Key result
This review summarizes the chemical structure, kinetics of thrombin inhibition, pharmacokinetics, and clinical use of direct thrombin inhibitors.
Provides a comprehensive overview of the pharmacology and clinical use of direct thrombin inhibitors.
Offers a reference for direct thrombin inhibitor selection in practice; leaves open needs for updated comparative trials.
This review deals with a newly-developed category of antithrombotic drugs - the direct thrombin inhibitors. These agents interact with thrombin and block its catalytic activity on fibrinogen, platelets and other substrates. Heparin and its derivatives (low molecular weight heparins and the active pentasaccharide) inhibit thrombin and/or other coagulation serine proteases indirectly via antithrombin, and the warfarin-type drugs interfere with the synthesis of the precursors of the coagulation serine proteases. The direct thrombin inhibitors approved for clinical use at present (lepirudin, desirudin, bivalirudin, argatroban) and another in the advanced clinical testing stage (melagatran/ximelagatran), are the subject of this review. The chemical structure; kinetics of thrombin inhibition; pharmacokinetics and clinical use of each of these is discussed.
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Karen L. Kaplan (2003) conducted a review in Thrombosis. Direct thrombin inhibitors (lepirudin, desirudin, bivalirudin, argatroban, melagatran/ximelagatran) was evaluated. This review summarizes the chemical structure, kinetics of thrombin inhibition, pharmacokinetics, and clinical use of direct thrombin inhibitors.
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