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The &Iost Irnp ortant teeftxres
Notes

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I fuwut, tfiis materin[ is not easy, a fot of drugs d a fot of information ; tsurf
ufiat I reaffy annt you to furoot dr' concentrate on ; is ufiat t saif aAout : rfi{Is
$'tEqy r^v{poKI%A(I dl ZLEASE U@EKL rNE "Irfis . . .,
'

Dfr" !{nkaffi A[-Hanili

...

Dear colleagues ,
As we all noticed , Dr. Hakam repeated that information a lot during his lectures, So,
we decided to collect these * IMPORTANT INFORMATION ' and put them in this
summary !!

>> BUT please , note that this summary is USELESS

without studying the lectures and

understanding the whole concept.

And please, note that the points in this sunmary are taken from OUR LECTURES
and from OUR O1VN NOTES and from a summary done by our colleague in the 6,h
year ( Ruba Abu-HarfiIe ).
>>

>> SO,

It

is

a STUDENTS'WORK from STUDENTS'

SCOURCES , BLII we rried our


best to make sure that this summary conrains (ALMOST) all IMpoRTANT
information and is free of any mistakes ; but as we all know , nobody is perfect , So
please , cooperate with us , and if you find any rnistakes in the summary or realize that
there is an important information we forgot to include , please, inform us at :

s*q.y't gid{y't

it

6*f

'' VERY IMPORTANT...''

Done By :
Shifa Summarizing group

lN Pharma Lectures...
*

n--:::l
' rel,

e
"
"e
e

l:-

/i^

\o

^a^^--lIsl dt r;
tc rlt rf , { ll I Htrl

Bactericidat .
lnhibits ce[[ watl synthesis .
NOT effective against B-l,artarhase producing microbes.
ln case of renat faiture ) Dose must be reduced.
Absorption is nearty comptete parentatty BUT lM is irritant

*" Adverse EffeEEs


>> Allergy

Tvpg5_of allerev :
A - lmmediate
Anapfuytaetie shoek !

Treatment

.
"
"
"

ts -

Potent airway ( By opening the mouth then giving oxygen


Epinephrine ( lV or SC , EUT NOT lM+vasoconstrictor)
Hydrocortisone
Antihistamine

Accelerated

e- Late

rGctiora

Penicillin Sensitivitv Test :

B Give low concentration of penicittin intradermaty


E lnject the other hand with distitted water.
E Wait 1-2 min .

in one hand (Using insorime syringe).

"oR:
E One or tow drops of penicittin in the eye .
>> lf there is attergy ) Eye watering and the eye witt start itching .
@@

Natural penicillin

* Benzvl Penicillin ( Penicillin G )


o

Drug of choice in

1- Streptococcus pneumonia ( Typicat pneumonia ), B-Haemolytic streptococci.


2- Meningitis caused by Neisseria meningitidis.

** By adding
PROCAINE
>> Procainepenicitlin

longer hatf life ( Detay the absorbance ).

* Phenoxvmethvlpenicillin ( Penicillin V )
. Administered oratty .
o Used in mitd infections ( ) ln atl types of tonsittitis )
" Benzathine Penicillin :
Used in Depot preparations .
. Used as a prophytactic drug in case of recurrent tonsittitis to prevent rheumatic fever

Semi svnthetic :
** fl-Lactamase Resistant:
@@

Used against B-lactamase producing Staph. Aureus

**Extended Spectrum penicillin


* Amino penicillin :

>> Ampicillln e nmoxicittin

o
e
c
e

Broad-spectrum.
Destroyed by lJ -tactamase enzyme
Used

in salmonetta infections

Adverse effect
Diarrhea ,rash .
Drug of choice in :
1- Meningitis caused by l-l-inftuenza.
2- Pregnant lady with pneumonia .

>> Auementin ( Amoxicillin + Calvulanic acid)

NOT destroyed by B -tactamase enzyme.

