Table 3. Overview of the non-vitamin K antagonist oral anticoagulants (NOACs) (according to [2, 28]).
Dabigatran | Apixaban | Edoxaban | Rivaroxaban | |
Standard dosing* | 150 mg or 110 mg twice daily |
5 mg twice daily | 60 mg once daily | 20 mg once daily |
Dose adjustment in patients with chronic kidney disease and for age, weight, co-medication* | No (creatinine clearance <30 ml/min contraindicated) |
2.5 mg twice daily in patients with atrial fibrillation and severe chronic kidney disease (creatinine clearance 15–29 mL/min) or at least 2 of the following criteria: age ≥ 80 years; body weight ≤ 60 kg or serum creatinine ≥ 1.5 mg/dL | 30 mg once daily, in the presence of the following factors: Creatinine clearance 15–49 mL/min, body weight ≤ 60 kg, co-medication with cyclosporine, dronedarone, erythromycin or ketoconazole | 15 mg once daily in patients with atrial fibrillation, if creatinine clearance 15–49 mL/min |
Bioavailability | 3–7% | 50% | 62% | 66% without food, almost 100% with food |
Prodrug | Yes | No | No | No |
Non-renal/renal clearance of the absorbed dose (with normal renal function) | 20% / 80% | 73% / 27% | 50% / 50% | 65% / 35% |
Hepatic drug metabolism: CYP450 involved | No | Yes (elimination; low CYP3A4 involvement) |
minimal (<10% of elimination) |
Yes (elimination) |
Absorption with concomitant food intake | No effect | No effect | No effect | +39% more |
Recommended to take with food? | No | No | No | Compulsory |
Absorption with H2 blocker/proton pump inhibitor treatment | –12–30% | No effect | No effect | No effect |
Asian patients | +25% | No effect | No effect | No effect |
Gastrointestinal tolerability | Dyspepsia 5–10% |
No problems | No problems | No problems |
Elimination half-life | 12–17 hrs | 12 hrs | 9–11 hrs | 5–9 hrs (younger) 11–13 hrs (older) |
Specific antidote available | Yes | No | No | No |
* Detailed information of the respective summary of product characteristics should be taken into account.