Abstract
Direct thrombin inhibitors represent a new class of anticoagulants that bind directly to thrombin and block the enzymes interactions with its substrates. These agents have been developed, at least in part, to overcome the limitations of heparin and vitamin K antagonists. This paper (a) reviews why thrombin is an ideal target for new anticoagulants, (b) describes the pharmacological profiles of the various direct thrombin inhibitors, (c) outlines the potential mechanistic advantages of parenteral direct thrombin inhibitors over heparin, (d) defines the potential benefits of ximelagatran, the first orally active direct thrombin inhibitor, over vitamin K antagonists, and (e) provides clinical perspective on the strengths and weaknesses of the various parenteral and oral direct thrombin inhibitors.
Keywords: Anticoagulants, thromboxane, heparin-induced thrombocytopenia (HIT), Hirudin, Ximelagatran, Vitamin K antagonists
Current Pharmaceutical Design
Title: Pharmacology and Clinical Potential of Direct Thrombin Inhibitors
Volume: 11 Issue: 30
Author(s): L- A. Linkins and J. I. Weitz
Affiliation:
Keywords: Anticoagulants, thromboxane, heparin-induced thrombocytopenia (HIT), Hirudin, Ximelagatran, Vitamin K antagonists
Abstract: Direct thrombin inhibitors represent a new class of anticoagulants that bind directly to thrombin and block the enzymes interactions with its substrates. These agents have been developed, at least in part, to overcome the limitations of heparin and vitamin K antagonists. This paper (a) reviews why thrombin is an ideal target for new anticoagulants, (b) describes the pharmacological profiles of the various direct thrombin inhibitors, (c) outlines the potential mechanistic advantages of parenteral direct thrombin inhibitors over heparin, (d) defines the potential benefits of ximelagatran, the first orally active direct thrombin inhibitor, over vitamin K antagonists, and (e) provides clinical perspective on the strengths and weaknesses of the various parenteral and oral direct thrombin inhibitors.
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Cite this article as:
Linkins A. L- and Weitz I. J., Pharmacology and Clinical Potential of Direct Thrombin Inhibitors, Current Pharmaceutical Design 2005; 11 (30) . https://dx.doi.org/10.2174/138161205774580598
DOI https://dx.doi.org/10.2174/138161205774580598 |
Print ISSN 1381-6128 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-4286 |
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