1. Broad spectrum AMAs 2. Macrolides 3. Misc.

AMAs Class II
Dr.U.P.Rathnakar
MD.DIH.PGDHM
22

Protein synthesis inhibitors

1. Broad spectrum AMAs Tetracyclines Chloramphenicol 2. Macrolides

3. Misc. AMAs Clindamycin, Streptogramins, Linezolid Aminogycosides

Vancomycin{Cell wall[-]}

Topical agents [Varied MOA] Mupirocin Fusidic acid Polymyxin B, Colistin, Bacitracin, Tyrothricin 21

Identify broad spectrum pair

A. Clindamycin & Erythromycin B. Tetracycline & clindamycin C. Chloramphenicol & vancomycin D. Tetracycline & Chloramphenicol

19

Protein synthesis inhibitor does not include

A. Chloramphenicol B. Vancomycin C. Aminoglycoside D. Oxytetracycline

18

Drug which prevents binding of tRNA to 30s ribosome at A site isA. Doxycycline B. Aminoglycoside C. Chloramphenicol D. Clindamycin
17

Anti ADH tetracycline isA. Doxycycline B. Tetracycline C. Demeclocycline D. Oxytetracycline

16

Highly lipid soluble TC isA. Doxycycline B. Tetracycline C. Demeclocycline D. Minocycline

15

TC administered once a day isA. Tetracycline B. Oxytetracycline C. Demeclocycline D. Doxycycline

14

TC which causes vestibular toxicity isA. Minocycline B. Tetracycline C. Doxycycline D. Demeclocycline

13

MOA of chloramphenicol isA. Inhibit binding at A site B. Inhibit amino acid transfer C. Inhibit translocation

12

TC which is safer in renal impairment isA. Doxycycline B. Demeclocycline C. Tetracycline D. Oxytetracycline

11

Gray baby syndrome is caused by

A. Chloramphenicol B. Demeclocycline C. Tetracycline D. Oxytetracycline
11

TCs are contraindicated inA. Pregnancy B. Lactation C. Children D. All of the above
11

Macrolides
With a macrocyclic lactone ring with attached sugars Erythromycin Roxithromycin, Clarithromycin and Azithromycin
Spiramycin [To prevent trans placental transmission of toxoplasmosis]

10

Macrolides
Erythromycin, Azithro, Clarithro, Roxithromycin]

W A
AG

tRNA

mRNA

Macrolides [Erythromycin-prototype] MOA

Bacteriostatic cidal [higher concn] Enters by active transport It combines with 50S ribosome subunit and interferes with translocation.

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 and chloramphenicol -binding sites for all these are next to each other.
7

Erythromycin-spectrum
S.Pyogenes, S.pneumoniae, n.gonnorrhoeae, clostridia, C.diphtheria, listeria- Erythromycin and penicillin Campylobacter, mycoplasma, pertusis, chlamydia, N.meningitidis- E.mycin

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]

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]
4

Erythromycin uses
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

Erythro
Source Efficacy Duration of action Oral
Dosage DI

Roxi
++ 12
Stable 150BD No

Clari
++ Long
Stable 250BD Yes
As erythro + MAC Leprosy H.Pylori [triple drug]

Azithro
Semisynth ++ Long
Stable

Natural + 6h
Enteric coated 500mgQID yes
Chlamydia Pertusis

Semisynth Semisynth

[Food does not interfere]

500 OD No

Spectrum M.Pneumonia Leginnaires & Uses

Tetanus Strepto Staphylo

As erythro

As erythro + MAC LGV H.Influenza Salmonella Malaria 22 2

Toxoplasmosis

Advantages of azithromycin over E.mycin

Acid stable Single dose/day Wider spectrum No drug interactions

Disadvantage-should not be administered in pregnancy

23

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 slightly prolong the QTc HEPATOTOXIC [restricted use] Visual disturbances CI in myasthenia gravis