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BLOOD AND BLOOD FORMING ORGANS › ANTITHROMBOTIC AGENTS › ANTITHROMBOTIC AGENTS › Vitamin K antagonists
warfarin
B01AA03
Forms & Strengths
- Oral tablets: 1 mg, 2 mg, 2.5 mg, 3 mg, 4 mg, 5 mg, 6 mg, 7.5 mg, 10 mg
Adult Dosing
- Initial dose: 2 mg to 5 mg orally once daily for the first 1 to 2 days
- Maintenance dose: 2 mg to 10 mg orally once daily, adjusted based on target INR
Pediatric Dosing
- Loading dose: 0.1 mg/kg orally once daily for 2 days (max 10 mg/day)
- Maintenance dose: Titrated based on PT/INR, typically ranging from 0.05 mg/kg/day to 0.33 mg/kg/day
Indications
- Prophylaxis and treatment of venous thrombosis and pulmonary embolism
- Thromboembolic complications associated with atrial fibrillation and/or cardiac valve replacement
Mechanism of Action
- Inhibits vitamin K epoxide reductase (VKORC1), preventing the regeneration of active vitamin K
- Depletes functional vitamin K-dependent clotting factors II, VII, IX, and X, as well as proteins C and S
Contraindications
- Hemorrhagic tendencies or blood dyscrasias
- Recent or contemplated surgeries of the central nervous system or eye, or traumatic surgery resulting in large open surfaces
- Bleeding tendencies associated with active ulceration or overt bleeding
- Major regional or lumbar block anesthesia
- Severe uncontrolled hypertension
- Pregnancy (except in pregnant women with mechanical heart valves)
Adverse Reactions
- Major or minor hemorrhage from any tissue or organ
- Calciphylaxis
- Warfarin-induced skin necrosis and gangrene
- Nausea, vomiting, abdominal pain, diarrhea
- Alopecia
Drug Interactions
- CYP2C9, CYP1A2, and CYP3A4 inducers (e.g., rifampin, carbamazepine) decrease warfarin efficacy
- CYP2C9 and CYP3A4 inhibitors (e.g., amiodarone, fluconazole, metronidazole) increase bleeding risk
- Concomitant use of antiplatelets, NSAIDs, and SSRIs significantly increases bleeding risk
- Vitamin K ingestion (dietary or supplements) decreases anticoagulant response
Curated Content: Needs Vetting Before Put to Clinical Use