Warfarin
Coumadin | Jantoven
Overview
Warfarin is an oral vitamin K antagonist anticoagulant used to prevent and treat thromboembolic disorders such as venous thromboembolism and stroke in atrial fibrillation.
Indications
- Venous thromboembolism treatment and prophylaxis
- Atrial fibrillation
- Mechanical heart valves
- Prevention of recurrent thromboembolism
Contraindications
- Active bleeding
- Pregnancy
- Severe hepatic disease
- Recent or planned major surgery with high bleeding risk
Classification
Mechanism of Action
Inhibits vitamin K epoxide reductase, reducing the regeneration of vitamin K and impairing gamma-carboxylation of clotting factors II, VII, IX, and X and proteins C and S.
Pharmacodynamics
Produces a delayed, dose-dependent anticoagulant effect monitored by the international normalized ratio (INR). Full effect takes several days as existing clotting factors are cleared.
Pharmacokinetics
- Absorption
- Rapidly and completely absorbed orally.
- Distribution
- Highly protein bound; small volume of distribution.
- Metabolism
- Metabolized by hepatic CYP2C9 (S-warfarin) and CYP1A2 and CYP3A4 (R-warfarin).
- Excretion
- Metabolites excreted in urine and bile.
- Half-life
- Approximately 20-60 hours
- Bioavailability
- Essentially complete
- Protein Binding
- Approximately 99%
Dosage
Typical dosage: Individualized to a target INR, commonly 2-10 mg once daily
Available Forms
- Tablet
- Injection
Side Effects
Common
- Bruising
- Minor bleeding
- Nausea
Serious
- Major hemorrhage
- Intracranial bleeding
Rare
- Skin necrosis
- Purple toe syndrome
Drug Interactions
Additive bleeding risk through combined anticoagulant and antiplatelet effects.
Inhibits warfarin metabolism, raising INR and bleeding risk; the warfarin dose usually must be reduced.
Warnings
Warfarin can cause major or fatal bleeding. Regular monitoring of INR is essential. Patients at high risk of bleeding should be evaluated carefully, and the drug requires careful dose management.
Pregnancy
Category X
Toxicity
Overdose manifests as bleeding, hematuria, and bruising.
Overdose
Manage with vitamin K (phytonadione); use prothrombin complex concentrate or fresh frozen plasma for serious bleeding.
References
Looking for patient-friendly information? Visit RemedyDoor for easy-to-read guides about this medication.