Anti-infectives

Parasitology
Parasitology
Schistosomiasis: is caused by S. haematobium &/or S. mansoni & causes liver cirrhosis. This
can be treated by praziquental.
Scabies is an exo-parasite caused by mites. It can be eradicated by gamma-benzene
hexachloride or benzyl benzoate or Sulphur ointment 10%.
Drugs used in the treatment & prophylaxis of Malaria include:
Chloroquine (Aralen) Pyrimethamine
Quinine (in treatment only) Primaquine
To be given one weak before exposure & 4-6 weeks after leaving the endemic area.
Primaquine is the most effective & least toxic of the 8-amino-quinolone group.
Drug of choice for prophylaxis of malaria: is Chloroquine.
Pyrimethamine ( usually with sulfadoxine), Fansidar, & Primaquine are only used in
treating chloroquine resistant cases.
Quinine: (an optical isomer of Quinidine) is only used in treatment. Available as the SO
4
(oral) or HCl (IV) salts.
Tape worms: Both Beef worm (Tinia saginata) & Pork worm (Tinia solium) are treated by
either Quinacrine or Niclosamide.
Quinacrine: should not be used in the treatment of tape worm in patients who have a history
of psoriasis, psychosis, elderly or those with liver disease.
Niclosamide: is an anthelmintic drug, most effective against beef & pork tape worms.
Hook worm (Ancylostoma duodenalis): is a parasite capable of entering the body through
intact skin. It is treated with thiobendazole or mebendazole.
Thiobendazole (Mintezol): is an anthelmintic drug, which is effective against multiple
infestations, e.g. whip worm, cat & dog hook worm, T. trichura, & strongyloids (thread
worm).

Anti-infectives
Anti-microbial
General
Thermal Death Point: is the temperature at which all bacteria of a given species are killed
after 10 min of exposure to heat.
Dry heat sterilization: this type of sterilization is an oxidation process.
Mineral oils are sterilized by dry heat process.
Gas sterilization (Alkylation): is used for sterilization of some substances (plastic). Ethylene
oxide is the agent used in the process.
How to kill spores: by moist heat at 100
o
C for 15 min for 3 successive days. Alternatively,
autoclaving at 121
o
C for 20 min.
Globigu: is a variety of Staphylococci that is resistant to heat.
Acid fast bacteria: are a special type of bacteria (e.g. Mycobacterium) which differs from
other types of bacteria in:
Containing high conc. of fatty acids.
Presence of mycolic acids & fatty substances.
Drug fastness: Mutational forms of the original bacterial strains usually appear due to
exposure to sub-clinical (sub-therapeutic) doses of the drug.
Pyoderma: is a pus forming skin infection (pyo = pus).
Bubble Point Test: is used to check leakage of bacterial filters.
Hepa filters: are used to remove particles from air. These are used in the laminar flow hood.
The pore size for bacterial filters is 0.22 nm.
A fomite: is a non-living material (e.g. needles, syringes) capable of transmitting infection.
Complications of corticosteroids therapy:
Increased susceptibility to infection (immuno-suppression).
Masking symptoms of infection.
Spread (dissemination) of local infection.
Negric bodies: these are spherical, eosinophilic inclusion bodies, found in nerve cells of
rabid animals or humans. They are formed due to allergic reaction.
Granulomas are caused by M. tuberculosis.
Agranulomas are caused by M. lepre.
General
Growth sequence of bacterial cells: When a given
bacteria is seeded on a suitable medium, at a suitable
temp., its growth will follow a definite course. The
growth curve can be divided into 4 phases:
a. The lag phase.
b. The logarithmic phase.
c. The stationary phase.
d. The phase of decline.
Conjunctivitis may be bacterial, viral, fungal, parasitic, or allergic.
Bacterial conjunctivitis is caused by S. aureus, S. pneumoniae & Hemophilus spp.
In Canada, Chlamydia trachomatis is often isolated from conjunctiva of children, ttt AgNO
3
Eye infections in Canada: the most common causative organism is P. aeruginosa. These are
treated by gentamycin eye drops & / or ointment.
In encephalitis, gentamycin is the most useful to treat infections caused by susceptible
P. aeruginosa strains (carbenicillin can be used but resistance develops rapidly).
Neonatal Meningitis in Canada: the most common causative organism is H. influenzae.
Causative pathogens in meningitis:
Neonatal (0-1 month) E. coli, Stept B, Lysteria, or Herps simplex
1month 4 yrs H. influenzae Adults S. pneumoniae / N. meningitidis.
In meningococcal encephalitis: tetracycline, chloramphenicol, or sulphonamides can be
used as they pass BBB. Streptomycin can pass the inflamed meninges only, it does not pass
the normal meninges. Crystalline penicillin can be used but has to be given intra-thecal.
Middle ear infections are caused by:
S. pneumoniae, H. influenzae in children
S. aureus, hemolytic streptococci in adults
S. aureus, E. coli in neonates
Generally, S. pneumoniae & H. influenzae are the most common isolates in AOM. Less
frequently isolated pathogens are GABHS, M. catarrhalis & S. aureus. G ve (P. aeruginosa,
E. coli, K. pneumoniae & Proteus) are rarely isolated. Clostridium is never found in ear.
Sinusitis & mastaditis are caused by S. pneumoniae & H. influenzae
In cases of mixed infections: we can use a combination of antibiotics (sometimes a
bactericidal + bacteriostatic).
INH, tetracyclines & erythromycin may result in hepatic toxicity & GIT problems.
Sulfaisoxazole, naladixic acid, primaquine & probenecid may result in hemolytic anemia
in patients with glucose-6-phosphate dehydrogenase deficiency (Favism).
a
b
c
d
Time (hrs)
L
o
g

