Table 5.
Main PK characteristics for oral anticoagulants and dosing recommendations, according to regulatory approvals (modified from refs79,80)
| Warfarin | Dabigatran | Apixaban | Edoxaban | Rivaroxaban | |
|---|---|---|---|---|---|
| Fraction renally excreted of absorbed dose | 80% | 27% | 50% | 35% | |
| Bioavailability | 95–100% | 3–7% | 50% | 62% | 66% without food Almost 100% with food |
| Fraction renally excreted of administered dose | 4% | 14% | 37% | 33% | |
| Approved for CrCl | ≥30 mL/min | ≥15 mL/min | ≥15 mL/min | ≥15 mL/min | |
| Dosing recommendation | CrCl ≥30 mL/min: no adjustment | CrCl ≥50 mL/min: no adjustment (i.e. 150 mg b.i.d.) | Serum creatinine ≥1.5 mg/dL: no adjustment (i.e. 5 mg b.i.d.) | 60 mg daily for CrCl 50–95 mL/min, 30 mg daily for CrCl 15–50 mL/min, weight ≤60 kg; not recommended for CrCl >95 mL/min | CrCl ≥50 mL/min: no adjustment (i.e. 20 mg qd) |
| Dosing if CKD | When CrCl <30 mL/min: use lower doses and monitor closely | When CrCl 30–49 mL/min, 150 mg b.i.d. is possible (SmPC) but 110 mg b.i.d. is recommended if high risk of bleeding79 | CrCl 15–29 mL/min: 2.5 mg b.i.d. Serum creatinine ≥1.5 mg/dL in combination with age of ≥80 years or weight ≤60 kg. (SmPC) or with other factors that increase bleeding risk (e.g. diltiazem): 2.5 mg b.i.d. |
60 mg daily for CrCl 50–95 mL/min, 30 mg daily for CrCl 15–50 mL/min, weight ≤60 kg; not recommended for CrCl >95 mL/min | 15 mg q.d. when CrCl 15–49 mL/min |
| Not recommended if | CrCl <30 mL/min | CrCl <15 mL/min | If CrCl >95 mL/min or <15 mL/min | CrCl <15 mL/min |