Table 1.
Pharmacological characteristics of oral anticoagulation agents.
| Warfarin |
Apixaban |
Dabigatran |
Edoxaban |
Rivaroxaban |
|
|---|---|---|---|---|---|
| Target | VKORC1 | Factor Xa | Factor IIa | Factor Xa | Factor Xa |
| Half-life (h) | 20- 60 | ~12 | 12-17 | 10-14 | 7-13 |
| Prodrug | no | no | yes | no | no |
| Renal clearance (%) | no | 25 | 80 | 50 | 35 |
| Hepatic clearance | 100 | 75 | 20 | 50 | 65 |
| Requires CYP450 | yes | yes | no | minimal | yes |
| Plasma protein binding (%) | 99 | 87 | 35 | 55 | 95 |
| Substrate for P-gP | no | yes | yes | yes | yes |
| Coagulation monitoring | Yes INR | no | no | no | no |
| Coagulation assay | INR | Anti Xa activity | Thrombin Time | Anti Xa activity | Anti Xa activity |
| Reversal agent | 4F-PCC, Vit K | Andexanet alfa | Idarucizumab | Andexanet alfa (Not yet FDA approved) | Andexanet alfa |
Modified from Qamar et al. 2018, with permission.