The hepatic cytochrome P450 system plays an important role in the metabolism of drugs by converting them from hydrophobic to more easily excreted hydrophilic forms. The biotransformation reactions can generally be divided into cytochrome P450-dependent phase I and phase II binding reactions. Within the last few years it has become clear that extrahepatic metabolism of drugs plays a role in the total degradation of drugs in vivo. Biotransformation in the gastrointestinal tract is very important as it reduces the bioavailability of orally administered drugs. Genetic polymorphisms, enzyme inhibition, enzyme induction, and physiologic factors can cause alterations in cytochrome P450 activity. This has some clinical implications as it can cause alterations in drug pharmacokinetics, lead to changes in drug efficacy, increase drug toxicity due to decreased metabolism or increased production of toxic metabolites, and lead to drug interactions.

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