Old Versus New Oral Anticoagulants: Focus on Pharmacology

Since the discovery of heparin nearly a century ago, there have been large gaps in the development of anticoagulants. The discovery of warfarin was the first step toward using oral anticoagulants, but warfarin use has been associated with its own challenges from the perspectives of the prescribing p...

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Bibliographic Details
Published in:Annual review of pharmacology and toxicology 2012-01, Vol.52 (1), p.79-99
Main Authors: FAREED, Jawed, THETHI, Indermohan, HOPPENSTEADT, Debra
Format: Article
Language:English
Subjects:
Administration, Oral
Anticoagulants - pharmacology
Antithrombins - adverse effects
Antithrombins - therapeutic use
Biological and medical sciences
Blood. Blood coagulation. Reticuloendothelial system
Factor Xa Inhibitors
Food-Drug Interactions
Hemostatics - metabolism
Heparin, Low-Molecular-Weight - adverse effects
Heparin, Low-Molecular-Weight - therapeutic use
Humans
Medical sciences
Pharmacogenetics
Pharmacology. Drug treatments
Prothrombin - antagonists & inhibitors
Thrombin - therapeutic use
Thrombosis - drug therapy
Vitamin K - antagonists & inhibitors
Warfarin - adverse effects
Warfarin - therapeutic use
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Summary:Since the discovery of heparin nearly a century ago, there have been large gaps in the development of anticoagulants. The discovery of warfarin was the first step toward using oral anticoagulants, but warfarin use has been associated with its own challenges from the perspectives of the prescribing physician and the patient. Warfarin, along with other coumarins, has a narrow therapeutic index, requires frequent monitoring, exhibits interindividual response variations, and is associated with several adverse effects. Frequent drug and food interactions contribute to potential safety and efficacy compromise. The indications for use of oral anticoagulants have increased, as these drugs are used not only for thrombosis management but also for cardiovascular indications, producing more challenges for oral anticoagulant use. Factor Xa and thrombin targeting has provided a rational approach to develop new oral anticoagulants with improvements over warfarin. In this review, the pharmacology of warfarin and the pharmacology of the newly developed oral anti-Xa and antithrombin agents are discussed.
ISSN:0362-1642
1545-4304
DOI:10.1146/annurev-pharmtox-010611-134633