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.
Export Options
About this article
Cite this article as:
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 |
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
New Advances in the Field of Calcium Channel Antagonists: Cardiovascular Effects and Structure-Activity Relationships
Current Medicinal Chemistry - Cardiovascular & Hematological Agents Rotational Atherectomy in Acute STEMI with Heavily Calcified Culprit Lesion is a Rule Breaking Solution
Current Cardiology Reviews Principles of Clinical Management of Patent Ductus Arteriosus in Extremely Preterm Neonates
Current Pediatric Reviews Preeclampsia: Placental Origins, New Predictors and New Therapeutic Strategies
Current Women`s Health Reviews Pregnancy, Programming and Preeclampsia: Gap Junctions at the Nexus of Pregnancy-induced Adaptation of Endothelial Function and Endothelial Adaptive Failure in PE
Current Vascular Pharmacology Central Blood Pressure in Chronic Kidney Disease: Latest Evidence and Clinical Relevance
Current Hypertension Reviews Regulation of Vascular Endothelium Inflammatory Signalling by Shear Stress
Current Vascular Pharmacology Brain Targeting of siRNA via Intranasal Pathway
Current Pharmaceutical Design Relationships Between Mitochondria and Neuroinflammation: Implications for Alzheimer’s Disease
Current Topics in Medicinal Chemistry Promising Therapies in Sickle Cell Disease
Cardiovascular & Hematological Disorders-Drug Targets Modulating Poly (ADP-Ribose) Polymerase Activity: Potential for the Prevention and Therapy of Pathogenic Situations Involving DNA Damage and Oxidative Stress
Current Pharmaceutical Biotechnology Intratubular Renin-Angiotensin System in Hypertension
Current Hypertension Reviews A Systematic Review of Analytical Profiles of SGLT2 Inhibitors and their Combinations for Treatment of Type 2 Diabetes Mellitus
Current Pharmaceutical Analysis Coronary Atherosclerosis The Implications of Being a Woman
Current Hypertension Reviews Peripheral Blood Mononuclear Cells of Alzheimer's Disease Patients Control CCL4 and CXCL10 Levels in a Human Blood Brain Barrier Model
Current Alzheimer Research Pathogens and Chronic or Long-Term Neurologic Disorders
Cardiovascular & Hematological Disorders-Drug Targets <i>In Silico</i> Study Examining New Phenylpropanoids Targets with Antidepressant Activity
Current Drug Targets Determinants of Human Coronary Collaterals
Current Cardiology Reviews Simultaneous Determination of Fenofibrate, its Metabolite and Co- Formulated/Administered Statins Using Reverse Phase TLC-Densitometry and HPLC-UV Methods: Application in Human Plasma
Current Chromatography Curcumin, an Active Constiuent of the Ancient Medicinal Herb Curcuma longa L.: Some Uses and the Establishment and Biological Basis of Medical Efficacy
CNS & Neurological Disorders - Drug Targets