*cMines:
" lnjectabte / Orat preparations
* 3 rd Generatisn Cephalgsporines :
o Active against gram -ve microorganisms .
. Weii distributed
>> Cross BBB & enters CNS + Used in meningitis caused by H-inftuenza.
the bones.) Used in osteomytitis .
the placenta.
Excreted by the kidneys ) Dose must be redriced in renat failure

>> Cross
>> Cross

* Ceftriax.r:ne & Cefoperazone


c

Excreted in the bite

coutd be given in renal failure

Adverse effects :
1- Cross Attergy with Penicittin .
2- Fal,se + ve glucose test in urine
3- Disutphiram like reactions if taken with atcohol
&, vomiting

severe abdominat pain

, headache

Aminoqlvcosides:

.
.
)
.
.
o

NOT given oratty

ln patients with kidney impairment :


1- Decrease the dose
2- Give the doze at longer intervats.
They are highty concentrated in the inner ear and in the renal cortex.
Used against aerobic gram -ve microbes.
They have narrow therapeutic index.

or

Adverse effects:
1. Aototoxicity:
r Auditory: tinnitus ) deafness.
o Vestibutar: headache, dizziness, Ataxia
2. Nephrotoxicity ) inabitity to concentrate urine. [Reversibte (doSe dependent)]
3, Neurotoxicity (muscte paratysis)) apnea(inabitity to breath).
4. Atlergic reaction ) haemotytic anemia .
,, (We can minimize the adverse effects by monitoring ptasma concentration )
NOTE : Penicillins , cephalosporines & Aminoglicosides can cause Haemolytic anemia !!

Preparations :
- Streptomycin , Gentamycin , I Amikacin & Nitilmicin (broad-spectrum)]
- Neomycin :
>> Coutd be given ORALLY or TOPICALLY
>> Prophytactic for Hepatic coma .

lllacrolide Antibiotics

* Ervthromvcin:
)
)

Enteric coated tabtets.


Does cross the ptacenta ) Not given during pregnancy E breastfeeding.
lt is metabotized by the [iver &. excreted in the bite.
Bimodat Distribution)1- stow metabotizers 2-rapid metabotizers
3- Normat metabolizers ) (geneticatty determined)
lnter-individuat variations & inter-ethnic variations
o lnhibitor of cyt p- 450 enzyme system

.
.

Uses:

.
.
.
.

Diphtheria
Chtamydiatinfections
Atypical pneumonia caused by Mycoptasma pneumonia
Legionettosis ( caused by tegionetta pneumoniae )

.
r

Prophytaxis: prior to dental protedures (with amoxicittin ]


acute BacteriaI Endocarditis)
Atternative to penicitlin in patient attergic to peniciltin.

)to

prevent SBE (Sub-

Adverse effects:
1-Liver toxicity: acute chotestatic hepatitis (reversibte)
>> Manifested by ) nausea, vomiting, jaundice.
2-Ototoxicity.

* Clarithromvcin

. Much better absorbed & distributed ) inctuding CNS.


" Lincomvcin & Clindamvcin:
. Very effective against anaerobic gram( -ve or + ve ) bacteria (becteroid fragitis).
. Very effective against staphytococcus Aureus.
o Do penetrate bones ) used in osteomyetitis.
.
cause pseudomembranous cotitis.
' ClindamycinCan
) Used in acne vutgaris with vitamin A.

* ehbramphenicol
o
e
*

Very active against anaerobic infections inctuding Bacteroid fragitis .


Metabotized in the liver by conjugation with gtucuronic acid or by reduction
Decrease the dose in patien.ts with tiver faiture.

Uses:

1- ln Satmonetta infections . (typhoid fever)


2- ln severe Rickettsial infections .
3- ln bacteriat meningitis caused by H-inftuenzae.
Adverse effects :
'l- Bone marrow suppression :
e Reversible erythroid suppression of bone marrow-.-'
e lrreversible AplE$lg rnsrnl!
/- Gray baby syndrome .
.# lnhibitor of Cyt p-450 enzyme comp[ex ( interfere with other drugs'metabolism

Tetracvclines
"
"-

Broad-spectrum activity
Absorption is IMPAIRED by :
Mitk , Anticids , tron preparations

. G Wett distributed , inctuding CNS .


.u Concentrated in thb liver & excreted in the bite ( given in renal faiture)

U,ses :

"
e
6

Atypical pneumonia .
Chlamydial infections 8. Rickettsial infections
Acne vulgaris .

Adverse reactions :
1- GIT upset
2- Permanent Brown discotoration of teeth .
* They are contraindicated in young peopte.
3- Do cross the ptacenta
) They are contraindicated in pregnant tadies
4- Phototoxicity ( Doxycyclin )
5- Vestibutar Ototoxicity ( lilinocyclin )
6- Btack hairy tongue .