B
a
c
t
e
r
i
a
l

N
u
m
b
e
r

The Bacterial Cell Wall:
In G +ve bacteria: the cell wall consists of peptidoglycan & teichoic acid.
In G -ve bacteria: the cell wall consists of peptidoglycan, lipoprotein layer & lipo-
polysaccharide + phospholipid outer membrane.
The Gram Stain: the basis of the differential gram stain is the cell wall structure.
The procedure begins with the application of a basic dye, crystal violet.
A solution of iodine is then applied. At this point all bacterial cells will be stained blue.
Cells are then treated (washed) with alcohol.
G +ve cells will retain the crystal violet iodine complex & remain blue.
G ve cells will be completely decolorized.
The last step is applying a counter stain (e.g. the red dye Safranin) so that G ve cells
will take a contrasting color.
G +ve retains the dye (gentian violet) because of teichoic acid.
G -ve does not retain the dye because of the lipid membrane.
G +ve pathogens a exotoxins G ve pathogens a endotoxins
Eukaryotic & Prokaryotic Cell Structure:
Eukaryotic (Fungi & Yeast) Prokaryotic (Bacteria)
Cell Structure More complex inside More complex outside
Nucleus Is bounded by a membrane that is Absence of nuclear membrane
continuous with endoplasmic reticulum & true nucleus [1 super-coiled
DNA strand (nucleoid)]
Ribo/Chromosomes: not distinguishable / on reticulum Only 1 chromosome / free
Cytoplasm Presence of endoplasmic reticulum, Absence of mitochondria
Golgi apparatus & mitochondria. & membranous inclusions
Mobile (plasmids, reticulum). Immobile
Protein synthesis 80 S ribosome 70 S ribosome
Reproduction Mitosis Asexually (binary fission)
Respiration Site Mitochondria Cytoplasmic membrane
Locomotion Ameboid / Flagellae Flagellae / Cilia
Cell size Large Small
Cell envelope Consists of 3 layers: Multilayered:
a. Cytoplasmic membrane a. Cytoplasmic membrane
b. Peptidoglycan layer absent b. Peptidoglycan layer
c. Outer membrane
c. Variable outer layer (capsule) d. Variable outer layer
(capsule)
Plasmids: are genetic elements that carry antibiotic resistance genes of a micro-organism.
A Mordant: is a substance that fixes bacterial stain & becomes permanent (to differentiate
G +ve bacteria, which retains the dye, from G ve bacteria that does not retain the dye).
Bacterial Infections
Gram-positive Cocci I nfections:
Scarlet fever: is caused by S. pyogenes & is characterized by fever, rash & strawberry
tongue; It is treated by sulfadiazine & penicillin (less commonly with chloramphenicol).
Rheumatic fever: is an immunological reaction to repeated infections by GABHS infections.
It causes cardiac valve damage.
S. viridans (a hemolytic streptococci): involved in sub-acute bacterial endocarditis &
pyorrhea alveolaris & UTIs. It can be treated with a long course of penicillin V. During the
infection, fever tends to peak during night & early morning hours (10 pm 6 am).
Postulant ear boils are usually caused by staphylococci in the anterior portion of the external
auditory canal.
Acute toxic shock syndrome: is caused by tampons. Symptoms include sudden high fever,
headache, sore throat, vomiting, diarrhea (flu-like syndrome). The causative pathogen is
S. aureus. It occurs both in men & women (esp. young females)
Gram-negative Cocci:
Neiserria gonorrhea: the drug of choice for urethral & urogenital gonorrhea is penicillin +
probenicid or tetracyclin. Spectinomycin is an alternative in penicillin allergic patients.
Gram-positive bacilli infections
Diphtheria is caused by Corynobacterium diphtheria & can be treated by benzyl penicillin or
erythromycin.
The diphtheria exotoxin causes laryngeal obstruction.
Schicks test for diphtheria: ID injection of diphtheria toxin (0.1 ml) in the forearm. A
+ve reaction means susceptible (not immune) to diphtheria. The reaction consists of
local redness after 24-36 hrs & persists for 4-5 days.
The Genus Clostridium: these are anaerobic, spore-forming G +ve bacilli, resistant to heat,
& capable of producing exotoxins. They can be subdivided into:
Clostridium difficile: pseudomembraneous colitis, treated with vancomycin.
Clostridium botulinum: botulinum exotoxins botulism (food poisoning), usually
associated with anaerobic growth of the organism in improperly canned food (meat &
non-acidic vegetables); it is destroyed by boiling for 10 min. The M.O is also found in
soil & GIT of domestic animals. Botulism is treated by polyvalent (bivalent) anti-toxin.
Clostridium tetani: tetanus, treated with vancomycin IV.
Clostridium preferengens (C. welshii): Gas gangrene which spreads rapidly & has a
necrotizing effect. The organism is capable of devitalizing living tissue.
Gram-negative Bacilli I nfections
Neonatal meningitis is caused by H. influenzae.
E. coli: is the most common causative pathogen in UTIs.
Pseudomonas sp. are sensitive to aminoglycosides, carbenicillin (but resistance develops).
They are generally not sensitive to cephalosporins (except ceftazidime & cefepime).
Salmonella typhi: is the causative pathogen of typhoid fever. The most common location of
the organism in a typhoid carrier is the gall bladder ( the UT may be involved). In culture
media, it does not ferment glucose nor sucrose & does not produce gas.
Shigella: is the causative organism in bacillary dysentery. It is generally classified as non-
lactose fermenter of the gp. Enterobacteriacae (also Salmonella), & the subdivided further
according to the antigen properties.
Cholera: caused by Vibrio cholera (Comma bacillus, Kochs bacillus), produces endotoxin.
Chlamydia trachomatis: constitutes part of the normal flora of the nose & throat & less
commonly of the vaginal cervix. It is the causative agent of trachoma including conjunctivitis
& urethritis. Infants may contract chlamydial eye infections during birth, from a maternal
cervical infection (treated by AgNO
3
eye wash).
