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Basic Sciences

Tutorial 179

The Role Of The Liver In Drug Metabolism

Jeanne Louise Schonborn, CT2 Anaesthesia

Derriford Hospital, Plymouth

Carl Gwinnutt, Consultant Anaesthetist

Hope Hospital, Salford

Correspondence to jeannelouise1@btinternet.com

17th MAY 2010

Abstract

Overall aim of drug metabolism is to produce a more water-soluble compound that can be excreted in urine & bile.

Drug metabolites can have the same, increased or decreased activity compared to parent compound.

The liver is the most metabolically active tissue

The microsomes of the smooth endoplasmic reticulum are the site of metabolism in liver.

The cytochrome P450 system is the predominant enzyme system. Other non-P450 enzymes are also involved however.

Divided into Phase 1 & Phase 2 metabolism.

Phase1 reactions include oxidation, reduction & hydrolysis.

Phase 2 reactions are conjugation reactions.

Drug interactions can influence the rate of drug metabolism

Genetic polymorphisms do exist