Table 3. Pharmacodynamic and pharmacokinetic properties of direct oral anticoagulants (DOACs).
Property | Apixaban | Dabigatran | Edoxaban | Rivaroxaban |
---|---|---|---|---|
Target | Factor Xa | Factor IIa | Factor Xa | Factor Xa |
Prodrug | No | Yes | No | No |
Dosing | BID | BID | OD | OD |
Bioavailability | 50% | 6.5% | 62% | 80–100% |
Half-life | 8–15 h | 12–14 h | 10–14 h | 5–13 h |
Renal clearance | ~27% | 85% | ~50% | ~33% |
Cmax | 3–4 h | 1–2 h | 1–2 h | 2–4 h |
Interactions | Strong inhibitors of CYP3A4 and P-gp | P-gp inhibitors | P-gp inhibitors | Strong inhibitors of CYP3A4 and P-gp |
Reproduced by permission of BMJ from: Spence JD. Cardioembolic stroke: everything has changed. Stroke Vasc Neurol 2018;3:76-83) (51). BID, twice a day; OD, daily; CMax, time to peak blood level; CYP3A4, cytochrome P4503A4; P-gp, P-glycoprotein.