Heparine, Thrombin- und Faktor-Xa-Inhibitoren

Zusammenfassung

Direkte Antikoagulanzien hemmen Serinproteinasen des Gerinnungssystems entweder indirekt über Antithrombin oder Heparin-Kofaktor II oder binden direkt an die einzelnen Serinproteasen. Heparin, niedermolekulare Heparine, Fondaparinux und Idraparinux potenzieren nach Bindung an Antithrombin die Inhibierung einzelner Gerinnungsfaktoren. Hirudin, Argatroban und Melagatran hemmen unabhängig von Antithrombin direkt und reversibel Thrombin. Zum Nachweis des antikoagulanten Effektes stehen globale und spezifische Gerinnungsmethoden zur Verfügung. Neue Antikoagulanzien, insbesondere orale Faktor-Xa- und orale Thrombininhibitoren, sowie Antikörper gegen aktivierten Faktor VII, gentechnologisch hergestellter Tissue-Faktor Pathway-Inhibitor und andere Proteine werden als Antikoagulanzien oder als Substanzen mit nicht antikoagulanten Wirkungen (wie aktiviertes Protein C bei Sepsis) entwickelt. Neue Methoden werden zur Verbesserung der Diagnostik und Therapie thromboembolischer Erkrankungen entwickelt.

Summary

Direct and indirect coagulation inhibitors are used to inhibit the activity of the serine proteases of the coagulation system. Indirect inhibitors act via antithrombin and heparin cofactor II. The main representatives are heparins, lowmolecular-weight heparins, fondaparinux, idraparinux and danaparoid. They bind to antithrombin and potentiate the inactivation of factor Xa and other serine proteases. Direct thrombin inhibitors bind reversibly to thrombin without cofactor. Anticoagulants are determined by global and specific anticoagulant methods. New anticoagulants are developed such as oral factor Xa inhibitors, oral thrombin inhibitors, antibody against activated factor VII, recombinant tissue pathway inhibitor to improve inhibition of blood coagulation or to induce nonanticoagulant effects (e. g. activated protein C in septicaemia). New anticoagulant methods are developed to improve and specify the anticoagulant effect of anticoagulants in thromboembolic diseases.

Schlüsselwörter

Heparin - Thrombininhibitoren - Antikoagulanzien - Gerinnungsmethoden - Thrombose

Keywords

Heparin - thrombin inhibitors - anticoagulants - coagulation methods - thrombosis

• Literatur

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