The importance of thrombin inhibitors in the antithrombotic pharmacotherapy
Journal Title: Postępy Nauk Medycznych - Year 2010, Vol 23, Issue 10
Abstract
Activation of blood coagulation is a physiological process which consists of a series of zymogens that can be converted by limited proteolysis to active enzymes leading to the generation of thrombin. Trombin is a multifunctional plasma serine protease which has a central role in controlling hemostasis. Trombin is responsible for conversion fibrinogen into fibrin, platelet activation and feedback activation of other coagulation factors. Consequently, control of thrombin generation regulates plasma coagulant activity. For this reason the thrombin inhibition is a key for successful novel antithrombotic pharmacotherapy. Thrombin inhibitors are classified as indirect inhibitors (heparin) and direct inhibitors. Currently for clinical use are available 3 parenteral direct thrombin inhibitors: hirudin and bivalirudin which bind both the catalytic site and exosite I of thrombin, and argatroban which binds only to the active site. The next novel class currently available for clinical use are orally bioavailable direct thrombin inhibitors: ximelagatran and dabigatran which reversible bind only to the active site of thrombin molecule. Clinical studies carried in last years show that the most promising drug is dabigatran, which may be an alternative to vitamin K antagonists. This article describes the thrombin generation mechanisms in vivo as well as mechanism of action and pharmacokinetic of indirect and direct thrombin inhibitors currently available in clinical use.
Authors and Affiliations
Michał Bijak, Mateusz Bobrowski
Keywords
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