Lncreascd 15. it becomes morc
metabolism ofdrugs inactive, more polar,
larger and morc easily
excreted in the bile &
urine)
16. Benzodiazepines, statins 17. Erythromycin, 18. Acetylation
(ALSj, Digoxin, Sildenafil Clarithromycin,
grapefruit juice,
Ketoconazole,
.
Cimetidine, Protease
INH
19. Sulfasalazine 20. Glutathione 21. CYP 1,2,3 and 4
conjugation
22. endoplasmic reticulum 23. decreased in elderly 24. Glucoronidation
25. hydrolysis
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what is the primary enzyme system involved in drug'metabolism? ( crtf 4(b )
what the induction of metabolism (. q../
what IS meant by lnhlbltlon of drug metabolism and what IS Its slgruficance? ( iYl /., 1{,I+ ("h1:f4,11.I"'f 4- t t
what happens to the drug after conjugation? (,-1- rnavn'vf-- /l1"l"""," pOIM I
what enzyme catalyzes most conjugation reactions? ( .i. ) Vl l.'"'""--
how does age affect drug metabolism? ( 1.3 )
what type of nutritional factors affect drug metabolism? ( .1 ,) IJ
How does genetics affect drug metabolism? (C;lru- P4to
the mas! common metabolic reaction in the GI( (j cLIl.dJlU') b2J...
the most common Phase I metabolic reaction is? ( rJ....t...J".( lAJ )
the most metabolic reaction in human ......
the most common cytochrome subtype enzyme is? ( c.y p.s I+-i
Benzodiazepine are metabolized by? ( C Yp3. )
Gluc?ronidation reaction is catalyzed by? ( UQ) PVr7) . 11 _
cytochrome is commonly located at? ( I&-J ....... ' &
What enzyme is responsible for drug metabolism? ( e.:"/p 1,2, '1
Acetaminophen detoxification mechanism involves, what type of metabolic reaction? (iI..J...... flt)lA- ,
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Biophannaceutics
c
Questions Alerts!
Common questions in pharmacy is to ask!
Oral drug pathway to systemic circulation (mesenteric vein --> portal vein --> liver --
> hepatic vein --> heart)
Partition coefficient (octanol/water)"
"i<?h!ziWbn;a!l''d:bhid'h'ifaW)I) like oH: aKa
.- e 'oiL 1(1 a '" I I !
This cbapter review on the concepts of physicochemical properties of oral drugs and dosage
form, and the effect of route of administration on absorption. Emphasis is on bioavailability
and bioequivalence studies.
Biopharmaceutics is the study of the relationship between the physiochemical properties ora
drug to those ofdosage fonn in which contained
The fraction of unchanged drug reaching the systemic circulation following
administration by any route.
The rate and extent ofabsorption from administered dose can be figured out by using
bioavailability
.. Calculated by comparing the bioavailability ofthe product to that of
an IV bolus dose
by comparing similar data for the product to another drug
product ofthe same dose and dosage fonn.
Bioequivalence or bioequivalent drugs; bioavailability of the active ingredients in the 2
products are not statistically different under suitable test conditions. Example: generic and
brand
Klcru
,
38-1
38-2
Therapeutic equivalence; exactly the same. The same therapeutically active drug, same
therapeutic effect, equal potential for adverse effects. Example: Apo-Atorvastatin and Ratio-
Atorvastatin.
Therapeutic altematives; different active ingredient, indicated for same therapeutic or clinical
objective. Example: Ramipril and Enalapril
{tuurf>o'1

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or different unbranded product over the prescribed drug:Generic
'can equivalent. ' . . .. ,
'Pfiarmaceu1bil equlvaient; same active drug ingredient, identical strength or concentration,
dosage form and route of administration. Examples: Ramipril generic and Altaee brand.
Pharmaceutical equivalent can differ in color, flavour, shape, scoring, configuration, packing,
preservative, expiration time and labelling.
Pharmaceutical substitute; Pharmaceutical alternative for the prescribed drug product.
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First pass effect =extent to which a drug is removed by the liver during its 1
st
passage in the
portal blood through the liver to the systemic circulation. In simple words it is the amount loss
during metabolism in the liver
Bioavailability and Bioequivalence
Time Response Curve
To-T
t
= onset
To-T2= peak
T
1
-T3= duration
MDR= max drug
response
NIEC =min. effective
Concentration
Ale,>!-
Bioavailability is rate and extent, C
Comparison of Tmax, Cmax and
AUC for IR and SR preparations.

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MEC
Time
To-T
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lag time
Peak Action MDR
T,
Onset ofaction
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Duration of action T1-T3
Trough level 0/ I. I
(..;) !' ,
Time of Onset; is the time from drug administration to MEC. . .
Intensity; is proportional to the number of receptors occupied by the drug to exhl it a
maximum pharmacological effect.
Bioavailability is rate and extent
RATE (SPEED): "C
MAX
" AND "TMAX"
Extent (amount): Area under the curve (AVC)
the totaJ amount of an unchanged drug
excreted in urine.
C
max
peak concentration and Tmax is time that take to reach C
max
. Bioequivalent are
. pharmaceutical equivalent + rate and extent are equal.
o./ Absolute bioavailability: is "F' which is the fraction of drug systematically absorbed from the
\.../" dosage form. Always AVC of iv is 100% or I , . d.A e..b
AVC IN I
AVCI.
V

Relative Bioavailability: AVC of the dosage form/dose S R
Ave of the reference/dose "'y
To determine the AVC? AVC = [F x Dose]N x K
38-3
Glycoprotein
mediated
Emux
Biopharmaceutics
paracellular
Diffusion
Passive
Diffusion
(transcellular)
;--,
Partition coefficient:
Partition Coefficient (P) = (Drug)lipid I (Drug)aquoous
P = solubility in OctanoVsol. in water

A drug is hydrophobic if partition coefficient is > I
A drug is hydrophilic if partition coefficient is < I
www.Phannacvorcp.com
Transport process across membrane
I I 1--------,
Carrier
/ mediated
J
Cell membrane (phospholipid layer): Drugs high in lipids move faster in a phospholipid
bilayer and Ihis means that waler soluble drugs used carrier proteins for transport
Passive absorption (diffusion);It is also rererred as simple absorption or diffusion. The

movement ofdrugs across lipid membranes driven down by their concentration gradient.
Characteristics
There is concentration gradient (high low) is essential for passive absorption
No energy is needed for passive absorption
There must be scm i permeable membrane
Fick's Law can detennine rate ofdiffusion ofabsorption
(
# Primary Active An energy dependent movement ofcompounds across
membranes against a electrochemical gradient that is carrier mediated and requires metabolic
energy. e.g. multi drug resistant transporters.
Characteristics: Er:: q'MPr.... D
Active transport also referred as active absorption A _
Nced energy I 'Jf!.Jivo.f
No need of concentration gradient , _ A
Can go against concentration gradient if facilitated by energy. _...... J....
Example ofaetive absorption includes: tubular secretion /lJ.1
Types of absorption: Four types of absorptions occur across membrane I-Passive absorption
(passive diffusion), 2Aclive transport, 3-Facilitated diffusion, 4-Endo/exocytosis
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Examples of primary active transport ion channels:
Na+, K\ ATPase (Na+-IC pump) in cell membrane transport Na+ from intracellular to
extracellular fluid and K+ extracellular to intracellular. Examples of drugs (digoxin) that
blocks Na K ATPase
W, IC, ATPase (proton pump) in gastric parietal cells transports H'" into the lumen of the
stomach against the electrochemical gradient. Drugs that block proton pump: Proton pump
inhibitor (PPI) such Pantoprazole
Ca
2
+ATPase (or Ca
2
+pump) in the sarcoplasmic reticulum or cell membrane transport
Ca
2
+against electrochemical gradient.
Facilitated diffusion7 The carrier-mediated transport ofcompounds down an electrochemical
gradient. e.g. the cation transporters in the kidney.
Characteristics .
Require carrier (proteins)
Similar to passive absorption because do not require metabolic energy.
Examples of facilitated diffusion
Glucose uptake into muscle and adipose cells facilitated by insulin. Ifimpairs this can lead
to diabetes mellitus.
Endo/exocytosis --> Intemalization of drug molecules (cell drinking)
Rate of Dissolution
. (Noyes-Whitney)
t
Disintegration
t
Dissolution
t
Factors that determines the absorption

_ Oral

a.,.,L..llJ/-fh ""-
Norr..el - L.'h' f""""l1
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(Absorption)
Ranking of various oral dosage (fastest slowest)
i"';" S.olutions (ready for
( Ficks Law
Hasselback &
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- Rate ofabsorption
Factors that affect the rate of absorption
'" pH effect
'" ionization & unionization
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Biopharmaceutics
NOTE: one changes the pH by I unit, the ratio of non-ionized to ionized changes by factor of
10. The direction of change and ration can be calculated in one's head when the pH changes are
I full unit
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PH t pOff
pH :=: pKa + log (Salt)
(Acid)
pKa pH - log (Salt)
Solubility
Extremes ofeither water or oil solubility is associated with poor absorption
Hydrophilic:=: water soluble (water lover), poorly absorbed
Hydrophobic or lipophilic:=: oil or lipid soluble, or oil and lipid lover. Removed faster from
the body,
Disintegration: Breaking down ofdrug so as to facilitate dissolution. This usually occurs in
oral routes
Dissolution: Dissolving substances in the GIT Ouids to facilitate absorption of the drug.
Rate limiting step: It is the time it takes for a drug to disintegrate and become available for .J lui.
absorpt ion Fat- Li pill Sil
I-4A.PA A-bWlfJJ.
Factor: that effect rate of absorption --;' Lf Y) Il.:JV'I , ----:t'.J 11 - "".. J J.
Degree of ionization _ --I :(..e:>'Y' '-::-' L.., L.D
IJrugs will pass thru a membrane at a faster rate if they are unionized. The size ofan ion
increases due to dipole-to-<lipole attraction especially water. Ionized portion ofdrug is less
soluble in lipid but more in water
pH (acidity or alkalinity of the substance)
Most drugs are weak acid or weak bases. Dissociation ofweak acids or bases is directly
affected by pH therefore absorption is directly affected by pH.
As pH rises (W decreases), the amount of weakly acidic drug in the non-ionized state
decreases
As pH falls (W increases) the amount of weakly acidic drug in the non-ionized state
increases; i.e. diffusion pressure increases
For weak bases the effect is opposite
\. t{)/Henderson-Hasselbalch Equation: Helps to detenninc; pH effect on absorption. (d enninin
the drug absorption by E!<a). If the pKa of drug and pH of the medium are known, the acUon
the molecules in the ionized state can be predicted by means oCthe Henderson-Hasselbalch
equati9n. How much of drug is found on either side of membrane. -
For an acid:
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pH = pKa + log (Acid)
(Salt)
You may also see the above as:
pH =pKw - pKb + log (base)
(salt)
Since pKw =pKa + pKb
Weak acid
Weak Base
Percent (To calculate percent of a weak acid or base that is ionized)
t>JJ ) ..J._ leO
701.0nlsea - .k\1
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Where charge =-1 if acid drug or 1 if basic drug
e
Important Concept!
If pH = Pka drug exist as 50% ionized and
50% unionized.
Notes on ionization
Ionized drugs; are water soluble and poor

absorption through stomach, BBB, and placenta, no
reabsorption across membrane and excrete faster.
Non-ionized (unionized); are lipid soluble = and
absorbed well in membrane (cell membranes are composed oflipids), have higher
reabsorption.
An acid in an acid solution will not ionize. (acid + acid =non ionized)
An acid in a basic solution will ionize (acid + base =ionized)
A base in a basic solution will riot ionize (base + base =non-ionized)
A base in an acid solution will ionize (base + acid =ionized)

50%.ofdrug is ionized Q%iis
ratio is the log
If pH - pKa =0.5, then the solution is 75% ionized! 25% unionized or 75% unionized /25%
ionized.
If pH - pKa > 1 then the solution is 99 to 100% ionized or 99 to 100% unionized.
If pH - pKa >2 then the solution is 100% ionized or unionized
/ .
Surface area (pick's law of diffusion)
.I:icks law predicts the rate of movement of molecules across barrier;

Rate of diffusion = D A x (C ]
D =Diffusion coefficient
A =Surface area of solid
C1 =Concentration near to stagnant layer
38-7
\ '
Factor Affecting solubility and Rate of Solution
Noyes-Whitney Equation
This relationship demonstrates the drug absorption is [aster from organs with large surface
areas. The rate ofdiffusion is directly proportional to the area ofthe solid, the concentration
difference between the concentration of solute in the stagnant layer at the surface of solid and
its concentration on the farthest side of the stagnant layer and diffusion coefficient. It is
inversely proportional to the length of stagnant layer. The driving force behind the movement
of the solute molecules through the stagnant layer is the difference in concentration of solute at
C
1
and its concentration at C
2
Solubility
Defined as the concentration of solute in a saturated solution under specific conditions of
temperature and pressure. It may be viewed as an equilibrium condition in which solute
molecules are leaving the solid (or undissolved phase) at the same extent as solute returning to
it.
Saturated solution: Is a state in which solute is at equilibrium with solid phase
Supersaturated Solution: Contains morc dissolve solute then it nonnally would contain at a
specific temperature if there were undissolved solute present. If upon cooling, the excess
solute fails to crystallize from the lower temperature, the solution is supersaturated.
Unsaturated solution: Contains dissolved solute in a concentration below that necessary for
complete saturation
Compendia expressions of approximate
Very soluble Less than I part
Freely soluble 1-1 0 parts
Soluble 10-30 parts .
Sparingly soluble 30-100 parts
Slightly soluble 100-1,000 parts
Very slightly soluble 1,000-10,000 parts
~ Types of Solvents
Polar solvent's
These consist of strongly alar molecules having high dielectric constants, e.g., water, and
~ e h y l alcohol, eth ohol.
Semi polar solvents
These are strongly dipolar molecules, but which do not [ann hydrogen bonds. Examples are
ketones and certain alcohols. They may induce a degree of polarity in nonpolar solvent
molecules.
Nonpolar solvents
These solvents have a small or no dipolar character. Theses include hydrocarbons, fixed oils,
and mineral oil. They have a low dielectric conslant and possess little tendency to reduce the
attractive forces between ions of strong and weak electrolytes.
Biophannaceutics
C
2
= Concentration of solute to other side ofstagnant layer
L = The length afthe slagnanllayer
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Biopharmaceutics
A thin layer of solvent, which behaves as an integral part of the particle and is referred to as the
diffusion layer, CI-C
2
, surrounds a particle of solute dispersed in a solvent medium. The
diffusion layer remains a part of the solute particle regardles's of extent of agitation of the bulk
solution. The rate ofthe solute is expressed by the Noyes-Whiteney equation:
Dc/dt == KA (C\-C
2
) ,
Where dc/dt is the change in concentration of solute in solution with respect to time.
Effect of Temperature
Solubility of a solid in a liquid is dependent on the temperature. If heat is absorbed in the
solution process; solubility of solute will increase with increase in temperature.
Effect of electrolytes on the solubility of non electrolytes
salting out and salting in; The addition of a salt may either increase or decrease the solubility
of nonelectrolyte. When the solubility is decreased, the effect is referred to ,as "salting out".
When the solubility is increased, it is known as "salling in".
Action potential cell membrane: Neuronal excitability depends on the influx of ions
through specific channels in membranes
Action potential across cell membrane
Membrane depolarization == Excitation = increase Na entry (influx), decrease K exit (efflux)
Membrane repolarization == Inhibition == increase cr enter in and increase K+ exit.
Agent Action Results
Botulinus toxin Blocks release of ACh from Total blockade
presynaptic terminals
Curare Competes with ACh for Decrease size of end plate potential:
receptors on motor end plate maximal doses produce paralysis of
respiratory muscles and death
Neostigrnin anticholinesterase Prolongs and enhances action of ACh at
muscle end plate
Hemicholinium Blocks reuptake of choline Depletes ACh stores from presynaptic
into presynaptic terminal terminal.
Tips
l. Oral 2. rectal 3. in the stomach and intestine but
mainly in the liver
4. first pass metabolism 5. sublingual 6. lungs
7. nasal mucosa 8. intramuscularly 9. intravenous
10 transdermal
The metabolism of the drug before the drug reaches the general circulation (4 )
Where does the first pass metabolism occur? )
Which route of administration is most likely to subject a drug to a first-pass effect? ( I )
38-9
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What sites of absorption have low first pass metabolism? ( l.,
What factors affect the bioavailability of a drug? )
What is responsible for the different phases of a two-compartment model of drug
elimination? ( f:., I
What is meant by first pass metabolism? -7 evvl-
Where does the first pass metabolism usually occur? -7
Which routes of administration is most likely to subject a drug to a first-pass effect? -7
What sites of absorption have low first pass metabolism?" -7
-
TRUE OR FALSE
After oral administration of Iron it is absorbed from duodenum by an active transportation
(TfF)
Ranking of various oral dosage (fastest -7 slowest)
Solutions (ready for absorption)
Suspensions (wetted and ready for dissolution)
Powder [(dispersed + GI fluid wet) absorbed]
Capsules (dissolve gelatine cap first then powder)
Tablets (disintegrate from tab. to smaller granulate then powder)
Sustained release tab (barrier of coating materials)
Whenever a drug is more rapidly and more completely absorbed from a solid form, the
rate-limiting factor is the dissolution process (slowest).
Write sequence of absorption for oral dosage, from higher to lower: solution> suspension
> liquid gel caps> powder>
Sustained release and immediate release fonnulations ofa drug have different of
bioavailability however the same extent.
38-10

Physical
- Physical Phar acy
I1/' C J Q-f-orv( C-. of tI <1-..eJ!(A--
Questions Alerts!
United States Pharmacopeia standards of alcohol and temperatures

J."" _-t,_ .. ..
' '.'iXr"thenitJ$ equation
Polymorphism
Sterile admixture techniques; USP chapter <797>
Ie.- f
4- 1
cJ...J.tr D State of the rrkitter
c-L i
/Gasesj ILiquids I Solids
Changes in state: Increase in temperature of a substance increases its heat content, or
enthalpy.
Melting: Solid to liquid state
Vaporization: Liquid to gaseous state
.' Volatile liquids: used as inhalation anesthetics eg: ether, halothane, and methoxyflurane
Also used in vasodilatation in acute angina nitrit;J .-
S6litl heated directly to gaseous or vapor,'state without passirlg through the,'
campBo:r:
... r L , ..,....
. Deposition: The reverse process to the sublimation, Le. direct transition from the vapor
state to the solid state. e.g., colloidal silicon dioxide and some form of sulphur.
Solids:
Polymorphism: Polymorphism is the occurrence or existence of the same substance in
different crystalline forms. Ability of a substance or drug to exist in different crystalline forms.
39-1
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Different properties such as melting points, solubility, dissolution rate, density, and stability.
Examples of polymorphism include theobroma oil or cocoa butter exhibit polymorphism.
Amorphous materials: solids and liquids - differ from crystals in that they do not possess long-
range periodicity of packing. They will therefore be isotropic. Window glass, basically Si02 is a
common example. Many plastics (perspex, PVC) are also amorphous.
Crystalline Versus Amorphous Form: The amorphous form of a compound is usually more
soluble than the crystalline form. Different polymorphic forms of the same compound may
demonstrate different physical properties including water solubility
Interfacial Phenomena
The Interface: Interfacial phenomena are attributable to the effect of the properties of
molecules located ator dose to the boundary between immiscible phases. The region of
influence is referred to as the interface. Interface may exist between a I!quid and a gas (a
foam) between two immiscible liquids (an emulsion), between a solid and liquid (a"
suspension), between solids, solid and gas, etc.
trs,aid to' .tjia lilitjiCl"'if't!1e Iifjuio;"sp'cj"'
rft
aneousfy
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over solid is not wetted by a iiquid if the latter cannot spread over the
former spontaneously. The contact angle is an important parameter reflective of the degree
of wetting of a solid by a liquid. This is the angle that a droplet of the liquid makes with the
solid surface at the point of contact. . .
liquids: With few exceptions, most organic solvents are irritating or toxic. Aromatic
hydrocarbons cause paralysis of the central nervous system and are irritating to the
: Methyl alcohol (methar'ol) :a.nd isoprop.v.' aJ.C;ptiol, ethylene glycol is
alcohol are irritating; volatile ethers pa'ralyse the central nervous system, and are irritating to
mucous membrane increases; ketones are mildly irritating; and the low weight
esters are irritating. Toxicity and irritation limit the many solvents internal use except;
Glycerine, ethyl alcohol, and propylene glycol can be employed for internal use as
pharmaceutical solvents.
/
Aliphatic hydrocarbons, ether, and glyceryl esters of aliphatic acids can be employed for
external use as pharmaceutical solvents.
Propylene glycol has been employed as a solvent for oral and parenteral solutions of drugs
such as antihistamines, barbiturates and vitamins.
Hydrogen bonding (H,_oN or H.... Q) increases the likelihood of cohesion in liquids and further
affects their physiochemical behaviour.
39-2
." .
Physical Pharmacy
Van der Waals forces impose regular arrangement among molecules.
Viscosity is an internal property of fluid that offers resistance to flow. Not, all liquids are the
same. Some are thin and flow easily. Others are thick and gooey. Honey or corn syrup will
pour more slowly than water. A liquid's resistance to flowing is.called its viscosity.
Gases: The intermolecular forces of attraction in gases are virtually non existence at room
temperature.
Pressure: Random collision of molecules with boundaries of the system is responsible for
pressure.
Ideal gas law: the interrelation among Volume (v), pressure (P) and the absolute temperature
(T) is given by ideal gas law: PV;::; nRT, where n =number of moles of gas and R=molar gas
constant (0.08205 t atm/mole deg). .py -:::.. 11 RT
Pharmaceutical gases:
Anaesthetic gases: Nitrous oxide and halothane
Compressed gases: Oxygen, nitrogen, carbon dioxide
Liquefiable gases: used as propellants in aerosol (pressurized package) products, eg:
ethylene oxide is gas used to sterilize or disinfect heat-labile objects.
i
Chemical kinetic & Drug stability
Factors that affect stability: The factors thataffect chemical stability include:
temperature, pH, moisture, air (oxygen) and light. Effect of temperatures on drug
degradation: The Arrhenius equation describes the effect of temperature on the rate of drug
degradation reaction. Heat increases rate of chemical reaction. Every WoC increase normally 2
k s -&yL'3eJ R1
.
.

.., ..: : ",\,.. .....,. '1;:
, e a]. == Boltzmar,dactor
::;,. , '." '1' ",
:: Pr;equency factor
'
logarithm
log k = log SEa/2.303 RT
Integration between two limits k
1
and k
z
at temperature T1 and T2
log K
2
/K
1
= Ea / 2.303 Rx (T
r
TdT
1
T
2
)
--..
39-3
At pH 1 to 3 (strong acidic) more susceptible to H+ (acidic)
At pH 5 to 14 (weak acid and base) more susceptible to OH- (base).
Modes of pharmaceutical degradation:
Hydrolysis, Oxidation and free radicals results in degradation and photolysis. Antioxidants
prevents free radical propagation peroxide, 'OH, and benzoyl peroxides)
Photolysis: Exposure to light wavelength less than 400 nm. Protect using amber glass or
opaque storage. Sodium nitroprusside has a shelf life only 4 hour, jf exposed to normal room
light, when protected form light, the solution is stable for at least one year.
Physical Pl1annacy
=k
o
dt
-de
Change pH effect on degradation of drugs: The magnitude of the rate of hydrolytic reaction
catalyzed by acid (H*) and base (OH"j can change with pH. Acid (H+) catalysis predominates at
lower pH, whereas base (OH") catalysis operates at higher pH
Wh.ere K
o
is zero-order rate constant [e/\]
Change in pH: Hydrolysis reactions are catalyzed by Hand OH ions, can change with pH
Acid (H) catalysis predominates at lower pH
Base (OH-J catalysis predominates at higher pH
The effect of pH on degradation kinetics, decomposition is measured by plotting the log of the
rate constant as function of pH. The point of inflection on the plot is the pH of optimum
stability. This value is useful in development of stable drug formulation.
To determine the effect of pH on degradation kinetics, decomposition is measured at several
H+ concentrations. The pH of optimum stability can be determined by plotting the logarithm
of the rate constant (k) as function of pH. The point of inflection of the plot is the pH of
optimum stability. The value is useful in the development of a stable drug formulation.
Stability, kinetics and shelf life: Most commonly zero order and first order reactions are
encountered in pharmacy_ A-v..J-i 6?<I
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'. _ "oM C-
C6'\s c.N.-t < &.
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Zero order
[Antioxidants: (
Water soluble: Ascorbic acid, sodium bisul{gte, ane:! soqium sulfite.
lipid soluble: Butylated hydroxyl anisole (BHA), butylated hydroxyl toluene (BHT), propyl
gallate, and the tocopherol (vitamin Ed
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First order
Physical Pharmacy
-dC
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Where C is concentration of intact drug remaining, t is time, (-dCldt) is
the rate at which the intact drug degrades, and k is the specific reaction
rate constant.
1< :=.
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Where Co is the initial concentration ofdrug
In natural log form:
InC=-Kt+ lnC
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Shelf life hO% or t9(l%
Buffers And Buffer Calculations
A buffer is a compound or a mixture of cO,mpounds that has the ability to resist changes- in pH
when limited amounts of acid or base are added to the solution 0 f the buffer or when the
solution is diluted with solvent.
Composition Generally, a buffer system consists of a weak acid and its salt of the weak acid,
,.. or a weak base a salt of the weak base. An example of the former is acetic acid and sodium
I acetate; and of the latter is ammonium hydroxide and ammonium chloride.
Mechanism of Action - In'the example of the acetic acetate buffer combination
the acetic acid is essentially unionized and the sodium acetate is completely ionized. When
acid is added to the buffer system, the hydronium ion reacts with acetate ion to form more
unionized acetic acid
CH
3
COOH + H30+ -------> CH3COOH + H20
B Ct>lr-5'(+ t l.-9e-e-k aCId -+
crt-- .. wu--k bWe- -f t1% clcJ..-f-
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And when base is added to the buffered solution, it will react with acetic acid to form more
acetate ion;
CHlCOOH + OH' -----> CHlCOO + H
2
0
Other Types of Systems - The combination of certain salts may function as a buffer system, as
for example, the combination of monobasic potassium phosphate and dibasic potassium
phosphate in the appropriate molar ratio. A study of the mechanism will reveal that the
buffer behaviour is essentially the same as the previous cases mentioned above.
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Hasselbalch equation.
pH =pKa + log [basel
[acid)
The above equation applies to all buffer systems involving a single proton transfer (conjugate
acid+base pair). .
6 )f a buffer system, for example, is composed of'O.l molar acetic acid and 0,1 molar sodium
~ acetate (Ka for acetic acid is 1.7S x 10-
5
); the pH of a solution will be: pKa is
pH = 4.75 + log 0.1 =4.75
0.1
pKa =-log of Ka
If the concentrations of ac'etic acid and sodium 'acetate are equimolar, the pH of the solution
will always be the same, 4.74. However, the higher the concentration of buffer. compounds,
the greater will be the buffer capacity or the greater the ability to resist change in pH.
Buffer Capacity; this is a quantitative expression of the ability of a buffer system to resist
change in pH.
~ = M
I ~ p H
where pis the buffer capacity and /) A is the addition in gnlm equivalents per litre of strong
acid (or strong base) to buffered solution to produce a pH change of Ii pH.
Colligative properties
CoHigative properties depend primarily upon the number of particles in solution. Example of
these properties include:
Lowering vapor pressure
~ > ~ _ ...... -....... ~
Increase in boiling point
39-6
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v
Physical
..P.,OiQt.'
.

vapour When a solute is added to a liquid, it will decrease the vapor
pressure of the liquid.
Increase in boiling point: The effect on the boiling point is just the opposite; that is, the
boiling point of a liquid is increased if something is dissolved in it. Boiling is the vapour
pressure of liquid not more than the atmospheric pressure.
Decrease in freezing point: When a solute or salt is added to liquid, it will decrease the
freezing point.
Osmotic pressure: Isotonic: The solute concentration is the same on both sides of the
membrane. The solutions are said to be isotonic compared to one another.
Hypotonic: The clinical significance of all this is to insure that isotonic or
solutions do not damage tissue or produce pain when administered.
Tips
0'1
Water-soluble antioxidants? -7 ViCe I I ""1 BH
Fat-soluble antioxidants? -7 V'r E, (toc.opNuuf) I
Theobroma oil and cocoa butter are? -7 1' .. o..lM rtLAI
D--'-/fYl
Arrhenius equation is used for? -7ctfrJ Jt- h .$fd;J,.!J pHtIc)L{
Watersolubleantioxidants?-7 V,t, 0 "1
Polymorphs are different in crystalline forms ofthe same drug, will differin 1M' f" X,+r1- cJ.4JA 0
USPofficialtemperatureis-7 .2.S-e.-
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transmission in the range of -7 2.9
0
- Lf Sl> M...i.JUL- 1-1.- ffl/ I W
Pycnometer is used for -7 4- luyl._{l! 7 d-
Hydrometerisusedfor-7
Boricacidis-7 MAIL vv-O'---t ''''''
Tannic acid is -7 1; h 10
Acetic acid is -7 -I.MA 4.1.L
Freonis-7
, USP (United States Pharmacopea):
Alcohol USP :>
Diluted alcohol
Rubbing alcohol -:7
i So +0" 'c. c$6 I
---
94.9% ethanol V/V
92.3% ethanol W/V
49% ethanol V/V
70% V/V absolute alcohgUdenatured)
39-7
40-1
Questions Alerts!
Purified water USP
Prepared by distillation, reverse osmosis, or ion exchange
Pharmaceutical
1 U+
_ elL
Pharmaceutical Excipients
agents,
'bacteriifl and
. Types of
Defections of glidant, antiadherent and lubricant
Water for injection USP - b u..1..k-
Prepared by distillation, or reverse osmosis
Free from pyrogen
Used as sofvent for parenteral solutions in manufacturing
Bacteriostatic water for injection USP -j .30 tv"i
not >30 ml
Contain 1 or more antimicrobial agent
Packed in singlE! or multiple use dose containers
Sterile water for injection USP -)
not> 1 liter
Sterilized and packed in single dose container of type r and II glass
limitation of total solids depends on size of the container
Sterile water for irrigation USP
-7 > I liter
Sterilized and suilably packed
It contain no antimicrobial agents or other added subSlance
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Should not-contain 10 ppm solid particle
Should have pH betWeen 5 and 7
Used in prescription arid fi!1ished manufactured product ..... I .
Not used in parenteral and ophthalmic products
Sterile purified water USP
It is purified water sterilized and packed
It does not contain antimicrobial agents
It is NOT intended for parenteral preparations
Ingredient Type
AcidifYing agent
Alkalizing agent
Adsorbent
Aerosol
propellant
Air displacement
Antifungal
Use
Used in liquid preparations to
provide medium for product
stability A1 so

d,..
Used in liquid preparation to
provide alkaline 'medium for
product stability. Also used for
acidic drug (ASA) overdo e.
An agent capable of holding
other molecule onto it surface
(adsorption) by physical or
chemical (chemsorbtion)
means.
An agent responsible for
developing the pressure within
an aerosol container and
expelling the product when
valve is opened.
An agent which is employed to
displace air in a hermetically
sealed contained to enhance
stability
Used in liquid and semi solid
Example
Acetic acid
Ammonium chloride
.:,{-

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Fumaric acid
Hydrochloric acid
Nitric acid
Ammonia solution
Ammonium carbonate
Diethanolamine
Monoethanolamine
Potassium hydroxide
Sodium borate
Sodium carbonate
Sodium hydroxide
IT'ri"etlIDbhhtiiiie+'-
.::' :.r t. '..... :.
Trolamine
.
Powdered cellulose
Activated charcoal'
Carbon dioxide
Dichlorodifluoromethane (CFC): not safe
Dichlorotetrafluoroethane (CFC): not safe
Trichloromonofluoromethane (CFC):
(HfA): safe -
m," ..!"r . J.
-
Nitrogen or inert gases (Ar, Ne, Xe, He)
Benzoic acid
40-2
40-3
preservative
preparations to prevent the 'Bulylparaben
growth of fungi. ' EthYJpara!x;o
Meifiy!j)rralien
hoplyparaben

Sodium nronionate
Antimicrobial
Used in liquid and semi solid
cWonac
-

." -.-
preservative preparations to prevent the
Benzothonium chloride
.
growth of micro organisms. Benzyl alcohol
Cetylpyridinium chloride
Chlorobutanol
Phenol
Phenylethyl alcohol
Phenylmercuric n II filM
-Thimcro",1 - I
Antioxidant An agent which inhibits
Water soluble (aqueous):
oxidation and thus is used to
As<:ofoic'acid c.. )
prevent the deterioration of
Sodium ascorbate
preparations by oxidative
Sodium bisulphite
process
Sodium formaldehyde
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Solfoxylate
Sodium metabisulfite
A l/,c
C
Hypophosphorous acid
4.s:C6 ,L od-
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Lipid soluble (non aqueous):
Ascorbyl palmitate
Butylated hydroxyanisole (BHA)
Bulyllated hydroxyloluene (BHD
Monothiglycerol
Propyl gallate
Tocoferal'lvitamin E, \
Buffering agent Used to resist change in pH Potassium metaphosphate
upon dilution or addition of Potassium phosphate Monobasic
acid or alkali. Sodium acetate
Buffers are made with Acid Sodium citrate anhydrous and dehydrate
and salt ofacid) or (base and
.
salt of base
Chelating agent A substance that fonns stable, EDTA
water soluble complex Edate disodium
(chelates) with metals. Edetic acid
Chelating agents are used in
some liquid phannaceuticals as
stabilizers to complex heavy
metals which might promote
instability. In such a case they
.
are also af!'eots.
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Phannaceutical Excipients
Colorant
Clarifying agent
Emulsifying agent
(Surfactant)

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Used to impart color to liquid
Used as filtering aid because
of adsorbent
Used to promote and maintain
the dispersion of finely
subdivided particles of a liquid
in a vehicle in which it is
immiscible. The end product
may be a liq\lid emulsion or
semisolid emulsion (eg.
Cream).
Emulsifying agents also
known as surfactahts.
FD&C
Caramel

Tartazine'
Bentonate
Acacia
Cetomacrogol
Cetyl alcohol
Anionic
',f ulo+ate ..
... . .. .. I.' ... "
Glycerl monoestearate
Sorbitan monooleate
Polyoxyethylene 50 stearate
Non ionic
TWfeIiS"'a:n'ifsJiM's' -
fit .. .I;1l .': ,I,
Cationic
0vu.M)11 .Mt-.
J
(, Benzalkonium chloride
f-=---;--:----+-:--:--:---:--:----:--;:--::;----:-----t-=::-:-:::=::::::::..:;:.:.=.::.:....=.:=.:..::..::.--------l
c: +cJ ,;: Encapsulating Used to form the shells for the Gelatin
cr agent of enclosing a drug Cellul<?se acetate phthalate (CAP)-7
r\u..t> oJ!!IL-- substance or drug fonnulation enteric coated
.s C11-=:-- -+:fi:-:o:-r_e:-as.:....e:-o.:....f.:....a_d_m.:....i_n_is:.-tr_a_ti_o_n__ :--7--<:p_lla-'s.:....ti.:....c-'iz::..::e..:...r --l
Flavorant Used to impart a pleasant Anise oil
flavor and often odor. Cinnamon oil
Cocoa
Menthol
Orange oil
Peppermint oil
Vanillin
Strawberry
Humectants
Levigating agent
Ointment base
Used to prevent the drying out
of preparation, particularly
ointments and creams due to
the agents ability to retain
moisture
A liquid used as an intervening
agent to reduce the particle
size of drug powder by
grinding together, usually in
mortal.
The semisolid vehicle into
which drug substance may be
Glycerin
Propylene glycol
Sorbitol
Mineral oil
Glycerin
Water soluble base:
ointment
40-4
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incorporated in preparing
Rose water ointment
""I-,k
medicated ointment.
0,
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-
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Lipid soluble

I'e.r.,.
'-""" ......
Lanolin
.
:;ell,u ""'" -!-
Propylene glycol
'f;'<Y'- I--<J Nd
"""" 't +L<- tpetrolatum
71-c.. I,
f\< J""''''
Hydrophilic petrolatum
".:J t.
'):5
White omtinent
I
jd-,L<l """
,yeliow'aintfnent

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,.,
Plasticizer
Used as a componen( of film
Diethyl phthalate
coating solutions to enhance
Glycerin
the spread of the coal over
Sorbitol
tablets, beads and Qranu\es.
Solvent
An agent used dissolve another
Solvent that are used in parenteral prep:
pharmaceutical substance. Olive oil \
13-t<LOh, "'-N
Com oil
Canola oil '7

evh
ev&M
'-'r><f Cottonseed oil)
-
r4'" 2
Peanut oil
,>,

L<eJ1PI Water for injection USP
1>'1
Sterile water for injection USP
Lh
-
0'>,

oJ
Solvent in oral prep:
Purified water
Sterile water for irrigation
Ethyl alcohol
oU-- Glycerin -
'Mineral.cHI
Oleic acid
Stiffening agent Used to'increase the thickness Cetyl alCDhol
or hardness of ointment Cetyl esters wax
Microcrystalline wax
Paraffin
Stearyl alcohol
.
White wax
Yellow wax
Surfactant Substance which absorbs to
Benzylalkonium chloride
tly\Ic..
surfaces or interfaces to reduce Nonoxynol 10
surface or interfacial tension. Oxtoxynol9
May be used as wetting afJents Polysorbate 80
d;tergents or emulsTfVlng
Sodium lauryl sulfate
-
A-t-i ,"" '--
a2cnts
Sorbitan monpalmitate
Suspending agent A viscosity increasing agent Agar
40-5
.used to reduce the rate of
sedimentation of particles
dispersed. throughout a vehicle
in which they are not soluble.
.. -; .
Pharmaceutical
ntonite
.."" :.....;
. '. ".ml os.e,str
. : '.. ....... .
Hydroxymethyl cellulose
Hydroxyproply cellulose
Hydroxypropyl methyl cellulose (HPM) .
Kaoline
ethyl cellulose
ragacanth
Vee
Tablet anti
adherent
Tablet coating
agent
Agent which prevent the
sticking of tablet formulation
in edients.
Used to coat a formed tablet
for the purpose of protecting
against drug decomposition by
atmospheric oxygen or
humidity to provide desired
release pattern for drug
substance after administration,
to mask the taste and odor or
the drug.
TI1e coating may be various
type:
Sugar coating
Film coating or enteric coating
Sugar coated is water based
and results thickened covering
around a formed tablet. Sugar
coating generally starts to
break up in stomach. A film
coated is thin cover around a
fonned tablet or bead. Unless
it is an enteric coated the film
coat will dissolve in the
stomach. An enteric-coated
tablet or bead will pass
through the stomach and break
up in the intestine. Some
coating that is water insoluble
may be used to coat tablets or
bead to slow the release of
drug as they pass through the
astrointestinal tract.
Used in direct compression
tablet fonnulation
Magnesium stearate
Talc
Silicon dioxide
Sugar coating: Liquid glucose
Sucrose
Film coating:
Hydroxethyl cellulose
Hydroxypropyl cellulose
Hydroxyproply methylcellulo
Methylcellulose (eg. Methocel)
Ethyl cellulose (eg. Ethocel)
Enteric coating: "...., ')
Cellulose acetate phthalate CCA-P../
Shellac (35% in alcohol, "phannaceutical"
glaze")
acid'
Dibasic calcium phosphate (eg. Ditab)
40-6
......
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Tablet /Capsule Used to render a capsule of a Titanium oxide
-, ,'6l.2-
apaquant tablet coating opaque. May be
,
used alone or in combination
with colorant
!?b1et pol.ishing
Used to impart an attractive Carnauba wax
sheen to coaled tablet White wax
,
Filler/diluents Filler functions: Incrcases.the bulk volume so that the final product has the
proper volume for patient handling.
Filler requirements: inert, compatible, non-hydroscopic, soluble, cheap,
compactable, and tasteful.
sorbitol,
gi:ilbi urn -carbomitc',cartdfbeil ulose
Binder Binder functions: to cause the adhesion of the powdered drug and inactive
ingredients'. bry powder added 10 the mixture prior to the wet granulation
process solution that is used in the wet granulation process
Binder types: Wet/Solution Binders: Gelatine, cellulose, cellulose derivatives,
polyvinyl pyrrolidone (PVP), starch, sucrose, and polyethylene glycol.
,Dry Binilers: Cellulose, meth"yl cellulose, polyvinyl pyrrolidone, polyethylene
1,H".cpl"am;!
Disintegrant Disintegrant Functions: To ensure that when tablets are in contact with water,
they are rapidly breaking into smaller fragments, facilitating their dissolution
Disintegnint Types: Facilitate water uptake, rupture the tablets
Disintegrant: Starch, cellulose, crosses linked polyvinyl pyrrolidone (PVP),
sodium starch glycolate, sodium cel,lulose.
To improve the flow ability of the powder or granules or both.
Example: Com starch, silica derivatives (silicon dioxide colloidal), and talc
'Lubrieant To ensure that tablet formation and ejection can occur with low friction
.swsJ:c
between the solid and the die wall. Example: Polyethylene glycols, stearic acid,
stearic acid salts rcalcium stearate, or.m.agnesium
Is used to reduce the adhesion the powder (granules) and the punch
faces and thus Drevent to the Dunches. ExamDle: talc, and starch
Sorbent Limited fluid sorbing in dry state
,
Tips
1 Anti-adherent 2. Polysorbate 3. alkalizing agent
4 lubricant stearic acid S. Water for injection USP 6. Anionic surfactant
7 improve flow ability 8. ascorbic acid 9. Sodium bisulfate
of granules
40-7
Po ftqell.{ '"1. "'--/
1M..., -::J

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Prevent sticking die wall is referred as? (1 ) odj-eJ..oN-f-:
G'idantis?l1
l
Impawe- ttow)
of water soluble are? f1 j) act' d b,oS" /l.-ttil ,
1
The type of stenle water used in parenteral preparation in manufacturing? (5) .... ,n.JKv..
In propellant action is given by? (11) <V'i)'"'-
Magnesium stearate is? (II LLJo co.. (;4- ct-= A-trf1
Tween is? (v)
!
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Pc:<f?'lfl is? ?!Jf!- I::::.tu +6 I/L
6

tDe- f5J 0 e-vJJ.od

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10 sorbic acid ester 11. hydrofluoroalkenes HFA
rl ocuJcJcLd
'Rc..h i f5 hIf:
--rha- pevJ, c(a,. 15 1ie- dJ.sr
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phO-{R.- (1}lJL r V1 CO
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41
Rheology
Questions Alerts!
Thix6tropy

Rheology'is study"df deformation '!i
Newtonian Fluids
The rate of shear (flow) should be the directly proportional to the shearing stress.
The reciprocal of viscosity is defined as fluidity.
The units of viscosity are poise. (gm/cm sec).
Rate
of
Shear
Sheari og Stress
Non-Newtonian Fluids
Non-Newtonian flow = Fluids that do not obey the Newton's law are described as 000-
Newtonian fluids.
Copyright 0 2000-2011 TIPS Inc. Unauthorized reproduction of this manual is prohibited. This manual is 41-1
being used during review sessions conducted by PhannacyPrep.
www.Pharmacyprep.com ..
Non-Newtonian flow is characterized into three types: pseudoplastic and dilatants
Rete
of
Shear
Plastic Flow
The substance that exhibits plastic flow and does not paSs through the origin; it normally
intersects the shearing stress axis
The point at which it intersects the shearing stress axis is known as yield value.
Plastic flow is also known as B' ham bodies.
Plastic flow materials: The 0 not start to flow until the applied shearing stress equals the
yield value.
At stress below the yield val ,material act as an elastic material. A A J- ..... t7 J .
b1/ /
,i'ciniilv.t 1
.... t,{!fr ." ' .
ost 0 the follow pseudo flow.
Pseudo plastic flow also known as sbear tbinning system
Flow begins at the origin
The viscosity of material decreases with increase rate ofshear 'torce.
It is thiXotropy
Examples: Suspending agents: Methylcellulose, carboxymethylcellulose (CMC) and its
derivatives. Emulsifying agents or viscosity enhancers: Sodium laurylsulfate
NC1
$hearina Stre$s
Dilatants flow
Also known as shear thickening systems, it is just opposite to pseudo plastic flow.
The increase in rate of shear force normally increases resistant to flow.
Normally suspension with high percentage of dispersed solid particles does follow dilatants
E
flow
. I ... h' h SO":l- . '11 d fl 1 d . 1
xamp es are: suspensIOn contammg Ig concentration 0 sma - e occu ate partlc es
witb thixotropy."Preducts that have
thixotropy: 'with shear stress, decrease in viscosity and increase flow ability
Pseudo plastic systems
Plastic systems
Thixotropy occurs in: Transformation of gel to solution
Thixotropy is used in formulation of suspensions dosage form where system remains gel
form upon resting and by application of shear stress this can be converted to solution form.
Copyright 2000-20 II TIPS Inc. Unauthorized reproduction ofthis-manual is prohibited. This manual is 41-2
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Anti-thixotropy systems: Products that exhibit opposite action of thixotropy are referred to as
anti-thixotropy:
.- Upon shear stress decrease flow and increase viscosity.
Increase in viscosity thereby decrease now rate.

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Example. dilatants flow
Example products: Fusidic acid ophthalmic and
Tips
1- Bentonite at high 2. is increase viscosity with 3. dilatants flow
cone increase shear stress
4. increase flow 5. decrease viscosity 6. antithixotropy
7. decrease flow 8. thixotropy increases flow and 9. Gel to solution"
decrease viscosity
10 Solution to gel
Term that referred to non force will increase difficulty in
suspension flow? (5 I dJ fo-/-a.."f- D--
Pseudoplasticflow(S, vu:,fAT
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Thixotropy systems (.1
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Anti-thixotropy systems (\Ot 1 )
Dilatants flow (2-. ) , r. _ ,
Rheopexy is? ( " ) A""'-d-J"i,>< E) f:;,.J0 } d; loJc, ..J ,:;P ---7
Agents to prepare dilatants flow ( \) B h l(fl C.ovv A, I.-
Shear thickening is? ('2..-1
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being used during review sessions conducted by PharmacyPrep.
Pharmacyprep.com Phannaceutical Dosage Forms
42
Pharmaceutical Dosage Forms
Questions Alerts!
Tablet manufacturing methods (for ASA) and problems
Soft gelatin and hard gelatin capsules
Methods of powdering (Jevigation, trituration, pulverisation)
Suppository calculatio!1
Suspending agents and flocculating agents
Solid Dosage Coarse Dispersion Solution Dosage
IMiscellaneous
I
Dosage
Tablets Pills
IInternal Use
I
Caplets
Suspensions
Inhalants
Lozenges
Gels
Aerosols
IPowder
I
Emulsions
External Use I
Lotions
Capsules
Liniments
Creams
Soft gelatine shell
-
/ Ointments
Hard shell
Vitamin drops
I
Suppository
I
'-I
Pellet/Bead
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Pharmaceutical "Dosage
I
'1o.klat
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Most commonly known dosage form is the tablet.
Direct
Wet granulation
Dry granulation
compression
Lamination
Disadvantages
Advantages
Solid Dosage Form
Picking
Sticking
Tablets
Pharmacyprep.tom
Accurate dosage
Lesser manufacturing cost
Easy to pack and ship, Easy to identifY, Easy to swallow
Appropriate for special-release fonns
Best for large-scale production
Most stable ofall oral dosage forms
Tampered proof
Some drugs are hard to compress into tablet
Some drugs may be difficult to fonnulate to have adequate
bioavailabillty
Some drugs has foul odour or disgusting taste, so they are preferably
done in [anns of capsules.
There are 3 methods of tablets preparation
...
... ...

This is a widely employed method for the production ofcompressed
tablets. This method NOT suitable for moisture sensitive drugs, like
ASA, this drug can undergo hydrolysis in moisture.
In the dry granulation method the granulation is fonned by compacting
large masses of the mixture and subsequently crushing and sizing these
pieces into smaller granules.
By this method either the active ingredient or the diluents must have
cohesive properties in order for the large masses to be fonned.
Some granular chemicals like potassium chloride and methenamine
possess free flowing as well as cohesive properties that enable them to If
compressed directly in a tablet machine without need of either wet or dry <c:::;<:::::::==
granulation. Vehicle should be compressible and have good flow. ,/-.4 .......Lt -fd
Example dried lactose, mannitol, and starch. A pl...-... ":WI" A/
.
/ CapPlOg The partial or complete separation of the top or bottom crown from the main I I
body ofthe tablet. +1-L -to-<>
Separation oftablet into two or more distinct layers. Air entrapment. Results .p6wJ.t.-t.
from: Excess powders which traps air in the tablet, deep marking or tablet ..s.Jtc
punches. Worm or Too much pressure. Moist and soft
granulation or unsuitable fonnula. &tuL
The removal oCthe surface material of tablet laid a punch. Up-IG #::;. iv.c
An adhesion of tablet material to a die. Picking and sticking results from or c:::
these problems are caused by excessive moisture or the inclusion of
substance with low melting temperature in the fonnulation.
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Pharmaceutical Dosage Fonns
. ; '. .
Mottling The uneven distribution of colour. Degradation of active ingredients can.
give rise to mottling, .
ef4aDlef.i .
... '... _.. .) '. ... ",", l- ," _'.:
Hardness .' Measures the degree of force required to break a tablet and also indicates
tensile strength oftablet. Hardness of tablet greatly effects dissolution and
disintegration.
Thickness
Friability
Measured by capillary scale (Vernier calipers)
Weight Measuring weight of tablet.
Capsules
U.s.a.- tfb'.S/Sbt
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A solid dosage fonn in which medicinal or inert substances are put inside a small gelatin shell.
Capsule shell sizes (5 to 000); 000; is the largest size of capsule, its capacity is 600 mg. The
c,ap'sQle sizy is 5 is 30 mg. Manufacturer also makes available number 10, I I, and 12 .
for veterinary use. The gelatin shell dissolved in 10 to 20 minutes after ingestion.
Capsule: comes in two types:
Soft gelatine shell manufactured in one piece with drug usually in liquid fonn inside the shell,
e.g. vitamins Aand E, Procardia (nifidepine), etc. soft shell capsule are made from
gelatine to which glycerin or some other polyol, such as sorbitol or propylene glycol has been
added as plasticizer. Spherical or ovoid capsules are sometimes called pearl or globules.
Soft gelatin capsules: Are made up of gelatin shell, glycerin or polyhydric alcohol are added to
make the shell elastic and plastic-like. It also contains preservatives to prevent microbes
groWth. Advantages ofcapsule dosage form are: good for drugs with objectionable taste or
odour and easy to swallow
,/ Hard gelatine shell: Hard shell gelatin capsules are made from the mixture of gelatin, sugar
. and water, with without suitable coloring agent. Hard gel caps contain powder and cannot fill
liquid. Sulfur dioxide is as a preservative. Capsules are made opaque with titanium
dioxide. Hard" capsule are available in variety of sizes and designated by numbers 000 to 5.
Manufacturer also makes available number 10, 11, and 12 for veterinary use.
Povvders
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I .
Comminution: The process of reducing the particle size: 3 Methods:
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Phannaccutical Dosage-Fanus
By intervention it is Ihe process of reducing a substance to a fine powder by
mean's of utilizing solvent which can evaporate easily. Used with hard
crystalline powders that do not crush or triturate easily, or gummy-type
substances.
This method is also used to reduce the particle size of insoluble materials
when ointments and suspensions. Reduces the particle size by
triturating it in a mortar or spatulating it on an ointment slab or pad with a
small amount ofa liquid in which the solid is not soluble.
The solvent should be somewhat viscous such as mineral oil or glycerin.
Ball or pebble mills, wiley mill, hammer mill fluid energy mills.
The continuous rubbing or grinding ofthe powder in a mortar with a pestle.
This method is used when working with hard, fractural powders.
Powders generally range from 0.1 to 10 micron (0. Ij..lM to 10 j..iM,
0.00 l nun) in size.
The screen size indicates the number ofopenings in the mesh screen per inch.
For example, a # 40 sieve has 40 openings pcr inch in the screen mesh.
Particles that can sift through that mesh are said to be "40 mesh" size.
Very small particles (below I posses high surface free energy that results
in absolute solubility.
Higher the mesh size, smaller the particle
Flexibility in compounding
Good chemical stability
Rapid dispersion of ingredient
Time consuming in preparing powder
The dose is inaccurate
Unsuitable for hygroscopic, deliquescent drugs and unpleasant tasting.
Advantages
Disadvantage
s
Particle size
Trituration
Pulverization
Mechanical
Comminution
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Where free-flowing, light powders are desired, the ingredients may be
brushed through a sieve. Ordinary household sifters may be used in sifting
pharmaceutical powders.
Powders may be mixed in a mortar by.gentle trituration with a pestle.
Sifting
trituration
*-
patulahon Small amounts of powder, having the same range of particle sized and
densities, may be conveniently mixed on a sheet or paper or tile with spatula.
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being used during review sessions conducted by PhannacyPrcp.
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Tumbling

dilution
When simple mixing of powders is desired without reduction in particle size.
Dissolving in small proportions. - .
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Special Powders
Hygroscopic
Del iquescent
Efflorescent
A substance that absorbs moisture from the air is termed hygroscopic.

Hygroscopic substances, which absorb moisture from the air to the extent
that they liquefy by partially, or wholly forming solution are termed
deliquescent. (i\oso'iption
Crystalline substances, which become powdery and liberate their water of
crystallization are said to be efflorescent. (Liberate H
2
0)
Effervescent salts Granules or powders consisting of sodium bicarbonate, a suitable organic
or inorganic acid, and medicinal ingredients are known as effervescent
salts. In the presence of water, the acid and base react to liberate carbon
dioxide, thereby producing effervescence. (Liberate CO
2
).
Examples of effervescent salts include Alka setzer (ASA with NaHC0
3
),
Calcitral.
Eutectic mixtures A eutectic mixture is defined as that proportion of components, which
will givethe lowest melting point. and 03ltfph0"r!"
/'1
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p
ound A 50C ,,'
o Compound B 80C ,.
Mixture 20
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SUppositories
Types of .
suppositor
ies
Rectal
Vaginal
Urethral
Solid or semi solid dosage form intended to be inserted into body orifice,
The most common method of suppository preparation is fusion Method.
Bullet-like shape 'to moves it inward when rectum contracts, 2g adult, children
smaller than adult.
Tapered shape
Rectal suppository can provide systemic medication
Ova shape and 5g. Have local absorption, but systemic absorption may occur.
Variable size, cylindrical shape, often contain polyethylene glycol (PEG), water
soluble base
Long and tapered. Has local effect.
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Pharmaceutical Dosage"Forms
Witepsol bases: (Lauric acid) 0 not exhibi olymorphism
High witepsol can be nil melting 0 to produce 34 to,44C.
Contain emulsifiers.
Criteria:
It should have a narrow or sharp melting range.
Hshould yield a clear melt just below body temperature or it dissolve or
disintegrate readily in the cavity fluid.
It should be inert and compatible with wide variety of drugs.
It should be nonirritating and non-sensitizing
Pharmacyprep.com
Supposito
ry Bases
Types of Suppository Bases
Lipid Cocoa butter USP (Theobroma oil, cocoa buner): Al34 to to
soluble produce a thin, oily liquid. It is a good base for r;clal ideal
For vaginal suppositories. -
Physical and chemical properties of suspension
Colloidal suspension; A suspension containing particles between I nm to in size.
Coarse suspension; the particle size is between I to I the suspension
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Wecobee bases (CQCOnut oil): These bases are derived from coconut oil.
The incorporation of glyceryl monostearate and propylene glycol monosterate
( them emulsifiable.
( Water Polymer of ethylene oxide and water, molecular weight range 400-6000
( soluble Polyethylene glycol (pEG) polymers e.g. carbowaxes
f Usually anhydrous, Water soluble and washable, nOll-greasy, non-occlusive
I lipid free.
( ' - cpJ.ID!i . . , Itgdll
(( . rr/I"", lower are available asdadUIt and -=- __
IS? VCtUtNJ.". .;.. -
( Preparation of suppositories:To prepare 10 suppositories, each containing 300 mg ASA are
(.' 0'" :>''/
/.. required what amount ofcacoa butter? Density factor (displacement value) of ASA is 1.1
() .\" "'" A u
\ All. Each, mold is 2 ml H-UV.'
(1 . q)V Solution: V '"
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\;' \ Y 10 suppositories x 2 ml = 20 ml M.a:1 r e,a,....",..ocJ!:::J
/ 20 ml- 2.73 ml ASA 17,27 ml ofcocoa buner JL?/'aJlrw-u "-14- a-
Suspension _ We,LA
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f,! Suspension is a two-phase system in which the internal or dispersed phase is solid external or
li continuous phase is liquid.
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Pharmaceutical Rorms
Purpose: Sustaining effect it necessitates drug dissolution prior to absorption.
Stability; drug degradation occurs more slowly with suspension compared to solution form.
It improves the taste.
Basic solubility; it provides alternative solvents.
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Factors for aD ideal suspension
Sedimentation
.""--"'"
-P2)g
9n
V = velocity of sedimentation in cmJsec
PI = density of disperse phase in g/cm
3
P
2
= density of dispersion medium in g/cm
3
R radius of the particles in cm
n viscosity of dispersion medium
g = gravity acceleration 980.7 cm/sec
2
The rate of sedimentation is indeendent of the lipophilic nature of particles.
.
Ideal Suspensions
A uniform particle size-uniformly distributes
Suspension that have no particle - particle interaction
Suspension that have no sedimentation. /1f!'
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Suspending Agent '.' . -D '"
Flocculating Agent .
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Sedimentation: The Stoke's law can express the eiationshtp oft'f1.e rate of sedimentatIOn with
various parameters.
Summary of Stokes equation: The of sedimentation of particles in a suspension can
determined by using the Stoke's eqt1ation.
Particle size: Larger particles will settle faster at the bottom of the container and too fine
particles will easily form hard cake at the bottom of the container. Larger the particle
increase in sedimentation..
Density of the vehicle: adding the following substances either alone or in combination can
increase the density of the vehicle of a suspension: polyethylene g,lycol, polyvinyl pyrolidone,
" glycerine, sorbitol, and sugar. Increase vehicle density decreases sedimentation. However,
the density oUhe dispersion medium cannot be altered thereby density of particle is changed.
!
Density ofpkticles: The settling decreases as (PI - P2) approaches zero.
Viscosity of the vehicle: The viscosity of a suspension is increased by adding the suspending
agents or viscosity enhancers. Increase in viscosity decrease in sedimentation
rate.
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Phannaceutical Dosage'Fonns
lays: Bentonite, veegum
Problems in suspension: Sedimentation, and caking
S lthetic hydrocolloids = Carbopol.
Semi synthetic hydrocolloids: Methylcellulose, sodium carboxymethylcellulose, and
carbomen.
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Floc.<.vV-"I '<t r if"""'d

....
Pair;:-
Flocculating Agents: The addition of flocculating agents to enbance .....
"dispcrsability". Flocculating agents are electrolytes. which carry an electrical charge
opposite that ofthe oel zeta potential suspeilded particles. The addition oCthe
flocculating agent, at some critical concentration, negates the surface charge on the suspended
particles and allows the formation offloccules or clusters as particles are held loosely together
by weak Van der Waals forces. The particles are linked together only loosely; they will not
cake and may be easily re-dispersed by shaking the suspension. Floccules have approximately
the same size particles; Examples of flocculating agents: Potassium stearate, potassium laurate,
acryl polymers and surfactants.
Emulsion is a two phase system consisting of at least two immiscible liquids: Internal or
discontinuous phase; The dispersed liquid, external or continuous phase; The dispersion
medium.
Emulsion is classified as five different categories:
Water in Oil (W/O): Oil is a continuous phase and water is a disperse phase, i.e., lotions and
liniments. Example: lotions and liniments.
Oil in Water (OIW): Water is a continuous phase and oil is a dispersed phase, i.e., most of
the oral emulsions to unmask the oily taste of a medication.
Microemulsion: Unlike emulsions, microemulsion is transparent with a small particle size. Il
is believed to be thermodynamically unstable. The particle size of microemulsion lies between
10 to 200 run. Il is generally used for the solubilization of the drug in pharmaceutical dosage
form.
Nanoparticles: Micro-emulsion- droplets size range 0.01 to 0.1 mm, the particle size of this
kind of emulsion is limited to nanograms. They are useful for the preparation ofglobulins'and
toxoid!>. Telanus toxoid and human immunoglobulin G
emulsion.
Multiple emulsions: Water in Oil in ware (W/OIW), Oil in Water in Oil (OIWIO). The
w/o/w emulsions are generally more preferable for preparation of various phannaceutical
Addition of viscosity enhancers to reduce sedimentation rate in the nocculatcd suspension.
Do not change volume. NO clear boundary is seen when the particles settle.
Emulsions
Suspending agents (viscosity enhancers): Natural hydrocolloids; acacia, tragacanth, alginic
acid, locust bean gum. guar gum, gelatin and cellulose.
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Phannaceutical Dosage Fonns
dosage fOnTIs. They are used to prolong the duration of action of various drugs, to localize
drug in the body and to prepare cosmetics .
Purpose of emulsion
.. Increase drug solubility
Increase drug stability
Prolonged drug action
Improve taste
Improved appearance
Stability of emulsion: Protect emulsions against the extremes ofcold and heat. Emulsions may
be adversely affected by microbial.contamination.
Emulsifying agents (surfactants): Emulsifying agents are categorized as:
Anionic agent: Sodium lauryl sulphate
Cationic agent: Benzalkonium chloride
Non ionic: Tween and Spans
Tween is -7 polysorbate
Span is -7 sorbital esters

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Problems in emulsion: can be classified into three different categories: Creaming, breaking
(cracking) and phase inversion
Creaming: It occurs due 10 flocculation of globules of tile internal phase. It is not a potential
cause of instability of emulsion, however, occurrence of creaming is a potential step towards
complete breaking of emulsion. The rate of creaming can be expressed by Stoke's law.
v l!'(Ps-Pol x g
18"
d = diameter of particle in em
'Ps = density of disperse phase
Po = density ofdispersion medium
g = gravitational force
n viscosity of medium
Breaking: Breaking generally results in separation ofthe internal and external phase. It
cannot be refonnulated.
HLB: Hydrophilic lipophilic balance measures the surfactants mixibility in water and lipids:
Classification of surfactants based on HLB values and uses. .JHp.J\
0-3----------------------- Antifoaming 6
4-6----------------------- w/o emuls;fying I4JJ 1
7-9----------------------- wetting 5pu V .\I.O? 1410
8-18---------------------- o/w emulsifying
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Mu -------------"--
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Combinations ofemulsifiers can produce morc stable emulsions than using a single emulsifier
with the same HLB number. The HLB value of a combination of emulsifiers can be calculated
as follows:
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detergent
10-18------------------- solubilizing agent
Pharmaceutical "Dosage Forms
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being use<! during review sessions conducted by -Fo/...w.-d '11 &II :.M/4 "J
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Cblorocresol and Hydroxybenzoates, both of which may cause skin
allergies
Barrier creams often contain water-repellent substances such as dimethicone
or other silicones. They give protection against irritation or repeated hydration
and is useful in the treatment of napkin rash and bedsores, etc.
Creams should be stored in cool place and supplied in well-closed containers
that prevent cyaporation and contamination of the contcnts
Eumovate, Elocom, Tridesilon Cream.
Ointments are semisolid substances that are greasy, normally anhydrous,
and insoluble in water, and intended for external use.
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Substances such as precipitated sulphur, salicylic acid, menthol and camphor,
hydrocortisone powder, hydroquinone, to mention a few, may be incorporated
into creams and/or ointment bases extemporaneously.
(0 uantily of surfa danl1)(HLB surfactanl1) ... (q ua nlily of surfa ciani 2) (HLB surfa dan! 2)
HLB '-----'---------"'---------"---"'------"-,------,------,--'-'------'-
quantity of surfactant 1+ quantity of surfactant2
Example: What is the I-ILB value ofa surfactant system composed of20 g span 20 (HJ...B =
8.6) and 5 g Tween 21 (HLB 13.3)?
(20 g)(8.6) + (5g)(13.3)
HLB = = 9.54
(20 9 + 5 g)
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Creams
Preservatives
used
Barrier
creams
Cold cream
Cream
examples
Ointments
Mechanism
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Therapeutic
use
Advantages
Disadvantage
Storage
Ointment
Preparation
Ointment bases
Pastes
The most commonly used ointment bases consist ofsoft paraffin or a
combination ofsoft paraffin with liquid paraffin and hard paraffin. Due to
their anhydrous nature ointments do not require any preservatives.
They are typically used as: Emollient: to make skin more pliable
Protective barriers: prevent contact to skin from harmful substances.
It moisturizes, morc occlusive than creams and fonning a protective film
over the skin.
The occlusive effect tends to prolong and enhance drug penetration.
They are messy to use.
They should be kept in well-closed container that prevents evaporation and
contamination in a temperature not exceeding 25C.
The material making up the container should be resistant to absorption or
diffusion of the contents.
Levigation: to reduce particle size, most commonly used method for
Pharmaceutical compounding.
Levigating agents: Levigating agents used for wet & disperse powder
Main agents: mineral oil, cottonseed oil, and caster oil
Glycerin: (propylene glycol PEG 400).
Surfactants: polysorbate 80 (Tween 80).
Not all surfactants are compatible
-.!usion metbod: used method if the base contains solid that has higher
-melting point.
Some examples ointments; ointments are generally used for treatment of
hemorrhoids. Preparations H, Anusol, Anusol HC and Anugesic.
Water and lipid soluble base: Polyethylene glycol (pEG) L I
Lipid soluble base: Lanoline Co lAce{' r
Occlusive bases: Petrolatum OCC.t (.q I ve
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Mechanism
, Therapeutic
use
Examples
Pastes are stiff preparations containing a high proportion of finely powdered
solids such as zinc oxide and starch.
They are less occlusive than ointments and can be used in subacute.lichenified.
or excoriated skin conditions. Due to the stiff nature, they can be applied
accurately to a particular lesion such as chronic eczema and psoriasis, and are
therefore useful for the local application of irritating drugs.
Anthralin OTC paste 0.025% and 0.2% for seborrhea and psoriasis
.Benzoyl for acne
being used during review sessions conducled by PhannacyPrep.
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being used during review sessions conducted by PharmacyPrcp.
Spirits
Spirits or essences are alcoholic or hydroalcoholic solutions of volatile substances prepared
usually by simple solutions or by admixture of tile ingredients (contain 50% 10 90% alcohol).
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Panoxyl, Benazagel-l 0, Honnone replacement (Androgel, Estrogel).
Topical gels: Tn;tinoin or tretinoin + c1indamycin (clindagel), tretinoin +
erythromycin gel should be stored in refrigerator and protect from light.
Gels are semisolids or solids prepared from high molecular weight polymers in
an aqueous or alcoholic base. They are easy to apply and wash ofT.
Gels are useful for promoting wound granulation (example: Actovegin Jelly),
in treatment of acne (example: Panoxyl gel) and
Scalp psoriasis (example: Synalar gel mix).
Due to their drying effect and especially the alcoholic ones,.they may cause
irritation to the skin.
Acne gel preparations: Made of synthetic polymers such as carbo vinyl and
polyoxyethylene laurel ether in hydroalcoholic liquids are used as bases for
benzoyl peroxide in the treatment of acne.
Diffusimax is a commercially prepared plUTonic gel that easily penetrates the
skin and is used as a vehicle to apply such drugs as Diclofenac sodium to ease
muscle pains.
Mechanism
Examples
Gels
Therapeutic
use
Pharmacyprep.com
Lotions
Examples
Counseling
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unbroken skin. Finely powdered drugs are suspended in a thin, base
and applied to the skin.
Therapeutic Cool skin by evaporation and should be applied frequently.
use Lotions are also used to apply drugs to the skin when only a thin layer of the
preparation is intended to be applied over a large surface area.
Shake lotions (e.g., calamine lotion) that contain insoluble powders are applied
to less acule, scabbed, and dry lesions.
In addition to cooling, they leave a deposit of inert powder on the skin surface
Benoxyl, valisone and scalp lotion, calamine lotion (Zinc oxide + Ferric oxide)
Lotions and suspensions require a 'Shake Well" label and if intended for topical
use, an "External use Only" label. A 1, , "
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Pharmaceutical Dosage Fonns
Spirits require storage in tight, light-resistant containers to prevent loss by evaporation and to
limit oxidative changes. Some of spirits are medicinal but mostly are used as flavouring
agents.
Tinctures
Tinctures are alcoholic or hydroalcoholic solutions prepared by mixing
chemical substances like iodine.
The alcohol content of the official tinctures varies fro 10% to 21
0
with
opium tincture USP; 74% to 80% with benzoin tincture . ycerin may be
added to hydroalcoholic solvent tOincrease solubility ofthe active content
and reduce precipitation during storage.
Tincture is categorized as protectant. It is used to protect and toughen skin in
the treatment of bedsores, ulcers, cracked nipples, and fissures of lips and
anus. Tinctures require storage in tight, light-resistant containers, away from
direct sunlight and excessive heat (may undergo photochemical change).
Topical
tinctures
Iodine
tincture
Benzoin
tincture
Iodine tincture, compound benzoin tincture and themerosal tincture
Iodine tincture is prepared by dissolving 2% of iodine crystals and 2.4% of
sodium iodide to an amount of alcohol equal to half the volume of tincture to
be prepared. ::r2. -r 14Cl "11- CL. -t 2-: e, )
Prepared by the maceration in alcohol 10% of benzoin and lesser amounts of
aloe, storax, and tolu balsam totalling about 24% of starting material.
Astringents
/
Common
astringents
Calamine
lotion
Locally applied solutions that precipitate protein. The protein precipitates
which fonns serve as a protective coat, allowing new tissue to regenerate
underneath. It causes constriction and reduces secretions; therefore they can
be used as astringent. These substances that stop oozing, discharge or
bleeding.
n ~ oxide: used for diaper rash treatment and hemorrhoids. Calamine
lotion used for cold sores or fever blister treatment and poison ivy.
Burrow's solution (Aluminum acetate): used for otitis external, and
dermatitis treatment.
Calamine lotion is mixture of zinc carbonate or zinc oxide colored with ferric
oxide.
Collodions .
Collodions are liquid preparations consisting of a solution of proxylin in a
Copyright :> 2000-2012 TIPS Inc. Unauthorized reproduction of this manual is prohibited. This manual is 42-13
Emollients
, Hl.ITIedants
Mechanism Humectants promote water retention due to their hygroscopic. They act by
being absorbed into the skin and attract water from atmosphere and serve as a
reservoir for the stratum corneum.
Commonly used humectants are propylene glycol and glycerin.
Unimenls
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mixture ofether and alcohol. When collodions are painted on the skin and
allowed to dry they leave a flexible film over the site ofapplication.
Collodions may be used to seal minor cuts and wounds or as a mean of
holding a dissolved drug in contact with the skin for a long lime.
Keep away from fire
Gargles are aqueous solutions, usually in concentrated fonns intended for use,
after dilution, for treatment of infections of oral cavity and throat.
A gargle does not, however, act as a protective covering to mucous membranes.
In the treatment of mucositis, try to avoid a gargle that contains a high
concentration ofalcohol as it may produce irritation.
Examples of gargles are thymol gargle, chlorbexidine gargle and dimam gargle.
Gargles may contain a drug to relieve sore throat such as Tanturn
(Bcnzydamine): commercially prepared mouthwashes or saline solution (0.9%
sodium chloride) may be used for stomatitis.
Chlorbexidine: used for stomatitis, mucositis, and gingivitis. Caution: stains
teeth after excessive use. Use chlorhexidine 30 min before or after use of
toothpaste. Chlorhexidine can interact with fluoride and can stain teeth.
Emollients are derived from animal or vegetable fats or petroleum products, used
to soften or protect internal or external body surfaces.
Emollients are fats or oils in a two-phase system (one liquid is dispersed in the
fonn of small droplets throughout another liquid).
Emollients soften the skin by forming an occlusive oil film on the stratum
corneum, thus preventing drying from evaporation from the deeper layers of skin.
Emollients are employed as protective and as agents for softening the skin and
rendering it more pliable in conditions like dry eczema, ichthyosis and psoriasis.
They also serve as vehicles for more active drugs.
Therapeutic
use
Counselling
Gargles
Therapeut
ic use
Examples
Therapeutic
use
Monitoring
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Phannaceutical Forms
'-'
Syrups
Some examples: Bcnylin OM Syrup, Chlor-Tripolon Syrup.
Counseling: Generally syrup contain sugars solutions, caution diabetic patients and recommend
syrup containing artificial sweeteners such as aspartame, in place of sugar.
Rubbingalcohol
Rubbing alcohol contains about 70% ofethyl alcohol by volume, .the remainder consisting of
water, denaturants with or without color additives and perfume oils and stabilizers. In each lOO
mL it must contain not less than 335 mg ofsucrose 9cta acetate of 1.4 mg.of denatonium
bentoatc, a bitter substances tha.t discourage accidental or abusive oral ingestion.
It is used as rubefacient externally gennicide for instruments and skin cleanser prior to
injection. This product is flammable stored in tight container far from fire.
Isopropyl rubbing alcohol: Isopropyl rubbing alcohol contains about 70% of ethyl alcohol by
volume, the remainder consistine. of water. Can be used as disinfectant
10, alcoholic and II.
Tips
12, anionic surfactant
hydroalcoholic liquid
mixtures
I. Has low accumul
4. disinteQTatinfY afYC
7. Stokes equation
Tocoferol alpha
13. disintegrating agents 14, sodium lauryl sulfate 15. Sterile Water for
iniection USP
16. small intestine>oral>mucus stratum corneum 18. capsule size 000
membranc>stomach 17,
mixing of2 subs. Leads to 20, glycerin 2l
crystall ization
19. lowering in melting point,
example includes camphor
and menthol
21,- o/wemulsion
The definition oftincture is? ( ) 10
Sodium lauryl sulphate is? (I L)
High HLB values associated with? (-:2.-4
Pharmaceutical Dosage Forms Pham13cyprep.com
What problem does not occur in suspension? (1..f)
Fick's law describes? ( L) F'e..tr cfl d<lJI;W/"'-
The rate limiting step in ophthalmic drops? ( )
Partition coefficient is described as? (S) (!) !{;..Jd h-
DO'8wi.b low llghl'"C ofdishibtttioA? ( 1&4 a(,<J)I<l1
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The most commonly used humectants is? (ol q VL--
Aluminum acetate is? (g) B cyDfJtb"l..--- eJ)<.-/ct-A
Eutectic mixture is? ( lj)
Oils used for parenteral preparations? ) L
Writel.hesequcnceofsurfaceareainGIT( $MeJ...{
The largest size of capsule is? ( (V )
The rate limiting step for the topical drugs ( 11)
Water used in parenteral(j/reparatiilis? ( I!:) <?-ftvU 1.<-
What is avoided in transdermal patch? ( )
What is an example of anionic surfactant( I" )
The tablets are disintegrated by? ( t, )
Relation of sedimentation and particle size can be explained by? (1 )
What type oftocoferol has the strongest antioxidant properties? ( \ I )
Complexation can modity which two properties in a drug? ( )
An example ofbiphasic include
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Drug Delivery Systems
Questions Alerts!
Common questions'in pharmacy exam is to ask!
Solvents in parenteral preparations like types water, and sterilization methods
Asthma devices in children: meter dose inhaler + spacer and nebulizers
Ophthalmic prep preservatives, viscosity enhancers like HPMC
fd outes 0 rug a miniS atlon
Route Site
Oral (PO, p.o.)
By mouth: Whenever possible, safest and most
convenient route
Sublingual (S.L.)
Under the tongue
When rapid effect is desired
Parenteral
Other than the gastrointestinal tract (by injection)
Intravenous Vein
Intraarterial Artery
Intracardiac Heart
Instraspinal or Spine
intrathecal
Intraosseous Bone
rntraarticular Joint
Inrasynovial Joint-fluid area
Intracutaneous or Beneath the skin
Intradennal or
Subcutaneous
Epicutaneous (topical) Skin surface
Transdermal Skin surface
conjunctival Conjunctiva
-
Intraocular Eye
Aural Ear
Intrarespiratory Lung
Rectal Rectum
R
43-1
Whenever a drug is more rapidly and more completely absorbed from a solid form, the rj.llC-
limiting factor is the dissolution process.
43-2
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Drug delivery Systems
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Vaginal
Urethral Urethra
Sublinl(Ual Under the tongue -7 fastest oral absomtion
p
Ranking of various oral dosage (fastest -+ slowest)
Solutions (ready for absorption)
Suspensions (welted and ready for dissolution)
Powder [(dispersed +GI fluid -I' wet) absorbed]
Capsules (dissolve gelatin cap first _then powder)
Tablets (disintegration from tab. to smaller granulate then --. powder)
Sustained release lab (barrier of coating materials) .
aren era prepara Ions
Parenleral These sterile, pyrogen free and particulate Croce preparations intended to be
'% CfM, chhi &
Requireme Restrictions on buffcrs, stabilizers, and antimicrobial pr:eservative; Do not use
4}.
nts coloring agents.
cw.
Sterile and pyrogen free
W'
Must meet compendia standards for particulate matter.
fOO
Must be prepared under aseptic conditions. Specific and high quality
packa.in.
Vehicles Aqueous: Sterile water for injection USP I liter), water for injection (> I
liter).
.
Non aqueous: Glycerin, polyethylene glycol (pEG), and alcohol
Must not contain paraffin or mineral oil, methanol
Fixed oils: Restrictions on fixed oils: Must meet the requirement of iodine
number and saponification number.
Iodine It repres.ents the number ofgrams of iodine absorbed, under the prescribed
number conditions, by 100g of the substance.
lodin'e number indicated the presence of number ofdouble bonds.
Saponificat It represents the number of mg of potassium hydroxide required to neutralize
ion number the free acids and saponify the esters contained in I.Og of the substance.
Saponification number indicates the number of ester functional grOUDS.
Water for
\... .
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injection
Solvents Pca nut oil, cotton seed oil, sunflower oil, olive oil, com oil, and canola.
Do not use mineral oils, and theobroma oil
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injection must not be of the probability of blockage ofa blood
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IntJapulmonarydrugs
Intrapulmonar
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delivery
devices
Components
of Aerosols
Formulation
of Aerosols
Inhalation
Therapy
Metered dose
inhalers
(MDI)
Dry powder
inhalers (DPI)
or turbuhalers
Nebulizers
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Aerosol inhalers (MDI), diskus, nebulizers, and turbuhalers
Propellants, valves, containers
Solutions, Suspensions, Emulsions
of in the lungs.
Metered dose inhalers, Powder inhalers, and Nebulizers,
Contain suspension or liquid
Suspension containing MDI should shake before-use
Safe propellant hydrofluorocarbons (HFA) or HFC
Aerosol flow rate 30 m/s or 100 km/h
Shake before use
Do not exceed prescribed dose
Good for under 5 year
known
No propellai1tiand1ho:need to_shake.
Requires patient's own inspiratory effort to form aerosol
Powder is delivered only
UsefuLin-childnm abov:e .f:ieais, teenagers' & arthritic-patients
. ... ..' ,
Can be used:()p;en rn'Outh and mouth techniqne
Turns an aqueous solution of drug into fine mist
Drug will be inhaled with normal respiration
Medication reaches lower airways more-effectively
Two types: jet & ultrasonic
Jet: Cools during operation, Small aerosol particle size, Less expensive, More
. .
nOIse
Ultrasonic: Heats up during operation, Larger aerosol particle, More
Less noise
43-3
, '
Rectal solutions or rectal suspensions (enemas)
Rectal route may be preferred over oral route in order to avoid liver by first pass.
Rectal Dosageforms
Rectal ointments: Some examples of ointments; Ointments are generally used for the
treatment of hemorrhoids. Some examples are: Preparations H, Musol, Anusol HC, and
Anugesic.
. Drug delivery Systems
Choice of inhalation therapy
Infants ----------Nebulizcr
, .
Children
< 4 years----Nebulizer
4 year-----DPVMDUSpacer
7 years------DPVMDI
Adults-----------MDUDPI
Acute-'cpisooes--' "Nebulizer,
Drug _ _ Albuterol (bronchodilator)
Surfactant. .................... Oleic acid, and propylene
Propellant. ...................... HFC (HFA)
Co-solvent. _ None
Type of output.. .............. Dry mist
Drug Miconazole
Surfactant. _.. Glycol
Propellant Propane or n-butane
Co-solvent. Isopropyl alcohol
Type of Drug output. Wetmis.
Drug Nonoxenol-9 (Contraceptive)
Surfactant. Triethanolamine
Propellant.. n-butane, and propane
Cosolvent. None
Type of output.. Stable foam
www.pllannacyprep.com
Example
compositions
Inhalation
aerosol
Vaginal foam
Topical spray
Rectal suppositories: Suppositories are topical dosage forms designed to soften when placed
/ in the rectum. They may be cylindrical or egg-shaped and are used for local action as laxative.
Suppositories should be protected from heat.
Some examples: dulcolax or glycerin, analgesic, anusol, preparation H
Anti+inflammatory effect: indomethacin or naproxen. Suppositories are also used for systemic
use when the oral route is either impossible or not desirable.
Some examples ofdrugs available for systemic use rectally antiemetics: Gravol, stemetil.
Non-steroidal anti-inflammatory agents: diclofenac (Valtaren), orudis
Analgesics: Acetaminophen and ASA.
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Enema is administered in a syringe or disposable squeeze bOUle with an applicator tip.
Some examples: Systemic anti-inflammatory effect: 5-ASA (Salofalk)
Vaginal dosageforms
Vaginal dosage fonns include tablets, creams, aerosol foams, jellies, solutions and ovules
(suppositories) and the sponge. The ovule is shaped differently from that ofa rectal
suppository-the laxative fleet enema arc larger, more oval in shape, and the base is walcr-
soluble.
Vaginal preparations: Most commercial vaginal suppositories use a base of polyethylene
glycolo/w An excellent choice of dilucnts for a compressed vaginal tablet would be lactose.
Vaginal products
Vaginal dosage fonns for contraception: Delfen Foam, the sponge ProtectAid
Some example of anti-infective: monistat, canes!en, flagystatin, douches (Massengil), Honnone
replacement (Premarin Vaginal Cream)
Metronidazole (Flagystatin): Partner should be treated same time, it is important to avoid
alcohol. Metronidazole indicated for trichomonas associated vaginitis.
Miconazole: drug ofchoice in vaginal candidiasis in pregnancy_ Cream is preferable over
suppositories and ovules. Cream effective decrease itching associated with vaginitis.
Topical Dosageforms
Four Bases are used: which are greasy to the touch (petroleum jelly)
Absorption bases, which are also greasy but allow the addition of liquid usually water or
dissolved chemicals in aqueous solution (Aquaphor, Eucerin) Water-removable bases, which
are mixtures, easily removed fonn the skin with water (Glaxal Base) and water-
soluble bases, which can be mixed with substances that will dissolve in water. (Polyethylene
glycol bases).
Opbthalmic Ointments/Solutions/Suspensions
Ophthalmic ointments are sterile ointments containing antibiotics or substances to relieve dry
eyes. Only sterile products are used in the eye. The advantage of using an ointment rather than
. a solution is that the ointment allows increased contact time in the"eye.
Ophthalmic ointments are packaged in 3 or 3.5 gram tubes.
Some examples: Cetamidc, Tobra-Dex, Garamycin_
Sterile solutions and suspensions are used in the eye (ophthalmic preparations) to treat
infections, allergies, innammations and dry eyes; in the ears (otic operations) to treat infection.
Examples of ophthalmic preparations used in the eye: Sulamyd, Opticrom, Inflamase,
prednisolone, Isopto Tears.
Osmotic release: Nifedipine (Adalat), and concerta (Methylphenidate)
Coating or sustained release tablets should not be crushed or chewed
Conventional dosage [onns, drug concentration rises rapidly, peaks, and then ra)ls !Jntil the
next dose is taken
Controlled/targeted delivery
An ideal controlled release mechanism for a device is the one, which exhibits a zero order drug
release. i.e. the; release of drug is independent of time.
Liposomes
Liposomes are lyotropic liquid crystals composed mainly ofampiphillic bilayers.
Liposomes have the advantage of primarily consisting of lecithin and cholesterol, which are
materials that occur naturally in the human body. Lecithin and cholesterol are also present in
the body in large amounts, and thus demand good bioacceptability.
Drug Systems www.pharmacyprep.com
Technological methods
Drug can be embedded in slowly eroding matrix, e.g., SLOW-K (KCI in a wax matrix),
SLOW-Fe etc.
Two-layered or tablets for sustained release.
Drug embedded in inert plastic matrix, e.g., Gradumet
Drug complexes with ion exchange resins, e.g., Pennkinetic systems
Floating capsules or tablets, e.g. slow release diazepam (Valrelease), a hydrodynamically
balanced (HBS) drug delivery system.
Controlled delivery systems
Advantages of controlled delivery systems: Maintenance ofoptimum therapeutic drug
concentration in the blood or in a cell predictable and reproducible release rates for extended
periods of time enhancement of activity duration for short halflife drugs the elimination of side
effects, frequent dosing, waste of drug, optimized therapy better patient compliance.
Drug may be coated on small inert beads of sugar & starch. Some beads can then be coated
with lipids to delay release. Beads with different coating thickness can then be combined in a
capsule to achieve sustained release, e.g., the Spansule technology (Contac, Dexedrine).
Ophthalmic drops:
Voltaren: Cause stinging and burning, and blurred vision.
Ketorolac: Cause stinging and burning
Trifluridine: Store in refrigerator
Pilocarpine: cause miosis
Latanoprost (Xalatan): causes pigmentation, and enlargement of eyelashes.
latanoprost +Timolol (Xalacom):
Some products may be used in both the eye and the ear, such as Sofracort, (ortisporin while otic
preparations have a glycerine or propylene glycol base and cannot be used in the eye.
Examples of otic preparations: Cortisporin Otic, Garamycin Otic, Garasone .otic, Locacorten
Vioform, ans Otic Drops.
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. This-liposome's can 'entrap dI1.\gs and may be used for drug targeting, sustained release or
reduced drug toxicity.
Phospholipid can spontaneously form concentric, bilayer lipid vesicles when
dispersed in water. Can be processed into various types & sizes
delivery involves diffusion ofthe drug through the skin
Nicotine patches: Nicotine patch: volatile (may evaporate), Androderm, Estraderm, Habitrol,
Nicoderm, Nitro-Dur, and Estalis
(0 ,/Nitroglycerin patch: Use nitrate free period to reduce tolerance (apply 12 hours and 12 hours
V without patch). Can be applied on chest. Avoid applying on lower extremities.
f'\ /' Fentanyl patch: Require written prescription only, no refills, no transfers, sales record
required. Effective for 72 hours. .
Estrogen patch: Do not apply on the chest. If it falls frequently apply new patch.
Scopolamine patch: Apply behind the ear, effective for 3 days.
Oxybutinin Patch: Anticholinergic drug for the treatment of urinary incontinence
Tolterodine Patch: Anticholinergic drug.
Clonidine Patch: Centrally acting antihypertensive drugs.
mplants for drug delivery
Implantable drug delivery systems are being developed to take the place of traditional drug
delivery systems, such as pills and hypodermic injection.
Implantable systems that are currently available include Norplant and various pumps; such as
insulin pumps. The systems are designed to deliver drugs directly into the bloodstream at a
controlled rate of transmission.
1. it is rapid onset & no 2. 8 to 12 hrs 3. drugs that act directly on
first pass metabolism the bronchi & inhalation
anesthetics
4. for drugs that cause GI 5. no shaking but 6. it is the most convenient
irritation and N, and pnme to both the patient
uncooperative or and physician
unconscious patient
43-7 ...........
, .
7. hydronuoroalkane hfa 8. IV 9. the physical and
chemical characteristics
of the drug
10. the tissue mass, extent ll. it is the fastest 12. lhey provide continuous
of ionization acting method drug adminislration
and no first pass
metabolism
13. 1m 14. ophthalmic and 15. injection in joints
oarenteral
16. salbutamol, fluticasone, 17. the taste and or 18. into the spinal column
budesonide, salmeterol smell and possible
first pass
metabolism and
slow
Drug delivery Systems www.phannacyprep.com
What are the advantages oforal administration? ( ( )

