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BETA-LACTAM ANTIBIOTICS

BETA-LACTAM ANTIBIOTICS. BETA-LACTAM ANTIBIOTICS. PENICILLINS CEPHALOSPORINS MONOBACTAMS CAEBAPENEMS. PENICILLINS. Originally obtained from penicillin notatum Fused thiazolidine and beta lactam rings - side chains attached amide linkage

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BETA-LACTAM ANTIBIOTICS

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  1. BETA-LACTAM ANTIBIOTICS

  2. BETA-LACTAM ANTIBIOTICS • PENICILLINS • CEPHALOSPORINS • MONOBACTAMS • CAEBAPENEMS

  3. PENICILLINS • Originally obtained from penicillin notatum • Fused thiazolidine and beta lactam rings- side chains attached amide linkage • Structural integrity of the 6-aminopenicillanic acid nucleus is essential for the biologic activity • Interferes with synthesis of bacterial cell wall

  4. Penicillin G

  5. Antibacterial spectrum • Cocci: streptococci, pneumococci, N.gonnorrhoea, N.meningitidis • Bacilli : B.anthracis, clostridia, listeria, spirochetes, corynebacterium diphtheriae

  6. Bacterial resistance • Elaboration of penicillinase • Alteration in target proteins (PBP) reducing affinity • Impermeability to antibiotic or its efflux

  7. Pharmacokinetics • Acid labile • Distributed extracellularly • Excreted through kidney

  8. Adverse effects • Local irritancy : pain at IM injection site, thrombophlebitis • Hypersensitivity : rash, itching, urticaria, fever, wheezing, edema, serum sickness, exfoliative dermatitis, anaphylaxis

  9. Clinical Uses • Pneumococcal Infections • Streptococcal Infections. • Staphylococcal Infections • Meningococcal Infections • Gonococcal Infections • Syphilis. • Diphtheria. • Anthrax • Tetanus & gangrene

  10. Penicillin V • Acid resistant alternative • Oral absorption better

  11. PENICILLINASE RESISTANT PENICILLINS Methicillin , Cloxacillin • AMINOPENICILLINS Ampicillin, bacampicillin, amoxicillin • CARBOXYPENICILLIN carbenicillin, ticarcillin • UREIDOPENICILLIN piperacillin

  12. Ampicillin • Spectrum: gram positive & gram negative • Not degraded by gastric acid • Oral absorption incomplete • Food interferes with absorption • A/E : diarrhoea, rashes • Uses : UTI, RTI, meningitis, gonorrhoea, typhoid, bacillary dysentry

  13. Amoxicillin • Close congener of ampicillin • Oral absorption is better • Less incidence of diarrhoea • Bronchitis, urinary infections, SABE, gonorrhoea

  14. Cephalosporins • Semisynthetic antibiotics derived from cephalosporin- C : cephalosporium • Beta- lactum ring fused to dihydrothiazine ring • Bactericidal

  15. Classification • First Generation: Cefazolin , cephalothin, Cephalexin ,Cefadroxil,Cephradine • Second generation : cefuroxime, cefoxitin, cefaclor, cefuroxime axetil • Third generation : Cefotaxime, Ceftriaxone, Cefdinir,  Ceftibuten, Cefpodoxime proxetil, Ceftizoxime ,Cefoperazone Ceftazidime • Fourth generation : cefepime, cefpirome

  16. Adverse effects • Pain after IM inj. • Diarrhoea • Hypersensitivity reactions • Nephrotoxicity • Bleeding • Neutropenia • Thrombocytopenia • Disulfiram like reaction

  17. uses • Respiratory, Urinary, soft tissue infections • septicemias • Surgical prophylaxis • Meningitis • Gonorrhoea • Typhoid • Hospital acquired infection

  18. MONOBACTAMS

  19. MONOBACTAMS • Aztreonam • Monocyclic beta-lactam ring • Resistant to beta-lactamases • No activity against gram positive & anaerobes • Active against gram negative rods • Hospital acquired infections originating from urinary, biliary, GI & female genital tracts

  20. CARBAPENAMS

  21. CARBAPENAMS • Imipenem, meropenam, faropenam • Potent & broad spectrum • Resistant to beta-lactamase • Combined with cilastatin • Serious hospital acquired infections- neutropenic, cancer, AIDS patient

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