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DOI: 10.12687/phleb2319-4-2016
Der lange Weg zu den NOAK
Eine Zeitreise vom Naturprodukt zur gezielten Gerinnungshemmung Artikel in mehreren Sprachen: English | deutschPublikationsverlauf
Received:
27. Juni 2016
Accepted:
28. Juni 2016
Publikationsdatum:
21. Dezember 2017 (online)
Zusammenfassung
Vor 100 Jahren war der Ablauf der Blutgerinnung nur in groben Zügen bekannt und über den Wirkmechanismus des damals entdeckten gerinnungshemmenden Wirkstoffs Heparin gab es nur vage Vorstellungen. Infolge des raschen pragmatischen Einsatzes haben Heparin, so wie auch das in den 20er- Jahren entwickelte Warfarin, einen jahrzehntelangen Siegeszug angetreten. Erst gegen Ende des letzten Jahrhunderts gelang die Synthese von Antikoagulanzien mit gezieltem Wirkmechanismus, wie z. B. dem Faktor-Xa-Hemmer Fondaparinux oder die rekombinante Herstellung des direkten Thrombinhemmers Hirudin, dicht gefolgt von der Synthese der Nicht-Vitamin-K-antagonistischen oralen Antikoagulanzien (NOAK). Letztere wurden seit Anfang des 21. Jahrhunderts klinisch entwickelt und sind mittlerweile für verschiedene Indikationen verfügbar. NOAK zeichnen sich durch reproduzierbare orale Bioverfügbarkeit, kurze Halbwertszeit im Vergleich zu Vitamin- K-Antagonisten, geringe Interaktionen mit anderen Arzneimitteln, fixe Dosierung ohne Laborkontrolle sowie ein günstigeres Nutzen-/ Risikoprofil als die konventionellen Gerinnungshemmer aus. Beim Einsatz dieser Präparate ist zu beachten, dass es Unterschiede in der Metabolisierung, der renalen Eliminierung und den Dosierungsregeln gibt.
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