Table 6.
Mechanism of action and pharmacological characteristics of DOACs.
Dabigatran | Rivaroxaban | Apixaban | Edoxaban | |
Mechanism | Oral direct reversible competitive thrombin antagonist | Oral direct reversible competitive factor Xa antagonist | Oral direct reversible competitive factor Xa antagonist | Oral direct reversible competitive factor Xa antagonist |
CYP3A4 substrate | No | Yes | Yes | Yes |
Metabolism | Glucoronic acid conjugation | CYP3A4, CYP2J2 | CYP3A4/5, CYP1A2, CYP2C8, CYP2C9, CYP2C19 | CYP3A4/5 |
Bioavability | 3%–7% | 66% without food, 80%–100% with food | 50% | 62% |
Prodrug | Yes | No | No | No |
Absorption with food | No effect | 39% | No effect | 6%–22% |
Clearance non renal/renal | 20%–80% | 35%–65% | 73%–27% | 50%–50% |
CYP, cytochromes P450; Factor Xa, activated coagulation factor X; DOACs, direct oral anticoagulants.