Table 1.

Pharmacologic properties of dabigatran [1–4]

Oral bioavailability	3–7 %
T max	1–3 h
Protein binding	35 %
Volume of distribution	0.7–1.0 L/kg (based on a 70-kg patient)
Onset of effect	0.5–2 h
Time to steady state	Approximately 3 days
Metabolism	Carboxylesterase 1 converts dabigatran etexilate to dabigatran (active)
Renal elimination	80 %
Dialyzability	62 % (at 2 h) and 68 % (at 4 h)
Drug interactions	P-glycoprotein inhibitors and inducers, and antiplatelets
Dosing	CrCl >30 mL/min; 150 mg twice daily
	CrCl ≤30 mL/min; 75 mg twice dailya
	CrCl <15 mL/min; contraindicated

^aPatients with CrCl <30 mL/min were excluded from the RE-LY study. The use of dabigatran in patients with a CrCl <30 mL/min is considered contraindicated in the European and Canadian product labeling. The US dose adjustment (75 mg twice daily) for patients with a CrCl 15 to 30 mL/min is based on a pharmacokinetic model. The predicted peak and trough dabigatran concentrations with this dosage are similar to those obtained in patients with moderate renal impairment receiving 150 mg twice daily. The safety and efficacy of the dosage reduction have not been formally evaluated