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Warfarin, trade name Coumadin, is a widely-used oral anticoagulant drug for the prevention of thrombosis and venous and arterial thromboembolism. It is a synthetic derivative of coumarin-derived dicoumarol. Warfarin is present as a racemic mixture of R and S enantiomers, both active, though not equally, and both metabolized via different routes. The S-warfarin is 3 to 5 times more potent than the R-enantiomer. Warfarin is metabolized, mainly in the liver, by several cytochrome P450 phase I biot

Pathway Diagram:

Elsevier Inc. UGT1A9 CYP2C18 (R)-warfarin (S)-warfarin 8-hydroxywarfarin ---> 8-OH-warf-gluc 7-hydroxywarfarin ---> 7-OH-warf-gluc 6-hydroxywarfarin ---> 6-OH-warf-gluc 4-hydroxywarfarin ---> 4-OH-warf-gluc UGT1A10 (S)-warfarin ---> 7-hydroxywarfarin (R)-warfarin ---> 10-hydroxywarfarin UGT1A8 UGT1A1 CYP2C19 CYP2C9 CYP2C8 CYP1A1 CYP1A2 CYP3A4 8-OH-warf-gluc 7-OH-warf-gluc 4-OH-warf-gluc 6-OH-warf-gluc 4-hydroxywarfarin 8-hydroxywarfarin 6-hydroxywarfarin 7-hydroxywarfarin 10-hydroxywarfarin 10-hydroxywarfarin ---| CYP2C9 7-hydroxywarfarin ---| CYP2C9 (S)-warfarin ---> 6-hydroxywarfarin (R)-warfarin ---> 6-hydroxywarfarin (R)-warfarin ---> 7-hydroxywarfarin (R)-warfarin ---> 8-hydroxywarfarin (R)-warfarin ---> 4-hydroxywarfarin

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References Associated with the warfarin pharmacokinetics pathway:

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