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BLOOD AND BLOOD FORMING ORGANS › ANTITHROMBOTIC AGENTS › ANTITHROMBOTIC AGENTS › Direct factor Xa inhibitors
apixaban
B01AF02
Forms & Strengths
- Oral tablets: 2.5 mg, 5 mg
Adult Dosing
- Non-valvular atrial fibrillation: 5 mg PO BID
- Non-valvular AF with $\ge$2 criteria (age $\ge$80 years, body weight $\le$60 kg, serum creatinine $\ge$1.5 mg/dL): 2.5 mg PO BID
- Treatment of DVT/PE: 10 mg PO BID for 7 days, then 5 mg PO BID
- Reduction in risk of DVT/PE recurrence: 2.5 mg PO BID after at least 6 months of treatment
- DVT/PE prophylaxis (elective hip or knee replacement): 2.5 mg PO BID starting 12 to 24 hours post-operatively; duration 32-38 days for hip, 10-14 days for knee
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- Reduction of stroke and systemic embolism risk in non-valvular atrial fibrillation
- Treatment of deep vein thrombosis (DVT)
- Treatment of pulmonary embolism (PE)
- Reduction in the risk of recurrent DVT and PE following initial therapy
- Prophylaxis of DVT and PE following hip or knee replacement surgery
Mechanism of Action
- Selective, reversible, and direct inhibitor of factor Xa
- Inhibits free and clot-bound factor Xa, as well as prothrombinase activity
- Prevents thrombin generation and thrombus development without requiring antithrombin III for activity
Contraindications
- Active pathological bleeding
- Severe hypersensitivity (e.g., anaphylactic reactions) to apixaban
Adverse Reactions
- Major bleeding events (gastrointestinal, intracranial)
- Minor bleeding (epistaxis, hematuria, contusion)
- Anemia
- Nausea
Drug Interactions
- Strong dual inhibitors of CYP3A4 and P-glycoprotein (e.g., ketoconazole, itraconazole, ritonavir): increase apixaban exposure; reduce apixaban dose to 2.5 mg BID or avoid concomitant use
- Strong dual inducers of CYP3A4 and P-glycoprotein (e.g., rifampin, carbamazepine, phenytoin, St. John's wort): decrease apixaban exposure; avoid concomitant use
- Concomitant antiplatelet agents, NSAIDs, SSRIs, SNRIs, and other anticoagulants: increase bleeding risk
Curated Content: Needs Vetting Before Put to Clinical Use