What dosage fonns require sterile? (13, g, In
intra articular injections ( IS)
What propeIlant used in meter dose inhaler? ( 7 > H r-A
Nitroglycerin patch require nitrate free period for? ('2-l 'B +0 J.:,w,I,k
Meter dose inhalers that require shaking ( Jb) c...1.b , I \
Nitroglycerin spray require (' No 5 P"""':lltIlL- -"
What are the disadvantages oforal administration? ( l, I ,1 )
What is the advantage of IV drug administration? ( IJ
What are the advantages ofsublingual administrationJof a drug? ( I I )
What is meant by the intrathecal administration ora drug? ( 'vt +-0 :s;;pi
Drug distribution into different tissues depends on which fastors? ( I M4..bS, '1--
What is the most direct route ofdrug administration? ('f) i V
What factors must be considered in choosing a specific route ofadministrntion? (3)
Which provides a more rapid absorption, [M or SC administration? (\.S ) .:::l...M
What type of drugs can be given by inhalation? )
What are the advantages of rectal administration of drugs? (4 )
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Sterile Preparations
Questions Alerts'
CommOn questions in pharmacy exam is to ask!
Contaminant; the most common source-contaminants like personals.
Types of needles, syringes, vials and ampoules
Leur-lock needles are used in cytotoxic preparations
The size of needle is measured by the "gauge". The higher the gauge tinier the
needle
Cytotoxic products sterile preparations use vertical laminar-airflow hood
Sterilization methods
Dry heat sterilization
Equipment: Oven
Method: Dry heat sterilization is carried out at 240C to 250 C for 2 to 4 hrs.
Application: Glassware, fixed oils, glycerine, petrolatum, liquid petroleum (mineral oil),
paraffin, and various heat stable powders, glassware and surgical instruments.
Dry heat method of choice when dry apparatus or dry containers are required, as in the
handling of packaging of dry chemicals or non-aqueous solutions.
Advantages & disadvantages: sterilization by means of heat requires higher temperatures
and longer exposures than sterilization by stearn. Heat transwris volume ofQil
and thin layers 0' powder should used.
Steam (wet) sterilization
Equipment: Autoclave
44-1
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Metbod: In the presence QfmoiwlFe, i,croorganisms aT strayed at a lower temperature
than in dry is the;method of choIce W"en product can
Application: Solutions sealed in containers: Ampoule, vials, bulk solutions, glassware,
surgical dressing, and instruments.
Advantages: Rapid, inexpensive, effective,
ojp,twJ;nt),
senSItIve preparations. I
Filtration sterilization
Physical removal of microorganisms by adsorption on the filter medium. Used for heat
sensitive materials.
Equipment: Porcelain filters, siliceous earth filter, sintered glass filters, asbestos filters
membrane filters
i{' I Bacterial filtration' Microbial filter used in water filtralions-70.22 mm (miJli microns)
I
Application: Thermo labile solutions of low viscosity.
Advantages & Disadvantages: Depend on filter media, thermo labile solutions can be sterilized
such as hormones, proteins.
Gaseous sterilization
Equipment: Special oven, for admission of gas and humidity & hermetic.
Method: ethylene oxide
Ethylene oxide gas require 4 to 16 hours
Humidity of.less than 20% RH
Ethylene oxide-carbon dioxide, pressure 30 psi, temperature 20 to 55C.
Application: Thermo labile powder, plastic/polymers, ophthalmic preparations,
subcutaneous, vaginal inserts, plastic syringes, and tubing sets
Advantages & Disadvantages: Explosiv.e haz<qd, appropriate for solutj0!ls
Radiation sterilization . . .-
Equipment: Ultraviolet lamp (laminar airflow hood), ionizatjon (beta rays, gamma rays-
from nucleus, X-rays)
Application: Thermo labile drugs (powdered)
". Disadvantages: Highly specialized equipment required, effect of irradiation on products
and their containers.
Sterile Preparations
To make sterile preparations aseptic techniques are procedure conducted under controlled
condition to minimize the chance of contamination.
44-2
www.Pharmacyprep.com Sterile Preparations
Sterility is the freedom from bacteria and other microorganisms. must be sterile,
which is not a rel!ltive tenn; an item is either sterile or not sterile. The word "sterile" refers to
as free of living microorganism.
If the sterile formulation is a solution, it must be free of all visible particulate material.
Pyrogen free 7 Pyrogen is a chemical substance that is produced by microbial cell wall.
f'.Heatingto and d<:>uhle
Aseptic preparation area: A limited access room of area in which laminar airflow hood is
situated. Usually separated from other pharmacy high traffic areas. Special measures should be
taken to reduce airborne particles.
Laminar Flows Hoods (Biological Safety Cabinets) that used for sterile preparations
categorized as two types based on direction of airflow: Horizontal laminar"airflow hood and
vertical laminar airflow hood.
Vertical laminar airflow hood: Recommended for cytotoxic, anticancer antibiotics like
doxorubicin and microbial preparations.
Class 100 clean room: A class 100 clean room is defined as an environment that contains no
more than 100 particles per cu. Ft. of 0.5 mcm or larger size.
HEPA filter: A HEPA filter is described as a high efficiency particulate air filter. It is
employed with laminar flow for preparation of aseptic parenteral products. It has an efficiency
of removing 99.97% particles of 0.33 mcm or larger.
1. filtration and 2. dry heat 3. Vertical laminar
radifjtion air flow hood
4. ethylene oxide 5. dealkalinizing by sulfur 6. For microbial
dioxide filtration O.22mm
in sterile H
2
O
7. Distillation 8. microorganism, 9. absolute form
pyrogen & particulate
10. free from bacteria 11 Autoclave, 121C 12 heat sensitive products
atleast 30 min.
13 Rabbit test and LAL 14 pyrogen free, sterile, 15 0.22mm
test particulate free, and
isotonic
16. needle
How do you prepare type II glass, from type III glass? (5)
44-3
Filtration sterilizations (b )
Steam (wet) sterilization autoclave temperatures ( II )
Gas sterilization (4 ) e.f{..!'w..-- """,cU-
Radiation methods {Il.} 2>QC./
Pyrogen test ( 13) q- LA-L +e&',
Hormones (I ) r; 4-
Tubing's sterilization method e..""f1.'\
Proteins sterilization methods (,) St"'
Petrolatum, waxes are sterilization methods ( 2.1 cJ/:;;l-
Parenteral solutions should be: (
Sterility is? ( 4ru-1:/'-""' fJM;z,-. 1- pwJ>elJJ. t....c.A.-
Cytotoxic drug preparationssliourd be done in?
Doxorubicin is an anticancer antibiotic prepared in? (
The size of HEPA filter that is used in laminar airflow hood? ( -I \' I (!)
Parenteral preparationsshould be free from? ( , ) t 'I/J..... . yr
Pyrogen are eliminated by? ( 7. ) c;b.dn
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What part of the syringe that should not be touched? ( , , I
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44-4
www.Pharmacyprep.com Extemporaneo,:!s Pharmaceutical Prep
Extemporaneous
COR1pounding
Questions Alerts!
Ointment preps (mix drug powder into levigating agent and then mix with
ointment base by geometric dilutions)
Storage conditi.ons
USP. chapter <797>: Sterile admixture techniques} ?tapility,and sterility testing
Clean room requirements, infusion, catheter devices
Compounding vs. Manufacturing: Compounding; The prescription, mixing, assembling,
packaging, or labeling of a drug or device as a result of practitioner's prescription drug order
or for the purpose of an incident research, teaching or chemical analysis and not for sale or
dispensing.
Manufacturing; The production, preparation, propagation, conversion or processing of drug or
devices either directly or indirectly, by extraction from substances of natural origin or
independently by means of chemical or biological synthesis and includes any packaging or
repackaging of the substances or labelling or re-Iabelling of its container and promotion and
marketing of such drugs or devices.
Example 1:
Rx
Salicylic acid 2%
Lactic acid 6 ml
Flexible collodion ad 30 ml
Caution: Flexible collodion is extremely
flammable.
Tight closed container to prevent ether and
alcohol. Expiration date month
Prepare salicylic acid 5%, menthol 0.5% in white petrolatum ointment!
Provided on desk:
Salicylic acid powder
45-1
45-2
Extemporaneous Phimnaceutical Prep
This preparation is tincture iodine thus require
precaution: A rubber or plastic spatula is used
because iodine is corrosive, and can stain.
A patient is having difficulty with propranolol
tablets, what type of propranolol is used in the
above preparation to liquid propranolol?
Rx
Iodine 2%
Sodium iodide 2.7%
Alcohol q.s. 30 ml
Rx
Propranolol Hel 4 mg/mL
Disp 30ml
Sig: Iml po tid
4 X30 =120 propranolol
Available: IR propranolol and CR
propranolol
Precipitated form usually used. Scabicide, pediculocide. Keratolytic & often combined with Sal
Acid to treat etc
1 to 2% = Keratoplastic
5 to 40% = Keratolytic, used to treat warts, corns etc.
Which of the above is levigating agent? A\cM I 0"1' I,
Which of the above is have eutectic properties? C1J.Ad
j

Which of the above is mixed in the first step? <Sj"-'-t'--; c..<'I -r
Menthol crystal
White petrolatum
Isopropyl alcohol
Glycerin
Take salicylic acid and menthol grind to a fine powder, use alcohol, mineral oil, glycerine
or water as a levigating agent depending on base. Incorporate using geometric dilution
Example 2:
Example 3:
EXijJT1ple 4
Prepare sulfur 10%
Y Grind to a fine powder, II AI I A I
's- ""',.".,IL ,..., G<rl'--'1
use IPA, Mineral oil, Glycerin or . Q
water to levigate. Incorporate using geometric dilution.
. 6/ Rx When preparing the above prescription, the
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Extemporaneous Phannaceutical Prep
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Vitamin A 60,000 units-

Tween 80
Water 120 mL

Acacia
Sig: 15 mL tid
Glycerin
Alcohol
Propylene glycol
What is the final dosage form? Emulsifying agents: Hydrophilic colloids (favor
Emulsion o/w o/w)
Water is? Continuous phase

Acacia
Solvent is -7Olive oil

What emulsifying agent is used? O/W

Tragacanth
is tween
Pectin
What is tween HLB -78 to 18
What tween is -7 Polysorbate

Ca rboxymethylcellulose
Methyl cellulose
Tween 'polysorbate 80)

Which of the following are precautions Lipophylic surfactants: Spans (sorbitan monoleate
needed for the above preparation? 80)
Do not refrigerate
Shake well
For external use

No preservative added
-
Use sunscreen
Store in amber glass bottle

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Example 5:
Rx
Morphine Img/mL
Flavoured vehicle q. s. 120 mL
Sig: 5 to 20 mg p.o. q 3 to 4 hrs prn pain
For one 1 day how many mg of morphine is
needed? 6 tablets of 20 mg for 1 wk
Morphine: 120 mg
The amount of morphine needed is 120 mg?
Powdered morphine alkaloid,should be used
when compounding this prescription
The final dosage form of this prescription is?
Solution
Example 6: Eutectic Mixture: Powders may cause problems because it may liquify. One
remedy is to add an inert powder, such as magnesium oxide to separate the eutectic
materials.
Rx .'
Starch 10%
Menthol 1%
The procedures should be blended together in
a mortar, using geometric dilution
The prescription should be prepared by
45-3
1- lipid soluble ointment base 2. o to 4C 3. White petrolatum
incorporate water (hydrous)
4. lipid soluble ointment base 5. 8tolSoC 6. 15 to 25C
7. 2 to 8 c also known as cold 8. Amoxicillin 9. Azithromycin
10. Clarithromycin 11- Cotrimoxazole 12- Clindamycin
Camphor 2% dissolving the camphor in a sufficient amount
Calamine ... (ZnO) of 90% alcohol.
Ethanol q.s. ad 120 ml
This preparation should be labeled The final product is? lotion
as?
For external use
Shake well
Use tightly closed container

ExtemporaneOus Pharmaceutical"Prep
What antibiotic available chewable dosage form? ('8i iu1''''''--'L
Suspensions that be stored at room temperature ( .5' I II, ,J f.c1U 'A _ A 1 Juf)
Lanolin is? 1.1. Lipid (,,<:1":"--')'
Examples of white petrolatum is? (<1 )
What are examples are used as levigating agent1..4-3)
www.PhannacypreD.com
Rx The pharmacist should do: Reduce the" particle
Salicylic acid 3g size of the powders using a mortar and pestle
Sulfur ppt 7 g or using the pill file with a spatula.
lanolin 10 g Place on an ointment tile and levigate the
White petrolatum 10 g ingredients, using geometric dilution. Package
the ointment in an ointment jar or tube.
What are labels? For external use Lanoline is? Water soluble ointment base
only White petrolatum is? lipid soluble ointmen"t
What type of container should be bC;lse
.
used? Wide mouth jar or ointment What is levigating agent? White petrolatum
tube
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45-4
Pharmaceutical Analysis
Pharmaceutical
Questions Alerts!
Chromatography methods like HPLC, GC, TLC
Spectroscopic methods like mass spectroscopy
Bioassays like ELISA, gel electrophoresis western blot,
Chemical separation or purification techniques include: Distillation, chromatography,
extractions and centrifuge.
Chromatography is a method of separation of mixture of chemicals that relies on differences in
partitioning behaviour between a flowing mobile phase and a stationary phase to separate the
components in a mixture. The commonly used chromatographic methods of analysis include:
Gas chromatography, HPLC TLC, and paper chromatography
, , - - -----------
Chromatographyinstrumental procedures
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46-1
Gas Chr-omatograpby (CC):
Gas chromatography is a chromatographic technique that can be used to
organic compounds. Example: volatile liquids, oils and alcohols etc. 1,...,
\ IJl Mechanism: The organic compounds are separated due to differences in their partitioning
\j behaviour between the mobile gas phase and the stationary phase in the column.
GLC (Gas Liquid Chromatography) .... \
Mobile phase: Example, helium, argon, or nitrogen \-Ie ,f>vl.. J I ..,

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High-Performance Liquid Chromatography (HPLC) Or High Pressure Liquid
Chromatography
46-2
Records
chromatogram
Detector
Liquid Chromatography
Used: thennally stable compounds to separates.E'lacromolecules,
species, labile natural products, polymeric materials and high-molecular weight compounds
Diagram:
) Columns
f1 Solvent Injector and
'i0J!Mobile phase; must be degassed Pump
/ Column: 4 to 5 mm heavy wall, glass-lined metal tubing or 10 to 30 em
Detectors:
UV-VIS photometers (diode array detector)
Fluoviometric detector
Electrochemical
Refractometers (RI)
Conductivity for ion chromatography
Radiodetector
..,parameter ,that affects resolution ,
.....'-_. 'I . '. .-
MobIle phase: Nature of solvent should be compatible with substance
Solubility's of mixture in mobile phase
Concentration of mixture substance .
Stationary phase, thickness of silica gel
Column size
Pressure in HPLC
Temperature (gas and column chromatography)
pH ofsolvent
Flow rate
Parameters that do not have an effect printers
Liquid chromatography (LC) is an analytical chromatographic technique that is useful for
separating ions or molecules thaI are dissolved in a ....
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Stationary Phase: Liquid surface on solid
GSC (gas solid chromatography)
Mobile phase: gas Example: helium, argon, or nitrogen
Stationary Phase (solid)
Used: For volatile and thermally stable compounds
Components of gas chromatography;
Gas chromatography col umns known as
columns
\Aven

Detectors
TCD-7Thermal conductivity Detectors
FID-7Flame ion detectors
ECD-7Electron conductivity detectors.
Phannaceutical A.IJ.alysis
Thin Layer Chromatography (TLC):
A simple and rapid method to monitor the extent of a reaction or to check the purity of
organic compounds. The mobile phase is a solvent and the stationary phase is a solid
adsorbent on a flat support.
Mechanism: Relies on capillary action
TLC Spray Reagent
Ninhydrin is used for detection of amino acids, amines, and aminosugars.
Ehrlich's ,reagev-t is dimethyl
For detection of amines, indole derivatives
Paper Chromatography
Stationary phase
Stationary phase is cellulose paper (paper is made from cotton fibres and highly purified
about 90% alpha cellulose).
Properties of stationary phase: Highly hydroxylated polysaccharide, this has great affinity
for water and other polar solvents.
/ The tightly bound is actual stationary phase and as mobile phase passes over the
surface of paper.'
Mobile phase: The solvents used for paper chromatography analysis are similar to those
employed in other forms ofchromatography
SpectroscopicMethOds ofAnalysis
46-3
46-4
Used in structural detennination of unknow c emical structures Detect mQ]ecular weigh of
substance.
Spectroscopic methods: Instrumental methods that are used to identify chemical structure and
analysis of drugs. The following instrumental techniques are commonly used in drug analysis
and structure determination of new and unknown chemical structures.
Collection &
recorder
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magnetic acid
Samplc
!
Inlet Inlet
M""
Ion
System Source Analyze
Collection
System
Vacuum
Data
System
Handling
System
General Diagram of a mass spectrometer
I
Spectroscopic I
Mass Ultraviolet light Nuclear Magnetic
Other spectroscopy
spectroscopy spectroscopy Resonance
Infrared (IR)
(MS) (UVNis) (NMIR)
Atomic Absorption
(AA)
electron beam
J
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Ion. zed mixed ion
.. Molecules mo cules
separated
ion beam
Mass Spectroscopy (MS)
Mechanism: The basics mass spectrometry is that a charged particle passing through a
magnetic field is deflected along a circular path on a radius that is proportional to the mass to
charge ratio, mle.
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Advantage: This can detect trace amount of substances.
Blood sample analysis (alcohol i';1 blood) -7 GC-MS
Pharmacokinetics analysis ofdrug samples.
Detection of environmental samples-7GC-MS
Probably the most useful information you should be able to obtain from a MS spectrum is
the molecular weight of the sample. .
Used in detection and analysis of: Unknown chemical structures molecular weight of
substances or drugs.
Type of detectors in mass spectroscopy;
CI-MS; Chemical Ionization Mass spectroscopy
FAB-MS; Fast Atomic Bombardment Mass spectroscopy
EI-MS; Electron Impact Mass spectroscopy
Ultra VioletNisible light spectrophotometer
Wavelengths (A.) -7 190 and 800 nm
Ultraviolet radiation -7 <400
Visible light-7 400 to 700 nm
Chromophore: any group of atoms that absorbs light whether or not a color is thereby
produced.
Auxochrome = A group which extends the conjugation of a chromophore by sharing of
nonbonding electrons.
Bathochromic shift = The shift of absorption to a longer wavelength.
Hypsochromic shift = the shift of absorption to a shorter wavelength.
Hyperchromic effect = An increase in absorption intensity.
Hypochromic effect =A decrease in absorption intensity.
Processes or Equipment Radiation:
Welding arcs -7 UV, visible, IR
Lasers-7 UV, visible, IR
Bactericidal lamps in ultra pure water system-7UV
Radiant heat sources; boilers, IR lamps-7IR
Infrared spectropbotometer
Infrared -7 >700 nm
Infrared light lies between the vi;ible and microwave portions of the electromagnetic
spectrum. .,
,
:. Infrared light has a range of wavelengths, just like visible light has wavelengths that range
from red light to violet.
Atomic-absorption spectroscopy
Atomic-absorption (AA) spectroscopy uses the absorption of light to measure the concentration
orgas-phase atoms. The analyte concentration is determined from the amount of absorption.
<
46-5
file law J .
the Beer-Lambert law (or Beer's law) is the linear relationship betweel1tabsorbance and
concentration ofan absorbing species.
A a (A) b c
Where
A is the measured absorbance,
a (A.) is a wavelength-dependent absorptive coefficient,
b is the path length,
c is the analyte concentration.
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CAT scan (computer assisted tomography)
Magnetic Resonance Imaging (MRl): MRJ is used to scan tumours, minor blood clots etc.
Bioand Immunoassay Methods
An assay (test) that detects antigens (Ag) or antibodies (Ab).
Even more sensitive assay (0.0001 to 0.001 Jlg/ml, 0.1 -I ng I ml).
This makes it suitable for measuring hapten-size drugs and hormones in the
blood, things you can't get in large concentrations needed for precipitation or
agglutination. -
A laboratory test that detects specific antigens or antibodies utilizing enzyme
tagged antigens or antibodies, and in the presence ofa specific substrate, it
produces a colour change that indicates a positive reaction.
The name stands for Enzyme- Linked lmmunosorhent Assay (ELISA).
It is a useful and powerful method in estimating nglml to pglml antigens (Ag)
or antibodies (Ab) in the solution, such as serum, urine and culture
supernalant.
Used for diagnosing viral infections
Gel electrophoresis is a method that separates macromolecules-either nucleic
proteins-on the basis of size. electric charge, and other physical
propedJeG- -
Electrophoresis System (pAGE), and
mIxture separations
Nuclear Magnetic Resonance Spectroscopy (Nl'vIR): NMR techniques are used to identify
unknown chemical structure.
ELISA Assays
Immunoassay
Radio
Immunoassay
Enzyme
Immunoassay
(EIA)
Gel
clectrophoresi
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Non-aqueous solvents: Acid base titration in non-aqueous solvents: Three types of solvents:
Amphiprolic, non-ionisabJe, and aprotic or inert

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46-6
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www.Phannacyprep.pom Pharmaceutical Analysis
Amphiprotic: Autoprotolysis produce both an acid and base or
such that it proquces cation and anion species. Example: H
2
0; meth"'anol,etlianol and acetic " -'
acid '
H
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0 -7 W +OR
CH
3
0H -7 CH
3
0- + W
Non-ionisable-with basio properties: No autoprotolysis, but solvent has a group that can react
with acids. No reaction bases. Only act to transport on pairs. E.g.: pyridine, ethers, benzene,
esters, ketenes, and aldehyde
Protic Upon reaction provides Wion. Example: Methanol, Acetic acid. Water etc.
Aprotic or inert There is no reaction with acids or bases, they simply provide medium in
which the sample species or titrant are'soluble (only contribute solubility).
Example: CCl
4
(Carbon tetrachloride)
Levelling effect Regardless of the type of acid and basis, the actual acid strength is actually
+ '
detennined by the strength ofH
3
0 .
Equilibrium reactions
At equilibrium hydrolytic reaction
The rate of forward reaction is equal to backward reaction
Example: In aproteolytic reaction of acetic acid with water, the rate of forward reaction
fflcreased as the hydronium ions are depleted or when acetate ions are depleted

GravimetricAnalysis
The quantitative detenrtination of a substance by precipitation followed by isolation and
weighing of the precipitate
The basic method of gravimetric analysis
A weighed sample is dissolved after which an excess ofa precipitating agent is added.
The precipitate which forms is filtered dried or ignited and weighed.
From the mass and known composition of the precipitate, the amount of the original ion can be
deterijlined.
Criteria for successful determinations
The desired substance must be completely precipitated.
In most determinations the precipitate is of such low solubility that losses from dissolution are
negligible.
An additional factor is the common ion effect; this further reduces the solubility of the
precipitate.
Example:
46-7
TIps
Solid phase extraction (SPE)
A solid sorbcnt material, typically an alkyl bonded silica, is packed into a cartridge or
imbedded in a disk and performs essentially the same function as the organic solvent in
liquid-liquid extraction.
Example.
Reverse-phase SPE employed to extract non-polar compounds, pesticides for instance, from
polar sam les such as water generally utilize a solid sorbent containin non-polar
functional groups sue as octa ecy II) or <>cryl (e
s
) nded silicas.
1. to dry wet 2. the method of ionization of 3. purification and analysis
powders, which are MS w/c results in well- of pharmaceuticals
heat sensitive established fragmentation
drugs pattern that are useful in
identification of unknown
4. Analysis and 5. protein separation 6. protein isolation
detection of volatile
chemical in samples
7. Enzyme linked 8. HPlC 9. UV. DAD, Fluorescent &
immunosorbent RI
assay
10. Gas 11. capillary action 12. amine, amino sugars and
Chromatography proteins
13. Increase in solubility 14. Decrease in solubility by 15. Detectors, printers
by addition of salt addition of salt
16. Detection of Hrv 17. Mass Spectroscopy
When Ag+ is precipitated out by addition ofer the (low) solubility of AgCI is reduced still
further by the excess of cr, which is added, pushing lhe equilibrium to the right.
Ag' AgCI (s)
Extraction Methods
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Liquid/liquid 1Y'"7:"'. }1111Y
Examples oCliquid/liquid extraction methods are fractional distillation, which functions
based on boiling points ofsolvents ' . ',rrz.cr
Mixture of two volatile liquids can be separated using fractional distillation techniques .----
Example: Ethanol in water, Hexanes in'Chloroform '
Immiscible liquids: this mixture can be separated by using separating fllnnel.
Example: Hexanes in water (Organic solvents in water)
Pharmaceutical Analysis www.Phannacyprep.com
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Phannaceutical Analysis
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. Pump is present in'what type of chromatography? (. H-flQ J
Types of detectors used in HPlC? ( () V I S'>f+.fS) I 5'
Drugs present in, blood samples can be by? (MS )
Salting in is? ( IV) sclt..-btht b Se..t.J
Saltingoutis?'( 4-
,., Mechanism of TLC is based (
Ninhydrin is used to detect? ( J I )
What are the factors that does not affect resolution in HPlC? ( dJ:fe,d-(YL,,)4.. p"tJ .
GC-MS is? ( Gre..J d. ""'ev1J
lyophilization (freezing) is used for? (
Electron impact (EI) ionization mass spectroscopy is? ( ,'dYl
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ELISA is used for? ( +t.
Western blot test for? ( tD A-- (... fl Nit- )
Gel electrophoresis separates? ( v-::J' )
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46-9
Part 3:
Social I Behavioral and
Administrative'Sciences
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www.Phannacyprep.Com Pharmacy practice and management
,
Beneficence
., CUR$
Boethics and Profess'ional
Ethics
Questions Alerts!
Beneficence = doing good
Nonmaleficence =preventing harm
Autonomy =patient right to choose (paternalism breaks autonomy) .
Veracity =honesty or telling the truth without deception. d e.hJJJi
Justice = equality or first come first service t1\f 5 kz'
This chapter provides basic understanding of ethical principles, code of ethics, professional
responsibility and liability. You will learn how to make ethical decisions. Lecture presentation
includes scenarios of ethical decisions and professional liability and legal issues.
Definitions
Beneficence = Doing good
Non maleficence =Preventing harm
Autonomy = Right of determination
Honesty =Tell the truth
Veracity =Honesty without deception
Justice =Equality with everyone
Paternalism =violating autonomy
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Beneficence =to do good or doing good. eLtJ I Y(J T I""L- -(J
The health professional should act in the best interest of the patient. Decisions made with
perception are based on what patient needed.
In other words:
Acting in the patients best interest; the best interest of patient
Current thinking is to involve patient letting the patient determine what is in their best
interest.
47-2
Pharmacists demonstrate beneficence whenever they provide critically needed prescription
drugs to their patients in emergency situations without regard to possible legal
consequences.
Autonomy
finaTdeci?jon, even if it is not in their best interest i.e. refusing
treatment, surgery, etc.
In other words: Patient's right to self-determination; to choose what will be done to them.
Non-ma"leficence
Non-maleficence; do no harm or prevent harm. Pham13cists who refuse to fill a prescription
order because of their concern for patient safety or well being observed the principle of non
maleficence.
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Euthanasia = Assisted suicide
x Paternalism
Paternalism
When one fails to respect another's autonomy, and. to the
Substitute their own belie(s, opinions'aildjudgmenl tothat ofanothei-"Claindhey acted in the'
person's best interest. .
...y A mother comes to your pharmacy for head lice medication for her 8 yr old daughter.
Honesty and Veracity:
The patient has the right to the truth medical condition, course of the disease and treatments.
Code ofethics states that: A pharmacist, "has the duty to tell the truth and to act with
conviction of conscience" Rapport is built on trust, which is based on honesty.
Veracity: Act with honesty without deception 1Vo. AAIA I-
Fidelity C Lo;rLJ -
.' In other words fidelity is the right ofa patient to have health professionals provide services that
promote patient interests rather than their own, The right of patients to have practitioners
provide services that are in the patient's best interest.
Infidelity from a prescriber couJd be: Recommending vitamins that patients don't need. Failing
to confront a doctor with an inappropriate prescription out of fear thai the doctor will direct
hislher patients elsewhere
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First come first serve; it means providing services equally.
47-3
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www.Pharmacyprep.Com
Pharmacy practice and management
There are two customers of phannacy, one customer all family members come to your
phannacy. Other customer family members go to other phannacy. A pharmacist takd NO
copayment from a customer who comes with all family members, where as customer comes as
single persons pays co-payment, What ethical principle is violated? A "" s : ::I lL6+; ce.
A phannacist refuses to dispense plan B, because of phannacist beliefs are against of using
contraception?
Professional Ethics

Requires honesty and autonomy to exist. Patients have thc right to full information of all
relevant facts and must give explicit consent before treatment.
Informed consent exists when:
All relevant information has been provided
The patient understands the information
Consent is freely given and there is no coercion
The patient is capable of understanding the information
Note: Often, practitioners rely only on the disclosure part of the list!.;.., I LA
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From the patients perspective this is "self-disclosure" and they should be the ones making this
.
.4'v...:+ In other words: 'me principle ofconfidentiality serves to assure the patient that information
) CoMc,;dtt,c#t:J; bout. th.eir health, medical condition. treatment will not be given to individuals without their
permiSSion.
Confidentiality of Patient lnformation: The pharmacist preserves the confidential ity of
information about individual patient acquired in the course of his or her professional practice,
and does not divulge this information except where authorized by the patient or required by
law.
/
Spouses: lfsomeone is asking a copy of his or her spouse's prescription infonnation, get
permission from the patient whose information is being released.
Tips
[!J Violating autonomy QJ Tell the truth
,
Right of determination
47-4
t .
47-5
Phannacy practice and management
www.Pharmacyprep.Com
4. Beneficence
5. Ethics
7. preventing harm
6.
Equality with everyone
8.
Best interest of patient
9.
deception
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Canadian Healthcare System
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Questions ."
- . C;anadian Health Act (CHA): 5 principles Comprehensiveness, Universality,
Portability, Pub'lic and Accessibility . "
.- Qrug drug. benefit and Provincial drug benefit
programs.' . "- . '. . . ." '. -", '
Federal drug benefit programs:' covers natives, inmates, refugees .and
. ... ....
RCMP
- Prpvincial drug ben,efifPrograms: seniors over"65 yf), social . '
recipients
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. This' ohapter provid.es information. about healthcare system; explore key concepts
around health care aelivery system ahlflieaItIl care professionals. This chapter is focus on
Canadian health act (CRA), the role of federal, provincial, & territorial government in health
care.
. .
I Healt,b Canada is a federal agency; it is responsjble for drug quality, safety and efficacy
;The Health Protection Brahch (HPB) or The Health protection Food, Inspectorate
:(lIPFEI) ofHealthCanada.J;egt1;lates drugs imported mto and for sale in Canada.
The health care system
The Ganadian care system is universal health care, this mean that all citizens and
immigrants will have access to health care regardless,ofthdr,abit.ity to pay. AU Canadian are
insured on equality basis and offered health in all ten provinces and three territories.
. ,
48.:r
48-2
Comprehensiveness The insurance must cover all insured services supplied by hospitals,
medical practitioners and essential services dentists. Each province detennines which services
are insured.
Portability A series ofobligations on provinces which essentially guarantee any Canadian
resident (after a maximum wait of three months upon first becoming a resident) access
anywhere in Canada on the same basis as local residents.
Canadian Healthcare SyStem
Universality
Public administration
Portability
Accessibility
Comprehensiveness
Canadian health act (eRA): Canada health act (1984) unanimously passed in parliament.,
with adherence to the 5 principles, enforced by threat of withholding funds. Extra billing is
banned as a restriction on access.
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Canadian health act (1984)-7 Five principle
UniversaJity7 All insured parties
Public administration7 Healthcare insurance is to be administered on a$
a public authority responsible to the province and subject to audit. The Canadian healthcare
delivery is decentralized and offered for provincial delivery ofcare.
The CHA covers
Medically necessary hospital services.
Medically required physicians' services.
Medically or dentally required surgical-dental services requiring a hospital for proper performance.
The coverage reflects the two-stage evolution of public health care insurance in Canada. The1959.
Hospital Insurance and Diagnostic Services Ad and the 1966 Medicare Ad respectively brought
hospital and medical insurance to the federal level.
CRA does not cover
The following services are not covered under the CHA: Services delivered by health-care
professionals other than doctors, particularly outside of hospitals (some provinces do cover
some of these services, but are not obligated to do so under the CHAI. Services in sectors
outside the hospital. These include long-term care facilities and home care. Pharmaceuticals,
rehabilitation services and dental care are also not covered when provided outside of
hospitals.
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Drug benefit program
I-Provincial drug benefit programs
2-Federal benefit programs
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Provincial Drug' Beoefit'Prog,rams covers
A;ge 9yer 65 year
Assistance (welf<rre)
Healthcare
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RCMP (Royal Canadian Mounted Police)
Non insured health benefit (NIHB) programs
The role of federal government in health care: The federal government sets and administers
national principles of healthcare system through Canada health act. Federal government gives
funds to provincial and territorial health care services through fiscal transfers. .
Delivers health care services to specific groups e.g. first nations (aboriginal), inuits. Canadian
forces and veterans, refugee claimants and penitentiary irunates and RCMP.
Provides other health related functions such as public healthlhealth promotion programs and
health research.
Role of provincial and territorial health care: As CHA principle is public administration this
means the administration and delivery of health care serviCes is the responsibility of each
province and territory. Provinces and territories fund health services with assistance from the
federal government in the fonn of transfer payments and some times equalization payments.
Some examples ofessential services that offered by provinces and territories are:
Physicians, diagnosis, and other health care services in primary clinics
Emergency services in hospitals.
Drugs coverage plans for specific groups, such as seniors, and social assistance
" Some provinces have supplementary health benefits
Levels of health care delivery systems
It can be categorized as primary, secondary and tertiary health care delivery systems
Primary care: This is first contact a person makes a with the system when a person feels the
necessity of health care. This usually occurs through the family physician, pharmacist, or nurse
at medical centres
48-3 -...-'
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Secondary care: This is specialized service from a specialist. This requires referral from
primary health care levels.
Tertiary carc: This is specialized in diagnosing and highly tcclmical care and treating
complicated or unusual health problems. This generally takes place in hospital setting where
generally diagnostic and complicated therapies can take place.
Health promotion and disease prevention
Health promotion was defined by the world health organization (WHO) "in. I?86 as the process
of enabling people to increase control over, and improve their health.
Disease prevention focuses on efforts to avoid disease and injury. Some examples of the
disease prevention include smoking cessation programs, breast screening, and Pap smear
screenmg.
Tips
l. Pharmaceuticals 2. Non essential services 3. Federal
4. Provincial or territories 5. Comprehensiveness 6. Ul)iversality
7. Portability 8. Public administration 9. Accessibility
10. Natives or aboriginals 1l. Inmates 12. Refugees
13. Veterans 14. RCMP
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What are the five Canadian health act principles? (S,t, 7/ 't,j U PPAC (:b 48
Federal Drug Benefit Program covers: { I (J ,II, 12., 1.>,17) N ath/esJ I,., mcJes, Re..trLJ3 0!s, \k.-k.c
What is not covered in CHA? ( '/2... I PhClh\Qc.e.uJ;c.o-! s 4- SeJ<""c.
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Funding for healthcare system is paid by? {-4 ) P 'PztL1V;"C.,4J
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/"J.PE-:r:>,e,.: Pe/L5011c..J :J.",?"""",JJ.., P/V>hc-h'.'1 a",cI Elec..f.ao""'G-
d Act:
48-4
www.phannacYDrep.com Canadian Phannacy Regulations
:. .
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Pharmacy Regu ations and
Administration
Questions Alerts!
categorized 'drugs(irito

Federal Drug Act (FDA) and Control Drug Substance Act (CDSA) regulates
benzodiazepine & targeted substance, and control substances.
as straight narcotics, narcotic preps, and OTC or
exempted narcotics
. .befitoin#teii;Me\abd'ta"rgeted substances: iazepine:..
.... - ..
., Cbnth}1 have 3 parts: The part 1: CNS stimulants part 2: barbiturates
part.3:anal:iol(c steroids' '. ':::.
Federal regulations
Food and Drug Act (FDA): This federal legislation controls the manufacture of all drugs in
Canada, Also, the act controls manufacturing conditions, packaging, advertising standards
and the sale of foods, drugs, cosmetics and therapeutic devices. As with all the laws in
Canada, the law exists to protect the consumer or the public.
Drugs regulated by the FDA are grouped into A to H schedules
Schedule A:. Disease which treatment may not permit to public,
Schedule B: Describe official standard
Schedule C: Radiopharmaceuticals: Drugs other than radionudides for use in preparation
of radiopharmaceuticals.
Schedule D: Allergic substances, vaccine, blood and blood __
Schedule F: Food and Prescription Drugs /11 ,-. AIeJlz. 1 ",'.
Schedule G: Controlled drugs L-l.u..t.&.fl QlA.-
Schedule H: Restricted drugs All P'1fe.5 ph011
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.National Association of Pharmacy Regulatory Authorities (NAPRA) or The Harmonized
National Drug Model: The National Association of Pharmacy Regulatory Authorities (NAPRAI is
an association comprised of mainly the provincial regulatory authorities (the registrars of each
province that has a college of pharmacy that licenses and regulates its member ....._-.....
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Benzodiazepines and Targeted substance: all benzodiazepines are included; one transfer is
allowed.
Exempted narcotics or OTC narcotics: opioid + non opioid
Tylenol # 1 (acetaminophen 300 mg+ codeine 8mg+caffeine 15 mg) (codeine .6mg/30ml)

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Canadian Pharmacy Regulations www.phannacvoreo.com
Narcotics regulations have categorized as: Narcotics or straight narcotics: opioids like
morphine, codeine, 300 mg + codeine 60 mg) etc.
Given by written Rx only. No repeats, no transfers, sales report require
Narcotic preparations or verbal narcotics: opioid + non opioid: Tylenol ttl, (acetaminophen
300mg+ codeine 15mg + caffeine 1Smg). Tylenol #3 (acetaminoPhen 300 mg +codeine 30 mg
+ Caffeine 15 mg), No repeat
The Controlled Drugs and Substances Act (CDSA): The Controlled Drugs and Substances Act,
1997, is an act sets standards for the control of narcotics, controlled drugs and targeted
substances_ It is a federal act and the strictest of all the acts that govern the pharmacy
industry.
Drugs regulated by the CDSA are grouped into 8 schedules.
Schedule I: Narcotics, opium poppy, cocaine, phenyl piperidine (pthedine)
Schedule II: Cannabis and cannabis preparations
SChedule III: Amphetamines, methylphenidate, LSD plus other listed psychoactive
.s.ubstances.
Schedule IV: Barbiturates, anorexiants, benzodiazepines, Anabolic steroids
Schedule V: Phenylpropanolamine and others
Schedule VI: Ephedrine, ergotamine, pseudoephedrine and others
Schedule VII: Cannabis that serves enforcement purposes regarding possession and
traffi>king. .
Schedule VII,I: Cannabis that serves enforcement purposes regarding possession and

Control drugs: The drugs are categorized as control drug part 1 to 3:
Part 1: CNS stimulants like amphetamines, dexamphetamine, methylphenidate: require
sales report, no transfers
Part 2: Barbiturates
Part 3: Androgens (performance enhancing drugs)
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NAPRA is incorporated under the Canada corporation act as a voluntary, not for profit
associations. Mission of NAPRA, is to evaluate the activities of the pharmaCy regulatory'
activities by:
Representing the common of the member organizations. Serving as a national
resource centre and promoting the national implementation of regulatory
programs and standards.
All provinces have similar conditions of sale.
Schedule 1-7 Require prescription ,
Schedule 11-7 Pharmacist intervention -7 t5-ei'iih'8.tHe'"'tbtin'fer."0r'"Ori"der,:thec0unter
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Schedule III -7 Pharmacist intervention -7 Over the counter, self selection,
Schedule U -7 Can be sold from any corner store
Schedule I
The Highest risk, these drugs require a prescription for sale and are provided to the public by
a pharmacist in a pharmacy. Most drugs in schedule F(FDA) and some drugs that were listed
under Schedule E. Some drugs are listed in Schedule I of the NAPRA schedules, but are not
listed under Schedule F, The Food and Drugs Act Regulations.
Schedule II
Prescription is NOT required. Requires professional from the pharmacist and
. possible referral to a physician. Need direct pharmacist supervision.
The decision to sell a Schedule II product must be made by the pharmacist. (e.g., injectable
epinephrine for anaphylactic Reactions)
The drugs are retainedin a non-patient access area (behind the counter) no opportunity for
patient self-selection and have no public access to the public.
Example:
Tylenol # 1 (Codeine 8mg + Acetaminophen 300mg + caffeine 15mg)
Nitroglycerin SL
Insulin
Epipen
Schedule III: Over the counter
The lowest risk however, may present risks to certain populations.
'. Prescription is not required. Need direct pharmacist supervision.
These drugs may be stored in a self-selection area of the pharmacy
The pharmacist should be accessible, and approachable" to assist the patient in making an
appropriate self-medication selection or to refer physician,
Pla.n B: Emergency contraception
Unscheduled Drugs:
May be sold from any corner store.
Labelling is considered sufficient to ensure safety of drug.
49-3
Tips
Institute of Safe Medication Practices Gather information about medical
incidents and develops, recommendations in Canada.
Adverse Drug Reaction Reporting (ADR reporting): New side effects and rare serious side
"effects of drugs should be reported through ADR forrnSJto .
Canadian Society of Hospital Pharmacist (CSHP)
Voluntary national association
Develop continuing education programs, residency training programs.
Canadian Pharmacy Regulations
www.phannacvprep.com
No pharmacy knowledge required.
Phannacy related professional associations in Canada
canadian Pharmacist Association (CPhA) (www.pharmacists.ca)
Voluntary national association
Identify, respond to emerging issues of importance to the profession, assisting and
acquiring new technologies, and using information.
Create educational and professional development tools.
(Ph. A publications include:
Canadian Pharmacy Journal (ePJ)
Compendium of Pharmaceutical Specialties (CPS)
Therapeutic choices (TC)
Patient selfcare (PSC)
Compendium of patient self-care products (CPS?)
E-therapeutics
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Practices Canada (ISMP)
4 Narcotics 5 Benzodiazepine & 6 Control Substances
Targeted Substance
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National Association of Pharmacy Regulatory Authority ( 2..)
Examples of pharmacy associations, where pharmacist can be a member? (J
Examples of medication incident reporting systems in Canada? (t )
Who regulates pharmacy profession in Canada? /'-of MM-
Who regulates pharmacist and its members in Canada? 14
Morphine, codeine, meperidine are regulated under (1
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Social, Behavioral,
Econornics.Asp'ects of
PharlTla,cy .Profession
Questions Alerts!
Patient behavior models toward therapy
Professionalism is described as the. competence and skill expected and required of a
professional. Professions have a formal knowledge base that.is continually upgraded and
practitioners usually require a long period of preparation and hands on training before they
become independent practitioners. To become professional a candidate must meet certain
educational standards, usually these set by regulatory bodies.
Professions are committed to the public through their code of ethics. Healthcare professions
are constantly changed with latest developmental technologies, identification of new diseases
& treatments consequently there is emphasis on adopt to change and meet the rising
expectations.
Personal attributes of professionals
Practice ethics and high moral standards
Reflection and self awareness
Responsibility/accountability of actions
Cooperative attributes of professionals
Respect for patients
Working as team
Taking social responsibility.
A report on professionalism in medicine, the CMA (2001) states that, professionalism is:
-g:t;>f.:e.th'Sf:s,
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High mO'nil;
50-1
Reporting requirement about sexually abused child: Contact child associate society (CAS)
Professional expectations: public expect professional to offer activities with responsibilities
and the best care.
Prescription scope of practice of some healthcare professions
Pharmacist
Reporting requirement about abused patients: Sexually abused adult patient -7 pharmacist
should report or give contact number of support groups or support agencies to patient.
Social, Behavioral and Administrative Sciences www.Pharmacyprep.com
Mastery of body of knowledge and skills
A high degree of autonomy .... . ,
Reporting requirements: Reporting wrong behavior of healthcare professional protect public
and reputation of healthcare system. Each regulatory body have set different requirement for
reporting by the members of the profession.
Professional boundaries
Professional boundaries are the defining lines that separate the professional relationship from
any other behavior. The professional relationship is a purposeful relationship in which the
clients healthcare needs are priority. There are warning signs, that can prompt professional. It
is health professional responsibility identifies and deal with boundary of violations if they
arise.
Some warning signs that professional boundaries are being crossed are:
Noticing sexual content in interactions with the client
Favouring one clients care at the expense of another's.
Giving/receiving gifts or continued or continued contact after discharge.
Acting and or feeling possessive about the client.
Giving special attention {treatment to this client which differs from that given to other clients.
Denying the fact that you have crossed the boundaries from professional relationship to non
professional relationship,
Here are some situations you may be expected to report:
Sexual abuse of patients
Misconduct, incapacity, incompetence
Unsafe practice
Patients centred care values:
Respect: respecting patients, wishes, concerns and strength
Human dignity: Caring for patients as whole or unique
Experts: Patient are experts of their own lives
Timelines: Needs deserve a prompt response
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Social, Behavioral and Administrative Sciences
. .
Physicians
Veterinarians
Dentists
Nurses
Dieticians
Midwife

Pharmaceutical Care Delivery System
The major pharmaceutical care activities takes place in the following systems
A. Community pharmacy
B. Hospital pharmacy
C. Long term care facilities
D. Specialty hospital units
Community Pharmacies:
Community pharmacies are considered one of the important components of the
pharmaceutical care delivery system. However, health related services are primarily
limited to dispensing medications and patient counselling.
They can be subdivided into three categories:
1. Chain-retail pharmacy services,
2. Individually owned pharmacy -16).. vcJh
3. Internet pharmacies (mail order pharmacies) - N0 D(lc, 1 . of'c. J .&
Retail pharmacy and individually owned pharmacies work in a similar fashion. However,
is bit different i.n aspect of retail pharmacy. " ne'latte!
face-to-face patient counsellmg and aTe services.'
.
Health Belief Model (HBM)
It was first proposed by Rodenstock and later modified by Becker. According to this
model, the authors have hypothesized that people generally do not engage in preventive
healthcare practices or participate in health .detection and screening programs unless they
view themselves vulnerable and/or have certain kinds of health relevant problems.
There are three categories of behavior related to healthcare, these include:
1. Health behavior
2. Illness behavior
3. Sick-role behavior
Health behavior: It is defined as any activity undertaken by an individual who believes himself
or herself to be healthy, for the purpose of preventing illness.
Weight reduction screening program
Exercise program
Stress reduction
Regular self-examination for breast or testicular cancer
Change in diet to reduce fat or cholesterol consumption
50-3
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Illness behavior: It is defines as any activity undertaken by an individual who believes he/she
may be ill.
Discussing health problems with a family member, friend or pharmacist
Making an appointment to see physician
Self testing to determine blood pressure or blood sugar level
Experimenting with OTC products
Sick-role behavior: It is defined as an activity undertaken by an individual who considers them
to be ill or who have been diagnosed by a health professional as being ill.
Following medical advice
Taking medication as prescribed
Selecting an appropriate OTe product
Staying home from work or school
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t ee....transtheocetiQal model"of W,'ilh,preco
. ........ ",,,,,,"__ ... I ......... ';- <."q\ .<'i1 .,;
terminatIon. .
Health behavior: It is defined as activity undertaken by an_ individual who believes
himself or herself to be healthy, for the purpose of preventing illness.
Professionalism is described as the competence and skill expected and required of a
professional.
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50-4
PhannacyPrep.Com _

Management
Pharrnacy Operatio
Ma,nagernent
Questions
Types of pharmacy ownership and formats of pharmacy
Financial statements like income statement and balance sheet
,". Human' resources management and delegation
Ihventory management (calculating turnover rate)
Pharmacy practice management in the,community
Pharmacy practice management in retail stores comprises several business issues, those
discussed include: terminology commonly used in pharmacy business, Starting and managing
pharmacy business, financial human resourcl'? merchandise
inventory management.
Starting ma':;aging apharmacy' business
Starting any business requires clear understanding and knowledge of the business. However,
it is clear that lay people start pharmacy business.' Like any other business, starting pharmacy
business requires; business plan, organizing, staffing, and budgeting.
Business plan
Business plan comprises: 8usineSs. structure; MarJu!t,ar.ea analysis, 8usiness products and
strategy, Positioning, Financing, Human resources, Operation and
I'
. monitoring of performance.
Types of business registration:
Sale proprietorship
Advantage-7Sole owner, low start up cost
Disadvantage-7unlimited liabilities
51-1
Collective ownership -7 Co-operative businesses
Franchises or banner pharmacy
Advantage -7 No skills, no business knowledge needed
Disadvantage -7 Franchise fee can be high.
Gorporations and- Limited Liability Companies (Inc)'7Most common business form, business
often ends with "Inc".
Advantage legal entity, several directors (several owners), and limited liabilities.
Disadvantage -7 Higher government involvement.
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Partnership
and knowledge can be shared
Rate of conflicts is high
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pharmacy, Banner pharmacy,
Chain pharmacy, Franchise pharmacy, Food store pharmacy, Mass merchandise, Specialty
pharmacy, Mail order pharmacy and central fill facilities (in hospital),
BUSINESS applied in locating community pharmacy decision
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focused on: 1
Region: broad geographical area; example: country, and provinces.
Market area analysis: Basic information about market like population, sites
consideration, tradin"g areas:
Population: Trading area: Business area, market area analysis: Population is of interesUo
business and professional practice.
Site considerations: There are scientific methods (techniques) to assess the site
location.
Trading area: Once location decisions are made regarding regional and market area, it is
necessary to select particular trading area; type of retail operation desired.
Example: outlets, supermarkets, discount stores, national departmental stores (already
established stores).
/ Site considerations: Important consideration in site selection is the relationship of cost to
pr.Qductivity. Physical characteristics of space in a bUilding under consideration should be
scrutinized. The shape of the space, its width and depth, exposed pipe and ductwork. Parking
---
S1-2
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Pharmacy Management
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is a key concern. Techniques in assessing site locations.;",The use of ratios as rule of thumb is
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fairlY commpn. Another rule of thumb deals. with convenience ani.ntlstance; Example: sales
per square feet
Financial Statements: There are three basic financial statements: a balance sheet, an income'
( .
statement and a statement of retained earnings.
Income Statement:
Income is an of sales, total sales; cost of the good sold, gross margin,
expenses,'total expenses, profit (net income), profit and loss statements I
31"'
Unit price x unit volume =Sales
Unit volume x unit cost =Cost of goods sold
Sales - cost of goods sold =gross margin or gross profit
Gross margin - expenses =Net profit
Balance sheet: Balance is a important indicator of assets and liabilities.
Balance sheet is an indicator of current assets (cash; current inventory, prepaid expenses),
total current assets (fixture, furniture), liabilities (account payable), and long-term lic1bilities'
(over one year)
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Total liabilities: Net worth = assets -liabilities.
Cash + Account receivable + Inventory + Prepaid expenses =Total Current Assets
Total current assets + Fixed assets = Total Assets
Accounts payable + Notes payable + Accrued expenses =Total current liabilities
Total Current Liabilities + long term liabilities =Total liabilities
Total liabilities + net worth (owner equity) =Total liability and net worth " L
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Retained_Earnings Statement - (!,
Retained earnings statement indicates business retained earning that includes dividend
payments (share profit to share holders) that will reduce retained earnings, and net income
that will increase retained earnings.
":f. Human Resource Management: Here is the summary of three commonly used steps in
human resources: Job analysis, position description and job description.
Job Analysis:
Job analysis is a concise and factual study of pharmacy's staffing need. The scope of each job
must be delineated, anticipated problems outlined, and hierarchy of position established.
A thorough job analysis will possess all areas of the work to be done, and alert the pharmacy
owner on functions. On long run, it will determine the responsibility of each
employee and help prevent conflict.
51-3
./
Safety and Security-7Performance report
Physiological most basic level
Maslow's theory describes that every person has five basic levels of needs
Physiological needs, Safety and Security, Social needs, Esteem Needs, self-actualization needs.
Pliiumacy PhannacyPrep.Com
A pharmacist manager maintains appropriate job description. Ensure adequate staff coverage
for pharmacy activity levels.
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Employee motivation:THE MANAGER WHO SUPERVISES, CONTROLS, AND MOTIVATES A
MANAGEMENT TEAM,
Basic principles of employee relation and motivations aspects are described by Maslow's
hierarchy:
. . ,
Position Description (Job advertisement): THE THE
COMPONENTS Of EACH POSITION. A GOOD POSITION DESCRIPTION SHOULD SE RELATIYELY
SHORT (NO MORE THAN TWO PAGES).
General description of the job includes: Nature and the scope of the position, the main areas
of responsibility. required qualification, experience, and other job related sliills.
Job description: The detailed job description should list, the entire task
accomplished, in order of importance and described in detail.
Pharmacists manager are responsible for the supervision of the activities of pharmacy and
non-pharmacist staff in their activities of pharmaceutical services. This is useful in establishing
the priorities of job functions within each position. , ';. r '
Authorizing job to others, The principle of delegation consists of three
components: Responsibility, authority, and accountability.
Responsibility: assigning a task or a project,
Authority: given certain authority to operate a business, Like hiring personnel's.
Accountability: manager or staff pharmacist is accountable for cdmpletion of task or
project.
Esteem the three levels are satisfied, employees will become interested in
addressing higher levels, through recognition of groups as leader or experts in a particular
area.
.' Social needs-7 every employee wants to become part of the group.
An employer may ask the following questions: What degree of sharing of information about
the business and it goals will be? ','
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Pharmacy Management
Self-,actualization,needs-7this is the highest level of needs, wherein"employees will strive
toward greater accomplishment and responsibility, because it ,gives them personal
satisfaction
Merchandise And Inventory Management
SKUs: stock keeping unit of each size, strength, format ,of stock items in one unit.
Individual items of inventory are referred to SKU.
UPC: Universal product code
NPN: Natural Product Number
fr.:: ,:' .. ' Provides efficient inventory control of merchandise in the
front store. This system has the ability to track inventory from the time it is received to the
time it is sold.
Ope" to buy badget system financial stdteR'lelits are used to determine botl. tile EOst,gf
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sold and gR RaRe iA'IeRtgry....
.. Each drug is identified with DIN, different strength of
,(''v-i; same drug have. different DIN, same drug with different quantity package have same DIN.
Cb'/ his is assigned by health Canada. . etu..t.:8
ABC analysis (Pareto's law): ). _..... J l w
. Category A: 20% of products stocked represent 80% of the inventory cost Fe;u.crv":r Qj4
Category B: 15%of the products represent 15% of the inventory cost
Category C: 65% of the products stocked represent 5% of the inventory cost. :-/
By closely monitoring the 20% of the items in category A, control is gained over 80% of the
inventory costs. Identify your top 20% SKUs and maximize inventory control efforts on
these. Some of the items in the 80% category of SKU should be probably not be stocked or
sold on a special order basis.
Third Party Insurance: The payment system can be classified into two different categories:
Retrospective payment and Prospective payment
Retrospective payment (reimbursement) System: In this type of payment service, payment is
generally.made after The payment depends'on
the service actually provided by the hospital. The payment depends on the service actually
.' provided by the hospital during the patient's stay. There is
keelil;.a'-patle,nt>in .the,hospitaHbr p,aymer'tJ:!ncre'i!ses7cis' 'fDQre cost i rred.
by third, party insurai'ices. '.
Prospective payment (reimbursement) system (PPS): This was introduced in 1982. A form of
payment (reimbursement) system usually pays the hospital on the basis o(DRG (Diagnostic
Related Group) services. DRG includes lists of different kinds of illnesses and a fair amount of
cost is required to such illnesses. Under this payment service, the'hospital will
reimburse a predetermined amount specific to the DRG in which the patient is classified. This
51-5
BusinessIndicatorsand Financial analysis
Co-payment: It is one type of cost sharing plan in which patient has to pay fixed amount each
time a service is provided. - . ; - ~ - -
Deductible: It is one type of cost sharing plan in which patient has to pay a specified amount
curing a specific period of time. Before benefits are paid by third party. .
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Pharmacy Management PhannacyPrep.Com
single payment will cover the entire episode of care regardless of the patient's stay in the
. .
hospital, the number of tests performed, or the number of drugs that are used.
Commercial third party insurances:
They offer a variety of services with the condition that an initial certain amount of money
should be spent by the consumer which is known as "deductible". Also, most of them do not
cover charges for certain types of services. They also collect the prepaid fixed monthly fees
from the enrolled ct,lsto.mers.. .' . . . . .
Maximum allowable cost (MAC): The maximum amount that.will be paid by a third party to a
pharmacy when the drug is available from more than one source.
Estimated acquisition cost (EAC): the third party estimate of the prices paid by a pharmacy for
a particular drug product.
Actual acquisition cost (AAe): The actual price paid by the pharmacy after all trade, volume
and cash discounts.
Average wholesale price (AWP): The published list price of a particular product.
Cash flow: a summary of cash receipts and disbursements of a business, for a defined period
of time
cash management: freeing up funds for operating purposes by minimizing assets and
maximizing liabilities, and specifically accounts payable.
,
Coinsurance': It is one type of cost sharing plan in which patient pay a specific percent of all
loss occurred.
Functions of ratios that indicates overall financial position of pharmacy:
Ratios indicating profitability
Ratio indicating efficiency
Ratio indicating liquidity and solvency
Ratio indicating financial position
Ratios indicating profitability:
Net profit to net sales (NP:NS): The normal ratio lies between 3 to 7%.
Net profit to total assets {NP:TA}: The normal acceptable ratio lies between 10 to 15%.
New profit to inventory (NP:INI: The normal acceptable ratio lies between $0.21 to $0.27.
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Phannacy Management
Net profit to net worth (NP:NW): The.ratio lies between 20 to 25%, and 15% is acceptable
for older' pharmacies and 40% is attainable for newer pharmacies.
Ratio indicating efficiency
turno.yer rate (IN: TOR): It is normally calculated by dividing the cost of goods
the average beginning and ending inventory. The inventory turnover rate should
be 4 as a minimum, with a target of 6 or higher. Theoretical number of times during a
special period, usually one year, that inventory is bought and complete sold.
Average turnover rate is = for retail pharmacy 4 min and 6 max or more, for hospitals 8 to
10 +'t.V&>1 OVl;\. J.,AtL : I 1t - Jttevu:.
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Inventory Turn Over Rate =Cost of goods sold laverage inventory capital

Or to Ie... <3 !2... .
Inventory turnoverrate = Cost of goods sold ,> D ... Lt.-t-vt--
Beginning inventory (opening stock) + End of inventory (closing stock)
2
Example: If inventory purchased two times a year, one at beginning of inventory and end rl V
of Inventory:
Net sales to networking capital (NS:NWq: The normal ratio range is:4 to B: Ratios
considered or A value below 4 iri'Hicates
or too mu'ch capitalization. .
Net sales to inventory (NS:IN): The ratio normally ranges from 6 to 9.
Net sales to net worth (NS: NW): The normal ration range is from 3 to 8. Greater than 8 is
considered under capitalization and overtrading while below 3 indicates under trading.
Net Sales to net worth =Net sales
Net worth
Account receivable collection time (AIR CT): This ratio is a direct measure of efficient credit
management. Normally, a 3D-day collection period is a reasonable target.
AIR
=
Year end account receivable
Mean credit sales per day
.' Account payable remittance time (Alp RT): This is normally calculated by dividing year end
accounts payable divided by mean credit purchase per day.
A/P= Year end account payable
Mean credit purchase per day
Ratio indicating liquidity and solvency:
51-7
"
Current ratio: The minimum standard value is 2:1.
Prescription pricing system
Acid test ratio: It is also known as quick ratio. The normal ratio is 1:1.
Liquidity normally measure's a pharmacy's ability to meet its current liabilities with little or no
interruption in the regular conduct of business.
Phanmicy Management PhannacyPrep.Com
.
SolvencY measures a pharmacy's ability to meet current liabilities with change in
the composition of current assets.
Inventory to networking capital (IN: NWq: Mean inventory is the average of the beginning
and ending inventory for the accounting period. This ratio is an indirect measure of liquidity
and solvency.
A high ratio indicates low liquidity and too much inventory. A ratio if 80% is a reasonable
target.
Ratio indicating financial position:
Total liabilities to net worth eTL: NW): It is the most direct measure of the financial position of
the pharmacy. Aratio of 50% or lower is acceptable.
Founded debt to networking capital FD: NWC): It is also expressed as a percentage. long
term liabilities are defined as liabilities extending longer than one year. The normal
acceptable value of a ratio is 20 to 25.
Fixed assets to net worth (FA: NW): This helps to identify over investment in fixed assets. A
high value indicates over investment in fixed assets while a low value indicates there is a need
for remodelling. The target value would be a 20% or less.
Dispensing Fee method = The Dispensing Fee method is the most acceptable method fo.r
pricing of prescription drugs. In this method, a fixed amount of fees (calculated on the basis
of direct, indirect and fixed cost of pharmacy services including the profit margin required) is
added to the acquisition cost of drugs.
Retail price =CD + Professional fee
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drug cost per patient per day, average pharmacy service cost per patient per day and the
required profit margin. This will make up the single price to charge a patient per day during
their stay in the hospital.
Retail pricing formulas =Retail prke" =CD:" co X"% "rilark.:lJif ,,'
51-8
,
CD =cost of drugs
Pharmacy Management
"
Marketing in pharmacy: "4 ps "of marketing management: These activities, which are under
the direct control of the business, were known as the "4 Ps" of marketing: product, place,
price, and promotion
Management use of Structure-Process-Outcome component (SPO)
Measure of SPO
Structure component-7 Examples: Facilities, equipment, and staffing, personal
qualification
Process component -7 Examples: Provider, healthcare .system etc
Outcome component -7 Examples: Mortality, morbidity, and consumer satisfaction
Tips
1. POS 2. salaries 3. income statement
4. Balance sheet 5. Turnover rate 6. 4 to 6
7. Nature and scope of 8. Market area analysis 9. Corporation
position
10 Sole proprietor 11 Partnership 12 Franchise
13 Cash 14 Account receivable 15 Furniture
16 Building
What are the forms of business structure in Canada? ('10 ,IIJ I 2-

What is banner pharmacy ownership? ( 1'2.-)
What is the most important in business location analysis? ( i )
What financial statement includes sales of prescription drugs? ( j
What financial statements include assets and liabilities? ( t,
Examples of current include? ( I \k ,
Examples of fixed assets include? (,S
What is the most expensive in pharmacy business? ( 2.. )
Cost of goods sold/average inventory capital ( 5) /
The average turnover rate for a pharmacy (0) 1
Staffing need is described as? ( 110" ct
Position description includes (1)
Point of sale system is ( I)
51-9
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Select True or False Statements
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an order is received, and an item has 'BO' means that item is out of stock
,-
at the supplier. The 'BO' signifies that the supplier will ship when the item becomes
available or it may need to be reorder).
51-10
Phannacoeconomics
52
Pharmacoeconomics
,
Questions Alerts!
of dru'gs to society
Pharmacoeconomic methodologies like cost effective analysis (CEA), cost
minimization analysis {CMAl, cost utility analysis (CUA), and cost of illness analysis
(COA).
/
Pharmacoeconomics is "the description and analysis of the costs of drug therapy or
healthcare systems to the Pharmacoeconomics research: Identifies, measures, and
compares the costs and consequences of pharmaceutical products and services.
Healthcare Outcome Research
Outcome researc;.h (OR): The study of health care interventions (treatments, such drug
therapy, surgery, pa)liative therapy etc) and healthcare quality that are evaluated to
measure the extent to which optimum desirable outcome can be
The purpose of OR is to aSsess the value of a program or therapy under study:
model: Provides framework for comprehensive evaluation of
Economic outcome: Acquisition cost associated with care, labor cost associated with .care,
side effect reactions, cost of treatment failure, hospital re-admission, cost of
emergency room, clinic visits. - - -
Clinical outcomes: length of hospital stay, side effect reactions, hospital readmission and
death. - . _._.-.-
Humanistic Outcome: Patient satisfaction, functional status of validated instruments,
quality of life assessment. - -
-'
IShoft Pdtm 3p (SF SF 36 was designed for use in clinical practice and research,
health policy evalu.ation, and general population survey
Pnarmacoeconomic Methodolo.gies: There are some scientific methods are used to evaluate
pharmacoeconomics
Cost-benefit analysis (CBA)
Cost-effectiveness analysis (CEA)
Copyright 0 2000-2012 TIPS Inc. Unauthorized reproduction orthis manual is prohibited. This manual is 52.1
( :
Quality-Adjusted Ufe Year (OAlV): The results of CUA analysis are normally expressed in terms
of quality adjusted life year gained.
QAlY: Includes both improvements in quantity of life and quality of life, QAlY is used when:
"...- . . .
Quality.of life is the only outcome. Quality and quantity of life are health outcomes. When
intervention affects both mortality and morbidity and combined unit of outcome is desired.
Cost-benefit analysis (eBA)
It is a basic tool that helps to improve the decision-making process in the healthcare program.
Cost and consequences:
The outcome is measured in dollars.
This study calculates all of the possible benefits that may acrue from the program. All
the benefits must be expressed in dollar value.
Disadvantage: (require the economic evaluation of a human life.)
Methodology Cost Outcome unit
measur
ement
Cost-benefit analysis (eBAJ Dollar Dollar
Cost-effectiveness analysis (CEA)-) Dollar Units such as blood pressure, mm Hg, blood
most commonly used in PE glucose or units of clinical effects (example:
calculations costs per year of life saved.
Cost-minimization analysis (eMA) Dollar Assumed to be equivalent in comparative
/' groups: only cost is compared, so cheap
intervention will be chosen.
Cost-utility analysis (eUAl Dollar Quality-Adjusted Ufe Year (QALYj: This is used
--
when the impact a health related quality of life
is important outcome to treat a condition
Cost of illness analysis (CIA) No comparison is made: Choose the best one
Willingness to pay (WTP) This technique is used to assess the perceived
value or benefit of the product and services
MAUT or MAUA (multi attributable Assessing utilities. Example: A hospital
utility theory or analysis) administrator may view clinical outcome 20%,
financial outcome 70% and the quality of life
10%.
The individual perspective will have a major
impact on the final decision made, based on
varying levels of priority chosen for evaluation.
Phannacoeconomics www.PhannacvPrep.com
Cost-minimization analysis (CMA)
Cost-utility analysis (eUA)
Cost-illness analysis (CIA)
Willingness to pay (WTP)
MAUT or MAUA (Multi attributable utility theory or analysis)
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It is very difficult to assign dollar values to non-financial benefits, e..g. of the.
program that may improve a patient's life.
Cost-effective analysis (CEA) (dollars -7 clinical effects
This technique is used to make a decision in order to select the most cost effective
intervention from the available alternative.
Cost and consequences
The output measure of this type of study is a health related measure rather than a
financial, example-.7 blood pressure, mm Hg, or blood glucose.
Cost-minimization analysis (CMA) (dollars -7 equal in both groups
It is defined as: when two or more interventions are examined and assumed to be
equivalent in terms of a given outcome. Cost associated with each intervention may
be examined and compared.
Example: The comparison of cost of two ca-channel blockers, which may successfully
produce similar blood pressure reduction, patterns in a selected group of patients.
Cost-utility analysis (CUA) (dollars -7 QAlY)
It is an economic toot that measures the consequences in terms of outcome of the
pr.ogram in of Cl..lL<;l--".!ity of life QAlY.
Cost and consequence's
The outcome measured in CUA is cost per QAlY (Quality Adjusted Ufe Year).
When the objective is to compare a gold standard intervention that already has the
cost per QALY, QAlYis calculated by multiplying the utility value obtained for the
specific health condition with quantity of life year spent in that specific health
condition. Comparison can be made for program and intervention.
Cost of illness analysis (COlor CIA) -7 Does not address both cost and consequences.
It is very important for evaluating new therapies.
No cost and consequences
Health Related Quality of Life (HRQOl):
QAlY focuses on all aspects of life. However, HRQOL only focuses on patient non- clinical
information such as functional status, well being, perception of health, return to work
from illness and other outcome that are effected by illness
Health Related Quality of Ufe (HRQOl): According to the WHO (World Health
Organization). health is defined as complete physical, mental and social well-being.
HRQOl normally focuses on non-clinical components of healthcare such as functional
status, well-being, and other important health- related outcomes.
HRQOl has a very large database. This database is prepared either by personal
interviews, by telephone interviews, or by postal survey.
Personal interviews, telephone interviews and postal surveys are defined standardized
questionnaires or instruments of HRQOl.
being tlsed during review sessions conducted by PhannacyPrep.
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Pharmacoecon"omics
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Multiattribute Utility Theory (MAUT):
Used in assessing utilities: This include, clinical, financial effects as well as quality of life.
Willingness To Pay (WTP):
This technique is used to assess the perceived value or benefit of a product and service.
lips
1. Units'" d,>V6J, 2. Society 3. Short Form 36
4 Cost Minimization 5. Quality Adjusted Life 6. Dollars
Analysis Years
7 cost utility analysis
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Pharmacoeconomics is the study that determine affordability of drugs to? ( 2-
Cost minimization analysis outcome is measured in? (J )
Cost effectiveness analysis outcome is measured in? (1 )
QALY is outcome of? (1)
What isSF 36?{3 )
To compare cheaper intervention, what methodology is used? ~
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being used during review sessions conducted by PhannacyPrtp.
www.Phaimacyprep.com Drug Information Resources
'Drug Information Resources
Questions
Canadian Drug References
,.". .. ..
: " TherapeutR:"ehoices, ,
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References like; ,
,Cochrane data base (' :(, , .
Martindale =foreign
USP 01 vol.l = US drugs
Motherisk program = safety of drugs in pregnancy
Peer review: Assessment of a clinical trial by experts for scientific .!!!erit, participant safety,
and ethical considerations.
Literature; It is defined as an extensive, heterogeneous collection of resources, which provide
information about drugs. Drug information sources can be categorized into primary literature,
secondary literature and tertiary literature
Primary Sources: .Journals'
Peer reviewed articles are published in scientific journals. The primary source literature provides
latest and current information.
Examples: Journal of American Medical Association Canadian Medical Association Journal
Pharmacy connection, Canadian Pharmacy Journal Clinical research data, Journal of
Informed Pharmacotherapy, Canadian Family Physician, Canadian Journal of Clinical
Pharmacology, Etc.
Gives most current information and keeps up latest development and research in
It is good resource of continuing education.
Limitation: Does not guarantee that the article is accurate, however respected journal' enhances
,.
q:edibility of contained in the artiCle.
53-1
,/Compcndium of PhannaceuticaIs Specialties (CPS)
\./"1>atient ScI f carc
VTherapeutic Choices
v"tompendium of Self care Products
VUnited States Phannacopeia DI-VoL I
v Martindale
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,I Pharmacy Reference Resources
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Secondary Sonrees Ex: ell h
Information published In s'tcondary sources obtained from various primary sources and compiled +
as abstracts and indexed into publications. Le0..t5' e.: :s
Example: Internet sources: Medline.
Current Content (Abstracts), Index Medicus (Indexex); Monthly-Biomedical research- results.
Clin-Alert (Index): abstracting service as a newsletter edition-Semi monthly (bi weekly)-Adverse
reaction.
Current content: Weekly-Clinical practice
International pharmaceutical abstracts-Monthly and quarterly--Pharmacy practice
Phannaceutical Abstracts
Online sources: MedLine
Leaflets (package inserts)
Benefits: It is an important resource for quick and selective screening of primary literature for
specific information, or article.
limitations: Each indexing service provider may provide specific list of journals, so this can limit
and thoroughness of literature search.
Tertiary Sources Ex: Text books and compendia
Information published in tertiary sources such reference book and textbooks are obtained from
primary and/or secondary sources.
Example: Martindale. Remington, Therapeutics choice, All text books, Compendium of
Pharmaceutical Speciatties (CPS)
Benefits: Provide eas and comprehensive topics;n one textbook.
limitatio: 0 recent information
Drugs available in Canada:
USP Dl-Volume I
Martindale
'Compendium of pharmaceuticals specialties (CPS)
-Discontinued products -
Brand and generic name index (green pages)
Therapeutic gUide (pink pages)
53-2
www.Pharrn.acyprep.com Drug Infonnation Resources
Product identification (pages containing photographs of the medicines)
Directory (yellow pages)
Clini-info (lilac pages)
Monographs (white pages)
Appendices (white pages at the end of the CPS)
Drugs that have peanut and soya proteins, lecithin's preps, ethanol
Drugs that can be crushed and chewed
Health Canada {Notice of Compliance - NOq
Drugs manufactured in United States:
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fij . .{:.t-'; ..
The American Drug Index (updated annually)
Drug Facts and Comparison (updated monthly and bound annually)
Drug Topics Red Book (released monthly and bound annually)
Physician Desk Reference (PDR) (updated annually)
AHFS Drug Information: American Hospital Formulary Society (supplemented quarterly and
updated annually)
Drug Manufactured in foreign countries:
Martindale: The complete drug reference
Index Nominum
USP Dictionary
USAN
For Investigational Drugs
Medline or Pubmed and Health Canada website
Martindale: The complete drug reference
Drug Facts and comparison
Unlisted drugs
FDA website: The NDA (New Drug Application) pipeline
For unknown drugs: Try to identify them by physical characteristics such as special marks,
color, shape etc. and or recommend chemical analysis: .
I USP DI volume I
The PDR
Drug facts and comparison
Manufacture
Laboratory
..
Side Effects
Compendium of pharmaceutical specialties (CPS)
USP DI Volume I: Drug Information for the Health Care Professional
53-3
)
) www.Pharmacyprep.com
Clin-Alert
Meyler's Side Effects of Drugs
AHFS Drug Information
Drug Infonnation Resources
Drug-Drug Interactions
.1}./ Drug Interaction Facts (Tatro)
Drug Interactions. In: Compendium of Pharmaceuticals and Specialties
Clin-Alert (Generali)
Hansten and Horn's Drug Interactions Analysis and Management
Drug-Drug Interactions. In: Handbook of Clinical Drug Data (Anderson)
Handbook of Adverse Drug Interactions
Drug Interactions: A Source Book of Adverse Interactions, Their Mechanisms, C(inicallmportance
th
and Management (Stockley: 6 ed. - 2003)
EDI: Evaluations of Drug Interactions
Concise Guide to Cytochrome P450 System: Drug Interaction Principles for Medical Practice
Drug-Lab Test Interactions
American Hospital Formulary Society (AHFS) Drug Information
Effects of Drugs on Clinical Laboratory Tests (Young: 5th ed. - 2000)
Drug-Laboratory Test Interferences. In: Handbook of Clinical Drug Data (Anderson)
Drug-Food Interactions
Drug Interaction Facts (Tatro)
USP-DI volume I
Reference Guide to Drug and Nutrient Interactions
Food Medications Interactions Handbook (Pronsky) ,
HIV Medication-Food Interactions Handbook (Pronsky)
Drug-Herb Interactions
Database of Natural product
Herbs: Everyday Reference for Health Professionals (CphA)
t:erb Contraindications and Drug Interactions (Brinker)
Herb-Drug Interactions Handbook (Herr)
Drug Interaction Facts: Herbal Supplements and Food
Interactions between Drugs & Natural Medicines: What the Physician and Pliarmadst Must
Know About Vitamins, Minerals, Foods and Herbs (Meletis)
Compounding or Extemporaneous prep
Remington: The Science and Practice of Pharmacy
Merck index
..
A Practical Guide To Contemporary Pharmacy Practice
53-4
Drug Information Resources
Pharmaceutical Dosage Forms and Drug Delivery Systems
Pharmaceutical Practice
The Art, Science, and Technology of Pharmaceutical Compound"ing
The Pharmaceutical Codex
Formulas For Compounding
USP-NF (United States Pharmacopea-National Formulary)
Merck index
British Pharmacopoeia Vol. 2
Contemporary Compounding Compendium
Extemporaneous Oral liquid Dosage Preparations (CSHP)
The-Ghen and Rains Physicians Guide to Pharmaceutical Compounding
Extemporaneous Formulations (Children's hospital of Philadelphia)
Pediatric Dru"g Formulations
Pocket Book of Extemporaneous Formulations
Allen's Compounded Formulations: The US Pharmacist Collection
The Art, Science, and Technology of Pharmaceutical Compounding
Trissel's Stability of Compounded Formulations (Recommended for parenteral solution
stabilites)
Minutes from manufacturer
Characteristic Of Specific Chemicals/Drugs
The Merck Index
Martindale: The Complete Drug Reference
Remington: The Science and Practice of Pharmacy
Handbook of Pharmaceutical Exipient
The Pharmaceutical Codex
The United States Pharmacopeia/ The National Formulary
Trissel's Stability of Compounded Formulations Compounding
Extemporaneous Ophthalmic Preparations
Guidelines for Preparation of Sterile Products in Pharmacies (CSHP)
Handbook on Injectable Drugs (Trissel)
Principles of Sterile- Product Preparation (ASHP)
Sterile Dosage Forms (Turco)
/
,
Compatibility And Stability Of Parenteral Drugs
Handbook on Injectable Drugs (Trissel)
Parenteral Drug Therapy Manual (Ottawa General Hospital)
Trissel's Tables of Physical Compatibility
Pocket Guide to Injectable Drugs (Trissel)
IV Index System (Micromedex - subscription required)
53-5
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Pharmacokinetic Monograp.hs .