Fluroauinolones

'

. Broad-spectrum activity.
. Wet[ absorbed oratty
+ BUT absorption is impaired by antacids &. iron preparation.
' . Poorty enters CNS
in atypical pneumonia
" Used
effects
.

Adverse
:
1- CNS side effects ( dizziness , headache
- NOT recommended in pregnancy.

* Ciprofloxacine

Uses :

1- UTI infections ( gonorrhea )


2- GIT infections ( satmonetta &. shegetta )
3- Respiratory infections

4- ln osteomytitis

Sutfonamides & Trimethoprim :

They interfere with Folic Acid synthesis .


u Sulfonamides enter the rxn in place of PABA .
. Trimethoprim Inhibits DHF reductase in bacteria
" Both are bacteriostatic .

" Sulfasalazine
".

Poorly absorbed oratty.


Used in utcerative colitis ( inftammatory bowe[ disease )

Adverse effect i
1- Crystatl,uria (crystattized in the urinary tract

* Trimethoprim
.
.

"

Given oratty or parenta[ty .


Used in UTI , Proastitis ft vaginatitis

Co:Tr inloxqZo_lg_;
. Bactericida[ .

.- e- Wet[ absorbed

& wetl distributed; including CNS


t

Uses :

1- UTI . (E-coti , proteus , ktebsetta )


2- Chest infections
3- Pneumocysits carinii in patients with
4- Satmonetta & shegetta infections
5- Chemoprophitaxis of UTI in women

AIDS

Adverse Effects:
1 - Megatoptastic anemia
( ) Fotic acid deficiency or Vitamin 812 deficiency .)

Anti-Protozoal Drues :
* Metronidazole : (flagyl)
o Active against anaerobic microorganisms .
) Used in empirical therapy
Broad-spectrum activity .
"o Given
in renal faiture , BUT NOT in liver faiture () Decrease the dose )
. Can cause disutphiram like effects when taken with atcohol .
Adverse effects :
1- Meta[tic taste in the mouth .
2- Cotors the urine into red-broyrnish color
3- GIT upset.
4- Dryness for the mouth & vagina .

Uses :

.
.
.
.
.
n

ln giardiasis & amibiasis .


ln Bacteroid fragitis infections (anaerobic bacteria ).
Prgvention of post-surgical abdominai and pelvic infeciions ( after bowets'surgery
ln treatment of peptic utcer caused by Heticobacter pytori .
ln treatment of utcerative gingivitis .
ln non-specific urithritis & vaginititis .

Treatment
.
)
.

of

Tuberculosis (TBr

Always use combination of drugs .


To prevent resistant .
Used to give streptomycin lM for 2 months

2 staees of therapv :
1- initial phase:
Minimum 3 drugs
lsoniazid & Rifampin & other drugs

)
*

2-Continuation phase :
) Minimum 2 drugs.
+ lsoniazid & Rifampin

'

" lsoniazid :

. The most active drug in treatment of TB


. lt inhibits the synthesis of mycotic acids
. lt crosses BBB and enters to CNS.
o Metabotized in liver by acetytation
) Bimodal distribution
1- slow acerylators 2- rapid acetylators

Adverse effects :
1- Peripheral neuritis ( peripheral neuropathy )
) We give Pyridoxine (vitamin 86) with it.
2- Liver impairment ) jaundice.
) You shoutd atways do Liver Function Test ( LFT ), before & during therapy

* Rifampin :

. Broad-spectrum activity ( against g+ & g- )


. lt induces the cytochrome p-450 enzyme system
) lt reduces the hatf tife of many drugs
. Most of it is excreted in the feces ) can be given in renal faiture .
. Cotors att body ftuids with orange-red cotor .
. Fixed combination with isoniazid.
o Chemo prophylactic in case of meningitis caused by H-inftuenzae.

* Ethambutol :
.
.
)

Affecting ONLY Mycobacterium tubercutosis .


NOT given atone ) ( ln combination with lsoniazid & Rifampin )
Because drug resistant wi[[ devetop rapidty
Adverse effects :
1- Optic neuritis ( lnflammation of optic nerve ) ( + diminished visual acuity )
>> Visuat fietd witt be narrowed, Tunnel vision , Lackdiscrimination between RED/GREEN
2- Increases uric acid concentration .

