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MACROLIDES

ERYTHROMYCIN

ROXITHRIMYCIN CLARITHROMYCIN

AZITHROMYCIN

SPIRAMYCIN

8/3/2019 Macrolides New

4/20

Mechanism of Action Bacteriostatic at low dose, cidal at high

concentrations

Acts by inhibiting protein synthesis

Binds with 50s ribosome interferes with

translocation premature termination of peptidechain suppression of protein synthesis

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5/20

Mechanism of Action

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Pharmacokinetics

Acid labile

Widely distributed in the body

Short half life

Excreted in bile in the active form

8/3/2019 Macrolides New

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Adverse effects

Gastrointestinal

Reversible hearing impairment

Hypersensitivity

Hepatitis (rare)

8/3/2019 Macrolides New

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UsesAs an alternative to penicillin streptococcal

pharyngitis, tonsillitis, mastoiditis, prophylaxisof rheumatic fever and SABE

FIRST CHOICE DRUG in atypical pneumonia,whooping cough and chancroid

SECOND CHOICE DRUG in campylobacterenteritis, legionnaires pneumonia, chlamydiatrachomatis infection of urogenital tract

8/3/2019 Macrolides New

11/20

Roxithromycin Semi-synthetic

Acid stable macrolide

Good enteral absorption and tissue penetration

Used as an alternative to erythromycin forrespiratory, ENT, skin and soft tissue and genitaltract infections

8/3/2019 Macrolides New

12/20

Clarithromycin

AMS resembles erythromycin, also includes MAC,atypical mycobacteria and some anaerobes

Used as a component of triple drug regimen iteradicates H.pylori in 1-2 weeks

8/3/2019 Macrolides New

13/20

Azithromycin Expanded spectrum

Improved pharmacokinetics acid stability, rapidoral absorption, marked tissue distribution andintracellular penetration

Once a dosing

Uses- legionnaires pneumonia, chlamydiatrachomatis infection of urogenital tract

8/3/2019 Macrolides New

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Lincosamides Clindamycin, Lincomycin

Inhibits protein synthesis by binding to 50s ribosome

Highly active against anaerobes and mixed infections

SE- diarrhoea, pseudomembranous colitis

8/3/2019 Macrolides New

16/20

8/3/2019 Macrolides New

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Glycopeptide antibioticsVancomycin, Teicoplanin

Acts by inhibiting cell wall synthesis

Active against MRSA, Strep. Viridians, Enterococcusand Cl. Difficle

Systemic toxicity high RED MAN SYNDROMEwithvancomycin

8/3/2019 Macrolides New

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