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BLOOD AND BLOOD FORMING ORGANS › ANTITHROMBOTIC AGENTS › ANTITHROMBOTIC AGENTS › Vitamin K antagonists
tioclomarol
B01AA11
Adult Dosing
- Initial dose: 5 to 10 mg orally once daily
- Maintenance dose: 1 to 5 mg orally once daily, adjusted based on International Normalized Ratio (INR)
Pediatric Dosing
- Safety and efficacy not established in pediatric patients; use generally avoided
Indications
- Prophylaxis and treatment of venous thromboembolism
- Prevention of thromboembolic complications associated with atrial fibrillation or cardiac valve replacement
Mechanism of Action
- Vitamin K antagonist (coumarin derivative)
- Inhibits vitamin K epoxide reductase, preventing the gamma-carboxylation of clotting factors II, VII, IX, and X, as well as regulatory proteins C and S
Contraindications
- Active bleeding or hemorrhagic tendencies
- Recent major surgery (central nervous system, eye)
- Severe uncontrolled hypertension
- Pregnancy (teratogenic and causes fetal hemorrhage)
Adverse Reactions
- Major and minor hemorrhage
- Nausea, vomiting, diarrhea, abdominal pain
- Rare: calciphylaxis, skin necrosis, alopecia, hypersensitivity reactions
Drug Interactions
- Potentiated by CYP2C9 and CYP3A4 inhibitors (e.g., amiodarone, fluconazole, macrolides)
- Antagonized by CYP inducers (e.g., rifampin, carbamazepine, St. John's wort)
- Increased bleeding risk with antiplatelet agents (e.g., aspirin, clopidogrel) and NSAIDs
- Altered response with broad-spectrum antibiotics due to reduction of gut flora synthesis of vitamin K
Curated Content: Needs Vetting Before Put to Clinical Use