Abstract
For the last 60 years warfarin has been the cornerstone for chronic anticoagulation in prevention of ischemic strokes and systemic embolization. Warfarin therapy has several limitations including frequent monitoring and various food and significant drug interactions, which make it a less than ideal chronic oral anticoagulant. The continued search for safe, effective, medications with predictable pharmacokinetic profiles has led to newer alternatives. Dabigatran is a potent reversible, competitive direct thrombin inhibitor which is available as the prodrug, Dabigatran etexilate. It was first approved in Europe and recently in October 2010, the US food and drug administration (FDA) has approved the use of this novel oral anticoagulation for prevention of stroke in those with non valvular atrial fibrillation. This review will cover the chemical structure, mechanism of action, pharmacokinetic profile, clinical trials, dosage, clinical implication and adverse effects of dabigatran.
Keywords: Anticoagulation, atrial fibrillation, BISTRO trial, chemical structure, dabigatran, diract thrombin inhibitors, PETRO trial, pharmacodynamics, pharmacokinetics, Re-Ly trial, RECOVER trial, stroke warfarin
Cardiovascular & Hematological Agents in Medicinal Chemistry
Title:Dabigatran - A New Chapter in Anticoagulation
Volume: 10 Issue: 2
Author(s): Shameer Ahmed, Vadim Levin, Robert Malacoff and Matthew W. Martinez
Affiliation:
Keywords: Anticoagulation, atrial fibrillation, BISTRO trial, chemical structure, dabigatran, diract thrombin inhibitors, PETRO trial, pharmacodynamics, pharmacokinetics, Re-Ly trial, RECOVER trial, stroke warfarin
Abstract: For the last 60 years warfarin has been the cornerstone for chronic anticoagulation in prevention of ischemic strokes and systemic embolization. Warfarin therapy has several limitations including frequent monitoring and various food and significant drug interactions, which make it a less than ideal chronic oral anticoagulant. The continued search for safe, effective, medications with predictable pharmacokinetic profiles has led to newer alternatives. Dabigatran is a potent reversible, competitive direct thrombin inhibitor which is available as the prodrug, Dabigatran etexilate. It was first approved in Europe and recently in October 2010, the US food and drug administration (FDA) has approved the use of this novel oral anticoagulation for prevention of stroke in those with non valvular atrial fibrillation. This review will cover the chemical structure, mechanism of action, pharmacokinetic profile, clinical trials, dosage, clinical implication and adverse effects of dabigatran.
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Ahmed Shameer, Levin Vadim, Malacoff Robert and W. Martinez Matthew, Dabigatran - A New Chapter in Anticoagulation, Cardiovascular & Hematological Agents in Medicinal Chemistry 2012; 10 (2) . https://dx.doi.org/10.2174/187152512800388911
DOI https://dx.doi.org/10.2174/187152512800388911 |
Print ISSN 1871-5257 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6182 |
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