Beta lactams
INHIBITORS OF CELL WALL SYNTHESIS
Natural: Pencillinase Resistant: (Anti staph) 1)Benzyl pencillin (G) k+ Na+1) oxcillin 2)Procaine pencillin (G) 2) Nafcillin 3)Benzathine pencillin (G)3) Cloxacillin 4)Phenoxymethyl pencillin (V)4) Dicloxacillin
Broad spectrum : Extended spectrum: (Amino) (Antipseudomonal) 1)Ampicillin A) Carboxypenicillin: carbenicillin, Indanyl carbencillin, Ticarcillin 2) Amoxicillin 3)Bacampicillin B) Ureidopencillin: Mezlocillin Pipercillin
- lactamase inhibitor Combination: 1) Amoxicillin + Clavulanate 2) Ticarcillin + Clavulanate 3) Ampicillin + sulbactum 4) Piperacillin + Tazobactum
Unique - Lactams:- 1)Monobactams – Aztreonam 2)Carbapenems – imipenem & Meropenem Doripenem & Ertapenem
Glycopeptides:- Vancomycin Dalbavancin Teicoplanin Telavancin Others:- Daptomycin Fosfomycin Bacitracin Cycloserine
Cephalosporins:- 1 st gen: Cefadroxil (PO) Cephalexin Cephradime (PO) Cefazolin IV.
2nd: Cefuroxime, (IV) – H influenzae Cefuroxime Axetill (PO), Cefaclor, loracarbef Cefoxitin (IV) – B fragilis Cefotetan (IV) Cefmetazole
3 rd :- Cefotaxime Cefoperazone Cefdinir Ceftazidime Cefixime Ceftibuten Ceftriaxone Cefpodoxime Moxalactum 4th: Cefepime
– Lactams – cell wall synthesis. Peptidoglycan matrix (Gram +ve more, – ve less). Glycan → NAG + NAM + Pentapeptide. 1,4 linkage. Final stage → cross – linking transpeptidase enzyme
D- ala – D -ala + trans peptidase. D- ala + acylenzyme intermediate + free amino group of pentapeptide of adjacent chain ↓ transpeptidase regenerated.
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.
1 unit = 0.6 micro gram of crystalline sodium salt of Pencillin G. Penicillin G & V: Kinetics -Oral - Parenteral - Distribution - Excretion
Uses: Pneumococcal infections 1.Streptococcal infections 2.Streptococcal toxic shock & necrotizing fasciitis. 3.Strept pneumonia, arthritis, meningitis, Endocarditis 4.Other sterptococci: Viridans; Endocarditis
6) Anaerobes 7) Streptococcal infections 8) Meningococcal infections 9) Syphilis 10) Actinomycosis 11) Diptheria 12) Gas gangrene
13) Gingivostomatitis 14) Rat bite fever 15) L. monocytogenes 16) Lyme’s disease 17) Erysipeloid Prophylactic uses: 1) Streptococcal infections 2) Syphilis