.
OSP-D1 Volume I: Information for the Health Care Professional
Handbook of Clinical Drug Data
Patient Counseling
Patient selfcare {(Ph.A) for over the counter products
USP 01: Volume II: Advice for the patient in lay language
Communication skills in pharmacy practice: a practical guide for students and practiti0n.ers
(Tindall: 4
U1
ed. - 2002)
Communication skills for pharmacists: building relationships, improving patient care (Berger).
Pregnancy and lactation. .

Mother Risk Program
Clinical Therapy in Breastfeeding Patients (Hale)
Nausea and Vomiting of Pregnancy: State of the Art 2000
Teratogenicity and Drugs, in Breast Milk. In Applied Therapeutics: The Clinical Use of Drugs (i
h
ed
-2001)
USP 01- Volume I: Information for the Health Care Professional
Breast-Feeding Precaution Listing. In: USP DI-Vol. II (22
nd
ed. - 2002)
Pregnancy Precaution Listing. In: USP DI-VoLlI (22nd ed. - 2002)
Pediatrics
Manual of Clinical Problems in Pediatrics (Roberts)
Manual of Pediatric Therapeutics (Graef)
Martindale: The Complete Drug Reference
Nelson Essentials of Pediatrics
Nelson's Textbook of Pediatrics
Neofax
Pediatric Dosage Handbook
Pediatric Pharmacology
Problems in Pediatric Drug Therapy
Red Book 2000: Report of the Committee on Infectious Diseases
Rudolph's Pediatrics
The Harriet lane Handbook
Drug Information Resources www.Pharmacyprep.com
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The Pediatric Drug (Benitz)
Poisoning and Toxicology
Refer to poison control centers: Addresses are found in Yellow pages CPS.
Casarett and Doull's Toxicology: The Basic Science of Poisons (6th - 3.996)
Clinical Management of Poisoning and Drug Overdose (3
r
d edition - 1998)
Comprehensive Review in Toxicology for Emergency Clinici_ans (3
r
d edition - 1998) .
Drug Toxic kinetics
Ellenhorn's Medical Toxicology: Diagnosis and Treatment of Human Poisoning (2nd edition -
1997)
Poisoning and Toxicology Handbook (APhA - 1997)
Principles and Methods of Toxicology (4th edition - 2000)
Veterinary Medicine
Compendium of Veterinary Products
Current Therapy in Equine Medicine (Robinson)
Current Veterinary Therapy 4: Food Animal Practice (Howard)
Development and Formulation of Veterinary Dosage Forms (Hardee)
The Exotic Animal Drug Compendium: An International Formulary
Handbook of Comparative Veterinary Pharmacokinetics and Residues of Pesticides and
Environmental Contaminants
The Veterinary Formulary: Handbook of Medicines Used in Veterinary Medicine
Veterinary Drug Handbook (Plumb)
Doses And Drug Administration
Physician desk reference (PDR)
Drug facts and comparison
Martindale: The extra pharmacopoeia
Intravenous and Intramuscularly Compatibilities
Handbook of injectables drug (TreseI)
Martindale: The extra pharmacopoeia
Teratogenicity
Physician desk reference (PDR)
/ Drugs in Pregnancy and Lactation (Briggs)
of, some important-reference sourtes
.1 ;'Marti.ndale: The complete reference: Reference books contained with complete source of
information about foreign drugs and approved .and off labeled' drugs.
53-7
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Martindale's Extra Pharmacopoeia is probably one of the most comprehensive, international,
single volume references on drugs and drug products. Martindale's is divided into three
parts;
The first part consists of monographs on drugs and ancillary substances. (Although drugs that
are manufactured in the England are stressed, generic and propriety products from many'
other countries are included.) The monographs include c!l!mical storage,
doses, and toxic effects.
The second part contains a supplementary discussion of new drugs, obsolete drugs, and
miscellaneous substances.
The third part lists formulas of OTe products sold in the England. There is also a directory of
worldwide pharmaceutical manufacturers.
information about chemical properties and compounding.
information about anatomy, physiology and pathophysiological
conditions.
US? 01
Available U$P 01
8
Drug Reference Guides include:
Volume I: Drug Information for the Health Care Professional
Volume II: Advice for the Patient in lay language
Volume III: Approved Drug Products and Legal Requirements
USP 01 Volume I
USP Ole Volume I: Drug Information for the Health Care Professional contains
In-depth monographs cover dosing
Indications
Interactions
Pharmacology/ pharmacoki netics
Side/adverse effects
Patient counselling gUidelines
Labelled and offlabel uses are discussed to facilitate third-party reimbursement.
USP 01 Volume II
USP Die Volume II: Advice for the Patient
e
- f!!.uq Information in Loy Language. Provides
patient-oriented drug information to help patients understand and successfully follow their
drug regimens. These include brand names, descriptions, proper use, and precautions, Side
effects. Insfructions for. how to handle missed d"Oses are included, as are guidelines for when
- - .
to seek-medical assistance or supervision.
, '
USP Die Volume III
5H
www.Phannacyprep.com Drug Infonnation
USP Volume III: Approved Drug Products and Legal Requirements. Staying apprised of
federal guidelines and legislations related to and dispensing drugs are time
consuming. This is a single, easy-to-use reference containing all the information you need
including the complete FDA "Orange Book." USP DI Volume III helps you quickly identify a
drug's chemical properties, determine if a drug has been discontinued, or select an
appropriate generic substitute for a more expensive brand name drug. Excerpts from USP-NF
offer data on quality, pa<:kaging, storage, and labeling requirements. Contains guidelines and
laws governing the safe handling and distribution of drugs.
USP Dictionary
USP Dictionary Content Overview
United States and international drug names
The USP Dictionary is the authoritative source for generic drug names established by the
United States Adopted Names (USAN) Council. The dictionary also provides other types of
drug names used worldwide: Brand names. Chemical names. International Nonproprietary
Names (INNs). British Approved Names (BANs). Japanese Accepted Names (JANs). Official
USP-NF names. FDA-established names.
The Medical letter
Its newsletters, The Medical Letter on Drugs and Therapeutics and Treatment Guidelines from
The Medical Letter, publish critical appraisals of new drugs and comparative reviews of older
drugs.
Clin-Alert
The adverse drug reaction events reported by Clin-Alert during the year 2000 have been
compiled, organized, re-formatted, indexed, and published in a convenient one-volume
reference book
Drug Interaction Facts
Drug Interaction Facts loose-leaf edition provides drug-drug and drug-food interaction
information in a quick reference format.
Drug Interaction Facts covers more than 20,000 brand and generic drugs and more than 70
therapeutic classes.
Drug significance ratings are also included.
" Drug Interaction Facts now includes
Drug Interaction Facts: Herbal Supplements and Food - which covers over 100 monographs
and discusses the significance, onset, severity, documentation, mechanism, and
more.
Updated quarterly.
53-9
53-10
Tips
Children immunization schedule is found in? (2.. ,-J
Dental prophylaxis clinical practice guidelines can be found in? ( 2... J
o The Science And Of Pha'rmacy i
V This textbook has been the definitive reference for all aspects of the science and practice of
pharmacy, and is used for pharmaceutics, therapeutics and pharmacy practice courses in
primary curricula.
Remington covers many education and practice issues, from the history of pharmacy and
ethics, to industrial pharmacy and pharmacy practice.
Drug Infonnation Resources
1 Second use of drug or 2. CPS 3, Therapeutic Choices
unapproved use of drug
4 Drug monographs. S, CPS or Immunization 6, Patient self care.
Guide of Health
Canada
7 Clinical practice 8 Remington; The 9 Antibiotic
recommendations for diseases science and practice of recommendations or
such as cardia, neuro, pharmacy clinical practice trial
psycho, respiratory, GI etc. recommendations
www.Pharrnacvprep.com
Indexes
Drug Interaction Index
FDA/Manufacturer Alert Index
First Report Index
Legal Action Index
Newly Marketed Drugs: 1997-2000
Drug Index
Internet Sources and search strategies
Benefits: Enhances the abHlty to search therapies recently published or currently in news.
Provides access community and government of public health issues and related information.
Limitations: Jhf6rmation obtained fro,m Internet may not be reviewed or editea before it
".-,,-.
is posted on the
..... . .
A website should be evaluated by its source of publisher, the name, location and sponsorship
should be disclosed.
Step By step approach in evaluating drug information request
It is important to obtain necessary information about drug before initiation information
search.
Collect more information about drug itself
Clarify drug identification and availability?
To identify or assess product availability, consider using the following resources:
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Initial treatment can be recommended using?J3 )
Off label indication is? (f )
Compendium of pharmaceuticals specialties (.2J
What is found in compendium of pharmaceuticals specialties? ( 4)
What is fOl:Jnd in patient self care (PSC)? ( \2....La.o ) 4-
. What is not present in patient self care? (.3 )
Compounding reference (
53-II
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Physician Physician Physician
Prescribine. orescribine orescribinl!
Pre-clinical
Clinical
Market
Regulatory Public access
studies
trials product
authorization
Public and
(phase
submission
By health
private drug
Prescribing
I, II,
Canada
plans/politic
practices
s listing and
Clinical
andll! rcimburseme
Notice of nl decisions
Real-world
trial Submission
Compliance
use studies
applications revIew
(NOC)
Common
(phase TV)
.:[f'!j)5,
Drug
Review
Therapeutic
(CDR)
cost-
New drug submission (NOS) or
Labelling and
effectiveness
product
abbreviated NDS (generic products)
monograph
or supplemental NOS (changes in
existing products)
Surveillance, inspection. and
investigation for safety and
regulatory compliance
54
Drug Development Process
New Drug Development
Process
Questions Alerts!
Role of Health Canada
Drug approval process: phase 1 to phase 4
www.pnannacypreD.cOm
Pre market Post-market
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Pre-clinical research (in animals)
,1,
Phase I trials (small healthy human population, PK, Safety)
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Phase II trials (small disease human population, effectiveness)
Phase III trials decisive phase)
,1,
Trial review and approval
,1,
Phase IV trials (post marketing surveillance)
Preclinical 'Research
Stage # of patients Duration Purpose
Pre-clinical research None 18 months -3 years Laboratory investigation for
efficacy and toxicity
Phase I trials
Phase I 20-100 Up to 2 years Safety and dosage
Human Healthy volunteers
Small or limited population
Designed to establish the effects of new drugs in humans, specifically determine a
pharmacokinetic studies, drug toxicity, absorption, distribution and metabolism.
Phase /I trials
Phase II 100-300 Several months-2yrs Some shows term
safety but mainly
effective
Test on disease patients
Slightly larger but limited population
Tested safety and efficacy in slightly larger populations who afflicted with the disease or
conditions, which the drug is developed.
Phase III Trials
Phase III 100-3,000 2-3 years Safety, relative
effectiveness
dosage
Tested on Disease patient
54-2
54-3
Drug Develop"ment Process
Who approves and authorizes the sale of medications in Canada? )
Who sets the prices of prescription drugs in Canada? (7 )
Who sets the prices of over the counter drugs in Canada? ( t)
Pre-clinical studies is done in? ( )
Phase I clinical studies is done in? (Bl
Phase II clinical studies is done in? (10 )
Phase III clinical studies is done in? (3 )
Phase IV clinical studies is done in? ( S)
What is notice of compliance (NOC)? ( ,)
Decisive Phase in clinical trials is &..)
tu- fW-'(jUrI' 'I 4- d-rc..
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1. Notice of 2 Phase III 3. Disease patient, large
Compliance number of patient, it is
decisive phase
4. Animals 5. Post marketing, 6. Health Canada
inspection of safety
and regulatory
compliance
7. Patented Medicine 8. Pharmacy 9. Healthy volunteers,
Price Review Board Manager/Owner pharmacokinetics & safety
PMPRB
10 Disease patient 11 NPN 12 Natural Product
and Directorate
smaller number
Phase IV Study
larger population than phase II
last pre-approval round of testing. Test the new drug.with comparison of standard drug.
The results of new trials usually provide the information that included in the package
insert labelling.
After approval drug from phase Ill, this can be sold in market.
Trail Review and Approval
After drug has been approved. StudIes are conducted to compare the drug to a competitor.
Explore addition side effects.
Tips
Stage It of patients Duration Purpose

Review and None 1-2 years Safety. effectiveness,
Approval dosage
Stage tI of patients Duration Purpose
Phase IV 100- severaI No limit Safety, effectiveness dosage
thousand
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55
Questions Alerts!
Epidemiology
Cross sectional, case control and cohort studies
Clinical study designs like parallel and cross over designs
L.
V - Types of bias and confounders
Types of blinding
\. The credible clinical studies are randomized double blind
General Design Elements: These are the several important tools that researchers use to
improve the validity of a clinical trial, its ability to achieve the clinical endpoints, and its ability
to provide the highest possible level of evidence.
IClinical Studies
I
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IDescriptive studies
I IExplanatory Studies
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Case reports II Case series I
Meta analysis
I Observational I
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Cross sectional (or)
I
prevalence (now)
Case control or retrospective or Cohort or follow up
Collect the data after both
(past): future or prospective
d.isease and exposure.
Good for rare disease, initial etiology. Get incidence and estimate.
Detennine prevalence rate_
No incidence and prevalence. Calculate the risk
No incidencc-:'-;;te
Odds ratio method I
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Important concepts: Epidemiological study designs to study drug use and outcomes
in large populations.
Prevalence: collect data after both disease and exposure. Measured by cross sectional study
Incidence: collecting data from exposed. Measured by cohort studies
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The strongest sequence of strength (the most credible) clinical trial design: is A>B>C>D>E
Al experiments B) Cohort C) Case control D) Case series E) Case report
Cross sectional examples:
Determines or identifies the risk factors and etiological agents or disease or conditions.
To evaluate receiver characteristics of diagnostic procedure .
To evaluate a new laboratory tests.
Advantage: results appears at the time of study
Case Control Trial
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Question Alert!
Methods for continually
monitoring side effects and safety
of medication use in large
populations.
Case control study ._
A case control study compares a population of patients with a specific pre-existing condition
to a similar population without - to establish the influence of a disease or other event (Eg.
Intervention, hospitalization, death). Data collection is usually dine using medica!"records and
patient interviews.
This study often the best way to study rare diseases that develops over a lortg period of time.
It can be less reliable than randomized controlled trials or cohort studies because the
difference that can be made about the influencing factors is limited by bias.
Pros and Cons
(+) Requires fewer subjects than cross-sectional trials
(+) Only way to study long-term, rare disorders
(+) Fast and inexpensive
(-) Difficult to select control
(-) Potential bias form patient selection and recall
(-) Exposure status relies on records and recall
Cohort Studies
An observational study that allows a large population of patients with a specific pre-existing
condition or treatment for a period of time, comparing them with another group unaffected
by the affliction or the treatment.
Cohort studies are employed when it would be unethical to test the effects of a condition or
treatment on otherwise healthy patients (Eg. Obesity in children), often in the etiology or
prognosis of a disease.
Pros and Cons:
(+) Lower cost, easy administration (compared
to RCTs)
(+) Can establish time and direction of eV;Q!s
(+) Ethical -) 0'" P
(-) Not randomized, difficult to blind
(-) Control difficult to identify
(-) Differences can take a long time to develop
(-) Participants can withdraw, develop other conditions, or die
Parallel group design: The more common of the 2RCT designs, the parallel group design, is
, often used for confirmatory trials. Participants are randomized into 2 or intervention, the
other treated with placebo (or current standard of care)
Pros and Cons:
(+) Randomized improves statistical analyses
(+) Unbiased distribution
(+) Can be blinded
(-) Requires extensive resources
(-) Can present ethical challenges
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Crossover Design: Participants afe randomized into 2 or more groups; however, each group
receives all the treatment (Eg. Intervention, standard, placebo) in a random order with a
"washout" period in between - a period of time between two active treatments when the
patient receives a placebo in order to remove the residual effect of the previous treatment
before initiating the next active treatment. The basic crossover design is 2x2, in which 2
groups receive 2 consecutive treatments
Pros and Cons
(+) Reduced error variance = reduced sample size
(+) All participants serve as own control
(+) All participants treated
(+) Can be blinded
(+) Comparative studies
(-) All participants receive intervention, Standard, and placebo
(-) Cannot be used for intervention with permanent outcome
H length washout period
{-I long duration
Parallel Group Design
Treannent Group
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4

- Meta Analysis
It thoroughly examines data"from a number of valid trials that are similar- enough to permit
them to be combined and analyzed as one large trial: The evaluation of quantitative evidence
from 2 or more trials involves combining the raw data or the summary of statistical results
using a special statistical methodology.
The meta analysis trial design provides the highest level of evidence of any trial design
because part of its methodology includes the analysis, critical appraisal, and summary of the
results of many selected randomized controlled trials.
Pros and Cons
(+) Top ranking in the levels of evidence
(-) Trials demonstrating a positive effect are published more often than those that don't,
exposing a meta-analysis to a publication bias
(-) Results from different trials do not always agree
(-) Authors of a meta-analysis could uncohsciously or intentionally omit trials that mayor
m-ay not support the clinical question
(-) "Grouping" results from trials with different designs, statistical analyses, and patient
populations may be problematic.
Randomization: Participants are selected by computer codes, randomization improves"the
validity of a trial's results.
Randomized Controlled Trials (RCTs)
A clinical trials that answers questions about the effectiveness of different therapies by
studying the effect of an intervention on randomized patients. This can be by using 2
possible methodologies designed to reduce bias and promote comparison between the
intervention group and 1 or more control groups (a.ka. 'arms') treated with a placebo and/or
the current standard of care. RCTs are the standard trial design for answering clinical
questions about therapy effectiveness.
Stratification:
In some trial designs, patients may have important differences that researchers know will
affect the outcome of the intervention, such as different stages in disease state or concurrent
conditions. In such a case, patients may first be intentionally divided into 2 or more groups,
example "smokers and non-smokers" or diabetics and non-diabetics".
Stratification enables researchers to evaluate how an intervention affects both groups by
studying whether or not there is a difference in the subgroup.
Population: Population, from which trial subjects will.be selected.
Sample size: The total number of participants included in a clinical trial is determined by the
change the researchers want to observe in the chosen primary outcome.
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Bias is systemic error or distortion of a test nieasurement
Trials
Multi-centre trials are conducted at more than one location, often by more than one
investigator, but using one central protocol. When conducted at multiple centres in more
than one country they are referred to as multi-centre, multi-national trials.
Placebo: A placebo is a device that imitates the active intervention but has no therapeutic
value. The placebo effect is important when discussing adverse events (AEs) with a healthcare
practitioner. AEs from the group taking the placebo can be compared with those from the
group taking the intervention to determine to what degree adverse events are really
attributed to the active agent.
Epidemiology www.PhannacyPrep.com
Systematic Reviews
Are critical assessment and evaluations of primary research trials that use rigorous methods
to combine the.current best evidence to answer a specific question on a clinical topic.
A comprehensive literature survey of the topic is conducted
Primary trials of sound methodology and the highest level of evidence are identified (eg.
Randomized controlled trials)
The results of each trial are appraised
All results are summarized using predetermined, explicit, reproducible methodology.
Asystemic review shares many common characteristics with the first 4 steps of the evidence-
based medicine process: phasing a clinical question (endpoint); researching the answer;
evaluating the evidence; integrating and applying the evidence (conclusion).
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Bias:
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Interview bias: Because of blinding of interviewers response may be influenced, known as
interview bias.
Recall bias: Differentials in the memory capabilities.
Lead time bias: The selection of cases from both of these groups introduces a form of non
random error known as lead time bias.
- Confounding: effects because of dependent and independent variables.
Berksons bias (admission rate bias): Distortion in risk ratios occur as result of different
,/ hospital admissions.
Confirmation bias: linking directly to results
Selection bias: The selection of subjects into your sample or their allocation to treatment
group produces a sample that is not representative of the population, or treatment groups
that are systematically different.
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Epidemiology
Confounder: A factor that is prognostically linked to the outcome of interest and is unevenly
. distributed between the study groups. If study is examining the effect of age on
ulcer relapse rate and several ulcer also smokers (smoking could be confounder).
Blinding: It helps limit or eliminate factors that could unconsciously influence results. Blinding
minimizes bias in several ways:
BUNDJNG
Blind Double BITnd Tcipre- Blind
Single blind: One if the most basic forms of blinding in which trial participants have no
knowledge of intervention (example patients cannot distinguish between the intervention,
placebo, or active product used to compare different treatment regimens.
Double blind: Neither the trial participants nor the investigators have knowledge of the
assignment to the various trial groups of the interventions, placebo; or active product used to
compare different treatment regimens.
Triple blind: Neither the participants, the investigators, those- monitoring the safety, nor any
of the personnel involved in the selection of participants or evaluation of the outcomes have
knowledge of the assignment of the interventions and placebo to the various trial groups.
Tips format 002: Epidemiology
1. case-control 2. cross-sectional 3. prospective

4. Cohort 5. Single-blind studies 6. Double-blind
7. Randomization of the 8. Parallel Studies 9. crossover studies
sample
10 Dependent variable 11 Meta analysis 12 Prevalence
13 Case report 14 15
16 17 18
Factors reduces best bias CS) C/7 )
The odds ratio associated with ( I )
A study designed to determine the relationship between em'otional stress and ulcers used
the records of patients diagnosed with peptic ulcer disease versus controls over the period
from May 2009-May 2010. This is an example of what kind of study? ( J )
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In this study, the odds ratio associated with smoking marijuana during pregnancy is (16)
Combining data from several studies (often via a literature search) to achieve greater
statistical power. ( )1
is the number of people who have an illness at a specific point of time { \ 2....J
Twelve patients are given a drug or a placebo to determine the effect of medication on
blood pressure. The dependent variable in this study is
A study was undertaken to determine if prenatal exposure to marijuana is a cause of low-
Epidemiology
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Mother smoked
birth weight. Mothers of SO infants weighing less than 5 Ibs (low-birth weight) and 50
infants weighing more than 7 Ibs (high-birth weight) were questioned about their use of
marijuana during pregnancy. The study found that 20 mothers of low-birth weight infants
and only 2 mothers of high-birth weight infants used the drug during pregnancy. This is an
example of what kind of study? ( , )
Low-birth weight babies

High-birth weight babies
Odds ratio = fMQl or
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iostatistics
Questions Alerts! .
Statistical significance; Probability of error (P) and confidence intervals
Types of error like alpha and beta
Calculating risk reductions: absolute and relative
Calculating number needed to treat
Characteristic of data. Descriptive statistical measurements are often used in medical
literature to summarize data statistical distribution. Frequently used in clinical medicine are
symmetrical distribution, measuring central"tendency and measures of dispersion.
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Number of standard deviations from the mean value
(Gaussian) distribution or bell shape curve.
The dispersion or spread form the mean is represented by the standard deviation 68% (two
thirds) of the value falls within one standard deviation of the mean. 95% of the values are
found within two standard deviations of the mean. 99% of the values are found within three
standard deviations of the mean.
Bimodal = Two lumps
Positive skew = Mean> median> mode: Tail on right handed side
Negative skew = Mean < median <mode): Tail on left handed side
56-1
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Mean: The sum of the scores divided by the number of scores that is, the average score.
Mean: Sum of the score! number of scores:: 3 +5 + 5 + 8 + 9 =30/5 =6
Measures Of Dispersion
A measure that described the spread or variation of the observations is referred to as a
measure of dispersion.
9,4, 3, 2, 1, 5
1,2,3,4,5,9 (arranged in increasing order)
3+4/2 = 3.5
Median: Midpoint of the sequence;; 5 (if there is an even number of values, the mean of the
middle two numbers becomes the median), 4, 3, 8, 5, 5
3, 4, ~ 5, 8 (arranged in increasing order)
Biostatistics www.Phannacyp"rep.com
Mode: The score that occurs most frequently or repeats is referred as mode.-Nate: All
measures of the central tendency may be" altered b ~ the addition of very high or very low
values is distribution, the mode is usually unaffected by such values, and the mean is
susceptible to the greatest degree of change.
3,4,5,6, 6,7------Mode is 6
4,4, 8, 5, ~ M o d e is 4 and 5, this is referred as bimodal
1, 2, 3, 4, 5, 9 ~ No mode
Measures Of Central Tendency (middle of distribution).
A measure that describes a typical value in a set of data is referred to as a measure of central
tendency. Three measures of central tendency describe such values when they are found in a
normally distributed sample; mean, median and mode.
Examples: In a follow up study of five patients admitted to the coronary care unit with
diagnosis of acute myocardial infarction, the length of stay was found to be 5, 3, 8, 5 and 9
days. Calculate the mean, median, and mode for these sample patients. First arrange the data
in ascending or descending order; 3, 5, 5, 8, 9
Mean =3, 5, 5, 8, 9 = 30/5 = 6
Median =5
Mode: The score that occurs most frequently =5
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Four measures of dispersion that are used in clinical epidemiology and medicine are: Range,
Standard deviations, variance, and standard error of mean.
56-2
Range: The difference between the highest and lowest observation
Example; 99, 105, 115, 125, and 130.
Range: (130 - 99) =31
Biostatistics
Standard deviation. The standard deviation is another way to calculate dispersion. This is the
most common and useful measure because it is the average distance of each score from the
mean. The formula for sample standard deviation is as follows.
~ E(X-X)2
n-1
Where X = sample score, S = mean of the sample and
n =sample size
For sample data 5, 6, 8 and 9, what is the standard deviation?
Correction =x bar
Variance: The third method of measuring dispersion. Compare the two-variance formulae
with their corresponding standard deviation formulae. Variance is the square of the standard
deviation.
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CoeffiCient of vanance: 1l"Al.Ce&/ ~ ,......,......r ~ . d I
Given (x bar) and Standard deviation (SO) calculate of % of variance coefficient
SD
Coefficient of variance = -=- x 100
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Standard error of the mean (SEM): The standard error of the mean play,s an important role in
many of thestatistical procedures used in epidemiology and clinical medicine. It is used for
confidence limit determination and becomes and estimates of standard deviation of
population through.
5 = Standard deviation, N: Sample size
As the standard error of the mean decreases as the size of the sample increases
S
SEM=-
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.' Statistical tests analysis: Statistical test can be divided into three categories that are:
Parametric and non-parametric tests, and meta analysis.
56-3
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nalysis of varia ce ANOVA): is also known as F test and is used to compare means of
tree or more samples or groups for the purpose of determining the s . tical si nificance of
the observed findings. Degree of freedom can be calculated by (n-2). onsist of positive va u
Non-parametric statistical tests
Non-parametric statistics are also known as "distribution free" statistics. They"do not require
assumption of same variances. Their observations are independent. Examples of non-
parametric statistics are mode, median and chi-square tests.
Biostatistics

I Stalis ical tests
I I
Parametric tests Non-parametric tests
Mean and standard deviation and (-test Chi square, median, and mode
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t tests: Used for comparing the means of 2 treatment, even if they have different number of
replicates. The student's t tests used to compare the means of small (n < 30) independent
samples for the purpose of determining the statistical significance (p value) of the observed
findings.
T-test checks difference between the means of 2 groups.
The degree of freedom (DF) in paired t test can calculated by (n-l)
The degree of freedom in two independent sample would be (nI-l) + (n2-1)
Example: A drug is used to treat 50 placebo and 50 patients. Find out the degree of
freedom.
Chi Square test: This test is used for comparing two or more dependent proportions within
,
two or more groups making it useful for multi group comparisons. Compares percentage (%)
or proportions. (not mean values). The degree of freedom is defined as (R-l) x (C+1). Here, R=
row and C= column.
Example: Find out the degree of freedom in chi-square tests table.
(R-1) x (e-1) = (2-1) (2-1) = 1 '----- -
Used to test differences of two proportions from two independent samples can calculate by
Chi-square: Tossing a coin, 50% tail and 50% head expected. A coin is tossed 30 times and 20
heads and 10 tails are occurred. Whereas expected was 15 and 15 head and tail.
can be calculated by:
r
Parametric statistical tests:
Parametric statistics are the most popular data analysis procedures that assume that data are
from populations that are normally and independently distributed. The population of
parametric tests must have the same variances. Examples of parametric statistic are t-tests,
mean, and standard deviation.
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omi ( 2
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::: J>bserved freguenc)expected freguency)-
, Expected frequency
The Wilcoxon signed-rank test: Non-parametric statistical hypothesis test used when
comparing two related samples or repeated measurements on a single sample to assess
whether their pop'ulation means differ
Data analysis
Statistical Significance:
It's important to determine whether a treatment effect is really caused by the study
intervention or whether it is merely due to chance. A result is said to be statistically significant
when it is reasonably unlikely to be due to chance alone.
There are two main measurements that can help us: p-value (probability of error) and 95%
confidence interval.
p is 0.05 or 5% means, 1 in 20 results are by chance.
pis 0,01 or 1% means. 1 in 100 results are by chance.
Important concept! determining statistical significance
Probability of error:
Confidence intervals:
Statistical hypothesis testing
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Type II C13-error)
False -ve
Sample size
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Type I (a-error)
False + ve
Chance
Null hypothesis (Ho): State that there is no difference between: Example: smokers and non-
smokers with respect to the risk of developing lung cancer.
" Alternate hypothesis (H
A
) (relationship hypothesis): The alternate hypothesis states that there
, is difference between smokers and non:-smokers with respect to the risk of developing lung
cancer.
Types of error
Types of error
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Measure Of Risk
Type II Stating that there is NO difference when different exists. Accepting null
hypothesis when it is false. Beta is probability of making type II error. The Grror is the
probability of declaring no difference between the observed value and the hypothesized value
of an experiment. Parameter, a difference of error delta exists. Accepting null hypothesis
when null hypothesis (Ho) is false.
Biostatistics
Question Alert!
Type I error is false positive.
Stating there is difference when
NO difference.
Type I (a-error): False positive error. Stating that there is a difference when NO difference
exists. Or mistakenly accept the experimental hypothesis and reject null hypothesis. Rejecting
null hypothesis when Ho is true
For example: convicting a innocent man.
P = Probability of making type I error, also
referred level significance.
The level significance is set at a 5% level or
0.05 levels. The alpha error is set in advance.
The 0:0 error is commonly ches as 5%,
however, sometime it may set up to 1%.
P =1/20 =5/100 =0.05 =not significant
P <0.05 significant
p =0.0005 =Highly significant
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Measure of risk: Factors that are likely to increase incidence, prevalence or mortality of
disease are called risk factors.
Absolute risk reduction (ARR): IS difference between treatment group and control group.
The difference in the absolute risk between the intervention and control groups.
ARR =(placebo events) - (treatment events) or
Attributable Risk
Risk Reduction
Relative Risk
Absolute Risk
Absolute Risk (AR) : The difference in risk between exposed and unexposed groups that is
also percent of disease occurrences that are result of the exposure (example: smoking causes
1/3 cases of pneumonia)
,/. Allows to separately calculating the incidence of a particular disease in both populations
of a risk factor study for the purpose of making individual risk comparisons for each
population.
P_ .Jo..evL The absolute risk = A/(A+B)
rv--- A =Drug, B =Placebo
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orEER-CER
EER =Experimental event rate (treatment event), CER =control event rate (placebo
events)
NNT = Number needed to treat = IjARR
NNT = Number of patient needed to be treated to prevent one bad outcome
Relative Risk (RR): Relative probability of getting a disease in the exposed group. Calculated
35 percent with disease exposed group divided by percept with unexposed.
Relative risk = a 1(a+b)/c[c+d) o...Cco / c.(Cf'dl
Relative risk gives riskas a ratio of incidence among subjects exposed to a particular risk
factor divided by the incidence among subjects who were not exposed to the risk factor.
Relative risk reduction (RRR): Reduction in adverse outcomes in the treatment group relative
to those in the control (placebo) group.
RRR =[EER-CER]/EER
RRR=ARR -i- placebo events
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RRR = 1 x CER
NNT
-
When experimental treatment reduces risk of When experimental treatment
bad event increases probability of good event
RRR [CER-EER) 1CER (EER-CER) 1EER
ARR CER-EER EER-CER
NNT 11 ARR 1/ARR
RRR - Relative Risk Reduction
Tips
The Wilcoxon signed-rank test is a?
When will be the results on the same point in symmetrical curve->
ce
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P= Probability of making type I error, also referred level significance. H
Chi square test: The degree of freedom is defined'as (R-l) x (C-l)
The absolute risk =A/(A+B). A = drug, B= placebo
ARR = (placebo events) - (treatment events) or (treatment event) - (placebo event)
RRR =[EER-CERJ/EER
RRR=ARR -i- placebo events.
56-7
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RRR = 1 x CER
NNT
Example: Astatistical data mean is 100, median is 100, and mode 100, the statistical
distribution is? symmetrical distribution
Astatistical data mean is 200, median is 150, and mode 100, the statistical distribution is?
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What are the examples of parametric tests are 1'Y\et1'1 J to..J.-.__
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What is specificity -7q3pe..e.'- /..> 0...-
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In a perspective study compaci'1&.the effe'ttiveness of two chemotherapeutic treatments for-
cervical cancer causes were one group of patient who had annual pap smears
for atleast five years prior to their initial diagnosis and from another groups of patients who
had no history of prior pap-smears screening. The selection cases from both groups in this
study may result in:
Bias = systemic error = Distortion of a test measurement
Interview bias-Because of blinding of interviewers response may be influenced, known as
interview bias.
www.Phannacyprep.com Biostatistics
Recall bias-Differentials in the memory capabilities.
lead time bias---The selection of cases from both of these groups introduces a form of
non random error known as lead time bias
Confounding---effects because of dependent and independent variables.
Berksons bias (admission rate biasI-Distortion in risk ratios occur as result of different
hospital admissions. .
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Questions Alerts!
Common questions in phannacy exam is to a$k!
Managing Drug Distribution and workflow (e MA 'R) Mc:-
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Un,it dose system
IV admixture and sterile preparations
Hospital committees (P&T prepare formularies, Medical advisory committee or
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Inventory management (Perpetual inventory is used for narcotics), pas
Medication Reconciliation (gathering patient medication history)
Assuiiiiree:ill..eporting medical incidence (ISMI';: institute of safe
medication Canadian Medication Incident Reporting Services
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/ Activities and services of hospital pharmacy can categorized into:
Clinical Phannacy Services
Drug Distribution Services
Drug and poisoning information services
Hospital Committees
Clinical Pharmacy Services
57-1
Unit dose dispensing
57-2
The delivery of medication in hospital is multi step process.
After physician orders a prescription, it is sent to pharmacy department, where 3 things
happen.
A pharmacist assesses the order appropdateness, according to patient diagnosis and
treatment plan.
A pharmacy technician fills the order for the medication, which maybe oral, topical, and
parenteral.
The pharmacy technician labels the medication: medication name, dose, how to
administer and patient info.-mation Pharmacist ove.-sees th.e process of medication
-, .
delivery from central phannaey. Phannacy technicians have important role to play in filling
medication and checking each olher's works.
A variety of programs, equipments and procedures are necessary to make sure medication are
delivered accurately. minimizing the chance of errors and medication waste;
Automatic machines for packaging labels
Unit dose system that package each dose of medication for each patient in ready to use fonn.
A sterile preparation room with equipment that can bc uscd for intravenous preparations and
chemotherapy. The most common contaminant? (personals)
The safe laminar airflow hood for chemotherapy or cytotoxic preps? (vertical laminar ,airflow
hood)
Narcotic legal liabilities: System for controlling narcotics for legal accountabil ity ofthese
medications.
Destroying of narcotics; mail a list of narcotics to be destroyed to office of control substance.
Participating medical rounds (review of patient cases) by the healthcarc team

Ensuring patient receiving COrTect dose of correel medication at correct time.
Evaluating patient medication list before, during stay and after the hospital stay to ensure
accurney and appropriateness (medication reconciliation): Institute of safe medication
practices (lSMP) have developed best possible medication history (BPMH)
Making sure what medication has been prescribed and they understand the correct way to use
and expected effects.
Working with heallhcare team to detennine whether medication having desired outcomes,
and if not evaluating to find if medication therapy need to change.
Drug Distribution Services
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In unit dose dispensing, medication is dispensed in a unit of use package that is ready
administer to patient
The unit dose system is part of the hospital's system ofdrug distribution in which
medications are dispensed for a 24-hour period.
CrVA (centralized intravenous admixture): this utilized prepackage iv drug admixture.
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Drug and Poison Infonnation

Pharmacist represents good source ofinfonnation about medications and their toxic effects
Phannacist working in drug infonnation centres provide infonnation eilher verbally or
written.
Drug Information Centres (y c.. )
Healthcare professional or public may have some questions ur-gently or some of
questions require detail literature search using electronic search programs, andjoumals
to find out information on variety aftopics:
Availability and uses of different medications
Side effects of medications
Drug interaction's
Mixing intravenous medications
Current approaches to therapy
Controversial topics on medical use
C?yMP"
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Pharmacy therapeutic committee (P&T)
Fonnulary committee
Drug and Therapeutic Committee
Paramedical committee
Pharmacy Therapeutics and Nutritional support committee
Poison information centres '.
Pharmacist working in poison infonnation centres answer questions from other healthcare
professional and public about poisons, toxicities and overdoses of drugs;
Management of accidental by children
Antidote to medications
Management of overdoses
Contents of household products
Identification of unknown medication ingestions
Poison prevention tips
Hospital Committees
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Drug Utilization Review (DUR): Examine the following quality and efficiency of;
Quality and efficiency of a unit drug distribution system
Quality and efficiency ofclinical phannacy services
../ Quality and efficiency of antibiotic drug use in a hospital
tbl' . Quality IV admixture program
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Phann.ciS! functions in hospital ph.nn.cy (P'-'.AcW '1) .. .f-
clUfI3"'JI
Phann.ciS! role in P&T committee HI f'..t(JVVe 4
d' if' I . s4T.....u
Therapeutic equivaJent drugs in hospital M.t- t:...I<c.l.o
What is least likely pharmacist functions in hospital phannacy -7 Col cft..r,'11
Who is the last person to check medications in hospital ward -7 It\
A patient in is using diffJSrent brand of drug, then hospital formulary. Patient wa ts
same drug? VIal- c<... n
Hospital funding --> PNVI tI"IOc./
R.econciliation: gathering nfe.&ication information from patient at the point of
hospItal admittance and discharge.
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www.PhannacyPrep.com Generic and Brand Names
t
Generic "and Brand ames
tlemetlcs: to treat vomIting
Generic Name" Brand Name Generic Name Brand Name
Dimenhydrinate Gravol (generics) Metoclopramide Generics
Meclizine Bonamine Scopolamine Generics
Ondansetron Zofran Domperidone
Prochlorperazine Stemetil (generics) Diclectin (vitamin
B6+doxylamine)
Promethazine Phenergan
,
h hm I h ltlarflyt mlcs: o treat lITe u ar eart" rwt s
,
Generic Name Brand Name Generic Name Brand Name
Amiodarone Cordarone (generics) procainamide PronestylSR, Procan (generics)
Disopyramide Rhythmodan Quinidine Biquin (generics)
(generics)
lidocaine Xyclocaine propafenone Rythmol (generics)
Cardiovasc"ular Drugs
AJ hh' T
ntihypertensive: to treat high blood pressure
car OOIC WI rase luretlcs
Hydrochlorothiazide Generics Furosemide Lasix (generics)
Metolazone Zaroxolyn
Diuretics (water pills): There are five types of diuretics i.e. Thiazides, Loop diuretics, potassium sparing, osmotic
and b . ahn d d' .
D
S otasslUm lpanng IUretics
amiloride + Moduret (generics) triamterene + generics
hydroclorothiazide hYdrochlorothiazide
spironolactone + Adactazide (generics)
hydrochlorothiazide
P
[3eta Blockers (suffix "101")
Acebutol Monitan, Sectral (generics) Nadolol Corgard (generics)
Atenolol Tenonnin (generics) Pindolol Visken (generics)
58-1
PhannacyPrep. .
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Bisoprolol Mococor ProPanolol InderaI lP:enerics
Carvedilol c..... Sotalol Solacer (s:,enerics
Labetalol Trandatc {eenericsl Timolol eenerics
Metoorolol Looresor, Betaloc le.enericsl
ne.iotcnsin II AT Receptor Blockers (ARBs (Suffix "sartan")
Candesartan Atacand Losartan
. Cozaar
E rosartan Tevelen Tclmisartan Micardis
Irbesartan Avo ro Vnlsartan Diovan
Calcium-Channel Blockers (CCBs) (suffix "di inc excent veraoamil and dihiazem)
Amlndinine Norvasc NonDihvdroovridines
Nifedipine Adalat XL Diltiazem Cardizem CD (p:enerics)
Felodipine Plendil, Renedil ER Vo mil Iso tin SR enerics
M.iOlensin-Convertinl!. Enzyme Inhibitors (ACE Inhibitors) (suffix rW)
Oonaze
"'
Lotensin Usinooril Zestril, Prinivil (2cnerics
Captopril C. len eneries Pcrindro ril Coversvl
Cila7.april Inhibaec I Quinapril Accu ril
Enalaoril Vasotcc Ramieri! Allace
Fosinonril Moneoril Trandolaoril Mavik
Generic and"Brand Names"
VasodllatlOP Apents
Hydralazine Apresoline (generics) Nitroglycerin SL spray Nitrolingual Spray
(eenericS)
lsosorbide dinilrate Cedocard SR Minoxidil Loniten
I (llenerics)
lsosorbide mononitrate Imdure
Nitro I cerin SL tablet NitrOS(al
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Catapres (generics)
Brand Name. Generic Name
Clonidine Aldomet (generics)
ertensivc A ents
Brand Name
loha-Adrenereic Olockers (aloha I receolor blockers) (Suffix "zosin")
Alfuzosin Xatral Prarosin MiniDress (penerics
Doxazosin Cardura enenes Tamsulosin Flomax
Terazosin H rin enerics
te20nes 0 U2S I.e. statlns I rates macln
""ns
Atorvastatin Li itor Fluvastatin Leseol
Bezafibrate Bezalip Gemfibroz.il Lopid (J!.enerics)
Cholestyrarnine Questran (generics) Lovaslalin Mevacor(generics)
resin
-
Fenofibrate Li idil enericsl, Pravastatin Pravachol (J!.enerics)
Centrall Actin Antill
Generic Name
Mcthyldopa
A
Anlihyperlipidemic Agents (HMGCoA reductase inhibilOrs suffix "statio"): To Ireat high eholesterol,lherc are 4
ca . fdru . fib .. and .
Copyright Cl2000-2012 TIPS Inc. Unauthorized reproduction of this manual is strictly prohibited and it is
PhannacyPrep.

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Lipidil Supra
RosuvaStatin Crestor
Simvastatin Zocor (generics)
plates t er arcotlcs
Codeine generics Meperidine Demerol
Dextropropoxyphene Darvon N, 642, Morphine' MS Contin and generics,
(generics) M.O.S.
Hydrocodone and Hycodan, Hycomine qxycodone ~ r s Percocel (generics)
preps Novahislex DH,
Novahistine DH,
Tussionex
Hydromorphone Dilaudid (generics) Pentazocine Talwin
Fentany.l DuragesiC
..
Oxycodone Oxycontin
CNS drugs
O' &0 h N
ticonvulsants (antiepileptics or aritiseizure drugs)
Carbamazepine Tegretol (generics) c10bazam Frisium (generics)
Phenytoin Dilantin clonazepam Rivotril (generics)
Gabapentin Neurontin (generics) diazepam Valium (generics)
vigabatrin Sabril lorazeoam Ativan (generics)
phenobarbital Generics primidone Mysoline (generics)
divalproex Epival (generics) lamotrigine Lamictal (generics)
valproic acid Depakene (generics)
An
P k' T D tlpar mson rugs: o treat ar mson's lsease
levodopa/carbidopa Sinemet (generics) Amantadine Symmetrel (generics)
levodopaibenserazide Prolopa pergolide Permax
bromocriptine Par/odel (generics) pramipexole Mirapex
trihexyphenidyI generics ropinerole ReQuip
benztropine Cogentin (generics) -selegiline Eldepryl (generics)
An' k'
onoamine Oxidase Inhibitors (MAOls)
phenelzine Nardil
tranylcypromine Pamate
Antidepressants: SSRls, TCAs, SNRls and MAOIs
M
ncyc IC tl epressants
Amitriptyline generics maprotiline Generics
clomipramine Anafranil (generics) nortriptyline Aventyl (generics)
desipramine Norwamin (generics) trazodone Desyrel (generics)
doxepin SineQuan (generics) trimipramine Surmontil (generics)
imipramine Tofranil (generics)
T' . r An'd
Selective Serotonin Re-u take Inhibitors (SSRls
PhannacyPrep. . ". .
58-3
Citalopram Cclexa nU\loxaminc Luvox
F1uoxetine Prozac (2cnerics I oaroxetine Paxil
sertraline ZoloR (I"cnerics
Serotonin noreoincohrine reuDuke inhibitors lSNRJ and Dual action antide ressants
Venlaraxine ElTcxor l3upropion Wellbutnn SR, Zyban
Mlrtaz.apine Remeron B irone B,S coeries)
Reversible InhibilOrs of Monoamine Oxidase RlMAsl
Moclobemidc I Manerix and .eencrics I
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Benzodia7.enines (suffix "am"} sleeninp oill
Alprazolam Xanax (generics) Temazepam Restoril (generics)
Chlordiaz.e xide enerics TriazoJam Haldan eneries
.
Diaze am Valium eneries Clonaze m
Fluraze am Dalmane enerics Dromaze
'm
,
Lorazepam Ativan eneries
Oxazepam Generics
Barbiturates (suffix "tal"
Phenobarbital Thiopental
.
I)sycholropic (neuroleptic (Antipsychotic dru.l!.s antischizoDhrenia drues)
Generic Name Urand Name Generic Name Brand Name
Chlorpromazine Novo-Chlorpromazine Hydroxyzine Atarax (generics)
FluDhenazinc Moditen ll!.cnerics Lithium Lithane Duralith (l1:cnerics)
Haloocridol I I!cnerics I nericvazine Neulentil
loxaoine I e:enerics I oemhcnazine Trilafon (l':encrics
I oimozide Omo I orochlomerazinc Stemcti! (l':eneries)
thioridazine I e:cncrics trinuooerazine I
thiothixene Navane
Sc:cood e:eoeralioo aotipsycbotics
Quetiapinc SefOQuel riS[leridone Risperdal
olanzapine Zyprexa, Zyprtta
Zydis 00
58-4,
Brand Name
Ritalin (generics), Ritalin SR
Generic and 'Brand Names .
Generic Name
mcthylphenidatc
Brond Name
Dexedrine
Aluminum hydroxide Amphogel Magnesium Milk of Magnesia
hydroxide
Aluminum and malUlesium Maalox. Sodiumloolassium Alka seltzer
dextroamphetamine
StImulants
Generic Name
Gastrointestinal Drugs
Antacids
Copyright 0 2000-2012 TIPS Inc: Unaulhorized reproduction oflhis manual is strictly prohibited and it is
PharmacyPrep.
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hydroxide Mylanta, Gelusil bicarbonate
Calcium carbonate Ttims Alginic Gaviscon
acid/aluminum
hydroxide'
Dihydroxy-aluminum Rolaids
sodium carbonate
2- eceptor antagonlsts u IX tl me
Cimetidine Nizatidine Axid (generics)
Famotidine Pepcid (generics) Ran.itidine Zantac (generics)
Anticholinergics
Anticholinergics, such as dicyclomine (Benrylol)
HR' .' .. (S ffi "'d' ") .
Proton pump inhibitors (suffix "azole"): To treat ulcers
esomeprazole Nexium omeprazole Losec
lansoprazole Prevacid pantoprazole Pantoloc
rabeprazole Pariel
Gastroduodenal C
Generic Name
sucralfate
Generic Name
misoprostol
Brand Name
Cytotec
Generic Name
domperidone
Brand Name
generics
wrOI ormones
Levothyroxine Synthroid Eltroxin Liothy<onine sod Cytomel
sodium
Thyroid Thyroid
Hormones
Th 'dH
rogens
Generic Name Brand Name
,
Generic Name Brand Name
Danazol Cyclomen Testosterone Andriol, Androgel, Androderm
Depo-Testosterone, DelatestryI
Sex hormones
And
Estrogen
estradiol-17p Estraderm, conjugated estrogens Premarin, C.E.S.
Estrace, Estalis,
Estrogel
estradiol-17P Climera hormone replacement Fem-HRT Premplus
micronized
estradiol Estring, Vaginal Ring
Pro estins
58-5
Copyright 2000-2012 rIPS Inc. Unauthorized reproduction of this manual is strictly prohibited and it is
illegal to reproduce permission. This. manual is being used during review sessions conducted by
PharmacyPrep. ....
\
lletinQ!) Humulin R.N,U Humalogill Humalog Mix25
Novolin Mixtures or 30no; NPI-I (intemlediatc)
20180' 50150; 40160
Glargine (long Lantus

58-6
Generic and Brand Names
Ievonorgestrel Mirenn mcgastrol acetate Megace (generics)
medroxyprogeslcronc Provcra (generics), norethindrone Norlutatc Micronor
acelate Dcno-I'rovcra
I orOQcstcronc Prometrium
om mc
'"
ontrace lives
Alesse Demulenl
I3rcviconil) Marvelonill
Diane-3S Ortho-Cepl
Ortho7nn Min-Ovral
Triohasit SynphasiC@
euromuscu ar DC In'" Al'CnlS
Generic Name Brand Name Generic Name Brand Name'
pancuronium Pavulon succinylcholine Quelicin
bromide
ral HVDoelvccmic AeenlS
acarbosc Prandasc pioglitamne Aelos
metrormin Glucoohage (generics rosiglitazone Avandia
rcDaeJinidc GlucoNonn chlorprODamide Generics
gliclazidc Diamicron glimepiride Amaryl
Diamicron MR
(r>enerics)
glyburide Eugluconill, Dialktaill
; (peneries)
ntlc 0 mcrp:lc
ru"
Atropine generics Ipratropium Atrovent
benztronine C02enlin (",enericsl Oxvbutinin Dilrooan
dicvclomine Benlvlol TiolrQpium S iriva
C b" dO Ie
Diabetes' Insulin
o
A . hr' 0
N
Adrenerpic Drul's (Decon estantsl
Generic Name Brand Namc Generic Name Brand Name
norepinephrine Levophed pseudoephedrine Sudafed
bitartrate
I (levarterenol)
oxymetazoline Claritin Eye drops I phenylephrine Prefrin, Mydfrin ..
xylomelazoline Otrivin
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P '"11" tI-1 ectlve agents: eOlcl inS
amoxicillin generics bacampicillin Penglobe
ampicillin generics c10xacilin Generics
penicillin V generics pivampicillin Pondocillin
An' 'w
C hI t1-m ec Ive agen s: e[ a oSDorlns
cefaclor Ceclor (generics) cefuroxime Ceftin'(generi cs)
cefazolin KefzoJ cephalexin generics
cefixime Suprax cefprozil Cefzil
cephradine Velosef
An" (i r
M tHn ectJve agents: acro I es
azithromycin Zithromax' c1arithromycin Biaxin
erythromycin Eryc (generics)
tHn ectlve agents: AmUl0g\ycosldes'
gentamicin Garamycin (generics) tobramycin Nebcin
amikacin Amikin
r T tJ-m ectlve agents: etracyc me
minocycline Minocin (generics) tetracycline generics
doxycycline Vibra-Tabs (generics)
fl t1-m ectlve agents: uroqumo ones
Ciprofloxacin Gatifloxacin
Norfloxacin Ofloxacin
Moxifloxacin
Brand Name Generic Name
Oh tl-m ectlve agents: t ers
clindamycin Dalacin (generics) vancomycin Vancocin
metronidazole Flagyl (generics)
..
tl unga s
Amphotericin B Fungizone
.'
Fulvicin UfF
c1otrimazole Canesten (generics), otraconazole Sporanox
Lotrimin- OTC
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PharmacyPrep. ,., . .' . .
58-7
Anti-Viral ~ n t s
abacavir Ziagscn@ lamivudine Heplovir
amorcnavir Agcncrase nelfinavir Vir"cept@
amantadine Symmclrcl nevirapine Viramune
(generics)
acyclovir Zovirax (generics oseltamivir Tamiflu
delavirdine Rescriotor ribavirin Rcbetron
didanosine Vidcxe ritonavir/lODinavir Kaletra
efavirenz. SUSlivaill saauinavir Inviraseill
famciclovir Famvir stavudine Zerit
anciclovir C Qvene) valacvclovir Vallrex
indinavir Crixivanill zakitabine Hividill
zidovudine Retrovir$ zanamivir Relenza
58-8
o
fluconazole Diflucan (generics) ketoconazole Nizoral (generics)
Sinl!.1e dose
Micona:to[c Monismt, Micati"!!> tcrbinafiflc Lamisil (generics)
OTe
Nystatin Nilstat, Myocostatin tolnaftate Tinactin OTC
I (2cncrics'-
undecylanatc Desemex aTe
ver the Counter Drugs
eelirizine Reaetine (generics) fexofenadine Allegra
chloroheniramine Chlor-Tripolon hvdro:wzine Atarax (e.enerics)
desloratadine Aerius loratadine Claritin
dimenhydrinate Gravol (l!.enerics) meclizine Bonamine
diphenhydramine Benadryl,
Allerdrvlill
AntHlcoplastlc
'""
bleomycin sulfate Blcnoxaneill ifosfamide Ifexill
busulfan Mvleranill methotrexate I 2enerics
carboplatin Paraolatin mitomycin MUlamvcinlil
chlorambucil Leukeranill mitoxantrone Novantronel
cisplatin Cisplatin@ I paclitaxel Taxolill
cyclophosphamide C)'loxanil) Proc)'loxe tamoxifen Nalvodex enerics)
cytarabine CYlosaJ), ARACe vinblastine sulfate Vinblastineil'l
dacarbazine DTIC vincristine sulfate Vincristine
daunorubicin Cerubidine
doxorubicin Adrillmvcin
fludaribine Fludara
I phosphate
5-fluororoucil Adrucilill, Efudcxill,
5-FU
idarubicin Idamycinf;)
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AntihistaminelDecongestant Products
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Drixoral Contac
Drisdan Tylenol Cold and
Sinus
tl-In ectlve agents: su a rugs
droperidol Droperidol prochJorperazine Stemetil (generics)
metoclopramide generics promethazine Phenergan
ondansetron Zofran
Coughs and Colds
An' . ii . If; d
D
d I An .. fl
N tlpyretlcs, AnalgeSICS; on-sterol a tHn ammatory rugs
acetylsalicyc1ic acid, Aspirin ibuprofen Motrin, Advil (generics)
enteric coated ASA Entrophen, indomethacin Indocid (generics)
Novasen
celecoxib Celebrex ketoprofen Orudis (generics)
dic10fenac VoJtaren (generics) ketorolac Toradol
diflunisal generics meloxicam Mobicox
floctafenine Idarac (generics) naproxen Anaprox, Naprosyn (generics)
fJurbiprofen Ansaid (generics) piroxicam Feldene (generics)
tofmetin Tolectin sulindac generics
tiaprofenic acid Surgam (generics)
Antidiarrheals
diphenoxylate/atropine Lomotil psyllium mucilloid Metamucil, Prodiem,
Mucillium
attapulgite Kaopectate bismuth subsalicylate Pepto-Bismol
loperamide Imodium (generics)
Laxatives
bisacodyl Dulcolax magnesium citrate Citro-Mag
cascara sagrada magnesium hydroxide Milk ofMagnesia
castor oil magnesium sulphate Epsom Salts
docusate sodium mineral oil (heavy)
docusate calcium polyethylene glycol GoLytely, Colyte
products
lactulose Acilac psyllium Metamucil, Prodiem,
(generics) Mucillium
senna Senokot
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58-9
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Questions Alerts!
2 . - - ~
Prescription Processing
Latin Phrase
Post cibum
Pro re nata
Per os
Quarter in
die
sine
I Ouaque die
I QuaQue
Right eve
Meaning
As needed
Every
morning
every
After meal
Pcr rectum
Pint
By mouth
Every other
day,
Evervdav
Every two
hOUTS... etc
Four times a
dav
without
.Left eve
I Quart
I prescription
',. . Iloth ,eves
.. . Ojienalf""
Q2h, q3h, etc
rx, Rx
5
q.a.m.
q.o.d.
q-i.d.
-.o.U
Abbreviation
IOD'
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Q.
ot
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I p.O.
D.r.n.
, pr
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Ante
Ad libitum
Ante cibum
Latin Phrase
bis in die
cum
Fracture
with
Before meals
Lett-ear
Twice a dav
Dram
Biopsy
With food
Diagnosis
As desired
Before
Grain
Hour
Gram
Drop
Hour
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cc
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b.Ld.
a
a.c.
Prescripuon AbbreViations
Definition of prescription
Essentials in prescription: prescriber name and address, patient name, date and
medication and directions, repeats. Prescriber signature.
Directions of ophthalmic and ear drop
Abbreviation Meaning
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h.s. At bed time Hora somni stat immediatelv

hx History supp suppository
ID Intradermal sx symptoms
1M Intramuscular T. ThSD Dr lhs tahleSDOOn
ill Internalional t, ISp teaspoon
unit
IV Inlravenous ci.d. JX a day ler in die
TYPB IV piggyback T.O. Telephone
order
k. Kilo2I'am IT lincture
L Litre IX treatment
Ih Pound un. ointment
.
mc. Microgram VO Verbal order
mEa MillieQuivalent 'Ex adurv .'
m. Millioram
ml Milliliter
oz Ounce
p I post post
Interpreting the prescription
caps ii tid PC-7 Take two capsules three times a day after meals (after food)
suppes I pr q6h pm -7 Unwrap and insert I suppository into the rectum every 6 hours as
needed..
tabs iss stat; tabs I q6h CC-7 Take one &one half tablets to start (at once): then take 1 tablel
every 6 hours with
fl. I tid cc two tablespoonful three limes a day with food
gtts ii ou qid for 7 Inslil 2 drops into both eyes 4 limes a day for 7 days
For a child: 10 mL stat, then 5mL tid for 10 2 teaspoonful at slart: then I
teaspoonful three times a day for 10 days
gtts iv au qid for 7 days-7 lnstil4 drops in both ears, 4 times a day for 7 days
tabs ii qam, ss at noon & tabs ii 2 tablets every morning, halflablet at noon and
two tablets at bed time.
"11. iv slat; fl. ii R4h ud-7Take teacupful (120 mL) at start: four tablespoonful every 4hours
Sirect
ed
.
app ung sp aa tid-7 Apply ointment sparingly to affected area three times a day
gns x po q12h ud-7Give 10 drops orally every 12 hours as directed
e ptJ,.dw-<L p--..ef'
Direction of administration of prescription order
For adults:
For eye drops, and nasal drops use-7 instil or place
For tabs and capsules-7 take
For lake
Suppositories-7 unwrap and insert 1 suppository into Ihe rectum or into vagina
Ointment and cream, apply

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I 'NoWL '%' 7".J,eP"
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The prescription: Wril1cn direction from a registered medical practitioner to a pharmacist for
preparing and dispensing a drug.
Rx
Patient
59-3

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3/12 = 3 month supply
Ifl4 = I hour
1/52 I week's supply
3/52 = 3 weeks supply
For children:
Oral liquid, tablets, or capsules usc-? give
Chewable tablet's usc-? chew
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Quantities in prescriptions:
In to denote I day supply
IOn = 10 days supply
Acrosols-? inhale
Sublingual tablets-? place or dissolve one tablet under the tongue
one tablet in waler and take
Prescriber name and title (number)
Prescriber office address
Prescriber phone number
Prescriber signature
rCiarify physidait
.... The'physician full name (last and first)
Patient name and address
Patient age
Date on which prescription was written
Prescription should consist of:
Prescriber
Drug name, strength
Quantity to be dispensed
Sig: direction to
. . Refill instructions
,
'The following infonnation should be addcd to the prescription if missing or clarified:
The correct spelling ofthe patient's full name (last and flIst)
The patient address
The patient home phone number
The age and date of birth (OOB)
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The following Infonnation added to the prescription at the time of dispensing:
The prescription number
Price (cost + professional fee = total)
Label: The infonnation which must be on the prescription label include:
Patient full name (first and last)
Prescription number
lnstruction for the patient use of the medication
Name ofdrug
Manufacturer (if drug was ordered by generic name)
The quantity
The strength
Filling date
Physician name/initial
Drug Identification Number (OtN)
Pharmacist namelinitials
.NOT on iilbel: expirj' dates
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4. ac S. prescription 6. expiry dates
7. ex aqua 8. au 9. AD
at is prescription? -7 /10
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The pharmaceutical care is the services rendered
..WPharmaceutical care requires the
phar.macist to incorporate some essential skills in practice, that
V Prescription processing and dispensing. . .
/ to use the
-., eiplJtcor.u.e,
'Skills in aSsessment of patient health status.
Identification of potential and actual drug related problems (DRP)
J .Identification of drug related problem and therapeufic choices'
::/ Developing and implementing therapeutic care plan
J Monitoring and evaluating patient progress with therapy
/" Documentation of finding and follow ups
60-1
Gathering patient information and Maintenance Of Patient Records:
A pharmacist must gather patient information and assess its relevance to patient care. This
process is often described as Pharmacists work! Ip of rime therapv (PV!DT). The PWDT
contains the thought proce!!es necessary for pharmaceutical care.
60
Phannaceutical Care
..
Pharmaceutical Care
PharmacyPrep.Com
Professional relationship with patient: A pharmacist must develop a professional relationship
with the patient, by collaborative efforts between pharmacist and patient. Offering empathy
is an important component of developing interaction. The pharmacist encourages patients to
participate in decisions about their health and s.upP.Q..!:Y.the patient's right to make choices.
/ The pharmacist develops professional relationships with patients and/or patient's agents'
and/or health care providers:
Questions Alerts!
Examples of drug related problems (DRPs)
Scenarios of DRPs of chronic therapy
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The patient specific information that gives a basis for or leads to the recognition of a
pharmacothera'py prdblem or indication of pharmacist intervention.
In short PWDT be presented as FARM Note and SOAP Note
FARM stands for: F:::I finding, A =Assessment, R=Resolution/recommendations, M =
- Monitoring.
SOAP stands for: Subjective data (5) separated from objective data (0), A =assessment P=
Plan
Information Collection And Maintenance Of Patient Records
The pharmacist collects and discuss the following information for new prescription or when
made necessary by.profession judgment. This information include:
Confirmation of the identity of patient
Current medical condition(s) being treated
Name, general description of the drug dispensed
Direction for use to get the maximum benefit of drug
Common or important side effects and appropriate management, and storage requirements
The pharmacist should respect the patient's rights to confidentiality and privacy by taking all
reasonable steps to ensure that personal health information is communicated in a manner in
which others cannot overhear the discussion. Pharmacist should offer a semi-private area
wLth suitable traffic and/or noise barriers or a private counselling room . . '.' .
The should communicate' using and appro'priate skills
while respecting the patient's personal, cultural and educational difference. The pharmacist
should demonstrate flexibility in recognizing the unique qualities of each patient in order to
find workable solutions.
Informed consent-7Taking permission and store personal information consent with
conscious.
provi?ed by patient is the property of patient; maintain
information confidentiality essential by the pharmacy. However, information may disclose to
physician, pharmacist, and insurance with the consent of
Developing therapeutic plan: A pharmacist must develop therapeutic plans, recommending
therapeutic options, doses, scheduling / administration, required drug devices and
compliance aids.
Therapeutic plan types: CORE pharmacotherapy plan:
CORE stands for:
C= (medical
/ a =Outcome desired for that conditio'ns
R= Regimen (treatment required to achieve outcome)
E=Evaluation parame.ters to assess outcome achievement
Documentation of pharmaceutical care: Formulate a FARM or SOAP progress note to describe
and document the interventions, intended or provided by the pharmacist.
{DRPs):'the pharmacist's focus is on the patient's use of a product, to
the patient's situation as a whole-including his or her need for the medication, the
60-2
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appropriateness of the product as prescribed, factors that could affect the patient's use of the
medication as prescribed, and whether the desired outc..ome will be (from both 'the
patient's and physician's points of view). An important' part of this focus for the pharmacist
involves the identification of current or potential drug-related problems and their subsequent
resolutions.
problems (DRPsJ; that are described in the,concept of pharmaceutical care
include: ..' ; - no;:'" 7tle-cJ!
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patient is taking/receiving a drug for which there is no valid. indication. : (j 9
patient requires drug therapy for an indication and is not receiving it
symptoms of disease .and of side effects). - - - - - ... -
v1-The patient is not the appropriate drug (includes allergies,
contraindications, or a drug that is not cost-effective, not working or not the (trug of choice).
vA-The patient is taking/receiving too little of a drug (includes insufficient dose, frequenCy and
drug-disease interactions, drug food interactions).
patient is taking/receiving too much of a drug (inCludes excessive dose, inapprppriate
frequency and drug-disease interactions). ., ,
v6"The patient is not taking/receiving the prescribed drug appropriately (economic constrC!ints,
dispensing or administration error;
v1'-The patient is experiencing an adverse drug reaction
v-B-The patient is experiencing a drug-drug, drug-food or druglaboratory test interaction.
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4. FARM S SOAP 6 improving patient quality' of life
Is the services offered by the pharmacist to improve patient quality of life within
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Finding, Assessment, Resolution, Monitoring FA-fZr<1 .
Subjective data, Objective data, Assessment, P!an ( _.. _..L. I t1 trl--11f-
Pharmaceutical care should be focus to? (6) I 'f .J-
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A 50 year old patient currently using enalapril for hypertension. Experiencing dry cough.
What alternative therapy should you recommend? (1) AR/I.!
A customer searching for OTC antidiarrheal medications. If you
associated with c1indamycin, what is appropriate action? ::::1In tilt 1./...
Pharmaceutical care should be focus to -7 I rnprvJ""I ,.....-'Qi..J C)......--.... -/ -v
IJI..Irite examples of drug related problem (DRP) -7
A SO-year-old patient currently using enalapril for hypertension. Experiencing dry cough.
What is alternative preferably therapy is recommended?-7 I}P4l Y
A customer searching for OTC antidiarrheal medications. If you realized'diarrhea is
associated with c1indamycin, what is appropriate action? -7 tf>
60-3
Phar.macyPrep.Com Pharmaceutical Care
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Clinical significant adverse drug reactions like most common and most serious side
effects
AORs affecting the cardiovascular system
Cardiovascular Causative drug Comments
disorder
-,

Hyoertenslon Vt,.l"'\kl
.........
Postural hypotension Alpha-blockers. ACE inhibitors,
Caution on standing
(syncope) diuretics, antipsychotic, opioids

Take first dose of alpha-blockers
and ACE inhibitors on at bedtime
Myocardial ischemia adenosine,
In patients with hypothyroidism
amphetamines. beta-agonist, beta- and.cardiovascular disease, the
blockers (withdrawal). caffeine, ergot initial dose of levothyroxin should
amine, nifedipine (shan-acting), be low and increased every 4 wks
theophylline, verapamil. Oral
-
contraceptive pills
Peripheral Beta-blockers
Choose a more cardia selective
vasoconstriction agent such as atenolol, which has
less affinity for beta 2-
adrenoceptors
'CbOb$i' a with
e.g. carvedilol
'8 0& '. ,. .
an' la etelo ;
Hemorrhagic stroke Anticoagulants, thrombolytic and

These should be avoided
antiplatelet drugs
61-1
www.Pharmacyprep.com Adverse Drug
Atrial fibrillation
Bradycardia
AV node arrhythmias
Antiarrhythmic: amiodarone,
disopyramide, procainamide,
propafenone, quinidine, sotalo!,
Antihistamines (terfenadine,
astemizolel, antibacterials
(c1arithromycin, co-trimoxazole,
erYthromycin), antifungals
(ketoconazole, itraconazole),
(chloroquine, quinine),
anti psychotics (chlorpromazine,
haloperidol, pimozide, thioridazine),
antidepressants, tricyclics,
mitriptyJine and imipramine),
cisapride, pentamidine, probucol,
tacrolimus, terodiline
eye drops).
an"iagonists,
carbamazepine, c1onidine, digoxin,

TCAs
Risk of torsade de (QT

: interval prolongation) or sudden
death due to ventricular
fibrillation
Recommended doses for
terfenadine should not be
exceeded
Terfenadine should be avoided in
hepatic impairment, hypokalemia
and pre existing QT interval
prolongation or with grapefruit
juice in addition to the risk factors
listed above
Drug causes are rare. Other
include hypertension,
hyperthyroidism, rheumatic heart
disease, infection and pneumonia
61-2
ADRs involving tlematological sYStem
Hematological causative drugs Comments
disorder
Aplastic anemia (total Antidiabetic (chlorpropamide. Reduced red cell (anemia). white cell
or partial failure of the tolbutamide), Antiepileetics (leucopenia), and platelets
bone marrow) (carbamazepine. phenytoin, . (thrombocytopenia) counts
lamotrigine), anti-inflammatory Often irreversible despite drug withdrawal
(diclofenac, gold, indomethacin,
penicillamine, phenylbutazone.
piroxicam, sulindac, sulfasalazinel.
Antimicrobials (chlorarT!phenicol, co-
trimO)(azole, sulphonamides).
antiplatelets (ticlopidinel.
antipsychotics (chlorpromazine),
-
antithyroid agents lcarbimazole,
propylthiouracil)
Agranulocytosis Antibiotics (penicillin's, Recovery usually 2 to 3 weeks after drug is
(profound reduction of cephalosporin's, co-trimoxazole, withdrawn; repeat exposure to causative
granulocytes with chloramphenicol, sulphonamidesl, drug not recommended due to
neutrophil count less antidepressants (imipramine, sensitization
than 0.5 x lO'/L clomipramine, desipraminel,
antiepileptics (carbamazepine,

phenytoin). anti.inflammatory (gold,
penicillamine,leflunomide,
sulfasalazine, NSAIOsl. antipsychotics
(chlorpromazine, thioridazine,
za I e antithyroid drugs
(met' Ima;ple, ij.,i'{.eY!fbTou'f4.til),
captopril, procalnamide,ffiElopitline:
Thrombocytopenia Antimicrobials (chloramtlllerill::bl, May present as easy bleeding, bruising or
(reduced platelets to trimoxazole, trimethoprim, penicillins, purpura; prolong bleeding time but INR
less than 150 x 10'ILl sulphonamides, rifampicin), remains normal. Usually occurs 7 to 10
antiepileptics (sodium valproate), days after drug started. Avoid future
inflammatory (gold, penicillamine), exposure to the causative agent
diuretics (thiazides, furosemide) ASA and NSAIDs reduce the effects or
tolbutamide, digoxin, methyldopa, remaining platelets and therefore should
tow be avoided during thrombocytopenia

Pure red cell aplasia Azathioprine, phenytoin, isoniazid, Anemia with a marked reduction in
(Total or partial failure penicillamine, chlorpropamide, reticulocytes (immature RBe). The coombs
or red cell production) chloramphenicol, erythropoietin, test is used to distinguish immune
cephalosporins, penicillins, mechanism; also G6PD deficiency.
tetracycline's, insulin, methotrexate, Red cells usually return to normal.after 2 to
isoniazid, quinidine, quinine, 3 weeks
rifampicin, sulphonytureas,
methyldopa, mefenamic acid, drugs
with oxidant effect on cell membrane
(particularly in G6PD deficiency
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61-3
www
Adverse Drug
. Megal0blastic anemia . Acyclovir, alcohol, antiepileptic, Impaired DNA synthesis usually due to
(large abnormaf"form methotrexate (dose dependent), folate or vitamin 8
12
deficiency,
- .
or precursors to RBC) - nitrofurantoin, oral contraceptives, Use folic acid supplements to treat patients'
proguanil, sulphasalazine, taking antiepileptic drugs.
trimethoprim (usually due to
worsening of pre-existing folate.
deficiency). Phenytoin
Causative drugs
Alcohol, amantadine, .(withqrawal),
It..c.... ....:A.: .. ,". - .' .
Antimicrobials (ciprofloxacin, sulphonamides)
Cardiovascular (lipophilic beta-blockers, alpha-blockers, CCB, Digoxin,
methyldopa, statins) .
Benzodiazepines, carbamazepine, levodopa, phenothiazines)
Hormones (corticosteroids, estrogens, progestogen)
Disulfiram, isotretinoin, mefloquine, metoclopramide, NSAIDs.
Psychosis Amantadine, amphetamines, anticholinergics (includes 1
st
generation
antihistamine), antiepileptics, bromocriptine, chloroquine, c1onidine,
digoxin, disulfiram, donepezil, ganciclovir, isoniazid, levodopa, mefloquine,
NSAIDs, quinidine, quinolone, zolpidem, drugs of abuse
Mania Baclofen, bromocriptine, chloroquine, cortic9steroids, dopaminergic agents,
isoniazid, levodopa, antidepressants
Behavioural toxicity Lamotrigine, dextromethorphan (children), diphenhydramine,
chlorpheniramine, vigabatrin
Antiparkinson drugs, barbiturates, beta-blockers, benzodiazepines,
cimetidine, corticosteroids, diuretics, H
2
-receptor antagonist,
MAOls, NSAlDs, Opioids, l't generation antihistamines,
Most common are benzodiazepines, cortic?steroids, opioids,
anticholinergics and drug with .anticholinergic effects including TCAs,
antiarrhythmics, antiparkinson agents, conventional anti psychotics,
ipratropium (high doses), oxybutynin, tolterodine and sedating
antihistamines.
are phenothiazines
;
Most common are ant'iparkinson's drugs, antipsychotics (phenothiazines,
. . . particularly chlorpromazine), barbiturates, benzodiazepines, carbamazepine,
opioids, antidepressants (amitriptyline, trazodone), 1
st
generation
antihistamines, and alpha blockers
ADR leading to Neurological disorder
Neurological Causative drugs Comments
disorder
61-4
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Adverse Drug Reactions

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Tolerance develops
.

rr;;rhacin, MAor vasodilator treatment and patients
interaction (hypertensive crisis), shpuld persist with treatment jf possible
analgesics (rebound after daily
administration, especially with
_..
caffeine), t{lptans (overuse).
ergotamine (withdrawal). SSRls
Aseptic meningitis NSAJDs. vaccines, ciproOoxadn.

