Table 1.
CLINICALLY IMPORTANT PROPERTIES | DABIGATRAN | RIVAROXABAN | APIXABAN |
---|---|---|---|
Clinical indications and doses | |||
• Atrial fibrillation (indefinite duration) | 150 mg or 110 mg twice daily | 20 mg daily* | 5 mg twice daily† |
• Acute VTE (3 to 6 mo) | 150 mg twice daily | 20 mg daily, 15 mg twice daily for initial 21 d | 5 mg twice daily, 10 mg twice daily for initial 7 d |
• VTE prevention after knee or hip replacement surgery (14 or 30 d, respectively) | 110 mg (initial dose) then 220 mg daily | 10 mg daily | 2.5 mg twice daily |
Key pharmacologic properties | |||
• Mechanism of action | Direct factor IIa (thrombin) inhibitor | Direct factor Xa inhibitor | Direct factor Xa inhibitor |
• Renal clearance | 80% | 33% (active drug) | 25% |
Half-life | |||
• Normal renal function (eGFR > 80 mL/min) | 11 h | 9 h | 9 h |
• Mild renal impairment (eGFR 50–80 mL/min) | 14 h | 9 h | 9 h |
• Moderate renal impairment (eGFR 30–49 mL/min) | 15–17 h | 10–15 h | 10–14 h |
Onset of action (after oral intake) | 1–3 h | 1–3 h | 1–3 h |
Key practical properties | |||
• Food or alcohol interactions | None | None | None |
• Drug interactions | Amiodarone, quinidine, azole antifungals (eg, ketoconazole), rifampin, ritanovir | Azole antifungals (eg, ketoconazole), ritanovir, rifampin, clarithromycin, anticonvulsants (eg, phenytoin, carbamazepine) | Azole antifungals (eg, ketoconazole), ritanovir, rifampin, clarithromycin, anticonvulsants (eg, phenytoin, carbamazepine) |
• Antidote | None to date | None to date | None to date |
Laboratory measurement of anticoagulant effect‡ | aPTT or TT, dilute TT (direct thrombin inhibitor assay) | PT or INR (reagent-specific), anti–factor Xa assay | PT or INR (minimal effect), anti–factor Xa assay |
aPTT—activated partial thromboplastin time, eGFR—estimated glomerular filtration rate, INR—international normalized ratio, NOAC—new oral anticoagulant, PT—prothrombin time, TT—thrombin time, VTE—venous thromboembolism.
Dose should be 15 mg daily if eGFR is < 50 mL/min.
Dose should be 2.5 mg twice daily if 2 of the following 3 criteria are met: creatinine level ≥ 133 μmol/L; age ≥ 80 y; weight ≤ 60 kg.
Laboratory tests might not reliably reflect levels of anticoagulation.