With regard to assays available to monitor the anticoagulant activity of dabigatran, while prothrombin time (PT) and international normalized ratio (INR) are commonly used to monitor warfarin-mediated anticoagulation, they have significant variability in monitoring direct thrombin inhibitors such as dabigatran. 2,3 It is primary renally-excreted (80%), an important consideration in patients with chronic renal impairment. 3 The half-life of dabigatran is 12-17 hours, warranting twice-daily dosing. 2 Its activity peaks between 30-120 minutes after administration and rapidly decreases by approximately 70% over four to six hours. Dabigatran is a prodrug, requiring hydrolysis to become active it binds to both free and clot-bound thrombin. This article reviews the current literature on reversing dabigatran function, with special focus on idarucizumab and the Reversal of Dabigatran Anticoagulant Effect With Idarucizumab (RE-VERSE AD) trial.Ī few key points on dabigatran's formulation and pharmacokinetics are critical to this discussion.
However, recent studies have shown promise of specific reversal agents for various NOACs, including dabigatran. Although dabigatran and the other NOACs have been extremely useful in the clinical setting, two major clinical issues remained unsettled: the lack of a reliable reversal agent, and difficulty with laboratory monitoring due to inter-patient variability in commonly assayed coagulation parameters. Food and Drug Administration (FDA) in 2010, with indications broadened to the prevention and treatment of VTE. In 2008, the European Commission approved dabigatran etexilate, a reversible direct thrombin inhibitor, for stroke and systemic embolization risk reduction in patients with non-valvular AF it was subsequently approved by the U.S. These drugs were developed to eliminate the need for routine blood monitoring with anticoagulants such as warfarin, and to achieve standard drug dosing with predictable pharmacokinetics. Over the past decade, novel oral anticoagulants (NOACs) have become more commonly used for prevention of venous thromboembolism (VTE), and management of stroke risk in patients with atrial fibrillation (AF).
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