Table 1.
Warfarin | Dabigatran | Rivaroxaban | Apixaban | |
---|---|---|---|---|
Target | Synthesis of vitamin K‐dependent clotting factors (factors II, VII, IX, and X) | Thrombin | Factor Xa | Factor Xa |
Bioavailability | >95% | ∼6% | >80% | >50% |
Time to peak activity | 72–96 hours | 2 hours | 2.5–4 hours | 3 hours |
Half‐life | 40 hours | 14–17 hours | 5–9 hours (young healthy patients),11–13 hours (elderly patients) | 8–15 hours |
Dosing frequency in patients with AF | Once daily | Twice daily | Once daily | Twice daily |
Interactions | Numerous drugs including substrates of CYP2C9, CYP3A4, and CYP1A2; various foods | Strong P‐gp inhibitors and inducers | Strong CYP3A4 inducers, strong inhibitors of both CYP3A4 and P‐gp | Strong inhibitors/inducers of both CYP3A4 and P‐gp |
Renal elimination (absorbed active drug) | <1% | ∼80% | ∼33%a | ∼27% |
Abbreviations: AF, atrial fibrillation; CYP, cytochrome P450; P‐gp, P‐glycoprotein.
An additional 33% of the absorbed rivaroxaban dose inactivated in the liver is also eliminated renally.