Human P450 metabolism of warfarin.

New York State Department of Health, Wadsworth Center, USA.

Pharmacology & therapeutics 1997

The anticoagulant drug warfarin occurs as a pair of enantiomers that are differentially metabolized by human cytochromes P450 (CYP). R-warfarin is metabolized primarily by CYP1A2 to 6- and 8-hydroxywarfarin, by CYP3A4 to 10-hydroxywarfarin, and by carbonyl reductases to diastereoisomeric alcohols. S-warfarin is metabolized primarily by CYP2C9 to 7-hydroxywarfarin. Potential warfarin-drug interactions could occur with any of a very wide range of drugs that are metabolized by these P450s, and a number of such interactions have been reported. The efficacy of warfarin is affected primarily when metabolism of S-warfarin is altered.