macrolides new
TRANSCRIPT
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MACROLIDES
ERYTHROMYCIN
ROXITHRIMYCIN CLARITHROMYCIN
AZITHROMYCIN
SPIRAMYCIN
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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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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
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Adverse effects
Gastrointestinal
Reversible hearing impairment
Hypersensitivity
Hepatitis (rare)
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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
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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
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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
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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
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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
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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
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