beta lactams. inhibitors of cell wall synthesis natural: pencillinase resistant: (anti staph)...
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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) Amoxicillin3)Bacampicillin B) Ureidopencillin: Mezlocillin Pipercillin
- lactamase inhibitor Combination:- lactamase inhibitor Combination:
1) Amoxicillin + Clavulanate1) Amoxicillin + Clavulanate
2) Ticarcillin + Clavulanate2) Ticarcillin + Clavulanate
3) Ampicillin + sulbactum3) Ampicillin + sulbactum
4) Piperacillin + Tazobactum4) Piperacillin + Tazobactum
Unique - Lactams:-
1)Monobactams – Aztreonam
2)Carbapenems – imipenem & Meropenem
Doripenem & Ertapenem
Glycopeptides:- Vancomycin Dalbavancin
Teicoplanin Telavancin
Others:- Daptomycin
Fosfomycin
Bacitracin
Cycloserine
Cephalosporins:-
1st 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
3rd :- 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