Table 2.
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 (under fasting conditions) | ~62% for 60 mg dose |
Time to peak activity | 24–36 hours | 3–4 hours | 0.5–2 hours | 2.0–4 hours | 1–2 hours for 10–150 mg single dose |
Half-life | 20–60 hours | ~12 hours | 11–14 hours | 5–9 hours (young individuals); 11–13 hours (elderly individuals) | 6–11 hours for 10–150 mg single dose |
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 inhibitors/inducers of both CYP3A4 and P-gp | Strong P-gp inhibitors and inducers | Strong inhibitors of both CYP3A4 and P-gp; strong CYP3A4 inducers | Strong P-gp inhibitors |
Renal elimination | <1% | ~27% | 85% | 66% of the dose undergoes metabolic degradation, with half then being eliminated renally and the other half eliminated via the hepatobiliary route. The final 33% of the dose undergoes direct renal excretion | ~50% |
Note: Data from Bristol-Myers Squibb, Pfizer,23 Boehringer Ingelheim International GmbH,24 Bayer Pharma AG,25 Daiichi Sankyo Inc.,26 Eriksson et al,28 Harder,30 Verma and Brighton,31 Stampfuss et al,94 Matsushima et al,95 and Mendell et al.96
Abbreviations: AF, atrial fibrillation; CYP, cytochrome P450; P-gp, P-glycoprotein.