Brucellosis (Malta fever): is characterized by fluctuating temperature (undulant fever) & is
treated by a combination of tetracycline + streptomycin or with rifampecin.
Plague is caused by Yersina or Pasturella pestis. It is transmitted from rats (carrier) by flees.
Tularemia: is transmitted by a bite of infected flees or ticks, the reservoir animals are rodents
(rats, rabbits, ) & semi-aquatic mammals (musk rats). It is treated by TC + streptomycin.
Mycobacterium infections
Tuberculosis: caused by Mycobacterium tuberculosis (G +ve bacilli), INH in prophylaxis.
Tuberculin test: is based on the fact that small amount of tuberculin, if injected in a
tuberculous subject will produce a local swelling at the site of injection.
Mantoux test: is the most accurate & sensitive type of tuberculin test.
Leprosy: is caused by Mycobacterium leprae & is treated with Dapson.
Spirochetes
Syphilis: is caused by Treponema pallidium (anaerobic rods / spirochetes) & can be treated
by benzyl penicillin. It is characterized by production of chancre.
Trench Mouth: is caused by Borrelia vincenti (spirochetes), normally found in the mouth
with Borrelia buccalis.
Leptospira icterohaemorrhagia: is the etiological agent of leptospirosis (Weils disease) &
cause infective jaundice in humans.
Viral & Rickettsial Infections: These differ from bacteria in that they do not survive
outside a living tissue, while bacteria can grow on synthetic media.
Rocky mountain spotted fever: is caused by Rickettsia rickettsi transmitted by ticks to man
& animals, & treated with chloramphenicol (CM) or Tetracyclines (TCs).
Endemic Typhus: caused by R. prowazikii & transmitted by lice; treated by CM or TCs.
Tetracyclines: are the most effective agents against rikettsial infections.
Mumps: the incubation period of mumps in humans is 14 21 days.
Koplicks spots: are white spots on mucous membranes & are associated with measles.
Passive immunization of contact children is made using gamma globulin.
Biavax II: is a mixture of living mumps & rubella viruses used for immunization (vaccine).
Hepatitis A: transmitted by food/water, droplet, direct personal contact, oral/fecal routes.
Hepatitis B is transmitted either through: Direct contact with blood & blood products or
Sexual transmission
Interferon: is a glycopeptide complex which inhibits viral replication.
Herpes simplex is a viral infection of the eyelid & conjunctiva. It is treated by iodoxuridine
eye ointment or drops (never given orally as it affects the DNA). It may also infect:
Oral cavity (through kissing) stomatitis.
Eyes (through contamination) kerato-conjunctivitis.
Penis & vulva (sexual intercourse) vesicular lesions (Herpes genitalis) associated
with cold sores or oral herpes simplex.
Fingers (through touching oral secretions) paranychia.
Skin (through droplet infection) vesicular lesions (chicken pox).
Herpes Zoster (schingles disease): is a neurotropic virus, transmitted through contact or
droplet infection acute CNS infection (posterior root ganglion) characterized by formation
of very painful vesicular eruptions in the area of the affected nerve.
Epstein-Barr Virus (EB virus): (Lysteria monocytogenes)
Is a herpes virus mononucleosis (# No of monocytes above normal).
Rabies: a viral infection characterized by CNS involvement paralysis & finally death. It
may be communicated to man through the bite of a rabid animal (saliva of a dog).
Iodoxuridine (Stoxil): is an antimetabolite that inhibits replication of viral DNA. It has
greater selectivity for viral (rather than host) DNA. It is the drug of choice for treating Herpes
Simplex of the eye lid & conjunctivitis (also for simplex kerotitis).
Vidrabine (Vira A): is an antiviral believed to inhibit viral replication & is effective against
herpes simplex eye infections.
Amantadine (Symmetrel): is a tri-cyclic antiviral (for influenza A)
Besides, it can be used to treat parkinsonism (it stimulates the release of dopamine).
Fungal Infections
Ring worm is a dermatophyte. Dermatophytes cause:
Tinea capitis in the scalp.
Tinea pedis cause athlete's foot.
Tinea ungium in nails (onchomycosis).
Tinea cruris in the groin.
Treatment of dermatophytes (ring worm):
Tolnaftate used in to treat tinea pedis as a dusting powder &/or cream. It is not
effective in candidiasis (only in dermatophytes).
Grisofulvin (only in dermatophytes). [ Also used to treat gout ].
Clotrimazol (Canesten) can also be used in treatment of candidiasis.
Miconazol (Daktarin) can also be used in treatment of candidiasis.
Ketonazol (Nizoral) can also be used in treatment of candidiasis.
Econazol can also be used in treatment of candidiasis.
Meconazol: is used to treat coccidio-mycosis & vaginally to control monilial infections.
Nystatin & Natamycin are only used to treat candidiasis but not dermatophytes.
Candicidin (Candeptin): is an antibiotic with a good antifungal action specially against
vaginal candidiasis.
Amphotrecin B: (obtained from streptomyces nodosus). It is related to aminoglycosides. It
acts on the cell membrane & is used to treat systemic fungal infections & deep mycosis.
Thrush is an inflammation of the buccal cavity caused by Candida albicans & is treated by
nystatin.
Barbiturates (microsomal enzyme inducers) $ the antifungal activity of grisofulvin.
Protozoal Infections
Trichomonas vaginalis is a flagellated protozoa, the causative agent for vaginitis. It is a
sexually transmitted disease that is treated by metronidazole vaginal suppositories after
menstruation. The normal pH of the vagina is 4.5 5. However during menstruation it
increases causing symptoms (of vaginitis) to appear.
Metronidazole (Flagyl): beside its anaerobic activity (can be used in clostridium deficile), it
is effective in amebiasis, giardiasis & trichomonas vaginalis. However it is not effective as an
antifungal.
Emetine HCl: has a direct lethal action on amebiasis.

