08/05 - RGD releases three interactive pathway diagram pages for the vitamin K antagonist and anticoagulant warfarin

Warfarin, under the trade name Coumadin, is a widely-used 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 target of warfarin is vitamin K epoxide reductase (VKORC1) of the vitamin K cycle metabolic pathway. Bleeding and thromboembolic effects can result due to relative dose of the drug, inter-individual variability and diet. Several side effects such as necrosis, particularly of the skin, osteoporosis and vascular calcification, warfarin-related nephropathy are observed.
Warfarin drug pathway


Warfarin pharmacodynamics pathway


Warfarin pharmacokinetics pathway


Warfarin, which has the trade name Coumadin, is a widely-used drug for the prevention of thrombosis and venous and arterial thromboembolism. Several effects due to dosage, diet or variants as well side effects are reported. Click here to see the overall aspects of the warfarin pathway. The target of warfarin is vitamin K epoxide reductase (VKORC1) of the vitamin K cycle metabolic pathway. Warfarin binding inhibits the cycle and thus, precludes the modification of ‘vitamin K-dependent proteins’ (VKDs), affecting their function.  As many of the important enzymes of the coagulation cascade are VKDs, warfarin inhibits blood clotting and is antithrombotic. Click here to explore the details. Warfarin is present as a racemic mixture of R and S enantiomers, both active, though not equally, and both metabolized via different routes. Phase I biotransformation enzymes produce several hydroxwarfarin metabolites which are then processed by several (UDP) - glucuronosyltransferases (UGTs), phase II enzymes, with various specificities. Click here to investigate.