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