Dabigatran
Trade names
PRADAXA
Actions
Factor IIa inhibitor
Route of Administration
Oral
Bioavailability
3–7%
Plasma protein binding
35%
Time to peak plasma concentration
2 h
Half-life
12–14 h
Duration of action
48 h
Metabolism
Hepatic
Enzymes involved
- Metabolized by esterases and microsomal carboxylesterases.
- No CYP involved.
Elimination
Renal 80%
Interactions
P-glycoprotein inhibitors increase the absorption of dabigatran leading to increased plasma levels.
Effect reversal
Idarucizumab (Praxbind) is a monoclonal antibody that specifically reverses the effects of dabigatran
Idarucizumab is given as a bolus 5g IV injection. The effect of dabigatran is annulled within minutes of administration.
Dabigatran treated patients with acute ischemic stroke that received idarucizumab have been successfully treated with tPA.
Dabigatran treatment can be restarted 24 hours after administration of idarucizumab.
Recommended dose
Stroke prophylaxis in non-valvular AF, DVT, PE:
150 mg twice daily
In patients ≥80 years or patients treated with verapamil, dose reduction to 110 mg twice daily is recommended.
Renal impairment
| Creatinine clearance | Dosage |
|---|---|
| >30 ml/min* | 150 mg twice daily |
| 15-30 ml/min | 75 mg twice daily |
<15 ml/min | Not recommended |
*If CrCl 30-50 mL/min and concomitant use of P-glycoprotein inhibitors, reduce to 75 mg twice daily.
Discontinuation before invasive procedures
| Creatinine clearance | High bleeding risk | Standard risk |
|---|---|---|
| ≥80 ml/min | stop 2 days before | stop 24 hours before |
≥50 - <80 ml/min | stop 2-3 days before | stop 1-2 days before |
≥30 - <ml/min | stop 4 days before | stop 2-3 days before |