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CLINDAMYCIN. Antibacterial activity Anaerobes, esp.Bacteroides fragilis . G+ve cocci , including penicillin- resistant Staph. Not effective against G- aerobes . Mechanism of action Inhibits protein synthesis ( 50 s subunit ). It’s not a macrolide. Pharmacokinetics
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CLINDAMYCIN Antibacterial activity Anaerobes, esp.Bacteroidesfragilis. G+vecocci, including penicillin- resistant Staph. Not effective against G- aerobes. Mechanism of action Inhibits protein synthesis ( 50 s subunit ) It’s not a macrolide
Pharmacokinetics • May be given orally, parenterally or topically. • Widely concentrated in tissues ( including bones ) & body fluids • It diffuses across the placenta but not BBB • 90% protein bound • Metabolized in liver( enterohepatic circulation), 10 % excreted unchanged • Both active drugs and active metabolites are excreted in urine and bile • t1/2 2.5 hr, prolonged in severe hepatic insufficiency
CLINDAMYCIN ( CONT. ) Clinical uses Limited because of pseudomembranouscolitis • Anaerobic infections caused by Bacteroids( metronidazole is preferred). • Staphylcoccal joint & bone infections such as osteomyelitis • Staph. Conjunctivitis ( eye drops ) • Diabetic foot infections • Acne ( 1% topical gel & lotion ) (has no side effects) • Treat penetrating wound (with AG or cephalosporins) • Prophylaxis of endocarditis • Pneumocystisjerovecii (with primaquine • Toxoplasmis of AIDS pts. (with pyremthamine) Side effects • Mainly GI disturbances: Diarrhoea is common • Psuedomembranous colitis (due to it’s eneterohepatic circulation, so it go &comeback to intestine. hence it will stay for longer time ) • Impaired liver function