Zusammenfassung
Die neu entwickelten HMG-CoA-Reduktase-Inhibitoren stellen aufgrund ihres klar definierten Wirkmechanismus, ihrer hohen klinischen Wirksamkeit und ihrer einfachen Applikationsform einen wesentlichen Fortschritt in der Therapie von Fettstoffwechselstörungen dar. Derzeit sind in Deutschland drei Cholesterinsynthese-Enzymhemmer, nämlich Lovastatin, Simvastatin und Pravastatin verfügbar. Die lipophilen CSE-Hemmer Lovastatin und Simvastatin sind Prodrugs, die nach oraler Applikation durch ubiquitär vorkommende Esterasen in ihre aktive ß-Hydroxysäureform überführt werden. Das hydrophile Pravastatin weist dagegen von vornherein die aktive ß-Hydroxy- säureform auf. Gerade diese unterschiedlichen Charakteristika der CSE- Hemmer - Prodrug versus aktive Form, Hydrophilie versus Lipophilie - werden derzeit im Hinblick auf ihre klinische Relevanz kontrovers diskutiert (24).
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Dammann, H.G. (1992). CSE-Hemmer: Besitzen Hydrophilie oder Lipophilie dieser Substanzen eine klinische Relevanz?. In: Schneider, J., Steinmetz, A., Kaffarnik, H. (eds) Hyperlipoproteinämie. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-77813-1_4
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