Particularly in patients with systemic
azathioprine, penicillin, isoniazid, lupus erythromatu5
co-trimoxazole

Difficult to distinguish clinically from
bacterial/viral meningitis, therefore a
drug history should be considered in all
cases.
Benign intracranial Amlodipine, corticosteroids
Symptoms. include headache, edema of
hypertension (including topical), danawl, optic nerve head, nausea, vomiting,
etretinate, nalidixic acid, tinnitus and visual disturbances
nitrofurantoin, oral
Usually resolves on cessation of
contraceptives, tetracycline's, treatment
isotretinoin, vitamin A (at high
doses and deficiency)

1<> generation drug withdrawal improves
antiflisfaiilines, anti psychotics, prognosis
I:lJ;
badofen,.chloroquine,

Risk factors include diabetes mellitus,
. .
.ens.o. cydosporine. corticosteroids alcoholism, vitamin deficiency (vitamin
. . .
(systemic), donepezil, isoniazid,
8 8nl, reduced renal/hepatic function, 'fel '.
lithium, mefloquine, ecstasy
poor acetylator status (hydralaZine,
agents (amphetamines), NSAIDs, isoniazid)
oral contraceptives, penicillins,
pethidine, quinolone antibiotics,
antidepressants (SSRls, and HAsI,
stimulants and anorectics,
theophylline, tramadol, vaccines.
Withdrawal effects of alcohol,
baclofen, barbiturates, aZD.
Guillain-Barre' captopril, corticosteroids, gold
Rare paraesthesia of toes or fingers
syndrome (disease salts, hepatitis 8 vaccine, influenza progresses to upper and lower limb
of peripheral nerve) vaccine, MMR vaccine, oxytocin, followed by total body weakness
penicillamine, streptokinase
Myasthenia gravis Corticosteroids (high-doseJ,
Avoid in myasthenia gravis
(chronic muscle phenytoin, aminoglycosides,
weakness involving quinolone antibiotics
.
reduced activity of (ciprofloxacin), beta-blockers,
acetylcholine at lithium, anticholinergic
neuromuscular
junction)
61-5
www.Phannacyprep.com ,Adverse Drug Reactions
1 generation anti psychotics such
as 0.' ,""" (also following
.....
witFmraw t''antiemetics
(metoclopramide,
prochlorperazine), CCB (verapamil,
amlodipine, diltiazem), lithium,
methyldopa, antidepressants
(TCAs and SSRls), valproate
TInnitus NSAIDs, including ASA,
antimalarials
ADRs affecting Respiratory system
Respiratory disorder Causative drugs Comments

;:, ,:,. A
.'1' :,,,h, 1-
4
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AngiotensIn receptor antagonists

(ARBs) may be suitable
alternatives
Renin inhibitors (Aliskiran)

Nasal congestion Chronic use of topical nasal
qf"top.jpal
decongestants
j&j...H,,,. ",.'
(stuffy nose) .gecon:gestant'vasoconstnctors

aria

-.ri.tn.(r,li'; ... ,:,",...-.':"
to
(methyldopa, prazosin, hydralazine, re!gtil'atjon 0f alpha-adr:enoceptor.
propranolol), antipsychotics, oral
- - -r'" '::"" .... I' '"1'. .... :i'
Q'if.! %>.pplnasal
contraceptives, ASA, NSAIDs, tissue edema. .
Bronchoconstriction Anticholinesterases,
Particularly in asthma and CGPD
Antibiotics (e.g. penicillin's and patients
cephalosporin's), aspirin, NSAIDs,

Allergic reaction to penicillins may
dipyridamole, beta-blockers, (including
also occur with other beta lactam
eye drops), ACE inhibitors, antibiotics (cephalosporins,
;
pharmaceutical excipients (tartrazine, carbapenems and monobactams)
benzoates, phenylmercuric salts,
paraben, benzalkonium chloride and
metabisulfite), general anesthetics and
muscle relaxants Radiological contrast
media ACE
Reflex, Ipratropium, inhaled beta2-agonist,

Direct irritation of bronchial
bronchoconstriction corticosteroids, cromoglicate, mucosa
zanamivir
Lung parenchyma- nitrofurantOin,

Generally allergic reactions
interstitial
... ..'''''''''., .
presenting as cough, gold salts, paclitaxel,
rQO'n
:-" ..... _. - .
penicillamine, sulfasalazine breathlessness and wheeze
,.- -':
Pati'ents on sh6, ,ld
_".' ',\' .... Il.. N
. not receive' nttrofurantOIn due to
ADR '
Early diagnosis and treatment
improve recovery
61-6
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pulmonefr'{fibrbsis'
:.! -.:' .,
Pulmonary edema
(adult respiratory
distress syndrome,
ARDS)
Pulmonary
eosinophilia

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(neuromuscular)
_
-
IV beta-agonists (SalbutamollV and
terbutaline), amphotericin,
diamorphine, haloperidol,

Indomethacin, methadone. naloxone,
protamine.
Nitrofurantoin, NSAIDs, antibiotics,
ant_ineoplastics
.tolllbined oral contraceptives-
..... >51-:"
';'-mortalit;Y.
Dose and duration of treatment
are impOrtant
Increased pulmonary vascular
permeability presenting as cough,
breathlessness and' frothy sputum
dose monitoring of women
re<eiving IV beta-agonists in
premature labour, especially in the
presence of fluid overload.
Symptoms include cough, dyspnea
and fever
Patients improve on cessation of
treatment
May be treated with
corticosteroids

r.espiratory in the
_.!1rai;f,iij Increase I)Iooal:tfi
__.....,.......
respiratory.muscle
function
Patients at risk include those with
pre-existing impaired respiratory
muscle function, renal failure and
myasthenia gravis
Reversible on cessation of
treatment
May present as sudden collapse,
pleuritic pain, breathlessness.
cyanosis and hemoptysis
61-7
www.Phaimacyprep.com Adverse Drug Reactions
ADR affecting EnQocrimi'System
Endocrine effects causative drugs
Altered glucose control
Thyroid dysfunction
Adrenal function Corticosteroids, ketoconazole (reduced), rifampicin (reduced)
Aldosterone synthesis Carbi:!Ooxolone, lithium, loop diuretics, oral contraceptives, spironolactone,
thiazides
Hypoaldosteronism ACE inhibitors (including angiotensin II receptor antagonist), NSAIDs, heparins
Gonadotrophin release
and gonadal function
Ovarian and testicular:
Corticosteroids (reduced), danazol (increased free testosterone), ketoconazole
'(reduced testicular steroidogenesis)
Gynecomastia-estrogenic:
Clomiphene, digoxin, estrogens, spironolactone
Gynecomastia - (due to reduced testosterone):
Alcohol, alkylating agents, cyproterone, flutamlde, phenytoin, spironolactone,
ketoconazole, cimetidine.
Gynecomastia:
Antipsychotics (chlorpromazine), CCB, isoniazid, marijuana, methadone,
methyldopa, protease inhibitors, stavudine, TCA
Methadone, morphine, antidepressants, antipsychotics, anti ulcer drugs (e.g:
cimetidine, ranitidine), benzodiazepines,'estrogens, methyldopa, verapamil
'Psychotropic's,
.
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ADR affecting musculoskeletal tissue
Musculoskeletal pathology Causative drugs Comments
Myalgia (muscle pain), Jibrates, niotiiiic,add,.

Myalgia presents as muscle
cramps or myopatliy carbimazole, pain, tenderness and/or muscle
cimetidine,
weakness
colchicine, corticosteroids

(withdrawal), danazol. diuretics, .,' "offWi:7*le
opioids, penicillamine, quinine,
level may
- -
chloroquine, quinolones,
.indicate myopathy)
zidovudine

;CPr-titbsteroids, heparin, thyroid
of .
".ilM,,..", '!'_"':

cfsteoma'lada' {rickets, hormones
)ionormal bone softening)
0 supplement
_ ,; ...... .. t '. -
for'housebound and fraileld.erly
Metabolic bone disease: Aluminium salts (including
A lack or defective metabolism
.I
osteomalacia (rickets, prolonged ingestion of of vitamin 0
abnormal bone softening) antacids), barbiturates,
' Poor diet arid lack of sunlight

bisphosphonates (overdose),
are contributing factors
phenytoin, long term total
parental nutrition
Arthralgia Ooint pain Penicillin, CCB,-carbimazole,
May accompany any drug-
without swelling) isoniazid, procainamide, induced skin eruption
quinidine, quinolone antibiotics,
Severe joint pain with swelling is
rubella vaccine, BCG
a component of serum sickness
(e.g. penicillin)
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61-8

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."a"ute go.ut.,' .
Arthropathy (erosion of Quinolone antibiotics
Restricted indications in
articular cartilage) children, growing adolescents
and avoid in pregnancy
Usually reversible on cessation

of treatment .
Tendinopathy (particularly Quinolone antibiotics (ofloxacin)

More common in people in over
Achilles tendon) SO years of age
Increased risk if renal
impairment and/or
corticosteroids treatment
Retroperitoneal fibrosis ASA. beta-blockers,

Symptoms include persistent
(development of fibrous bromocriptine, codeine, pain in the loin and groin,
tissue behind peritoneum) ergotamine, haloperidol, oliguria, pain on micturition,
methysergide myalgia and edema
Symptoms improve on
-
withdrawal of treatment

procainamide,
Symptoms include arthralgias,
eJYttletn'atd5us-(5lEj beta-blockers, carbamazepine, myalgias, malaise, fever,
chlorpromazine, disopyramide, pleurisy and pericarditis
methyldopa,
Symptoms improve within days
nitrofurantoin, penicillamine, or weeks of cessation of
phenytoin, quinidine, suspected drug
sulphasalazine, sulphonamides,
Usually occurs after several

tetracycline's (minocycline,
months or years of continued
particularly young patients)
therapy
thiazides, thiouracil
Presentation of drug-induced
iiBfflM'Q
SlE differs from SLE
leucopenia, thrombocytopenia,
anemia, elevated ESR and
antinuclear antibodies may be
present
Increased risk in slow

acetylators
ADRs affectine Gl system
Adverse GI effects causative drugs Comments
Taste disturbance ACE inhibitors, CCB, Usually resolves on cessation of treatment but may
,
etidronate, griseofulVin, take for months.
isotretinoin, Il?\'Odopa,
Z'dpiifonef"Bitter.taste losartan, penicillamine,
terbinafine
.
Metallic taste Allopurinol, gold, lithium,
metformin, metronidazole,
penicillamine, zopiclone
Jiingiial Phe[Jytoin. occurs 'o\(ithin 3 months of starting treatment.

hygiene increases its risk.
Pigmentation of the Tetracycline's Rare
oral mucosa Particulac.bl.minocycline
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May caose-wiiight loss,: candidiaSis; 'dentalcaries, poor
.-Cxei'< __ miai ' . ,
TCAs, . adherence to drug regimens, reduced efficacy of
anticholinergic, CNS sublingual drug (e.g. nitroglycerin)
stimulants, phenothiazines
Saliva secretion Cholinergic agonist (e.g. Risk of choking at night
(Ptyalism) pilocarpine, c1ozapine)
Stomatitis and Aspirin, barbiturates, Usually resolve quickly when drug is stopped.
Mouth ulcers captopril, griseofulvin,
isoniazid, nicorandil, NSAIDs,
proguanil, sulphasalazine
esbpfrageal A!!A, Usually occurs within hours to days of taking causative
.,>.'.:"-' ...-
disbrMrs . drug
Wtrln1famyElR; doXycycline, Most cases heal within days or weeks of treatment
ferrous sulfa'te, NSAIDs, cessation
potassium salts, quinidine,
tetracycline;theophylline
Acid reflux or CCB, opioids, nitrates, and Due to relaxation of the lower esophageal sphincter
heartburn anticholiriergics
Nausea and Many but often occurs with Symptoms may resolve with continued use or
Vomiting anti!':ali'celi-d,fl,lgs, .el1)ergencY occasionally by taking the drug after food
It may indicate toxicity of digoxin or theophylline
levodopa, opioids, SSRls, iron
salts, bromocriptine,
erythromycin, estrogens
Gastro toxicity
CCB,
with NSAIDs
'..
. - - .,- .
It may be difficult to diagnosed at early stages, as the
,... . 'but liKely' if inflammation is asymptomatic
_ :; ..:Pr.'.t ..... ",;
This may be a cause of "unexplained bleeding". NSAlBs
Complications include iron-deficiency anemia due to
blood loss, hypoalbuminemia due to protein loss,
ulceration and stricture formation (results from
postprandial colicky pain)
Associated with alcohol abuse
Diagnosis may follow the detection of iron-deficiency
anemia, usually after long-term treatment,
hypoalbuminemia (associated with peripheral edema
and other signs of fluid retention due to protein loss
from damage intestinal mucosa)
Blood loss is not often sufficient for detection

f
Paralytic ileus and Acarbose, CCB, c1ozapine, bulk Phys1Cal obstruction or anticholinergic effects
pseudoobstruction forming laxati,:,es, loperamide, inhibiting smooth-muscle activity, particularly if more
opioids, phenothiazines, than one anticholinergic agent is prescribed
potassium salts, TCAs,
from cblestlpol, Supplements of fat-soluble vitamins may be required.
m .
.. "':' ............ ,pl.... .",: - ....... .......... ...
Serum vitamin B12 may be reduced in .patients taking ,
.mertormin metformin but clinical significance appears to be small
61-10
www.Pharrnacyprep.com Adverse Drug Reactions
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In, bile salts.
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colchicine. cytotoxics,
dipyridamole. gold. iron salts.
laxatives,
''On'"'''' !lR""' r l!1 (- go
antacids, NSA s
acid), orl15tat, ticlopidine.
misoprostol, olsalazine
Amphetamines, cocaine,
digoxin, ergot amine,
sumatriptan, methotrexate,
methyldopa, methysergide,
NSAIDs, estrogen, salicy1ates
Mi.QiJ.. are.
o'pibJds
iron
"ll;tJlV, :M;'.. :,.a,u,
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<ift-:--veraJ:!<!m
V
, TCAs,-
Do ... -,
an clozapine.
mebeverine, MAOls.
peppermint oil,
phenothiazines, sucralfate,
diuretics
'"fjlay be.thei\1ftjresult of
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m ronous,c IS. reatmehntio Id6e
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Severe dia(rhea may to treatment cessation of
diarrhea causing drugs
PresentS as sudden onset of severe abdominal pain,
nausea, vomiting, diarrhea, and abdominal distension.
pyrexia, leucocytosis, and bloody stools
may be present,
,- '.
imriiobllffY; advarice age and low-fibre diet,
':Op.ioidS induced constipation is treated by'stool
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f:::::::::
ADRs 'nYQ!J'!Jg the KIDNEY
Dark stools Iron slats, bismuth Salts, You must counsel the patient
pancreatitis aminosalicylates, ACE rare but mild if causative agent is stopped
inhibitors, azathioprine, risk factors may include gallstones, alcohol
furosemide, HI receptor consumption, hyperlipidemia, hypercalcemia
antagonist, metronidazole, Presents as sudden onset of upper abdominal pain,
estrogen, propofol, sodium vomiting, tachycardia, fever, jaundice and rigid tender
valproate, sulindac, thiazide abdomen. Serum amylase is raised
diuretics
,
V)
:Renalo.SorCter causative drugs Comments

.
Djutetic6; laxatives Due to reduced renaJ'perfusion

when volume is Due to effects on mechanisms controlling
4ffi to GFR) . ePleled).-ACE inhibitors, diuretics the tone of renal arterioles,
, ,
.
Increased risk in patients with bilateral
renal disease
Monitoring is essential in at-risk patients

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Intrarenal failure
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NSAIDs, bE:ta-lactam antibiotics, Hyper,sensitive, inflammatory reaction"
(acute interStitial
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(furosemide); aliopuririo.i, to renal tubules".
0" ",
nephritis AIN) ." azathioprine, captopril, cimetidine, co- Diagnosed by biC?psy
trimoxazole, phenytoin, rifampicin,
'presents as acute renal failure. Dialysis may
Thiazides, sulphonamides
be required but most patients recover up
to several months after causative agent is
withdrawn
Intermittent rifampicin therapy should be
avoided due to Immunological response.
Re-exposure to rifampicin should be
monitored closely
Intrarenal failure Amphotericin, cyclosporin. A common direct toxic effect
(acute tubular Ciprofloxacin, gentamicin,
necrosis) methotrexate, radiological contrast
.
agents, rifampicin'
Intrarenal failure Gold, penicillamine, NSAIDs Bilateral, immunologically mediated
(glomerulonephritis: . hydral,!zine (acetylator status
damage to glomeruli
..
membranous, minimal important), procainamide Presents as proteinuria, which may
change, lupus
progress to edema and hypoalbuminemia
nephritis)
(nephritic syndrome)
Postrenal failure Chem'otherapy, acyclovir (IV), Due to urinary tract obstruction
methotrexate, sulphonamides may also follow drug-induced
rhabdomyolysis
renal especia,Uy
A problem particularly associated with
compound analgesic preparations including
combinations of-acetaminophen with
salicylates, codeine or caffeine
Nephrogenic diabetes Lithium Does not respond to desmopressin

Serum lithium and creatinine levels should
be monitored regularly
Hemolytic uremic Cyclosporine, mitomycin C, oral Hemolysis leading to obstruction of renal
syndrome contraceptives, metronidazole (in arterioles. Also causes anemia,
children), quinine Thrombocytopenia with risk of severe
hemorrhage
Disc61oration of urine Rifampicin, dopaminergic ;tliis"may a"'.aln;\lng and therefore
"'
drugs, metronidazole, :.paJier:Jtsshouldbe"warned before starting
phenzopyridine, triamterine,bismuth .Hie treatment
pyrantel pamoate"
ADRs affecting sexual function
Sexual dysfunction Causative drugs Comments
,I
Primary infertility Cytotoxics (alkylating agents),
May include a toxic effect on the
anabolic steroids, colchicine, gonads or altered secretion of
diethylstilbestrol, methotrexate, gonadotropin hormones by
NSAIDs'(females), sulfasalazine pituitary gland
(mC!/es)
Anovulation and Anabolic steroids, danazol, isoniazid,

May result from drug-induced
Amenorrhea metoclopramide, cimetidine, hyperprolactinemia
NSAlDs, SSRls,. estrogens,
NSAIDs may inhibit ovulation and

risperidone, spironolactone
should preferably be avoided
around the time of ovulation in
women trying to conceive
I
61-12
----
(1
1. rapid infusion of 2. Oindamycin 3. ASA
. .
vancomycin
4. aozapine 5. Methimazole
Propylthiouracil (PTU)
7. CK-MM
Halothane 9. abrupt discontinuation of

antipsychotic
10. hypertensive crisis 11. decrease renal 12. alpha blockers
perfusion
13. Carvedilol 14. Labetalol 15. TlClopidine
1. Sympathomimetics!pseud 17. Oindamycin
".
Mg antacids
oeohedrine
19. statim 20. Metformin 21. Orlistat
22. anticholinergics 23. opioids 24. antihistamine
25. AIOH 2. Verapamil
"-
Caldun
2. Iron 29. TCA 30. Nitroprussides
31. Nitroglycerin 32. vasodilators 33. Hydralazine
34. CC. 35. Amiodarone 3. Bromocriptine
37. Bleomycin 3. Phenytoin 39. inhibit levodopa conversion to
catecholamine in brain
40. nausea & vomitinR; 41. dil!.italis toxicity 42. low blood oerfusion
....
anabolic
Wffi'ei:"ractd}:s'ih'tf3cle"smbkirii.\- ".
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{impq ence . sterOl $, antic 0 Inerglc,
.... . .
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peripheral vascurar'
. benzodiazepines, spinal cord injury
.
(carbamazepine, gabapentin,
,. TY.\s may used to
phenytoin) digoxin, methyldopa, pr".mlature 'eJaculation
metoclopramid!?,omeprazole,
,
prazos(n, spiron6laetone, thiazide
diuretics
"
Anticoagulants, alprostadil,

Immediate treatment is required

to prevent fibrosis or gangrene
. .,.. ...... '-.;".... ..-......
antlpsychotics (includes atypical),
hydralazine, nifedipine, prazosin,
trazodone
Female orgasm Antidepressants, benzodiazepines,

Patients 'prescribed f1uoxetine or
dysfunction, libido cimetidine, doridine, methyldopa, clomipramine have reported
changes,reduced propranolol, spontaneous orgasm
vaginal lubriCation spironolactone, thiazide diuretics,
trazodone
Reduced libido Spironolactone, cimetidine, oral

libido may be increased rarely by
(reduce sexJal , c6ntraceptives, thiazide trazod9ne, modobemide or'
diuretics, antidepressants levodopa
(particularly SSRls)
Gynecomastia Gi11liiCl1Ae.Clridsspironolaetone,

-""""",.. ,. --'. - ..
lCetoconazole, anabolic"5teroids
Tips
Malignant hyperthermia is caused by? '.
Pre-renal failure may cause due to? (li ) Jl)(...A...-'"
6113
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Syncope is caused by? (1\2,...) P<. - .
MAO inhibitors with pseudoephedrine (sympathomimetics) gives? ('0) (,l.U4 --..--
Neuroleptic malignant syndrome is caused? (
Nitroglycerin'gives?( I 15
What creatin kinase indicates myopathy?, (Ckr of'.'""
Gray baby syndrome caused by? (
Red man syndrome caused by? ( fA-1m} ciA- VCf
Reye syndrome is caused by? ( MA' .
Pseudom:mbranous colitis is mainly caused? L C' Itda ..L
Agranulocytosis is caused by? ( L" prO, II
Hypokalemia + digoxin gives? (4' ) d 1.:1
Levodopa + pyridoxine gives? ( t--\l-\Y Net c...v
Levodopa + Tolcapone ( <1"'
Gingival hyperplasia caused by? ( 0
Pulmonary fibrosis is caused by? ( 3' t J.!i At-Y)'/ocla..J.DV\L I 15).DM[)
Headache is side effect of? ( 3 \ )HI t<rt> 1 4- c.. CO
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What antiplatelets drug gives neutropenia side effect? ( ) -Ii c.l Cp' dJ......e...
constipation is a side effect of? ( M lei d.4 j M L. Cot
Diarrhea is side effect of? ( M j Col 1
Glaucoma is a side effect of? ( $-rnp:41-r y...., \ (Jh.A...
Spironolactone side effect? ( CJ:; ""e(A ..--1
Choose a beta blocker with vasodilator action ( c...e:u.. /4 f 4 t.,
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61-14
Complexation and adsorption
Drug Interactions
-Drug Interactions
t/
exam __
01 with antacids, Ca, and Fe; tetracy ine, bisphosphonates, thyroxin, quinolones
, -. .
CYPdA4 inhibitors; Erythro and c1aritfJrorl\ycin, itra'tonazole;,protease inhi!jitors
(yp 3A4 inducers: phenytoin, phenobarbitals, carbamazepine,
01 with OCP: phenytoin, carbamazepine, topiramate.
Warfarin 01: vitamin K, NSAlDs, anti platelets,
Theophyll;ne 01: age, smok;ng, "-' _I I _. _ , ,_!..<.v,
L.,j-{,flI"",tDI', A-Ck
/l.-.t. ", - L./.-d4t <l--
Pharma 0 I CIn '(}fb
Alteration of Gl flora
Alteration of pH
lA-Iteration Hz blockers and Both Hz blockers and antacids increase gastric pH.
of gastric antacids The dissolution of drugs like ketoconazole and omeprazoJe
pH are reduced, causing decreased drug absorption.
Bi5acodyl and Bisacodyl and antacids should not taken together
antacids
-
"
,
Alteration Antibiotics (e. g Digoxin has better bioavailability after erythromycin.
of intestinal tetracycline's, Erythromycin administration reduces bacterial
flora. penicillin, inactivation of digoxin.
Pseudomem erythromycin) Clindamycin may cause severe P. colitis
.--
branous
,
colitis.
-
Anticoagulants and Cotrimoxazole increase INR in warfarin
-
antibiotics
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Calcium, Quinolones (cipro and levofloxacin) complexes with divalent
magnesium, or cations, causing a decreased bioavailability.
c
aluminium and Tetracycline (must avoid with dairy products), complex with
0
iron salts. divalent and trivalent cation
+-'
Ctl
Bisphosphonates (alendronate): Take empty stomab.
Q}
Levothyroxine separate from iron supplements. u

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0
+-'
Sodium Cation in antacids bind to sodium polystyrene sulphonate, causing Ctl
x
Q}
polystyrene reduced renal clearance of bicarbonate, resulting in systemic
0-
E sulphonate acidosis.
0
u
(kayoxylate)
Cholestyramine Reduce absorption of all drugs, thus all drugs should be separated
and colestipol for 2 to 4 hrs.
Penicillamine
-
and AI and iron
Charcoal Adsorb with other drugs
. .
Higher surface area the higher adsorption
The more pure, the higher adsorption
Alteration of motility/Rate of gastric emptying time
Increased GI Laxatives, Increased Gl motility decreases of drugs
motility cathartics that are absorbed slowly. May also affect the
bioavailability of drugs from controlled-release
products.
Decreased Anticholinergic Propantheline decreases the gastric emptying of
GI motility agents acetaminophen, delaying acetaminophen absorption
--- .........
from the small intestine.
Alteration of metabolism in GI tract
Inhibition MAOls: MAOls inhibit metabolism of tyramine containing foods in the
of drug Phenelzine intestine, leading to hypertension caused by high tyramine levels:
metabolism Tranycyprami (hypertensive crisis).
in infestinal ne Levodopa converts into dopamine leads to peripheral side effects
cells such as nausea and vomiting
Grapefruit Inhibit' the metabolism of drugs substrate with CYP3A4
juice Avoid grapefrUit juice with Atorvastatin, lovastatin and
simvastatin (ALS), DHP-CCB, amiodarone, carbamazepine
62-2
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Drug Interactions
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Alteration of distribution: Phenytoin and valproic acid
Stimulation of metabolism
Warfarin and phenobarbital
Warfarin and carbamazepine -7 carbamazepine increase clearance ofw'arfarin
Oral contraceptives and phenobarbital, and rifampin-
Smoking -7 induces CYP1A2
Pyridoxine induce metabolism of levodopa,
Metabolism inhibitors: Theophylline and macrolide: Macrolides such as
erythromycin, c1arithromycin inhibit -7 CYP3A4,
Phenytoin and folic acid: Phenytoin enhances folic acid metabolism gives
,
megaloblastic anemia.
Mercaptopurines (azathioprine) and allopurinol: Allopurinol inhibit xanthine oxidase enzyme.
This enzyme is essential for the metabolism of azathioprine. Thus increase concentration of
azathioprine, and thjs can lead to azathioprine toxicity,
Reduce 1/3 or 1/4 dose of azathioprine in patient who are using allopurinol.
Reduced or delayed Increased Not affected by food
NSAIDs Griseofulvin Theophylline
Aspirin Metoprolol Metr.onidazole
.
Acetaminophen Phenytoin
Antibiotics (tetracycline and Propoxyphene
penicillin) Dicumarol
Ethanol Morphine
Pharmacodynamic interaction: Drugs having opposing pharmacological effects
Diuretics and insulin -?diuretic gives hyperglycemia whereas insulin gives hypoglycemia
Drugs having similar pharmacological effects ."
Sedative and alcohol:-Benzodiazepine and alcohol
Anticholinergic drugs: Anticholinergic drugs with sedatives
62-3

; Drug
. ;

-
O'icYd

Antihypertensive drugs (sildenafil, tadalafil, vardenafil and nitrates). Combination of
PDE
s
inhibitors with nitrates gives severe hypotension. .
NSAIDs: Two NSAIDs should not be combined
Alteration of electrolyte interaction: Digoxin and diuretics -7 Hydrochlorothiazide and
furosemide cause hypokalemia, thus if its combine with digoxin can give digitalis toxicity.
ACE Inhibitors and potassium sparing diuretics-7 Both ACE inhibitors with potassium diuretics
cause hyperkalemia.
Lithium and diuretics: Diuretics gives side effect of hyponatremia (,J.,Na), thus this increase
lithium levels, and it can lead to lithium toxicity.
Interaction at receptor site: MAOI and sympathomimetics (pseudoephedrine,
xylometazoline)-7 MAOI and sympathomimetics such as pseudoephedrine, and
xylometazoline combination can lead to hypertension crisis.
MAOI and TCAs combination can give serotonergic syndrome.
MAOI and SSRls combination can give serotonergic syndrome.
TCA + SSRI
55Rl + venlafaxine
Alcohol and drug interactions
Must avoid alcohol
Metronidazole -7 gives disulfiram like reaction
Disulfiram -7 gives disulfiram reaction
V Chlorpropamide (sulfonylureas) -7 gives disulfiram like reaction
Metformin -7 gives lactic acidosis
. Phenothiazines (antipsychotic) -7 gives .sedation .
Benzodiazepine, opioids -7 gives sedation
Antihistamines -7 gives sedation
-I
Drug that can lead to complication if combined with alcohol
Cimetidine may increase ethanol blood concentration (cimetidine increases alcohol
absorption in GI, and reduce activity of alcohol dehydrogenase enzyme)
Methadone-may increase sedation.
/. Acetaminophen-7 liver toxicity
Aspirin-7 may cause increase GI bleeding
Methotrexate -7 may increase hepatotoxicity
Insulin-7 may increase hypoglycemia
Glyburide-7 prolong hypoglycemia, and disulfiram like reactions.
Glipizide-7 prolong hypoglycemia, and disulfiram like reactions.
Ketoconazole-7 may results in disulfiram reaction (flushing, vomiting, increased
respiratory rate, tachycardia)
62-4
1. Bupropion 2. 3. Fluvastatin
4. Lovastatin 5. Simvastatin 6. Atorvastatin
7. Carbamatepine
,.
gives disulfiram 9. Severe orthostatic
increase clearance of reaction hypotension
warfarin
10. hypertension crisis 11. MAOI +TCA 12. MAOI +SSRI
13. MAQI+ MAQI 14. Nitrates 15. alpha blockers
16. Lactic acidosis
Nitroglycerin-7may result in hypotension
Paroxetine-7may result in increase risk of impairment of motor and mental skills.
Sertraline.-7 may result in increase risk of impairment of motor and r;nental skills.
Venlafaxine-7may result in increase risk of eNS effects.
:=:. Warfarin-7 increase INR or PT (acute alcohol) or decrease (chronic) INR or PT
Zaleplon-7 may result in impaired psychomotor function
Zolpidem-7 may result in increase sedation
Phenytoin-7 decrease phenytoin serum concentration; increase seizure potential, and
additive eNS depressant effect.
Morphine-7 may result in increased sedation (during withdrawal period, alcohol may
Accelerate withdrawal effect of medication)
may increase risk of seizures.
Cefotetan (2
nd
gen) -7disulfiram like reaction
cefometazole(2
nd
gen) -7disulfiram like reaction
Cefoperazone-(3,d gen) -7disulfiram like reaction.
Food-drug interactions
. Food can increase, decrease, or not affect the absorption of drugs.
Food can influence the bioavailability of a drug from a modified-release dosage form (eg.,
controlled release, delayed released (enteric coated) rather than from an immediate-
release dosage form.
Complexation and adsorption cif the drug in the GI tract with another food element is a
common drug interaction that reduce the extent of drug absorption. For example,
quinolone antibiotics and tetracycline complex with calcium (found in milk products).
Food can be metabolized by the same liver enzymes that metabolize drugs, causing
enzyme inhibition or induction, and resulting in toxic or sub therapeutic drug levels. For
example, grapefruit and valencia oranges inhibit the CYP3A4 isoenzyme system, causing
increased levels of substrate drugs such as saquinavir, indinavir, midazolam,nifedipine,
lovastatin, cyclosporine, carbamazepine, and verapamil.
Food can pharmacodynamically antagonize the effect of some drugs. For example,
spin(lch provide dietary sources of vitamin K, which antagonizes the effect of
. warfarin. 1<- ""II. u-<l"'"
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Drug Interactions

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W, "')1- CAwtL
Sildenafil caRRet Be cembinea 'N+th prazosin it.eel:l'Se? l1' )
MAOI, & tyramine gives? ( I () )
Serotoni!:1ergic syndrome is caused by? ( J I
A patient using sildenafil should avoid? ( ", If"
Sildenafil + nitroglycerin can cause? ) -.
What statins should be avoided taking with grapefruit juice? ( 1,6"/ (. )
What antidepressant can be used with MAOI? ( , )
What statins should be taken with food? (j I ' r= L
Warfarin + carbamazepine (7 )
Metronidazole + alcohol (<i" )
Metformin + alcohol )
List of drug that should be taken empty stomach
Atracycline

v1"afirlukast
Etidronate

vPP1s, levothyroxine
v*on supplement
/
62-6
Therapeutic Drug Monit,oring
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Therapeutic Drug Monitoring
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Questions Alerts!
Anticoagulants: Warfarin, Heparin and lMWH
Thyroid hormones: Serum TSH, TT4, FT4, TT3
Antipsychotic drugs: CBC, Weight '"
lithium: serum levels <1.5 mEq/l
Statins: lFT and CK-MM
Amiodarone: chest x+ray, eye exam, serum TSH
laboratory test Therapeutic ranges Monitoring guidelines
,
monitored of test
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Serum amikacin peak 20-25 mcg/ml Wait until the administration of the third dose to
trough 5-10mcg/ml check drug levels. Obtain blood for peak Jevel30
Serum gentamicin/ minutes after I.V. infusion or 60 minutes after I.M.
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tobramycin peak 4-8 mcg/ml administration. For trough levels, draw blood just
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trough Serum 1-2mcg/ml 0.6 -1.3 before the next dose. Dosage may need to be
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creatinine mg/dl adjusted accordingly. Recheck after three doses.
Monitor creatinine clearance and BUN levels and a

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urine output for signs of decreasing renal function
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Serum creatinine-
0.6-1.3 mg/dl
Monitor serum creatinin, BUN, and serum
BUN
5-20 mg/dl
electrolyte levels at least weekly during therapy.
Serum electrolytes Potassium: 3.5-
Also regularly monitor blood counts and liver
(esp'edally 5mEq/L
function test values during therapy.
and magnesium) Magnesium: 1.5-
2.5mEq/L
Sodium: 135-145
mEq/L
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Chloride: 98-106
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Uver function tests mEq/L
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CBC w/ differential and
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platelets
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WBC with differential
Specimen cultures and sensitivities will determine
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cultures and *****
the cause of the infection and the best treatment.
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Monitor WBC count with differential weekly during 0
sensitiviti es .
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therapy.
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Serum creatinine FBSL: 5 to 6 mmol/L
Check renal function & hematologic parameters
Fasting seruf!1 glucose
before initiating ther?py and at least ?r.'nually
Glycosylated HbA1C: 5.5% to 7% thereafter if patient has impaired renal function,
hemoglobin (HbA1C) of total hemoglobin
don't use metformin because it may cause lactic
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CBC
acidosis. Monitor response to therapy by
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Test shows past 3 periodically evaluating fasting glucose and
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mo BSL
glycosylated hemoglobin levels. A patient's home
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monitoring of blood glucose levels helps monitor bO C1J
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Test q6months for compliance and response.
patient on insulin Decrease mortality
Test q1yr for type II
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WBC with differentiar Gives Obtain WBC count w/ differential before initiating
C1J .or CBC therapy, weekly, during therapy, and 4 weeks after
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discontinuing the drug.
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Serum digoxin 0.8 to 2 mg/ml Check serum digoxin levels at least 12 hours, but
Serum electrolytes Potassium: 3.5 to 5 preferably 24 hours, after the last dose is
(especially potassium, mEq/L
administered. To monitor maintenance therapy,
magnesium, and Magnesium: 1.7 to check drug levels at least 1 to 2 weeks after therapy
calcium 2.1 mEq/L is initiated or changed. Make anY,adjustments in
/ Serum creatinine Sodium: 135 t0145 therapy based on entire clinical picture, not solely
x
mEq/L on drug levels. Also, check electrolyte levels, renal 0
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'0 Chloride: 98 to 106 function periodically during therapy.
mEq/L
Calcium: 8.6 to 10
.
mg/dl
0.6 tol.3 mg/dl
63-2
serum electrolytes Potassium: 3.5 to 5 To monitor fluid and electrolyte balance. perform
mEq/l baseline and periodic determjnations of serum
serum creatinine Magnesium"; 1.7-2.1 electrolyte, serum calcium, BUN, uric acid, & serum
BUN mEq/l glucose levels.
Uric acid Sodium; 135-145
Fasting serum glucose mEq/L
Muscle pain Chloride: 98-106 u

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mEq/l
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caldum: 8.6-10
mg/dl
0.6-1.3 mgfdl
5-20 mgfdl
2-7 mg/dl
70-110 mg/dl
Hematocrit Women: 36% to After thef"apy is initiated or changed, monitor the

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hematocrit twice weekly for 2 to 6 weeks until
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dose determined. Monitor hematocrit regularly
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thereafter.
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Serum ethosuximide 4 to 100 mcg/ml Check drug level 8 to 10 days after therapy i,
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initiated or changed
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laboratory test Therapeutic ranges of test Monitoring guidelines
monitored
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Serum lipids Total cholesterol: < 5 Therapv is usuallV withdrawn after 3 months
mmol/l if response is inadequate. Patient must be
Gemfibrozil LDL <2.2 mmol/L fasting to measure triglvcerides level.
(Fibrates) HDl women: >0.9 mmol/l
Triglycerides: <3.2 mmol/L
Glucose
Niacin
Increase BSl
I Activated partial 1 to 2 times control When drug is given by continuous IV infusion,
thromboplastin time check aPTT q4 hours in the early stages of
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(aPTT) therapy when drug is given by deep S.c.
injection, check apn4 to 6 hours after
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injection
Serum lipids CK-MM is indicator of Perform liver function tests at baseline, 6 to
liver function tests myopathies 12 weeks after therapy is initiated or
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(LFT) changed, and periodicallv thereafter. If
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and creatin kinase
adequate response isn't achieved within 6 - u --
C> :3,g
(eK) ~ ~ weeks consider changing the therapy
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63-3
www.phannacyPrep.com Therapeutic Drug Monit?ring.
Fasting 5 to 6 mmol/L Monitor response to therapy by evaluating
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5.5 to.5% of total serum. glucose and glycosylated hemoglobin
glucose .
glycosylated hemoglobin levels glycosilated hemoglobin level is a good
hemoglobi!, (HbAiq
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long-te'rm control. A patient's c
h9me of blood glucose levels help

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measure compliance and response -
Serum lithium Serum levels: 0.8 to 1.5 Ch,ecki.ng blood lithium levels is crucial to the
Serum creatinine mEq/L safe use of the drug. Obtain serum lithium
CBC levels immediately before next dose. Monitor
Serum electrolytes K: 3.5 to 5 mEq/1 levels twice weekly until stable. Once at
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(esp Kand Na) Mg: 1.7 to 2.1 mEq/1 steady state, levels should be checked
::> fasting serum glucose Na: 135-145 mEq/1 weekly; when the patient is on the
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thyroi? function tests CI: 98-106 mEq/1 appropriate maintenance levels should
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70-110 mg/dl be checked every 2-3 months. Monitor serum
TSH: 0.5-5.4 microU/ml creatinin, serum electrolyte and fasting serum
T3:80 to 200ng/dl glucose levels; CBC and thyroid function test
5.4 to 1l.5mcg/dl before therapy is initiated and periodically
during therapy.
Serum methotrexate Normal elimination: Monitor methotrexate levels according to
CBC with differential <10micromol 24 hours dosing protocol. Monitor CBe differential,
Platelet count post dose
'. platelet. count and liver and renal function
Liver function tests <1 micromol 48 hours tests more frequently when therapy is
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Serum creatinine postdose initiated or changed and when methotrexate
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Chest x-ray <0.2micromol 72 hours levels may be elevated such as when the
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postdose patient is dehydrated.
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150-450x10
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/mm
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O.6-1.3mg/dl
Serum phenytoin 10 to 20 mcg/ml Monitor serum phenytoin levels immediately
CBC before next dose and 2 to 4 weeks after
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therapy is initiated or changed. Obtain a CBe
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at baseline.and monthly early in therapy.
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Watch for toxic effects at therapeutic levels. OJ
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Adjust the measured level for
hypoalbuminemia or renal impairment, which
can increase free drug levels.
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Serum potassium 3.5 to 5mEq/L Check level weekly after oral replacement
::l OJ therapy is initiated until stable and every 3 to
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Serum procainamide 4-8mcg/ml (procainamide) Measure procainamide levels 6-12 hours after
5-30mcg/ml (combined a continuous infusion is started or
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Serum N- procainamide and NAPA) immediately before the next oral dose "tJ
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acetylprocainamide
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combined (procainamide and NAPA) levels
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can be used as an index of toxicity when renal
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eBC impairment exists. Obtain eBe periodically 0
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during'rong-term therapy.
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63-4
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Therapeutic Drug Monitorrr{g
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Serum quinidine 2-6mcg!ml
Obtain levels immediately before the next
CBC

oral dose and 30-35 hours after therapy is
Liver function tests
*
initiated or changed periodically obtain blood
Serum creatinine 0.6-1.3mg/dl
counts, liver and kidney function tests values
Serum electrolytes K:3.5-5 mEq/l
and serum electrolyte levels
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(esp K) Mg: l.7-2.1mEq/l
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CI: 98-106mEq/l
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Fasting serum 70-110mg/dl
Monitor response to therapy by periodically
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glucose 5.5-8.5% of total
evaluating fasting glucose an9 glycosalated
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Glycosylated hemoglobin
hemoglobin levels, patient's home
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hemoglobin
monitoring of blood glucose levels helps
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VI m measure compliance and response.
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Serum theophylline 10 to 20 mcg/ml
Obtain serum theophylline immediately
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0 product and at least days after therapy is
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initiated or changed
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Thyroid function TSH: 0.5 00.5'.4 ,microU/ml
1VJ0nitor thyrojd function tests every 2-3
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tests ~ 8,0 tp .20p flgfdl
weeks until appropriate maintenance dose is
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'Serum vancomycin 20-35 mcg/ml (peak)
Serum vancomycin levels may be checked
5-10mcg/ml(trough)
withthe third dose administered, at the
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Serum creatinine 0.6-1.3mg/dl
earliest. Draw peak levels half hour after the
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IV infusion is completed. Draw trough levels
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immediately before the next dose is
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administered. Renal function can be used to c \ ,
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> adjust dosing and intervals
For an acute MI, atrial
Check INR daily beginning from 3 days after
. fibrillation, treatment of therapy is initiated continue checking it until
.
pulmonary embolism, therapeutic goal is achieved and monitor it
prevention of systemic periodically thereafter. Also, check levels 7
PT and embolism, tissue heart days after any change in warfarin dose or
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INR 2 to 3 valves, valvular heart concomitant, potentially interacting therapy. .;::
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disease, or prophylaxis or
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3:
treatment of venous
thrombosis.
'2 to 3 for mechanical
prosthetic valves or
,
recurrent systemic
embolism: 2.5-3.5
Note: ***** For those areas marked with asterisks,
the following values can be used:
Hemoglobin: Women: 12-16 gldl Differential: Neutrophills:
Men: 14-18 g/dl Bands: 0%-8%
Hematocrit: Women: 37%-48% Lymphocytes: 16%-45%
Men: 42%-52% Monocytes: 4%-10%
RBCs: 4-5.5 x 106/mm3 Eosinophills: 0%-7%
WBCs:5-10 x 103mm3 Basophills: 0%-2%
* For those areas marked with one asterisk
the following values can be used:
ALT: 7-56 unilsIL
AST: 5-40 unilsIL
Alkaline phosphatase: 17-142 units/L
LDH: 6-220 unitsIL
GGT: <40 unils/L
Total bilirubin: 0.2-1 mg/dl
63-5
www.pharmacyprep.coni.
Tips
1. LFT & CK 2. shows BSL for past 3 3. serum TSH
months
4. CHF S. liver and renal 6. lactic acidosis
diseases
7. blood work 8. renal function 9. wac
10. CBC 11. 0.8 to 1.5 meq/L 12. PT & INR
13. 10 to 20 mcg/ml 14. increase CL=smoking 15. oliguria, CrCI<SO
age 1 to 9 ml/min, increase BUN
16. Post dose antibiotic 17. Require low dose for 18. Have no oral dosage
effect UTI form
19. Treatment of anemia 20. Folic acid 21. CK-MM
in chronic renal failure
lithium normal serum levels ( \,) 0 '<6 -\-t)'. S' L-
Warfarin monitoring ( PT 4-"J..-rlR
Statin monitoring ( I) L F1' d M
Serum levels of phenytoin ( 10 -1. 0 M OIl .
Factors that affect theophylline clearance (11) i7\ C 1 ::. J / ..... j
HbA1C test monitoring ( 2-) '-"J as L /itt-- pe..:t<l-.J
Symptoms of renal disease (I')) I < ...." ......." .,...a.t:( Bf'-t
Monitoring. hypothyroidism ( ..s ) -r SJ-l
What laboratory tests indicates myopathies? (,!.J. C. k' - M .
What supplements recommended with phenytoin therapy? ( .,Lu) F &t L J
Amino glycosides have? ( I" ) P Av-h1,.'0
Metformin is contraindicated in? C5,<0) 1.'VVL-4- , 4<...cLD'-J
What is true about erythropoietin's? (j ) eli- ''1 ,i.LWlf J-J-
Clozapine mechanism & monitoring (I ).,g t f-9C-, e.,BC
Propylthiouracil (PTU) and methimawyshould be monitored for? ( ) C-.!3 C-
Vancomycin is monitored for? ( ) tu.,J,.."1
A-mlo&ataiA) J
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63-6
Safety ofMedications in Special Populations
Safety of Medications in Special
.,
eopulations
Geriabic Population
Drug absorption:
Rate of may be altered in some patient
Extent of No effect
I
64
Decrease with age
Acid secretion
OJ motility
Renal function (CrCl)
Serum albumin
Total body water
Cytochrome P450 enzyme
First pass metabolism
Note; serum creatinine is not a good predictor because creatinine production decreases
ags. e
Increase with age
Gastric pH (basic) or achlorhydric
Body fat/lean muscle mass ratio
Phannacokinetic factors
Calcium supplements:
Calcium supplements:;ROO mg/day and vitamin D 800 ru
Calcium carbonate is required acidic medium, thus it is not preferable in seniors.
Calcium citrate is recommended
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Safety of Medication,s in
Calcium carbonate takes in divided doses
- Distribution:
Decrease in total body water: Decreases water distribution ofwater:-soluble drugs.
(e.g., acetaminophen)
Lipid soluble drugs (diazepam, propranolol) distribution increases.
Albumin levels are decreased with age therefore albumin bound drugs have
greater free concentration.
Renal function: Renal function (renal excretion) decreases with age.
50% decrease of renal function by age of 70.
Geriatric patients have sensitive reaction drugs cause.
Anticholinergic effects and should be ilv9rt3e"d:'
Vitamins in seniors
Vitamin B12 supplements is recommended
Predictors of adverse drug effects in elderly
A. Age 85 years or older
B. Multiple chronic medical conditions (6 or more)
C. Creatinine Clearance <50 ml/min
D. Low Body Mass Index
E. Polypharmacy
1. Medications number nine or more
2. More than 12 medication doses daily
II. Methods to improve compliance to medication.
A. Reduce number of daily doses (once daily is best)
B. Time doses to meal times
C. Establish partnerships to ensure compliance
1. Patient
2. Family (educate on indications and adverse effects)
3, Pharmacists
4. Home health aids
D. Use devices that aid taking of medication
1. Pill boxes and pill calendars
2. Label containers with type
3. Pill contai.ners should open easily
4. Keep accurate medication list
E. Ensure easy access to medications
I. Affordability
2. Medication delivery
F. Evaluate for patient factors affecting compliance
I. Dementia
2. Major Depression
Medications to use lower do'sages (decreased clearance) due to decreased renal
clearance in the elderly
64-2,
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Aminoglycosides
Vancomycin
Fluoroquinolones
Penicillins
Imipenem
Digoxin
ACE Inhibitors
Beta Blockers (Atenolol, Nadolol)
SOlalol
Glyburide
Ranitidine, Cimctidine, Famotidine
Lithium
Decreased hepatic clearance in the older adults
Benzodiazepines
Lidocaine
Phenytoin
Celecoxib (Celebrex)
Theophylline
Imipramine or Desipramine, Trazodone
Isoniazid
Procainamide
Medications to avoid in older adults
Anticholinergic Agents
Sedating Antihistamines (e.g. Benadryl, Periactin)
Ticlopidine
Methyldopa
Reserpine
Disopyramide (Norpace)
Meperidine (Demerol)
Propoxyphene (Darvon)
Barbiturates (e.g. FiorinaI, Nembutal, Seconal)
Benzodiazepine (e.g. Librium, Valium, Dalmane, Ha1cion)
Meprobamate
Sedating Antidepressants (Elavil, Doxepin, Imipramine)
Methylphenidate (Ritalin)
Antiemetics (Phenergan. Tigan)
OJ antispasmodics (e.g. Donnatal, Bentyl, Levsin)
Antidiarrheals (Lomotil)
Urinary antispasmodics (Ditropan)
64-3
Safety of Medications in Special Populations.
NSAIDs (especially indocin, ponstel, feldene)
Drugs in-Pregnancyand Lactation
Most critical period in pregnancy for drugs therapy: 14 to 56 days (2 to 8
weeks).
Most critical period of fetotoxic drugs: N.inth week to
Embryo toxic Results in termination of pregnancy
Drugs Examples: Honnones (estrogen, progestin, androgen), oral contraceptives,
plan B, ACE I, ARBs, statins, misoprostol and antidiabetic drugs
Teratogenic
Drugs
FDA
classification
Drugs not
used in
pregnancy
Risk is highest in 1SI trimester. Teratogenicity causes mental and physical
deformation to the developing fetus.
Examples: Accutane (isotretinoin), Retin A (tretinoin), warfarin, tetracycline,
finesteride, dutasteride, and quinolones.
Category A -7 Safe
Category B -7 Animal studies showed safe. Can be safe in human?
Category C -7 Animal studies shows risk, but human data not available?
Category D --) Demonstrate risk to fetus
Category X -7 Positive evidence of risk to fetus
The positive evidence of risk to fetus. Contraindicated in woman who are
pregnant or who may become pregnant.
Vitamin A derivatives: isotretinoin, and tretinoin
ACE inhibitors, ARBs, and statins
Warfarin: causes Fetal Warfarin Syndrome (fIrst trimester)
Estrogen and androgen: Can cause genital tract mal format jon.
Methimazole and carbimazole.
Leflunomide
Finasteride and dutasteride
Methotrexate and chemotherapeutic drug
Alcohol in large quantities can cause abnormalities in growth, cardiac,
skeletal development: Fetal alcohol syndrome (FAS)
Tetracycline--) Mottling of teeth (taken by mother after 18 week of
pregnancy).
Metronidazole-7 Use in first trimester must be evaluated carefully.
Completely contraindicated for Trichomoniasis in 1st trimester.
Quinolones-7Not recommended in arthropathies
(cartilage erosion)
64-4

Lithium -7cardiovascular malfonnations
Drugs in lactation
Anticonvulsants: contraindicated in first trimester. Phenytoin; Valproic acid;
Sodium valproatc. Phenytoin -7 cleft-palate, spina-bifida
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Safety of Medications in Special Populations www.phannacyprep.com
Factors that effect on dtuS secretion into breast milk
Lipid solubility
Membrane penneation
Molecular weight
.Can be used in Pregnancy:
omycm -
Cephalexin-
Ampicillin-
Amoxicillin
Anticancer or antineoplastics are contraindicated in pregnancy
Finasteridc-7cause abnormalities in male genetalia, should avoid contact
with men who are on this medication
The most teratogenic antibiotic:
Nalidixic acid derivative as quinolone
Amantadine
Sulfa drugs
Tetracycline
Nitrofurantoin
Dr'ug of choiceS in. pregnancy:
'Nausea and'vomiting (morning sickness) -7 Diclectin (vitamin B
6
+doxylamine)
Anti hypertension -7 Methyldopa, hydralazine, and labetalol
Diabetic Type I and 11 -7 Insulin
Epilepsy -7 Carbamazepine
Hyperlipidemia -) Cholestyramine
Hyperthyroidism -) Propylthiouracil (PTU)
Ulcerative colitis -7 5-ASA or sulphasalazine
Constipation -) Psyllium (bulk laxative), stool softener
Stomach ulcers -) Antacids, H2 blockers, and PPJ
Vulvovaginitis Candida -7 Clotrimazole (except 1$1 trimester), miconazole or nystatin
Migraine -7 Acetaminophen, NSAID's
Depression -7 Fluoxetine
Urinary tract infections -7 Cephalosporins (cephalexin) and Nitrofurontoin
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Tips
1) Eat in small & frequent 2) Urinary tract infection 3) Diclectin
meals, 'avoid fat, oily' and
spicy food, avoid heavy
meals
4) decreased renal 5) Dimenhydrinate 6) body fat/lean muscle
,clearance, mass ratio
7) fiber diet 8) stool softeners 9) lactulose
10)Calcium citrate 11) Vitamin BI2 12)Drugs must be able to
diffuse across lipid barriers
to enter the fetus
13)ginger root 14) There is decreased rate 15) Neurotubular defect
of absorption as well as
change in drug distribution
16)Category X 17) Folic acid & 18) morning sickness
multivitamins ,
Phannacokinetics factors that increase with age? ( )

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Calcium supplements that are preferably given to seniors? ( )' b.
What vitamin supplements are recommended to seniors? ( ) II " , t1 n,L ttl
What therapy recommended for constipation in seniors? ( .., c, 'F; beAM ,..s\ce
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Drugs that should be discontinued in pregnancy? ( ,t ) 'f- "-t.-
Supplements that should be recommended in pregnancy? ( t1 ) 'FD' I Co AcI
Folic acid supplements in pregnancy prevents? ( ,r)
Nausea and vomiting in pregnancy also referred as? MC9lv\'ll 5 ch ---'
Drug of choice therapy nausea and vomiting in pregnancy is? (j ) CD r d LA-- uk-
aTC drug therapy against nausea and vomiting in pregnancy include? ( 5 ) &-1
Self care that is recommended for nausea and vomiting in pregnancy? ( , )
i OJw+. Cranberry juice is used against? ( )...) U-r..l
How do phannacokinetic characteristics in the very young differ from that of an
adult? ( ,
What phannacokinetic characteristics change in elderly? ( , 4 ,
What is the significance of the placental barrier? ( \ . . J
Herbal products that is recommended for nausea & vomiting in pregnancy? (
64-6
Safety of Medications in Special Populations

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A pregnant comes to your phannacy, and wants to know, which of the' following
vitamin supplements can be toxic in pregnancy? ,
A)Vitamin B
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B)Vitamin D'C)Vitamin C D)Vitamin A!
Ans: D
A man comes to your phannacy for his wife because she is ill, not eating food and not
talking for the past two day. She is pregnant and have severe nausea vomiting. She has
vomited time in last two days. What to do?
A) give dimenhydrinate B)refer dOctor"get Dicleetin prescription C)refer to emergency
d)recommend self care
E) give oral rehydration solution
Ans: B
A pregnant women has mild to moderate nausea and vomiting. What is the correct self
care? .
A) minimize meals and take liquid food
B) take large meals and reduce the time of meals
v) take small and frequent meals
D) increase activity at the time of nausea and vomiting
E) none
Aus: C
64-7
www
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of Medications in, .Pop';1lations
Safety of Medications in
Populations
GeriatricPopulation
Pharmacokinetic factors
Increase with age
Gastric pH (basic) or achlorhydric
Body fat/lean muscle mass ratio
Decrease with age
Acid secretion
GI motility
Renal function (CrCI)
Serum albumin
Total body water
Cytochrome.P450 enzyme
First pass metabolism
Note: serum creatinine is not a good predictor because cre.atinine production decreases
with age.
Drug absorption:
Rate of may be altered in some patient
Extent of No effect
Calcium supplements:
Calcium supplements: 1500 mg/day and vitamin D800IU
Calcium carbonate is required acidic medium, thus it is not preferable in seniors.
Copyright 2000-2012 TIPS Inc. Unauthorized reproduction oflhis manual is prohibited. This 64-1
manual is being used review sessions conducted by PharmacyPrep.
,
www.pharmacyprep.com Safety ofMedications in Special Populations
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Calcium citrate is recommended
calcium carbonate takes in divided doses
Distribution:
Decrease in total body water: Decreases water distribution of water-soluble
drugs. (e.g. acetaminophen)
lipid soluble drugs (diazepam, propranolol) distribution increases.
Albumin levels are decreased with age therefore albumin bound drugs have
greater free concentration.
Renal function: Renal function (renal excretion) decreases with age.
50% decrease of renal function by age of 70.
Geriatric patients have sensitive reaction drugs cause.
Anticholinergic effects and should be avoided:
Vitamins in seniors
Vitamin B12 supplements is recommended
Predictors of adverse drug effects in elderly
A. Age 85 years or older
B. Multiple chronic medical conditions (6 or more)
C. Creatinine Clearance <50 mlfmin
D. low Body Mass Index
E. Polypharmacy
1. Medications number nine or more
2. More than 12 medication doses daily
II. Methods to improve compliance to medication.
A. Reduce number of daily doses (once daily is best)
B. Time doses to meal times
C. Establish partnerships to ensure compliance
1. Patient
2. Family (educate on indications and adverse effects)
3. Pharmacists
4. Home health aids
D. Use devices that aid taking of medication
1. Pill boxes and pill calendars
2. label containers with large type
3. Pill containers should open easily
4. Keep accurate medication list
E. Ensure easy access to medications
1. Affordability
2. Medication delivery
F. Evaluate for patient factors affecting compliance
1. Dementia
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Copyright 0 2000-2012 TIPS Inc. Unauthori;.:cd reproduction of this manual is prohibited. This
manual is being used during review sessions conducted by PhannacyPrep.
64-2

2. Major Depression
. ,
Medications to use lower dosages (decreased clearance) due to decreased renal
clearance in the elderly
Aminoglycosides
Vancomycin
Fluoroquinolones
Penicillins
Imipenem
Digoxin
ACE Inhibitors
. Beta Blockers (Atenolo!. Nadolol)
Sotalol
Glyburide
Ranitidine, Cimetidine, Famotidine
Lithium
Decreased hepatic clearance in the older adults
Benzodiazepines
lidocaine
Phenytoin
Celecoxib (Celebrex)
Theophylline
Imipramine or Desipramine, Trazodone
Isoniazid
Procainamide
Medications to avoid in older adults
Anticholinergic Agents
Sedating Antihistamines (e.g. Benadryl, Periaetin)
Ticlopidine
Methyldopa
Reserpine
Disopyramide (Norpace)
Meperidine (Demerol)
Propoxyphene (Darvon)
Barbiturates (e.g. Fiorinat Nembutal, Seconal)
Benzodiazepine (e.g. Ubriurn, Valium, Dalmane, Halcian)
Meprobamate
Copyright 0 2000-2012 TIPS Inc. Unauthorized reproduction of this manual is prohibited. This 64-3
, .
Drugs in Pregnancyand I.Lictation
Sedating Antidepressants (Elavil, Doxepin, Imipramine)
Methylphenidate (Ritalin)
Antiemetics (Phenergan, Tigan)
GI antispasmodics (e.g. Donnatal, Bentyl, levsin)
Antidiarrheals (Lomatil)
Urinary antispasmodics (Ditropan)
NSAIDs (especially indocin, torado!, ponster, feldene)
www.pharmacyprep.cortl
Examples: Accutane (isotretinoin), Retin A (tretinoinj, warfarin, tetracycline,
finesteride, dutasteride, and quinolones.
Finasteride and dutasteride
Methotrexate and chemotherapeutic drug
Alcohol in large quantities can cause abnormalities inwowth, cardiac,
Most critical period in pregnancy for drugs therapy: 14 to 56 days (2 to 8
weeks).
Most critical period offetotoxic drugs: Ninth week to birth
Risk is highest in 1
st
trimester. Teratogenicity causes mental and physical
deformation to the developing fetus.
Results in termination of pregnancy
Examples: Hormones (estrogen, progestin, androgen), oral contraceptives,
plan B, ACE I, ARBs, statins, misoprostol and antidiabetic drugs
Category A -7 Safe
Category B -7 Animal studies showed safe. Can be safe in human?
Category C -7 Animal studies shows risk, but human data not available?
Category 0 -7 Demonstrate risk to fetus
Category X -7 Positive evidence of risk to fetus
The positive evidence of risk to fetus. Contraindicated in woman who are
pregnant or who may become pregnant.
Vitamin A derivatives: isotretinoin, and tretinoin
ACE inhibitors, ARBs, and statins
Warfarin: causes Fetal Warfarin Syndrome (first trimester)
Estrogen and androgen: Can cause genital tract mal formation.
Methimazole and carbimazole.
leflunomide
Embryo toxic
Drugs
Teratogenic
Drugs
FDA
classification
Category X
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64-4
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Drugs not
used in
pregnancy
skeletal development: Fetal alcohol syndrome (FAS)
Tetracycline7 Mottling of teeth (taken by mother after 18 week of
pregnanCy).
Metronidazole7Use in first trimester must be evaluated carefully.
Completely contraindicated. for Trichomoniasis in 1
st
trimester.
Quinolones-7Not recommended in pregnanCY7causes arthropathies
(cartilage erosion)
Lithium 7cardiovascular malformations
contraindicated in first trimester. Phenytoin; Valproic acid;
Sodium valproate. Phenytoin 7 cleft-palate, spina-bifida
Anticancer or antineopfastics are contraindicated in pregnancy
Finasteride7cause abnormalities in male genetalia, shoul9 avoid contact
with men who are on this medication
The most teratogenic. antibiotic:
Nalidixic acid derivative as quinolone
Amantadine
!f . Sulfa drugs
Tetracycline
Nitrofurantoin
Can be used in Pregnancy:
Erythromycin
Cephalexin
Ampicillin
Amoxicillin
Drug of choices in pregnancy:
Nausea and vomiting (morning sickness) 7 Diclectin (vitamin B
6
+doxylamine)
Anti hypertension 7 Methyldopa, hydralazine, and labetaldl
Diabetic Type I and II 7 Insulin
Epilepsy 7 Carbamazepine
Hyperlipidemia 7 Cholestyramine
Hyperthyroi"dism 7 Propylthiouracil (PTU)
Ulcerative colitis 7 S-ASA or sulphasalazine
_Constipation -7 laxative), stool softener
Stomach ulcers 7 Antacids, H2 blockers, and PPI
Vulvovaginitis Candida 7 Clotrimazole (except 1
st
trimester), miconazole Of nystatin
Migraine 7 Acetaminophen, NSAID's
Depression 7 Fluoxetine
Copyright CO 2000-2012 TIPS Inc. Unauthorized reproduction of this manual is prohibited. This 64-5
\
Drugs in lactation
Urinary tract infections Cephalosporins (cephalexin) and Nitrofurantoin
Factors that effect on drug secretion into breast milk
lipid solubility
Membrane permeation
Molecular weight
Safety ofMedications in Special Populations
Tips
PharmacokinetIcs factors that Increase with age? (6)
Calcium supplements that are preferably given to seniors? (10)
What vitamin supplements are recommended to seniors? (11)
What therapy recommended for constipation in seniors? (7,8,9)
Drugs that should be discontinued in pregnancy? (16)
Supplements that should be recommended in pregnancy? (17)
Folic acid supplements in pregnancy prevents? (15)
Nausea and vomiting in pregnancy also referred as? (18)
Drug of choice therapy against nausea and vomiting in pregnancy is? (3)
aTC drug therapy against nausea and vomiting in pregnancy include? (5)
Self care that is recommended for nausea and vomiting in pregnancy? (1)
Cranberry juice is used against? (2)
How do pharmacokinetic characteristics in the very young differ from that of an
adult? (14)
What pharmacokinetic characteristics change in elderly? (14, 6)
What is the significance of the placental barrier? (12)
Herbal products that is recommended for nausea & vomiting in pregnancy? (13)
I) Eat in small & frequent 2) Urinary tract infection 3) Diclectin
meals, avoid fat, oily and
spicy food, avoid heavy
meals
4) decreased renal 5) Dimenhydrinate 6) body fat/lean muscle
clearance, mass ratio
7) fiber diet 8) stool softeners 9) lactulose
lO)Calcium citrate 11) Vitamin 8
12
12)Drugs must be able to
diffuse across lipid barriers
to enter the fetus
13)ginger root 14) There is decreased rate 15) Neurotubular defect
of absorption as well as
change in drug distribution
16)Category X 17) Folic acid & 18) morning sickness
multivitamins
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64-6
Prevention and Intervention in Medication Overdose
. .
Prevention and
in Medication Overdose
Questions Alerts!
Drugs often cause overdose and managing overdose problems
Acetaminophen
Iron
Tricyclic antidepressants
Benzodiazepines
Opioids
ASA
The commonly overdose toxicities associated medications are:
Tricyclic antidepressants
Iron supplements
ASA
Acetaminophen
Opioids
Benzodiazepines
Tricyclic.Antidepressant (TCA)
Overdose symptoms: TCA are extremely toxic in overdose. Consultation with poison
control center is recommended.
Symptoms: Mydriasis and anti-cholinergic symptoms, and severe arrhythmias (AV node).
Treatment is symptomatic and supportive; arrhythmias and CNS involvement pose the
greatest risk.
Toxic dose is variable but in general: 10 to 20 mg/kg may result in serious toxicity and may
be lethal.
In child SO mg dose can manifest the overdose symptoms.
65-1
65-2
Prevention and lntervention in Medication Overdose' www.Phannacyprep.com
Acetyl Salicylates Overdose
Overdose: more .than 4 gJday can cause toxicity
Symptoms of overdose: Mild rapid, deep breathing, nausea, vomiting, vertigo, tinnitus,
flushing, sweating, thirst, and tachycardia. ~ Q.IL vvJJlc.hd\1
Severe acid base imbalance, respiratory alkalosis, metabolic acidosis, fever, hemorrhage,
excitement, and confusion.
Acute ASA intoxication can result from single ingestion of ISO mgJkg or more chronic A$A
intoxication also known as salicylism can occur. Salicylism can occur in high dose >100
mg{kgJday for 2 or more days.
Salicylism most often occurs in elderly, being treated for chronic conditions such as
rheumatoid arthritis
Treatment: Acute symptoms of overdose should be treated by supportive thera"py by
removal of unabsorbed ASA from gut. ASA overdose is treated by NaHC0
3
diuresis
Opioids Overdose
Symptoms: Lethargy, sedation, coma, bradycardia, hypotension, hypoventilation
(respiratory depression), pinpoint pupils (miosis), cool skin, decreased bowel sounds, and
flaccid muscles
Antidote is naloxone, full opioid antagonist
Opioids withdrawal are treated by methadone (partial agonist mu receptors and NMOA
antagonist)
Naltrexone is used for chronic alcohol withdrawal treatment
There are 15% mortalities with overdose of TCA are reported. Toxicity begins within 2
hours of ingestion.
Initial symptoms are mild and can precipitate to eNS and cardiac symptoms.
All cases of accidental, pediatric or adult overdose Should be monitored at healthcare
facility.
Acetaminophen Overdose
In.adult hepatotoxicity'may occur after ingestion of a single dose of more than 7,5 g
(adults), or ISO mg/kg (ch;ldren).
A dose of 10 g or more is potentially fatal. However, reports have indicated hepatic . ~ o
necrosis with single dose of 6 g and death occurring with single dose of 13 g. O:t fJc..Jz.wv J
Treatment: Consider consultation with poison control centers. " .-v-""
Consultation with toxicologist is highly recommended in cases of hepatotoxicity associate<1J_-#,. J
with sub acute acetaminophen overdose, ~
Antidote: Acetylcysteine, this administered within 8 hours.
Iron supplement overdose
Toxicity can occur: 60 milkg may Cause GI symptoms
Symptoms: clinical overdose symptoms are Gl: nausea, vomiting, and diarrhea. melena,
hematemesis may cause hemodynamic instability.
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If GI symptoms does not occur within 6 hours of ingestion suggest, it is non-toxic dose.
Iron overdose should NOT be treated by charcoal.
Antidote is:.deferoxamine (it works by chelation)
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Benzodiazepine
Antidote: flumazenil
Withdrawal symptoms: insomnia, and anxiety
-
Amoxicillin
3 g daily maximum
Symptoms: diarrhea
Nystatin
Nystatin. cream or suspension:30 gram (3 mU) or more can cause stomach upset
-
Tips
l. opioids 2. TCA's 3. Deferoxamine
4. lethargy 5. sedation 6. coma
7. bradycardia 8. hypotension 9. hypoventilation
10. pinpoint pupils (miosis) 11..cool skin 12. decreased bowel sounds
13. flaccid muscles 14. mydriasis 15. anticholinergic symptoms
16. severe arrhythmias 17. charcoal 18. NaHC0
3
diuresis
19. Naloxone 20. Removal of 21.
benzodiazepines with
lavage, treatment with
charcoal & treatment with
Flumazenil
22. Flumazenil 23. 8 hrs of overdose of 24.
acetaminophen
CAMH: Canadian Addiction and Mental Health
Iron overdose should not be treated by? (
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What is the acetaminophen antidote?
N-acetylcysteine should be administered within? ( is W 1-
Benzodiazepine antidote is? (
Benzodiazepine overdose treatment? ( l'
/. Opioid antidote ( t4d.o)t64J /....U..H, 4-
Pinpoint pupil is overdose symptoms of? { {fftll'iJ4
What drugs overdose can cause proarrhythmias? ( 1c/t:)) I... 1'/1..-u A
, A'A/..a. .. t< .. ./.
/'. What is true about charcoal? ( -rv __ ..)
/ Iron overdose is treated by? (
( TCA overdose symptoms ( 'i d/.t A.&) ct '
Increase surface area, increase decrease impurities on
\. increase adsorption. However, increase temp on surface of charcoal
65-3
Skills
Professional Communication
Type of communication methods:
Verbal communication methods
Non-verbal communication methods
Phannacy Practice and Management
Questions Alerts!
The best communications skills: verbal and writing
Barriers in communications: Environmental barriers, personal barriers, Financial and
administrative barrier
Verbal communication
Verbal communication comprise: Speaking, and listening
The sender: One who transmits a message to another person
The message: It is an element that is transmitted from one person to another
The receiver: One who receive message from sender
Feedback: It is the process of replying to sender
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Barriers in communications: The interference that affects the receiving, sending transmitting
of message.
Environmental barriers (noise, music, counter heights etc).
'. Personal barriers (no confidence, shy, incompetence)
Patient barriers (knowledge)
Administrative and financial barriers
Environmental barriers:
Distraction in environment ohen can result into environmental barriers like: Height of
prescription counter separating the patient from the pharmacist.
Crowded and noisy prescription areas inhibit one to one communications.
Presence of support workers like technician who' stands between pharmacist and patient.
l
66-1
Phannacy Practice and Management
. .
Distraction or Loud noise, telephone rings, music, and traffic.
Check the following potential factors that are associated with environmental barriers:
Is pharmacist visible?
Is counter top or stuff on counter tops blocking pharmacist visible?
Does it easy to get pharmacist attention?
Is it private counselling area available to conduct private interview?
Is that lost background noise or distractions?
Is it easy to get pharmacist attention?
Recommendation to minimize environmental barriers:
Place computers terminal near the patient counselling area to minimize distractions
Create a quite private counselling area
Make countertops wider to accommodate computers, printers etc.
Personal barriers
Low self-confidence
Cultural differences (cultural competent)
Discomfort to sensitive situations
Conflicting values of therapy
Shyness
Patient barriers
The following are the examples of patient barrier;
Patient perceive being as knowledgeable?
Patient perception about pharmacist knowledge? ..
The perception of impersonal atmosphere
Patient perceptions about their medical conditions as minor?
Patient may be anxious about their conditions.
Administrative and Financial barriers
There are several factors of administrative and financial aspects effects pharmacy practice.
Like:
(. Pharmacist are not paid directly for educating or communicating with patients, therefore
many managers perceive the task of talking with pharmacist is expensive service and not a
high priority.
Pharmacy policies that encourage minimum number of pharmacist.
Excessive tasks to pharmacist by typing label, count medications, talk on phone, and
completing other tasks while communicating with patients.
Time barriers
66-2
NonVe...bal Communication
Kinesics or body language:
Written: It is powerful nonverbal communication tool.
Tips
Pharmacy Practice and Management
L low self-confidence 2. Distractions 3. language
4. Promotion sales s. Telephone 6. Noise
7. Verbal 8. Written 9. Cultural differences
10. Discomfort to 11. Conflicting values to 12.
sensitive situations therapy
The best communication skills are? ( ) 74-
Examples of communication barriers includes? ( j / z....)
Examples of communication distractions includes? ( )
Examples of personal barriers includes? ( I /2-

Communication does NOT require verbal language.
The elements of communication: Kinesis and proxemics.
Setting inappropriate timing of appointment
Large number of prescription need to be filled in short time
The manner in which one uses her/his eye contact, arms, legs, hands head to convey a
message to receiver.
Example: Relaxed posture, slight lean toward the other person, eye contact, smile etc.
Proxemics:
The distance between two interactive people put more emphasis on content of
communication, and it is defined as proxemics.
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Medicaton
rrors
Questions Alerts!
Common.questions in pharmacy exam is to ask!
ISMP: Institute of Safe Medication Practices.
ISMP: is an non profit independent agency established for the collection and
analysis of medication error reports and development of recommendation of
enhancement of patient safety
This chapter focuses on errors that occur during the medication use process that includes the
prescribing, dispensing, and administration phases of medication use. Monitoring the patient
for expected and unexpected drug related problems and patient compliance. It reviews
common causes of medication errors and suggest measures to safe and use of
medications/strategies to prevent dispensing errors.
Types of medication errors', '
\
According ASHP guidelines'orn preventing medication errors in hospitals, medication errors
,
can be categorized 'into 11
Prescribing errors
Omission errors
Wrong time errors
Unauthorized drug errors
Improper dose errors
Wrong dosage form er'rors
'. Wrong drug preparation errors
Wrong administration errors
Deteriorated errors
Monitoring errors
Compliance errors
Other errors .
Prescribing errors
67-1 '-'
Medication Errors
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A prescribing error occurs at the time a prescriber orders a medication for specific patient.
These errors may indude the selection of incorrect drug, dose, dosage form, route of
administration, length of therapy, or number of doses.
Omission errors
Failure to administer an ordered dose to a patient in hospital, nursing home, or other facility
before the next scheduled dose is considered an omission error.
Wrong TIme
Timing of administration is critical to effectiveness of some medications. Maintaining an
adequate blood level of some drugs such as antibiotics, frequently depends on evenly spaced,
around the clock dosing.
Unauthorized drug error
Administration of a medication to a patient without proper authorization by a prescriber is
categorized as an authorized drug error
Improper dose
Improper dose error occur when a patient is given a dose that is greater or less than
prescribed dose
Wrong dosage form errors
Doses administered or dispensed in a different form from the o r e r ~ by the prescribed are
classified as wrong dosage form error
Wrong drug preparation errors
Drugs requiring reconstitution (adding liquid to dissolve a powdered drug), dilution or special
preparation prior to dispensing or administration are subject to wrong drug preparation.
Wrong Administration Technique Errors
Doses that are administered using an inappropriate procedures or incorrect technique are
categorized as wrong administration technique error.
Preventing dispensing errors: In order to prevent dispensing errors, pharmacy should have
policy and procedures in place.
College of Pharmacists, and professional regulatory agencies provide guidelines to prevent
dispensing error. All pharmacy staff should obey and discuss those guidelines.
Before you dispense any medication, check the following-7 (7 point check)
Name of patient
Name of medication
Name of doctor
Pharmacist and technician initials (check expiration date)
67-2
Check DIN
I a
Quantity of medication
Number of refills
3 point check during preparation:
read label when drug from shelf
read label before preparing'label
read label when placing back on the shelf
Medication Errors
Strategies in reducing dispensing errors
. / '
Procedures al1d policies must be developed to.qeal with these errors, keeping in mind that
,. . ..' ,f _
the patient safety is paramount. .
Discuss commonly dispensing error drug with staff. .
Bringing the common drugs that may have dispensing problems to others attention, that
means everyone is extra careful as they are dispensing them.
Drugs that look similar separate and label them.
Dispensing error occurred.
When dispensing errors. occur, rapid resolution of the problem is essential,.including the
recall of the product.
Inform the pharmacist manager immediately for any misfills or other serious problems.
Do not try to handle the situation yourself.
Inform
Inform manager
Inform doctor
Documenting all errors and discussing them with all staff helps keep everyone aware of
mistakes that are easily made.
Resolving dispensing errors: Pharmacy should have policies and protocol about resolving
dispensing error, Follow the guidelines provided by the provincial college of pharmacists.
However, this is a general discussion to help you get started understanding resolving
dispensing errors.
In case an error has occurred the patient needs to be informed of the error that has occurred
that the medication she is taking is not the correct the pharmacy has made an
/ error in dispensing the medication she was supposed be taking diclectin as the doctor has
. prescribed but the pharmacy dispensed dicetel 7 by mistake. Tell her to stop taking the
medication, Ask her how many dicetel 7 she has taken, apologize for the mistake that has
happened, take reasonability for the mistake, Call the doctor and report the mistake, replace
the medication with the right medication, speak to the staff about the error: that has --
occurred.
Examples of medication error that could occur if auxiliary labels are not used or used
inappropriately:
67-3
Medications that should be taken with plenty of water:
Recommended for sulphonamides to decrease likelihood of
Expectorants to enhance viscosity reduction of bronchial secretions
laxatives'": Bulk laxatives to increase stool bulk and decrease the likelihood of compaction
drugs: Such as pot"ss[um supplements, Chloral hydrate, theophylline
and some antibiotics.
Actions that should be taken 0 resolve dispensing errors;
Discuss with all staff to keep everyone aware of mistake
Discuss and identify drugs that have similar names such as:
Biaxin -7 one tablet twice a day (500 mg)
Biaxin -7 2 tablets once a day (SOO mg)
lasix (furosemidlil)
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Medication Errors

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Take with food or milk: Recommended for the drugs that cause stomach upset when this
effect may be decreased by taking medication with food. 0
Medication examples include:
NSAJDs,
Aspirin
Erythromycin
Nitrofurantoin
Valproic
v-J"or
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Take Medication On An Empty STOMACH 1 hour before or 2 - 3 hours after 3 hours after
meals unless or otherwise directed physician:
Recommended for drugs that have decreased absorption or increased destruction in stomach
when taken with food.
Examples of drugs that should be taken empty stomach like ampicill.!!: and tetracycline
1) Codeine containing medication auxiliary label: dizziness may occur be careful when
operating machinery, A car accident may occur if the patient is not aware that this medication
may cause dizziness.
2) Fosamax auxiliary labels: drink with plenty of water, remain upright for about Yt hour after
taking the dose, take on an empty stomach, If the patient is to take the medication and lie
down right aher taking it then the patient may experience oesophageal adverse experiences
3) Ventolin auxiliary labels: shake well; don't take too much of the medication
If the patient is to take too much of the medication then the patient may experience adverse
drug reactions such as palpitations, tachycardia, tremors, nervousness, hypokalemia.
Fll.lH c.aJ.:o6...... 4) Flovent auxiliar;y labels: shake well, rinse mouth after using this inhaler. If you doh't wash
your month a phatyngeal candidiasis fungal infection in the mouth may occur in the mouth.
5) lipitor avoid grapefruit juice. Grapefruit juice may have the potential to
increase plasma Ie of HMG CoA reductase inhibitors metabolized by this isoenzyme
causing increased potential for adverse effects such as muscle weakness and pain.
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www.Pharmacyprep.com Medication Errors
Losee (omeprazole)
Procedure and policies must be developed to deal with these problems.
Check DIN (Drug Identification Number)
DIN for different quantity packaging
Expiry date
Check patient name and date of birth
Check allergy
Paediatric dose child weight
Expired drugs: Do not sell expired drugs
.',
Handling Products .j
It is against the I<;lW. to rte/lace returned medication as stock bottle once it has been
dispensed and to: e patient.
- Exceptions are h'Q,spitalj harmac;ie-s- -
Prescription drugs' may/not be returned by a customer and placed back in stbck.
Sometimes, the attentfon needs to be d.rawn to a complaint; in other cases,
policies will need developed; e.g. for product recalls and dispensing
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Medical incident reporting
ISMP: Institute of Safe Medication Practices.
is an non il','dependent agency established for the collection and analysis of
medication error reports and development of recommendation of enhancement of
patient safety
Reference:
American Society of Hospital Pharmacists. ASHP guidelines on preventing medication errors in
hospitals, Am, J Hosp Pharm. 1993; 50: 305-14
ISMP recommendations:
use units instead "u" or "IU"
Use "od" instead of "o.d"
/. Use meg instead of "Og"
I
use "0.5" instead of ".5"
Use "5" instead of "5.0"
Use "qd" instead of "q.d"
67-5
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Questions Alerts!
Insulin storage conditions
Extemporaneous suspensions: Azithromycin, Clarithromycin, CHndamycin, and
Cotrimoxazole.
Pharmaceutical Preparation
Storage Conditions
C [(Of - 32) 19] (5)
C = [(OF - 32)(5)J 19
C = (Of _32) (0.56)

Four ways to convert Celsius to Fahrenheit
of [(C)(9) I 5J + 32
of C x (9/5) + 32
of (OC x 1.8) + 32
OF (9C + 160) 15
Four ways to convert Fahrenheit to Celsius
68
Suspension: With or without food.
Shake well before use (suspension)
Temperature
Deep freeze: -10 to -72 DC
Frozen: DoC
Refrigerator or cold: 2 to 8 DC
Cool:810IS
D
C
Room temp: 15 1025 DC
Wann: 30
0
e

Amoxicillin

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Phannaceutical Prep Storage Conditions
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Refrigerate, if unused for 14 days discard it.
Suspensions, store in refrigerator. Discard afte@ays.
Combination with c1avulunate: use within 200 and 400 mg 7 days. 125 to 250
V
mg use within 10 days
Clavulin suspension: Store in refrigerator for 7 days

Ampicillin

Take empty stomach.
Shake well before use
Refrigerate, if unused fo 14 days discard it.

