Basic Sciences
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
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