Classification of Antibiotics
Cephalosporins: similar to broad spectrum penicillins but they are more stable to
penicillinases, thus they are used instead of penicillins in S. aureus infections.
Macrolides: These are the drugs of choice in patients with:
d Penicillin hypersensitivity d M. pneumoniae d Legionaries disease
Erythromycin can be used during pregnancy.
The oesteolate salt of erythromycin has higher blood levels than the stearate salt,
however it may cause cholestasis (since the erythromycin is excreted hepatically).
It is a good choice in patients with renal impairment.
Erythromycin oestolate: causes reversible cholestatic hepatitis with fever & jaundice (a
hypersensitivity reaction to the oestolate salt, thus the stearate salt is preferable).
Tetracyclines: These are bacteriostatic antibiotics.
They inhibit protein synthesis in the bacterial cell.
Most commonly used in patients with mixed infections (Ricketsial).
All tetracyclines suffer cross-sensitivity & cross-resistance.
Long-acting tetracyclines include Doxycycline (Vibramycin) & Minocycline
(Minocyn), used in RTIs.
Tetracyclines have the following adverse effects:
d GIT disturbances d Photosensitivity
d Fanconis syndrome: characterized by: nausea, vomiting, polyurea, acidosis. It
results from the administration of expired (out-dated) tetracyclines.
d Tooth discoloration: In children as a result of complex formation with Ca
++
.
Minocycline (Minocyn): is a long acting tetracycline used against resistant staph.
Minocycline & Doxycycline (Vibramycin): have much lower renal clearance rates
than tetracycline & are not effective in UTIs (Tetracycline HCl can be used in UTIs).
Chloramphenicol: These are bacteriostatic antibiotics.
They inhibit protein synthesis in the bacterial cell.
Most valuable in treatment of G +ve & G -ve infections (Salmonella, Rickettsia) & also
against ampicillin-resistant H. influenzae.
Adverse effects:
d Bone-marrow depression & blood dyscrasis including agranulocytosis (most
common) & idiosyncratic aplastic anemia (most fatal)
d Gray baby syndrome (in infants & preterm babies): immaturity of drug metabol-
izing enzymes (glucoronyl transferase) in infants excessive serum conc. of
unconjugated chloramphenicol maintained for several days circulatory collapse
Lincomycin (Lincocin) & Clindamycin (Dalacin): These are macrolide type antibiotics.
There use is restricted to anaerobic infections.
They cause serious diarrhea & colitis (pseudomembranous colitis).
Vancomycin: This is a bactericidal antibiotic with excellent G +ve coverage.
It is the drug of choice for MRSA / MRSE; it is too toxic for routine use.
Administered IV, except in cases of pseudomembranous colitis, where it is given orally.
Sulfonamides: these are bacteriostatic drugs that $ bacterial growth through competing with
PABA in folic acid synthesis (inhibit folic acid synthesis) (competitive antagonism). Folic
acid is an essential co-enzyme in the bacterial cell for the synthesis of nucleotides.
Can pass BBB (i.e. diffuse in the CSF).
Converted in the body to the non-substituted
aromatic amino gp. to have useful antibiotic activity.
Effective against G ve & G +ve bacteria.
Metabolized by acetylation of the p-amino gp.
Excreted through the kidney used in UTIs.
Side effects: Steven Johnsons syndrome, Agranulocytosis, photosensitivity.
d Succinyl Sulfathiazole: is a sulfonamide that is not absorbed from the GIT, used to
decrease intestinal bacteria.
d The most successful sulphonamides are the alicyclic type. If substituted, they will be
better absorbed.
Trimethoprim: is an enzyme inhibitor, inhibiting folate reductase enzyme prevents
conversion of dihydro-folic acid to tetrahydro-folic (folinic acid) (essential for DNA synthesis
in the bacterial cell). [Dihydro-folate reductase inhibitor].
Co-trimoxazole (Bactrim / Septrin): is a combination of sulfamethoxazole + trimethoprim.
Synergism exists between sulphonamides & trimethoprim against many bacterial spp.
Aminoglycosides: inhibit protein synthesis (30 S ribosome)
Are not absorbed from GIT (might be given orally to act locally in GIT infections).
Are useful in serious infections (e.g. gentamycin is the most useful in encephalitis).
Cause dose dependent nephro-toxicity.
Cause dose dependent oto-toxicity (damage of 8
th
cranial nerve esp. with streptomycin).
May produce neuromuscular blockade (may enhance the neuromuscular blockade of
skeletal muscle relaxants as succinylcholine & tubocurarine).
Drugs as gentamycin, kanamycin & tetracycline are excreted through the kidney by
glomerular filtration. Carbenicillin is excreted by renal tubular secretion.
Quinolones: e.g. norfloxacin, ciprofloxacin, pefloxacin, cinoxacin, enoxacin, naladixic acid,
oxalinic acid.
NH
2
SO
2
NH R
Mechanism of Action of Antibiotics
Inhibition of cell wall synthesis: These are bactericidal antibiotics.
d Penicillins d Cephalosporins d Vancomycin
d Bacitracin d Cycloserine d Carbapenems
Inhibition of cell membrane function: These are mostly antifungals.
d Amphotrecin B d Polymexin B d Nystatin
d Polyenes d Imidazoles d Colistin
Inhibition of protein synthesis:
d Tetracyclines (30 S) d Streptomycin (30 S) d Aminoglycosides (30 S)
d Macrolides (50 S) d Lincomycins (50 S) d Chloramphenicol (50 S)
Inhibition of nucleic acid synthesis:
d Quinolones d Actinomycin D d Clofazimine
d Rifampicin d Grisiofulvin d Pyrimethamine
Inhibition of folic acid synthesis:
d Sulfonamides d Trimethoprime d Dapson
N.B: Sulfonamides inhibit bacterial growth through competitive antagonism.
Classification of Penicillins
Acid-labile, Penicillinase-sensitive:
d Crystalline P d Procaine P d Benzathine P (L.A.)
d Ticarcillin d Carbanicillin
Acid-stable, Penicillinase-sensitive :
d Ampicillin d Amoxicillin d Phenoxy methyl P (P-V)
Acid-labile, Penicillinase-stable:
d Methicillin
Acid-stable, Penicillinase-stable :
d Oxicillin d Cloxacillin d Dicloxacillin
d Nafcillin
N.B: All penicillins, & their analogues exhibit cross-sensitivity.
Unit of Penicillin: This is the reference standard.
1 unit penicillin = the antimicrobial activity of 0.6 mg of USP sodium penicillin G.
500,000 units of penicillin G = 300 mg of penicillin, thus 1,600 units = 1 mg of
penicillin.
General Structure of Penicillin:
Substitution at R` affects the solubility
Salts are water soluble & can be given orally.
Esters (procaine / benzathine) are poorly soluble & must be given IM
Substitution at R affects the stability of the lactam ring
Acid-labile, Penicillinase-sensitive:

