Dabigatran etexilate

Dabigatran etexilate

Dabigatran etexilate is a prodrug without any anticoagulant activity. It gets converted in vivo to the active form dabigatran, which is a specific, reversible, direct thrombin inhibitor that inhibits both fibrin-bound as well as free thrombin. The drug inhibits coagulation of blood by preventing thrombin-mediated effects like thrombin-induced platelet aggregation, breakdown of fibrinogen to fibrin monomers and the activation of clotting factors V, VIII, XI and XIII.

Indications

It is indicated for the prevention of stroke and systemic embolism in patients with nonvalvular atrial fibrillation. It is also indicated for postoperative thromboprophylaxis in patients who have undergone total hip or knee replacement procedures.

Contraindications

Contraindications to the drug would include serious hypersensitivity (anaphylaxis) to dabigatran and active pathological bleeding.

Precautions

Dabigatran should be used with caution in patients with severe renal impairment having Cl_cr in the range of 15-30ml/min. Use of dabigatran etexilate in patients with Cl_cr < 15 ml/min is not recommended due to insufficient evidence to support use in this group.

Drug interactions

Drug interactions are in general rare with dabigatran etexilate unlike warfarin as cytochrome P-450 is not involved in the metabolism. But P-glycoprotein inducers like rifampicin should be avoided in combination with dabigatran. Food has no effect on the bioavailability of dabigatran but delays the time to peak concentrations by 2 hours.