Comparison of the pharmacologic properties of warfarin, rivaroxaban, apixaban, and edoxaban
. | Warfarin . | Dabigatran . | Rivaroxaban . | Apixaban . | Edoxaban . |
---|---|---|---|---|---|
Target | VKORC1 | Thrombin | Factor Xa | Factor Xa | Factor Xa |
Prodrug | No | Yes | No | No | No |
Bioavailability (%) | 100 | 7 | 80 | 60 | 62 |
Dosing | OD | BID | OD (BID) | BID | OD |
Time-to-peak effect | 4-5 d | 1-3 h | 2-4 h | 1-2 h | 1-2 h |
Half-life (h) | 40 | 14-17 | 7-11 | 8-14 | 5-11 |
Renal clearance as unchanged drug (%) | None | 80 | 33 | 27 | 50 |
Monitoring | Yes | No | No | No | No |
Interactions | Multiple | P-gp | 3A4/P-gp | 3A4/P-gp | P-gp |
. | Warfarin . | Dabigatran . | Rivaroxaban . | Apixaban . | Edoxaban . |
---|---|---|---|---|---|
Target | VKORC1 | Thrombin | Factor Xa | Factor Xa | Factor Xa |
Prodrug | No | Yes | No | No | No |
Bioavailability (%) | 100 | 7 | 80 | 60 | 62 |
Dosing | OD | BID | OD (BID) | BID | OD |
Time-to-peak effect | 4-5 d | 1-3 h | 2-4 h | 1-2 h | 1-2 h |
Half-life (h) | 40 | 14-17 | 7-11 | 8-14 | 5-11 |
Renal clearance as unchanged drug (%) | None | 80 | 33 | 27 | 50 |
Monitoring | Yes | No | No | No | No |
Interactions | Multiple | P-gp | 3A4/P-gp | 3A4/P-gp | P-gp |
OD, once daily; BID, twice daily; P-gp, P-glycoprotein; VKORC1, C1 subunit of the vitamin K epoxide reductase enzyme; 3A4, cytochrome P450 3A4 isoenzyme.