Naficillin

Give oral drug with water: (acid form: fruit juice or carbonated beverage-
inactivates drug
Take empty stomach
Complete the full course of therapy

Cloxacillin

Give oral drug with water: (acid form: fruit juice or carbonated beverage-
I
inactivates drug
Take empty stomach.
Complete the full course of therapy

Cephalosporins

Cefuroxime (2
nd
gen)
Take with food (for better absorption)
Others with or without food
Shake I.M solution gently before use. Check solution for particulates.
Cefuroxime: may be reconstituted with cold water, milk, apple, orange,

lemonade juice. Stir and drink immediately.
Tabs: do not crush or chew because of bitter of taste and take with glass of
water
In all three generation cases food increases absorption.
Cefaclor, cefadroxil, cefexime, cefprozil- food decrease GI side effects.

Streptomycin
Reconstituted solution does not shake: Use immediately.
Discard after 8 hours.
Always 1M only
Erythromycin

Erythromycin: refrigerate di 5 cAA.d Atfth-- 1, 'K U"l"-"--'
Azithromycin

Do not refrigerate
Suspension
Clarithromycin

Do not refrigerate
Shake well before use and do not store in refrigerator.
Discard unused portion after 14 days.

Quinolones
Store cipro otic suspension at room temp (15 to 25C).
Do not use otic suspension under 2 year of age.

,
Clotri moxazole

Take oral dose with full glass of water.
Suspensions
With or without food. (Food decreases GI side effect)
Store in amber glass of bottle.
Store at room temp and protect from moisture.

68-2
Drugs stored. in Refrigerator ( 2 to 8 c or 3S to 46F)
68-3
Diltiazem injection
Promethazine suppositories
Phannaceutical Prep Storage Conditions www.Pharmacvorep.com
Xalatan (latanoprost)
Protect from figHt
Store' unopened bottles in refrigerator
Opened bottles may be stored at room temperature up to 25C for up to 6 weeks
Xalacom (latanoprost +Timolol)
Protect from light
Store unopened bottles in refrigerator
Opened bottles may be stored at room temperature-up to 25 Cfor. up to 10 weeks
Insulin's or premixed insulin's
v Store in refrigerator LI ~ M )
.......... Do not freeze (. 6""""",, ~ r - pdj f ~
v. Can be stored at room temperature for a month
Vaccine
All vaccine should be stored in refrigerat6r
Do not freeze
Do not store at room temperatures
Flu vaccine
Hepatitis A and Hepatis B
MMR vaccine
Tetanus taxoid
Ducoral
Erythromycin ethyl succinate suspension
Calcitonin salamon (nasal spray and injections)
Sterile bacitracin powder
Pepsid injection
Urokinase
.
Store until expiry date

Chloramphenicol

Refrigerate ophthalmic solution. Avoid prolonged sun exposure.
Clindamycin

Do not refrigerate
suspension
Clindoxyl gel

Clindamycin + benzoyl peroxide store in refrigerator
Metronidazole

Refrigerate for 60 days
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Gencyclovir
Pepscicles
Tips
Pharmaceutical Prep Storage Conditions
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1. Streptomycin 2. Xalatan 3. Amoxicillin
4. Insulin 5. Ampicillin 6. Clarithromycin
7'.
Combination + Amoxicillin + 8 Azithromycin 9. Clindamycin
c1avulanate
10 Cotrimoxazole 11 15 to 25C 12, 8 to 15 c
13, 2 to 8 c also known as cold) 14 oto 4C 15. Erythromycin
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What is room temperature in Canada? (II)
What is cool temperature? ( t2)
What is freezer temperature? (llt)
Suspensions, store in refrigerator. Discard after 14 days, (3/), 7,
Reconstituted solution does not shake. Use immediately, Discard after 8 hours. (' ) .t.'"
Store in refrigerator, do not freeze and can be stored at room temperature for a month('i) I
Store unopened bottles in refrigerator. Opened bottles may be stored at room
temperature up to 25C for up to 6 weeks (2) r , I . -c.:h
Use within 200 and 400 mg 7 days. 125 to 250 mg use within 10 days ("1) t-
Refrigerate, if unused for 14 days discard it. (J,S'",7. IS)
Shake well before use and do not store in refrigerator. Discard unused portion after 14
days. A-J' c.f'-)')dtt m(f-C' 'J , .,1
Suspensions stored at room temperature (e, L I Q(J-
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Extemporaneous azithromycin suspension -7 " RP " , S-- C0-
Extemporaneous c1arithromycin suspension -7 " Roo,"", - IS-'- 'l..-r'<:
Extemporaneous c1inda'mycin suspension -7 "f I - 9-<"" L

Cotrimoxazole suspension -7J' , J-i'c
Insulin stored at -7 '3 .2. -f-'1S'c.. 2 '5
c:Juuzp c1ov/A.
dPd Au,rMU- I V) 0 a - c.,cLu
Md-:>Ohib,yl 60 daJ:o 4doND1 FRf;f;1...l";
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68-4
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Questions Alerts!
Treatment: Treat all contacts if you notice head lice. Treat infected contact after close
examination.
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OTt and Prescription drugs for Dermatological Conditions
69
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Hair to hair contact, commonly shared items such as combs, brushes, hats and
stuffs toys. It does not fly.
Lice live on the skin with short or long hair. Scalp and back & sides.
Female lay eggs daily, these nits hatch after 7 to 10 days.
Hygiene is not criteria of head lice transmission.
All physical contact should be treated, ifhead lice or nits are found
PhannacyPrcp.com
..
Head lice mode of transmission, treatment
Acne and rosacea symptoms and treatments
Dermatitis: diaper rash self care, uncomplicated and complicated therapy.
Psoriasis symptoms (red scaly patches). treatment
OTC and Prescription Drugs
for Dermatological
Conditions
Non-phannacological
lnfected fomites: soak combslbrushes in hot water for 5 to 10 min (1:4 vinegar in
water) or wash in pediculicide shampoo
Store unwashable items in plastic bags for 10 to 14 days
After treatment with pediculicide shampoo remove nits using fine toothcomb.
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Pharmacological:
Inform daycare' but still go.
Not effective iri"'killing eggs, after 10 d<!Xs
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Pennethrin 1%: rugofchoice. n f-ks. I Affl"::!. AJl.AI"#I wu-lt6/A,.
.1. Leave on for 10 min -p..> - U ........ - d-
Apply to towel dried hair l,. f-' tU-f>e.-.1"
Best ovicidal activi among all treatment with 70 to 8.0% efficacy,
Re treatment afte 7'to' 'i 0 ays .
=; -1 % Lindane' ,
. Contraindicated in seizures
V. Caution in under 2,year age and nursing mothers, pregnancy. and elderly, inflamed
skin
Apply for 4 minutes to dry hair

ff neurotoxic'pr9duc, '. Isopropyl mersteat IPM (Resultz)
[Scabies 1
es a'lOn of the skin with human mites
Clothes/linens should be cleaned with soap and hot water or...stored in bags for 5 to 7
days (separate from host die in 2 to 3 days) -
'. Vacuum a:ll ,surfaces (rugs,. carpets, furniture)
'.. Av.oid qm,taQt with others
All conta'cts should be treated
It is a hygienic problems
Treatment
Treat infested individuals and all close physical contact with topical scabicides
Pennethrin 5%
Drug of choice in adults and children> 2 month old
Under 2 months require prescription (medical supervision)
Effective 96 to 100%
Low systemic absorption
Caution individual
Applied to entire body (include t<;>es: nails, genitirareas), except in eY%,illouth
5 neck down to toes. In children head down to toes. <.
Must be washed off after 12 hours
Retreat after 7 to 14 days to prevent ping-pong effect
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69-2
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Sulphur 6% in petrolatum:
DOC in pregnancy. lactation, and children under 2 months
Apply bid for 10 days
Unpleasant odor and local irritation
tb use: Massage into all skin areas, from the
every bit of the skin must be treated, including the
neave on for 8 -14 b, then wash off (shower may
.
Treatment:
Nonphannacological
Squeezing pimples may increase risk of scarring, avoid excessive cosmetic use
and use only products. Washing; not more than
twice daily with mild soap.
safety razors (soften with soap)
Comedone Wash with hot water and place extractor on acne.
Ullravoiletlight-7 currently not recommended
Shampoo hair keep from falling on to face. Reduce hair spray
Keep nails short and clean
Balanced diet is good for overall health, but there is no evidence that acne is
caused by specific food. Food does not aggravate acne
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Topical acne preparations: Av.0 /.,J.l.- "'" o.ta-l T'1"c..L-
Ben<oyl peroxide f"'f'AAho,,",- ", I. ) O..,J
Cream, gel. lotion 5% without Rx) AC.c:.tclokL 1
Is a peeling agent that also has some antibacterial action, mainly used in . . ")' L to.
papulopustular acne. A (.tAA--+i.".,'y I! ",r
Retinoids
Lindane cannot be used by children < 10 yrs old, elderly, pregnancy and lactation,
seizure disorders
Patients with extensively excoriated skin, elderly & children may be enhanced
percutaneous absorption and increased potential tox icity
10% systemic absorption & accumulates wi repeated exposures
Killing time.i.!!..can repeat treatment in 7 to 10 days
Sulfur 5-10% ointment is used in small children and pregnant woman.
\ Acne : P;MPIe....>
Acne is due to:
Increased follicular keratinization
lncreased sebum production
Prop;on; bactedu1fJ acne lncreased (bacterial) lipolysis of sebum triglycerides
to free fatty acids
lnflammation
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aTe and Prescription drugs for Dermatological
Cieain, ge.l, solution
-. Used in comedogenic acne,
,e' Antibiotics
,. ,Erythromycin (gel, lotion, solution, pads), and clindamycin (solution)
. Used,to decrease colonization of skin mainly in papulopustular acne
e Salicylic acid 2%
Available without prescription
Systemic Antibiotics:
Tetracycline
The most commonly prescribed oral agent
Reduce the number of acnes and may exert an anti-inflammatory effect by inhibiting
leukocyte chemotaxis
Contraindicated in pregnancy
SE: GI effects, photosensitivity, may exacerbate azotemia in'patients with pre- 7
existing renal disease "
DI: GI absorption of tetracycline may be impaired by iron, bismuth, aluminum,
calcium, magnesium in drugs and foods (e.g. dairy products) separate doses by 2
hours.
Minocyclioe
Once daily
Can be given with food or milk
SE: dizziness, vertigo, ataxia, abnormal cutaneous pigments
DI:
Doxycycline
Contraindicated in pregnancy and child < 8 years of age
Erythromycin
Alternative to tetracycline due to its safety
, SE: nausea, vomiting, epigastric distress, diarrhea
DI: may increase blood levels oftheophylline, cyclosporine, carbamazepine,
warfarin, digitalis, ergotamine, methylprednisone
Concurrent use with astemizole, terfenadine or cisapride is contraindicated
I
Retiooids (Accutane and retinol)

SE: tetiatogenicity, dn::: skiP, lips, ocular effects (conjunctivitis, might decrease
vision), increaSe TG..Jeve'l, increase cholesterol level, increase liver function,
reversible hair loss.
. 0 adv.erse reaction known between retinoids and oral
taking vitamin A supp ement
CI: complete y' In pregnancy and planning to be pregnant.

69-4
Dermatitis
. Atopic dennatitis or eczema
Contact dennatitis
Diaper dermatitis (diaper rash)
Hormonal Therapy
Used for women with moderate acne
Used for several months to see improvement
Differential diagnosis
Contact dennatitis - pattern of lesions, distribution, identification of allergic,
chemical or physical cause can differentiate it from atopic dermatitis
aTe and Prescription drugs for Dermatological Conditions
PharrnacyPrep.com
Nonphannacological treatment
Minimize use of bath soaps and solvents
Reduce laundry soap residue in clothing
Avoid bleach and fabric softener
~ Use cool air humidifiers to reduce room dryness
Avoid wool, nylon or rough fabrics

UV lights may be helpful
Atopic dermatitis or eczema - chronic inflammatory pruritic dermatosis associated with
personal or family history of allergic disease
Affects up to 1% of population
Common in young people .
: . : = = = = ~ S .
Prone to viral, bacterial and fungal skin infections
Signs and symptoms
Pruritus
Lesions due to scratching
Weeping erosions, vesicles and excoriated, reddened, scaling papules or plaques
Skin may be thickened with pigmentation changes
Phannacological treatment
Topical hydrocortisone is mainstay therapy
Oral antihistamine
Coal tar
C
Burrow's solution for weepmg lesions. Compress for 2 to 3 days for astringent and
antibacterial effects
tBo antibiotics]
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OTC and Prescription drugs tor Dermatological
Pharmaceutical agents
Bath products; soothing to itchy, irritated skin
Emollients
Cover tiny fissures in skin
Provide soothing protective film
Topical hydrocortisone 0.5% - relieve the itching associated with atopic dermatitis
Most common local side effects: contact dermatitis, allergic reactions, pain and
pruritus
Oral antihistamines
Older sedative types may help relieve itching associated with dry skin
May cause drowsiness, gastrointestinal disturbances paradoxical excitability,
Nervousness and difficulty in sleeping .
Contraindicated in patients with angle-closure glaucoma, kidnS)' or liver disease,
prostatic hypertrophy, pregnant or breaskfeeding women
Coal tar - best applied under an emollient due to their drying properties
Often messy, had unpleasant odour, stains hair, skin and clothing
May cause folliculitis, tar acne, contact dermatitis and photosensitivity
t
How to manage atopic dennatitis
Possible causes:
Stress
Skin irritants such as soaps or chemicals
Environmental factors such as high heat or humidity
Foods, molds or pollens to which the person may be allergic
Allergic Contact ermatitis
Allergic contact dennatitis is an itchy skin condition caused by an allergic
reaction to material in contact with the skin.
It arises some hours after contact with the responsible material, and settles down
over some days providing the-skin is no longer in contact with it. .
Contact dermatitis should be distinguished from contact urticaria, in which a rash
/ appears within minutes of exposure and fades away within minutes to hours. ;;fhe
allergic reaction to latex is the best-known example of allergic contact urticada.
Active dermatitis is usually treated with the following:
Emollient creams
Topical steroids
Topical or oral antibiotics for secondary infection
Oral'steroids, usually short courses, for severe cases
Photochemotherapy.
69-6
\ '
Diaper Dermatitis: (Napkin rash)
Azathioprine, cyclosporin or other immunosuppressive agent. -
Tacrolimus ointment and pimecrolimus cream are immune modulating drugs
Uncomplicated
-YZinc oxide, and petrolatum
Acutc urticaria
is sometimes due to allergy. Allergy depends on previous exposure to the
material, and the development ofan reaction to it. A protein calle@is
involved. _ >
---
aTe and Prescription drugs for Dennatological Conditions PharmacyPrep.com
Usc lanolin-free protcctant barrier with each diaper change

Zinc oxide 40% for treatment and 15% for prevention
Zinc oxide 15 to 20% or silicone.
Reapply every few hours in a thick layer,
Remove with mineral oil or water
If not effective: Confluent tomato-red plaques, white scaly border
-7Anti yeast agents: Miconozole, c1otrimazole, nystatin-77 to 10 days
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Anti yeast agent: Clotrimazolc, miconozole-7(imidazole).
Nystatin: Effective only against Candida
C. alhicans likely cause if condition present> 3days
Should be discontinued once inflammation has subsided
Anti inflammatory agents (hydrocortisone 0.5% OTC, 1% Rx): Should not be used>
-7 Use 1% hydrocortisone only under physician forder 2 year

Urticaria
Urticaria refers to a group of disorders in which swelling occurs in the skin. The
release of chemicals such as histamine causes small blood vessels to leak and
results in tissue swelling...
Synonyms: Diaper rash, napkin rash
Non-phannacologicaltreatment:
V4' Use wann water to clean diaper area and air dry diapering (NOT alcohol wipes).
Change diaper frequently.
Maintain hygienic conditions.
Discontinue aggravating factors.
air drying. Avoid powders as barriers (NO cornstarch, talc. and baking soda)
Geode cleansing with mild soap and water. (Avoid baby wipes & acid pH cleanser)
Avoid food that increase urinary output and fecal pH (high protein diet, caffeine,
citrus juices)
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PharmacyPrep.com OTe and Prescription drugs ,for
Treatment: .-
Oral antihistamines control wealing and itshing for the majority of,patients with
urticaria.
Non-sedating antihistamines (Ioratidine, fexoferi'adine, terfenadine;' cetirazine, and
astemizole) are less likely to cause drowsiness than the less expensive 'conventional
antihistamines.
Oral steroids (prednisone) - useful for severe acute urticaria but unsuitable long term.
If you have generalized urticaria, ask your doctor if a medicine could be the cause:
Avoid aspirin and codeine, and reduce your intake of acidic fruits'
Dry, Scaly Skin
Dry skin - due to dehydration of stratum corneum
May be present with other dermatoses such as atopic dermatitis, in normal skin due to
aging, illness or environmental factors
d
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Signs and symptoms
Roughness, flaking, scaling and chapping in front of lower legs, back of hands and
forearms
With inflammation, pruritus and fissuring
Atopic, contact and seborrheic dennatitis
Dandruff
Psoriasis
Nonpharmacological treatment
Bathe once a week and sponge on other times
Use emollients or protectants to maintain hydration
Increase water intake
Pharmacological treatment
/ Bath products and skin moisturizers that contain lactic acid, phospholipids or urea
Oral to help relieve itching
Topical hydrocortisone preparations to reduce inflammation
1.) Bath products -Contains oil such as mineral pil or lanolin, salts such as sodium
bicarbonate. or colloidal solids such as oatmeal may not enhance hydration but may sooth
itchy, irritated skin
69-8
Hydrocortisone cream 0.5% can help relieve itching and red skin that may occur with
some cases of dry skin. It will not cure dry skin. Hydrocortisone should not be used for
How to prevent dry skin
Use a humidifier on forced-air heating systems
Keep the room temperature at the lowest comfortable level in lIle winter and use a
humidifier
Avoid air conditioning when possible
Use a mild or superfatted soap; if dry skin continues, usc soaps to cleanse only the
groin, underarms and feet
Avoid wool and rough clothing that will irritate skin
Protect skin from wind, extreme cold and sun
How to treat dry skin
Add a bath oil to the water in the last 5 minutes of your bath; adding it earlier will not
allow water to get into your skin .
Add baking soda or oatmeal to your bath ifskin is itchy
Rub an ointment into your skin after your bath to help skin hold in the moisture
Rub a moisturizer into your skin often during the day and at bedtime; special dry skin
creams can be tried if regular moisturizers are not helpful
Oral antihistamines can help relieve itching especially at bedtime
To correct a dry skin tendency from any cause reduce contact with soap and water
and apply a moisturizer or emollient
2.) Cleansing products - soaps made from saponification of animal and/or vegetable fats
or soaplike synthetic detergent cleansers
Both emulsify fats with water to remove oil and dirt from skin
Any type of skin cleanser can aggravate skin dryness depending on its pH,
cleansing ability, composition and additives
3.) Emollients - bland oleaginous substances applied to skin by rubbing
Used to replace natural skin oils. cover tiny fissures in the skin and provide a
soothing protective film
Don't hydrate skin, they slow evaporation of moisture from skin
Maintain hydration ifapplied immediately after bathing
Common emollients: petrolatum, glycerin, urea, lactic acid, mineral oil, lanolin
and fatty acids
4. Topical hydrocortisone 0.5% - to relieve minor itching and inflammation associated
with dry skin
Most common local side effects: contact dennatitis, allergic reactions, pain and
pruritus
5. Oral antihistamines - relieve itching associated with dry skin
May cause drowsiness, gastrointestinal disturbances, paradoxical excitability,
nervousness and difficulty sleeping Contraindicated in patients with glaucoma,
kidney and liver disease, prostatic hypertrophy, pregnant and breast-feeding
women
OTe and Prescription drugs for Dermatological Conditions
PharmacyPrep.com
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69-9
Phal1!1acyPrep.c.0n:t
aTC and Prescription drugs for Conditions
long tenn control of dry skin. If the itching and redness do not after 7-10 days of
treatment, see your'doctor: '.
bathing
Reduce washing to every second day, or less often, although the body folds may be
sponged daily if desired.' .
Baths or showers should be kept as brief as possible.
Water should be lukewarm.
Minimize the use of soap. Reduce the need .for bathing by. keeping as as
possible both at home and at work.
Moisturizers and emollients
The tenns 'moisturizer' (to add moisture) and 'emollient' (to soften) are interchangeable as
they describe different effects' of 'these agents on the skin. Basically they have two
actions:
Occlusives, which provide a layer of oil on the surface of the -skin to slow water loss
and thus increase the moisture content of the stratum corneum.
Humectants, which are substances introduced into the stratum corneum to increase
its water holding capacity.
Some moisturizers contain both occlusives and humectants
Humectants, agents adding water to the stratum corneum, include:
Glycerine
Urea
Alpha hydroxy acids such as lactic acid or glycolic acid. At higher concentrations these
also have a descaling or keratolytic action by thinning the stratum corneum: they are
often known as peeling agents .
Psoriasis
Psoriasis is a disorder of the skin that typically consists of red scaly patches
covered by silvery white scales. Psoriasis is very common. Approximately 2% of adults
have psoriasis.
Sunshine: Sunshine may help to clear psoriasis; in many people it improves
dramatically during sunny holidays. Take care, as psoriasis may develop in areas of
sunburn, and fair skin exposed to ultraviolet radiation becomes prematurely aged and
may develop skin cancer. .
69-10
Anthralin
69-11
Salicylic acid
Hydrocortisone
OTe and Prescription drugs for Dennatologlcal Conditions
Batbs: Soaking in wann water with a bath oil or tar solution can soften the 'psoriasis
and lift the scale. Bland soaps or soap substitutes are useful; detergents and
antiseptics are nol necessary and may irritate.
Emollients: Even if no medicated preparations are applied. the psoriasis should be
kept soft with moisturizing creams to prevent it cracking and becoming sorc.
Vaseline, emulsifying ointment and S,e,rbolene cream are among suitable
preparations. "- .
,---
Occlusive dressings Patches of psoriasis which are limited in extent may improve
with occlusive dressings i.e. waterproof adhesive dressings
PhannacyPrep.com
Topical Preparations
Crude coal tar:
Coal tar has been used for many years. In the 'Goeckennan' regime in hospital, it
is applied twice daily to the patches after exposure to ultraviolet light. The
psoriasis clears in 4 to 6 weeks and may stay away for months
Oral medications
Methotrexate
Methotrexate tablets are taken once a week.
Signs and symptoms
Dandruff - characterized by excessive scaling and irching ofthe scalp
Dry, white, grayish scales spread unifonnly in scalp
Seborrhea - excessive scaling and itching but found in the axilla, back, chest, ears, face
and groin
Is an inflammatory dcnnatosis
Dandruff and seborrhea; scaly dennatoses occurring in area of high sebaceous gland
concentration
'. Dandruff affects most adult
Seborrhea occur most often in infants less than 3 months of age (cradle cap) and
adults 30 to 60 years ofage
2-5% of population is affected with more men than women
Exacerbated with stress. Lw humidity and temperature
Worse in winter
Skin irritation. bacterial and yeast infections have been implicated
Dandruff and Seborrhea
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aTC and Prescription drugs for Dermatological Conditions
Lesion is a patchy areas of yellowish scales with slight to moderate redness of
underlying skin
Cradle cap in infants is seborrheic dermatitis but not itchy
Regular cleansing of the scalp or other affected areas with non medicated shampoo
Should shampoo and massage scalp at least 3 times a week to control the condition
I.Cytostatic/antifungal shampoo with selenium sulfide, zinc pyrithione
soften and detach .
Coal tar relIeves ItchIng and lower population of bactena or yeast on the-scalp
1. Antiseptics: (benzalkonium, chlorhexidine, povidone iodine
Kill bacteria or fungi
2. Coal tar: have astringent, keratolytic, antipruritic and antiseptic effects
Available in ointments, lotions, gels, shampoos and bath preparations
Tar often messy, unpleasant odour stain skin, hair and clothing
May cause folliculitis, tar acne contact dermatitis and photosensitivity
3. Ketoconazole: cytostatic effect that slows cell turnover and antifungal effect against
Pityrosporum ovale
Not be u ed within 2 weeks oftreatrnent with topical corticosteroids
4.Salicylic acid (2-3%): keratolytic effect
Useful in resistant cases of dandruff and seborrhea
Not be used more than twice a week
5. Selenium sulfide: cytostatic and antifungal effect
Remove all jewelry before use and wash hands thoroughly after
Not to be used within 2 days of applying hair tints or perm solution
Excessive use causes oily hair and hair loss
May stain blond or grey hair
Don't apply to inflamed or damaged hair
Only used twice a week
6. Sulfur (3 to 5%): keratolytic effect
Useful for dandruff but not proven to be effective
Used twice a week
Odor or stinks
7. Zinc pyrithione: cytostatic and antifungal effects
More effective than others
Can be used daily to control dandruff and seborrhea
c{3e-( "'1 ,.bllJ.(2.
b IOt'1d

69-12
Com and calluses
J"
HammerToes
Fig 69.1
\
PhannacyPrep.com OTe and drugs for Dennatological Con"ditions
Heel Pain
.Athlete's Foot .
Foot Conditions
Bunions
Athlete's Foot
Signs and symptoms
Itching, peeling, scaling, vesiculation, patchy hyperkeratinization and inflammation
occurs between the toes are the main clinical signs
Malodor may be present .
_iUiiiWi,,!W1'EF ..INM'........i't1!tUIIt
Dennatophytes mitiate the infection by invading and disrupting the horny layer of the
skin. Secondary bacterial infection may cause inflammation and additional maceration
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PharmacyPrep.com " 0TC and Prescription for Dermatological
The acute form is characterized by fissuring, scaling and peeling and the skin between
toes appears white, macerated and soggy .
Chronic form is characterized by hyperkeratotic, scaly eruptions on weight bearing
surfaces of feet,. soles and borders of the
Should be differentiated from contact dern1atitis, pustular psoriasis and drug eruptions
Patients failing to respond to non prescription antifungal preparations used correctly
for several weeks should be referred to a physician te...U hotl1 A-'e-.. _ I)
Nail involvement requires prescription treatment q;4b+ 1- A-+hWlet. b---- (
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'tz.hzJ 1?0.f-
Counsel patieots on proper foot hygiene
Bathe daily and dry feet well between the toes
absorbent socks, changed or twice daily ifthe patient is susceptible to
hyperhydrosis.
Wear shoes that "breathe" (sandals, if possible)
Change shoes dailyand wear different shoes for .
Dust with talcum powder or cornstarch especially between the toes
Pharmacological Treatment
Expose feet to the air to dry them and suppress bacterial proliferation
Soak feet with an astringent or dust with a medicated powder (talcum poWQer)
Use a topical antifungal agent such as c1otrimazole, miconazoJe, tioconazole,
naftifine, tolnaftate or undecylenic acid
0/ Clotrimazole, miconazole or tioconazole are the preferred agents since they have both
bacterial and antifungal activity and there is less chance of recurrence
Clinical be apparent within 2 weeks _
Use a topical antifuhgal agent such as c1otrimazole, miconazole, tioconazole,
tolnaftate or undecylenic acid
Clinical improvement should be apparent within 2 weeks
'"S= -
I. Clotrimazole, Miconazole, oxiconazole and tioconazol, imidazole antifungal agents
Have some antibacterial activity
Adverse reactions are infrequent like mild skin irritation, burning, stinging and
Erythema
Sensitivity reactions occurs rarely
2. Naftifine and .butenafine; effective antifungal but no antibacterial activity
Can cause sensitivity reaction in some patients
Mild burning or stinging, dryness, redness, itching or local irritation may occur
3. Tolnaftate; effective antifungal agent, no antibacterial activity
Recurrence and treatment failure is common
69-14
Rarely cause irritation or hypersensitivity reaction
Tips
4. Undecylenic acid; oldest antifungal agents
Can be as effective as toln<t;ftate, \:>utchar:acteristic odour is objectionable
HyperscQsitivity and skin are rare' ..
) .,How to
Athlete's foot is a skin infection caused by fungi. Since fungi prefer moist, warm places,
they thrive on the feet and between the toes of people whose feet are often hot and
sweaty.
can Be "prevented by few simple measures;
Wash the feet once or twice a day witli soap and water and dry them thoroughly,
espec.ially betwee.f.1 toes"
Wear san,dals or shoes socks that allow adequate ventilation
. Avoid socks made of synthetic fibers as they retain heat and moisture. Light cotton
socks are best.
Do not wear occlusive footwear such as rubber boots or athletic shoes for any longer
than flccessary
Change shoes daily.to allow tt:lem to dry inside
Change socks regularly and wash them thoroughly in hot water
Dust the feet, espeCially betweeli the toes,.with a foot powder to aid drying
"
OTe and Prescription" drugs for Dennatological
PhannacyPrep.com
1. sebaceous gland L Diane & Alesse 3 Erythromycin or
,
Clindamycin
4, cool humidifiers, 5, petroleum jelly, ZnO 6 cleaning wi alcohol
moisturizer cream wipes
7, it transmits by head 8- Permethrin 1% 9 avoid sharing combs,
to head contact or brushes, hats & pillows
common shared
items
10 gives blisters, hot 11. full thickness, painless 12 superficial, sunburn
,
H20, flame oil leathery, flame & hot
metal
13 UVB 14 5PF 15 UVA
16 coal tar 17 sulfur 18 anthralin
19, UV light 20 salicylic acid 21 corticosteroids
n Methotrexate 23, antifungal + ZnO 24 petroleum jelly, ZoO
25, Propioni bacterium
25
Second application
acne after 7 to 10 days of 1
st
application
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PharmacyPrep.com
aTC and Pt:escription drugs for Dermatological Conditions
. . . ',' . .
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How do the head lice transmit? (7)
What is correct self care measure for head lice? (.1 )
Drug of choice for head lice? ( )
How often head lice treatment should be applied? (2(.)
What b5lcteria cause acne? (.9...f) P D,., i AcM...--"
What gland secretions can cause acne? (l) Se.6q ' .. .. J
1.1- ." M el,
What is pharmacological therapy for acne in pregnancy? (.1) 1'V"'V""(fc.,., IT-
What oral contraceptives can be used for acne treatment? (.g.,) 8
What is self care measure should be recommended for dermatitis? (,,)
What is the treatment for uncomplicated diaper rash? 1'2:\110
What is pharmacotherapy for complicated diaper rash? (u) -f 1.JL,f-4-
What self care measure is not recommended for-diaper rash? (,)
WhatJs for psoriasis? I" 11 ,11>,11,12-'" OJlt:'"' :;:!"
What topical dermatological agent that gives stams? (I',t7) -c::.olk
What topical dermatological agent gives odor? (t'J 17 )
1st degree burn examples ( b&c..lt') I ho.J- U }
2": degree burn examples (10) I H-ut. ,
3 degree burn examples (") -H,"c/<. 1\Il.tI./ 1.0 "'""
Photptoxicity, photoaging, immunosuppression & skin c.ancer can cause (UV A)
immunosuppression & skin cancer ({)V..B ) --
Sun protection factor (SPF) 15,30 or 50 ( )
----4 , 1M.f1p.ltUJ1d UV 13
Select True or F'alse Statements
Clouds, snow, beach gives high sun burn (True)
High altitude have high sunburn (TruelFalse)
Water, beach areas, snow have high sunburn (TruelFalse)

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69-16
Fig 70.1
Eye problem: Mild blepharitis. single hordeolum (stye), conjunctivitis and dry eye.
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70
..
Ophthalmic, OTIC and Mouth Conditions
Ophthalmic, Otic and Mouth
Conditions
Prescription directions of ophthalmic & otic drops
Hard and soft lenses
Questions Alerts!
ophthalmic preparations to treat red or pink eye, dry eye
Mouth conditions like canker sores, and cold sores therapy
Blepharitis: Inflammation of the eyelid margin
Burning, irritation, itching and hyperemia along lid margins
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Crusting and scaling around eyelashes may be present hordeolum; acute
inflammation in the eyelash follicle or eyelid gland
Tenderness, edema and redness
Pus may appear along the eyelid margin in a few days
Blepharitis and hordeolum
Commercial eyelid cleanser useful for blepharitis
Indiscriminate use of nonprescription ophthalmic anti-invectives should be
avoided
Thorough cleansing sufficient for self-limited disorders
Conjunctivitis (red or pink eye): Inflammatory condition of the membrane that lines the
inside of the eyelids' and' covers the expo'sed surface of the sclera. ' Snoi1 ' (
1SnI-LcJw..4c. Ctx;o!rh(jW
Bactenal \.7r I r\
Viral "OJ
.et treh'h... 9.
Conjunctivitis diffuse redness in both eyes
Redness is more marked in the outer aspects of the eye and less around the,cornea
Purulent discharges is more common with bacterial conjunctivitis
Clear discharge in viral or allergic conjunctivitis
Intense itching occurs with allergic conjunctivitis
Bacterial Allergic
Symptoms Abrupt onset, Btinllng..selisation, itc!i')Hey.es
discharge, lids Wa.te--lW,'<diseh8!'i8e, mild redness +/-
endomatus +/- stuck AM. Self lid swelling
resolved in 7 to 10 days, chronic if>
2wks. Minimal itching
Non..Rx

Allergen avoidance, :..,..!JJr
" .
the eyes, wateli'
polymyxin B/gramicidin (eye

drops), polyrnixin B/bacitracin Jens6Sf
(ointment).
Rx tfitttetlit'5 '
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o-pHtltIDifi.itt'tl'afilihistaminp, oray
(ointment), sJllfa"ce'fifiriide 1(JO/o atltilristaifiiifi,""
s.Qlut.!QQI aIJ.OfQ.r..
Common cause:S. aureus, S. pneumonia (mQst in
....in diililreii)'
Symptoms: Abrupt onset, purulent or mucopurulent discharge, endomatus +/-
AM. Selfresoi'Veain 7 to 10 days, chronic if> 2wks. Minimal itching
70-2
Dry eye
Rx therapy: artificial tears 4 to 6 times a day, ophthalmic antihistamine, oral
antihistamine, mast cell stabilizers, and for chronic corticosteroids
Non Phannacologic therapy: Allergen avoidance, Q:ver tm,\eyeS', water
irrigation BID, and avoid contact lenses.
Lipid deficiency: decrease lipid layer is common in patients with blepharitis.
Epitheliopathies: defects in the corneal epithelium that can impair tear film stability.
Ophthalmic, OTIC and Mouth Conditions www.Pharmacvprep.com
Symptoms: Dry eye, sandy, gritty sensation, photosensitivity and difficulty moving the
eyelids
Etiology: Aqueous deficiency; decrease lachrymal gland secretion
Mucin deficiency: Damage or inflammation of goblet cells can be cause by condition
erythema multifonne.
Allergic conjunctivitis
ommon GrasSl5ol1en, ltthirl-es's is
Symptoms: Burning sensation, itchy eyes watery discharge, mild redness +1 lid swelling
Nonpharm3cological: G. c. . ncrease comfort.
NonRx therapy: Ocular decongestants and/or lubricants may be useful.
Rx ,
Non-prescription th.erapy: Clean gauze compresscs, avoid cleanser and avoid eye
patches. Polymyxin B/gramicidin (eye drops), polymixin Blbacitracin. (ointment).
Rx therapy: Trimethoprim/polymyxin B (drops), erythromycin or bacitracin (ointment),
Sulfacetamide 10% solution
Viral conjunctivitis
G:Ommon cause: sirnp)ex_viruS"
Symptoms: is profuse, serous
.- . .
for itchy and watery eye, Qwpatadinl!
(antihistamine and mast cell stabilzer), Nedocromill"'lodexamid&(mast cell stabilizing
agent) alleviates. f<?eforol3e (Nonsteroidal anti-inflammatory eyedrop)-for itching &
redness.
Other types ofConjunctivilis include:
Chlamydial Conjunctivitis: Trachomatis
Fungal conjunctivitis: In rare cases:
Rickettsial conjunctivitis: Rare
Parasitic conjunctivitis: Rare
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oOphthalmic, OTIC and
Drug causes dry eye
Anticholinergics: Antimuscarinic drugs
First generation antihistamines
B-blockers: propronalol, tiroolol
Diuretics: hydrochlorothaiziodes, indapamide
Isotrentenoin
Niacin (in hyperlipidimia)
Phenathiazine antipsychotics (eg. Chlorpromazine)
TCA's (amitryptiline)
Goals ofTherapy
Ease patient discomfort and minimize symptoms.
Prevent or delay complications
Educate patientsoabout their condition and oencourage compliance, especially those
with long-term disease
o
.
Cleanse eyes thoroughly
Blepharitis and hordeolum benefit from warm, moist compresses applied for up to 15
minutes, 3 to 4 times a day
Cool, moist compresses have a soothing effect for conjunctivitis and dry eye
Treatment
Nonprescription Therapy: Artificial tear solutions: An ideal tear replacement product
would posse:
Electrolytes in concentration similar to that normal tear.
An osmolality of2000 to 280omOsm
Viscosity of less than 20 centipoise
No cytotoxic
Preservative free.
Pharmacotherapy
Substituted cellulose ethers:
Carboxymethylcellulose 1%
/ Polyvinyl Polymers
Polyvinyl alcohol 1.4%
Sodium hyaluronate
Ointments: Petrolatum and caorbomer
Artificial tear inserts - hydroxypropylcellulose .
Prescription therapy:
704
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Acetylcysteine
Methylprednisolone
Instillation of artificial tears every 1-6 hours for a trial period of48 hours
Emollients can cause blurring of vision and are better suited at night
Any eye irritation that fails to respond to nonprescription therapy within 48 hours should
be referred to an eye care professional for proper diagnosis
J. ,(ntibistaminos - may cause photophobia or allergic reactions
Antazolinc::. pbeniramine. pyrilamine
2. Anti-invectives - polymyxin Bcombined with bacitracin or gramicidin
3. Artificial tears - chemically inert and coat the eyes
Help them retain moisture
Protect from irritation
Slow turnover of teaTS
Examples are: dextran, melhylcellulosc, hydroxypropyl methylcellulose,
Polyethylene glycol, polyvinyl alcohol and sodium carboxymethylcellulose
4. Astringents - not to be used for hordeolum or allergic conjunctivitis
Zinc sulfate a mild astringent that clears eye secretions
5. Decongestants - can cause rebound hyperemia if overused
Contraindicated in patients with glaucoma
Examples: naphazoline, oxymetazoline, phenylephrine. tetrahydrozoline,
xylometazoline
6.Emollients - soften eye tissue and protect it from drying
Lanolin. mineral oil, petrolatum
U.$f; 0 '" tUedt (
How to administer eye drops ,
Wash hands thoroughly Ii 1+hflp"J h<...k do,.,......
Tilt the head oack or lie down
With eyes open, gently pull the lower lid below the eyelashes away from the eye to
form a pouch
Approach the eye from the side and hold the container near the lid (at least 2.cm
away). no not touch the lid or lashes
Look toward the ceiling, Looking up moves the center of the eye away from' the
instillation site, minimizing the blink reOex.
Instill one drop into the pouch. Hold this position to let the drop fall as deep as
possible into the pouch
Look down for several seconds and then slowly release the lower lid. Looking down
brings the cornea into maximum contact with the drop,
70-5
. . '
Gently close (don't squeeze) the eyes for 1 to 2 minutes while applying gentle
pressure to the bridge of the nose for 30 to 60 seconds. Gentle pressure prevents the
drops from being drained from the eye
A tissue may be used to blot around the eye, but do not rub. Closing the eye helps
prevent loss of solution caused by blinking. If the eye is closed too tightly, 'the
medication may be expelled
Don't rub the eye. Try not to blink
To apply several drops, wait 3-5 minutes after the instillation ofeacndrop
Never contaminate the dropper tip or the top 0 the container by allowing it to touch
the eye, eyelid, eyelashes, fingers or counter surface
Eye care products
Contact Lenses
Types of contact lenses
Rigid gas permeable lenses -7 Hydrophobic; Silicone, fluorosilicone acrylate, polumethyl
methacrylate (PMMA).
Soft lenses7 hydrophilic: Hydroxymethacrylate
Contact lens solutions (cleaning solutions)
Two types:
Surfactants; remove loose debris
Protein cleaners-remove proteins-soft lens
Drugs interaction with contact lens:
Oral contraceptive alter tear composition results decrease lubrication.
Antihistamine, Hypnotics, Sedative decrease blink rate (blink increases hydration)
Anticholinergics, antihistamines, TCA's7 decrease tear volume
Isotrentinoin4 itching and decrease wear time in soft lens users.
'. Aspirin-7. Ocular irritation, redness in soften wearers.
Drugs cause discolorati'on of soft lens.
~ r Dopamine
~ Nitrofurantoin
S-r' Sulfasalazine
& e-.... Tetracycline
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~ Q.,t"?' re:p' Phenazopyridine
(Sf) Phenolpthalene
~ ., Rifampine
CV ~
Disinfecting solutions kills bacteria
Preservative-7 maintain sterility of solution
Saline solution preservative minimize the risk ofcontamination
Wetting and rewetting solutions provide wetting, lubrication and cushioning
functions.
70-6
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www.Phannacvprep.com Ophthalmic, OTIC and Mouth Conditions
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Pnirltr
Mouth Ulcers
Non-prescription Medications
1. Local anesthetics (topical): Benzocaine, lidocaine
2. Oral analgesics: Acetaminophen; ASA o.
3. Protectant: hydroxycellulose; base agent (Zilactin, Oractane)
Prescription Medications
I. Corticosteroids
2. Fluocinonide
3. Clobetasole
4. Triamcinolone
Dental Abscess: accumulation of puss in dental cavities.
Drug of Choice: Pcn V or Amoxicillin or Erythromycin (base for adults and estolate for
children)
Cold Sores
Cold sores sign and symptoms begins with prodromal symptoms of mild burning or
itching on the lips
Small vesicles filled with clear fluid which eventually ruptures and crust over
Last for 3 to 10 days

Oral herpes infection; also called fever blisters is caused by herpes simplex virus I
(HSVI); transmitted through direct contact. Usually appears on the lips also on hard
palate or gums.
'also'!cuoWuas tfclirrent,lie;p<,s4i!tialisl
Usually caused by activation oflatent herpes simplex virus type I
Primary infection occurs between 6 and 36 months of age
15% of adults have primary infection
Recurrent infection occur in 20 to 45% of previously infected people
Mostly get first infection with herpes when they are infant
Virus remains in the body and spread through physicaJ contact
Abreva (docasanol): is used for recurrent cold sores
Acyclovir ointment
Nonprescription medications
Phannacotherapy
Topical anesthetics
70-7
I'
Ester type: Benzocaine, tetracaine; contact sensitizers

'. .
External analgesics
Camphor, menthol, and benzyl alcohol
Counterirritants commonly found in cold sore balms
Astringent: Burrow's solution or cold compresses with tap water applied 3 to 4 times
daily is helpful for cold sores
Sunscreen with SPF 15; recommended to prevent cold sores in those with recurrence
after exposure to sun'
Protectants
Petrolatum, ZnO, cocoa butter, allantoin, and calamine
Prevent drying of lesions from cracking or fissuring
Heparin sodium and zinc sulfate (Iipactin) - reduces pain duration
Shorten time required for lesions to heal
Pre cription medication
I. Antiviral
Acyclovir
, CANKER SORES
Recurrent aphthous stomatitis; usually appear on the cheeks, tongue, soft palate floor of
the mouth
Canker sores: visible manifestation of recurrent aphthous stomatitis
Streptococcus sanguis partly the cause
Autoimmune mechanism is also implicated
At least 20% is affected
'}\T.orfien. tyv:',ice:-<l$"sUseepti Qlef<\SiJlltmq
Susceptibility appears to be inherited
Canker sores sign and symptoms: painful; recurrent ulcers in the oral mucosa ,
3-10 mm shallow lesions
Round with white center and red halo
Persist for 7-14 days
Treatment:
Topical anesthetics ,
Ester type: Benzocaine (contain up to 20% benzocaine), tetracaine; contact
sensitizers
Applied to only small areas of the mouth to prevent a "cotton-mouth" feeling
and loss of oral sensation.
Protectants
Petrolatum, ZnO, cocoa butter, allantoin
70-8

HeialtsaliVW
Emollient mixtuFes or denture can alleviate pain
Chlorhexidine gluconatc rnouthw.ashes; help resolve cankers
Xerostomia (dry mouth): Xerostomia is a dry mouth conditions in which there are no
salivary secretions and also caused by improper functioning oflhc salivary gland
(Sjogren's syndrome).
Treatment of eruption cysts
In general cysts rupture spontaneously.
Rare cases surgically removed, if significant discomfort or interferes with feeding
occurs.
Ophthalmic, OTfC and Mouth "Conditions www.Phannacyprep.com
Dental Caries: Destruction of calcified tissue resulting from an infection. Dental caries
most commonly caused by Streptococcus mu/ans. This acids that

Treatment:
I. Tooth paste contains
Detergents (sodium laurel sulfate; sodium sarcosinate)
Humectants (glycerin, propylene glycol)
Whitener (peroxides; sodium triphosphate)
Fluorides - reduce caries formation
2. Mouth wash contains
Cetylpyridinium chloride may cause staining ofteeth
Chlorhexidine; may cause stains, taste change, discoloration of tongue
3. Triclosan
Oral fhrush
Also known as Candidiasis; caused by fungus Candida albicans.
Drugs that commonly cause oral thrush arc inhaled corticosteroids
Patient self care tips: Rinse mouth with water after inhalation corticosteroids spray
Teething pain
Nonphannacological tips
Hard, sl1100th and clean products may be given to the child to bite and chew on such
as frozen face cloth.
Safe teethers cooled in refrigerator before use can be helpful.
The Canadian dental association recommends rubbing the back ofa small, cold spoon
on the gum.
Non-prescription medication
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Ophthalmic, OTIC and Mouth Cond.itions
. .:.-.
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Antiplaque . . .
Antimicrobial agent helps gingivltis:plaque cavities an4 tartar.
Gingivitis/periodontitis
The infection of gingival tissue is gingivitis.
Non-prescription
Mouth hygiene
Anesthetics: Benzocaine, and eugenol
Analgesic- Acetaminophen
Prescription
Chlorhexidine mouth rinse
Endocarditis
Caused by S. viridens and S.
Prophylaxis
Amoxicillin Ig before surgery, followed by 500 mg TID for 3 days
Azithromycin 19lday followed by 500mg OD x 2 to 3 days (for patients allergic'
to betalactam)
Clindamycin 600 mg followed by 300 mg QID x 3 days' (for patients allergic to
betalactam)
Reference: Canadian Pharmaceutical Specialties (CPS)
Trench mouth
Definition: Acute necrotizing ulcerative gingivitis (ANUG) is caused by overgrowth of
spirochete and fusiform microorganism
Otic disorders
Excessive/impacted earwax

Narrowed ear canal
Large amount ofhair in the canal, occurs often in elderly .
Ineffective or insufficient chewing or talking, especially in elderly
Improper removal methods
Earwax softening agents:
the only approved as safe and effective agent for earwax
re1noval. . . .
70-10
OTe:
..%, (Burosal)
Benzothenium chlorideiL03%
.Acetic acid 2%
Prescriptions:
Gentamycin otic solution (amino glycosides actiye against gram -ve,
(pseudomonas), and S. aureus (side effect: ototoxicity)
Ciprofloxacin ophthalmic solution (no ototoxicity)
To prevent vertigo, medication in the vial should be warmed in the hands and put 5-
10 drops in the ear BID for 4 days .
Do not usc ifear drainage, discharges, pain, irritation or rash occurs
Do not use if there is injury of perforation of ear drum
If the patient feels pain or severe fullness upon instilling the drops, this might be an
indication ofruptured t'mJ i cmbranclJ ":j;:e;o.__7
Ophthalmic, OTIC and Mouth 'Conditions . www.Phannacyprep.com
Non-phannacological
Hot compresses; pain, discontinue sticking
Cold compresses; swelling, itch
Avoid using shampoos
Do not manipulate with swabs
Removal earwax
Use blow drier aner shower. Bath not shower
Otitis Externa (swimmer ear)
It is the inflammation of ear canal. This is commonly known as swimmer's car or hot
weather car. Most often it occurs during summer.
othe-f-'Cbmmon
t'til:@uSijjrganisl1\l.
Symptoms includes itching, moving pain in air, a fluid discharge from canal in severe
cases, decrease or loss of hearing
Altitude and car pressu re:
This is caused by not functioning rob.eiproperly
. . .. 'r",
Pam can be reduced or prevented through:
Swallowing (chewing gum or eating candies) to activates the muscle lhat pull open
the Eustachian tubes and helps to unblock the ear. Giving a bottle of milk or juice to
the baby may reduced or prevent ear pain among babies.
Yawning is effective in opening Eustachian tubes.
Pinching the nostrils using the cheek and throat muscles, and forcing air back of the
nose, may help in unblocking the ear.
Decongestant may be a great help either an oral agent (Sudafel) takcn an hour before
descent, or topical agent (oxymetazoline) should be administered 10-15 minutes
before descent.
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www Ophthalmic; OTIC and Mouth Conditions
Boils:
Are infected hair follicles in the ear canal that usually cause by S. auretis. This is
self-limiting and is best treated by application of warm Compress".
Otitis Media
Is the infection of middle ear.
4 types:
Myringitis
Acute otitis media (most common cause: Spneumonia, H influenza, and M
catarrhalis
Chronic suppurative otitis media
Otitis media with effusion
Symptoms:
o Pain in the ear
o Fever
o Fluid
Drug of choice: Amoxicillin or +/- clavulanate
Tips
l. 1 gtt au 2. 1 gtt AU 3. Carbamide peroxide
4. otitis extema 5. cold sores 6. wax removal
7. antibiotics & 8. inflammation of the 9. HSVI
corticosteroids eyelid margin
10. HSV2 11. CMV 12. Epstein barr
virus
13. VZV 14. pain in eye 15. blurred vision
16. blepharitis 17. dry eye 18. diabetes
19. polyvinyl 20. hydroxypropylmethylcell 21. Thimerosal
alcohol ulose (HPMC)
22. 0.01% 23. sterile & isotonic 24. Tropicamide
25. emollients, 26. Acyclovir 27. cerumenous
anesthetics, gland
astringents
and Acyclovir
What ophthalmic conditions require referral to doctor? ( 14, If, ,',,-7 )
What is added in ophthalmic preparation to increase eye contact? ( '1,2. 'll )
the most allergic ophthalmic preservative? (1- , ) -
Benzalkonium chloride concentration as p'reservative in ophthalmic drops? ( )
Ophthalmic preparation should be? ( )
What eye drops that are used in eye exams? (2... )
Cold sores are caused by? ( .1 )
What is treatment of cold sores? ( Q!:,l" )
What is not a treatment cold sores? ( 7 )
70-12
Both eyes is directed as? ( I )
Both C is directed as? ( 2.. )
Earwax removal is? ( .s )
Swimmer's ear is? ( it )
Abreva is used for? (5" )
What is active drug of valacyclovir? tl-' )
Ear wax glands are also known }
Mineral oil in ear is used as? (C. )
Acyclovir is effective against? (j,'., ll,' 2- )
Blephantis is? ( i )
An autoimmune disease characterized by destruction of the lacrimal and salivary .
glands resulting in the inability to produce saliva and tears. 5 I ceq
Stye (hordeolum) require warm compress where as blepharitis require cold compress
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70-13
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aTe Drugs, aptihistamine, decongestants and
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OTC
Decongestants
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Questions Alerts!
Topical and oral decongestant precautions and contraindications.
Antitussives like dextromethorphan, codeine DIs with MAOI
Pharmaceutlca Agents
1. Analgesics/antipyretics; acetaminophen, ASA or ibuprofen
Helpful for pain and fever
Don't administer ASA to infants, children, teenagers or young adults because of
Reye's syndrome
2. Antihistamines - relieve rhinorrhea, sneezing and watery eyes associated wHh cold
Often cause drowsiness and drinking alcohol or taking other antihistamines or
sedatives can increase effect
Paradoxical excitability, nervousness and difficulty sleeping sometimes occur in
children ! .
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3. Antitussives: tlJfl
congestion is not present
mmIB when
4. Decongestants:
Oral agents are more effective but contraindicated a ellts.. rt
__
71-1
Available treatments lessen the severity of symptoms
OTe Drugs, antihistamine, decongestants and antitussive" www.Pharrnacyprep:com

5. Expectorant: guaifenesin is the only one available in Canada
Adverse effects are rare
Overdose can cause nausea and vomiting
Contraindicated in patients with chronic, persistent cough, patients with lung
disease and in women who are pregnant or breast feeding
Infection is transmitted by:
patients taking antidepressants, and

Topical agents can cause rebound congestion if used for more than 3 to 4 days

i
bli
iijjft!tcl44IS' "'eudumwmyitt',,(iQSQ%)
Expectorants: Guifenesine
productive cough (cough with sputum)
Antihistamine: To treat Allergies, Allergic rhinitis, Insomnia, Motion sickness, Nausea
and Vomiting
Precaution: driving, operating machine, anticholinergic side effect, constipation

Congestions and cough, shortness of breath
Contraindications: uncontrolled blood pressure, uncontrolled diabetes, glaucoma
01: MAO I, is not taken with oral decongestants

01: MAO! can cause serotonin syndrome
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aTe Drugs, antihistamine, decongestants and antitussive
.' '. . .'. . .'.
Hand to hand (Virus contact nasal mucosa) and via aerosol particle.
, . .
Signs And Symptoms
First sign is usually sore throat, described often as dry or scratchy. sensation
Rhinorrhea and nasal congestion follow the sore throat. Nasal discharge is
initially clear and watery, but becomes thicker as the infection progresses
Congestion may lead to sinusitis and headache or to etic symptoms
(especially in children)
.Postnasal drip is.common and can cause coughing or laryngitis.
A dry cough often follows the nasal congestion
Prevention:
Wash hands often
Cover mouth while coughing
Avoid direct contact with contaminated objects
Treating the common cold
No cure for common cold. Remedie? that may help relieve some of the
discomfort
Stay at home if possible and rest in bed
Drink plenty of fluids (up to 8 glasses of water or other fluid a day). Hot liquids
are particularly helpful for a stuffed up nose
Keep the air around you well humidified to make breathing easier

Bed rest
Drinking plenty of fluids
Humidifying the air
Pharmacological Treatment
- spothing to a sore thro3t
First generation antihistamil],g,s - relieves rhinorrhea and watery eyes
Topical and oral nasal decongestants - relieves stuffy nose and sinuses'
Oral decongestants more effective than topical but produces more adverse
systemic effects
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Zinc - controversial but zinc gluconate lozenges may reduce some symptoms of
common cold but may cause nausea and impart bad taste
71-3
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Recognizing A Common Cold
OTe Drugs, antihistamine, ahd"antirussive .
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Typical signs and symptoms:
Sore throat: often dry, scratchy feeling rather than a painful feeling
Runny or stuffed up nose: appears just after sore throat. Nasal discharge is clear
and watery at first and become thicker as cold progresses
Watery eyes: common in early stages of cold
Headache and sinus pain: discomfort usually from inflammation of the
sinuses
Dry cough: usually follows the nasal congestion. Becomes watery as the cold
progresses
Fever: common in children
Fever
Fever: Body temperature, which is above the normal range (37C) resulting from an
elevated t.hermoregulatory set point in the anterior hypothalamus
Generally caused by infection, inflammatory diseases, neoplasms and immunological
mediated conditions
Enhances the body's ability to fight infection
An important clinical tool in monitoring the progress of an infection or response to
antibiotics
Signs and symptoms

wmifiOf
High fever in children can cause convulsions (fabrile seizures) while in adults can
cause confusion or even delirium

Hyperthermisa - increase in body temperature without an increase in the
thermoregulatory set point
Sponging with tepid water may soothe but wont reset the hypothalamic set point
Alcohol sponge is not recommended
Remove all excess clothing and bedding to allow for heat dissipation
Give fluids to ensure adequate hydration
71-4
www.Pharmacyprep.com aTe Drugs, antihistamine, decongestants and antitussive
.' .
Antipyretics - reduce body temperature by reducing the hypothalamic set point to
normal
Don't administer ASA in infants, child or teenager because it can cause Reye's
syndrome
1. Acetaminophen - effective antipyretic
Treatment of choice for fever in infants, children and teenagers
Patients with liver disease or who consume 3 or more alcohol containing drinks per
day should consult a physician before taking acetaminophen
2. Acetylsalicylic acid (ASA) - useful antipyretic in adults
Can cause stomach irritation leading to heartburn, bleeding and ulcers
Has marked antiplatelet effect
Patients with asthma or kidney disease or taking other medications should consult a
physician before taking /lSA
3. Ibuprofen - fever in adults, children and infants
ian cause stomach irritation, leading to heartburn, bleeding and ulcers
by immunoglobulin IgE.
al

.

Seasonal and perennial allergic rhinitis often co-exist in the same time patient
Th . .: but idl_
I .. s.
Symptoms of seasonal alle'rgic rhinitis are often worst in the morning when pollen
counts are highest
Allergens Pollens, molds, house dust mites, cockroaches, and insect allergies stimulate
the lease of chemical mediators such as:
Histamine
Leukotrienes LTC
4
, LTD
4
and LTE
4
,
Prostaglandins Dz,
Kinin
71-5
71-6
"tflda..gr lire ;;u.
Watery eyes
Fatigue
side effects: sneezing, nasal stinging, irritation, bad taste
OTe Drugs, antihistamine. decongestantS and antitussive
in the mouth
Treatment:
Antihistamines"? sneezing, itching of eyes, ears, nose, and throat, runny nose,
tearing.
AiibmTJnlii)rdgsl.pJ;ata.dWelje.xeMJClsa!;liOOgestj,,""
Corticosteroids
Mast cell stabilizer
Others
Anticholinergics
Antifeukotrienes
Mast cell stabilizers
Symptoms
Runny nose
Pruritis of eye ear and throat
Sneezing
Cough
Risk factors:
Gender childhood, male, age before 20 years (80%), family history of atopy
increases risk for rhinitis, asthma and eczema
Environmental control
Pollens
Molds
House dust mites
Animals
Insect allergies
Influenza (flu)
Caused by: viral infection. Two types of virus cause serious infections: Influenza A
(most common and more severe) and Influenza B.
Effects are on the superficial epithelium of the airway tract. OI..A....
Symptoms: t -/...
II, ,;,/<.
Dry cough f-M /.....-u. (]
Sore throat .J.J
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VQCC/L0(2.
Nasal distharge D'
Chills and fever (immune response), and sweat
Muscle pains
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Weakness/fatigue
aTe Drugs, decongestants and antitussive
Persons at high risk of flu
Persons over 65 years age
Any resident of nursing home or other care facilities regardless of age.
Adults and children with,chronic cardiac or pulmonary disorders sever enough to
require regular medical condition.
Adults with chronic condition such as asthma. COPD, diabetes mellitus, cancer,
im.munodeficiency or immunosuppression, renal disease, anemia or
hemqlobinopathY. - ---
Children over 6 months of age to 2 years
----------------
Pregnancy
.-
Persons who should not take flu vaccine?
Less than 6 mo age

Person with flu symptoms
....-e:::::W: :::,IJU'''
Treatment:
Nasal decongestants
Antihistamines
Antitussive
Expectorants
Flu shot are given annually
Influenza season between October through April
_.... -
Immunization season from October t rough November
J." - ..
Sinusitis
Inflammation of sinus in response to infection or allergy and may be influenced

by anatomical abnormalities.
Sinusitis is more common in children.
Caused by (70%):

Symptoms persist more than three months consider as chronic sinusitis: Caused by
H. influenza (50%, S. aureu, P. aeruginosa, Fungi patient)
Treatment:
Nasal decongestants, Antihistamines, Antitussives, Expectorants
71-7
Medications: Nasal decongestants,Antihistamines, Antitussives, Expectorants, Analgesic
.. fWISIit!J6)

Inflammation of pharynx. (Part of other illnesses cause by infections)
irahpI15JOOJJfitW: Eestein-bar infection, Influenza, Common cold, Measles, Vericella
Allergic rhinitis, Sinusitis, Or allergies.
.
OTe Drugs, antihistamine, decongestants and antitussive www.Pharmacvprep.com
Pharyngitis
Symptoms:
Sore throat
Fever, headache
Swollen lymph nodes, usually in neck
Runny nose
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Ref: Formulary for general practice drug of choice, p.98, 1998
Antitussives (for cough): Non-narcotics antitussive: Dextromethorphan,
Diphenhydramine
Narcotic antitussive: Codeine and hydrocodon
a) Dextromethorphan
Widely used in aTC cold remedies to suppress non-productive cough
Cough
Symptoms of many respiratory diseases. Can result from many chemical or mechanical
effects.
Common causes of cough are: Asthma, Chronic bronchitis, Congestive Heart Failure
(CHF), Drugs (eg. ACE inhibitor), Emphysema, Foreign body, GERD, Post nasal drip,
Upper/lower Respiratory Tract infection.
Treatment: antitussive such as: Dextromethorphan, expectorants:
p' ! H, P. ... ;8.'liI.. IIIIl:h1i1JlIl1!l")
Treatment:
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aTe Drugs, antihistamine, decongestants and antitussive
. '. .. ,
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P.O onset 15- 30 min
Duration 3 to 6 hours
Side effects: Nausea, Drowsiness, Dizziness
Contraindications: CNS depression will increase if drug used with: Alco"hol," Narco"tics,
Sedatives-hypnotics, Barbiturates, Depressants
Narcotics Antitussive:
Codeine:
Side effect: Drowsiness, Sedation, Constipation (Stimulant laxative b"isacodyl or senna),
Nausea, Vomiting
15-30 mg of dextromethorphan =8 -15 mg of codier:le
Expectorants
Gauifenesen (extract of tar)
Ammonium chloride
Expectorants reduce sputum viscosity and allow more effective removal of secretions
from the respiratory tract.
Gauifenesen (extract of tar)
Mechanism:
Increase ciliary action
Fluid from the respiratory tract less viscous
Facilitate the removal of mucus
High doses cause emesis
Side effects:
Rare (drowsiness, nauseas, vomiting)
Ammonium chloride:
Mechanism: Irritant .to stomach, Causes reflex increase in airway mucus
secretions. High doses will cause acidosis in individuals with renal failure
Decongestant
Topical decongestants
Oxymetazoline
Xylometazo/ine
Decrease nasal airway resistance and nasal blood flow, but usually do not cause
systemic action.
Act rapidly within 10 min
Lead to rebound nasal decongestion (rhinitis medicamentosa) w.hich usually
occurs 5-10 days of treatment.
Short term treatment, 2-3 days
71-9
Nasal decongestants:Phenylephrine, Propylhexedrine
Tips
Side effects:local burning sensation, Sneezing, Dryness of the nasal mucosa.
Bradycardia, Tachyc:ardia, Hypertension
Contraindication:
Uncontrolled hypertension, Severe coronary artery disease, MAOI, Glaucoma,
BPH
OTe Drugs, antihistamine, decongestahts and antitussive
Common cold is caused by? (self-limiting viral infections of rhinovirus (30 to 50%) &
corona virus ( I' )
Common cold symptoms{runny nose, sore throat, watery eyes, sneezing, low grade
fever & malaise) (j,' ,10)
Contraindications of oral decongestants J Bf, d,cJ.d-e& .(
www.Phannacvorep.com
Side effects:
eNS stimulation (mild), Insomnia, Headache, Irritation, Tachycardia or
palpitation, Increase of BP in hypertensive patient. Affects blood sugar levels in
diabetics.
Systemic decongestants:
Pseudoephridine (Sudafed, Actifed)
Epinephrine
Phenylephrine
Phenylpropamine
Cause nasal vasoconstriction and decreased nasal edema within 30 minutes and
continues for 6 hours (regular formulation)
Oral (onset of action 30 min)
Caution with patient, Hypertension, heart disease, hyperthyroidism, diabetes,
narrow angle glaucoma, BPH.
Topical: Onset of action 5-10 min.
Phenylephrine
Naphazoline
Xylometazoline
1. glaucoma 2. hypertension crisis 3. runny nose
uncontrolled BP 5. diabetes 6. sore throat

7. BPH 8. watery eyes
,.
sneezing
10. low grade fever 11. self-limiting viral infections of 12. malaise
rhinovirus {3D (0 50%) & corona virus
(10 to 20%)
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,/
MAOI + sympathomimetics like pseudoephedrine give __> 04S,.1
Echinacea purpurea probably can be effective in the prevention and treatment of
common colds in adults. . L... "ILL c..r
1.(r.CQc. dt<t\tC..
Topical antihistamine examples Le.\focoha..s:-Hra.. aVG.lloJ.lL. a.,J e,pH1 1-{Go:Sc.{
avt:"L Cs- '-""'fW'ff
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Flu vaccine is taken every -7 ' 0'
When is the flu season in Canada -h
Flu immunization season -7 b.t!5I" .... IY yt.-L.se.AJtJ'1 tte.., ck:l- -h,
Contraindications of antihistamines o....t{OUJ1 SCI m
Cautions of oral decongestants -7 13 p
I
71-11
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OTC drugs for Nausea,
Vomiting, Constipation,
Diarrhea, and Hemorrhoids
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72-1 d
A\ul<J.
i'l<!qe!
ltaUJ... :t"...

Pr c associated nausea and vomiting: Also known as
'Morning Sickness
Copyright 0 20002011 TiPS Inc. Unauthorized reproduction of this manual is prohibited. This
manual is being used during review sessions conducted by PharrnacyPrcp.
Nonprescription
Self care measure
.
Eat at all times of the day when nausea is less severe
Eat before getting up from bed (in the morning)
Discontinue iron supplements (temporarily) because this causes nausea and'
vomiting
mg may reduce nausea and vomiting
...
NAUSEA & VOMITING

Non-prescription anti-emetic drugs
v- Dimenhydrinate: used for all types of N&V (except post chemotherapy N&V);
given 30 min before exposure
J'" Meclizine: used for all types of N & V
Promethazine
Diphenhydramine: alternative for dimenhydrinate
NO Pyridoxine (vit. B
6
) used only for pregnancy induced N&V (PANVj _> No .se,dc..JiO'1
Scopolamine: used only for motion sickness
Ginger root
. Sedation.i.s common side effects of non-prescription antiemetic drugs (except
pyridoxine). H alertness is required, scopolamine or promethazine + ephedrine or
dexamphetamine.(used by airline pilots)
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Dimenhydrinate: use only for 2 to 3 days; refer to physician jf ineffectIve
Pyridoxine (vitamin 8
6
): can be used alone; no SI e ec s rug interactions.
Prescription V,f-t3 '"
.Drug of choice Diclectin (pyridoxine 10 mg + doxylamine)
Opioid induced nausea and vomiting (OINV)
Management:
Alter administration schedule (make sure nausea does not interfere with meal)
If pain does not-decrease, attempt an increase in opioid dosage (pain could be
caused by nausea and vomiting)
Switch to a'.!other narcotic drug
V Use other anti-emetic: Metodopramide Perchlorperazine
72-2
M..Js1

'"ouR" <t ?
-- --
-
.r
Post chemotherapy nausea and vomiting (PCNV)
Self care: Alter diet (emphasize on mall & frequent meals; avoid fatty or spicy foods)
Non-prescription medicines ar not seful; Prescription medicines are metoclopramide,
dronabinol, and perchlorperazine.
. " ....
low emitogenic drugs '_--, 0
Treatment start withJdexamethasone pm ]
Delayed nausea and vomiting
The drug of choice for moderate emitogenic is dexamethasone
Drug of choice for acute emitogenic is SHT3 blockers: Ondansetron +
dexamethasone
o. Highemilogenicdrugs MJ:l Co M "0"\ sic k""",::,'
The drug of choice for --=-:.:.;:"Tl":";:;-"'--;:-::-:-:
Anticipatory nausea and vomiting _ :::::DOC is Sc.o
The drug of choice is benzodiazepine (Iorazepam)
= Not- F cJ.,; 1a/A.tM->
Motion sickness
Self care measures
/"Avoid eating large meal with in 3 hours of travel
dairy products or food high in protein content, high-calories, or high in sodium
fore travel. -- -
, void alcohol, smoking and bad smells
Treatmen
. The drug of choice is scopolcrmine trans dermal patch
.. ' }; not be used in children
0\\ G Placed behi.nd ears. 1 patch every 72 hrs; can be removed and reused within 72
\ \-tfV hours but should rotate site of application
...>-P .effects include constipation, dry mouth, blurred vision, skin rash, disorientation,
i""
.V Copyright C 2000-2011 TIPS Inc. Unauthorized reproduction oflhis manual is prohibitcd. This
c., manual is being used during review sessions conducted by PhannacyPrep.

