Old versus new oral anticoagulants: focus on pharmacology Journal Article


Authors: Fareed, J; Thethi, I.; Hoppensteadt, D
Article Title: Old versus new oral anticoagulants: focus on pharmacology
Abstract: 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.
Journal Title: Annual Review of Pharmacology Toxicology
Volume: 52
ISSN: 1545-4304
Publisher: Unknown  
Journal Place: United States
Date Published: 2012
Start Page: 79
End Page: 99
Language: English
DOI/URL:
Notes: ID: 12323; Record Owner: From MEDLINE, a database of the U.S. National Library of Medicine.; Status: MEDLINE; [Review]; Publishing Model: Journal available in: Print-Electronic Citation processed from: Internet; NLM Journal Code: 6e4, 7607088; CAS Registry/EC Number/Name of Substance: 0 (Anticoagulants). 0 (Antithrombins). 0 (Hemostatics). 0 (Heparin, Low-Molecular-Weight). 12001-79-5 (Vitamin K). 81-81-2 (Warfarin). 9001-26-7 (Prothrombin). 9002-04-4 (Factor IIa). EC 3-4-21-5 (Thrombin). EC 3-4-21-6 (Factor Xa).; Electronic Date of Publication: 20110805; Entry Date: 20120503