Table 4.
Absorption and metabolism of the different NOACs
| Dabigatran106,376 | Apixaban517 | Edoxaban518 | Rivaroxaban519,520 | |
|---|---|---|---|---|
| Bioavailability | 3–7% | 50% | 62% | 15 mg/20 mg: 66% without food, 100% with food |
| Prodrug | Yes | No | No | No |
| Clearance non-renal/renal of absorbed dose | 20%/80% | 73%/27% | 50%/50% | 65%/35% |
| Plasma protein binding | 35% | 87% | 55% | 95% |
| Dialysability | 50–60% | 14% | NA | NA |
| (In part dialysable) | (Not dialysable) | (Not dialysable) | (Not dialysable) | |
| Metabolism | Glucoronic acid conjugation | CYP3A4 (25%), CYP1A2, CYP2J2, CYP2C8, CYP2C9 CYP2C19 | CYP3A4 (<4% of elimination) | CYP2A4 (18%)519, CYP2J2 |
| Absorption with food | No effect | No effect | 6–22% more; minimal effect on exposure | +39% more (see above) |
| Absorption with H2B/PPI | −12% to 30% (not clinically relevant) | No effect | No effect | No effect |
| Time to peak levels (h) | 3 | 3 | 2–4 | 2–4 |
| Elimination half-life (h) | 12–17 | 12 | 10–14 | 5–9 (young) 11–13 h (elderly) |
NOAC, non-vitamin K antagonist oral anticoagulant.