d Benzyl penicillin R =

d Carbanicillin R =
( a-carboxy-benzyl penicillin)

d Ticarcillin R =

N.B: Both Ticarcillin & Carbanicillin are broad spectrum (anti-pseudomonal) but are acid
labile (no oral form) & penicillinase sensitive.
H
N
COO R`
S
N
R CO
O
CH
2

CH
COOH

CH CH COO

S
Acid-stable, Penicillinase-sensitive:
d Ampicillin R =
( a-amino-benzyl penicillin)

d Amoxicillin R =
( p-hydroxy a-amino-benzyl penicillin)

d Phenoxy methyl P (P-V) R =
Acid-labile, Penicillinase-stable:
d Methicillin R =
( 2,6 dimethoxy phenyl penicillin)
The side chain confers b-lactamase stability

Acid-stable, Penicillinase-stable :
d Oxicillin R =
d Cloxacillin R =
d Dicloxacillin R =
d Nafcillin R =

O CH
2

CH
NH
2
HO
CH
NH
2
OCH
3
OCH
3
O
N
CH
3

CONH
O
N
CH
3

CONH
Cl
O
N
CH
3

CONH
Cl
Cl
OC
2
H
5
CONH
Penicillins are short acting: because of the high rate of tubular excretion.
Probenicid prolongs the action of penicillins. It prevents rapid excretion of penicillin in
proximal tubules (by competition).
Both probenicid & penicillin are acids & are uricosuric agents. In low doses they $ tubular
excretion of uric acid (competitive inhibition). However in higher doses they inhibit the re-
absorption of uric acid, # its excretion, thus can be used in gout.
There are 3 types of hypersensitivity reactions to penicillin:
Immediate Reaction: occurs within 20 min. & cause anaphylactic shock.
Accelerated reaction: occurs within 30 48 hrs & cause urticaria & laryngeal edema.
Delayed reaction: occurs after 3 days & usually involves urticaria.
Patients allergic to penicillin may show cross-sensitivity to cephalosporins & other beta-
lactams (they share the same beta-lactam ring).
10 20% demonstrate positive Coombs test.
Penicilloyl polylysine: is the substance used for skin test for penicillin allergy.
Penicillium Crysogenum: is a mould used commercially for production of Penicillin G.
Non-specific vaginitis: the organism most commonly involved is Haemophilus. It is treated
with ampicillin 500 mg q 6 hrs for 6 10 days.
Penicillins & cephalosporins: have no effect on mycoplasma because it has no cell wall.
Penicillin is hydrolyzed to penicilloic acid by the action of penicillinase enzyme.
Penicillin is not used in combination with erythromycin since both have similar spectra.



Immunity
Immunity can be classified as:
Active Immunity: is done by the administration of an antigen (which might be a toxoid
or an attenuated or killed bacteria). The body will develop its own antibodies as a
reaction to the injected antigen. Active immunity is of long duration.
The following biologicals are used for active immunization:
d Toxoid: e.g. tetanus.
d Killed bacteria (bacterial antigen): e.g. cholera or diphtheria.
d Live attenuated bacteria (bacterial vaccine): e.g. mumps or measles.
d Multiple antigen preparations.
Passive Immunity: Supply of ready made antibodies e.g. human immune serum
(antitoxin). This supplies rapid immunity but of short duration (2-3 weeks).
Additionally, it may cause allergy (being prepared from animal serum)
d Immune gamma-globulin: is administered IM providing passive immunity
which lasts for 1 2 months (e.g. infective hepatitis, chicken pox, measles).
d Antibodies in immunity: interact directly with, & neutralize toxins.
N.B: toxins are used as diagnostics, e.g. Schicks test for diphtheria.
Toxoids: these are obtained from culture filtrate of viable organisms & the exotoxins thus
obtained are treated with formaldehyde. The toxoid (inactive toxin) is used for active
immunization against some organisms.
Toxoids: d Are detoxicated toxins. d Are antigens.
d Are available in precipitated or adsorbed forms.
d Produce artificial active immunity. They need a booster dose
in order to sustain immunity (e.g. tetanus every 10 years).
Antitoxins: these are antibodies produced against bacterial toxins (or other toxins e.g.
scorpion or copra venoms). Antitoxins are usually bound to a globulin fraction of the animal
from which they were prepared & taken.
Antitoxins are given:
d IM or IV for therapeutic effects.
d IM or SC for prophylaxis.
Endogenous vaccines: are prepared from the patients own micro-organisms.
Adsorption of vaccines / toxoids allows for slow release & prolongs the presence of antigen.