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DIARRHEA
Management ;
Rehydration and maintain electrolyte balance can reduce diarrhea
Children:
Continue breastfeeding & ofal rehydration solution (DRS) should be offered;
otherwise, discontinue all food and drinks and give DRS.
Give DRS as soon as diarrhea begins until diarrhea is less frequent
Rapid refeeding should immediately follow rehydration
If diarrhea with vomiting, give DRS 15 ml every 10 to 15 minutes (using a
spoon).
Oral rehydration therapy (ORT) is the most effective treatment for children with
acute diarrhea
Pregnant: maintain fluid intake; loperamide is safe in pregnancy
Elderly: prompt rehydration is essential
Fruit juice pop, or tea with sugar to high carbohy rate content
of dehydration: dry mouth, crying without tear, sunken eyes, less or low
frequency urination and skin turger. Sweating or frequent urination is NOT a
dehydration symptom
Treatment:
Nonprescription
1. loperamide (Imodium)
Not given to children under 2 years old also in children less than 12 years old
without doctor's advice
Not recommended for acute dysentery! infections diarrhea (bloody stool with
fever).
SE: include abdominal cramps, drowsiness, dry mouth, skin rash
Maximum dose is'16 mg/day (4mg start then 2 mg after each loose BM)
2. Attapulgite (Kaopeetate) - may be used for drug-induced (mild to moderate)
diarrhea; not to be used for less than 2 days
.3. Bismuth Subsalicylate (BSS)
Should be avoided in patients taking anticoagulants, salicylates,
probenecid, or methotrexate.
Avoid in N$AIDs or ASA allergies
Not for children less than 2 years old due to Reye's syndrome
Used in chronic diarrhea, fa! travelers diarrhea & H. pylori management
SE: include black tongue and stools, and tinnitus
4. Psyllium (Metamucil)
l
Copyright e 200<>-2011 TIPS Inc. Unauthorized reproduclion orthis manual is prohibited. This
72-3
/. P.:>-\llitL7Y1 (Me.1-qrrl
4
c..il)
'I d NO\--
taken within 2 hours of other medications because it
reduces absorption of other medicines
Should be taken with at least 2S0ml water to prevent fecal impaction
r
.. 1 and/or esophageal obstruction

Cholestyramine - for treatment of bile acid induced diarrhea
Codeine - for patients who do not respond to non-prescription medicines
Clonidine - for diarrhea associated with opioid withdrawal and diabetic neuropathy
Diphenoxylate with atropine (lomotil) less effective than loperamide
&ilid-ftl 4UZi&OOI15P..V1lJjjQM&tttrJefMtd$U
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Herbal and other Remedies:
Herbal- chamomile, carob, marshmallow, slippery elm, bayberry
Probiotics -live microorganism (bacteria and yeast)
Refer
Refer to physician if diarrhea does not improve in 48 hours with high fever, blood in
feces, severe pain in belly, children less than 6 months old, with vomiting for more than
4 to 6 hours with sign of rehydration; more than 6 8M in one day. .
NONINFECTIOUS diarrhea -drug induced diarrhea could be caused by:
1. Antibiotics
2. agents
3. Anti-inflammatory agents (NSAIDs, Colchicine)
4. Anti-arrhythmics
5. Anti-hypertensive ACE inhibitors)
6. Antacids (Mg-containing antacids'i,raflitidjne, 0lT'!eprazole)
7. Miscellaneous: Misoprostol and theophylline
TRAVELLERS DIARRHEA: caused mainly by E. coli, Shigella sp and Campy/obacter
Prevention: A!pfl .
Hot and cooked meals, cooked vegetables _a'idslwnptfW'Sppm;m)
Peeled fruits, boiled/bottled water, carbonated beverages without ice cubes, TM..elle4.-
pasteurized milk (properly stored) Ca d
Bismuth sub salicylates as prophylactic agent e c S
Typhoid vaccine recommended for travelers C l'
Cholera vaccine for healthcare workers in endemic areas loaJo.L. .
f<["- :jLlunt
Nonpharmacologicaltherapy - 5'/"
1. Children and elderly should use oral rehydration solution.
2. Adults maintain hydration with canned juices, purified water, clear salty soup,
carbonated soft drinks
Pharmacotherapy: Prior to departure, travelers should see physician for appropriate
antibiotics
Copyright 0 2000-2011 TIPS Inc. Unaulhorized reproduction of this manual is prohibited. This 72-4
\
CONSTIPATION
Treatment (prescription)
Drug of choice is ciprofloxacin SOOmg (BID X 3 days)
Alternative: C1zithromycin, cefixime.
Co-trimoxCizole: of limited use due to widespread resistance
Self care measures
High-fiber diet (for children less than 2 years old should have dietary levels of ,fiber
equal to or greater than their age + 5 g/day; 25 to 30 g intake for adults)
Minimum fluid intake of 1500 ml daily
Regular toilet routine (children should be encouraged to defecate 5 to 15 min after
meal)
Moderate physical activity
Heed the urge to defecate, weight loss for overweight patients
Prune and other juices with sorbitol may also help
Pharmacological treatment: laxatives
Drug inducing constipation:
Anticholinergic agents: antidepressants, antipsychotics, antiparkinsons
(Ievodopa)
Cationcontaining agents: Aluminum containing antacids, sucralfate, CaC03, and
Ca supplements, bismuth, and iron supplements
Other drugs: Verapamil, c1onidine, diuretics, cholestyramine, NSAIDs, opiates,
vinca alkaloids, sympathomimetics agents, and ganglion blockers
B....JJ< LA"..}jva. ~ u #
<>All-<, ~ .}!c><.1 "Is- ~
1. Bulkforming (psyllium, bran, and methylcellulose) a.,cI ~ ~ ......... b1.
Adsorb water to soften the stool and increase the bulk, which stimulates peristalsis.
Should be taken with at least 250 mL water to prevent esophageal obstruction
and/or fecal impaction.
Side effects include flatulence, bloating; safer to use in pregnancy
Contraindication in patients with fluid restriction and mechanical obstruction of the'
GIT
Not to be taken within 2 hours with other medications because it reduces drug
absorption
2. Osmotic laxatives: (Lactulose, and glycerin)
MOA: Retains water and allow the stool to pass easier through the bowel
laetulose: not tolerated by most patients because of too much sweetness in
taste
can be used by diabetic patients
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72-5
Side effects include flatulence, abdominal cramps, NVP
;C6rifrairidicated
: ";. ... \! ... _ ':- .- ''''\' .'
Taken with fruit juice or milk only to improve' palatability
Lactulose is the drug of choice for hepatic encephalopathies; it
absorbs ammonia.
Glycerine: softens the stool and lubricates the bowel by increasing water
retention (osmotic properties) in the intestinallurrien; also stimulates rectal
contractions; S/f rectal irritation
3. Saline laxatives (Mg hydroxide, and Mg sulfate)"
MOA: Same mechanism of action as osmotic laxatives
Mg hydroxide
Sf: diarrhea, dehydration and electrolyte imbalance, hypermagnesemia
C/: Patients with cardiac or renal disease
Chilled before administration to increase palatability
Mg sulfate (Eip:g{{;tiVsaltf
Na phosphate (Fleet enemas)
Best administered on an emptY stomach, 30min AC or HS
Sf: includes hyperphosphatemia, hypocalcemia, hypokalemia,
hypernatremia
CI: for pregnant and lactating women
l!6emai] -r Nu
It is not recommended in children < 2 years old and caution in children
below 2 and 5 years.
Not recommended in Na restricted patients
'. Use with caution in patients with renal or cardiac disease
Stimulant laxatives:
. .
o Increase the secretions of water and ions into the lumen and stimulate
\;/' the bqwel wall to contract. MoA- A.
SE: is abdominal cramping -0
More effective
Senna
May discolor the urine from red to pink or brown to black; excreted into
breast milk
., The drug of choice for opioids induced constipation
0 Faster onset of action than laxatives
Bisacodyl
Preferred stimulant laxative for long term,use in patients on H
2
antagonist
and should not be taken within 1 hour of antacids
Tablets should not be crushed, or broken, or chewed (swallowed whole).
Cascara sagrada ("sacred bark")
Copyright (0 2000-2011 TIPS Inc. Unauthorized reproduction of this manual is prohibited. This 72-6
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CI: In children
Excreted in breast milk
May d.iscolor urine red to pink or brown to black
.t castar eil ..
Not recommended in children < Z yrs
(I: in pregnancy due to !urc;ative
Used in emergency procedures
Steel seftener: (Docusate sodium)
Soften hard stools
Used in combination with bulk laxatives
Primary rule is in prevention of constipation
SE: include abdominal cramps, diarrhea, nausea, rash
luitricantfEmeJlient, mineral eil: not recommended in children < 1 year old
Warning:
1. Can decrease absorption of fat-soluble vitamin (ADEK)
2. Increase anticoagulant effect due to decrease absorption of vitamin K
3. Risk of lipid pneumonitis
4. Can lead to hepatotoxicity
5. Can cause anal seepage and perianal discomfort
6. Should be taken on empty.stomach
Best laxatives for:
Infants:
NOT recommended: enemas, mineral oil, stimulant laxative
Recommended: glycerin supplement; lactulose or sorbitol (as stool softener)
Children:
Mg hydroxide, mineral oil, lactulose and sorbitoL
Pregnancy:
Bulk-forming agents, stool softener, osmotic, c1I MG laxatiees
Avoid: stimulant laxative, mineral oil, castor oil
Breastfeeding:
Buik and osmotic laxatives (1
st
line therapy),
Mg Sulfate, cascara and senna (2
nd
line therapy)
Cancer patients:
Stimulant laxatives with enemas intermittently; avoid bulk laxatives
Elderly patients:
lactulose or glycerine supplements (initial treatment)
Bulk laxatives for prevention; stool softener
Avoid stimulant and saline laxatives
long-term use (in opioid patients)
Bisacodyl (with physician supervision)
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manual is being used during review sessions conducted by I'hannacyPrcp.
72-7
... See physician if no BM for 7 days, pain or bleeding in rectum, fever, pain in
belly, and feeling of vomiting. ~ (QUQ5..ffQl.1 Mt.H-.J I.
Flatulence (Gas) and Cramps S; me.+-l1 t CotUJ. U Q 11
Non-prescription treatment: a..u-t!J1 q ~
nD-galactosidase; taken with 1
st
bite of fo09 ~
Lactase; taken with or before ingestion of lactose
~ Sjmethicone: acts by preventing bubbling of liquids in the stomach; not absorb
from GIT. Does not have significant side effects
Peppermint garlic, ginger are alternative therapy
**Refer to physician if symptoms persist for more than 1 to 2 weeks or non-prescription
therapy is ineffective
HEMORRHOIDS (Pile): Abnormally swollen veins in the rectum and anus, caused by too
much pressure in the rectum forcing the blood to stretch and bulge the walls of the
veins, and sometimes rupturing them
Treatment:
Anti-inflammatory agents: Hydrocortisone 0.5% (should not be used> 7 days)
Astringent: ZnO (relieves irritation and burning sensation), calamine (5 to 25%)
local anesthetic: Benzocaine (5 to 20%)
Antiseptics: Domiphen (0.05% cream/ointment)
Protectants : Glycerine, white petrolatum, ZnO
Vasoconstrictor: Ephedrine, naphazoline, phenylephrine
Wound healing: Shark liver oil, yeast
Pregnancy: Correct constipation and taking sitz bath
Analgesic: Menthol, camphor
Prevention:
Avoid constipation
Increase fi.ber diet, fluids, and physical exercise
Regularize stool habits and minimize strain and time on seat
Intestinal worms: (Pinworm, ascariasis, and whipworm)
PINWORM: e..LAte.{obilL!
. VeMvl. culfly
Nonpharmacologlcal measure:
~ l J s f ; ,4/"";'
5
!
P,"" !-OOM<-! S.fl.tfj CQN-
Take shower every morning
Regular cleaning or bedding, nightclothes, under wear and hand towels.
Hand wash, nail cleaning mainly before meals.
During week the follOWing treatment, all family members should wear cotton
underpants. (washed in soap water). Worn day and night change twice daily.
Copyrighl C 20002011 TIPS Inc. Unauthorized reproduction of this manual is prohibitcd. This 12-8
manual is being used during rcview sessions conducted by PharmacyPrep.
.,
Cleaning.of floors .Qf sleeping place.
Clean bedroom curtains where high concentration of eggs.
Avoid shaking linens, curtains before wash.
Avoid thumb sucking in children.
Not effective: Cleaning or vacuuming entire house or washing sheets e'1lery day is
probably not effective to prevent re-infection.
Avoid sharing dishes
Avoid sharing undergarments
P..revention:
1. Proper hygiene
Treatment:
CD Drug of choice Pyrantel pamoate
SE: nausea, vomiting, di?-ziness, headache, anorexia
. .. .: '. .
Avoid in pregnant and with liver disease
Liquid should be shake well before use.
(f) Pyrivinium pamoate
'-r:;fe nausea, vomiting, abdominal pain, photosensitivity
Tablets should be swallowed to avoid staining the
Will color stool red for 24 to 48h after dose; iiso stain and clothes
. (J) p;peraz;neail\Pate PI adlF
Can be used In pregnancy _.JP'---_7: 0<- _
Prescription: . > L../.seJ I",
CD Mebendazole I t'Vl.--
Drug of choice (lOOmg single dose, repeated after 1-2 weeks) a.va..vJ-
For adults and children> 2 yrs . d
SE abdominal pain and diarrhea
Taken with meal _ J1 ,
, Co L.tt",,-,,-, f ...0-- , V)
Tips
1. Psyllium 2. Diclectin Vit B6 + 3. Docusate sodium +
Doxylamine senna or bisacodyl
4. Dexamethasone S. Ciprofloxacin 6. Benzodiazepines
7. Bismuth 8. uncooked food 9. contaminated water
subsalicylate
10. ice cubes 11. fresh salads 12. dry mouth
13. sunken eyes 14. less frequent urine 15. loss of skin turger
16. crying without tears 17. 18.
DOC for pregnancy induced nausea and vomiting (2) idu/ll1 l 'lit D,
t o.y,
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72-9
DOC for low emitogenic chemotherapy induced N& V(t,)
DOC for delayed chemotherapy induced N&V(4)
DOC for anticipated nausea and vomiting((i) m
symptoms of '1., 16', I ,
diarrhea mainly caused by? ( ) <6,1,1 0 J-;::
black stools and tongue is side effect of? ( ) hI s,m:/l,
DOC for traveler's diarrhea( ) 5' WI
DOC in pregnancy for constipation(' ) L.{IV'- d cJ:;...;:eli l.ic....
DOC for opioids induced constipation(3) lois'" c..."Jr-- I
What is the drug of choice for pregnancy induced nausea and vomiting --72-. v,I-B, + 4-
What are the self care measures recommended for N&V associated with PCNV--7 Av&td
DOC for low emitogenic chemotherapy induced N&V --7 c:[
DOC for delayed chemotherapy induced N&V --7
DOC antiCipated nausea and vomiting
Symptoms'ofdehydration--7 C n..J baOet.J'Y'lI1/i
. Traveler's diarrhea mainly caused by --7 B 1 sJ.., ,seJJ4 -I'f 0 'Y'1 r d" 0
- ./3fJMt.Af'f,
What type of food 'should be avoided by travelers to prevent infectious diarrhea --7 t.{
Drug of choice for travelers diarrhea 1-1-'-0..0'1 , I
" 0'- I' I c.eo c..........
What are the most important self care recommended relieve 1 I,
constipation? l5JbeL chKJ-, 'fflMd I o.mvtJ
Drug of choice in pregnancy for constipation? bu-Lk (\I'"" )
Drug of choice for opioids induced constipation--7 5e..JA 4 d 6C-UA"c....tL- '-.-/
.What are the self care measures to relieve hemorrhoids":.7 i Y} hAf' 1
If-Id I ...,Jt:.J.. ,
. ..
Copyright 2000-2011 TIPS Inc. Unauthorized reproduction of this manual is prohibited. This
72-10
Questions Alerts!
Analgesics, and Topical Pain Relievers
Headache: Generally headache is characterized as: Tension, duster and migraine
Tension: associated with stress, tension etc. No nausea and vomiting.
Severe and ultrasevere attacks: Butraphanol, chlorpromazine, dexamethasone,
ketorolac, meperidine, metoclopramide, prochlorparazine, and sumatriptan.
73
Analgesics and Topical Pain Relievers www.phannacyprep.com
N$AIDs side effect and maximum dose
Triptans mechanism and onset of actions (sc is fastest)
Migraineprophylaxis. 4nIdl-,uPf:Jhlof, f>of""''''''! I vtf."'pC/Ml! ,
Migraine:
Unilateral headache, often associated with usea and vomitin
Associated with nausea and vomiting. triggers y Ig t, smell, noise, and food etc
- - - -
Migraine Therapeutic Plan
Mild migraine attacks: ASA, ibuprofen, (adjunctive dimenhydrinate,
metoclopramide), acetaminophen (weak evidence)
Moderate attacks: NSAID, SHT agonist (sumatriptan), DHE (weak evidence),
Combination drugsacetaminophen +cOdeine. ASA + codeine + caffeine + ASA +
butalbital + caffeine
Mild Migraine attacks
ASA: Dose" 650 to 1300 IJ1g q4h Buffered or soluble tablets (not enteric coated)
Ibuprofen: Dose: 400 to 800 mg q6h, rapid dissolVing tablets available
Acetaminophen: Weak evidence of be'nefit. Monitoev
Moderate migraine attacks
NSAlDs (ibuprofen, naproxen, mefenemic acid)
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www.pharmacyprep.com Analgesics and ,Topical Pain Relievers
..
5HTIbId agonists: Sumatriptan (Imitrex), rizatriptan (Maxalt), zolmitriptan (Zornig),
naratriptan (Amerge) ;(!) "'0&"\ {.
Sumatriptan: SE: Chest tightness 0: pregnancy '-4lA..Q...6
Oral 25 50 mg, MR q2 hrs (max 200 mg/24 hrs) -t)Cl p}q., I
Intranasal 5 to 20 mg: 1 spray in 1 nostril per dose f- odl'';j .-f-o
MR in 2 hours (max 40/day): Do not shake and prime U
SC 6 mg, MR 1 hr/max 12 mg/24 hr '0
Take at first sign of headache or at aura ,
"If NO,relief first dose, DO NOT use second use. If it relieved, and second attack, use
after 2 hours.
'. Avoid other triptans use with 24 hours
Combination analgesics
Acetaminophen + codeine + caffeine (Tylenol #1)
OTC Narcotics (Sct,ledule 2)
, ,
'. No prescription req'uired
ASA+ codeine + caffeine (222)
OTC Narcotics (schedule 2)
ASA+ butalbutal + caffeine (Fiorinal); Control drug part 2
Low Back Pain:
Avoid unnecessary bed rest for uncomplicated pain. As well as premature
physical therapy
F.or acute uncomplicated low back pain, NSAIDs are effective for pain relief
particularly during the first few weeks.
For back pain and chronic soft tissue pain, tricyclic or other types of antidepressants
have equivocal efficacy, but ma'y be useful for their antidepressant effect.
Acetaminophen
NSAIDs; ASA
Skeletal muscle relaxant (chlozoxazone, methocarbanol)
Sports Injuries
Goals of therapy:
To reduce acute symptoms (pain, inflammation) and recurrences
To correct contributing factors (e.g. malalignment, muscle weakness)
To return the athlete's weight-bearing capability, flexibility, range of motion,
strength and proprioception to normal
To enable that athlete to participate comfortably and fully in all pre-injury activities
General approach
73-2
---..." I
Pressure Ulcers; Also known as decubitus ulcers (rectal ulcer)
Ulcer care:
Wound debridement; wound cleansing; dr:essing of wound
- Note that for wound cleansing, antiseptic agents/hydrogen peroxide and other
wound cleaners may be toxic to the wound and should be avoided.
. ? /- Cleansing or irrigation of wound should be done with normal saline.
V Tips
Analgesics and Topical Pain Relievers
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R- Rest the injured part
r - tce application to the injured part for 15 to 20 minute x/day for the 48 hours
or longer.
C- Compress the injured part with elastic bandage if there is swelling.
E- Elevation
Other injuries requiring immediate medical attention: eye, hei!d, and nosebleed.
Along with the R-I-C-E therapy ASA or NSAlDs could be. used for 5.hort period for pain
and swelling
Note: a patient with DVT and injury should not follow the full The,rap"
because ice and compression could lead to stasis hence rest and elevation of limb
would be options for such kind of patient .
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1. Propranolol 2. NSAIDS or 3 Triptans,

Acetaminophen alternatively
ergot alkaloids
Avoid prolong bed 5. Throbbing pain; feels 6 Unilateral
4. rest hitting w/ a hammer headache
7 Nausea & vomiting 8. SHTl
b
/
1d
agonist 9 R-I-C-E
10 Amitriptyline 11 Valproic acid 12 Verapamil
What are the symptoms of migraine headache-7 5,',1
What is drug of choice for acute migraine attack-7 3,i( . _ b
What are the drugs used to treat migraine prophylaxis _> 1,10,11, It,
What is prophylaxis is recommended for migraine inpatient experiencing 3 to 4
migraine attacks every month and having constipation -7 :t.
What is mechanism of action of triptans-7
15
General approach for sports injuries (-R-J.-c.- L; )
What drugs are used for migraine prophylaxis? ( '0. I,"I12)
What are recommended self measures for back pain? ( }""I l..at.t
What is the treatment for back pain? ( .....S',4'l.l\! oM..) ArrJa,.,.,,""" f
Migrai ne pain is? ( -rhMlob""3. pb-a, I"""- l" T-+1 ""l va<-1-1, /.Q'" '""--
Pressure ulcers also known as -7 L9 e.c..Ltl,:ft.u wI Ce,..L t..J (e1...t
Mechanismofmusclerelaxants-7 t4-cJ--lS., 1'1 ;011
73-3
Analgesics andTopical Pain Relievers

Drugs used in multiple sclerosis
Select True or False statements
"
A 45 yo man diagnosed with benign prostatic hyperplasia, and migraine prophylaxis.
Propranolol appropriate therapy for migraine prophylaxis?
after taking sumatriptan migraine headache does not relieve than double the dose
of sumatriptan
after taking sumatriptan migraine headache does not relieve than decrease the dose
of sumatriptan
after taking sumatriptan migraine headache does not relieve than do not use
sumatriptan
73-4
www.PhannacyPrep.Com Asthma and COPD
Asthl11a and COPD
Questions Alerts!
Asthma triggers
Mild, Moderate and Severe asthma therapy
. Theophylline drug interat:tion
Predniosone side effects and dose tapering
Asthma: Chronic inflammatory disorder of the airways, l' airways responsiveness,
causes reversible obstruction. In asthma esinophils, mast cells and T lymphocytes plays
significant role. Sensitivity, and hypersensitive of airways to specific and non specific
stimuli, such as air, odour, allergens, virus etc.
Inflammation Normal bronchus
Inflamed bronchial tube
of an asthmatlc
Normal bronchial tube
EsosinophUs
Neutrophlls
n'mphoO'tes
Eplthellum
Fig 72.1
HeaItW
74-1
www.PhannacyPrep.Com Asttuna and COPD
Beta2 Adrenergic Agonist
MOA: beta2 stimulation causes increase camp in smooth muscle leading to
bronchodilation
Short acting beta2 agonist (SABA)
Inhaled: Albuterol (salbutamol), terbutaline, isoproterenol
Onset within 5 min
TV: relieve branchoconstriction, the acute symptoms of cough, wheezing and chest
tightness, asthma emergencies and exercise induced asthma.
SE: Tremors, nervousness, weakness, flushing of face or skin nausea and vomiting
Regular use can lead to decline in lung function.
Oral Beta2 agonist: Albuterol (salbutamol) Orciprenaline, and TerblJtaline
More SE and less bronchodilation effect than inhaled preparations
Long acting beta2 agonist (LABA)
Inhaled: Fonnoterol (full B
2
agonist), salmeterol (partial agonist)
Onset: 14 min and duration upto 24 hours. Regular BID treatment
TU: Maintenance therapy and exercise induced asthma NOT for acute. Used in
patients already taking corticosteroids
Fonnoterol can be used for acute and maintenance
Anticholinergic: Ipratropium bromide: useful as alternative for patients who are already
susceptible to tremors or tachycardia from B
2
agonist
Tiotropium is long acting anticholinergic once daily, it is administered by handihaler
Corticosteroids
rcs: Benefit t lung function, 1aif\ay hyperreponsiveness, 1symptoms of
excerbations
Max clinical effects in 2 to 4 wks. Fluticasone in few days
Given 2 to 4 pfBID
SE: oral pharangeal candidiasis, dysphonea from vocal cord myopathy, and cough
Mouth rinsing and using spacer can minimize SE,
Oral corticosteroids (Po CST)
TU: Severe asthma with intensive airway inflammation
Leukotriene antagonist: Montelukast and Zafirlukast
". Only oral available
TU: Asthma (steroid sparing agents), and ASA induced asthma
,. :"
74-2
Chronic Obstructive Pulmonary Diseases
. t
Empbysema is a disease in which the small air exchange sacs (alveoli) in the lungs'
become pennanently enlarged and damaged (alveoli walls destroyed) thus decreasing
oxygen absorption and resulting in
.. ,"
COPO: Chronic obstructive pulmonary diseases; COPD is due to chronic obstruction of
the airWay. There are two types aCCOPD:
Emphysema (high altitude sickness)
Chronic bronchitis.
I. Salbutamol 2. short actin!! beta2 a!!onist 3. Terbutaline
4. Corticosteroids 5. 5Prednisonel 6. Zafulukast
Prednisolone
7. Theoohvlline 8. Diohenhvdramine 9. Codeine
JO. Ephedrine \I Cromolvn sodium 12 Ioratrooium bromide
13. Exercise 14 Emotional stress 15 Cold air
16. montelukast
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,
Asthmaand COPD
...
WWV.... Ph3rrn3cyPrep.Com
. .
Recommend: flu '(annually) and Pneumococcal vaccine
Drug used'for the treatment ofCOPD
Anticholinergics: Ipratropium (Atrovent) and tiotrop.,ium (Spiriva)
. 0 11 is a blocker and- acts as bronchodilator
Befa adrenergic agonists
Corticosteroids
TIleophylline
Antibiotics: azithromlJin, and amoxicillip
References: Allergens, Asthma lnfonnation Association (www.aaia.ca)
Tips
Chronic brODchitisis an inflammation ofthe airways that causes lungs to produce
excessive amounts of mucus (phlegm), associated with chronic productive cough. This
reduces the flow of air to the lungs. Onset age 45 years.
Risk factors that cause COPD:
,_ Smoking (80 to9Q%)
Family history.
. Occupationa1 exposures tQ.certain ducts and fumes
Air pollution
Second hand smoking
Asthma

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Asthma and COPD www.PhannacyPrep.Com ,
CoJd ArfA,
Triggers of asthma (l3,rlt"S, td"!l ), HM: air conditioner, hot air.
Rescue medications or treatment of acute exacerbations and prevention of exercise-
induced asthma (i ) so..Lbu;}qmo1
It relieves the symptoms of astluna, chronic bronchitis and emphysema (II i
l
f 2 )
It may interact with MAOls and cause a dangerous rise in blood pressure ( '0 )
-0 Rinsing mouth and using spacer can minimize the side effect of this drug ( 4
1
S )
It is use for the treatment of skin diseases, rheumatic disorders and certain blood
disorders (5 ) pAJLoI n 'sok.L- / n ,.s olo &AR........
It is the drug ofchoice for Aspirin induced asthma (',If:, )
This drug should be use with caution in patients with peptic ulcer and seizure diseases
jon narcotic antitussive elL;} C(J+
What narcotic antitussive that causes addiction and tolerance ( 3. ) Cod.LJ vJ.-
What caUses slight increase in blood pressure and'lias both alpha 'and beta effects ('0)
/',. of .. J.Ilto\. Wh' J'. h I
L..t'-Ort't 1J1..)tU1l1 . ...., at IS use lor prop ylactic treatment and not used for acute asthma attack (") I I r
What is the drug ofchoice for chronic obstructive pulmonary disease{f2.1. . I
Indications of short acting beta2 agonists include E:J.A , 4-- ,
Indications of long acting beta2 agonist include MCc..f ce <1 "'t ". I
Sequence of asthma therapy: SABA pm :l.C$ -I) I...A-f3A' c."1$ I v
When LARA are initiated in asthma patient? -7 IIf' no.J-,.
What are asthma triggers? -7'3,'4, fS- i
What is NOT a trigger? U-ih- b I
Leukotrieneaare-7 .s-mJttz. froW,'d .tt.:t.s>t,,,q'
Theophylline clearance in 3 year old? M&ad d"/Cj,a", (
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74-4
Smoking Cessation
Pharmacological aids to smoking cessation
Questions Alerts!
withdrawal and overdose symptoms
Bupropion mechan,sm and side effects
Vernacline (Champix) mechanism
I
I
I Nicotine Replacement Therapy (NRT) I
I Other Therapy
I
I
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Nicotine gum
Nicotine patch Vcmact.lin
Nicorette
Nicodenn or (Zyban)
(Champix)
Nicorette plus
Habitrol
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Nicotine overdose symptoms: Palpitation (heart racing), difficulty in breathing, nausea,
vomiting, and diarrhea
Nicotine withdrawal symptoms: Severe craving, anxiety or irritability, restlessness,
nervousness, difficulty with concentration. Sleep disturbance, headaches, increase appetite or
eating habit.
Drug
Bupropion ould be used with or without NRT
Nicotine inhaler is contraindicated if allergy to nicotine or menthol. Use with caution in
patients with bronchospastic disease
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If patient has CVS disease, weight less than 45kg, or smokes !ess than Yz pack/day
begin with 17to ?4 for 6 weeks then decrease to 7mg/24h for 2 weeks
NICOTINE BASED: Nicotine patch or gun; Stop smoking completely .
NON-NICOTINE BASE: Bupropion (Zyban); Can smoke for first two weeks of treatment.
Nicotine replacement therapy
Almost every smoker can benefit from using nicotine replacement therapy. In
- .
pregnancy and heart or blood vessel problems, its,use requires precaution.
The nicotine replacement therapy available in patch, gum, nasal s'pra'y
- .
forms. .
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Most smokers should start using a full-strength patch (15 to 22 mg of nicotine) every
day for 4weeks a weaker patch (5 to 14 mg of nicotine) for another 4 weeks.
-
Directions for use: At the start of each day, place a new patch on a part of your body
between the neck and the waist. Put the patch on a new spot each day to lessen skin
irritation.
Treatment period: The patch is usually used for up to 8 weeks.
Side effects: Some peC?ple who use the patch get a rash on their body where the patch
is placed. Skin rashes are usually mild and easily treated. Moving the patch to another
area of the body helps.
Jb Nicotine Gum
-1f Start using the 2mg dose. However, start with 4-mg gum if you smoke more than 20 '---'
cigarettes a day.
Smoke as soon as you wake up in the morning.
Have severe withdrawal symptoms when you don't smoke.
Have tried to quit on a lower dose and failed.
If you are a ver Ii ht smoker (less than 10 to 15 cigarettes a day)
Directions for use:
The gum must chewed in a special way to make it work. Chew it slowly until you
feel a "peppery" taste. Then stop chewing and move the nicot,ne'gum,betWeen: your
cheek and your gum. Each piece of nicotine gum should be kept in your mouth for
about 30 minutes.
Treatment period:
A regular schedule (at least one piece of nicotine gum every 1 to 2 hours for 1 to 3
months) may give the best results. Some people don't chew enough pieces of gum a
day and or they don't chew the gum for 8 weeks. They might not get the most benefit
from nicotine;gum.
Maximum 6 months
. Side effects: mild side effects such as hiccups, stomach upset or sore Jaws: Most of these
side effects disappear if the gum is used correctly.
75-2
www.pharmacyprep.com Smoking cessation
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B::!.:D to'
7-+0 /2.
Mechanism of action: act nicotmlC receptors
Used in combination with quit smoking education.
Helps to relieve tile craving and withdrawal symptoms associated with stopping smoking.
This drug works by affecting niJ:otine receptors (actsUke a weaker .version of nicotine
.' ... . .
receptors and also blocks nicotine receptors.
Starting dose is O.5mg once daily for the first 3 days, then O.5mg bid for next 3 days and
then Img bid daily thereafter. Treatment for 12 weeks.
Stop smoking in 1 to 2 weeks of starting this -
Nicotine Nasal Spray
Directions for use: Apply one spray in each nostril. Use the spray one to two
each hour while you are awake. Use the spray at least 8 times a day. Don't use it more
than 40 times a day.
Side Effects:
The nasal spray may cause nasal irritation, diarrhea and a fast heart rate. If you have
hay fever or sinus infection, ask your doctor about using one of the other forms of
nicotine replacement therapy.
Nicotine inhaler
Directions for use: Inhale from a cartridge when you have a desire for a cigarette. Use
no more than 16 cartridges a day for up to 12 weeks.
Side Effects:
You might have irritation of throat and mouth when you first start to use the inhaler. It
might make you cough. You should get over this after a while.
Bupropion (Zyban)
150 mg daily x 3 days than 150 mg BID for 7 to 12 weeks.
Begin 1 to 2 weeks before the selected quid date.
Monitor in hypertensive patients
Contraindicated in:
Pregnancy
History of seizure
Anorexia nervosa
Bl:llimia AeNosa-
,
Precaution in taking MAOl's
Side effects:
More common: Dry and. i'nsomnia
less common: Hypertension, myalgia, arthralgia, dizziness, tremor, somnolence,
bronchitis, pruritus, rash,'and taste prevention
Nicotine available
Vernecline (Champix)
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SE: Dizziness, drowsiness, dry mouth, flatulence (passing gas), gingivitis, headache, N&V,
rash, insomnia, unusual weakne;ss and constipation
CI: Pregnancy, breastfeeding, children,
01: Insulin, NRT, warfarin, theophylline
Contact Dr: if constipation, abdominal pain, appetite changes.
Symptoms to be monitored in case of nicotine withdrawal are:
Severe craving
Anxiety or irritability
Restless, nervousness, difficulty with concentration
Sleep disturbance, headaches,
G.I symptoms, Increase appetite or eating behavior
Symptoms are peak after 24 to 72 hours of last cigarette
Smoking is single most common preventable cause of death and disability in Canada
Tips
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1. Severe craving 2. Anxiety or irritability 3. Dry mouth
4. Insomnia s. Restlessness 6. Nervousness
7. Difficulty with concentration 8. Sleep disturbance 9. Headaches
10. Nicotine gum 11. Nicorette 12. Nicorene plus
13. Nicotine patch 14. Nicoderm or habitrol 15. Champix
16. Increase appetite or 17. Bupropion 18. Room temperature
eating behavior
75.<1
. What drugs are used for smoking cessation? ( 10 -f'D l6"

How nicotine patches are stored? (IS)
What is incorrect about nicotine patch? ( (, ) . haltA.. D?tdJ"l
The types of nicotine dosage forms? ( 10, If, 1.2., ('1, (?- r) 111 . f
Nicotine replacement therapy products (10 ,1/, II , 111 h..a.1k--<t 3
NRT used in combination with quit smoking education (True/False)
Nicotine withdrawal symptoms ( ',t, 4,s,tI '1, tr,gI ill
This could be used with or without nicotine replacement therapy ( I 1)
More common side effect of bupropion dJ.j i s D",nl'i k 4ko.. etf5e<1-
Vernacline mechanism of action ( b &ft....
Bupropionsideeffectsinclude? e _,
''j: :LTIS f>aIJ' "'1
Bupropion contraindications? p,wI +-0 tU.p1t", z., - lltfa1.
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Insomnia
Questions Alerts!
Insomnia self care (avoid exercise before bedtime)
Benzodiazepine classifICation and side effects
Non pharmacological Choices
Sleep hygiene
Relaxation exercises
Sleep restriction and stimulus control
Aerobic ex'ercise: decreases daytime rest and increase exercise
Sleep hygiene
Keep regular sleep wake schedule for 7 days/wk
Restrict sleep time to average sleep time
Avoid extensive horizontal rest or daytime napping
Get regular exercise every day (avoid exercise before bedtime)
Avoid heavy meals just before bedtime
Do something which is boring before bed time
Avoid before bed time
Caffeine
Alcohol
Heavy meals
.,
Hungry
Minimize noise and light, high temperatures.
Minimize drinking fluids
Avoid vigorous exercise 2-3 hours before bed
Over !he counter.
Diphenhydramine
Valerian
Melatonin
76-1
(
www.pharmacyprep.com Insomnia
G? u e.s+,OI.1 AJVLJ--
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Pharmacological choices:
Prescription:
Benzodiazepines
'.
Barbiturates
Antidepressants (TCA's)
Ch';lpral hydrate
Benzodiazepines:
Benzodiazepine act on Bl
l
and Bl
2
receptors
Benzodiazepine act on GABA
A
receptors
Short acting benzodiazepines: Triazolam, midazolam,
Long acting benzodiazepine: Diazepam, c1onazepam, flu.razepam
Intermediate benzodiazepine: Oxazepam, temazepam, and lorazepam.
Least hangover effect: short acting benzodiazepine
lopiclone is a non-benzodiazepine, it acts on Bl
l
receptors
Tips
l. Temazepam 2. Short acting 3. Loraz"epam
4. Midazolam 5. Zopiclone 6, Oxazepam
7. Diazepam 8. Triazolam 9. Exercise before bed
Short acting benzodiazepines ( '-1, !)
Long acting benzodiazepines (7 )
Intermediate benzodiazepines (r,3,b)
The least hang over effect (4, f.,f(,
What benzodiazepine is indicated for initiating sleep? ( 4,
What drug may cause less rebound on withdrawal? (5 )
What is inappropriate self care measure (.1 )
A non benzodiazepine act on BZ
l
receptors ( S )
Benzodiazepine act on BZ
l
and BZ
2
receptors
/. Benzodiazepine act on GABA
A
receptors
What drug give bitter or metallic taste (S) .
Benzodiazepine withdrawal symptoms --> t ""5
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76-2
'-
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www.phannacyprep.com Eating Disorders
Eating Disorders
"
Questions Alerts!
Definitions of bulimia (loves to eat then purge) and anorexia (fear. of eating) nervosa
Drug related problems orlistat
Anorexia Nervosa: It is characterized by deliberate loss of weight (to <85% of expected
weight), refusal to maintain normal body weight, fear of weight gain and amenorrhea.
There are 2 sub types: Restricting, non purging: excessive exercise or fasting.
Drug of.choice is metoc!opramiW -7 reduce the feeling of fullness.
-=-
Bulimia Nervosa: It is characterized by repeated episodes of binge eating followed by
. , '
inappropriate compensatory behavior such as self-induced vomiting, misuse of laxatives/
diuretics, emetics, other medication, long time fasting, or excessive exercise.
There are two subtypes: Purging: using laxatives, or emetics. DOC is SSRI, and venlafaxine
Medications
Appetite suppressant: Diethyl propion (Tenuate), Bupropion (Wellbutrin)
Satiety enhancers
l Sibutramine (Meridia): Serotonin and norepinephrine reuptake inhibitor (SNRI)
Lipase inhibitor: Orlistat (Xenical): Gastric lipase inhibitor reduces 30% fat absorption
Cannabinoid type 1 receptor antagonist
Rimonabant: Blocks the central and peripheral effects of the endocannabinoid system
mediated by cannabinoid (CB)-l receptors
., Drugs that are used for weight loss therapy
Drugs that give anorexia (loss of appetite)
\,/ Orlistat Metformin
\,/--5ibutramine Amiodarone

v Buprapione CNS stimulants (amphetamine and
v
77-1
-. \..
Eati!1g
Topiramate methylphenidate)
Drugs that increase appetite Drugs that cause weight gain
TCAs.
,
Insulin
,
Corticosteroids TCAs
contraceptives MAOI
Sulfonyl ureas Antipsychotics
Sulfonyl ureas
Meglitinides
Tips
1. Domperidone 2. Metoclopramide 3. Orlistat
4. Anorexia nervosa 5. Bulimia nervosa 6. Purging
7. Non purging 8. Loves to eat 9. Fear of eating
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It is characterized by deliberate loss of weight (it ) A- \.1 o/vJ>(1 Cf 11l.A.. V0..5 q
Excessive exercise or fasting (1) No P lt1- eN:J.-
Reduce the feeling of fullness (1,.2.) do / tv) e.+-v c..1 rv"'1
It is characterized by repeated of eating (5) t\
Intestinal lipase inhibitor (3)
Using laxatives or emetics V(f-
What type of eating disorder patient use purging? (5 ) J'l'V7 e,
Bulimia nervosa == CO l-oVe- to
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78-1
This chapter review the symptoms and therapy of gastroesophageal reOux disease
(GERO), ulcers, irritable bowel syndrome (IDS), and inflammatory bowel disease (ffiD).
eartbum (pyrOSIS, it is a substernal burning or pain that may radiate to the
neck, back, or throat. ymptoms occur shortly after meals or when reclining after meals,
or upon lying down at bedtime. Often symptoms may awaken one's sleep. Symptoms arc
, exacerbated by eating a large meal (high fat meals), and bending over.
Gastoesophageal Reflux Disease. It is defined as chronic symptoms or
mucosal damage produced by the abnormal reflux ofgastric conlent into the esophagus.
Risk factors: High fat meal, carbonated drinks; pregnancy, obesity and increase age
,
78
GERD, Ulcers, lBD, and LBS www.PharmacyPrep.Com

Nonphannacological measures
: Quit smoking & reduce alcohol and caffeine intake
Take smaller, more frequent meals (avoid high fat and spicy foods)
Avoid exercisinglbending on full stomach
Avoid tight fitting clothes around the waist
Elevate head of bed 10 em high
Avoid lying down after meal
**Refer to the physician if symptoms are more than 2 weeks
GERD, Ulcers, Inflammatory
Bowel Disease, Irritable Bowel

Questions Alerts!
.Common questions in pharmacy exam is to ask!
GERD symptoms and heart bum management
Ulcers: causes and triple therapy to treat H.pylori ulcer
Ulcerative colitis and Crohns disease treatement
Irritable bowel syndrome svmotoms
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GERD, Ulcers, mD, and ms
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Gastroesophageal reflux disease is categorized into mild and severe.
Mild GERD, relief of symptoms is wiili antacids, alginates or non-prescription
strength H2RA.
Severe GERD: PPJ are the drug of choice. Use PPJ for 2 to 4 weeks
.The goal is to. raise pH.4'during periods when refluX is likely-ihoeclrr:
Pharmacologic treatment. Symptom control: For minor or intennittent symptoms use
antacid alginic acid, or H2 RA. Moderate to severe GERD use PPI, H2 RA, or
CmetoclopramldeJ - - -
Food induced GERD, drug ofchoice is H2RA
Special populations: Pediatric: non prescription H
2
RA are in children < 12 yrs
old
Pregnant: can be used antacids. except sodium bicarbonate N.a JtLiu
Elderly: can use antacids and non prescription H2 RA
Antacids: AI hydroxide, Ca carbonate, and Mg hydroxide and Na bicarbonate
Al hydroxide: SE; constipation and hypophosphatemia (in prolonged use)
Ca carbonate: SE; constipation, milk alkali syndrome (hypercalcemia); u$'(
rebound
Mg hydroxide: hypennagnesia (in renal failure)
or chew well; quick acting with cathartic effect. Should be avoided in renal
failure and limited use in elderly due to risk ofhypennanesemia.
AI-Mg combination products, SE; diarrhea (in long term use)
Na bicarbonate: Not often used because
All antacids have drug interactions with quinolones, tetracycline, digoxin separate
dosing by 2 hours
Alginic acid: It works as foaming agent. Tablets must be chewed with full glass ofwatcr
taken when patient is in upright position; should not be taken at bedtime.
Prokinetic agent: Metoclopramide and domperidone
H
2
- receptor antagonists (MzRA): cirnetidine, ranitidine (Zantac), famotidine (pepcid),
nizatidine (Axid) dhvv I h #.t-
o equally elTective: usually elTective in mild GERD, ID $4 AMpo"M. ...
the efficacy is limited by the rapid development of chyphylaxi & the inability to
properly suppress meal-related acid secretion.
Step-down therapy: H
2
RAs are instituted after symptomatic reliefhas been achieved
wiiliPPls
SE: diarrhea, constipation, headache J.Ah-v
01 PItSO Cimetidine SE: gynecomastia, impotence (rare)
\d Famotidine; potent Ret,....
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78-2
78-3
OJ: Ranitidioe: decrease clearance oftheophylline, phenytoin"and warfarin
Cimetidine; CVP450 inhibitors,
Use to reduce the "night-time
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GERD, Ulcers, lBD,\md lBS' www.PhannacyPrep.Com
Ulcers.
Proton pump inhibitors (pPO: omeprazole (Losex capsules, MUPS. tablets),
esomeprazoJe (Nexium), lansoprazole (prevacid), pantoprazole (pantoloc), rabeprazole
(Pariet)
Drug ofchoice in the most GERD patients
Side effects: abdominal pain, diarrhea and headach.
take Y2 hour before meals: the most effective acid suppression, once daily
acid rebound occurs with discontinuation (tachyphylaxis is not a problem)
At equivalent doses, available PPIs offer similar efficacy and safety ,
,9E.,lreflicacy ofarugs req-uilinwait:acid'mooiuin for'3bsorpii'on-(e:<mIaoonmlcf,
y ifitlinavi"r)' -
Omeprazole: DJ; Omeprazole may decrease metabolism of warfarin, diazepam and
phenytoin (require dosage adjustment), and c1opidogrel
may confer a modest advantage over other agents for severe
esophagitis
l

Pantoprazole; ra id onset G\ ' 1+
Ra prazole; tdigoxin level .:::D D
6s0 r"'ft'I--Lr
E.s Ulcers are categorized based on their of ulcers such as:
Peptic ulcers
Gastric ulcers: Due to reflux since it has weak pyloric sphincter
Duodenal ulcers: Excessive secretion froffi'parietal cells
Acute stress ulcers (Curling's ulcer): Tumors
Pathologic states (ZOllinger-Ellison syndrome)
JSympto.;) Epigastric paio occurring) to 3 hours after meals that is relieved by ingestion
of food or antacids is classic symptoms of peptic ulcer disease. Pain can occur and
episodes lasting from weeks to months and may be followed by variable periods of
sPQntaneous remission and reuccarence"
11== .J '-7 H'P.2J1Oh-i T,AJpl.e..-
For neutralization of gastric acid use antacids
To reduction of gastric secretion use H
2
receptor blocker, and proton pump inhibitors
For cytoprotection use sucralfate
To eradicate Helicobacter pylori use triple therapy of2 antibiotics + PPJ
Triple 2 antibiotics + J PPJ
Losee I Clanthromycin 500 mg bid + omeprazole +amoxicillin
,Losee 1-2- . larithromycin 250 mg bid+ omeprazole + metronidazole
Quadruple therapy: Tetracycline+ metronidazole + bismuth subsalicylate +
Omeprazole
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$
@hoosethealternatiVe)Omcprazole + +c1arithromycin-) Losee
Ifpatient is allergic to amoxicillin or if patient is having diarrhea or ifpl)tient IS more
o prone to having anaerobic infection
Gastritis: The gastric ulcers are associated with a corpus predominant (diffuse
predominant) gastritis. This pattern gastrit,is is associated with low acid output, gastric
atropy. and adenocarcinoma.
Inflammatory Bowel Disease. Consist of two conditions ulcerative
colitis and chIon's. The ulcerative colitis mainly colon and
"'< ..- " :.. '
Causes of intlamatory bowel disease:
Infection with and other pathogens
Genetic factors
Environmental conditions
Non-pathogenic intestinal flora
Crohn's disease: Inflammation is present from the esophagus to the anus but
in the small bowel or colon. Obstruction of the bowel abscess fonnation
Drug of choice to treat mild and moderateW'1 bUd6s.erl-{diand
Ulcerative colitis: Relapsing inflammatory condition in the colon with symptoms of
bleeding; urgency, diarrhea and tenesmus
Erosion and ulceration of the mucosa
Decrease in the number ofgoblet cells
Frequent infection secondary to fever and anemia
Drug of choice in:miId.torrli:lCletiare;is
ofchoice)n.se'!ere
Aminesalicylates: Sulfasalazine and 5 ASA.
Sulfasalazine metabolized to sulfapyridine + 5 ASA (mesalamine)
Sulfpyridine has systemic absorption and is responsible for SE's NN, headache,
anorexia, and folate malabsorption.
. (J/ Sulfa free compounds: Mesalamine olsalazine (two molecules of 5ASA
l,.../ linked to diazo bpnd)'
I The side effects experienced with mesalazine and olsalazine are less then
sulfasalazine
Irritable Bowel Syndrome. It is defined as abdominal discomfort
associated with altered bowel habits. It is characterized by symptoms ofabdominal
\. A cramping, constipation or diarrhea. 11. ()S
,,(I [)Jo phannacologlcal measure:' . ,

. Regulating dietary fibre and lactose intake - t) is &'rv?D
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Dicyclomine: It has anticholinerg,ic side effects
,
Loperamide: Used for diarrhea
Magnesium hydroxide: Used for heartburn
Lactulose: Used for constipation
Cholestyramine: For patients with bile salts malabsorption
Tips
GERD, Ulcers, mo, and ms www.PhannacyPrep.Com
Stress management
Probiotics may help
,
1. High fat mealj 2. pregnancy 3. increase age
carbonated drinks
4. obesity 5. Al antacids 6. Mg antacids .
7. ea antacids 8. Alginic acid 9. Sucralfate
10. Famotidine 11. Ometidine 12. Omeprazole
13. Esomeprazole 14. lansoprazQle 15. Pantoprazole. Rabeprazole
16. Misopmstol 17. GERD 18. IBS
29- H. pylori 20. Ulcerative colitis 21. Chrons
12-
S-ASA
"-
Prednisone 24. Infliximab
25. . Ulcers 26. Colon 27. Simethicone
. cJ- 3J P- "" ,h/Ikla
Triggers of t)eartburnorGERD( f,2.,3,.l.rJ M I -'0
Symptoms are heartburn, epigastric pain (f1,lSJ (JtE-R.'J> I UI CeTl-
It is defined as abdominal discomfort associated with altered bowel habits. It is
characterized by symptoms of abdominal discomfort, bloating, cramping.
constipation or diarrhea. ( ,I< ) If0.+"J,f.L.
Symptoms are relapsing inflammatory condition in the colon with signs of bleeding, . \
urgency, diarrhea and tenesmus. (2-
o
,e\ U Ic<JvJive. CJ:>/,M>J Uv<-olt:s eu_ /
Symptoms of inflammation is present from the esophagus to the anus but
predominantly in the small bowel or colon. Obstruction of the bowel abscess
formation. ( 2\) C.4M.,:s' _
Takes Yz hour before meals; the most effective acid suppression, once daily ( 12. 1 P
Gram negative bacteria that cause gastric ulcer ( 11) 14 fctldA.-i
Active metabolite of sulfasalazine (2.2...) 5 - ASA CM M't-e.. )
What is an antiflatulence agent ( 't.7) S t f-o"')..e..-f'I1 i CtJlt'-L-
What antacids may gives the side effect of diarrhea (Mg =must go) ( ,) d
Gives the side effect of constipation AI, CC\
Isomer ofomeprazole ( !S) dJ
- Gives rare side effects as gynecomastia, impotence ( I') CI /.A.Ii!..-
';Po not"take with ciprofloxacin, tetracycline, biphosphonates and thyroxin (.s; it?) M'lG,.
Has rapid onset proton pump inhibitors ((S' ) R
Decrease efficacy of drugs requiring an acid medium for absorption ( s,',7 I f P1
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Usually effective in mild GERD, as BID (
Step down therapy; are instituted after symptomatic relief has been achieved with
PPls )
::::Lactulose is used in what type of chronic liver disorder -7
"'An example'of ecosanide is-7 ( 'b) M'I &:>
Misoprostol is analogue of -7 PGr-i.
Type of pain in GERD is-7
Increase in bilirubin causes -7 --.\ cu.(.. ...cL c.e.. e....t:h.
What are the side effects of aluminum salts -7 Coc,.,,S-HP 0V1
What are 'the side effects magnesium antacids -7 d i
H. pylori will cause U{ceJl,.
What type of hepatitis is chronic -7 He..pc...l1+'..s B a"J c.
or
..-' .
NSAIDs induced ulcers can be treated bY-7 Pp-:r.
Ihdependent':risk
p
factors for peptic ulcer's'are:J1.pvlorf cind NsAIDs (True/False)
Epsom salt is? -7 M.jS0lr
Ulcerative colitis occurs at? -7 Col oVl
Antiflatulance agent? -7 S; iCOllJ2-.
What vaccine 'be used for traveler's diarrhea (;E:toli, cholera)?
Symptoms of ulcers? epi'J-a.At'".(.fC p4i'r) " ..., L J
Symptoms of irritable bowel syndrome (16S)? -7 B I 'tJ.' 1
Symptoms of ulcerative colitis? t.::J F'VJ . Jo-4at- VJ
Symptoms of Crohn's disease? -7 I pCA-f'1 -----
Select TRUE OR FALSE Statement
Y Na bicarbonate is contraindicated in patient with hypertension, CHF, severe renal
disease, and edema. This also contraindicated in ulcers. (True/False)
g / acidity-due to stimulation ofacid secretion.
\./' _ (True/Fiilse) ,
CaC0
3
antacids should be avoided in hypercalcemia pati,ents. (True/False)
fupophosphetemia and osteomalacia can occur with long-term use of aluminum
containing antacid$. (True/False)
/ Antacids bind with. tetracycli,ns, and fluroquinolone and reduce their absorption.
, riuiy (True/False)
-Mg antacids can cause cathartic side effects. (True/False)
Zollinger-Ellison syndrome: Gastric hypersecretory states in systemic mastocytosis
which is a rare disorder with increase number of mast cells systematically and in skin.
H pylori: bacteria that cause gastric ulcer (True/False)
78-6
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5 j \ l ~ W \ 15 l-Ijft'A-':l :1l'9"''''
-
Insulin and Antidiabetic Drugs
Questions Alerts!
Common Questions in pharmacy exam is to ask!
long actin Insulin (glargine)
Insulin dose management
long acting sulfanyl ureas
Metformin side effects
Sitagliptine mechnisms: DPP4-inhibitor
Rosiglitazone cardiovascular side effects
Incretin hormone analogs (liraglutide (victaza))
Acarbose mechanis
.. Podl<Uf-/'>is+:
This chapter review of insulin therapy for diabetes mellitus and antidiabetic drug for the
treatment of type II diabetes. .
Diabetes mellitis, type I and type II.
Type I: Insulin dependent DM (lDDM) 5 Type II: Non-insulin dependent DM (NlDDM)
tolO% >90%
Juvenile onset Adult onset (40 yrs)
Destruction oft3-cells in pancreas Milder form
No production of insulin associated with Very strong genetic pr.edisposition
treatment is by diet and insulin. Inability of beta cells to produce adequate
Ketoacidosis occurs
insulin and doesn't meet the body's
requirements.
Mainlv due insulin resistance
Nonnal Blood Sugar Levels (BSL)
Fasting BSL 5 to 6 mmollL
Random BSL < 11.1 mmollL
Post prandial <11.0 mmol/L
HbAICis4t06%
79-1
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PharmacyPrep.com Diabetes
, .
Measures past three months blood sugar levels
Used to determine antid.iabetic drugs- compliance of patient
Types 'of n s u l ~
old
Long-acting
Regular
Semilente
5c. ~ .... 1...
NPH. Ultralente
Lente Protamine Zinc
NO. Glargine
. --1..( Detemir
Types of insulin are categorized by their onset of action, and these re atIve positIons
true for their effectiveness and their duration of action as well.
Insulin SE: Weight gain and hypoglycemia, lipohypernophy at site of injec!k>ns.
-
Insulin Duration Onset Peak Duration of
(hours) (hours) . Action (hours)
1
Humalog (H) (lispro) Very short 5-10 . 30-40 min 2-3 h
synthetic (Fastest) min
5c..
OIL lv
BC or iv form
Clear solution
{
Regular (R) Rapid (short) Y2 -1 h 1-3 h 5-7 (dose-
(suitable for iv dose). Both SC or iv (in dependent;
human and animal source emergencies) maybe
Sc. D/l1v
clear solution longer)
i
NPH (N) Isophane Intermediate 2-4 h 6-10 h 14-18 h
Amorphous precipitate of Semilente (30%) not suitable
insulin with zinc ion ~ for iv dose
buffer Sc.. 0
Ultralente
....,
Long (70%) 4-5 h 18-28 h -
Zinc suspension crystals in Slowest onset of
acetate buffer contain large action but
particles that are Sl0;t Longest
dissolve' SC. 0 ~
hypoglycemic
effect.
Glargine ...., No llW1 od" Longest acting
..
Should not be
Detemir Single daily dose , mixed with
,9C Oh\;\- other insulins.
I
Very Rapid-acting Insulin Analogues: clear
insulin aspart (NovoRapid)
insulin glulisine (Apidra)
insulin lispro (Humalog)
Rapid-acting Human Insulin-clear
79-2
Mixed Insulin Analogues- cloudy
insulin lispro Ilispro prolamine (Humalog Mix25) .
Meglitinides: Nateglinide (Starlix.), repaglinide (GlucoNorm)
MOA: Increase secretions, Decrease post prandial blood glucose levels
Insulin storage conditions
Should be stored in refrigerator
Can be stored at room temperature 28 days (I month)
Do not shake vigorously
If you notice turbidity or vapors or precipitation, do not use, discard it
Long-acting Insulin Analogues: clear
clear, don'( mix with other insulins, duration 24 hr (no discernible peak)
" insulin detcmir (Levemir)
insulin glargine (Lantus); acidic solution (pH4), microprecipilates form (slowly
released), NO im or iv.
Mixed (regularINPH) Human lnsulin- cloudy
insulin regular I insulin NPH (Humulin20/80,30170. Novolin qe 10/90, 20/80, 30170,
40/60,50/50)
.;5u.f>o ...1- UW
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Diabetes PharmacyPrep.com
insulin regular (HumulinR, Novoline ge Toronto)
Intermediate-acting Human Insulin- cloudy
insulin NPH (Humulin N, Novoio ge NPH)
Oral antidiabetic drugs
Sulfonylureas; Chlorpropamide, gliclazide (Diamicron), -gliclazide long-acting

(Diamicron MR), glirnepiride (Amaryl), glyburide (Diabeta), tolbutamide
Stimulate release ofendogenous insulin thus increase insulin secretions.
SE: b:ypog1ycemia ,and weight gain ayoid obese or over
i4 .' Ifaallergies .
. ,,->-< .
CI: pregnane SE: hypoglycaemia, weight i
Ch ororopamide; dose adjustment in real impairment, once daily long half life
Associated with disulfiram reaction with alcohol may give nausea, vomiting,
headache, flushing uPQn ingestion ofalcohol. oflnapp.Np.iatc
leads to edema.
SE: alcohol-associated flushing, lNa
gliclazide - produce an earlier insulin release than others
gliclazide long-acting - once daily
glimepiride CAroary!) - once daily
glyburide CDiabetal - dose adjustment in real impairment, loweSt risk-Of.
and high hypoglycemia.
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PhannacyPrep.com Diabetes

51:-;
- tAche..
Qc'do:<iS

.l, \It"
SE: hypoglycemia and weight gain, (esp. ifnot take meal), CI:
pregnancy
ay e taken prior to meals (skip dose if you miss meals) -7 take at first bite of
meals
take 0 to 30min before meal_ lowering postprandial glucose levels
Repaglinide - DI: gemifibrozil (Trepaglinide conc. - avoid)
mguanides, me!formin (Glucophage) -;> Lo>6 & ORA-LJ
MOA: Reduce gluconeogenesis, and increase glucose utilization, Increase glucose
uptake into cells
SE: Less common but more serious SE is lactic acidosis. No hypoglycemia, can give
weight loss. To avoid GI SEs, start low & titrate up q2-4wk .
Dose adjustment in real
ONLY oral, NO weight r---0 good fOfooese patient, NO hypoglycaemia on its own.
Take with food or after food
01: alcohol (potentiates hypoglycemic effect)
tel: fiepatic impairment, renal" impainnent, CHF, hypoxemicstates patient
'c'auiron"ifCrCl 60 mVmin
Decrease mortality
Does not cause sulfa allergy
Alpha-glucosidase Inhibitors, acalhose (Glucobay) - T4Kf- off' AJ/5T B;11<'- OF F(jJJ)
MOA: Inhibit alpha glycosidase intestinal enzymes
Decrease absorpt ion of starch and sucrose (do not stop absorption of glucose)
Decreases the postprandial plasma glucose level
an_d and diarrhea
With meal, not used as monotherapy.
Meal-time dosing; may take several weeks for maximum effect. Taken with the first
bite of food
Maximal ellect takes weeks; t dose q4-8wks
SUlphanilureas +acarbose
Does not by itself cause hypoglycemia
GI intolerance: flatulence >41%, diarrhea >28%, sucrose oat absorbed
79-4
ThiazoJidinediones (TZDs): pioglitazone (Actos), rosiglitazone (Avandia)
, rosiglilazone/glimepiride (Avandaryl), mctfonnin (Avandamct)
".) 1v' MOA: Increase peripheral insulin sensitivity, and reduce gluconeogenesis
r('. - Effective in lowering HbAIC
tY' G CI: Liver disease, and CHF
SE: WtT(most), fluid retention edema 4.8% (HF; HTN); TWeight; anemia -1% mild
. 1 HDL, NO hypoglycaemia on its own
V DI: gemifibrozil (Trepaglinide conc. avoid), CI: CHF pts, can use renal impainnent
\ '\;' pIS
/ 1 of pregnancy if adequate contraception not used (ovulation resumes)

Act on cell membrane receptors to increase glucose uptake (P) .I11\..$ VJ
Blood sugar levels if a person is diabetic ( ',1,.' ) d _11- I
Symptoms of hyperglycemia (4,f,1) P.l,jL1)\"I><!, pob IPJ.e<l,
Symptoms of hypoglycemia I p&<tprh:.-h
D
"1, Co 0'1
79-5
NO use with insulin (not approved by health Canada)
Pioglitazone - 1 TO, have more lipid effect. More 01 than rozigiitazone
Mon: Ifbaseline ALT is elevated (>2.5 times normal), do not use glitazones
Rosiglitazone - t LOL TO, Increase .HOL, Once daily with or without food
Monitor liver function (ALf) when indicated;'
Delayed action... Onset -2-4wks Max effect in 8-16 wks.
Rosiglitazone / mctformin - associated with overall lower glucose & HbA Ic_
Diabetes
h bl fr t002 F' d
PharmacyPrep.com
Incretin analogs: Liraglutide (Victoza),
TIpS
, '
Di.peptidyl peptidase-4 (DPP-4s}j Sitagliptin (Januvia), saxigliptine
MOA: Inhibitor of dipeptidyl peptidase enzyme (DPP-4) that enhances the incretin
hontJope . .
SEs: Nasopharyngitis I;>ls: low potential (do not inhibit CYP450), Can cause
hypoglycemia' with sulfonyl ureas. .
Take with,m'etfonnin, with or without food, do NOT potentiate hypoglycaemia.
100 mg once daily taken with or without food '0A1.i s-\c-J
Not used in type I diabetes, there is no clinical studies _,
I3lock the.. Ad,." f "',.... '"
4- Fa.., eV1"
CUJ'a5e) +J.."'* dIrt
Intestinal Lipase Inhibitors - orlistat (Xenical) ' So fcJ-3 ?
SE: Diarrhea, steatorrhea, abdominal discomfort, and oily leakage. F..A-i V I t- (fl,.':D --k.....
Take with food, impair absorption of fat soluble vitamins (A, D, E, K) fHIrJ:L 140 1- 01 b S,?l1.h ''1
+II "-- bc&;j -> 5+,,4../
liPS anna : -m answers omteta e
L FBG >7.1 mmol/l 2, HbA1c> 7.0% 3, Random >11.0
1.
4
.
Palyurea 5, Palydipsea 6, weight in Kg/{height in m)2
7, Weight loss 8, Sweating 9, Palpitation
10, Rapid acting Insulin lL Insulin regular 12, Intermediate (NPH)
13. long acting insulin 14, Premixed insulin 15, Sulfonyl ureas 1st gen
16, Sulfonyl ureas 2nd gen 17, Meglitinides 18, Metformin
19, Thiozolidinediones 20, Acarbose 2L Incretin enhancers (DPP-4
Inhibitor)
22, Diabetic complications 23, Insulin 24, Intestinal lipase inhibitors
25, Waist line >102 cm 26, Waist line >86 cm 27, Confusion
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All insulins are clear solutions, except ( 12 ) NP1+. k-tv-
Sitagliptine and saxigliptine are ( 2. \ ) hal1c.eA... C:J) PP-4 ,11 1
What drug may give lactic acidosis if taken with alcohol and renal diseases, liver
diseasy'( 11) ) ,Y1
dlseasbs, and
hepatildrihosis -( 2:2.<), '
Waist'line that have risk of diabetes in meri (L$') '>- 10L c...1f'V\
Waist line that have risk of diabetes in (.2.' ) 7 <tb Cvv- 1 J
increase glucose uptake ( 1 4-
. Drugs increase 'insulin secretion ('$,",)0 .,puJ.lJow;ll.4.A..J.,l.- 4 _1_ I?
Drugs that should be taken with first bite of meals ( n, f2 0 M VI...uJ...L 1
Drugs.that are withdrawn due to heart failure side effects ( Rt>s r v--t.-
Drug used for weight loss therapy (2 OJJ,i -7 '1
l..nl-,l b'fw't.--
Select.True or False Statements
A 65 yo uncontrolled diabetic patient have got foot ulcers. Patient wants to know
. diabetic foot care. The pharmacist should refer this patient to Podiatrist? (True)
. 'premixed insulins Used for stable lifestyle patients (True) ...
'premjxed insulins Can be self adminstered by patient (True)
premixed insulins Cartridges cannot be exchanged with different mixture of
insulins (True)
premixed insulins is an expensive than insulin (True)
premixed insuJins Require insulin pen to adminster (True)
79-6
Questions Alerts!
Symptoms of hypothyroidism and hyperthyroidism
Monitoring of thyroxine: Serum TSH, FT3, FT4
DI:s of thyroid hormone with antacids, Ca, Fe supplements
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Thyroia disorders
80
Thyroid Disorders
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Hypothyroidism. Symptoms that are caused by deficient thyroid hormone production,
thus resulting into slowing down of all body metabolic functions.
Types of hypothyroidism:
Primary hypothyroidism: caused by thyroid gland failure.
Hoshimoto disease: It is an autoimmune disease resulting from cell and antibody
mediated thyroid injury.
The hyposecretion of the thyroid hormone causes myxedema, goiter and cretinism.
Symptoms: Sensitivity to cold, constipation, bradycardia, and weight gain
Signs: Dry flaky skin, coarse hair, slurred speech, puffy face, hands, feet, and hearing
loss. Decreased libido, slow return of deep tendon reflexes, if untreated myxedema
and coma will develop.
Diagnosis: Initial test is serum TSH assay and TSH levels are elevated in primary
hypothyroidism and low serum free T4.
Pharmacotherapy: Levothyroxin-T4 (Eltroxin, Synthroid) or dessicated thyroid hormone
Thyroid hormones
levothyroxine (Eltroxin, Euthyrox, Synthroid):
T4 dosage: 1.Gll&'kg/day (adults), 12.S to 2S M1day (patient with coronary artery
disease or elderly)
Pregnancy: dose l' (thyroid binding globulinsl'l; check TSH each trimester & 4 to
6wk after any dosage adjustment.
It takes 6 weeks to attain a new steady state
Take empty stomach, SE: exacerbation of angina
01: Absorption...r.. by Fe, Ca, cholestyramine (separate administration by 6 hours),
colestipol, sucralfate
80-1
Phannacyprep.com Thyroid disorders
. .
Blood sugar controll1)ay decline with initial therapy (dosage adjustment of
antihyperglycemic agents)-liothyronine: triiodothyronine (Cytomel): T3
Use for shor:t-term management of patients with thyroid cancer undergoing' .
withdrawal of levothyroxine (T4)
In the elderly (because of age) or in patients with coronary artery disease, start with
a dose as low as 12.5 Og/day as tolerated and t i t r t ~ ~ e r y four weeks. TSH levels
changes after 6 to 8 weeks.
Iron salts, Clacium and sucralfate decrease absorption of levothyroxine thus
separate 30 min. Resins like cholestyramine, cholestipol separate 6 hours. Do not
take aluminium compounds with thyroid preparations. Dessicated thyroid hor.mone
may contain pork proteins.
.Hyperthyroidism. The hypersecretion of the thyroid horm'one may cause thyrotoxicosis
or Grave's disease and Plummer's disease.
Type of hyperthyroidism: The hyperthyroidism normaly is divided into two
categories: Grave's disease or diffuse toxic goiter and toxic nodular goiter.
Grave's disease: The most common form of hyperthyroidism. It is an organ specific
autoimmune disorder in which antibodies produced against autoantigens stimulates
the secretion of the thyroid hormone. It may cause protrusion of the eyeballs..
Hasimoto's disease is completely opposite, as the resultant antibodies due to
autoantigens inhibit the secretion of the thyroid hormone.
Symptoms: Intolerance to heat, and weight loss, weakness and anxiety. Signs; heart
palpitation, nervousness, diarrhea, and tachycardia.
Diagnosis: -L- TSH and 1'T4 and T3
Pharmacotherapy: Anti thyroid drugs (methir:nazole, propylthiouracil), and lugol'
solution (KI + 1
2
),
Antithyroid Agents
Methimazole: MMI (Tapazole), propylthiouracil: PTU (Propyl-Thyracil)
Stop about Sdays prior to a thyroid scan, RAIU or treatment with 1311
SE: allergy, rash, agranulocytosis, hepatotoxicity arid nephrotoxicity (rare)
Stop if rash, fever, sore throat (agranulocytosis) or jaundice develop
PTU - daily, block theconversion of T4 to T3, DOC: pregnant &lactation women
MMI-TID
Anti thyroid drugs (methimazole, propylthiouracil): Both cross the placental barrier
and can accumulate in the thyroid gland of the fetus
Methimazole; Monitor TSH sensitivity test, side effects are cough, fever and
agranulocytosis
Propylthiouracil: Preferred in pregnancy for it does not cross the placental barrier.
80-2
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More agranulocytosis seen than tha"t of methimazole. Rapid absorption after oral
administration."Drug choice in pregnancy. Monitor; coniplete blood count
lugol solution (KI + 1
2
): Given as oral drops, and it may cause stains
Iodine
oral Lugol's solution, iv sodium iodide
Blocks thyroid hormone production, use in the acute management of severe
hyperthyroidism
Administer 1 h after PTU or MMI; blocks radioactive iodine uptake
iv sodium iodide - use for thyroid' storrrr . :
Lugol's solution - use for thyroid storm & prior to thyroidectomy (2 to 6 drops TID
7d preceding operation), 6.3 mg iodide/drop
Iodine, radioactive
sodium iodide 1311(lodotopeJ
SE: hypothyroidism, (I : pregnancy, in patients with significant ophthalmopathy-
with caution or steroids
Use to ablate thyroid tissue in patients with Graves' disease, toxic'autonomous
nodules and toxic multinodular goitres
Givmg.as single oral dose(usually only one dose required)
nonselective: propranolol
Selective
atenolol (Betaroc, lopresor)
use adjunctively in the management of"Graves' disease or toxic nodules
CI: asthma patients
Propranolol; 'conversion of T4 to T1
Selective Betat-blocker; foster onset of action than propranolol
Corticosteroids, systemic
dexamethasone, hydrocortisone sodium succinate (Solu-Cortef),
Use adjuvant therapy in treatment-resistant cases for hyperthyroidism
dexamethasone - for thyroid storm
hydrocortisone - for Myxedema coma
80-3
Phannacyp.rep:com .
-1 ..
Thyroid disorders
." .' ...
Tips
fr th t bl t 002 F' d IpS onna ill answers om e a e:
l. Bradycardia 2 Hypotension 3 Constipation
4. Diarrhea 5 Dry skin 6 Sensitive to heat
7. Weight loss 8 Weight gain 9 Sensitive to cold
10. TSH <0.5 1l. TSH > 5.5 12. Graves disease
13. Hashimoto disease 14. Thyroxin 15 Methimazole
16. Propylthiouracil 17. Lugol solution 18
T
Symptoms of hypothyroidism ( \ ,'3
,
5) 8', j )
Symptoms of hyperthyroidism ( 2, " I ' ,7 )
Hyperthyroidism ( 10 )
(If)
What is the drug of choice for hypothyroidism ( )
What is the drug of choice for hyperthyroidism (I S 4-)' ,
What is the drug of choice for hyperthyroidism in pregnancy (I ')
What drug that are taken empty stomach ( '4)
Drug absorption is decreased if taken with calcium supp or dairy products, iron,
antacids (11 )
What drugs that stain (r1)
Severe fever, sore throat and agranulocytosis are the side effects of ( r.t.)
Calcitonin is stimulated co.J <:eM. 4lC,... .........
TSH is secreted from cf' - 4
In treatment of hypothyroidism with T
4
have e'tIect on hl.-dcJive. O'{d; t'tt.fh1
Hypothyroidism is monitored by Seut,.., .,SIJ I '2:t3, f=.i '7
T
4
metabolized to T
3
by deiodinase enzyme in --> PeMpk.Q.(JiLI
Sweating is symptom of h Jy,.,
Lugol solution is an oral drops of? 16-(. 1<"1 l' 5/ !
Thyroxine absorption is decreased by Co, 1"'11 1M ,'M'1.-
Hyperthyroidism in pregnancy: PTU is drug of choice, with the lowest possible
,/ doses used to maintain the maternal T4 level in the high normal range. (True)
A 55 yo women using levothyroxin 75 meg to treat hypothroidism. She is
experiencing sweating, heat sensitive and diarrhea. Indicates overdose..(True)
levothyroxin take in the morning empty stomach(True) .
levothyroxin take with full glass of milk (False)
Lugol solution used to treat thyrotoxicosis, (Graves disease) (True)
hypothyroidism, Total T4 decrease(True)
hypothyroidism, Free T
4
decrease(True)
hypothyroidism, Total T
3
decrease(True)
80-4
hypothyroidism, Serum TSH decrease(False)
hypothyroidism, Free Thyroxine index decrease(frue)
IT4, Tf4, TT3 and ITI decrease in hypothyrodism, only serum TSH increase.
For hyperthyroidism, exactly opposite changes. (True)
Myxedema; In this disease, the patient may have slow speech, a puffy face, slow
pulse, low BMR and scanty hair. (True)
Cretinism: The growth and height of the child is stunted. The patient has low
BMR and a bloated face. The patient is also mentally retarded. (True)
Goitre: It is also known as simple or non-toxic goiter. A dietary deficiency of
iodine may be responsible for this. The neck of the patient is swollen. (True)
Toxic nodular goiter: It is due to benign neoplasm or adenoma or may be
because of long standing normal goiter. (True)
Hashimoto thyroiditis: Illeads to hypothyroidism(True)
Diseoniinue antithyroid if patient notice even a single rash (Pruritis
Maculopapular rashesh associated with vasculitis)
Why is it beneficial to add propranolol to a drug regimen of a patient diagnosed
with hyperthyroidism? decrease heart rate. anxiety, tremors, and heat intolerance
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Thyroid disorders
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G1J tft--a-
Contraception PhannacyPrep.!=om
Contraception
Questions
Emergency contraception like plan B, side effects (N&V) I JI
Side effects of oral contraceptive pills .
OCP Dis (phenytoin, Carbamazepine, topiramate)
OCP CI's: coronary artery disease, DVT, PE and liver diseases
Barrier methods: condoms: male (latex, polyurethane, lambskin)

. Protect against STls including HIV (latex condoms only)
Lambskin: G? protect@9gainst STI
latex: SE: hypersensitivity in either partnerEater integrity)
Condoms: female
Not to be used with male condoms, shelf-life of up t.o 5 years
inserted up to 8h prior to intercourse & removed immediately after
Diaphragm: U.s-e-d
SE:(fuxic shock syndrome]
Use with spermicidal, can be 6 h before intercourse & used in breastfeeding
women
Use silicone diaphragm (allergy to latex)
t7\O I'" 10"" L>.s G- :DUR::!.HUT /Xl f-N.5 -rRlJA-T3-01'J.
/ Sponger-:.:....-_...v-=____--,
; SE: oxic shock syndrom spermicidal is released in a sustained fashion for ip to 12h
r<
Do no us urmg menstruation
USi1 . ro At+elL- 6 [16 /Yl ov.#t J d&.J"(J
Cervical cap 4 \r
shock syndromg] can be left icefor up to multiple acts of
intercourse
Can be used in breastfeeding women, Not to be used within 6wk of delivery
-
81-1

S iO"'c..I at
oCPs
ACflES '.
---------
Contraception
Intrauterine devices (IUD): copper-T IUD (Nova-T, Flexi-T);
Spermicides: nonoxynol-9 (Vaginal Contraceptive Film)
Not effective against HIV or STI
PharmacyPrep:Com
Contraceptives, oral combination
Avoid in lactating women during the first 6 wk postpartum, with caution in the first 6mo
postpartum
Sf: chloasma, hypertension, breakthrough bleeding/spotting, N/V, breast tenderness,
,
mood changes-. .
use backup barrier method during therapy
Obesity affects metabolism to compromise contraceptive efficacy; Not effective
ACHES: danger sign3lls: Abdominal pain/Chest pain/Headaches/Eye problems/Severe leg
pain
Diane-35 (EE35ug I cyproteroneZmg): 3ft . +J.. .....1
Drug of choice ir('[ere (Not for birth control) alovVL-- l;"G - e.: lTVJ' J.,.,U.
Discontinue 3 to 4 me after signs of acne have completely resolved LGj p'lJOl-t?AV'-- .4 (
=It Contraceptives, .transdermal; EE/norelgestromin.(Evra)
(. Applya new patch the same day of the wk for 3 w
If off for> 24 h - start new patch & use backup method for 7 days
OCPs-) patch: the first patch on the first day of withdrawal bleeding
If later than the first day of withdrawal bleeding, use backup method for 7 days
Depot patch: start on day of scheduled injection
Not effective - Weight 90 kg or more
Do not apply on chest
1f Contraceptives, progestin medroxyprogesterone acetate (Depo-Provera)
=#' Contraceptives, vaginal ring - EE/etonorgestrel (NuvaRing)
CI:< 6 wk postpartum jf breastfeeding
Do not use diaphragm or cervical cap as backup, vaginal tampons (ok: after removing
vaginal rjng)
,
Can be left at RT for 4 mo, 3 wk inside then removed for a lwk break
left out longer than 3h -) efficacy use backup method for 7days
=If Contraceptives, (Micronor) .
'" Inhibits cervical sperm penetration by thickening the cervical mucus
V ,//C;n use IJover 35 years old smoke;, 2j intolerate ethenyl estradiol, 3)have unwanted SE
.'7,J1KY with COCs 4)breastfeeding, 5)migraine with neurologic symptoms
q SE: ectopic pregnancx, irregular bleeding, DOC: lactating women, contraindication to EE
Contains 28 tablets of active drugs
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PharmacyPrep.Com O.
I

