Beta-lactam antibiotics

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Beta-Lactamase Inhibitors

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Presentation transcript:

Beta-lactam antibiotics Pencillins Cephalosporines Carbapenems

Pencillin-History 1928- Alexander Fleming discovers a mold which inhibits the growth of staphylococcus bacteria 1940- penicillin is isolated and tested on mice by researchers at Oxford 1941- penicillin mass produced by fermentation for use by US soldiers in WWII 1950’s- 6-APA is discovered and semi-synthetic penicillins are developed. 1960’s -today- novel β-lactams/ β-lactamase inhibitors are discovered and modified from the natural products of bacteria

Pencillins &Cephalosporines β-lactam ring

How do they work? The β-lactam binds to Penicillin Binding Protein (PBP) PBP is unable to crosslink peptidoglycan chains The bacteria is unable to synthesize a stable cell wall The bacteria is lysed

Pencillin –Classifiication A.Natural penicillins Pencillin G (Benzyl pencillin) PencillinV (Phenoxy methyl pencillin) Benzathine Pencillin, Procaine Pencillin B. Pencillinase resistant pencillin Flucloxacillin, Cloxacillin Methicillin,Temociilin etc.

Pencillin –Classifiication C. Broad spectrum/extended spectrum pencillins. Aminopencillins:- Amoxycillin,Ampicillin,Bacampicillin etc. D. Antipseudomonal pencillins Carbencillin,Ticarcillin, Piperacillin,etc. E. Mecillinams Pivemecillinam HCL

Beta-Lactamase inhibitors Beta lactamase are a group of enzymes produced by many gram+ve,gram-ve bacteria that inactivate Beta-lactam antibiotics by opening the beta-lactam ring. There are 3 types of Beta lactamase inhibitors 1.Clavulinic acid 2.Sulbactum 3.Tazobactum

Examples Amoxycillin+clavulinic acid:- Augmentin,Co-amoxiclav,Enhancin,etc Piperacillin + tazobactum:- Tazocin, Zosyn etc Ticarcillin+sulbactum:- Timentin

Cephalosporines-Classification 1st Generation Cefradine,Cephalexin, Cefazolin,Cefadroxil 2nd Generation Cefoxitin, Cefuroxime, Cefaclor 3rd Generation Cefotaxime, Ceftriaxone,Cefixime, Ceftazidime,Cefperazone,Cefpodoxime,Cefdinir 4th Generation Cefepime,Cefpirome

Carbepenems& Monobactams Drugs are Imipenem Meropenem Doripenem Ertapenem Faropenem Imipenem:- inactivated in the kidney by some enzymes; combination with Cilastatin a specific enzyme inhibitor to block renal metabolism. Monobactam(monocyclic betalactam ring):- Aztreonam

Major adverse effects Hypersensitivity reactions :- Rashes, itching,urticaria,angioedema,bronchospasm, anaphlyaxis/serum sickness, Jarisch –Herxheimer rection Pain, Bleeding,Diarrhea,GI disturbances,Renal toxicity,neutropenia etc.

Thank u Philip k Mathew Clinical instructor School of Pharmacy University of Nizwa