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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Veröffentlicht in:	Annual review of pharmacology and toxicology Jg. 52; S. 79
Hauptverfasser:	Fareed, Jawed, Thethi, Indermohan, Hoppensteadt, Debra
Format:	Journal Article
Sprache:	Englisch
Veröffentlicht:	United States 01.01.2012
Schlagworte:	Administration, Oral Anticoagulants - pharmacology Antithrombins - adverse effects Antithrombins - therapeutic use Factor Xa Inhibitors Food-Drug Interactions Hemostatics - metabolism Heparin, Low-Molecular-Weight - adverse effects Heparin, Low-Molecular-Weight - therapeutic use Humans Pharmacogenetics Prothrombin - antagonists & inhibitors Thrombin - therapeutic use Thrombosis - drug therapy Vitamin K - antagonists & inhibitors Warfarin - adverse effects Warfarin - therapeutic use
ISSN:	1545-4304, 1545-4304
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Zusammenfassung:	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.
Bibliographie:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 ObjectType-Review-3 content type line 23
ISSN:	1545-4304 1545-4304
DOI:	10.1146/annurev-pharmtox-010611-134633