CJnLY "
Depot injection, can use in the postabortal state (5 days postpartum), during
(6wk postpartum)
Can use over 35 years old smoker, and' intolerate ethenyl
:CI: pre'gnanCV7:breast cance.r, SE:
b Injected within first Sdays of onset of menses, interval between injections must not
V exceed 13 wE)
Ovulation & regular menstrual periods ma@esume for up to a year after the
injection '
Contraceptives, progestin only intrauterine system (IUS) onorgest;j)Mirena)
Inserted within 7 days of onset of menses, remains in place for 5 y
Highly, efficacious ( 0.2%)
. ,
if: Emergency contraceptive methods
y. EE SOllg+levonorgestrel 0.25mg/dose (Ovral)
SE:
dose of l.Smg used within 24hr (prevent 95%) can take up to 5 days after
unprotected intercourse
copper-T IUD (Nova-T): consider up to 7 days after unprotected intercourse
Contraception and breasrfeeeJing
Oral contraception should be avoided in postpartum women and breast-feeding until 6
I
weeks after delivery. Barrier contraceptives can be used.
.
Progestin contraceptives only-be used during lactation (without increase of
thromboembolic events). be
(progesterone unlike estrogens do not inhibit the bindin of prolactin to
its decrease in breast milk, therefore Progestin i preferre
C:?
-::IF Starting OC's
1st tablet either,on the day of menses (eliminates the need for alternate means of
Y contraception) or take 1
st
tablet on the first Sunday after beginning of menses and use and
use extra contraception method for 7 days of OC's
Oral contraceptives are best taken in the eveRing (before bedtime, to decrease the side
effects such as nausea, breast tenderness, chloasma (exacerbated by sunlight when
estrogen concentration are high and can be prevented by the use of sUrlscreen wide hats).
11
Missed pills
If 1 pill, then take as soon as you remember and next pill as per schedule (no need for
extra contraception method) ", .
If 2 pills missed,oin a row 1
st
/2
nd
week take 2 pills when remember and 2 pills the next day,
and use alternative method of contraception for 7 days from the day missed.
81-3
'0
If 2 pills missed in 3
rd
week, discard pack and start new pack or continue a pill everyday till
Sunday and then start a new pack and use alternate method for 7 days.
The same applies for 3 pills in a row for any week.
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Tips
Find answers from the table
1. Owal 2. Plan B 3. Condoms
4. nonoxynol-9 5. Pregnancy 6. breast cancer,
7. Deep vein thrombosis 8. Vaginal bleeding
Alesse
10. Dian 2S 11. Nausea and vomiting 12. Dimenhydrinate
13. Chloasma 14. Breast tenderness 15. Chest pain
16. Headache 17. Eye problems 18. Severe leI!: pain
".
Tampons 20. Evra patch 21. Nuva ring
22. IUo. 23. Depo provera 24. Abdominal pain .
Spennicidal: Vaginal contraceptive film ('f) \t10\"LO'lOj'
. Contraception method may protect STls and HlV (..3) CO\l\ (JA..
P1ta'k..-0 .
Oral contraceptives approved to treat acne ( ) 0 d'l e.tl\t..4 AI I, <:r
WhalisthecommonsideeffectofplanB( ) If ' h
What is used as treatment for nausea and vomiting for contraceptives (11) l.9f w.eJ1
What contraceptive methods and hygiene prQciuct that can cause toxic shock syndrome (",) 2.1, J...l- 4---
Contraceptive method that applied for o'nce a week, (10)" r=..vAP.. tW'A
NI
The side effects oforal contraceptive pills ( ) f rJ 13, '4 ", .3..
The dangersignals of oral contraceptive pills ( A-l>d.... -.e-l ) (1.1. I duf- (7'-", kJ.oJcL.) e"ll'-fl'O'to
D.."..f ,l'lq'1.B ....... r..., "....: 4"H"" (1<)
Emergency contraception plan B side effeots y
If missed one pill, what should be done ( ) {4.L. l.. pIli "",,} d.<l-
Contraceptive method that used once a month (removed after 21 -days) (
Select True 'or False Statements
Non contraceptive health benefits of OCs include decrease endometrial cancer, ovarian
cyst, endometriosis pain, fibroids. dysmenorrhea, and pelvic inflammatory disease.
(True/False)
Oil based lubricants should not be used for latex condoms (male), diaphragms, cervical
caps. (TrueIFalse)
Diaphragm and cervical caps do not require a prescription but need a trained health
professional to insert. (TruelFalse)
81-4
PharmacyPrep.Com G,ontraception
..... I'
....
used along condoms, diaphragm, and cervical cap. (diaphragm
spenmcidal for every mtercourse where cervical cap does not require extra
spermIcidal for subsequent intercourse. (True/False)
STI are only prevented transdennal patch contraceptives. (False) A
STI are only prevented subdermal progesterone implants (False)/
STr are only prevented ,by condoms contraceptive methods (True)
_
' 0./ contraceptive Evra patch should be applied to the abdomen buttocks upper
V torso, and upper ann at the beginning of menstrual cycle (True) ,
Absolu..fL -+0 oM!
CovJt.".c.... C.e.p h d VL / COYT"l bI N2.. a w;L- p?J1lij acJ, Vl-- Go ..Jc.,N
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CeAJL/qAo u...1.f:;vL d
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0A-o. pt>--!>T v.is..Jv'Cf '1 VeAA-<'LU
cl ,cxkefhC:;1 VY'l1:cHJ CCJkhtJ'CcdJ61'
1+1 s+tJ"(f at M"l-Clll-
f"-nOL<> 111 O>CJ4},O'1 d1r'
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,LI va.J'L-- fy'N) M-. . (J
AuWL-
IdI4;- /' S B P :;;. I (, 19 Iv) r<> H:d
BP . >: I (JfD . f,v.,. tJ-rJ
C' . .
/7)
-'
81-5
Gynaecological and Genitourinary
Conditions
Male sexual dysfunction
Erectile dysfunction treatment: POEs inhibitors: Sildenafil, vardenafil, and tadalafil.
effects: headache, flushing, dyspepsia, nasal congestion, transient visual disturbance,
dizziness, and skin rash. Rarely: priapism, and permanent visual loss
pru_g bladeers, CYP3:A"4 ihHi15it6rs, gfapefrUffluice, and

Questions Alerts!
Risks associated with endometriosis
Menopause symptoms
Toxic shock syndrome causes
Drugs to treat erectile dysfunction like sildenafil, tadalafil and vatdenafil 01 with
nitroglycerin

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82
Gynaecological and genitourinary conditions www.phannacyprep.com
Dysmenorrhea :DOc. c. Ac::r<D
Painful menstruation is referred to as dysmenorrhea
Increase levels of prostaglandin during ovulation" cycles, in endometrium it gives cramps,
this leads to menstrual pains. Thus problem can be treated by prostaglandin inhibitofS.
Drug of choice is mefenemic acid or dielafenae.
Endometriosis
Endrometriosis can cause pelvic pain, dysmenorrhea and infertility.
Treatm.ent for oral contraceptives, progesterone only oral contraceptives,
androgen agonist: Danazole and gonadotropic releasing hormone (GnRH) analogs
Treatment of fertilitY: Clomiphene
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PDE
s
inhibitors: sildenafil (Viagra), vardenafil (Levitra), tadalafiJ (Cialis)
CI: nitr?tes emergency care if chest pain present within 24 to 48 hr of taking PDEs
inhibitors,or use for 5 days after stopping long-acting nitrates)
non selective a-blockers, CYP3A4 inhibitors
SE: headache
Sildenafil- 30 to 60 min before sexual activity
Dose adjustment: hepatic or renal disease 30mljmin) & in the elderly
L- .. f:. . .
., (go to see a doctor).
.'..;.
Vardenafil- 30-60 min before sexual activity
Dose adjustment: in moderate hepatic or renal disease & in the elderly
. (go to see a doctor)
li! . . take empty stomach
activity
Dose adjus'tment: No need in the elderly
&.p.efmanent vision -loss (go to see a Dr)
YV:hI\,.. - no more frequently than _
t><V\;\. CI impairment . 1 I?u J (.
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he"" :J
PGEl analogues: alprostadil; intracavernosal injection (Caverject), intraurethral
pellet (MUSE) .
Use to Pts with taking nitrates or a-blockers ./. __
Injection - not use more than once daily or times /wk, t least 24hr between each dose
----.,
Pellet - not use more than once per 24hr perio, : BP (detect asymptomatic
hypotension) -
Menopause
Cessation of menstrual periods is referred as menopause.
The average age of !Jlenopause in Canada is years
flushes, night sleep disturbances, lethargy, vaginal
dryness, dyspareunia (painful sexual intercourse). .
These symptoms are mainly due to the depletion 0 strogens and progesteron
Toxic shock syndrome (TSS)
It is a infection resulting from toxin-producing strains of S. aureus.
TSS is a severe life threatening condition, can evolve clinically in rapid becoming
severe ill in less than 12 hours.
r. .
TSS is associated with use of tampons, reservoir types of contraceptives such as sponges,
IUD, and cervical caps. However condoms are not associated with TSS.
82-2
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Benign prostatic hyperplasia (BPH)
It is a condition where a male prostate becomes enlarged to the point that it causes
discomfort.
There are two categories of symptoms:
Obstructive symptoms: Weak urinary stream, difficulty initiating stream, stream starts and
stops, inability to terminate, post void dripping, urinary retention, sensation of
empty bladder.
Irritative symptoms: Urinary frequency, nocturia, pain during urination, urinary urgency
Treatment: Sa reductase inhibitor; finasteride and dutasteride and Qadrenergic
antagonist tamsulosin, prazosin. doxazosin, and terazosin.
enzymeCatalyzes
Premenstrual symptoms (PMS)
Cyclic re occurrence of physical, behaVioral, and psychological symptoms during the luteal
phase of menstrual cycle (after ovulation).
PMS symptoms occur 1 to 2 days before periods: may be due .J., progesterone, or estrogen
A sever PMS include, and mood changes.
luteal phase of menstrual cycle
All women have no PMS.
There is(f!o treatmenl)for PMS
Evening prime rose oil is used for PM5.
Vaginitis ar vaginasis
Infection of vagina caused by vaginal microorganisms or overproduet;ion.
-!-/:;- [.eaeterial-vaginosisrJ
-rr -7 Creamy and fishy odor discharge (yellow/grey)
Most common form of vaginitis
Sexually transmitted disease thus partner requires treatment
=If . .I oi'fiTiU(<#J.rJp!9!,i ,J
-7 Severe pruritus, with white cottage cheese discharge (only recommended for self
treatment).
It is tra.o_smitted disease thus partner d.oes not r.equire treatment'
Qver the counter antifungal are drug of choice

Yiconazole,
=#' . Trichomoniasis : ----7 p,A:lf:rD 'Z.0 A :w.,te-
cho
'1'
.;.--- -7 frothy, wet discharge
It protozoa infection
It is a sexually transmitted disease thus partner require treatment
Atrophy ,,-
-7 Vaginal discharge, spotting, and soreness, burning.
Drug of
82-3
Gynaecological and genitourinary conditions
LJrY6 1-

Urinary incontinence in adults ..... t,.v.e.AH
Bladder symptoms the leakage of moderate to large amount of urine to
hyperactivity, stress, and over distended bladder. .
Stress incontinence; loss of urine due to an increase in intra-abdominal pressure.
Examples: cough, and exercise.
Urge incontinence; symptoms of overactive bladder which caused by inability delay
voiding when urge is perceived. Examples eNS condition, like Parkinson's disease and
stroke.
Overflow incontinence; involves the leakage of urine due to an over distended bladder,
commonly resulting from outlet abstractions. ie"causes
t..: .... "1'. - l-r ..--'
:.I'1eut<:1pat or'miJ tIJJle's"derosls. .
Functional incontinence; loss of urine caused by the inability to get to toilet. Example;
physical disabilities, difficulty removing clothing, cognitive factors such as dementia,
depression, or environmental factor such as distance to tOilet, positioning.
Drug of choice is anticholinergics; oxybutynin (Ditropan)
. rin'ar\li ncoht1nence;" aiITretics,
Enuresis in children (bed wetting)
. Drug of choice is: Antidiuretic hormone derivativestgesmopressinfDDAVP)
Smooth muscle relaxant: Oxybutynin and imipramine
Tips
Find answers from table:
"J ..... I. _ pe..lVIc..
peV" l-.. , IUt'J I pAJ"'"
Symptoms of dysmenorrhea -7 ..2. c. , V[)........
Symptoms of endometriosis -7 fd"rC fCJ" I
What microorganism cause toxic shock syndrome -71( 5 ::(lJ.:D ceJ\v,a:J rzo.42J
What contraceptive methods can cause TSS -7 2.1, 23.ct 11 J _ I.W)
WhatdrugsareinhibitorsofPDE
s
enzyme-7.t5"" S' IdeJ'\a.f J
l. Mood changes (-swing) 2.. Flushing 3. N.ight sweat

4. Vagina dryness 5. PDE
s
inhibitors 6. ox'Y.butynin
7 Luteal phase 8. Urinary incontinence 9. Benign prostatic hyperplasia
(BPH)
10 Premenstrual syndrome 11. dysmenorrhea 12. Jet urination
(PMS)
13. Difficulty in urination 14. Finasteride 15. Dutasteride
16. Prazosin 17. Tamsulosin 18. irritation
19. Saw palmetto 20. Pelvic pain before periods 21. 5. aureaus
22. Contraceptive sponges 23. IUD 24. Cervical caps
I
25. Sildenafil
.
82-4
82-5
Select True or False Statement
A customer of your pharmacy presents with symptoms of vaginal discharge, yellow and
fishy odour. Refer to doctor is appropriate? (True)
Color discharge and fishy odour is indicator of bacterial infection, thus refer to doctor.
tr as.y.mptomatic sex:uCl 11y:'t['ansmittechi rifeGti'ons; Gan'calise
disease and infertility (True) -
pre menstrual symptoms occur during luteal phase. (T-rue)
toxic shock syndrome caused by infections of S. aureus. (True)
toxic shock syndrome can cause by tampon use. (True)
toxic shock syndrome Can cause by condom use (False)
toxic shock syndrome can cause by candida infections. (True)
toxic shock syndrome Can cause cervical cap contraceptives. (True)
patients experienced priapism condition avoid using sildenafil? (True)
patient have reported visual disturbances condition avoid using sildenafil? (True)
patient using nitrates condition avoid using sildenafil? (True)
Nitrates-+ sildenafil should not take together because -7 LO vf '11J.
Menopause symptoms I +0 4 Moo<i <.1-<."'(1- """'..,, I POd I '<I- I Nlo:, <.S , kJ..-
Benign prostatic hyperplasia symptoms include all except -7 12 .Te.t- 0'1 cht;l.
What phase of menstrual cycle does PMS symptoms occur -7 7 pl1.a.5..e-
What drugs should be avoided in urinary incontinence d j c.s
What is the drug of choice enuresis in children -) jynj .o;\... d ,e&':""Op-<f-f'1
Symptoms of menopause ( ) l-f-b 4 Mood tfIW Lul.oj, I -q.. ":"J
Sildenafil, tadalafil, vardenafil are (5) P.::D G-s- iY\h\ .
The drug of choice of urinary (b) 0')<..:3 h ul:1
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Occurs in premenstrual syndrome (PMS) (7) L..u:te.oJ
, , \' tv<-' -j-.J),"'--
Symptoms of benign prostatic hyperplasia ( 13
1
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The drug of choice forBPH ( Ilj) "
The drugs that used to relieve the symptoms of BPH (14,6/ ". '7 >1
&-. -ra,........$ O'-(GCS,..,
What is not symptoms of BPH (12 ) t...V'4J1CJ/"1 " . . I
What anticholinergic drug that acts on M
l
receptors ( b - o)(..d)buJj"" '1
is u'sed- to treat prostatichyperplasia'(. 15' ) - .$c.b:'
Gynaecological and genitourinary Conditions
www.pharrhacyprep.com
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Osteoarthritis, Rheumatoid arthritis and o ~ t arthritis
Oste:o-arthoritis, Rheumatoid
.. ": ..
Arthritis' arid GO,ut Arthritis
Questieos Alerts!
Osteoarthritis therapy: acetaminophen 650 mg q4-6h
Rheumatoid arthritis therapy: Methotrexate and Infliximab
Methotrexate dose ( max 25 mg/wk)
o. Acute o ~ t attack therapy: Indomethacin, colchicine and prednisone
Acute gout risk factors:
Osteoarthritis (OA) is a degenerative joint disease caused by a breakdown of the
cartilage between bones.
Rheumatoid arthritis (RA): Inflammation of joints with frequent acute attacks.
Rheumatoid arthritis occurs when body's immune system attacks the tissue
lining and results in the joints causing cartilage to erode.
Causes:
RA; autoimmune
OA; aging of cartilage and trauma
Sex distribution:
RA; more common in females
( OA; equal in both sex
Symptoms:
~ RA; Joint stiffness in the morning, painful and swollen joints
e OA; Painful joints, restricted joint movements
Diagnosis:
eo RA; Rheumatoid factor, erythrocyte sedimentation rate, x-ray, antinuclear
antibody
OA; X-ray only
Treatment
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Osteoarthritis, Rheumatoid arthritis and Gout arthritis
lab'irwestigations of RA.
Question Alert!
Question Alert!
Initial therapy to treat osteoarthritis;
acetaminophen 650 mg q4-6h
Non-prescription:
Acetaminophen is initial drug of choice for
symptom relief. Maximum therapeutic dose
should be tried for 2 to 3 weeks
Acetaminophen 650 mg 4 to 6 times a day
ASA/NSAIDs/lbuprofen is 2
nd
line therapy
Acetaminophen + caffeine + codeine
Glucosamine/Chondroitin
Topical counter-irritants (Methyl salicylate/Menthol/Capsaicin)
Rheumatoid arthritis -7 NSAID's, and DMARD's
Osteoarthritis -7 NSAID's
Osteoarthritis
A degenerative joint disease caused by a breakdown of the cartilage of the bones.
Degradation of articular cartilage in synovial joints
Prescription Medication:
CQX-2 inhibitors (Cetecoxib) as effective as NSAIDs but lower incidence of GI side
effects.
Intraarticular corticosteroids (3 to 4 injections year)
Hyalunon injections only for those who failed other therapies
Narcotic analgesics
Rheumatoid arthritis
A chronic systemic, autoimmune inflammatC?rv condition. Symmetric synovitis affecting
similar joints bilaterally.
It is non organ specific autoimmune disease
Type III hypersensitive reaction
Blood contain rheumatoid factor
Stiffness occurs in the morning
Large of areas of joints are effects
Symptoms Osteoarthritis Rheumatoid arthritis
Stiffness Morning or after inactivity (last 30 min) In the morning (last 1 hour)
limited affected joints.
Localized Worsens with activity or Not localized
Pain after prolong use, (weight bearing activity) Worsened with prolonged inactivity. (usually
Generally weight bearing joints improves with activity).
Affects on .weight bearing and non weight
bearing joints
Inflammation Uncommon Common
Risk factor >6S years Autoimmune
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Question Alert!
Methotrexate dose.
Lab tests before initiating methotrexate
Not associated with frequent of use of joints
It effects on weight bearing and non-weight bearing joints.
Pharmacological Choices:
Disease modifying anti-rheumatic drugs (DMARDs)
Methotrexate is the gold standard for the treatment of RA
Should be started within 3 months of disease onset (max effect in 3 to 6 months)
Initial dose of 20 to 25 mg po/wk, do not exceed> 25 mg/wk
Minor SEs oral ulcers can be reduced by concurrent use of folic acid
Should be avoided in patients with hepatitis Band C, renal insufficiency, or lung
disease, serious SEs are cytopenia, and hepatic
toxicity.
Hydroxychloroquine; SE corneal and retinal
deposition
Sulfasalazine
Leflunomide: Can be used in combination with methotrexate (CI in pregnancy) or in
place of it for patients who have failed or have contraindications to methotrexate.
Should be stopped in both males and females at least 3 months before attempting
conception (patient must undergo drug elimination by taking cholestyramine 8 g TID
for 11 days.
Azathioprine a purine analog immunosuppressive agent
Cyclosporine
Minocycline
Penicillamine
Gold sodium thiomalate
NSAIDs
Glucocorticoids; Prednisone/Triamcinolone - safest therapy during
pregnancy and lactation
Biological response modifier: Infliximab, etanercept,
adalimumab
Infliximab
Biological response modifier act as TNF 0 inhibitorlt is monoclonal antibody
Only available as Lv. Store in refrigerator
Approved for ulcerative colitis. Question Alert!
It is always used with methotrexate. Infliximab mechanism, SEs and monitoring
SEs: The most common SEs are headache,
fever, chills; fatigue, diarrhea, pharyngitis
upper respiratory tract and UTls.
83-3
NSAIDS: Indomethacin
It is prostaglandin type I NSAJDS
It has the highest anti inflammatory action in all NSAIDs
""""'''',,'m
Normal joint
PharmacyPrep.Com
Gout Arthritis
Gout is a disease in which monosodium urate monohydrate (M5U) crystal are deposited
in joints, soft tissues such as cartilage, tendon and bursa or renal tissues such as
glomeruli, interstitium tubules. Gout arthritis involves 4 stages Asymptomatic
hyperuricemia, Acute gouty attacks, Intercritical gout, Tophaceous gout
Risk factors: protein diet, meat, beer and male gender
Asymptomatic hyperuricemia
Normal serum urate levels: Woman 360 DmoVLand men 420 unollL More
common in men over 40 year of age
Hereditary metabolic disease that is a form of acute arthritis and is marked by
inflammation of the joints.
Gout is associated with increased body stores of uric acid.
Acute attacks involve joint inflammation caused by precipitation of uric acid crystals.
Hyperuricemia Urate crystal in joints inflammatory response
Acute gout (attack) arthritis
Abrupt onset of excruciating pain and inflammation of joint at night or early
morning.
Patient cannot tolerate even light pressure such as a bed sheet on the affected joint.
Attacks bften resolve spontaneously over 3 to 10 days.
1
st
line treatment is NSAIDS like indomethacin, colchicines (if NSAJDS
contraindicated) and corticosteroids (if colchicine is contraindicated)
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It has high GI irritation SE (add'gastroprotection with PPI for patient with risk
increases o ~ GI bleed) .
It does not decrease uric acid
Colchicine
It is anti-inflammatory drugs
It has no analgesic action
The most common SE is GI irritation
Cl: in severe renal diseases (CrCI <50 ml/min)
Corticosteroids
Given intraarticular injections for monoarticular pain
Given oral for polyarticular pain
Question Alert!
Colchicine CI in severe renal disease
._0- _.
Treatment of hyperuricemia: Antihyperuricemic agents as Allopurinol, sulfinpyrazone
and probenecid
Allopurinol
Inhibit xanthine oxidase (XO)
Allopurinol and azathioprine drug interactions is due to which enzyme: XO
SE: Rash is the most common, can form urate crystal in kidney. Take with plenty of
fluids
Dis: Half life of azathioprine and 6 mercaptopurine increased by allopurinol so this
may increase toxicity from increased plasma concentration of these drugs.
Oxypurinol is metabolite of allopurinol
SuIfinpyrazone
Probenecid
Tips
1. Acetaminophen 2. Methotrexate 3. Minocycline
4. Hydroxychloroquine S. Infliximab 6. Allopurinol
7. Sulfinpyrazone 8. Colchicine 9. Indomethacin
10. Weight bearing joints 1I. Non weight bearing joints 12. Obesity
13. Family history 14. Inadequate Ca & Vitamin D 15. Deficiency of
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Morning stiffness is symptoms of [9
Rheumatoid arthritis can occur on '7 10 11 ld J-I,ltlPWV
Examples of DMARDs -? 2,9 ,t, :;..J :D _f
en
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Biological response modifiers a1.p}.q 4- ,a..feAku.kt".
TNF-alpha blockers -? 5/ E-1-<1"'-Veft-, Ad",.!,,,,,,..,,,, lo' .
Biological modifier that blocker Il-l -7 5 / I r
Methotrexate maximum dose for rheumatoid arthritis treatment is -7 l.L-
Infliximab is a .2.3 .
Acetaminophen have least activity as -7 f+t,.J1 ,. n,a:J..r!Jt<t/- /l-c.hIJ'}
Probenecid, sulfinpyrazone and allopurinol should be taken with "f5t.A
This may cause renal damage or bone marrow depression (1....)
The drug of choice against osteoarthritis (' )
An anticancer drug used for the treatment of rheumatoid arthritis (2. 4- ItJH'hJ.-e
Drug that used to treat rheumatoid arthritis and malaria (4)
A broad spectrum antibiotic used in the treatment of rheumatoid arthritis (3)
Drug ysed for rheumatoid arthritis and Crohn's disease treatment (5)
A suicide inhibitor of xanthine oxidase (XD) (, )
Drugs that promotes uric acid excretion in urine { IS, '1
Drugs used to treat acute gout attacks (9',1
long term use acetaminophen is associated with -->
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19.
22.
Hyaluronic acid
RA
25 mgfWK
17. Intra articular
20. Osteoarthritis
23. TNF alpha blocker
estrogen
lB. Probenecid
21. Gout

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Questions Alerts!
Osteoporosis
84
Osteoporosis
Risk factors of osteoPorosis . ,
Calcium and vitamin 0 supplements
Calcium and vitamin 0 dose and ol's
Bisphosphonates like alendronate, etidronate and 1Olendranoic acid
doses
' ..
Osteoporosis: Overall reduction of bone mass {osteopenial. resulting in thin, fragile bones that is prone to
fracture.
Paget's disease; Bone remodeling disorder, resulting in excessive bone resorption followed by
disorganized.
Risk Factors and Supplements
Non Modifiable Modifiable
Age>6Sy lowcalcium intake 1000 mg elemental
Vertebral compression fractures calcium per day)
Postmenopausal woman (not on estrogen

Inadequate sun exposure.
therapy)
Cigarette smoking
Premature menopause 45 years)
Excessive alcohol intake
Gender (Female)
Caffeine containing beverages.
Family history
Sedentary life style
Thin and small boned

Excessive heparin therapy
Hypogonadism

Oral corticosteroid therapy
Race: Caucasians. Asians

Hyperparathyroidism
Hypocalcemia
Prevention

migration and osteot'tIc
.ctlvl1Y. pmeto,.
Modulate signallIng from
osteoblasts to osteoclasts
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Concentrated In newb'
mineralising bone and
under osteoelasts
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Selective Estrogen Receptor Modulators: raloxifene (Evista)
Vitamin 0
Vitamin 0: < SO Y400 IV/day: > 50 y: 800IU/day
SE: hypercalcemia, hypercalciuria, renal calcification, renal stones (usually at very
high doses)
Vitamin 0
3
(cholecalciferol) is preferred over vitamin O
2
(ergocalciferol).
Nutritional Supplements: Ensure adequate intake of both Calcium and
vitamin 0 of these nutrients when prescribing pharmacologic therapy
Ca - Premenopausal women: 1000 mg/day, menopausal women & men> SO y
1500 mg/day
SE: constipation & nausea
. Osteoporosis
calcium Salts;
Calcium carbonate (40% elemental calcium)
Tricalcium phosphate (calcium phosphate, tribasic) 39%
(aldum chloride 27%
Calcium citrate good choice for seniors
Calcium lactate (13%)
Calcium gluconate least elemental calcium
wWw.PharmacyPreD.Com
Pharmacotherapy:
Bisphosphonates: etindronate (Oidronel, Oidrocal: packaged with calcium in 3 .
month kit)
Alendronate (Fozamax), alendronate/VD (Fosavance)
risedronate(Actonel), risedronate/Ca (Actonel Plus Cal
Safety in impaired renal function (CiCr < 35 ml/min) is unknown.
SE: GI symptoms, muscle pain, osteonecrosis of the jaw (ONJ)
Take on an empty stomach and only with water - very poor intestinal absorption
etindronate - Cyclic use: 14 days Q3M, then Ca alone
take at bedtime, at least 2 h before or after eating
Ca supplements should be separated by at least 2 h before or after.
Alendronate: Prevention: 5 mg/day, treatment: 10 mg/day or 70 mg once weekly
Take at least 30 min before the first food, beverage, or medication
SE: esophageal ulceration NOT lie down for 30 min after taking
Risedronate - 5 mg/day or 35 mg once weekly
Take at least 30 min before the first food, beverage, or medication
SE: esophageal ulceration NOT lie down for 30 min after taking
aJendronate/VD - VD : once weekly
risedronate!Ca - Ca: day 2-7
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www.PhannacyPrep.Com o _ Osteoporosis,
Prevent postmenopausal bone loss, estrogen NoO 1'car.diovascular.risk

absence of hip fracture prevention data - consider 'after bisphclsphonate therapy
SE: Leg cramps, hot flashes (not be'startei:l until menopause is established) 0 0
Venous thromboembolism risk similar to estrogen
Calcitonin Peptides: calcitonin salmon, intranasal (Miacalcin NS) & sc
(Calcimar, Caltine)
Second line therapy, reduces pain associated with acute.vertebral fractures
Nasal spray prevent vertebral fractures
Anabolic Agents - (Forteo)
SE: orthostatic hypotension (in a supine or sitting position for administration)
parathyroid hormone (PTH) analogue
sc for 18' lifetime exposure in Canada (2 years in the USA), due to occurrence of
osteogenic sarcoma
Consider for severe cases characterized by more than one fragility fracture and a
very low BMD
lips
1. Alendronate 2. Calcium carbonate 3. Risedronate
4. Raloxifene 5. Calcium citrate 6. Calcitonin
7. Family history 8. Inadequate Ca & Vit D 9. Deficiency of estrogen
10. Swimming 1l. Weight bearing 12. Obesity or overweight
,

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Risk factors of osteoporosis ('1

Approved for prevention and treatment of postmenopausal bone loss, treatment of
established osteoporosis and glucocorticoid-induced osteoporosis ( ',J )
40% elemental calcium; provides the most calcium (2. )
Selective estrogen receptor modulator (SERM), estrogen like action on bone and
lipid metabolism ( 't )
A hormone secreted from thyroid gland ( ()
Calcium supplement recommended in elderly (S )
this drug should be taken first thing in the morning on an empty stomach ( ',.3)
What is NOT risk factor of osteroporosis -7,2-
Bone remodeling occurs, which is present-7
Osteoporosis is caused by -7 Ck,.5 I C!..(
Androgen deficiency cause -7 P0!vtr.11J ,.'" t'Y)eJ1 (.
Recommended daily allowance of vitamin D over SO year old is -7 0 'U
Elderly may absorb calcium poorly due to -7 a cJ, ro"'-"dc/A.J (,
Paget disease-7 aJ,"4M-1d bo"'L-
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Osteoporosis
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calcium carbonate (40% elemental calcium)-7 0"" .0. C teJ.:."c. e.nVI..to.. 4b..so.Af'l,

What excercise is the least beneficial forosteoporosis ._> S,&..f"'Y)Mf'd-
Inadequate Ca and vitamin 0 can cause osteoporosis (True)
Smoking increase risk of osteoporosis? (True)
Physical activity like weight bearing excercises like stair climbing, walking, and
jogging decrease risk of osteoporosis. (True)
Increase in dietary soy intake decrease risk of osteoporosis. (True)
Increase intake of broccoli decrease risk of osteoporosis. (True)
A 35 yo women get the prescription of 50,OOO/wk unit of vitamin D. What to do? talk
to doctor and dispense. (True)
protein diet like dietary are plant derived phyoestrogen present in soy
(True)
Drugs that cause osteoporosis: Corticosteroid, prednisone, levothyroxine.'(TriJe)
anticonvuJsants, phenytoin, heparin (long term use), and AI-containing antacid
(True) .
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Hypertension

Questions
Cardiovascular risk
Clinical praCtice guidelines of hypertension monitoring
Drug of choices to treat high blood pressure in patient with diabetes, renal, and
coronary artery disease, stroke patients.
Hypertension is defined as a systolic blood pressure >140 mm Hg, a diastolic blood pressure
>90 mm Hg. Diagnosis criteria from joint national committee (JNC-7) report recommendations
for follow up in adults:
<130/85 Recheck in 2 yrs
130-139/85-89 -7 Recheck in 1 yr
140-159/90-99 -7 Confirm within 2 months
160-179/100-109 -7 Evaluate or refer to source of care within 1 month
>/-180/110 -7 Evaluate or refer to source of care immediately or within 1 week depending
clinical evaluation
/
SphYgmomanometet
Maintain BP below
140/90 uncomplicated hypertension
140/90 with target organ damage or CV disease
Isolate systolic hypertension >140/<90
Diabetic or renal impairment <130/<80
<125/75 with proteinuria >1g/24 hrs
BP Measurement
Patient should avoid smoking or caffeine for 30 min
prior to BP measurement
Rest 5 min before BP measurement
Position arm (bronchial artery) at heart level
Uncover arm, do not put cuff over cloths
Position cuff 1 inch above antecubital crease
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Ask patient about previous reading. Inflate cuff rapidly ~ approximately 30 mm Hg above
previous readings.
Deflate cuff slowly, and completely. Measure pressure in both arms.
Wait 1 to 2 min before repeating, and take average of 2 reading. If second reading differ
by> 5 mm, additional reading should be performed.
Treatment
I ISl line therapy
I
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Thiazide ACE inhibitors
I
ARBs
I
Calcium Beta
>65 yrs
Channel Blockers
Blockers <65 yrs
Combining antihypertensive: Preferably combine from type 1 and type 2
Type 1 Type 2
ACE Inhibitors Thiazide
ARBs Beta blockers
Alpha blockers
Ksparing eCB
Thiazide Diuretics
Thiazide Diuretics -7 hydrochlorothiazide, chlorthalidone, indapamide, meta/azone and
combinations
MOA: Direct arteriole dilation, inhibit Na reabsorption in the distal tubule.
SE: HYPERGLUC
Increased lipid (cholesterol); increased LDL and increased TG.
Increased uric acid; Hyperuricemia
Increased glucose; Hyperglycemia (Mon: BSLJ
Increased ci+ = Hypercalcemia
Decreased K+ =Hypokalemia
Decreased Na, cr = metabolic alkalosis
Beta blockers (BBs)
non-selective BBs -7 Nadolol, propranolol, and timolol
Cardio selective BBs are -7 Esmeolol, Metaprc;>lol, atenolol, acebutolol (EMAA selective)
Cardioselective BBs with ISA -7 Atenolol, pindolol (non selective)
Beta and alphal blockers -7 labetalol and carvedilol
MOA:,j, Cardiac contractility -7 ,j, CO
,j, HR ~ ,j, CO
...L- central sympathetic output
85-2
www.l?hannacyprep.com .Hypertension
Block rennin secretion
SE: Increase LDL and TG
CI: Peripheral vascular diseases (Reynaud's and claudication), prinzmetal angina
(vaso.spastic aAgina)
DOC: stable angina, hypertension 65yr), post MI (STEMI), CHF edema) in
general avoid CHF because of bradycardia.
Beta blockers -7 DOC: stable angina, hypertension 65yr), post MI (STEMI), CHF
(pulmonary edema) in general. avoid CHF because of bradycardia.
Propranolol (Inderal LA) indicated for -7Social anxieties (stage fear) migraine prophylaxis,
and hyperthyroidism
Beta blockers precaution and CI-7 Peripheral vascular diseases (Reynaud's and
claudication), prinzmetal angina (vasospastic angina)
The most selective BBs that has been studied in lung dysfunction -7 Bisoprolol
Angiotensin converting enzyme inhibitors (ACE I)
ACE I-benazepril, captopril, cilazapril, enalapril, fosinopril, lisinopril, perindopril, quinapril, .
ramipril, trandolapril
MOA: Inhibit conversion of ACEI to ACEII thereby l' peripheral vasodilation
and -t fluid volume
SE: angioedema, dry cough treat by switching to other class of drug. It has NO effect on
LOL, TG and HDL, gives hyperkalemia (do not combine Ksparing)
CI: in pregnancy, initially increase serum Cr up to 30% is OK, if more discontinue ACE f
. MON: K+ level should.not exceed 5 mEq/mL
TU: BP, CHF, posts MI, diabetic nephropathy, (microalbuminurea > 1 g), intermittent
claudication': '.
Captopril and Iisinopril are NOT prodrug
ACEI -7 Inhibit conversion of AT
1
to'AT
2
thereby l' peripheral vasodilatation
and -t fluid volume
Captopril:7 Taken Q8H, All ACE I daily single dose, except captopril
Take on an empty stomach, lh a.c.
Enalapril -7 is 3 time more potent used once daily and NO sulfhydril group
/ Angiotensin receptor blockers (ARBs)
ARBs: Candesartan, eprosartan, irbesartan, losartan telmisartan, and valsartan
Direct Renin Inhibitors -7Aliskiren (Rasilez)
Alpha. blockers -7 doxazosin, prazosin and terazosin
Why is bedtime.the best time to dose terazosin? -7 syncope
Alpha. blockers -7 avoid with PDEs inh. (Sildenafil, vardenafil, tadalafil)
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Hypertension
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Calcium channel blockers (CCBs)
DHPs '7 am/odipine, feJodipine. nifedipine XL.
SE: Ankle edema, flushing, headache, and palpitation (reflex tachycardia)
NDHP ? diltiozem, veropomif
SE: Headache, dizziness, bradycardia, 2
nd
and 3
rd
degree heart block, new onset or
worsening of heart failure and constipation.
Amlodipine long acting DHP
Verapamil -7 SE: constipation and take with or after meals
FeJodipine -7 DOC Reynaud phenomenon
Non dihydropyridines -7 Additive effects with beta blockers (bradycardia), digoxin,
amiodarone,
Diltiazem -7 SE: stomach irritation Take Reg: before meals and SR: with or without
food
Dihydropyi'idines -7 SE: reflex tachycardia, headache and ankle edema
Alphaz agonist
Methyldopa and c10nidine
MOA: l' alpha2 action and .J, sympathetic outflow to heart
Methyldopa Drug of choice for pregnancy
Sf: hemolytic anemia Mon: CBC
TIf:E
1 Propranolol 2. Thiazide diuretics 3. Clonidine
4 Hydrochlorothiazide 5. Methyldopa 6. Triamterene
7 Captopril 8. Furosemide 9. Enalapril
10. Minoxidil 1I. Sodium Nitroprusside 12. Hydralazine
13. FeJodipine 14. Terazosin 15 losartan
16. BP >160/80 17. Ramipril
What is the recommended sodium intake for a patient diagnosed with hypertension?( <'/1'5 dldP.J-
The drug of choice against uncomplicated hypertension age over 65 yo is ( 2. )
The drug of choice against uncomplicated hypertension age less than 65 yo is (
The drug of choice for hypertension in pregnancy (,5" )
Use in non complicated hypertension and also indicated in opioids and benzodiazepine
withdrawal symptoms (3 )
Decrease BP in both supine & standing position, especially in elderly )
Diuretics that gives ototoxicity, hypokalemia, dehydration, allergy, nephritis and gout ( J
What drug turns urine into blue color ( b )
What antihypertensive drug should be taken 1 hour before meals rf )
85-4
www.pharmacyprep.com Hypertension
it is 3x more potent and used once daily and no sulfonil group

it is use for hypertension and alopecia treatment ( lo)
The drug of choice for hypertensive crisis (
It causes salt and water retention which may lead to CHF ( 1.2..)
The drug of choice for Reynaud phenomenon ( )
This drug may cause a sudden drop in blood pressure that can result in loss of
consciousness ( 11 )
Drugs may increase the effects of potassium supplements, potassium sparing diuretics,
cyclosporine, leading to raise of potassium in the blood ( 1,tj, f 7
Hypertension with diabetes drug of choice is -7 Ac
G
j
Hypertension with renal disease drug of choice is -7Ac.&.!.-
.' Isolated systolic hypertension which drugs should not use-7 1-J,!6d<.tvv
Car-dio selective ,beta blockers are -7 , .
The most beta 1 selective blockers that has been studied in lung dysfunction; -7 :8,.5
6
p
Name the cation most prevalent in the extracellular fluid of the body.-7 Nq
Why is bedtime the best time to dose terazosin?-7 +-0 aV01d
It is an antihypertensive drug which is also used prophylaxis migraine ( I )
Select True/False Statements .

A customer of your pharmacy checked two times blood pressure in your pharmacy blood
pressure monitor and found to have average 190/95. What is appropriate to do? talk to him
first and refer to doctor
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86
Coronary Artery Diseases
Questions Alerts!
Examples of coronary artery diseases
Risk factors and investigations ICK-MB, Troponin-r, ECG)
Treatment of NSTEMI (Non ST segment elevated MIl: A5A, 88
Treatment of STEMI (ST segment elevated MIl: Alteplase, ASA
Blood dot

1'f;-=t7Coronary arteries
__Zone l:Neausis
14,+-<tZone2; Injury
-----. Ze.r,e. 3: Isd'teml:l
Myocardfallnfurclion(MI)
Fat deposits
(plaque)
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Types of angina
Stable/Exercise induced angina Prinzmetal/Varian/ Vasospastic Unstable/Crusendo angina
Due to coronary partial blood angina
clot Acute with platelet aggregations.
-I, coronary blood flow. Due to non-occlusive thrombus in
-J, ST segment (subendothelial) an area of coronary ,
l' ST segment (transmural) atherosclerosis / or disrupted
Due to vasospasm effect of TXA
2
plaques
Definition: Angina is those symptoms of myocardial ischemia that occur when myocardial
oxygen availability is insufficient to meet myocardial oxygen demand.
Symptoms: discomfort or pain in the chest, arm, shoulder, back or jaw. Frequently worsened
by physical exertion or emotional stress.
Stable angina
Caused O
2
supply due to blood flow
Symptoms: Pain located over sternum and may radiate to left shoulder or arm, right arm
or neck, or jaw. Duration 0.5 to 30 min
Patient description of symptoms: pressure or heavy weight on chest, burning, tightness,
deep, suffocating, squeezing, aching, and crushing.
Precipitating factors: exercise, cold weather, sexual activity and emotional stress.
Approximately 75% of ischemic episodes are silent and not detected especially in
diabetes.
Symptom's occurring for weeks without worsening consider stable angina.
Usually relieved by rest or nitroglycerin SL.
Tx: NTG-SL, -7 All BBs, or NTG-LA or CCBs, -7 ASA, or c1opidogrel, -7 ACEI (in OM)
Prinzmetal angina (vasospastic)
Caused by spasm, do not increase MVO
z
Mainly due to atherosclerosis
Symptoms: pain usually occurs at rest awakens from sleep
Characterized by recurrent, prolong attacks of severe ischemia
/- Tx: NTG-SL -7 CCBs (nifedipine, amlodipine)
Acute coronary syndrome (ACS), term describes the symptoms that may lead
to acute myocardial infarction (acute MI). Acute MI further ,characterized as STEMI and'
NSTEMI and as weil as unstable angina.
Diagnosis:
- Chest pain: generally lasting for >30 min
ECG: ST segment elevation
86-2
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NSTEMI
STEMI
Tips
UA: Unstable angina, STEMI: ST segment elevated myocardial infarction, NSTEMI: Non ST segmented elevated
Myocardial infarction, GPI; Glycoprotein llb/llla receptor antagonists
I Acute Coronary Syodrome (ACS) I
Cardiac isoenzymes: CK-MB elevated and cardiac troponin T or t elevated.
Patient presentation: diaphoresis (sweating), nausea, vomiting, weakness, and shortness
of breath, arm tingling, and syncope. May confuse as heartburn symptoms.
Caused by: Disruption of an atherosclerotic plaque or formation of platelet aggregation

thrombus.
Symptoms: Crushing fhest pain that can radiafe to neck, back, shoulders, arms and jaw.
Pain is similar to angina but r:nore severe. May occur at rest and may be caused by less
exertions.
Pain is NOT relieved by NTG
Diagnosis: Chest pain is NOT relieved by NTG and persist longer than Smin.
Treatment: MONA therapy: Morphine Oxygen Nitrates ASA; BBs without ISA or
CCBs -7 Heparin or LMWH
The most common type MI (85%) is due to thrombus formation caused by precipitated by
atherosclerosis plaque rupture. This propagated thrombus leads to occlusive thrombus.
The complete blockade due to occlusive thrombus results in persistent ischemia that
clinically manifest as STEML If this is not treated, occlusion of coronary arteries can lead to
sudden cardiac death.
Symptoms: similar to UA!NSTEMI, however it is common in women, elderly, and OM.
1. Nitroetycerin 2. Amlodioine 3. ea channel blockers
4. Nitrates 5. Nitrites INa Nitro russideJ 6. A5A
7. Heparin 8. Dihydropyridine 9. Clopidogrel
10 LDl:> 2.2 11 Beta blockers 12 Thrombolytics
13 Diltiazem 14 verapamH
,
NSTEMI: Partial blockade of coronary blood flow STEMI Completely occlusive thrombus
Involves only subendocardial myocardium Effect entire thickness of myocardial wall. Cause
ST depression or NO ST elevation on EeG necrosis
Positive: CK-MB and Troponin-I ST elevation on ECG
Tx: Antiplatelets (A$A orland c1opidogrel and GPls More damage
are used
,
Positive: CK-MB and Trapanin I
Tx: Thrombolytic (Alteplase) or angioplasty .
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86-3
PhannacyPrep.Com
These drugs may cause hypotensi<?n with sildenafil ( I )
The drug of choice for hypertensive crisis '( 5' )
This can be safely used by astlunatic and non-insulin dependent diabetics (.3)
It is effective for acute and chronic angina ( r' )
These are the treatment of choice in patients with coronary arterial spasm (1,4,)( ,II,
It is use for STEMI treatment (ST-segment elevation MI) (' 1- )
It is use for NSTEMI treatment (Non ST-segment elevation MI) ( , )
It acts on peripheral vascular system that causes reflex tachycardia ('b .)
It is appropriate drug for'those who cannot take ASA (-3 ) .
Symptoms of stable angina -7 pC4.l h I etbu.c.J', , PCJ" -h rszAt
The drug of choice for stable angina -7 (If )
Prinzmetal angina is due to -7
The drug ofchoice for prinzmetal angina is -7
Neutropenia is side effect of -7 +, c lop,'dikl.
A patient is intolerant or allergic ASA, should get alternate drug of prophylaxis for vascular
diseases -7 0 h.. -hd 6f',cbiM-
Nitroglycerin act as smooth muscle vascular dilator due to -7 N c oX,dIz... CNo)
Venous pooling effect is caused by -7 4
Nitroglycerin storage conditions -7
The drug of choice for STEMI -7 ,.2. dQ.)J.... noJJ t')
What are the examples of LMWH -7 G 111 o>ld.pau'" I '1IGf I 6' I
Mechanism action ofLMWH -7 Blocks bflS"\Xl -?(A-
What laboratory test is used for monitoring LMWH -7 L"DLA-..
Headache is side effect of -7 I', 13
Protamine sulphate is antagonist of heparin, which react bY-7
. WW- PC<J,,\ O<:..CtuJ
Select True or False statements:
Symptom of coronary artery diseases? chest pain, sweating, shortness of breath (True)
IV dosage of form of nitroglycerin is the fastest acting or have rapid onset of action?
(True)
Nitroglycerin onset of iv ( 1 to 2 min), SL ( 1 to 5 min), oral (40 min), ointment (20- to 60),
I patch ( 40 to 60) (True)
Alteplase is least likely used after myocardial infarction after 6 hr of acute attack? (True)
Nitroglycerin SL spray is used to relieve angina symptoms (True)
nitroglycerin SL spray should spray on or unger the tongue(True)
nitroglycerin SL spray should store at room temperature(True)
nitroglycerin SL spray do NOT require shaking before use(True)
86-4
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nitroglycerin SL spray relieve angina symptoms(True)
nitroglycerin iv is faster acting than nitroglycerin SL (True)
LMWH have predictable response thus no monitoring required(True)
Heparin is the drug choice anticoagulant in pregnancy(True)
Warfarin is monitored by PT and INR(True)
warfarin should not be taken with vitamin K supplements(True)
Protamine sulphate is antidote ofheparin(True)
With isoniazid take vitB6, with levodopa avoid vitamin 86, with warfarin avoid vit. K.
(True)
Isotretinoin and tretinoin avoid vitamin A because analogs of v i l a l ~ i n A and Phenytoin &
methotrexate take folic acid(True)
Coumarin derivatives anticoagulants is used as rat poisoning? (True)
Angina, MI, transient ischemic stroke medical conditions are associated with ischemia.
Omega 3 polyunsaturated fatty acids are abundant in fish oils? (True)
Ecosapentanoic acid (EPA) and docosahexanoic acid (DHA) are derived from Omega
3(True)
86-5
Stroke
Stroke
Questions
of stroke: dizziness, headache, confusion, blurred vision, fainting
Stroke risk factors: coronary artery disease, DVT; high cholesterol, age
Transient Ischemic attack: ASA
Acute stroke therapy: G1lteplase or anticoagulant
Thrombolytic inclusion and exclusion criteria
lYpes of strokes
Break In blood
vessel In braIn
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.;.":.,:;.:......:;,s....
Cereb1-al
hepl,$"rrt1age
1
Plaque or blood dot
breaks aWi!1 and flows
to brain where it
blocks an arteD'
Stroke symptoms: Headache, dizziness, blurred,vision, confusion, and incoherent
speech.
Pharmacotherapy:
Anti-platelets: ASA, Clopidogrel, Ticlopidine, DipyridamolejA5A
DOC: 2
nd
prevention of Noncardioembolic ischemic strokes
ASA - initial tnerapy (50 -':'325mgjday for prevention)
Clopidogrel- 7Smg/daily, alternative agent, somewhat more effective < ASA alone
Avoid grapefruit juice
I
87-1
A$A + Clopidogrel; should NOT be used for long-term secondary prevention of ischemic
events (fbleeding)
Ticlopidine ; 2S0mg bid. SE: diarrhea, skin rash neutropenia need monitoring). Not
routine use
Dipyridamole SR/ASA; 2oo/25g bid, J., risk of stroke (mostly for ischemic stroke)
Stroke
I. Headache 2. Dizziness 3. Blurred vision
4. Confusion 5. Incoherent soeech 6. Warfarin
7. ASA 8. CloDido.rel 9. TicJooidine
10. Alteplase II. BP> 140/90 12. LDL> 2.6 mmollL
13. Seizure
Symptoms of stroke ( 1,2,g,S", r , DU' IS''''''''''' VIoI<",
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Anticoagulants; Warfarin, nicoumalone
DOC: 2
nd
prevention of Cardioembolic ischemic strokes prevent cerebral and systemic
emboli in patients with acute MI, valvular and nonvalvular AF and prosthetic cardiac
valves. Nonvalvular AF and prior riA/stroke require INR of 3.0 instead of 2.5
Warfarin: LNR 2 to mechanica I heart
valves)
-
INR35 & NO significant bleeding: lower dose or omit dose and monitor
INR>S to <9 & NO bleeding: skip dose
INR>5 to <9 & bleeding: skip dose & give VK orally Smg)
INR>9 &NO bleeding: hold WF &give high dose of VK orally
INR>9 & bleeding: hold WF g give VK
Tips
Tips format 002' Stroke
What is the initial symptoms of stroke (. I

What are the drugs of choice for long term prevention of atherothrombotic events (7
I ASA /. I;; L<l>L > fvo,>v-oi!L
Risk factors for stroke (II, If 2- 13 P >- II () l' I
What is the drug of choice for transient ischemic attack (TIA) (..,) A-5A
What is the initial therapy for stroke prevention (1) As 4 ".1.....cJ -J.., 1. .10 J..<
Combination of drugs increases the risk of bleeding ( 6, "r,t,3, 1. MA, (...,.1 ",AI
What drug gives neutropenia infrequently but is serious and require
monitoring ofCBC(everylto2wks)(.9) d.J
What is recommended routine protection of stroke. (j 1,c.LrpJ J -,
What drug cerebral and systemic emboli in patient with acute MI (.() /rS) l,A../
Drugs that are used in within 3 hrs of acute ischemic stroke (/0) .tH 1'e1>'gL-
What is nota stroke symptoms. (/3 )
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87-2
Stroke
/
Dizziness and head ache are the initial symptoms of stroke. (True)
Pathophysiologic of cer.ebral ischemia are associat.ed with carotid atherosclerosis
that can' result into stroke. (True)
ASA is the drug of choice for transient ischemic attack (TIA)? (True)
Migra.ine headache is least documented risk factor of stroke? (True)
Thrombolytics like alteplase should be used within 3 hours of
is not a symptoms of stroke? (True)
87-3
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88
Congestive Heart Failure
Questions Alerts!
CHF symptoms: dyspnea, edema, weight gain
(HF Treatment: ACE Inn. furosemide, digoxin
Digoxin mechanism: + inotropic, -ve chronotropic and vagomimetic
Digitalis toxicity: quinidine, thiazides, loop, erythromycin, tetracycline, verapamil
Digoxin (l's: ventricular arrhythmias
Digitalis toxicity symptoms: severe nausea vomiting, anorexia, muscular weakness, bradycardia,
and ventricular premature contractions. Severe toxic symptoms include: blurred vision,
disorientation, diarrhea, ventricular tachycardia, AV blockade which progress to ventricular
fibrillation.
Symptoms: Typical symptom of CHF include dyspnea, fatigue and fluid retention.
The primary manifestation of heart failure are dyspnea and fatigue that may limit exercise
tolerance, and fluid retention the may lead to pulmonary or peripheral edema. Other
symptoms may include paroxysmal nocturnal dyspnea, orthopnea (shortness of breath that
prevents lying down), tachypnea (rapid breathing). cough, ascites and nocturia.
Other symptoms include jugular venous distention, hepatojugular reflux, hepatomegaly
(enlarged liver), bibasilar rales, pleural effusion (increase in fluid in pleural surfaces),
tachycardia, pallor (pale skin) and S3 gallop. Symptoms of advanced heart failure are the
same but more severe.
Causes of CHF: In 65% of patients coronary artery disease is the cause of heart failure, other
causes include nonischemic cardiomyopathy example hypertension, thyroid disease or
valvular disease. These patients usually have reduced left ventricular dysfunction; usually
ejection fraction is <40%.
Nearly 20 to 50% of patient with heart failure is secondary to diastolic dysfunction. This is
ohen seen in elderly.
Diagnostic tests
The echocardiogram is one of the most useful diagnostic tests in CHF.
88-1
PharmacyPrep.Com
. B-type natriuretic peptide (BNP) is often acute care at emergencies. The test is useful in
differentiating CHF exacerbations and other causes of dyspnea such capo, asthma or
infections. Patient dyspnea secondary to CHF will have elevated plasma BNP
concentrations.
left ventricular ejection fraction <40% is indicates systolic dysfunction
J co ---.. +BP ... tRenal Blood Flow --...
/ tAngiotensin II
CHF !
tVenous t Aldosterone
pssu
t Capillary --.... _1 EDEMA , ........ ......---t NalH
2
0 retension
, Filtration
Pharmacotherapy:
Diuretics (hydrochlorothiazide, metolazone, furosemide, bumetanide, and ethacrinic acid,
spironolactone)
MOA: Na/H
2
0 retention by inhibiting reabsorption of Na in loop of henle
SE: hypotension, hypokalemia and hypo magnesia
01: Take empty stomach, food bioavailability
ACE Inhibitors (captopril, enalapril, Iisinopril, ramipril, and trandopril)
MOA: Inhibit potent vasoconstrictor ACE II, reduce mortality 20 to30%, l' CO, and,
HR
TU: all patient with left ventricular systolic dysfunction should receive.
0: Pregnancy, and lactation
ARBs (Candesartan, and valsartan): Same as ACE I
Beta blockers (Bisoprolol and carvedilol)
MOA: antagonize sympathetic activity. Negative inotropic effect is a disadvantage.
/. Therapy: Bisoprolol and metaprolol b
l
selective and car'vedilol a al, a2 and b
l
receptor
inhibitor are effective
CCBs: Only dihydropyridine CCBs are used
Digoxin
Does not improve mortality only produces symptomatic relief.
MOA: Inhibits Na+K+ATPase pump. l' +ve inotropic effect, and vagomimetic effect.'
SE: bradycardia, cardiac arrhythmias, and heart blockade
88-2
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01: verapamil, "erythromycin, and hyp.okalemic drug
loop and thiazides gives.digitalis toxicity
CCBs (amlodipine, felodipine)
Verapamil and diltiazem are not used because -ve inotropic effect
Vasodilators (hydralazine, isosorbide dinitrate, nitroglycerine, and nitropruside
Inotropic agents (digoxin, milrinone, and dobutamine)
Tips
I. DiQoxin 2. Di.ifab 3. LOOD diuretics
4. Cantonril 5. Vcraoamil 6 Thiazides
7. Dyspnea., fatigue 8. Impaired left ventricular (LV) 9. Fluid retention
function and reduce LV reserve
10 11 Edema
Symptoms of congestive heart failure (1, I,)
Characterized as congestive heart failure ( '? )
Inilial CHF symptoms include (7 )
What is the common type CHF characterized by decreased pump function, dilatation of LV,
and decreased LV ejection fraction ( 10 )
What is the most widely used cardiac glycoside (I )
What drug should be avoided in ventricular arrhythmias ( I )
What it is the antidote for digoxin toxicity (2. )
What dnlgs that increase digoxin levels (3.s.);
Decrease NalH
2
0 retention by inhibiting reabsorption ofNa in loop of henIe (3)
What drugs has the most common side effect of this drug is cough (J,)-
Drugs that decrease K levels (3.')
to +ve inotropic agents i.
-ve inotropic agents -7 fl- hl6c.ktYt-
The drug of choice for CHF-7
The drug of choice for CHF -7 A-CC:l ,3 4-i.
"" l.<>J' I s f-4- C. II-/" l M! aIL CA-.:D
Select True or Farse Statements
Symptoms of left ventricular heart failure cause pulmonary edema (True)
Symptoms of right ventricular heart failure cause -7peripheral edema
Weight loss is NOT a symptoms of congestive heart failure? (True)
ACEI, furosemide, and digoxin are the drug of choice for CHF? (True)
A patient while discharging from hospital emergency doctor has prescribed atenolol and
ramipril. Patients comes to home and calls your pharmacy to know he was using digoxin
88-3

. : .
before hospital admission. If he should continue digoxin or discontinue. Pharmacist calling
doctor is better response. (True) . .,
In the above patient scenario, medication reconciliation, could have prevent this
conf.usion?
Academic detailing educational programs conducted by pharmacy with doctor to enhance
prescription practices. Medication reconciliation is counselling to patient at the point of
hospital admittance and discharge. ISMP gather information about medication incidents.
Advanced legal directives = a type "will" that describes in the event if patient is in coma or
dead. (True)
Beta blockers are NOT a positive inotropic drug? (True)
Digoxin, beta agonist and phosphodiesterase inhibitors
88-4
Symptoms: it is mainly related to poor cardiac output i.e dizziness, syncope, chest pain,
fatigue, comfusion and exacerbation of heart failure.
Tachyarrhythmias: May have palpitation
Atrial fibrillation/flutter: May experience signs and symptoms of transient ischemic
attack or stroke.
Ventricular tachycardia and ventricular fibrillation: May be asymptomatic.
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Questions Alerts!
Mechanism of Class la, Ib, Ie, II, and 111 drugs
Examples of Clas's la, Ib, Ie, II, and III drugs
Treatment of atrial fibrillation and atrial flutter
Amiodarone SEs and Monitoring
. ,
Antiarrhythmic drugs
89
Arrhythmias
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Supraventricular (atrial) SVA Ventricular arrhythmias (VA)
Premarure atrial contraction Premature Ventricular Contraction (PVC)
Atrial flutter Ventricular tachycardia (VT)
Atrial fibrillation Ventricular fibrillation (VF)
Paroxysmal supraventricular tachycardia (PSVT)
Sinus tachycardia
Sinus bradycardia
89-1
. . ,
Antiarrhythmic drugs
Supraventricular (iltrial) .SVA treatment: Rate control drugs
Cardiac glycoside (digoxin), Beta blockers (propranalol, atenolol, metoprolol,
nadolol), CCBs (verapamil and diltiazem), Antiarrhythmic. class I C: flecainide,
propafenone; Antiarrhythmic Class III: Sotalol, Amiodarone, and dofetilide
Ventricular tachycardia treatment:
Class IA(Quinidine, procainamide); Class IB (mexiletine); Class IC (flecainide,
propafenone); Class III (sotalol, Amiodarone); Beta blockers (metoprolol)
Antiarrhythmic Drugs Classification
I
I
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I I
I
Class I Class II Class nI
Ia-Na+ channel
13-blockers
K+ channel
Class IV
Ca
2
+channel
blockers Esmolol inhibitors
Quinidine Propranolol Amiodarone
blockers
Procainamide Timolol Bretylium
Verapamil
Dis.opyramide Atenolol Dofet iI ide
Diltiazem
Metoprolol Sotolol
Nifedipine
Miscellaneous
Ib: Lidocaine
Nadolol
Adenosine
Mexiletine Magnesium
Tocainide
Ie: Flecainide
Propafenone
Class la drugs are Na+channel blocker slows phase 0 depolarization (Qunidine)
Class Ib drugs are Na+ h n n e ~ blocker shortens phase 3 repolarization (Lidocaine)
Class Ic Na+ channel blocker significantly slow phase 0 depolarization (Flecainide)
Class II beta blockers decrease phase' 4 depolarization (Beta blockers)
Class III K+ channel blockers prolong phase 3 repolarization '(Amiodarone)
Class IV Ca
2
+channel shortens action potential (verapamil and diltiazem)
Quinidine
Mechanism
/ Therapeutic use
Drug-Drug
interaction
Binds to sodium activated channels, Inhibits ectopic arrhythmias, VA
Atrial, AVjunctional, and ventricular tachycardia.
Maintain sinus rhythm after direct atrial flutter or fibrillation.
Antihypertensive, Anticoagulant - Quinidine may increase the.effects of
these drugs.
Phenobarbital and.Phenytoin - reduce the effect of quinidine
Digoxin-Quinidine increases the effects of digoxin (decrease 50%
digoxin dose).
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"An'tiarrhythinic drugs
SA and AV block or asystole, nausea, vomiting, diarrhea (cinchonism-
large doses-blurred vision, tinnitus, headache, disorientation and
psychosis. Torsos De pointes (VA)
Toxic level-induce ventricular tachycardia.
Increases steady state cone. Ofdigoxin by displacing PPB
Amiodarone is structurally related to thyroxine, and it contains iodine.

DOC antiarrhythmic & recommended in more severe LVD & ifCI with I
BB
TV Amiodarone is effective in tenninating VT, more so in preventing
recurrence
Most effective for in electrical stonn
Usually used as an empiric therapy
Respiratory: Pulmonary, including intererstitial pneumonitis; Respiratory
muscle impairment
01: nausea, anorexia, constipation; hepatitis and cirrhosis;
Hypothyroidism; hyperthyroidism; Amiodarone inhibit peripheral
conversion ofT4 to T3
Blue skin color (pigmentation), corneal deposits, hepatic toxicity, optic
neuritis, erectile dysfunction, photophobia
Avoid exposure to sunlight, use sunscreen and grapefruit juice
Atrial arrhythmias
Ventricular fibrillation and hypokalemic patients
. *May be taken \yith or without food
*Meals wI bran fiber, antacids may reduce amt ofdrug absorbed
Store bet:weenI 5-25 deg, C. in a tight container and protect from
light
Procainamide
Binds to sodium activated channels
Chronic use: lupus like syndrome (25-30%), toxic levels-asystole or
induction of VA.
GI intolerance is less than quinidine.
eNS: depression, hallucinations and psychosis.
Amiodarone
Digoxin
Therapeutic use
Contraindicated
Counseling
Side Effects
Side effects (4P)
Therapeutic use
Mechanism
Side Effects
Counseling
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Tips
Find answers from the table:
1. Quinidine 2. Amiodarone
3. Propranolol 4. Lidocaine
5. Procainamide 6. KChannel blockers
7. phase 1 to 3 8. Phase 3
drugs
89-4
/
Slows phase 0 depolarization ( 1,5)
What class drugs prolong phase 3 repolarization (increase refractory period) ( 2,3, 'f>
What drugs is used to treat related arrhythmias ( 2 )
Competitively block catecholamine induced stimulation of beta receptor thereby
suppress phase IV depolarization (,3 )
Chronic use of this drug may cause lupus like syndrome( I, P
When taking this medication grapefruit juice should be avoided ( 9.. )
Drugs that cause QT prolongation (torse des pointes) ( , , 2, /11 5"
What phases of action potential curve have no effect of stimuli ( 7' )
What is relative refractory period is ( 3 ) f: " o_il' CMa-r I )
Phase I action potential is 40 (+ve) due to deft' q}{1
What drug causes QT prolongation (torse des ((,,)2
Digoxin is contraindicated in what type of o,..,vv-O' "
Class la drugs act on '1 .... W&-/ I O.
Proarrhythmic drugs are A-rn f.r/IJ PTW2./ 1<+ el.a k
la Quinidine, procainamide Slows phase 0 depolarization
disopyramide
Ib Lidocaine Shortens phase 3 repolarization (shortens duration of refractory
period)"
Ic Flecanide,. propafenone Significantly slow phase 0 depolarization (slow conduction)
II Propranolol Decrease phase 4 depolarization (beta 1 blocker action)
III Amiodarone and sotalol Prolong phase 3 repolarization (increase refractory period)
IV Verapamil Shortens action potential (increase refractory period AV node)
Amiodorone side effects are: Photosensitive reactions, skin pigmentation, blurred
vision, pulmonary toxicity, and pneumonitis. (True/False) dVl-
'8 Qh.Lj#,fv)J(:U
. D'1
i -:)
PR -::J '
-, J
P tfuv-e. i ccltt -;J
Fig 90.1
90-1
90
Peripheral Vascular Diseases
...-..d"l ............. _
Deep vein thrombosis symptoms and treatment
Reynaud's phenomenon treatment
Drug should avoid in peripheral vascular disorders:, BB, Ergot alkaloids
_.....-
--
Questions Alerts!
Peripheral Vascular Disorders
Peripheral vascular disease occurs in arteries and veins of periphery, other than heart and
brain.
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Peripheral V. Diseases
IPeripheral Vascular Diseases
I
. Disease of Veins
Disease ofArteries
Venous blood clots
Arterial blockage
Pulmonary embolism
Aortic aneurysms
Phlebitis
Buerger's disease
Varicose veins
Reynaud's phenomenon
Intermittent claudication
Deep vein thrombosis (DVT) is obstruction of vein by blood clot. l.t is m'ost common witllin the
deep veins of calf muscles of the leg. The affected leg may become swollen and tender. The
main risk is that the clot may become detached and give rise to pulmonary embolism.
Regular exercise of leg and anticoagulant therapy are used for prevention and treatment.
Treatment -7 LMWH (enoxaparin, dalteparin, tinzaparin, nadrop'arin), specific factor Xa
inhibitors (fondaparinaux) and unfractionated heparin (heparin) and warfarin
Prophylaxis Graduated compression stockings and intermittent pneumatic compression
devices, Caval interruption by filters
Drugs (LMWH & UFH)
Treatment
LMWH
For treatment of established DVT and/or PE start oral warfarin together with sc
LMWH, or iv illIF.
LMWH or UHF is continued for minimum of5 days or until the INR is
therapeutic for at least 2 days. The duration of oral anticoagulant is dependent
on the risk of recurrence ofVTE. .
In most analysis of treatment ofVTE, LMWH use has typically more effective
and less costly overall compared to unfractionated heparin.
During UFH is the anticoagulant of choice during pregnancy. Injection sc twice a day
Pregnancy to achieve the therapeutic levels. Warfarin or UFH may be used for about 6
weeks after delivery for secondary prevention.
I Arterial Thra:n
boembolism
Acute
therapy
Chr.onic
therapy
Heparinized (80 ulkg) followed by thromboembolectomy (thrombolytic
treatment in all patients)
Warfarin (maintain INR 2-3 for cardiac source; 2.5-3.5 for prosthetic
mechanical valve). If the risk of recurrence high (e.g. cardiac source,
significant vascular disease or abnormality of coagulation cascade) we can
consider ASA in combination with warfarin
90-2 --'"
lntennittcnt claudication is a cramping pain, induced by exercise and relieved by rest, that is
caused by inadequate ,supply. of blood to the affected muscles. It is most often seen in the calf
and leg arteries. The pulses are absent and feet may be cold.
Combination ofglycoprotein Db/HIa receptor inhibitors with thrombolytic
therapy may improve outcomes for arterial thrombosis
IrrtermiIlent ClaucfICalion (Fig90.1)
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Ramipril Ramipril demonstrated similar effects in patients with or without PAD.
Contraindicati Beta blockers (TC page 3747 Use cautiously in sever disease with
ons hypertension). .
Rheologic modifiers pentoxifyline
Reynaud's phenomenon is a'condition in which arteries of the fingers become spastic
(vasospastic). This may result from atherosclerosi's, connective tissue disease, ingestion of
ergot alkaloids, or frequent use of vibrating tools.
NonMPharrnacological Choices: Minimize cold exposure, and use warm gloves
Therapy: CCBs (nifedipine, felodipine, amlodipine) and dilliazem
Alpha bleeker 7'pra,zocin
PGh analog iloprost
Peripheral vasodilator may relieve this condition.
CI: "Avoid prescribing medications with vasoconstrictive potential: ergot derivatives,.methyl
sergide and betaMblockers.
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AntiplalclclS
agent's
Clopidogrel
ACE
inhibitors
CCBof
dihydropyri
dine
PGI,
Antipiatelets agents reduce vascular death in high-risk patients about 25%
and are equally effective in those with coronary artery disease and PAD.
Clopidogrel may be more effective than ASA in patients with PVD but is
. .
usually reserved for those who cannot tolerate ASA or continue to have
events while on ASA
ACE I reduce the risk of ischemic events beyond that expected from
lowering blood pressure in patients with (PAD).
Medication taken daily (as opposed to PRN) during the winter will increase
tolerance to side effects (headache).
DOC isCCBs
ofdihydropyridine class (e.g. XL 30 mg or fclodipine 5 to 10
mg) should be used 60 minutes before cold exposure.
i.v. iloprost (PGh analog) may be useful for short term use; oral iloprost is less
90-3
www.PharmacyPrep.Com Peripheral Vascular Diseases
.
analog
CI
TIpS
effective
Erg6t:alkaloids, Methysergide and Beta blockers?
Find answers from the table
l. Smoking 2. Obesity 3. Increase age
..
4. Immobility S. Severe pain in legs 6. Pale finger tips
7. Effects extremities 8. plaques 9. iv heparin
10 sc LMWH 11 Warfarin 12 fondaparinux
13 Embolism 14 Pulmonary embolism 15
What is the drug of choice in Reynaud's phenomenon --7
What is the pharmacotherapy for deep vein thrombosis --7
Intermittent claudication symptoms --7
5
Reynaud's phenomenon symptoms -7 b
Risk factors of venous thrombosis (

Symptoms of deep vein thrombosis (S )
Symptoms of Reynaud's phenomenon ( b )
What is not a cause of Reynaud's phenomenon ( <6 )
What is the initial treatment of established DVT or PE ( " )
What is the first of a new class of antithrombotic agents, the specific factor Xa inhibitors. ( 12
)
R
..I l,el\l?lNW16h CIQ.\l' :
Examplesofvasculardiseases--7!i>Vt, p t
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Symptoms of deep vein thrombosis --7 5
ceo (&1 Ih"fd,+rr""J
What drugs should be avoided in Reynaud's phenomenon --7 J3-bl6-<keM
I Select True or False Statements:
LMWH is the most important drug is used to prevent peripheral vascular diseases?
(True/False)
Anticoagulants like warfarin is commonly used to treat acute peripheral embolic disorders.
(True/False)
Beta blocker are least likely used to treat peripheral vascular diseases? (True/False)
90-4
beta blocker cause vascular constriction thus it is contraindicated in peripheral vascular
diseases (True/False)
Reynaud phenomenon symptoms occurs in limb extremities (True/False)
calcium channel blockers are the drug of choice (True/False)
Reynaud phenomenon can be trigger cold exposure (True/False)
Reynaud phenomenon is may occur in old age (True/False)
arterial plaques is risk factor intermittent claudication (True/False)
estrogen/progesterone have risk of blood clots in peripheral vascular system(True/False)
lMWHs like enoxaparin, dalteparin, tinzaparin, and nadroparin are approved for both
prophylaxis and treatment of venous thromboembolism (VTE) (True/
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Anticoagulants
Questions Alerts!
Intrinsic (01972)and extrinsic Blood clot factors
Warfarin, e p r i n ~ and LMWH mechanism
Warfarin Dis and Monitoring
Dabigatron (Pradox) Faundoperinaux mechanism: Factor Xa inhibitors
MOA Increase rate of thrombin (lIa) and lMWH preps are insufficient length to catalytic
antithrombin (factor Xa) reaction at least a 1000 inhibition of thrombin produce an anticoagulation
fold by serving as catalytic template to which effect mainly through inhibition of Xa by
both inhibitor + protease bind antithrombin. (anti thrombin Xa activity)
PK tl/2 depends on amount. Heparin has immediate longer tl./
2
than heparin (takes 4 hours for action)
action when iv. (within minutes), SC takes 1 to 2
hours Once or twice daily SC
Q8 to 12h dosage
Dose is based on body weight Absorbed more uniformly
Monitoring apn No monitoring (predictable response)
Antidote Protamine sulfate Protamine sulfate
./
Bioavailability 20% 90%
Pregnancy yes Yes
Side effects Bleeding is more comrpon Bleeding is less common. HIT is less common
Heparin induced thrombocytopenia (HIT)
91-1
l. Heparin 2. iv & sc
3. Protamine Sulfate 4. Warfarin
5. lMWH 6. Vit K
7. Enoxaparin 8. A5A
9. Alteplase
What drug interacts with warfarin because of its antiplatelets action f3')
The major thrombolytic drug for DVT and pulmonary embolisml1)
Drug catalyzes the factor (thrombin activation factor) 2a, 9a, lOa, 11a, 12a,&13a ( I I
Drug used to prevention of OVT or PE, NSTEMI and unstable angina (1s'1
it acts longer and do not require close blood monitoring tsT
What anticoagulant used to prevent blood clots, mainly in areas where blood flow is
peripheral (4)
PT & INR should be monitored when taking this drug (,,)
it is the antidote for warfarin (6 I
What it is the safest anticoagulant used in pregnancy ( I l
What it is the antidote for heparin and it act by neutralization ( ) '3
/,Jeut
CVv
'1 ",e.cJ,.cu...,,,,, '1> ''1 9 I;I(V),
c: <t Its .5J -oJ +he-
CI<>#t'd -+0 t-t,e. s/fe.. "t O'1d
Clo+H1- f J1 Huz.. ,
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Mucopolysaccharide
Tip'>
Find answers from the table:
Fractionated mucopolysaccharide
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91-2
Anxiety Disorders
Anxiety
Questions
Antidepressants mechanism and DI with MAOI
Benzodiazepine classifications (intermediate acting BZDs daily) for max 2 to 4 wks
Anxiety is a normal response to fear, threat, or psychological stress and is
experiencE!d occasionally byevery one..
Anxiety disorder involves a state of distressing chronic but fluctuating nervousness
I that is inappropriate in certain circumstances.
Anxiety disorder can be categorized into several types, such as panic attack, social
anxiety disorder, social phobia, obsessivecompulsive disorder, generalized anxiety
disorder etc.
Panic attack and panic attack with or without agoraphobia
Panic is acute, short lived; extreme anxiety with some physical symptoms. This could
occur any anxiety disorder person with any specific situations. For example, a person
with phobic of snake maylpanic when encounter with snake.
Patient may actively avoid situations in which panic attacks are predicted tQ occur
Lntolerance of physical wmptoms of
Social anxiety disorder (SAD) and (or) social
Excessive or. unrealistic fear of social o'r performance situatJons
IntSllerance of embarrassmeQt or scrutiny by others
Specific phobia '
Excessive or unreasonal:>le fear of a circumsc(ibed object or situation usually
associated with avoidance of the feared object (for example, an aniinai, blood,
injections, heights, storms, driving, flying, or enclosed places).
Obsessive compulsive disorder (OeD)
Presence of obsessions; recurrent, unwanted, and intrusive thoughts, 'images, or
urges that cause marked anxiety (for example, thoughts about contamination,
doubts about actions, distressing religious, aggressive, or sexual thoughts)
92-1
Reference:
i-Can J Psychiatry, Vol Sl, Suppl2, July 2006
2-The Merck Manual of medical information
3- Treatment choices are modified from data from Compendium of Pharmaceuticals and
Specialties 2006
Tips
Anxiety PO SAD OCD GAD PTSD
disorders
SSRls
Fluoxetine (Prozac) Y
Fluvoxamine (luvox)
y
Paroxetine (Paxil)
y y y y y
Paroxetine (Paxil CR)
y y y
Sertraline (Zoloh)
y y
Dual action antidepressant
Venlafaxine (Effexor XR) Y Y Y
Azapirones
Buspirone (Bu5par) y
5HTto agonist
Benzodiazepines y
Propranolol Y(stage ear)
www.Pharrnacyprep.com
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Anxiety Disorders
Compulsions; repetitive behaviors or mental acts that are performed to reduce the
,
anxiety by the obsessions (for example, checking, washing, counting, or
repeating)
Generalized anxiety (GAD)
Uncontrollable and excessive worry occurring days not, about a number
of everyday, ord inary experiences or activities. Often accompanied by physical
symptoms (for example, headaches or\Jpset stomach)
Intolerance of uncertainty.
Post traumatic stress disorder (PTSD)
Occurs after a traumatic event to which patient responds with intense fear,
helplessness, or horror; patients relive the event in memory, avoid reminders of the
event, and experience emotional numbing and symptoms of increased arousal
Intolerance of experiencing trauma
Find answers from the table'
1 Benzodiazepines 2. Flumazenil 3 Fluoxetine
4 Sertraline s. Paroxetine (PaxiJ) 6 Ftuvoxamine
7 Venlafaxine 8 Paroxetine (PaxiJ CR) 9 Buspirone
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What are minor tranquilizers used to treat insomnia and anxiety ( I

