Kaminsky L S, Zhang Z Y
New York State Department of Health, Wadsworth Center, USA.
Pharmacol Ther. 1997;73(1):67-74. doi: 10.1016/s0163-7258(96)00140-4.
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.
抗凝血药物华法林以一对对映体的形式存在，它们被人类细胞色素P450（CYP）以不同方式代谢。R-华法林主要通过CYP1A2代谢为6-和8-羟基华法林，通过CYP3A4代谢为10-羟基华法林，并通过羰基还原酶代谢为非对映异构醇。S-华法林主要通过CYP2C9代谢为7-羟基华法林。华法林与这些P450代谢的任何一种范围非常广泛的药物之间都可能发生潜在的药物相互作用，并且已经报道了许多此类相互作用。当S-华法林的代谢发生改变时，华法林的疗效主要受到影响。
