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1. Broad spectrum AMAs
2. Macrolides
3. Misc. AMAs
Class II
Dr.U.P.RathnakarMD.DIH.PGDHM
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Protein synthesis inhibitors
21
1. Broad spectrum AMAsTetracyclines
Chloramphenicol
2. Macrolides
3. Misc. AMAs
Clindamycin,
Streptogramins,
Linezolid
Vancomycin{Cell wall[-]}
Topical agents [Varied MOA]
Mupirocin
Fusidic acid
Polymyxin B, Colistin, Bacitracin, Tyrothricin
Aminogycosides
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Identify broad spectrum pair
A. Clindamycin & Erythromycin
B. Tetracycline & clindamycin
C. Chloramphenicol & vancomycinD. Tetracycline & Chloramphenicol
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Protein synthesis inhibitor does not include
A. Chloramphenicol
B. Vancomycin
C. AminoglycosideD. Oxytetracycline
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Drug which prevents binding of tRNA to
30s ribosome at A site is-
A. Doxycycline
B. Aminoglycoside
C. ChloramphenicolD. Clindamycin
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Anti ADH tetracycline is-
A. Doxycycline
B. Tetracycline
C. DemeclocyclineD. Oxytetracycline
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Highly lipid soluble TC is-
A. Doxycycline
B. Tetracycline
C. DemeclocyclineD. Minocycline
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TC administered once a day is-
A. Tetracycline
B. Oxytetracycline
C. Demeclocycline
D. Doxycycline
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TC which causes vestibulartoxicity is-
A. Minocycline
B. Tetracycline
C. DoxycyclineD. Demeclocycline
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MOA of chloramphenicol is-
A. Inhibit binding at A site
B. Inhibit amino acid transfer
C. Inhibit translocation
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TC which is safer in renal
impairment is-A. Doxycycline
B. DemeclocyclineC. Tetracycline
D. Oxytetracycline
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Gray baby syndrome is caused by
A. Chloramphenicol
B. DemeclocyclineC. Tetracycline
D. Oxytetracycline
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TCs are contraindicated in-
A. Pregnancy
B. LactationC. Children
D. All of the above
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Macrolides
With a macrocyclic lactone ring withattached sugars
Erythromycin
Roxithromycin,
Clarithromycin and
Azithromycin
Spiramycin [To prevent trans placental transmission of toxoplasmosis]
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9
AG
EP A
mRNA
tRNAW
MacrolidesErythromycin, Azithro, Clarithro, Roxithromycin]
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Bacteriostaticcidal [higherconcn]
Enters by active transport It combines with 50Sribosome
subunit and interferes with
translocation.
8
Macrolides [Erythromycin-prototype]
MOA
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Erythromycin
Bacterial resistance Less permeable to erythromycin
Acquire the capacity to pump it out.
Enterobacteriaceae have been found to produce
an erythromycin esterase. Alteration in the ribosomal binding site for
erythromycin
Cross resistance with clindamycin andchloramphenicol -binding sites for all these arenext to each other.
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Erythromycin-spectrum
S.Pyogenes, S.pneumoniae,
n.gonnorrhoeae, clostridia, C.diphtheria,
listeria- Erythromycin and penicillin
Campylobacter, mycoplasma, pertusis,
chlamydia, N.meningitidis- E.mycin
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Erythromycin
PK Erythromycin base is acid labile. - enteric coated tablets,
Food delays absorption
Does not cross BBB-crosses placenta
Partly metabolized and excreted primarily in bile in the
active form.
Renal excretion is minor;
Dose need not be altered in renal failure.
Enzyme inhibitor CYP3A4 Erythromycin stimulates motilin receptors in the g i t -
thereby induces gastic contractions, hastens gastric
emptying and promotes intestinal motility [used
postoperatively to promote peristalsis]5
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Erythromycin
ADEs & DIs GIT
Hypersensitivity [Skin and hepatic]
Chlolestatic jaundice [E.estolate-acid stable]
DIs [Erythro and Clarithro]
Enzyme inhibitor [ toxicity of theophylline,
carbamazepine, valproate, warfarin, digoxin etc
VT with cisapride, astemizole, terfenadine Ototoxicity in high doses
Pregnancy- E.mycin safe [Others may not be]
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Erythromycin uses
3
First choice
1. Mycoplasma pneumonia
2. Whooping cough
3. Chancroid
Alternative to penicillin
1. Str. Pharyngitis [Rh.fever]
2. Diphtheria, Tetanus
3. Syphilis
4. Leptospirosis
Non-infective uses
1. Antiinflammatory-rarely used-decreases cytokines
2. Improve post op. gastric emptying
E th R i Cl i A ith
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Erythro Roxi Clari AzithroSource Natural Semisynth Semisynth Semisynth
Efficacy + ++ ++ ++Durationof action
6h 12 Long Long
Oral Enteric
coated
Stable Stable Stable[Food does not
interfere]
Dosage 500mgQID 150BD 250BD 500 OD
DI yes No Yes No
Spectrum
& Uses
M.Pneumonia
LeginnairesChlamydiaPertusisTetanusStrepto
Staphylo
As
erythro
As erythro +
MACLeprosyH.Pylori[triple drug]
As erythro +
MACLGVH.InfluenzaSalmonella
MalariaToxo lasmosis2
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Advantages of azithromycin
over E.mycin Acid stable
Single dose/day
Wider spectrum No drug interactions
Disadvantage-should not be administeredin pregnancy
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KETOLIDES
Telithromycin & Cethromycin
Ketolides are semisynthetic14-membered-ring macrolides
Macrolide-resistant strains are susceptible to ketolides because
- structural modification renders them poor substrates for efflux
pump-mediated resistance and they bind to ribosomes of some
bacterial species with higher affinity than macrolides
Inhibitor of the CYP3A4 enzyme system and may slightlyprolong the QTc
HEPATOTOXIC [restricted use]
Visual disturbances
CI in myasthenia gravis 1
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