Table 1 Pharmacokinetic characteristics of NOACs compared to Warfarin
From: Switching from warfarin to direct-acting oral anticoagulants: it is time to move forward!
Characteristics | Warfarin | Apixaban | Dabigatran | Rivaroxaban | Edoxaban |
|---|---|---|---|---|---|
Bioavailability | > 95% | ~ 50% for doses up to 10 mg | ~ 7% | > 80% for 10 mg dose (regardless of food intake) and 20 mg dose (taken with food); 66% for 20 mg dose (fasting) | ~ 62% for 60 mg dose |
Time to peak activity | 24–36 h | 3–4 h | 0.5–2 h | 2–4 h | 1–2 h |
Half-life | 20–60 h |  ~ 12 h | 11–14 h | 5–9 h (young individuals); 11–13 h (elder individuals) | 6–11 h |
Dosing frequency in AF | Once daily | Twice daily | Twice daily | Once daily | Once daily |
Drug interactions | Numerous drugs including substrates of CYP2C9, CYP3A4, and CYP1A2; various foods | Strong inhibitor/inducer of both CYP3A4 and P-gp | Strong P-gp inhibitor and inducer | Strong inhibitor of both CYP3A4 and P-gp; strong CYP3A4 inducer | Strong P-gp inhibitor |
Renal elimination | < 1% | ~ 27% | 85% | 66% of the dose undergoes metabolic degradation then 50% eliminated renally and 50% eliminated via hepatobiliary route. Other 33% undergoes direct renal excretion | 50% |