Zusammenfassung
Vitamin-K-Antagonisten und Heparine sind seit Jahrzehnten Mittel der Wahl zur Gerinnungshemmung. Trotz ihrer guten Wirksamkeit ist ihr Einsatz mit Limitationen verbunden, was zur Entwicklung neuer Substanzen geführt hat. Diese hemmen direkt und spezifisch entweder Thrombin oder Faktor Xa. Vielversprechend sind die orale Applikation und die fixe Dosis ohne notwendige Laborüberwachung. Zugelassen sind der Thrombininhibitor Dabigatranetexilat und die Faktor-Xa-Inhibitoren Rivaroxaban und Apixaban zur postoperativen Thromboseprophylaxe nach Hüft- und Kniegelenkersatz. Dabigatranetexilat ist seit August 2011 zur Antikoagulation bei Vorhofflimmern zugelassen, Rivaroxaban wird in den nächsten Monaten folgen. Zulassungen für weitere Indikationen wie z. B. Therapie und Sekundärprophylaxe vernöser Thromboembolien sind in Planung. Im Umgang mit diesen neuen oralen Antikoagulanzien ist das Wissen um deren Pharmakokinetik und -dynamik wichtig. Sie beeinflussen die Gerinnungsdiagnostik und erschweren deren Interpretation. Gleichzeitig gibt es gegenwärtig keinen etablierten Gerinnungstest, um die Antikoagulation im Fall von Blutungen zu überwachen. Spezifische Antidots für die neuen oralen Antikoagulanzien stehen noch nicht zur Verfügung.
Abstract
Vitamin K antagonists and heparins have been standard anticoagulation drugs over the past decades. They are effective and safe but they have several drawbacks which has led to the development of new oral anticoagulants. Dabigatran etexilate is a specific oral thrombin inhibitor and rivaroxaban and apixaban are oral inhibitors of factor Xa. These agents produce a predictable anticoagulant response after fixed-dose administration so that routine coagulation monitoring is unnecessary. Currently, dabigatran etexilate, rivaroxaban and apixaban are licensed for thromboprophylaxis after elective total hip or knee replacement surgery. Since august 2011, dabigatran etexilate is licensed for patients with atrial fibrillation, rivaroxaban will follow. However, indications will be expanded e.g. for therapy of venous thromboembolism. It is important to be aware of the pharmacokinetic and pharmacodynamic profiles of these new agents. The drugs considerably influence the global test of coagulation thus making an interpretation of test results difficult. Currently, there is a lack of suitable coagulation tests to monitor anticoagulation in emergency cases, such as bleeding. Specific antidotes are not yet available.
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Interessenkonflikt
Die korrespondierende Autorin weist auf folgende Beziehungen hin: K. Heidinger hat von folgenden Unternehmen Aufwandsentschädigung für Vortragstätigkeit bzw. Teilnahme an Studien erhalten: Bayer Health Care, Roche Diagnostics, Pfizer, Boehringer Ingelheim. B. Kemkes-Matthes hat von folgenden Industrieunternehmen Aufwandsentschädigung für Berater- oder Vortragstätigkeit bzw. Teilnahme an Studien erhalten: Bayer Health Care, CSL Behring, Novo Nordisk Pharma, Pfizer, Boehringer Ingelheim, Baxter, Siemens Diagnostics.
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Heidinger, K., Kemkes-Matthes, B. Neue Antithrombotika. Med Klin 106, 198–204 (2011). https://doi.org/10.1007/s00063-011-0014-9
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DOI: https://doi.org/10.1007/s00063-011-0014-9
Schlüsselwörter
- Faktor Xa/Antagonisten und Inhibitoren
- Direkte Thrombininhibitoren
- Administration, oral
- Blutgerinnung
- Blutgerinnungsteste