| Dabigatran | Rivaroxaban | Apixaban | Edoxaban |
|---|
| Mechanism of action | Direct thrombin inhibitor | Direct factor Xa inhibitor | Direct factor Xa inhibitor | Direct factor Xa inhibitor |
|---|
| Tmax (hours) | 1-3 | 2-4 | 3-4 | 1-2 |
|---|
| Metabolism | Phase II – glucoronidation | CYP3A4, CYP3A5, CYP2J2 | CYP3A4, CYP3A5 | Minimal via hydrolysis, conjugation, oxidation by CYP3A4 |
|---|
| Excretion | 80% renal | 2/3 liver, 1/3 renal | 25% renal, 75% fecal | 50% renal, 50% fecal |
|---|
| Elimination half-life (hours) | 12-17 | 5-9 | 9-14 | 10-14 |
|---|
| Dose | 150 mg PO BID | 20 mg PO daily | 5 mg PO BID | 60 mg daily; Avoid use if CrCl >95 ml/min |
|---|
| Dose – Renal Impairment | CrCl 15-30: 75mg BID
CrCl <15: not recommended | CrCl ≤50: 15 mg daily | Any two: SCr ≥1.5; age ≥80 or weight <60kg: 2.5 mg BID | CrCl 15-50: 30 mg daily
CrCl <15: not recommended |
|---|
| Dose – Hepatic Impairment | Moderate-severe: not recommended | Child-Pugh B or C, or coagulopathy: not recommended | Severe impairment: not recommended | Moderate-severe: not recommended |
|---|
| Drug Interactions | Ketoconazole or dronedarone & CrCl 30-50 ml/min: 75mg BID; P-gp inhibitor & CrCl 15-30 ml/min: not recommended;
P-gp inducer: avoid | Strong dual- inhibitors or inducers of P-gp and CYP3A4: avoid;
Combined P-gp and weak-moderate inhibitors of CYP3A4, & CrCl 15-50ml/min: use caution | Strong dual-inhibitors of P-gp and CYP3A4: reduce dose to 2.5mg BID or avoid if 2.5mg BID is already indicated based on above factors; Strong dual-inducers: avoid | Strong P-gp inducers: avoid |
|---|
