dabigabran

Dabigatran, sometimes spelled dabigabran, is an oral anticoagulant that acts as a direct thrombin inhibitor. It is marketed as dabigatran etexilate, a prodrug that is converted in the body to the active molecule dabigatran. It was developed by Boehringer Ingelheim and approved for use in several countries to prevent stroke and systemic embolism in nonvalvular atrial fibrillation, to treat deep vein thrombosis and pulmonary embolism, and to prevent DVT after hip or knee replacement in some settings.

Mechanism of action: Dabigatran directly inhibits thrombin (factor IIa), reducing the conversion of fibrinogen to fibrin and decreasing thrombus formation. This mechanism provides anticoagulant effects without the need for routine coagulation monitoring in most patients.

Dosing and administration: The standard dose for nonvalvular atrial fibrillation is commonly 150 mg twice daily, with reduced dosing for older patients, those with renal impairment, or those with drug interactions as specified in labeling. Dosing for postoperative DVT prophylaxis varies by region and indication. The drug is taken orally and can be administered with or without food.

Pharmacokinetics and monitoring: Dabigatran has a rapid onset and a half-life of about 12–17 hours in individuals with normal kidney function. It is predominantly cleared by the kidneys, so renal function influences exposure. Routine laboratory monitoring is not required, though kidney function and bleeding risk are assessed prior to use.

Safety and regulation: The principal risk is bleeding. Common adverse effects include dyspepsia and other GI symptoms. It is contraindicated in active major bleeding and is not approved for use in patients with mechanical heart valves. It interacts with P-glycoprotein inhibitors. A specific reversal agent, idarucizumab, is available for emergency bleeding. Use in pregnancy is limited by a lack of data.