Dabigatran Etexilate (Pradaxa)

Pharmacologic profile and clinical uses

Mechanism of action

Direct thrombin inhibitor: Dabigatran directly inhibits thrombin (factor IIa), which is a key enzyme in the coagulation cascade responsible for the conversion of fibrinogen to fibrin, thus preventing clot formation.

Indications

• Non-valvular atrial fibrillation: To reduce the risk of stroke and systemic embolism.
• Deep Vein Thrombosis (DVT) and Pulmonary Embolism (PE): Treatment and reduction of recurrence.
• Prophylaxis of DVT and PE: Following hip replacement surgery.

Key aspects of drug therapy management

Dosage and administration

• Non-valvular atrial fibrillation: 150 mg orally twice daily.
• DVT/PE treatment and reduction of recurrence: 150 mg orally twice daily after 5-10 days of parenteral anticoagulation.
• Post-Hip replacement prophylaxis: 110 mg orally on the first day, then 220 mg once daily.
• Renal Impairment: Dosage adjustment may be necessary; contraindicated in severe renal impairment (CrCl < 30 mL/min).

Side effects

• Bleeding: Increased risk of bleeding, including gastrointestinal and intracranial bleeding.
• Gastrointestinal symptoms: Dyspepsia, gastritis-like symptoms.

Drug interactions

• P-glycoprotein inhibitors: Such as ketoconazole, which can increase dabigatran levels.
• Antiplatelet agents and NSAIDs: May increase bleeding risk.

Reversal agent

Idarucizumab (Praxbind): A monoclonal antibody fragment specifically indicated for reversing the anticoagulant effects of dabigatran in cases of emergency surgery/urgent procedures or life-threatening or uncontrolled bleeding.

Monitoring and considerations

• Routine monitoring: Not required, unlike warfarin. However, renal function should be monitored periodically.
• Transitioning: Care must be taken when transitioning from or to other anticoagulants to minimize the risk of thrombosis or bleeding.