Oral heparin: status review
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BioMed Central
Open Access
Review
Oral heparin: status review Ehud Arbit*, Michael Goldberg, Isabel Gomez-Orellana and Shingai Majuru Address: Emisphere Technologies Inc. 765 Old Saw Mill River Road. Tarrytown, NY 10591, USA Email: Ehud Arbit* - [email protected]; Michael Goldberg - [email protected]; Isabel GomezOrellana - [email protected]; Shingai Majuru - [email protected] * Corresponding author
Published: 10 May 2006 Thrombosis Journal 2006, 4:6
doi:10.1186/1477-9560-4-6
Received: 14 February 2006 Accepted: 10 May 2006
This article is available from: http://www.thrombosisjournal.com/content/4/1/6 © 2006 Arbit et al; licensee BioMed Central Ltd. This is an Open Access article distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/2.0), which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
Abstract Unfractionated heparin and low molecular weight heparin are the most commonly used antithrombotic and thromboprophylactic agents in hospital practice. Extended out-of-hospital treatment is inconvenient in that these agents must be administered parenterally. Current research is directed at development of a safe and effective oral antithrombotic agent as an alternative for the effective, yet difficult to use vitamin K antagonists. A novel drug delivery technology that facilitates transport of drugs across the gastrointestinal epithelium has been harnessed to develop an oral dosage form of unfractionated heparin. Combining unfractionated heparin with the carrier molecule, sodium N-(8 [2-hydroxybenzoyl]amino) caprylate, or SNAC has markedly increased the gastrointestinal absorption of this drug. Preclinical and clinical studies to-date suggests that oral heparin-SNAC can confer a clinical efficacious effect; further confirmation is sought in planned clinical trials.
Introduction The current use of anticoagulants is extensive and it is estimated that 0.7% of the population in the Western world receive these drugs [1]. Broader indications for anticoagulants and their increased use in the outpatient settings as well as for long-term dosing has stimulated renewed interest in developing oral anticoagulant and antithrombotic agents. At present, the cornerstone of oral anticoagulants are the vitamin K antagonists, of which the coumarin derivative warfarin, (Coumadin) is the most widely used. It has been used clinically for more than 50 years, and has consistently demonstrated that adequate dosing virtually eliminates recurrent venous thrombosis [2,3]. Nevertheless, warfarin has serious drawbacks that require steady vigilance on the part of clinicians. These drawbacks include significant drug-drug and food-drug interactions, a slow onset and offset of effect, and a narrow therapeutic index. Because of the inherent variability in response over
time and the consequently unpredictable pharmacodynamics of the drug, frequent monitoring is necessary, an inconvenience for the large numb
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