beta lactams. inhibitors of cell wall synthesis natural: pencillinase resistant: (anti staph)...
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Beta lactams
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INHIBITORS OF CELL WALL SYNTHESIS
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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
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Broad spectrum : Extended spectrum: (Amino) (Antipseudomonal)1)Ampicillin A) Carboxypenicillin:
carbenicillin, Indanyl carbencillin, Ticarcillin
2) Amoxicillin3)Bacampicillin B) Ureidopencillin: Mezlocillin Pipercillin
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- 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
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Unique - Lactams:-
1)Monobactams – Aztreonam
2)Carbapenems – imipenem & Meropenem
Doripenem & Ertapenem
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Glycopeptides:- Vancomycin Dalbavancin
Teicoplanin Telavancin
Others:- Daptomycin
Fosfomycin
Bacitracin
Cycloserine
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Cephalosporins:-
1st gen: Cefadroxil (PO)
Cephalexin
Cephradime (PO)
Cefazolin IV.
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2nd: Cefuroxime, (IV) – H influenzae
Cefuroxime Axetill (PO) , Cefaclor ,
loracarbef
Cefoxitin (IV) – B fragilis
Cefotetan (IV)
Cefmetazole
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3rd :- Cefotaxime Cefoperazone Cefdinir
Ceftazidime Cefixime Ceftibuten
Ceftriaxone Cefpodoxime Moxalactum
4th: Cefepime
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– Lactams – cell wall synthesis. Peptidoglycan matrix (Gram +ve more, – ve less). Glycan → NAG + NAM +Pentapeptide. 1,4 linkage.Final stage → cross – linking transpeptidase enzyme
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D- ala – D -ala + trans peptidase.
D- ala + acylenzyme intermediate
+ free amino group of pentapeptide of adjacent chain
↓
transpeptidase regenerated.
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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.
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1 unit = 0.6 micro gram of crystalline sodium salt of Pencillin G.
Penicillin G & V: Kinetics -Oral
- Parenteral
- Distribution - Excretion
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Uses:Pneumococcal infections
1.Streptococcal infections
2.Streptococcal toxic shock & necrotizing fasciitis.
3.Strept pneumonia, arthritis, meningitis, Endocarditis
4.Other sterptococci: Viridans; Endocarditis
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6) Anaerobes
7) Streptococcal infections
8) Meningococcal infections
9) Syphilis
10) Actinomycosis
11) Diptheria
12) Gas gangrene
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13) Gingivostomatitis
14) Rat bite fever
15) L. monocytogenes
16) Lyme’s disease
17) Erysipeloid
Prophylactic uses: 1) Streptococcal infections
2) Syphilis