Subkutane Applikation von Apomorphin - Pharmakologische Eigenschaften und alternative Applikationswege

J. P. Sieb; A. Storch

doi:10.1055/s-2004-834697

Aktuelle Neurologie 2005; 32: 40-44
DOI: 10.1055/s-2004-834697

Übersicht

Subkutane Applikation von Apomorphin - Pharmakologische Eigenschaften und alternative Applikationswege

Subcutaneous Application of Apomorphin - Pharmacological Properties and Alternative FormulationsJ. P. Sieb¹ , A. Storch²

¹Klinik für Neurologie, Geriatrie und Palliativmedizin, Hanse-Klinikum Stralsund
²Klinik und Poliklinik für Neurologie (Direktor: Prof. Dr. Heinz Reichmann), Technische Universität Dresden

Abstract

Zusammenfassung

Apomorphin ist ein Non-Ergot-Aporphinalkaloid vom Dibenzochinolintyp und wirkt als potenter Dopaminagonist. Der schnelle hepatische Metabolismus („First-pass-Effekt”) von Apomorphin macht die orale Applikation unmöglich, sodass die subkutane Injektion in der Therapie des Morbus Parkinson favorisiert wird. Weiterhin sind auch die intranasale, sublinguale, rektale und intravenöse Gabe in der Behandlung des Morbus Parkinson getestet worden. Bei subkutaner Applikation ist die maximale Plasmakonzentration im Mittel nach 10 - 20 Minuten erreicht (T_max), die klinische Wirkung tritt zwischen 7 - 17 Minuten ein. Apomorphin wird im Wesentlichen über nicht enzymatische Oxidation abgebaut, daneben findet die N-Methylierung, Sulfatierung, Glukuronidierung und Catechol-O-Methylierung von Apomorphin statt. In dieser Übersicht werden die pharmakologischen Eigenschaften von subkutan injiziertem Apomorphin detailliert geschildert und die alternativen Applikationswege diskutiert.

Abstract

Apomorphine is a non-ergot aporphine alkaloid with a dibenzoquinoline structure and acts as a potent dopamine agonist. The high hepatic first-pass metabolism of apomorphine prevents its use by the oral route, but the subcutaneous injection is the usual route in the treatment of Parkinson's disease. Furthermore, the intranasal, sublingual, rectal and intravenous application has been investigated in Parkinson's disease. After subcutaneous application the maximal plasma concentration occurs after 10 to 20 minutes (T_max), and the clinical effects start after 7 to 17 minutes. Apomorphin is metabolized mainly by non-enzymatic oxidation, but enzymatic pathways including N-methylation, sulfation, glucuronidation, and catechol-O-methylation are also detected. In the present review we summarize the pharmacological properties of subcutaneously administered apomorphin and discuss the alternative application routes.

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Referenzen

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Prof. Dr. Jörn P. Sieb

Chefarzt der Klinik für Neurologie, Geriatrie und Palliativmedizin · Hanse-Klinikum

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18410 Stralsund

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