What is the action of Warfarin sodium?
What is the action of Warfarin sodium?
Warfarin is commonly called a “blood thinner,” but the more correct term is “anticoagulant.” It helps to keep blood flowing smoothly in your body by decreasing the amount of certain substances (clotting proteins) in your blood.
What is the mechanism of action for warfarin?
Mechanism of action — Warfarin and related vitamin K antagonists (VKAs) block the function of the vitamin K epoxide reductase complex in the liver, leading to depletion of the reduced form of vitamin K that serves as a cofactor for gamma carboxylation of vitamin K-dependent coagulation factors [1].
How is warfarin metabolized in the body?
Warfarin is metabolized via the cytochrome P450 system by CYP 2C9, 1A2, and 3A4. It is a racemic mixture, with the S-enantiomer being 2.7 to 3.8 times more potent than the R-enantiomer.
Where is Warfarin sodium metabolized?
The elimination of warfarin is almost entirely by metabolism. COUMADIN is stereoselectively metabolized by hepatic microsomal enzymes (cytochrome P-450) to inactive hydroxylated metabolites (predominant route) and by reductases to reduced metabolites (warfarin alcohols).
What is the pharmacokinetics of warfarin?
Warfarin is essentially completely absorbed, reaching a maximum plasma concentration between 2 and 6 hours. It distributes into a small volume of distribution (10 L/70kg) and is eliminated by hepatic metabolism with a very small clearance (0.2 L/h/70kg). The elimination half-life is about 35 hours.
Is there a difference between warfarin and warfarin sodium?
Warfarin sodium is an anticoagulant medication. “Anti” means against and “coagulant” means causing blood clotting. Warfarin controls the way that blood clots (thickens into a lump) inside your blood vessels. The brand names of warfarin are Coumadin® and Jantoven®.
How does warfarin work clotting factors?
Warfarin blocks one of the enzymes (proteins) that uses vitamin K to produce clotting factors. This disrupts the clotting process, making it take longer for the blood to clot.
How is warfarin metabolized in the liver?
Warfarin accumulates in the liver, where the two isomers are metabolized via distinct pathways. Oxidative metabolism of the more active S isomer is effected by CYP2C9. Two relatively common variants, CYP2C9*2 and CYP2C9*3, have reduced activity. Patients with these variants require a lower maintenance dose of warfarin.
Is warfarin metabolized in the liver?
(Warfarin is metabolized in the liver. CYP1A1, CYP1A2, and CYP3A4 metabolize the (R)-enantiomer and CYP2C9 metabolizes the more potent (S)-enantiomer.
Does warfarin have active metabolites?
Warfarin sodium and its major active metabolite 3′-hydroxywarfarin were directly provided by Bristol-Myers Squibb Company whilst rodenticide Coumatetralyl was used as internal standard (IS; Riedel-de Haën, Sigma Aldrich, Laborchemikalien GMBH).
How does warfarin inhibit clot formation?
Warfarin is taken for a period ranging from a few weeks to lifelong, depending on the individual’s diagnosis and future clot risks. It works by inhibiting the liver’s ability to make coagulation proteins that require vitamin K for their synthesis.
Why is warfarin called rat poison?
Warfarin is a synthetic derivative of dicoumarol, and since 1948 has had a major role in slaughtering rats and mice by stimulating internal bleeding. In 1954, warfarin was also approved for therapeutic use as an anticoagulant in the prevention of thrombosis and thromboembolism.