Opsonins: these are antibodies that unite with bacteria facilitating their phagocytosis by
phagocytic cells.
Agglutinins: When an antibody unites with an antigen to form suspended particles. The
suspended antigens clamp together to form visible aggregates. This phenomenon is called
agglutination & the antibody is called agglutinin.
Precipitins: when an antibody unites with a colloidal solution of the corresponding antigen, a
precipitate (or visible floccules) will be formed & the antibody is called precipitin.
Complement Fixation: when the antibody unites with the corresponding antigen in presence
of a third nonspecific normal serum constituent known as complement. The antigen antibody
complex will attract & fix (or deviate) the complement in some way.
Bacteriolysins: these are antibodies that cause bacterial lyses through the fixation of
complement.
Bacteriotropines: these are antibodies that are not bactericidal, but they mobilize the body
defense against bacteria; i.e. promote phagocytosis.


Organism
Diphtheria

Tetanus
Pertusis
Cholera
T.B
Poliomyelitis V

Mumps, Measles
& Rubella
Rabies
Hepatitis B
Influenza

Snake Bite
Active Immunity
Toxoid (DPT)
(Diphtheria, Pertusis, Tetanus)
Toxoid (DPT)
Killed bacteria
Killed bacteria
Attenuated bacteria (BCG)
Attenuated viruses Trivalent
orally (Sabin)
Attenuated viruses
(MMR)
Killed virus
Killed virus
Killed virus
(elderly & cardiac pts)
Passive Immunity
Antitoxin, Globin

Anti-Tetanus Serum (ATS)





