Warfarin
Vitamin K antagonist; oral anticoagulant with narrow therapeutic window
Mechanism of Action
Warfarin is a vitamin K antagonist (VKA) that inhibits vitamin K epoxide reductase (VKORC1), preventing the recycling of vitamin K epoxide to its active hydroquinone form. Vitamin K is a required cofactor for gamma-carboxylation of clotting factors II, VII, IX, and X, as well as anticoagulant proteins C and S. By depleting active vitamin K, warfarin produces a state analogous to vitamin K deficiency, reducing functional clotting factor synthesis. The anticoagulant effect is monitored via INR (international normalized ratio). Warfarin has a narrow therapeutic window and extensive drug-drug interactions via CYP2C9 metabolism.
Evidence Level
Clinical Trial - Human
6 studies published
Pharmacology
Molecular Weight
308.3 g/mol
Half-Life
Approximately 20-60 hours (R-enantiomer); 20-60 hours (S-enantiomer)
Bioavailability
Approximately 100% oral bioavailability