What it is the antidote for benzodiazepine (2.J
92-2
Anxieo/
/
What drugs that are use for Obsessive-Compulsive Disorder (OCD) ( 3,4, y)b
What drugs that are use for Post Traumatic Stress Disorder (PTSD) ( )
What drugs that are use for Generalized Anxiety Disorder (GAD) ( S" )
What drugs that are use for Social Anxiety Disorder (SAD) & social phobia (.5,1)
Paroxetine is indicated for -7 C)Cj) OrA--&> SA-(])
_ I L. , f r. . , ,
Obsession is -7 MC'v-fl f
Compulsion is -7 /l.41e!>+'VL
92-3
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Depression
93
Depression
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Questions Alerts!
Antidepressants mechanism and
DIs with MADI gives serotonin syndrome
SSRI discontinued symptoms and serotonin syndrome
Dual acting antidepressants like venlafaxine. bupropion, mirtazepine
MAOI drugs interactions with sympathomimetics and antidepressants
SE's of TCAs like amitryptiline
Depression is a feeling of intense sadness; it may follow a recent loss or other sad event
but is out of proportion to that event and persists beyond an appropriate length of time.
Signs and symptoms: sadness, tearfulness,_dejection, self-criticism, loss of ability to
experience pleasure, loss of appetite, inability to sleep and loss of libido.
Depression can be categorized into: Major depression, and bipolar depression
SSRls - Fluoxetine (PROZAC), Sertraline (lOLOFT), Paroxetine (PAXll), Citalopram
(CElEXA), Escitalopram (C1PRALEXI, Fluvoxamine (Luvox).
SE: sexual dysfunction, GI, CNS
Discontinuation: taper slowly over four to 6 weeks.(particularly important for
Paroxetine and ventafaxine)
e Fluoxetine - can use in children & adolescents & pregnancy SE: insomnia, potent
CYP2D6 inhibitor
Sertraline -least 01, Take with food, breastfeeding, SE : diarrhea
Citalopram - least 01, breastfeed patient
e Paroxetine - breast-feed
e. Escitalopram: isomer of citalopram
SNRls - Venlafaxine
SE: BPt(lf dose >225 mgJday)
93-1
. ,
Dual action: Bupropion, mirtazepine, trazadone
Bupropion: NE&DA reuptake inhibitor
DOC: depression & smoking cessation
CI: anorexia or bulimia nervosa, head trauma or prior seizure.
SE: insomnia, sexual dysfunction (low r ~ t e
Depression
.: 1
Mirtazepine act on NE (directly) & serotonin (indirectly), alpha2 anta?onist
SE: sadation, weight gain (GI & sexual dysfunction is less)
Trazadone: SHT2 antagonist with some serotonin reuptake inhibitory properties
Excessive sadation (300 to 400mg daily) ~ s a hypnotic (SO-lOOmg)
With other antidepressants
SE: drowsiness, priapism
TCAs: Desipramine, Nortriptyline, Amitriptyline, Imipramine, Clomipramine, Doxepin,
Trimipramine
2
nd
or 3
rd
line agent
SE: Anticholinergic
C1omipramine- obsessive-compulsive disorder
Amitriptyline - chronic pain
Nortriptyline - elderly' depressed patients
Tetracyclic antidepressants - Maprotiline
Higher risk of seizures than the others
MAOls;
Reversible: Moclobemide
Dietary precautions are NOT required at standard doses
SE: nausea, insomnia (persist)
DI: Avoid sympathomimetics (pseudoephedrin.e, ephedrine), meperidine.
Caution with opioids, antihypertensives, antipsychotics, SSRls,
selegiline, excessive tyramine, alcohol. Reduce dose with cimetidine.
Irreversible: Phenelzine, Tranylcypromine
Reserved for the treatment of resistant depression
Food and drug cautions must be followed during treatment and for 2 weeks
After the last dose of the MAOI
01: Sympathomimetics may l' BP
Meperidine may cause agitation, hyperpyrexia, circulatory collapse
SSRls, TCAs, levodopa may l' effects and side effects
Tyramine containing food may cause hypertensive crisis.
93-2
Tips
Serotonin syndrome occurs with the following agents:
All SSRIs Miztazapine
Venlafaxin Moclobemide
The syndrome is possible when these agents are combined with:
-each other
-MAO!s
-lithium, meperidine, pentazocine, and dextromcthorphan
Fatigue, nausea, dizziness, and lightheadcdness, tremors"chills, insomnia, anxiety and
diaphoresis are the most common cffects of abrupt discontinuation ofSSRls,
Symptoms of serotonin syndrome are:
-increased muscle tone, tremor, jerks -sweating
-diarrhea -elevaled.temperature
-fever -agitation
-'shivering -increased blood pressure
Treatment: Symptoms resolve..quickly as soon as drug is discontinued.
Pharmacist has to contact the physician and tell the patient to withhold the serotonergic
agent.
Depression
Drugs selectively blocks the prejunctional neuronal reuptake pumps in the eNS ( ) 10
What is the most anticholinergic and sedative TCA { ).3
What drug is used to treat depression with insomnia, what is therapy ( )7
What antidepressant requires S weeks washout period ( ) 15
1. Phenelzine
.
2. MOclobemide
3. Mirtazepine 4. Venlafaxine
5. Bupropion 6. lithium
7. 'Trazodone 8. Fluoxetine
Amitriptyfine 10. SSRI

11 TCAs 12. MAOlnh.
Washout period
Generally there is no need for a washout period, and a crossover technique can be _1..... ,
applied (i.e., tapering one agent while titrating the other). I tLe...1;ol1 t:r'C.bIC:1
jixception ;u..,...v..., 0<1
Irreversible MAO] (phenelzine/tranylcypromine)......) other antidepressants: 2 weeks
Moclobemide --+ other antidepressants: 5days
Fluoxetine --+ ill irreversible MAOI: 5weeks
Caution: when starting other antidepressants after fluoxctine discontinuation.
Find answers from the table'
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93-3
{
www.PhannacyPrep.Com Depression
_/
--
(
Antidepressant also used for smoking cessation ( ) 5 ,
What drug is used to treat depression in sexual dysfunction, what is the best therapy

. An example of an irreversible non selective MAO )
it is the only reversible & seledive inhibitor: of MAO that is cpr.r:ently. available( )
Drugs,acts directly on noradrenergic system & has low rate of GI and sexual side
effects but is associated with sedation and weight gain (.! )
Antidepressant also use for generalized anxiety (GAD) (<b)
Its is used in prophilactically in treating manic-depressive patient, treat manic
episodes & bipolar depression (6 )
What drug serum level should not exceed 1.5 mEq/L (6)
SSRI onset of action is -7 -h l, LJe.e( <.
Fluoxetine washout period -7 5"
Drug of choice in depression with sexual dysfunction -7 2.,3,5
Depression with insomnia -7 r - " ,. ,.. 1.L
TeA M4CJ du...f..t, -t? (J
Depression with diabetes 7 ,A.VO'l
Depression with diabetes, the drug of choice for major depression-7 fo
Higher dose of venlafaxine (225mg/day) have effect on -7 51+"f a "14 N c:
A on antidepressants and shows with dilated pupil, may be due to-7
TCA onset of action is -7 2 -h.3
A substance found commonly in fermented foods which can be toxic when MAO
inhibitors are used7
MAO is classified as -7
SSRI like fluoxetine inhibit cytochrome CYP2D6 (True/False)
Mirtazepine may cause higher weight gain (True/False)
Avoid cheese with 7 12.-
Milk + MAOI 7 No AtAc.;H
o
t1
St. John wort has antidepressant effect (True/False) I. J .. _ .. 1-"
j
rt11 h.;w",fvu,' 6'1
Serotonergic symptoms-7 fJIZ-VVl/ 1 """llSc.1 _. / <:7
1
The drug of choice against bipolar disorders and manic depression -->
Lithium toxicity symptoms --> I, I., UJ , t, I
What antidepressant is used as pharmacotherapy for smoking cessation -7 ..!5
Paroxetine therapeutic use --> 4
What antidepressants are NOT used to treat Q,ulemia and anorexia nervosa -- -7 .5
Select TRUE OR FALSE Statements :,_ ," PI e;huo
SS R't. J,D, du r llD'k -'--
Buprapion, trazadone and mirtazepine have feast sexual dysfunction (True/False)
Take SSRI in the morning and TCAs in evening or bedtime (True/False)
Normal blood levels of lithium in adult should not exceed is 1.5 mEq!L (T/F)
93-4
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It conc. increases with decrease Na" and It conc. decreases with Increase in Nat-
(T/F)
ACE I, NSAID, Thiazides, decreased renal perfusion -7 increase li toxicity
Fluoxetine (SSRI), dehydration and renal dysfunction increase It toxicity(T!F)
93-5
Phannacyprep.com
Antipsychotic Drugs
.'
Anti Psyc otic D.rugs
Symptoms: The schizophrenic individual is out of touch with reality, hallucinates, hears
voices and exhibits bizarre behaviour. These symptoms are only one aspect of
schizophrenia,. Other symptoms are: social withdrawal, and an inability to communicate
or to concentrate.
s motoms symptoms
Negative Cognitive Positive
symptoms
Positive Symptoms Negative Symptoms
Reality distortions: Delusions persecution
Grandiosity, thought broadcasting, hought
insertion, Loose associations, Gestures,
Mind-reading, and Being controlled
Blunted affect: Lack of expressed emotion,
Poor eye contact and inattentiveness, and
Reduced spontaneity
Hallucinations: Auditory (most common)
Olfactory, Somatic, and Visual
Alogia: Lack of spontaneity of conversation
and poor ability to concentrate
Disorganizations: Disorganized speech
Incoherent speech, Tangentiality and Loose
association
Avolation/apathy: Lack of interest in
activities, No motivation, social withdrawal
and Poor hygiene.
Disorganized behavior: Agitation, Hostility
Assaultiveness, Uncooperativeness,
Inappropriate sexual/social behavior,
Inappropriate dress and Catatonia
Anhedonia: Loss of pleasure and Few
recreational activates
Attentional impairment: Lack of ability to
concentrate on tasks or conversation
Treatment: 1
st
& 2
nd
genereration Treatment: 2
nd
generation
Copyright 2000-20 II TIPS Inc. Unauthorized reproduction of this manual is strictly prohibited and 94-1
conducted by PhaimacyPrep.
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Antipsychotics side effects are associated extrapyramidal symptoms: Parkinsons like
symptoms (tremors), akthisia (motor restlessness), tardive dyskinesia (inappropriate
postures of neck, trunk and limbs).
Parkinson's symptoms include: T =Tremor, R= Rigidity, A =Akithisia, P =Postural
instability
1
st
gen (haloperidol, loxapine, chlorpromazine, thioridazineJ is effective in positive
schizophrenic symptoms. However, 2
nd
gen (dozapine, risperidone, olanzapine,
quetiapine) covers negative schizophrenic5ymptoms. Olanzapine, not effective for
the treatment of resistance, and resperidon works for negative and positive
symptoms.
Orthostatic hypotension is SE of -7 2
nd
generation antipsychotics (can cause additive
effects with other antihypertensive drugs)
Copyright <:I 2000-2011 TIPS Inc. Unauthorizcd reproduction of this manual is strictly prohibited and 94.2
it is illegal to reproduce without pemission. This manual is being used during review sessions
Phannacyprep.com
. .
1
nd
-generation Antipsychotics
low potency
Chlorpromazine - SE : QTc prolongation
Methotrinieprazine
Antipsychotic Drugs
/
Intermediate potency
Loxapine, Perphenazine
Zuclopenthixol.-injectable FGA, long T1/2, Do not use in antipsychotic-naive patients
High potency
Fluphenazine, Flupenthixol .
Halop'eridol: with Lorazepam im for acute phase. SE:' QTc prolongation
Pimozide; SE : QT
c
prolongation with dose> 8mg/day (avoid use with sertraline)
Thiothixene and Trifluoperazine.
2
nd
-generation Antipsychotics (SGAs)
Advantage in first-episode psychosis, in improving negative symptoms, mood and
cognitive deficits and in preventing relapse and rehospitalization.
First-line treatment
Depression in the acute phase: effectivity SGAs>FGAs
SE: tglucose abnormalities
Clozapine: only antipsychotic with proven efficacy in treatment-resistant schizophrenia
Not first-line (Sf: agranulocytosis, need for regular blood monitoring)
MOA: Inhibit D, SHT, HI, M and Q
SE: Weight gain (greatest), hyperlipidemia, agranulocytosis> (1%), increase risk of
diabetes, dyslipidemja, orthostatic hypotension, and high weight gain
TU: Drug of choice in resistance psychosis, -ve and +ve symptoms
MON: CBC q week,
Risperioone - SE: hyperprofactinemia (dose-related). EPS
Risperidone-tabs oral disintegrating - do not split
Sf: hyperprolactenemia
OJanzapine - SE: Weight gain (greatest), hyperlipidemia, EPS (especially akathisia)
Use for acute phase.: do not combine with parenteral BDZs
(cardiac & respiratory problems)
Olanzapine- orally disintegrating May stir into 125 mL of water, milk, coffee, orange
juice or apple juice consume immediately.
Approved for acute treatment of mania
SE: no hyperprolactenemia
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".
Tips
akathisia if dose reduction is not P-blockers (e.g., propranolol 10 to 120
mgfday); anticholinergics are ineffective
dystonia torticollis or oculogyric crisis) -). 1M benztropine or diphenhydramine
. (acute), followed by reduction in dose or switch to SGA
Quetiapine - SE: Increase risk of diabetes, hyperlipidemia (iTG), and J. thyroi.s hormone
levels
Antipsychotic Drugs Pharrnacyprep.com
Comparison of antipsychotic drug side effects'
Neuroleptic malignant symptoms: Fever, muscle rigidity, Autonomic disturbance,
fluctuation in BP, Tachycardia, elevated WBC, and CK.
DOC for NMS: dantrolene, or bromocriptine
Extrapyramidal side effects
(EPS; dystonia, parkinsonism, akathisia, tardive dyskinesia, tardive dystonia)
Management: Prevention -use SGAs first-line
if EPS occurs, first reduce dose; consider switch to SGA if on FGA; anticholinergics
(benztropine, procyclidine and trihexyphenidyl) should NOT be used prophylactically
even with FGAs, and should usually only be used on a short-term basis to treat
parkinsonism associated with FGAs; anticholinergics are generally not recommended
with SGAs
In gen (haloperidol, loxapine, chlorpromazine, thioridazine) is effective in positive
schizophrenic symptoms. However, 2
nd
gen (clozapine, risperidone, olanzapine,
quetiapine) covers negative schizophrenic symptoms. Olanzapine, not effective for
the treatment of resistance, and resperidon works for negative and positive
symptoms.
Orthostatic hypotension is SE of'" 2
nd
generation antipsychotics (can cause additive
effects with other antihypertensive drugs)
Mechanism of c10zapine 7 O
2
, 0., SHT, H
t
, M and,Q blockers
,
Typical (1" generation) Atypical (2
nc1
generation)
High sedation low sedation (respiradone)
low weight gain High weight gain (clozapine)
High tardive dyskinesis low tardive dyskinesia - c10zapine
High anticholinergic SE loY{ anticholinergic side effects
High Sexual Dysfuntion low sexual dysfuntion (quitiepine)
High EPS low EPS
"
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conducted by PhannacyPrcp.
\
I.
Pharrnacyprep.com Antipsychotic Drugs
Drug of choice for acute agitation in seniors-7 Quetiapine
1st generation 4 to 8 weeks no response, change to 2nd generation.
Severe case of psychosis (schizophrenia) or bipolar disorder -7 add mood stabilizers
(Valproic acid, carbamazepine)
For 1 episode of psychosis, continue for 1 to 2 yrs and for 2 episode, continue
treatment for 2 to 5 yrs
1. Zuclopenthixol 2. Haloperidol 3. Chlorpromazine

4. Risperidone 5. Clozapine 6. Olanzapine
7. High EPS 8. Tardive dyskinesia 9. Weight gain
10. Ag.ranulocytqsis 11. wac
1
st
generation 4 to 8 weeks no response, change to 2
nd
generation.
Severe case of psychosis (schizophrenia) or bipolar disorder -7 R It. i e.r'soJi.,
2
nd
gen (c1ozapine, olanzapine) increase risk of lipids and diabetes, EXCEPT:
Respiridone
Least extra pyramidal symptoms -7
Highest EPS -7
Patient experiencing hallucination -7
Patient experiencing social withdrawal -7
2
nd
generation covers-7 h . cJ" 4 I
Schizophrenia is characteriz:d by -7 _ U
Metoc!opramide -7 <J
Chlorpromazine -7 j I J _c
Tardive dyskinesia is caused by -7 P.5(f('jN:1'T'"V
TO symptoms -7
For resistance schizophrenia DOC,-7 d,.;'
Mechanism of c10zapine -7 ..0 2, ID4, Sfo+'f I ""' f I M Q" 11\,
Drug of choice for acute agitation in seniors-7 f.J..Jl:l1o..fl"
it is not use in antipsychotic-na'ive patients ( ) 1,5
it is the only antipsychotic with proven efficacy in treatment-resistant Schizphrenia ( S
)
the most widely used treatment for psychotic agitation (.1)
it is used in patients experiencing withdrawal
this can cause lupus like syndrome (3 )
this should not combine with parenteralbenzodiazepines ( (,)
highest extrapyrimid.al symptoms
WBC should be monitored because of high agranulocytosis (5)
act on dopamine & serotonin receptors almost equally ( ) '-7
. Alec.t.qU l4.J- tt.U4
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Drugs for Alzheimer's disease
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5-1
Symptoms: memory loss, disorientation, impaired executive functions, behavioural
distrubances, depression, psychotic disturbances, and inability to care for self.
Risk factors: Age, family history (genetic link), head injury, cardivascular risk
factors.
Tacrioc: Oldest drug, it is non selective and limited used because of its
hepatotoxicity.
Donepezil: Centrally active reversible, non competitive. It selective and have
greater affinity for AchE! in brain than periphery. Little or no hepatotoxicity.
Dementia
95
Dementia
I
Reversible
Acetylcholinesterase inhibitor
I
I I
Nonselective Sflective
IGalanthamine I
I
I Donepezil I
Rivastigmine
(relatively selective)
Severity of dementia:
Mild dementia:" forgetting daily activities: Example: taking medicines, tel. phone
number, finances, directions
Moderate: Forgetting personal activities: bathing, dressing, eating (remember upon
reminders)
Severe: Forgetting personal activities but C3flJ:lOt recall upon reminders.
Tenninal: Patient must be fed, immobile ~ mute
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www.PhannacyPrep.Com Dementia
Rivastigmine: is centrally selective arylcarbamate AchEI, it has short half life of
2hoUfS, but able to inhibit AchEI upto 10 hours. Because of slow dissociation of
carbamate 'enzyme it is referred as pseudo-irreversible AchE!.

/
Mechanism

Side effeCts
Dosage

Advantage

Drug and Drug

Interactions
Monitor

RivasD;)mine
Mechanism
Side effects
Therapeutic use
Dosage
Mechanism
Therapeutic use
Acetylcholinesterase inhibitor
GI effects Nausea, vomiting, diarrhea
CNS effects Fatigue / insomnia" headache
Other effects Muscle cramps, anorexia, difficulty in passing
urine
Daily one dose in the morning or evening
Initial: 5mg/day Target: 1Omg/day Adjust dose after 4 wk
Daily one dose
Toxicity may be t by inhibitors ofCYP2D6 or CYP3A4 (e.g.,
paroxetine erythromycin, prednisone, grapefruit juice,
nefazodone)
Effectiveness may be Lby inducers ofCYP2D6 or CYP3A4 (e.g.,
carbamazepine, phenytoin, rifampin)
Periodic checks may be performed to see benefit of drug
Selective acetylcholinesterase inhibitor
Weight loss due to reduced appetite
Nausea, abdominal pain
Depression, agitation, confusion
Drowsiness, dizziness
Weakness, trembling
Sweating, malaise
Convulsions (rare)
.. Effective in Lewy body dementia (TC page 35, 4
th
edition)
Treatment of Lewy body dementia. Avoid antipsychotics
Acute pain such as dysmenorrhea (painful periods)
For rivastigrnine, the initial dose is 1.5 mg PO BID, and can be
doubled to 3.0 mg PO BID after 30 days, which is the
minimum effective dose.
Effective in Alzheimer's and vascular dementia
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(
(
( www.PhannacyPrep.Com Dementia
I Donenezil 2 Rivastilmline
3 Galanthamine 4 Memantine
5 Tacrine 6: Mild dementia
7: moderate dementia 8: decrease Ach
Copyright 0 2000-2012 TIPS Inc. Unauthorized reproduction of this manual is strictly prohibited and
Tenninology
Dementia is a decline in mental ability that usually progresses slowly, in which
memory, thinking,judgrnent, and ability to pay attention and learn are impaired, and
personality may deteriorate.
Delirium: Acute mental disorder, with symptoms ofacute agitation. hallucination,
extreme excitement, and disorientation.
Delirium tremens: Acute psychosis caused by alcohol withdrawal.
Aphasia: Impaired ability to communicate
Amnesia: short time loss of memory
Dysarthia: difficulty ofspeech
Dosage
95-3
Nausea, vomiting, abdominal pain, diarrhea, indigestion,
decreased appetite and weight loss, headache. dizziness, tiredness,
sleepiness or sleeplessness, confusion, runny nose, urinary tract
infection, falls
16- 32 mg bid
it is non selective & limited use because of its hepatotoxicity( )
causes Alzheimer' dementia ('3 )
the drug of choice of Alzheimer' dementia (J )
elTective in Alzheimer's & vascular dementiae )
effective in Lewy body dementia
drug thai has anorexia side effect ( )
it is effective for patients with dementia associated with Parkinson's disease( )
N-methyl D-aspanale (NMDA) blocker
forgeting instrumental activities of daily living (phone #s, keys, driving direction,
finance) ( )
forgeting daily activities (bathing, feeding, dressing), recalls upon reminders. <r )
DOC for Alzheimers is
Alzheimers occurs due to
Donepezil and rivastigrnine and galatamine all have anorexia SE. # v--k V"'I
Delirium is 7 ,4",v-1:t. I Lc..",k "5- -J 4o/...yJM..J et- ' I or
Amnesia is-7 rfk.A:I- {crr.& 4 ,..,HVt')d.PcJ- +.
What are risk faclors for Alzheimers disease 7 4re ? /)aMI b ,:r
Levy body dementia 7 de.>v>""'/''' <.>Jf<, .... C (","""-c., ,
Galantamine is classified as -7 4+-h' cJ.....c{,"-.U't.L4:P-U2- I'" l, I b,""lCt"L
Side effects
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www.PhannacyPrep.Com Epilepsy
--
Epilepsy
Antiseizure drugs by mechanism of action
r
Reduces NMDA
Affect GABA Reduce Na+ Reduce Ca
2
+
Receptor acti vation
receptors conductance in current
hyperactive neurons through T-
chal1llels
I
*Felbamate
Phenobarbital
Primidone
Ethosuximide
I
Carbamazepine
Diazepam
Phenytoin
Vigabatrin
Fosphenytoin
Topiramate
Lamotrigine
Tiagabine
Gabapentine
Valproate
Pregabalin
Valproic acid
Simple
partial
,/
Partial Seizure
Comments
Seizures begin locally
Consciousness not impaired
With motor symptoms-7 Jerking, lip smacking,
chewing motions
With autonomic symptoms-7Sweating, pupil
dilation.
With behavioral symptoms
Drug of choice
1
51
Carbamazepine
2
nd
Phenytoin
3
rd
Primidone
4
th
Gabapentin
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-1
it is illegal to reproduce without pennission. This manual is being used during review sessions
, '
,
Benzodiazcpines (BDZs): Clobazam, Clonazcpam, Diazepam, Lorazepam, Nitrazeparn
Rapid onset, tolerance
Iminostilbene Derivatives: Carbamazcpine, Oxcarbazepine
Carbamazepinc: SEs. transient neutropenia may worsen absence (petit mal) seizures
Stevens Johnson syndrome
Oxcarbazepine: SEs: hyponatremia, skin rash with carbamazepine
NO aulO indllction of liver enzymes.
Tclearance of warfarin, Des, TeAs and risperidone
DOC for partial seizures, tonic clonic seizures, treat trigeminal neuralgia
Hydantoin Derivatives: Phenytoin
Available as: Phenytoin 100% suspension & chewable. Phenytoin sodium (capsule &
iv) are phenytoin 90% sodium 10%
SE: Skin rash, gingival byperplasia, and nystagmus
NOT effective for absence (PetitMal) seizures.
Phenytoin suspension and chewing tablets are 100% phenytoin
Gingival hyperplasia: Mouth hygiene and 0.15% chlorhexidine mouth rinse
Space 30 min before or after food
Swish and swirl1hen spit out.
Drug ofchoice:
I$l. Carbamazepine
2
nd
Phenytoin
3
rd
Phenobarbital
4
th
Valproic acid
Epilepsy
Seizure begin locally
With conscious impainnenl
Begin as simple
With or without automatism (automatism:
picking at cloths is common may follow visual,
auditory hallucinations)
Generalized seizures
True absence seizures (petit 10 to 30 seconds, causes alteration
of consciousness, starts with occasional blinking (Nystagmus)
Avoid Phenytoin and carbamazepine use in absence seizure
Sudden very brief involuntary jerking of facial, limb, and trunk
muscles or all body.
Tonic occurs in children, muscle stiffening (tone)
Clonic seizures = Sustained muscle contraction altering with
relaxation '
Sudden loss of -7 Consciousness, become rigid, falls to the ground....
last about I minute.
Single prolonged seizure lasting more than five minutes.
In some cases no regain ofconsciousness between attacks-DOC is iv
diazepam.
Absence
Complex
partial
seizures
(Petit mal)
Myoclonic
seizures
Tonic-clonic
seizure (grand
mal)
Status
epilepticus
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conducted by PharmaeyPrcp.
96-2
{
Regulatect: Can be once only
Destroying: Can be witness by: Pharmacist, Intern and
Inspector from a college of pharmacy
Tolerance to therapeutic effects.
Diazepam iv; used for status epilepticus
Succinimide Derivatives: Ethosuximide
For absence seizures only, few DI
Least teratogenicity
Epilepsy
/
GABA Derivatives: Gabapentin, Vigabatrin
SE: vision changes and tnnors, and visual changes,
Gabapentin: No DI, can use in liver failure, "add on"drug, TID dosing
Vigabatrin: few DI, can use in liver failure, worsen absence seizures
DI: No interaction with oral contraceptives
Safe in pregnancy. Not metabolized. Can be used in liver failure.
Gabpentin: Administration with Al/Mg, Ca antacid may lbioavailability.
Gabapentin: drug of choice to treat trigeminal neuralgia, diabetic neuropathy.
Vigabatrin: worsens absence seizure
Pregabalin: Post herpetic neurologia (PHN) and deiabetic neuropathy (DeP)
Barbiturates: Phenobarbital, Primidone
Used for generalized seizure
Tolerance is common
Phenobarbital- take at bedtime (long tin)
Primidone - metabolized to phenobarbital
Control Drug Substance and require sales reports
Carboxylic Acid Derivatives: Valproic acid, Divalproex
SE: teratogenicity, GI (Valproic acid> Divalproex). Very low incidence of rash
No .tOCs efficacy
DOC: mixed 1
0
generalized seizures (generalized tonic-clonic, myoclonus, absence)
PregnancY7 Neural tube defects
No interactions with oral contraceptives
Low incidence of rash, Steven Johnson's syndrome
Other Anticonvulsants - Lamotrigine, Levetiracetam, Topiramate
Lamotrigine - SE: insomnia, rash, no enzyme induction
Levetiracetam - No DI
Topiramate: SE: kidney stones, weight.t, cognitive (limit use), ! efficacy
ofOC'S, word fmding difficulties. ! efficacy ofOC'S, expensive
Also used as weight loss drug
Tips
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96-3
1Carbamazepine 2iv Diazepam
3 Phenytoin 4
5 Topiramate 6 Valproic acid
7 c10bazam 8 phenobarbital
9 RinRerva[ hvperplasia 10 steven ihonson syndrome
11 simple partial seizures 12 Generalised seizure
13 petit mal (absence) seizures 14 tonic clonic
15 Status epitepticu$
96-4
Epilepsy www.PhannacvPrep.Com
It has the least drug interaction With oral contraceptives ( ) 4,', I"
the drug of choice for status epilepticu5 (.2..)
it is use for partial seizures and tonic clonic seizures ('/3
it causes Steven Johnson syndrome side effect (1,t>;"
it is not effective in absence (petit mal) seizures ( I,).}
the drug of choice for trigeminal neuralgia ( IAt
it enhances GABA activity; antagonizes amino acid (.5)
the drug of choice for generalized seizure ( , I
it decrease the efficacy of oral contraceptives (I, )3,7
Carbamazepine interferes with thyroid function test. Ht1 6o)
Phenobarbital and phenytoin stimulates _> Hepc:...J-,c.. h1 IC/\()SlIli'o1e-J eMJ'lfM.i!J C
CarbamazepineisDOCfor--> TN';l"""""-! crn<l pO<Af,<-!
DOC for status epilepticus is --> .2.
Avoid phenytoin in --> 13
Phenytoin have --> eM> "A.JM. (5c.J-u,flk4) /<., "-""'U
Gingival hyperplacia associated with phenytoin is treated by mouth hygiene and
chlorohexidine mouth wash. )
ChJorhexidine is used for __>. <3-' i l"Hs, .5-f-o.....,c:..Ji+u-
Carbamazepine, phenytoin, cJonazepam -.> de.euz.c-u;. e../J!;7CJJ..
C
<:t e1fs fA{M
Gabapentin and valproic acid, Jamotrigine have no interaction with oral
contraceptives s+o&;4J

Gabapentinha,leasl-? VS'-II--I1 oef I.11...(I...f)
Phenytoin available a,-->. 5","""''<'1'" (Iooj,) hi (90-/'/ c.1..vve-/.... 0-"""
r I ) 4- /.
Carbamazepine available as -> CNz.tvo..-bl<..- I (,tt . ....
Clobazam has high c.1Z-
Gabapentin and lamotrigine
Xerostomia -? d.c.j """" 4-
Sialorrhea .sG.!;vC\
Vigabatrin + carbamazepine f,..!)t:J}J. eA1 o.b..sG6t1c.J!- sdJu,I.12A
A patient is on phenytoin but now dose is increased, when is the appropriate time to
measure steady :; -f-o:1 0 .:.
Phenytoin blood levels monitored for r 0 mC3 JM 1
list the monitoring parameters for phenytoin-7 N) Ll...) PI--J N
, I'A<- j<>J.cJ,., i d i CPJed {;YI- dl o..J.,ehc, f,l J' 'I-'
. u, ......tM'P"'- J..,o"<Z- 10'" roU 'If pefJll'VrJ,J
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IllS Illegal to reproduce wlIhout permission. This manual is being used during review sessions

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'Anti-Parkinson's Drugs
Parkinson Mechanism
, .
Parkinsons
RigidItY '
Symptoms: dysarthria, gait disorders, postural instability, cognitive
dysfunction.
Levodopa and Levodopajcarbidopa
Decarboxylase inhibitor: & used to
minimize acute side effects
Motor fluctuations & dyskinesia in up to 50% of
patients after 5 years
Slow-release preparation good for patients having
"wearing-o,ff" .
cognitive dysfunction poorly responsive to levodopa
therapy ."...
SE:D1'& V, orthostatic hypotension, dyskinesias,
hallucinations, confusion
Avoid VBs supplements Short shuffling steps
Copyright 2000-2012 TTPS Inc. Unauthorized reproduction of this manual is strictJy prohibited and 9i-1
it is illegal to reproduce without permission: This manual is being used during .
NMDA receptor antagonists: Amantadine
Improves l-dopainduced dyskinesia in the later stages of the disease
MOA: releasing dopamine from the presynaptic terminals or by blocking its reuptake
SE: leg edema, erythema, livedo reticularis
Caution: patients with cognitive deficits a (tconfusion)
MAO-B I: Selegiline, Rasigline
Good for the first year of treatment (very mild effects & don't delay the
development of dyskinesia or fluctuations associated with l-dopa therapy)
Potent: Rasagiline > SelegHine
SE: insomnia
Selegiline: may need J...dose in women taking OCs
Dopamine agonists: Bromocriptine, Pergalide, Pramlpexole, Ropinirole
Adjunctive therapy with levodopa good for an advanced Pts with motor
complications
Initial therapy in younger patients JOy) add levodopa if they need
SE: GI upset, orthostatic hypotension, psychiatric reactions (hallucinations and
confusion) > levodopa
Ergot dopamine agonists (pergalide & bromocriptine). SE: pulmonary fibrosis (chest
X-ray before initiating therapy), erythromelalgia, cardiac valve fibrosis (pergolide)
Non-ergot dopamine O
2
selective agonists (pramipexole & ropinirole). SE: sudden
sleep attacks, better choice than ergot dopamine agonists
bromocriptine: take with food
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Take empty stomach preferably
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Anticholinergic agents: Benztropine, Ethonopropaz;ne, Proeyclidine,
Trihexyphenidyl
Effect on tremor, bradykinesia (little or no effect)
Use as monotherapy or as adjuncts to dopaminergic therapy
Benztropine - take with food
(GMT Inhibitors: Enlaeapone
COMT (catechol-O-methyl transferase), an enzyme that helps metabolize ldopa, is
found in both the brain and in the peripheral nervous system
MOA: prevent peripheral metabolism of ldopa, which increases its availability to the
brain
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it is illegal to reproduce..without pennission. This manual is being used during review sessions .
SE: relate to t dopaminergic activity in the brain (dyskinesia,
confusion/hallucinations etc.)
J..30% dose of Ldopa with COMT inhibitor
Tolcapone; SE: hepatotoxicity (only through the Special Access Program, Health
Canada, for use in exceptional cases)
Entacapone; SE: diarrhea (often weeks to months after initiation), discoloration of
the urine, NO hepatotoxicity
lips
1 deficiency of dopamine 2 Amantadine
3 Entracapone 4 Levodopa
5 Selegiline 6 Tolcapone
7 levodopa/carbidopa 8 Bromocriptine
9 does not cross blood brain barrier 10 tardive dyskinesia
11 MAO- type Binhibitor 12
it is a non selective dopamine agonist (i)

it is converted to dopamine within presynaptic dopaminergic neurons (1)
it is indicated in Parkinson's disease and also for prevention and treatment )of
Influenza A viral infections ( 2-
it a selective MAO type B inhibitor (S )
it help prevent peripheral metabolism of levodopa, which increase its availability to
the brain (3, )1
PD is due to decrease in t bl J '1
Levodopa does penetrate into brain ( ) J 00.
Dopamine does not penetrate into brain ( )
Carbidopa not penetrate into brain ( ).. L
Dyskinesia-7
Metochlopramide an antiemetic drug should be avoided in PD patient
All antipsychotics require caution in PD
Levodopa/carbidopa is DOC in PD
Selegline is a selective MAO- type Binhibitor
Akinesia
Bradykinesia -->
Over treatment of Parkinsonism drugs can result into -7
Sciatic nerve: are found in all foot branches
Why do we add entracapone to levodopa in parkinson's
'0' c... a.pat1 DA..e- Co'4 -f lAY' /VL.
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, I
Protein Synthesis Aminoglycosidcs, Macrolides. Tetracycline's, Lincosamide
inhibitors
Cell Wall synthesis Penicillins. Cephalosporins. Vancomycin
inhibitors
Bcta-Lactamase Inhibitors
Clavulanate, Sulbactam and'Tazobactarn
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it is illcgal to reproduce without pcnnission. This manu31 is being used during rcvicw sessions
Ilntimicrobials
98
Antimicrobials
Penicillin G, Penicillin V. Methicillin, Nafcillin,Oxacillin
Carbenicillin, Ticarcillin. Piperacillin
Amoxicillin, Ampicillin
Cell wall synthesis inhibitors
Gram + ve and Gram -ve
Hypersensitive reactions.,-rash. nausea & vomiting,
Pseudomembranous CQlilis7 diarrhea
Intestinal nephritis
Hemolytic anemia (Coombs test)
Antibiotics classifications
DNA Synthesis QuinolonesIFluorOQuinQlones. Metronidazole
inhibitors
Folate Inhibitors Sulfonamides, Trimethoprin
C1avulanic acid
Beta-lactamase inhibitors such as c1avulanic acid can be combined with sensitive
Beta-Iactams to yield an active combination with resistant organisms
Penicillins
Aminopenicillins
Mechanism
Therapeutic uses
Side effects
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AntimiGrobials
Penicillins or all beta lactarns are NOT effective for
mycoplasma bacteria.
C b I epl a osponns
1S1-Eeneration Cefazolin Long duration of action in 1
st
gen. (Long acting)
None of them Cephalothin
enter in CNS. Cepbalexin Oral (DOC pharyngitis, cellulites)
Cephapirin Renal and hepatic elimination
Shortest half life (0.6 - 0.8 h)
Cephradine
Cefadroxin Oral
2.
illI
generation Cefaclor Oral (associated with serum sickness)
Cefarnandole
Cefoxitin
Cefuroxime sodium Can cross BBB, can be used in community
..
aquired bronchitis or pneumonia in elderly
Cefuroxime auxetil Oral, stable for 24 hours when dissolved in apple
juice
Cefotetan
Cefproxil Oral
Cefonicid
Loracarbef
J.m generation Cefixime Oral
Contain Cefoperazone Hepatic elimination only, does not get in CNS
methylthiotetraz Cefotaxime Renal and hepatic elimination. Can penetrate in
ole side chain.
CSF.
Can cause
Cefpodoxime
hypoprothromb
Ceftazidime
onemia and
Ceftriaxone Longest half life (8 hours) -7 Single dose, it has
bleeding
bile excretion.
problems
Cefdinir Oral
Ceftibuten Oral
1!!! generation Cefepime
/
Vancomycin
Mechanism
Therapeutic use
Side effects
Cell wall synthesis inhibitor
A.very important drug for treating methicillin-resistant
staphylococcus aureas infections (1v1RSA), and it is an
drug for treating superinfection (Superbug) by Clostridium
difficile in patients with P. colitis.
Narrow spectrum, active against Staphylococcus; Streptococcus
and Clostridium sp. (gram +ve bacteria)
Chills, Fever, Ototoxicity and nephrotoxicity
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Pharmacokinetics:
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Aminoglycosidcs
Gentamicin, Streptomycin, Tobramycin. Kanamycin, Amikacin
Pharmacokinetics
All aminoglyoosides rcoally eliminated
Half-life 2 to 4 hours.
Post dose antibiotic effect (PDAE)
Only kanamycin and neomycin have oral and topical usc.
Commonly aminoglycosides used as 1M or TV
Streptomycin has only 1M
Pharmacokinetics is not completely understood.
Contain aminosugars structures and have low bioavailablity
Primarily used in infections associated with gram negative organisms.
Aminoglycoside have little activity against anaerobic organisms.
Aminoglycoside summary
Side effects
A Allergy
M = neuroMascular Blockade
I = Inactivated when physically mixed with 13-lactams
N = Nephrotoxicity
0= Ototoxicity. Optic nerve toxicity
Halflife is 2 to 4 h, however parenteral injections are given every 6 to 12 hours.
Aminoglycoside have post antibiotic effect
Highest ototoxicity is observed with Streptomycin
Highest nephrotoxicity observed/experienced with Neomycin
Ototoxicity symptoms associated with gentamycin and streptomycin are: Vestibular
damage causing tinnitus, vertigo, and ataxia.
Ototoxicity symptoms associated with amikacin and kanamycin are: Auditory
damage which may lead to hearing loss.
Tobramycin can cause both and auditory damage
To prevent serious side effects associated with aminoglycosides monitor: Blood drug
levels, BUN, Serum creatinin levels
Blood levels are monitored by peak and trough levels: Trough levels ofgentamycin
greater than 2mcglml can cause nephrotoxicity.
Macrolidcs
Erythromycin. Clarithromycin, Azithromycin, and Telethromycin (ketolides)
Antimicrobials
Rapid administration causes red man syndrome (flushing)
In renal failure patient drug will accumulate (renal Toxicity)
IV and oral (oral use only to treat P. colitis)
Renal elimination
Halflife 6 '0 8 h
Precautions
Dosage
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Antimicrobials
All macrolides are hepatically eliminated, except: c1arithromycin, which is renally
eliminated.
All macrolides are administered orally except erythromycin gluceptate and
lactobionate which is administered by rv route.
Azithromycin has long half-life of68 hours and it is used as single daily doses.
Erythromycin has short half-life 1.2 to 2.6 hours.
Erythromycin is the preferred drug for the treatment of Mycoplasma infection.
Important alternative in patient allergic to penicillins
Erythromycin estolate may cause cholcstatic jaundice in-patient with prolonged
use of more than 10 to 14 days. (resolved after trealment is discontinued)
Erythromycin is inbibitor of CP3A4, lhereby potentiates toxicities of drugs that
are metabolized by CVP3A4, eg: digoxin, corticosteroids, lovastatin or (ALS), and
carbamazepine.
Clarithrornycin increase warfarin INR (monitor PT), increases digoxin and
theophylline levels.
Azithromycin is more active against gram negative H. influellza than erythromycin.
Clarithromycin is effective for H. pylori (used along with PPls in triple therapy)
Tetracycline's
Tetracvcline, demeclocycline, doxycvcline, and minocycline
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Tetracycline
TIlerapeutic Uses
Side Effects
Contraindication
Counselling
C1indamycin
Uses
Side Effects
Contraindication
Broad spectrum antibiotics
Acne treatment, Chlamydia (lymphogranuloma, Psittacosis)
Rickettsia (Rocky mountain spotted rever), Mycoplasma pneumonia
Lyme disease
Tetracyclines should not be given to renally impaired patient.
(accumulated increase azotemia).
Pregnancy, breast-feeding, children under 8 old,
Must be taken on empty stomach with glass of water. Binds with bi
and tri valent ions such as calcium, magnesium and aluminum ions.
Tetracycline may stain teeth and in topical application (uses)
Avoid prolong sun exposure.
Topical: Can continue use ofcosmetics.
Stinging may occurs and that may resolve shortly.
Tell patient to report continuous nausea, vomiting, yellowing of eye
and skin.
Lincosamides class ofdrug'
Gram +ve anaerobic bacteria Bacteroidfragilis (abdominal
infection)
Diarrhea (c. difficile is resistant to c1indamycin7treatment-
Treatment discontinue medication, and start vancomycin or
metronidazole (oral)
History ofcolitis, regional enteritis, or antibiotic associated
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it is illegal to reproduce wilhout permission. This manual is being used during review sessions
conducted by PhannacyPrep. .
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Antimicrobials
Quinolones & Fluoroquinoloncs
Quinolones Nalidixic acid (disinfectant)
Fluoroquinolones 1
st
gen: Nalidixic acid, Norfloxacin
2
nd
gcn: Ciprofloxacin, Oflaxacin
3
rd
(Respiratory tract quinolone): Gatifloxacin, Moxifloxacin (safe
in renal disease), Levofloxacin
4
th
Travoiloxacin
Mechanism of action: DNA gyrase inhibitor (topoisomerase II) and topoisomerase 1'v
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Counseling
Precaution
Ciprofloxacin
Mechanism
Therapeutic
Uses
Side Effects
Counseling
Auxiliary
labels
Phototoxicity
Metronidazole
Mechanism
Therapeulic use
colitis.
Take with qr without food (discourage with food)
Capsule: take with full glass (240 ml) of water to prevent
dysphagia.
Do not refrigerate the reconstituted solution since under
condition of low temp, the solution may thicken and difficult
to pour. Stable at room temp for 14 days.
LM injection may be painful
Inhibils DNA replication of bacterial DNAg (gyrase) or lopoisomerase
II and topoisomcrase IV
UTI ~ E coli
s'm ~ Gonorrhea
Respiratory ~ alternative to ampicillin in pneumonia
GJ infections ~ E.coli travellers diarrhea
Most common; nausea and vomiting, light-headedness nephrotoxicity
Cartilage toxicity. Avoid use in under 18years and pregnancy
Tendonitis/tendon rupture-eommon in elderly and renal failure patient.
Cipro otic suspension:
Slore cipro otic suspension at room temp (15 to 25C).
Do not use otic suspension under 2 year of age
With or without food. The preferred time is 2 hours after meal (for
faster absorption)
With full glass of water, (avoid dairy products), take calcium after two
hours.
Avoid taking with antacid, iron, or calcium together
Sunscreens may not be effective; drug should be disconlinued at the
first ofsign of toxicity-sun bum like rashes.
Classified as antiprotozoal drug and has antibiotic actions (anaerobic)
Mode ofaction is thought to be through breakage ofcell DNA.
Indicated in anaerobes such as Bac/eroides, C. difficile, C. vagillaUs
Protozoans (Giardia, En/amoeba, Trichomonas) - GET Metro
This drug is also active against trophozoites in the intestinal lumen
and walls.
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it is illegal to reproduce: without permission. This manual is being used during review sessions
. ,
Antimicrobials
Side effects
Drug-Drug
interaction
Precautions
Pregnancy and
lactations
Dosage
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Metronidazole has direct anti-inflammatory effect (antioxidant
action that contributes to its anti-inflammatory activity),
Giardiasis and trichomoniasis metronidazole used orally
Metallic taste, furred tongue, glossitis,
Must avoid taking alcohol while on this drug as it can cause
disulfiram like reactions.
Rarely neurotoxic.
Cimetidine - prolongs metTonidazole half-life and decrease its plasma
concentration
Warfarin: Potentiates effects resulting in prolongation of prothrombin
time.
Disulfiram: Causes acute psychosis even if taken within two weeks.
Phenobarbitone: Increases metronidazole metabolism
It can cause dark urine
Do not mix i.v metronidazole with any other drug.
Caution require in pregnancy and lactation
. Injectionto treat anaerobic infections and protozoal infection
Oral capsule, and tablets. Vaginal cream and inserts, vaginal gel: for
treatment of bacterial vaginitis
Topical cream or gel: drug of choice for rosacea twice daily morning
and evening for 9 weeks, then as needed.
Folate Sulfa drugs
(
Sulfa drugs
Combination: '
drugs
Mechanism
Therapeutic
Use
Side effects
Counseling
Sulfamethoxazole, Sulfadia,zine, Sulfisoxazole, Sulfasalazine
Trimethoprim
Cotrimoxazole
Folate antagonists
UTI E. coli
Drug of choice i'n traveller diarrhea
Trachoma-chlamydia trachoma-m.ost common cause of preventable
blindness.
Topical: burns and wounds
Crystalluria: adequate hydration and alkalinization prevent this
problem
Hypersensitivity: rashes, Stevens-Johnson syndrome-occurs with
longer acting agents: (diuretics, acetazolamide, thiazide; furosemide,
bumetanide, diazoxide).
Hemolytic anemia G6PD deficiency
Kernicterus:'newborns because sulfas displace bilirubin from binding
Sulfasalazine: drugs colors urine and may colo.r skin orange yellow.
May permanently stain soft lenses
Take drug after meals to reduce GI distress and to facilitate passage
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Antimicrobials
into intestine.
Chronic treatment of UTI
Gram -ve: H. influenza. Gonorrhea, E. coli, Klebsiella, Salmonella,
shigella sp. V. cholera. Gram +ve: S. pyogenes (GAS), S. viridans, S.
aurells
UTI-Acute, recurrent, chronic.
Upper and lower rasp-chronic bronchitis.
lmmullocompromised children: P. carinii
Not indicated in infections associated with pseudomonas, mycoplasma.
Skin reaction (severe in elderly)
GI --> N and V
Blood related: Megaloblastic anemia, Thrombocytopenia, Leukopenia:
The above three effects can be reversed by concurrent administration
of folinic acid. Hemolytic deficiency due to SMX
Drug is not for 1M injections. Shake oral suspension thoroughly before
use. Take oral dose with full glass of water. With or without food.
(food decreases Gf side effect). Store in amber glass ofbortle.
Store at room temp until expiry and protect from moisture.
Last trimester of Pregnancy, lactation.
Cl'ld d 2 I M k
Counseling
Cotrimoxazole (SMX + TMP)
Cotrimoxazole
Therapeutic
Use
Side effects
Contraindicatio
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it is illegal 10 reproduce without pennission. This manual is being used during review sessions
ns H ren un er mont 15. ay cause emlc erus
Drug of choice
Chlamydia Alithromycin, Doxycycline
trachomatis
Escherichia coli Cefazolin, Cephalexin, Cefotaxime, Ceftriaxone, Gentamicin, Tobramycin
Hemophilus infuenzae Augmentin, Cefotaxime, CeftizOlcime, Ceftriaxone, Azithromycin, Oarithromycin,
TMP-SMX, Oral3rd generation Cephalosporins
listeria Ampicillin, TMP-SMX
monocytogenes
Moraxel1a catarrhalis Augmentin, Azithromycin, C1arithromycin, TMP-SMX
Mycoplasma Azithromycin, Clarithromycin, Erythromycin, OproOoxacin
pneumoniae
.
Neisseria gonorrhoeae Ceftriaxone, Gprofloxacin, Gatifloxacin, Moxifloxacin, levofloxacin
Neisseria meningitidis Pencillin G
Pseudomonas Zosyn, Imipenem, Meropenem, Ceftazidime, Cefepime, Amikacin, Gentamycin,
a/ruginosa Tobrartlycin, Ciprofloxacin
Salmonella SOD ceftizoxime, Ceftriaxone, Gprofloxacin
Shigella spp Gprofloxacin, Gatifloxacin, levofloxacin ,
Staphvlococcus aureus Dicloxacillin, Nafcil1in, Oxacillin, Cefazolin, Cephalexin,
aureus Vancomycin
(Methitillin-resistantl- .
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MRSA
Staphylococcus Vancomycin +/- Rifampin
epidermidis
Streptococcus Ampicillin, AmoxiciUin, Penicillin Gor V
pyogenes IGroup AI
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www.PharmacyPrep.Com Antimicrobials
Streptococcus Ampicillin, Amoxicillin, Penicillin Gor V
pneumoniae
Streptococcus viridans Vancomycin, Unasyn, TImentin, Zosyn, fmipenem, Meropenem, Cefazolin,
Cephalexin, Ceftriaxone, Cefepime, Gatifloxacin, Levofloxacin, Moxifloxacin,
Clindamycin, TMP-SMX
Treponema pallidum Penicillin G
Syphilis
Helicobacter pylori Omeprazole 40 mg QD + clarithromycin 500 mg TID x 2 wks, then omeprazole 20
mg QD x 2 wks OR
Lansoprazole 30 mg BID + amoxicillin 1 g BID + c1arithromycin 500 mg TID x 10
days OR
.
OmeprazoJe 20 mg BID + c1arithromycin 500 mg BID + amoxicillin 1 g BID x 10 days
OR
TIpS
\ Steven-Johnson's Syndrome (SJS): Rash, skin peeling, and sores on the mucus
membrane. In Steven Johnson's syndrome, a person has.blisterjng of mucus membrane,
typically in mouth, eyes.and vagina. Patchy areas of rash. SJS can occur in all age groups.
Due to: SASPAN (Sulfonylurea, anticonvulsant (phenytoin, carbamazepine, valproic
acid), sulphonamide, penicillin, allopurinol and NSAIDs). Topical sulfadrugs are
contraindicated because it may cause disease like SJS, this disease is life threatening.
Treatment ofSJS is cortisone
Tips Cell wall synthesis inhibitors
1 Amoxicillin 2 Penicillins 3 Amoxicillin
4 Type 1 allergy 5 Type 2 allergy 6 Azithromycin
7 Minocycline 8 Clindamycin 9 Metronidazole
10 Doxycyclin 11 Ciprofloxacin 12 Cotrimoxazole
I
Methicillin is only IV and 1M

Penicillin G benzathine has long halfJife 7 24 '0I,.ud
Naficillin is mainly hepatic elimination
Beta lactamase sensitive drugs: Pen G, Amoxi, Pen V and Ampicillin (PA-PPr-)
Endocarditis prophylaxis is (Dental extraction prophylaxis) 7 I A-m6)l;C; J" Y\.--
A child less than 2 y allergic penicillin, what is the drug choice for otitis media ) I' JaTJ11 c.J
treatment.-7 g I IY a ow- "3 'd..t.AA.I , mq ,J-b ClU\ I"..L- c:.'''' <1
A patient has heart diseases and underwent prostatic valve surgery. Dentist plan to .
tooth antibiotic i.s suitable for endocarditis n 'Il;(lliJ'1 ..
ChewableantlblOtlcs.-7 t"vuJT ..,; .--
Beta lactams that should be taken empty stomach .-73, p..eMio' /", V if. e
Aminopenicillins are: L,"3 A-tv,8)c){.,'f'l1, /+Mp'l..III,,,,...L
Penicillin allergic patient, alternate drug of choice is? G - '""d-ell)
, ,
Macrolides Tips
0 2000-2012 TIPS Inc. Unauthorized reproduction orthis manual is strictly prohibited and 98.. 9
It IS Illegal to reproduce without permission. This manual is being used during review sessions
conducted by I'hannacyPrcp.
Antimicrobials www.PhannacyPrep.Com
Azithromycin suspension stored at 7 10\(.1""""
Clarithromycin suspension stored at 7 .
Which macrolide suspension have to refrigerate after reconstitution I
What antibiotics should caution and require monitoring in patient receiving warfarin .(2)
What antibiotic potentiate the effect of digoxin and can cause digitalis toxicity ',2, ve
Azithromycin is the drug ofchoice in traveler diarrhea for patient traveling to 1], c::U lC2l"'\ '1
T t r T
e raeye 10 IPS
,
I Tetracyclin 2 D6xycyclin 3 Minocvclin
4 Photosensitive 5 Must take emotv stomach 6CC/PC
7 Room temoerature 8 RefriRerator 9 H. influenza
10 Calcium supplements I I Dairy 12 Cotrimoxazole
'I Erythromycin'
, ,
2- Clarithromycin
,
3 Azithromvcin
4 TYpe J allergy 5 Type 2 allergy 6 Gastric upset
--
7 Room.temoeralure. 8 RefriQ.crator 9 H. influenza
10 Doxvcvclin 11 Ciorofloxacin 12 Cotrimoxazole
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.."l a,S(-.NC- L t< <Z:<=-I 0>
Penicillins are ineffective in treatment of bacterial infections associated with -7 Md-GeptGUM"1
MRSA infections are treated by Va Y'lGOW'tJ0'1
P.colilis associated diarrhea is treated by -7 Oa.-' val"ICDmJ.c.' "\
Bacteria is inhabitant in GI, what location ofGI tract is commonly found:7 C.O10'1
Typeofbacleria mainly present in colon is -7 qo
Penicillin hypersensitive reactions
If allergic penicillins the best alternate choice of antibiotics is macrolide.
Penicillins gives what type'hypersensitive reaction -7 Type I to V
Tetracyclin are contraindicated are contraindicated in pregnancy and children.
Tetnlcyclin can slain teeth causing discoloration.
Oral or topical tetracycline are drug ofchoice for acne treatment
Tetracyclin MUST BE taken on empty stomach. _ , )
B; d"J r,(J ...e..t"v-t- Cce-lou"", OA.. G-fllMIl'l!lI"'J
GI distress (abdominal discomfort, diarrhea) are most common SE. This can be
prevented by taking with food or decreasing dose. _ I _ '.l.-I
Expired tetracycline can lead RR,nc..l +-Jou-M.. IIeC.M.J<" lJ/l.- -r=<' C"-J
Doxycyclin is the DOC Ja.1o,.s I V)
Doxycyclin should be -) v......H.. t!JA-
Minocyclin maybe taken with or without food.
Photoloxic reactions (sever skin lesions) can develop with exposure to sunlight.
Pholoxicity is the most Commonside effect ofdoxycyclin or demeclocyclin.
Epimcrizal'ion is a -7
"""""""-ctracyclins = Take empty stomach
Doxycyclins = Take with or after food
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M!nocyclins = Regardless of food
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ID amyclD IPS
1 Clindamycin 2 Diarrhea 3 P. colitis
4 photosensitive 5 Must take empty stomach 6 CCIPC
7 Room temperanire . 8 Refrigerator 9 H. influenza
10 Calcium supplements 11 Dairy 12 Cotrimoxazofe
Most common complication of clindamycin is -7 t p. 'CD r,}t.-.c
Clindamycin is active against -7 ..Gh')1 -t-y(l. , ,..YL, a."d
Pseudomembranous colitis symptoms include: fever, abdominal pain, bloody stools. .-..1..
Clindamycin can cause -7 Ce..sDJ')6pJ,ifI
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, h6 "[J'" .J
drug associated diarrhea is treated bY-7 \/oV)0""':!10 tl Itz
Clindamyciri suspension can be stored at -7 7 +e-M At1ch1
Clindamycin should be taken -7 l,..J-f h-, .:f-
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dfl Quino one an urOQulDo one IPS
1 Ciprofloxacin 2 moxfloxacin 3 Nor floxacin
4 Photosensitive 5 Must take empty stomach 6 CCIPC
7 Room temperature 8 Refrigerator 9 UTI
10 Calcium supplements 11 Dairy 12 Cotrimoxazole
Fluroquinolones are indicated for UTI, Infectious diarrhea (Travellers diarrhea),
lower respiratory tract infections, bone and joint infections (osteomylitis).
Gatifloxacin, Moxifloxacin SE are -7 r f>O' -......-
FluroquinolonesContraindicated in children, under 18 y, pregnant women due to its-7 a:uh /a..spz-
Antacids, bivalent and trivalent ions significantly decrease absorption of -7 fJf O,u)
Fluroquinolone increase INR in patient receiving warfarin, therefore monitor -7 ... :
Fluroquinolones can cause hypo or hyperglycemia, therefore monitor -7 B6r '''1 a>M ntoot(ffJ
Fluroquinolones at higher alkaline pH can cause -7
Cipro is the drug of choice in -7 'r-}.J:4vall0l.- UT:L e>luc1
M d I T" etroDl azo e IPS
1 Metronidazole 2 Alcohol' 3 Trichomonas
4 Amoeba 5 Must take empty stomach 6 CCIPC
7 Room temperature 8 Refrigerator 9 anaerobic bacteria
10 Calcium supplements 11 Dairy 12 Disulfiram like reaction
/
Alcohol with metronidazole can cause -7 [) i.su.1.fJ'}.Pf t""'") 1.i1<:..l.
Metronidazole is classified as: Antiprotozoal drug aI1d b, "
Metronidazole is effective against -7 C&rei- A- N e:tv) J.iIJfr' l. k. }Bo'i'f.alJ' t.f,
Metronidazole discolor urine c.. vo..gil1t:J..,u
Metronidazole caution in pregnancy
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1 Vancomvcin 2 Penicillins 3 Tetracvcline
4 5 Streptomycin 6 Azithromvcin
7 Minocvclinc 8 Clindamvcin 9 Metronidazole
10 Doxvcvclin II Ciorofloxacin 12 Cotrimoxazole
I. Amoxicillin
.
2, Cenhalexin 3, Penicillin G and V
4. Cefuroxime 5, Tetracvclin 6, Ceftriaxone
7, Ervthromvcin
8. Clarithromvcin 9, Azithromvcin
Io. J I. Ofloxacin 12. Clindamvcin
Sulfadrups Tins
I Cotrimoxazole 2 Sulnhamethoxazole 3 Minocvclin
4 Photosensitive 5 Must take cmotv stomach 6 PCP
7 Room temoerature 8 Refril!cratof 9UT!
10 Calcium sunnlements II Dairv 12 orel!Ilal1cv
-Sulfamethoxazole +trimethoprim.have -7 is.J.,c.. (1 )
. A 22 year old patient currently using cotrimoxazole for UTI, reported sever rashes on d.c.o 'f- ,
" anns, neck and back, what are Ihe possible reactions"? Sf-,e.V\?I1S ""',' 1. .....
What ire the folic acid synthesis inhibitors7
Patient with G6PD deficiency, takes sulfadrugs can cause -7 HaeJ'1otr\-i"-- SFtJ
Hypersensitive reactions of sulfadrugs most commonly involve -7 d.of
Life threatening hepatitis caused by sulfadrug toxicity or sensitization rare SE. the P
signs and symptoms include-7 He.adc.l..rL, V 0"""", -H-t'$ I .J a It,,,dJCf2-
Sulfamcthoxazole have high frequency of skin hypersensitive r.eaction in patient with -1
Jfused in last trimester o[prcgnancy, can cause kernecterus in new born.
Cotrimoxazole suspension stored at room temperature in amber color glass bottle.
P. carinii pneumonia (PCP) drug ofchoice is Cotrimoxazole.
use in gram +ve anaerobic bacteria Bacteroid fragilis (abdominal infection) (,9) C Jii1darflJe_HJ
it should be stored at room temperature (<Ii, y., Y l'lJ' d,,,J,,,,,JP
it is not effective for Mycoplasma bacteria (L) ell', V\.
it increase Warfarin INR, increase Digoxin & theophylline levels (a.y ClaAJf1v....ot"t'l}
CJ
l1
it is effective for H. pylori (used along with PPls in triple therapy (2,}3, 4 , ,
it is use in treatment ofacne (j)r. t, , 0
drug for treating methicillinresistant Staphylococcus aureus infections (1, ,
it has the highest ototoxjcity (5)
it is more active against gram-ve H. influenza than Erythromycin (,)
it is use for acne and rheumatoid arthritis (7)
must avoid alcohol while on this drug because it cause disulfiram like reactions CJ
it is use as prophylaxis in traveller's diarrhea (lD)
the drug ofchoice for UTI 7 traveller's diarrhea (f I)
it is use in chronic treatment ofUTJ ( to
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conductc<l by PharmacyPrep.
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www.PhannacyPrep.Com Antimicrobials
I
13. Trimethoprim- 14. Metronidazole 15. Vancomycin
sulfamethoxazole
(TMP-SMX) -
is commonly causes dose-related GI tract disturbances, including nausea,
diarrhea (7,S,)
raises blood levels oftheQphylline and potentiates terfenadine in
ventricular arrhythmias( 7,8) EPjf1",,wW1..cwJ
have enhanced activity against Haemophilus influenza (9 ) V) ,
, inhibit the activity 'of DNA gyrase and topoisomerase IV ( 10, II ) C I '''', dg!(J)fdtO,
'are effective in'pactehal"prostatitis and bacterial diarrhea except that caused by C.
'di]ficile'{ 13')' ,
as competitive inhibitors of p-aminobenzoic acid in the folic acid metabolism
cycle( 13)
it is used pr'im'arily for of trichomonas, amebiasis, giardiasis and P,
. colitis ( 14) 'M.e.f'?J:ohY
Steven-Johnsons syndrome is a severe form of erythema multiforme (13 )'
characterized by bullae on the oral mucosa, pharynx, anogenital region, and
conjunctiva, target like lesions, and fever (erythema multiforme major)
antacids containing Mg or aluminum interfere with absorption if taken within 4
hours (5, 10, 11 )
Copyright 0 2000..2012 TIPS Inc. Unauthorized reproduction of this manual is strictly prohibited and 98-12
it is illegal 10 reproduce without permission. This manual is being used during review sessions
Phann"acology
99
Anticancer Dmgs and
Chemotherapy
Action of DNA
I
Damage DNA
Inhibit synthesis or
functions
I
latian:
Others
Antimetabolites
hlorc:thamine
* Actinomycin D
lophosphamide
"Etoposide
*5fluorouracil
famide
*Teniposide
'Cylanlbinc
rambuciJ
*Amsacrinc
Mercaptopurine
-
"Thioguanine
phalan
ulfan
Methotrexate
ustine
ustine
Free radicals:
plazalin
'---
"Bleomycin
latin
Topoisomerase
platin
inhibitors
arbazine
"Doxorubicin
arbazine
*Daunorubicin
lamineJ
-
'Topotecan
amcthylmelamine
*lrinotecan
mycin
Alky
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Ifos
Chlo
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Pharmacology
Definitions:
Neoplasm = New and diseased form of tissue growth
Benign neoplasms = Non cancer form of tissue growth, which can be removed by surgery. No metastases.
Malignant neoplasms = Cancer form of tissue growth. Invasive growth of cancer.
Malignant neoplasms can be categorized as;
Bone marrow = Leukemia (cancer of cells in blood)
Connective tissue =Sarcoma
Epithelium =< carcinoma
Lymphoid tissue-= Lymphoma (also named as Hodkins disease)
Myeloid stem cells = Myeloid leukemia
Endothelium = Kaposis sarcoma
Skin (melanocytes) = Malignant melanoma
Cell Cycle Phases All cells must traverse the cell cycle phases before and during cell division.
Anticancer drugs may act on specific phase. Tumor cells are more responsive to
specific drugs
Go phase - Resting phase
G
1
phase - Synthesis of enzymes needed for DNA synthesis
Sphase -DNA replication (DNA synthesis)
G
2
phase -Synthesis of components needed for mitosis.
M phase - Mitotic tubule formation -7Vincristine and vinblastine
Cell cycle phase specific More active against cells that are specific phase of cycle:
drugs G
1
phase-7 L-aspraginase and prednisone
Sphase-7 Methotrexate, 6-thioguanine, cytarabine
G
2
specific-7 Bleomycin and etoposide
M phase-7 Vincristine and vinblastine, peclitaxol
Cell cycle specific drug Alkylating agents, Antitumor antibiotic, Cisplatin
(phase-non specific)
Cell cycle non specific Effective whether cancer cells are in cycle or resting phase-.7 radiation,
agents nitrosoureas, mechlorethanime
Chemotherapy
The treatment of cancer with drugs is called chemotherapy. Antineoplastic drugs, also
referred to as chemotherapeutic agents, are drugs that are used to treat cancer.
Side effects of chemotherapy:
Acute:
Extravasation (effects the adjacent tissue)
I Vessicant drugs (damage to tissue / necrosis) Example: Bleomycin, cisplatin,
dactinomycin, domorubicin, vincristine, vinblastin etc.
Thrombophlebitis (inflammation associated with thrombus): Patient with cancer: can
develop thrombosis after chemotherapy. Due to activation of fibrinogen.
Hypersensitive reactions. Example: Etopiside, peclitaxol, rituximab, trastuzumab.
Rapid tumor lysis syndrome
Nausea and vomiting
2000-2012 TIPS Inc. Unauthorized reproduction of this manual is strictly prohibited and 99-2
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Chronic, organ specific:
Pharmacology
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Skin-7alopecia, dry skin, nail changes, pigmentation (melanoma), xerostomia
Alopecia is the loss of hair: Drug that cause alopecia is doxorubicin, daunorubicin,
cyclophosphamide. vincristine, and paclitaxel.
Vessicant agents include: daetinomycin, doxorubicin, mechlorethamine, mitomycin,
vincristine, and vinblastine.
Hair regrowth occurs after 1-2 months after stopping chemotherapy.
Xerostomia: Dry mouth is one of the most common complications associated with
radiation therapy. Reversible after 6 to 12 months of therapy.
Can be managed by: sugar free hard candy, chewing sugar free gum stimulates
salivation. Ice chips, sugarless candies, and commercially available saliva substitute or
cholinergic agonist (Pilocarpine Smg tab).
Bone marrow depression (Myelosuppression):
Bone marrow depressfon-7Neutropenia, and thrombocytopenia
Neutropenia -7 treated by colony stimulating factors (G-CSF and GM - CSF):
Filgrastim or pegfilgrastim
Thrombocytopenia 7 for prevention use Oprelvekin (lnerleukin-ll)
Complications: Bone marrow suppression is the most dose limiting side effect of
cancer
Myelosuppression in general the onset is 7 - 10 days and peak is 10 - 14 days.
Recovery count occurs usually occurs in 2 - 3 weeks.
Megaloblastic anemia by methotrexate-7Folinic acid (leucovorin, 5-
formyltetrahydrofolic acid)
Neutropenia associated anticancer drugs-7 can be treated by filgrastim (human
granulocyte colony stimulating factor)
Least bone marrow depression anticancer drugs is: Bleomycin
Cancer patient with anemia -7 Erythropoeitins are useful
Cardiotoxicity:
Risk of CHF, commonly seen with doxorubicin, daunorubicin, epirubicin,
mitoxantrone.
S-FU, capecitabine; Cause coronary spasms, mimicking a myocardial infarction (avoid
in know coronary artery disease patients).
Cardiotoxicity can prevented or lessen by using cardioprotective agent: Dexrazoxane
Pulmonary toxicity:
Pneumonitis, pulmonary fibrosis commonly seen with bleomycin, carmustine,
cyclophosphamide, mitomycin, methotrexate, vinca alkaloids.
PharrnaC?logy
Symptoms of pulmonary toxicity include: SOB, non-productive cough, and rarely low
grade fever.
Neurotoxicity:
Common with vincristine, vinblastine, Cytarabines, Methotrexate (very little), 5FU,
interferon alpha
Peripheral neuropathies associated with: Vincristine, peclitaxel: Peresthesia
(numbness and tingling) can occur with vincristine, which often appears within few
weeks of therapy.
High dose of cytarabin may produce cerebllar toxicity that manifest initially as loss of
eye-hand coordination and progress to coma.
Fludrabine cause severe neurotoxicity
Caramustine and other alkylating agents cause little or no neurotoxicity.
GI toxicity
Mucositis or stomatitis:
Mucositis: Generalized burning, and pain on the ventral surface of tongue. Floor of
tongue,'mouth looks erythromatus. Stomatitis: generalized inflammation of oral
mucosa.
Mucositis or stomatitis: Common with Doxorubicin, Methotrexate, 5-fluorouracil,
Actinomycin, Bleomycin capecitabine.
Recommend mouth hygiene, xylocaine, viscous sucralfate, nystatin, sodium
bicarbonate, for severe cases peliformin (growth factor) can be used.
Avoid alcohol, antihitamine, steroids, spicy food
Mucositis treatment and prevention:
Topical anesthetics: Viscous lidocaine, or dyclonine HCL 0.5 or 1%
Corticosteroid provides anti-inflammatory action.
Capscisin: Produces burning and pain and ultimately desens,itizes pain.
Sucralfate suspension may proVide benefit by coating.
For Localized effect: use benzocain in orabase.
Mucositis prevention:
Chlorhexidine gluconate 0.12% (Peridex, Periogard) may reduce severity and
frequency of mucositis infections.
/ Nausea and vomiting-7
Very high emetics anticancer drugs
Cisplatin
Streptozocin
Cyclophosphamide
High emetics anticancer drugs
Doxorubicin
Methotrexate (250 mg to 1000 mg)
it is illegal to reproduce-without permission. This manual is being used during review sessions
Cytarabine
Lowest emetic anticancer drugs
Bleomycin
Methotrexate (under 50 mg)
Vincristine
Vinblastine
Tamoxifen
Non pharmacological therapy
Take small and frequent meals
Avoid high fat and heavy aroma
Take dry, starchy foods like crackers
Pharinacology
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Management of nausea and vomiting associated with cancer chemotherapy:
The lowest emitogenic drugs nausea and vomiting can be treated by
-7 Dexamethasone PRN
High and very high emitogenic drugs associated acute: nausea and vomiting can be
treated bY-7 Dexamethasone+ Ondansetrons
DOC for delayed nausea and vomiting -7
Anticipatory nausea and vomiting-7 Benzodiazepine.
Hepatotoxicity
Hepatotoxicity monitor LFT, jaundice, or hepatitis: asparaginase, cytarabine,
mercaptopurine, and methotrexate.
Nephropathy:
Elevate BUN and electrolyte abnormalities: methotrexate may precipitate in kidney.
Cisplatin and streptoiocin. Amifostine may be used to protect the kidney from the
nephrotoxicity associated with cisplatin.
Sexualdysfunction:
Cyclophosphamide, melphalan, and procarbazine associated with significant infertility in
men and women.
Hemorrhagic cystitis
It is a bladder toxicity that is seen most commonly after administration of
cyclophosphamide and ifosfamide.
These drugs produce a metabolite called acrolein, which cause chemical irritation in
bladder mucosa, resulting in bleeding.
Hemorrhagic cystitis caused by Acrolein can be preven!ed by excessive hydration
and subsequent frequent urination. The other method is by administering
Copyright 2000-2012 TiPS Inc. Unauthorized reproduction of this manual is strictly:prohibited and 99-5
www.PharmacyPrep.Com Pharmacology
uroprotecting agent called MESNA, which bind acroleine and prevent from
contacting the bladder mucosa.
Pulmonary toxicities:
The mo.st common with bleomycin, mitomycin, carmustine
Rationale for combination therapy: Overcoming or preventing resistance. Cytotoxicity
to resting and dividing cells' Biochemical enhancement of effect: Beneficial drug
interactions' Rescue host cells
Some agents can be administered intrathecally: Methotrexate, Cytarabine' Thiotepa
Warning: Vincristine should be labelled as Intravenous only. Intrathecally vincristine
causes death.
Tips
Examples anti metabolites include -->
Examples of alkylating anticancer drugs ->
Non pharmacological measures to prevent nausea and vomiting associated with
caneer 4vol d sMa..L\
Melonoma is -7 S"'; Yl CO t1('
Metoclopramide and dexamethasone are more effective nausea related to -7 t,
Methotrexate is used for -7 RA , 4 psa,ua..sL5
Which anticancer drugs cause pulmonary fibrosiS-7 b(fl...) Mj L' ..,
-Hypertropy is -7 et1 tJ1>
Hyperplasia is -7 et ce1U
Least emetic anticancer drug is -7
Cancer patient on cancer chemotherapy, reports shortness of breath, non
productive cough, she may be using drug -7 hfe..oYr"..1 c....r...,
DOC for delayed Nausea and vomiting -7 dexamethasone
Mesna is -7 .
Doxorubicin preparation should be performed in -7 ca..l la'rnl cilA. h
011
9
Hypertropy is -7
Hyperplasia is -7
Melatonin -7 $( tz-L-f'
Peclitaxef and docetaxel act on -7 M
Cancer estirryated deaths in men: Lung cancer 31% and Prostate cancer 11%
Cancer estimated deaths in women: Lung cancer 25% and Breast cancer 15%
Exa"mples antimetabolites include ->*5-fluorouracil, *Cytarabine, *Mercaptopurine,
*Thioguanine and Methotrexate )
, C '. TV/ec.Ce.)/ (ha.J.otl1
,. 2.. c.hlo!-A1""")bl.l..
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2000-2012 TIP Inc. Unauthorized reproduction of this manual is strictly prohibited and 99-6
It IS Illegal to reproduce without permission. This manual is being used during review sessions
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100
Pharmacognosy & Natural
Products
Natural Products
Naturaloroduct Classification Use
Cranberry Antioxidant, Cleanses and stops infections in the urinary tract.
Vaccinium bacteriostatic
macrocarnon effect
Dong Quai Tonic, immune- Used to treat all symptoms of menopause as an
Angelica sinensis stimulating, anli- alternative treatment to estrogen therapy.
spasmodic Regulates the hormonal system. Overall tonic for
female reproductive system. Reduces high blood
pressure and PMS. Caution: Contra-indicatioD
in nrePnaDCV
Ecbinacca Antibiotic, anti- Stimulates and boosts immune function. Has
Echinacea fungal immuno- cortisone-like activity that helps wound healing.
angustifol ia/purpurea stimulating Fights bacterial and viral infections. Contra-
indication in auto-immune diseases (i.e.
Multiple Sclerosis AIDS)
Evening Primrose Anti-spasmodic Used in treatment of multiple sclerosis and PMS.
Oenothera biennis Helps prevent heart disease and stroke and
maintains healthy skin. Excess consumption can
result in oily skin.
Feverfew Anti- Helps prevent migraine headaches and also
Tanacetum inflammatory, useful against swelling and arthritis. Stimulates
parthenium emmenagogue digestion and improves liver function. Caution:
Not to be used by lactating or pregnant
women.
100-1
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Garlic Antibiotic, anti- Reduces high blood pressure and blood
Allium sativum fungal, anti-viral cholesterol. Immune support for respiratory
system. Anti-cancer and digestive tonic. Caution:
Not to be used by lactating women because it can
I oass to the breast milk and cause colic in infants.
Licorice Demulcent, Gastric ulcers, adrenal insufficiency hypoglycemia.
Glycyrrhiza glabra diuretic, Good for coughs and other bronchial complaints.
expectorant. Caution: Contraindicated for tbose with higb
laxative blood pressure or if Ofe2.D3nt.
Ginger Diaphoretic. Relieves indigestion and abdominal cramping.
Zingibcr officinale cholagogue, Benefit in relieving motion sickness, dizziness,
carminative, nausea and colds. Ginger lowers blood clotting.
stimulant
Ginkgo Biloba Anti-asthmatic, lncreases blood flow to the brain. Improves
Ginkgo biloba bronchodilator, memory loss. Alzheimer's disease cerebral
platelet activating vascular insufficiency and inhibits blood clotting.
factor (PAFl with war-farin and Aspirin. Take witb food.
inhibitor
Ginseng Tonic, stimulant, Stimulates both physical and mental activity. Anti-
Panax schin-seng demulcent, fatigue (insomnia, nervousness. poor appetite).
stomachic Enhances immune system, inhibits exhaustion of
adrenal 21and and anti-stress.
Echinacea-7 Common cold
Saw palmctto-7 Prostate (BPH-Benign Prostate Hyperplacia)
Garlic -7 lipid levels
Feverfew -7 Migraine
Gingko-7 Increase memory
St. Johns wart -7 antidepressant
Bitter melon-7 anti-diabetic
Prime rose oil -7 PMS (premenstrual syndrome)
Atropine-7 anticholinergic
Vincristine and vinblastin-7anti-cancer
Taxol (pec1i-taxol)-7 Yew plants (himalayas)-7several types ofcancers
100-2

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com Evaluating Exam Review Guide

Misbah 13iabani, Ph.D

10 Biceos bronchi 11- Triceps bronchi 12. dvsohagea

Glucagon Most cells MaiRt9ins glucos.e le.vets in the bloodstream

PhamiacyPrep.Com Endocrine System

.f1 Y\ AsH-, 0 Wc.JJ'

Excessive blood urea nitrogen in blood ( ) It;...

Increased branchial secretion

Upper respiratory tract

The bulb canal,conta!ns b!ood supply and nerve terminals.

esinophils, and mast cells.

l. linolenic (Omega 3) 2. linoleic (omega 6) 3. Arachidonic

Nitric oxide (NO) is a derivative of what amino acid? (

Cardiac Troponins (Tn):

Bacterial infections generally increase neutrophils to 80% and decrease lymphocytes to

It is rapidly converted to its active form: Thiamine

Wernicke-Korsaskoff syndrome (Thiamine related disease

It is a precursor for coenzyme flavin rnononucteotide (FMN) and

Riboflavin decomposes when,exposed to visible light. This

1.2 to 1.7mgfday for normal adults

Both nicotinic acid and nicotinamide can serve as the dietary

Nicotinic acid therapy is not recommended for diabetics or

Several physiological conditions (E.g. Hartnup disease and

Vitamin B;o;vri oxine, Pyridoxal, and Pyridoxamine)

It must be hydrolyzed from protein in order to be active.

Following absorption the vitamin is transported to the liver in the

Treatment of pernicious anemia: Use vitamin 8n parenteral (im or

All persons over SO and elderly should get vitamin 8n

Elderly are achlorhydric, thereby have decreased vitamin B

A conjugated molecule consisting of a pteridine ring structure

Animal cannot synthesize PABA nor attach glutamate residues to

Anticonvulsants, oral contraceptives, methotrexate, S-flurouracil

Hydroxylation of proline residues in collagen is the most important

Cause of vitamin Cdeficiency is poor diet and increased

An acidifying agent used to treat overdose of base drugs

Vitamin Cis deficient in smokers, thereby vitamin C

B-carotene retinol '7 retinal '7 retinoic acid

Retinol, retinal (retinaJdehyde), and Retinoic acid

Rhodopsin is active form of vitamin A in vision

B-carotene consist of 2 molecules of retinal linked at their

Very effective as antioxidant

Overdose of vitamin A can cause toxicity.

Excessive accumulation of vitamin A in the liver can lead to

Isotretinoin (Accutane) is 13-cis retinok acid and this is oral only

Tretinoin (Retin-A) is 13-trans retinoic acid and this is topical only

Active form is: 1, (Vit 011 is derived

Chronic renal failure can cause deficiency of vitamin 0

Ergocalciferol (02) is formed by UV irradiation or ergosterol

In the skin 7-dehydrocholesterol is converted to cholecalciferol

Osteomalacia is characterized by demineralization of previously

Vitamin 0 supplement 800 IU

Newborn (infant) on breast-feeding should get vitamin 0 drops.

Act as a natural by sC3ven.ging free radicals and

Vitamin K2 (Menaquinonej is produced by intestinal bacteria

Vitamin K] is a synthetic menadione. When vito K] is

Select True/False Statement

Insulin antagonist is? { ;3

@A doctor want to prescribe orlistat (xenical) to patient to I I

a patient is determined to have 100 mg % of blood glucose, what is the eqUiValen

31-How much of a substance is needed to prepare 1l of a 1: 10,000 solution?

P2tassium phosphate injection contains a mixture monobasic potassium