Gamma-globulin

Anti-rabies serum / immunoglobulin



Anti-venom
Small pox vaccine: is a killed vaccine. It is made by making a glycerol suspension of
vesicles of vaccinated animals.
Yellow fever vaccine (D17 vaccine): is a living attenuated vaccine, provides immunization
that lasts for less than 1 year. (Yellow fever is endemic in tropical climates).
Tetanus antitoxin: This should be given IM or SC & its effect lasts for 10 days.
Sabin vaccine (Polio): is a living attenuated vaccine used for immunization against polio
virus. It has a pink color & is administered orally. It is superior to Salk vaccine.
Rubella = German measles
Rabies Vaccine: (semple vaccine or Cow pox). It is a killed vaccine & to ensure this it must
be tested for being non-infectious in rabbits.
Immunization against rabies: Rabies immunoglobulin has the advantage of lower incidence
of allergic reactions compared to anti-rabies serum.
Influenza vaccine is given during October & November.
N.B: Typhoid fever is a bacterial infection. Viral infections include: polio, measles, mumps,
rabies & influenza, etc.
Peritonitis: caused by bacteroid fragilis (gm ve anaerobe) treated with clindamycin,
metronidazol, or Imipenem
Dental infection: caused by Streptococcus viridans, Group A streptococci; treated with
benzyl penicillin, procaine penicillin, penicillin G, Amoxicillin
Community acquired UTI: caused by E. coli, treated with gentamycin
Traveler diarrhea: caused by E. coli, Salmonella, or Shigella; treated with doxycyclin
metronidazol or co-trimazol. It can be prevented by drinking boiled water, avoiding raw food
???????????????????????????????
Pneumocystic Carinii: Fungal infection cause interstitial pt (causes pneumonitis in
infected elders & AIDS patient) treated by septrin
Lymes Disease: caused by Spirocharts, transmitted by rodents and deer by ticks bits. Treated
by tetracycline or ceftriaxone.
Pseudomembranous colitis: caused by Clostridium dificile, associated with the use of
clindamycin, ampicillin, ciproflaxin; treated by vancomycin.
Aminoglycoside vestibular gentamycin
auditory kanamycin , amikacin
Grisiovulvin inhibits the growth dermatophytes
3 6 months nail
3 6 weeks hair, skin
Oesteomyletis
Amoxicillin Cefixime (cephalosporins)
Penicillin /clindamycin /gentamycin
Otitis Media
Acute Recurrent
Amoxicillin Amoxi/clav
Pivampicillin Cefaclor
Septra Azithromycin
Pediozole or Septra
Meningitis
(3-6 months) H. influenza ampicillin or Ceftriaxone
(> 6 months or adult) S. pneumonia Penicillin G or Vancomycin
Neisseria Penicillin G or Ceftriaxone
UTI (acute uncomplicated): 1) Septra 2) Nitrofurantoin
3) Norflox. 4) Amox./clav 5) Cephalosporin
Vaginitis:
1) Bacterial: grey discharge + bad odor treatment clindamycin
2) Candida: cheesy discharge treatment nystatin / miconazole or chlotrimazole
3) Trichomonas: bad odor + pruritis + nurul
Anti-bacterial Drugs:
Bactericidal:
Beta-lactams (penicillins & cephalosporins) inhibit cell wall synthesis
Aminoglycosides bind to ribosomes
Quinolones inhibit DNA gyrase
Bacteriostatic:
Sulphonamides inhibit folic acid synthesis
Tetracyclines bind to ribosomes
Azoles bind to DNA
Macrolides (erythromycin) bind to ribosome
Chloramphenicol: interferes with protein synthesis by ribosomes (mainly bacteriostatic but
may be bactericidal # H. influenza, N. meningitides, bacteroides spp.)
Clindamycin: bind to bacterial ribosomes inhibits protein synthesis
Anti-viral Drugs
Drugs that directly impair virus replication
Acyclovir (Zovirax) Idoxuridine
Vidarabine Amantadine
Zidovudine (Retrovir) Ganciclovir
Drugs that modulate the host immune system
Interferons
Antifungal Agents
Polyene antibiotics bind to cell membrane leakage death
Amphotericin & Nystatin
Azoles
A) Imidazoles: Interfere with fungal oxidative enzymes # H
2
O
2
, Interfere with cell
wall??
Ketoconazole Miconazole Clotrimazole
Isoconazole Tioconazole Econazole
B) Triazoles: Damage fungal cell membrane: itraconazole, fluconazole
Others
Griseofulvin
flucytosine
1. Bacteria is characterized by the absence of:
a. Flagella c. Mitochondria
b. Neoclid d. Nucleus
2. Influenzae vaccine is:
a. Vaccine is from killed virus (for A & B but not C)
b. Vaccine is especially given to elderly & pts with heart disease
c. A new vaccine is developed each year
d. Period of infection is during the winter
e. Contains RNA
3. The most common organism in UTI is:
a. E. coli b. S. pyogenes
4. The most common organism in neonatal eye infections is:
a. P. aeruginosa b. S. aureus
5. The most common organism in neonatal conjunctivitis in Canada is:
a. Chlamydia tricmontosa c. S. aureus
b. P. aeruginosa d. Neisseria spp.
6. Which organism is not found in the ear:
a. Clostridium b. S. pneumoniae
7. If you get a smear from the middle ear, you expect to find:
a. Clostridium b. S. aureus c. E. coli
8. Metronidazole (Flagyl):
a. Can not be used as antifungal.
b. Not effective in gonorrhea.
c. Is used in the treatment of Trichomonas vaginalis
d. Is very potent in treating amoebiasis & giardiasis.
9. Nosocomial infections can be prevented by:
a. Hand washing c. Using aseptic technique
b. Isolation of infected pts d. Proper use of antibiotics
10. Which organism is least detected in neonatal meningitis:
a. H. influenzae b. S. aureus
11. Which organism is anaerobic:
a. Clostridium b. S. aureus c. Enterobacter
12. Which drug affects plasmids in micro-organisms:
a. Norfloxacin b. Cephalexin
Treated with gentamycin
Treated with silver nitrate
13. Which of the following bactericidal drugs cannot be given orally:
a. Streptomycin c. INH
b. PASA
14. Which of the following would be the best prophylaxis against TB:
a. INH c. Penicillin
b. Streptomycin
15. Mode of transmission of rabies (viral infections):
a. Saliva on an infected animal c. Direct contact
b. Inhalation of nasal secretions
16. Route of transmission of malaria (Plasmodium vivax, P. falciparum & P. malaria) is:
a. Mosquito bite b. Contact or droplet infection.
17. Which of the following agents is not an antifungal:
a. Tolnaftate. c. Metronidazol.
b. Miconazole.
18. Which of the following is considered to be an effect of the antibiotic on the host cell:
a. Affects the cell membrane b. Affects the cell wall
b. Affects folic acid metabolism c. None of the above
19. What damage is common to pathogen & host cell:
a. Cell membrane c. Cell wall
b. Cytoplasm
20. On which part of the penicillin molecule does the oxidase (or amidase) enzyme act:
a. The side chain b. The b-lactam ring.
21. On which part of the penicillin molecule does the penicillinase enzyme act:
a. The side chain b. The b-lactam ring.
22. Trichomonas vaginalis is similar to:
a. Flagellated protozoa c. H. vaginalis
b. G +ve bacteria d. G ve bacteria
23. The micro-organism with techoic acid in its cell wall is:
a. S. aureus c. E. coli
b. Chlamydia
24. Which of the following drugs can pass the BBB (or meningococcal encephalitis is best
treated by): confirm the answer ???
a. Penicillin. d. Cephalosporins. g. Vancomycin.
b. Tetracycline. e. Sulphadiazine.
c. Streptomycin f. Chloramphenicol.
25. The drug used in prophylaxis of malaria is:
