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Beta lactams

Beta lactams. INHIBITORS OF CELL WALL SYNTHESIS. Natural: Pencillinase Resistant: (Anti staph ) Benzyl pencillin (G) k+ Na+ 1) oxcillin Procaine pencillin (G) 2) Nafcillin Benzathine pencillin (G) 3) Cloxacillin

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Beta lactams

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  1. Beta lactams

  2. INHIBITORS OF CELL WALL SYNTHESIS

  3. Natural: Pencillinase Resistant: • (Anti staph) • Benzyl pencillin (G) k+ Na+ 1) oxcillin • Procaine pencillin (G) 2) Nafcillin • Benzathine pencillin (G) 3) Cloxacillin • Phenoxymethyl pencillin (V) 4) Dicloxacillin

  4. Broad spectrum : Extended spectrum: • (Amino) (Antipseudomonal) • Ampicillin A) Carboxypenicillin: carbenicillin, Indanyl • carbencillin, Ticarcillin • 2) Amoxicillin • Bacampicillin B) Ureidopencillin: • Mezlocillin Pipercillin

  5.  - lactamase inhibitor Combination: 1) Amoxicillin + Clavulanate 2) Ticarcillin + Clavulanate 3) Ampicillin + sulbactum 4) Piperacillin + Tazobactum

  6. Unique - Lactams:- • Monobactams – Aztreonam • Carbapenems – imipenem & Meropenem • Doripenem & Ertapenem

  7. Glycopeptides:-Vancomycin Dalbavancin Teicoplanin Telavancin Others:- Daptomycin Fosfomycin Bacitracin Cycloserine

  8. Cephalosporins:- 1st gen: Cefadroxil (PO) Cephalexin Cephradime (PO) Cefazolin IV.

  9. 2nd: Cefuroxime, (IV) – H influenzae Cefuroxime Axetill (PO) , Cefaclor , loracarbef Cefoxitin (IV) – B fragilis Cefotetan (IV) Cefmetazole

  10. 3rd :- Cefotaxime Cefoperazone Cefdinir Ceftazidime Cefixime Ceftibuten Ceftriaxone Cefpodoxime Moxalactum 4th: Cefepime

  11. – Lactams – cell wall synthesis.Peptidoglycan matrix (Gram +ve more, – ve less).Glycan → NAG + NAM +Pentapeptide.  1,4 linkage.Final stage → cross – linking  transpeptidase enzyme

  12. D- ala – D -ala + trans peptidase. D- ala + acylenzyme intermediate + free amino group of pentapeptide of adjacent chain ↓ transpeptidase regenerated.

  13. Transpeptidases – PBPs, - 5 in Gram +ve, 6 in Gram – ve • Bacterial swell & bursts • Long filamentous structure – fragment • Autolysins • Resistance:-  - lactamase • - failure to reach target PBP • - failure to bind to target PBP.

  14. 1 unit = 0.6 micro gram of crystalline sodium salt of Pencillin G. Penicillin G & V: Kinetics -Oral - Parenteral - Distribution - Excretion

  15. Uses: • Pneumococcal infections • Streptococcal infections • Streptococcal toxic shock & necrotizing fasciitis. • Strept pneumonia, arthritis, meningitis, Endocarditis • Other sterptococci: Viridans; Endocarditis

  16. 6) Anaerobes 7) Streptococcal infections 8) Meningococcal infections 9) Syphilis 10) Actinomycosis 11) Diptheria 12) Gas gangrene

  17. 13) Gingivostomatitis 14) Rat bite fever 15) L. monocytogenes 16) Lyme’s disease 17) Erysipeloid Prophylactic uses: 1) Streptococcal infections 2) Syphilis

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