* Pyrazinamide

:
in combination therapy .
in short coarse therapy of TB.
in the initiat phase
Adverse effects :
1- Jaundice . ) tiver function must be checked
2- Hyperuricemia .

.
.
.

Used
Used
Used

Anti-l,Aalaria Druqs :
The Staqes:
1-Hepatic stage :
. c Drugs used:
>> Primaquine, Proguanit, Pyrimethamine .
2-Blood stage :
. Drugs used :
>> Chtoroquine , Quinine , Meftoquin, Pyrimethamine, Proguani[

3-Sexua[ stage :
Drugs used:
>> Quinine , Chtoroquine

* Chloroquine

, Primaquine , Mefloquin .

Uses :
1- ln acute attacks .
2- ln chemoprophylaxis in alt forms of plasmodium

Adverse effects :
. Hemotytic anemia, particularty in peopl,e with G-6-PDD (Gtucose-6-Phoshphate
Dehydrogenase Deficiency )
r Ototoxicity * irreversibte loss of hearing .
. Cardiac arrhythmias (abnormat ECG )
" Retinopathy ( irreversibte ).

* Primaquine
.

Atways shoutd be combined with btood schizonticide


lt affects tissue stage &. sexual stages .

Adverse effects :
1-Hemotytic anemia

in

peopte with G-6-PDD

* Pvrimethamine & Proguanil :

. lnhibit DHFR enzyme .(DiHydroFotate Reductase )


. When combined with Sutfunamide ) synergistic effect.
Fansidar >, Pyrimethamine + sutfonadoxine .
. For hepatic ft blood stages + NOT for sexual stage

Adverse efiect:
1 - Megatoptastic anemia.

Quinine :
Used in btood &. sexual stages ( But NOT in hepatic stage )
" give

) we
Primaquine with it .
Adverse effects :
1- Hemotytic anemia in peopte with G-6-PDD
2- Cinchoniraty (cinchonism ) ) ototoxicity .
3- Cardiac arrhythmias .
4- Btackwater fever (DlC, Haemogtobinuria , Dark urine , Azotemia ,Renal Faiture)

* A{etloquine :

e ii is used mainty in prophyiaxis thei-apy .

Adverse effects :
1- Cardiac arrhythmias

Anti-Viral Drues :
*

Aqyclovir

.
e
.
"

lnhibits viral DNA synthesis .


Distributes we[[ in our bodies
Does cross the ptacenta ft is secreted in the mitk
Given TOPICALL\' ( NOT wett absorbed oi-atty )

Adverse effects

'

1-

CNS side effects .


2-. Reversibte renal dysfunction

Uses :

"
"

Herpes Simptex Virus lnfections. (HSV)


Varicetta - Zoster Virus lnfections.

* Ganeiclovir
,
"
'

Inhibits virat DNA synthesis .


Low bioavailabitity .
Used against CytoMegaloVirus (CMV).

Adverse effects

1V"

Myetosuppression ( neutropenia , thrombocytopenia ).


CNS side effects

* Foscarnet
Adverse effects

*'

Nephrqtoxicity & Hypocatcemia


Paresthesia (toss of sensation in the periphery)

Uses ;

"
"

CMV

retinitis

Acyctovir- resistant

HSV

infections

I -'l

* Trifluridine
"o

Broad spectrum
Used

in keratoconjuctivitis

* ldoxuridine

&,

Keratitis in eyes due to HSV types 1 or 7.

lt is topicat therapy ( straight in eyes ) for Herpes Keratitis

Without treating coutd lead to btindness.

* Amantadine & Rimantadine


.
o
.
o

Affects influenza - A virus BUT NOT type B .


Excreted in kidney ) kidney function must be checked .
Embryogenic & teratogenic ) NOT given in pregnancy .
NOT given in epiteptic peopte.

* Ribavirin :
.
.
"

Broad spectrum of antivirat activity .


Given oratty or lV.
NoT given in pregnancy
Embryogenic & teratogen'ic

Adverse effect :
1

- Hyperbitirubinaemia.
4F&A&

Drugs used

* Zidovunadine

."

iffi

in AIDS :

dtJ#*

Used against HIV 1 e.2.

Distributed very welt

Adverse effects

enters the CNS

1- Bone marrow suppression (granutocytopenia & anemia


2- Myopathy.

- The

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.

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