a. Quinacrine c. Quinine
b. Chloroquine
26. Why is mycoplasma resistant to penicillin:
a. It is a G ve organism c. It is a penicillinase producer
b. It has no cell wall
27. What is the causative organism of scarlet fever:
a. S. pyogenes c. Rubella virus
b. S. aureus
28. Which antibiotic is penicillinase resistant but not acid resistant:
a. Methicillin c. Oxacillin
b. Ampicillin d. Nafcillin
29. Which antibiotic is acid resistant but not penicillinase resistant :
a. Methicillin c. Oxacillin
b. Ampicillin d. Nafcillin
30. Which antibiotic is both acid resistant & penicillinase resistant :
a. Dicloxacillin c. Oxacillin
b. Cloxacillin d. Nafcillin
31. Which organism causes mitral valve prolapse (endocarditis) & may cause infection during
tooth extraction:
a. S. viridans (a-hemolytic strept.) treated with penicillin V
b. S. aureus
32. Which of the following is classified as a broad-spectrum antibiotic:
a. Ampicillin c. Streptomycin.
b. Cloxacillin d. Penicillin G.
33. The organism against which either penicillin V or erythromycin can be prescribed is:
a. S. aureus c. S. pyogenes.
b. E. coli d. H. influenzae.
34. Influenza virus is transmitted by:
a. Respiration b. Direct contact
35. The difference between human & bacterial cell is:
a. Presence of cell wall b. Presence of cytoplasmic membrane
36. Conjunctivitis may be:
a. Viral c. Bacterial
b. Fungal d. Allergic
37. Acne is treated by:
a. Penicillin c. Fucidic acid
b. Tetracyclin
38. Chicken pox lesions are treated by:
a. Calamine c. Oak bath
b. Diphenhydramine
39. Schistozoma mansoni (most common in Africa) causes:
a. Liver cirrhosis
40. Which type of organism causes athletes foot:
a. Fungal (Tinea pedis) c. Protozoal
b. Bacterial d. Yeast
41. Which agent is used to treat atheletes foot:
a. Tolnaftate c. Metronidazole
b. Nystatin
42. Herpes I virus is transmitted by while Herpes II virus is transmitted by :
a. Respiration or lesions / direct contact
43. Which is synonymous to Herpes Zoster:
a. Schingles d. Herpes Simplex
44. Which is the causative organism of syphilis:
a. Triponema palladium
45. Botulism is due to:
a. Exotoxin b. Endotoxin
46. Which is true about UTI:
a. More common during pregnancy
b. Most commonly caused by E. coli
47. Which agent(s) is used to treat N. gonorrhea:
a. Penicillin G + Probenicid c. Tetracycline
b. Procaine penicillin
48. Mantoux test is similar to:
a. The old tuberculin test
49. Schistozomiasis is treated by:
a. Praziquental
50. Which of the following is (are) viral disease:
a. Polio c. Measeles
b. Rabies d. Influenza
51. Tape worm is treated by:
a. Niclosamide
52. Which of the following is an anthelmentic:
a. Pyrivenium pamoate c. Penicillin
b. Pyrantel pamoate d. Cephalosporins
53. Sulfamethoxazole & trimethoprim:
a. Have the same spectrum d. Taken with water
b. Have synergistic action e. Must be shaken before use
c. TMP is more potent with SMZ
54. Which type of organism causes shock syndrome:
a. S. aureus
55. Which agent is used for prophylaxis of meningitis:
a. Sulphonamides (sulfisoxazole)
56. In newborns, erythromycin is used to prevent blindness caused by:
a. Chlamydia
57. Nosocomial infections are caused by:
a. P. aeruginosa c. E. coli
b. S. aureus
58. Which organism causes granulomas:
a. M. tuberculosis
59. Bacteruria & pyuria are related to:
a. UTIs c. Nephritis
b. Renal failure d. Glomerulonephritis
60. Which of the following is (are) used as antifungal for scalp infections:
a. Miconazole c. Tar
b. Metronidazole
61. Which of the following is (are) true about trimethoprim:
a. Inhibits dihydrfolate reductase enzyme
b. Has a larger molecular size than folic acid
c. Has higher affinity for the receptors
62. Which of the following causes photo-sensitivity:
a. Penicillin c. Thyroxine
b. Sulfa d. Tertacycline
63. Which oral antibiotic is available as chewable tablets:
a. Amoxicillin
64. Metronidazole is effective in all except:
a. Amebiasis c. Giardiasis
b. Trichomoniasis d. Gonorrhea
65. Which of the following is not a predisposing factor to infection:
a. Congenital heart malformation
66. 1
st
stage syphilis is characterized by:
a. Chancre
67. Endocarditis is treated by:
a. Penicillin
68. Influenzae vaccine might cause allergy because:
a. It is a protein of a killed virus
69. Acyclovir is used in:
a. Herpes simplex b. HIV
70. Acyclovir is available as:
a. Tablets c. Topical
b. Syrup d. Injection
71. Probenicid .. the action of penicillin:
a. Potentiates
72. Al / Mg hydroxides .. the action of penicillin:
a. Inhibit
73. Herpes simplex:
a. Is schingeles disease c. Affects peripheral nervous system
b. Affects central nervous system
74. Pyogens are removed from water by:
a. Filtration b. Distillation
75. Meningitis in adults is caused by:
a. N. meningitidis
76. Which of the following does not cause genital infection:
a. Chlamydia
77. Which organism can cause eye infections in new borns leading to blindness:
a. N. gonorrhea b. E. coli
78. Penicillins have different spectra of activity because:
a. Difference in the side chains
79. TB may lead to:
a. Liquefied necrosis c. Gaseous necrosis
b. Gangrenous necrosis
80. Syphilis is treated by:
a. Penicillin + Probenicid
81. In community acquired pneumoniae, all can be used except:
a. Penicillin V
82. Diaper rash is complicated by:
a. Candida albicans
83. Hepatitis B is transmitted by:
a. Blood b. Sex c. Food
84. Hepatitis A is transmitted by:
a. Blood b. Sex c. Food
85. In antibiotic treatment, which is more affected:
a. PABA b. Folic acid c. Follinic acid
86. Penicillin is short acting because:
a. It has high rate of tubular excretion
87. Scabies can be treated by:
a. Gamma benzene hexachloride b. Benzoyl benzoate ?? c. Lindone ???
88. Aminoglycosides:
a. Cause nephro / oto toxicity c. Prophylaxis in intra-abdominal surgery
b. treat severe G ve infections d. Specific agents for G +ve infections
89. Which makes inclusion bodies with penicillin:
a. Cu b. Pb c. Zn d. Hg
90. Which of the following agents has the highest ability to penetrate bacterial cell wall:
Drug pKa
Methicillin 1.5
Oxacillin 2.0
Penicillin 3.0
Doxacillin 5.0
a. Doxacillin b. Methacillin
91. The drug of choice (DOC) for treating endocarditis due to methicillin resistant staph. is:
a. Vancomycin c. Cephazolin
b. Vancomycin + gentamycin
92. DOC in bronchitis is:
a. Amoxicillin or Septrin ??? b. Erythromycin (DOC)
93. DOC in Otitis Media:
a. Penicillins c. Erythromycin
b. Sulpha
94. DOC for anaerobic bacteria:
a. Penicillin (1st) b. Vancomycin (2nd)
95. DOC for H. influenzae:
a. Ampicillin or amoxicillin c. SMX
b. 2nd or 3rd generation cephalosporin
96. DOC for Streptococcus pyogens:
a. Penicillin c. Erythromycin
b. Cephalosporin
97. DOC for the treatment of Chlamydia:
a. Tetracycline (doxycyclin) b. Erythromycin
98. DOC for the treatment of Gonorrhea:
a. Cephalexin b. Cefuroxime
99. DOC for the treatment of peritonitis:
a. Clindamycin c. Lincomycin
b. Ciprofloxacin d. Metronidazole
100. DOC for the treatment of Mycoplasma pneumonia:
a. Tetracycline c. Erythromycin
b. Clindamycin
101. DOC for the treatment of a pregnant female with UTI:
a. Ampicillins c. Amoxicillin
b. Cephalexin