Thienopyridine (Ticlopidin, Clopidogrel)

Zusammenfassung

Thienopyridine (Ticlopidin und Clopidogrel) hemmen spezifisch die ADP-medi- ierten Mechanismen der Thrombozytenaktivierung. Der genaue molekulare Wirkmechanismus der Thrombozytenfunktionshemmung durch Thienopyridine ist nicht bekannt. Nach bisherigen Daten beruht das wirksame Prinzip auf einer nichtkompetitiven und möglicherweise irreversiblen Reduktion der ADP-Rezep- tordichte auf Thrombozytenmembranen. Im Gegensatz zu früheren Annahmen, nach denen Thienopyridine »Prodrugs« sind und für ihre Wirksamkeit einer hepatischen Bioaktivierung bedürfen, konnte in neueren Arbeiten eine ln-vitro- Wirksamkeit dieser Substanzen nachgewiesen werden. Klinisch weisen die Thienopyridine eine gut gesicherte Wirksamkeit auf. So zeigte Clopidogrel in der kürzlich publizierten CAPRIE-Studie bei Patienten mit symptomatischer Atherosklerose eine geringe aber statistisch signifikante Überlegenheit gegenüber Acetylsalicylsäure hinsichtlich der Prävention von Schlaganfall, Myokardinfarkt und vaskulärem Tod. Neutropenien, wie sie unter Ticlopidin bei etwa einem Prozent der Patienten beobachtet werden, traten unter Clopidogrel nicht auf. Dennoch muß das Nebenwirkungsprofil dieser im Vergleich zur Acetylsalicylsäure noch jungen Substanz sorgfältig beobachtet werden.

Schlüsselwörter

Thienopyridine - Ticlopidin - Clopidogrel - Pharmakologie

• LITERATUR

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