Cephalosporins

Pharmacology of antibiotic cephalosporins. Mechanism of action, pharmacokinetics, uses and adverse effects

1. Cephalosporins

2. Introduction Cephalosporins are Beta-lactam antibiotics. Source : Cephalosporium acremonium , a fungus Later synthetic cephalosporins were developed. They are divided into four generations based on their general features and antibacterial activity.

3. Mechanism of action Cephalosporins Inhibits transpaptidase Preventsts peptidoglycan synthesis Cell wall deficient forms( Spheroplasts and filamentous forms) Autolysis Cell death

4. Pharmacokinetics Administration : Oral or parenteral distribution: Throughout the body Metabolism: Some drugs are metabolized in liver via deacetylation but most of the drugs remain unchanged. Excretion: Excreted unchanged through kidney either by glomerular filtration or by tubular secretion. Deacetylated Cefotaxime is excreted through bile.

5. Source: Pharmacology of dentistry

6. Adverse effects Hypersensitivity : They are skin rashes, urticaria and rarely anaphylaxis. Gastrointestinal disturbances: D iarrhoea , vomiting and anorexia. Pain at the site of i.m . injection mainly with cephalothin . Intravenous cephalosporins can cause thrombophlebitis . Nephrotoxicity may occur. Co-administration of cephalothin and gentamicin increases the nephrotoxicity . Intolerance to alcohol (a disulfi ram-like reaction) has been reported with cefotetan and cefoperazone . Severe bleeding can occur either due to hypoprothrombinaemia (which responds to vitamin K therapy ) or thrombocytopaenia and/or platelet dysfunction.

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