Klinische Pharmakologie von Apomorphin

Zusammenfassung

In dieser Übersicht werden die historische Entwicklung, Struktur, Wirkweise, pharmakologischen Eigenschaften und Nebenwirkungen von Apomorphin zusammengefasst. Apomorphin ist ein kurz wirksamer D1- und D2-Rezeptoragonist. Subkutan appliziertes Apomorphin wird zur Behandlung von Off-Phasen im Rahmen motorischer Fluktuationen bei Morbus Parkinson intermittierend oder als kontinuierliche Infusion eingesetzt. Aufgrund der ausgeprägten hepatischen Metabolisierung (First-Pass-Effekt) ist eine orale Therapie nicht praktikabel. Daneben wurden jedoch auch der intranasale, sublinguale, rektale und intravenöse Einsatz in der Behandlung des Morbus Parkinson in Studien untersucht. Nach einer subkutanen Injektion wird die maximale Blutkonzentration nach 10–20 min erreicht und die klinische Wirkung beginnt nach 7–17 min. Die Metabolisierung von Apomorphin erfolgt überwiegend durch eine nicht enzymatische Oxidation.

Abstract

The article reviews the historical background, structure, mechanism of action, pharmacologic properties and side effects of apomorphine. This short-acting D1 and D2 receptor agonist was the first dopamine receptor agonist used to treat Parkinson's disease. Subcutaneous apomorphine is currently used for the management of „off states” in fluctuating Parkinson's disease either as intermittent rescue injections or as continuous infusions. The high hepatic first-pass metabolism of apomorphine prevents an oral therapeutic use. Beside a subcutaneous application, intranasal, sublingual, rectal and intravenous routes of application have been investigated in Parkinson's disease. After subcutaneous injection the maximum blood concentration occurs after 10–20 minutes and the clinical effects start after 7–17 minutes. Apomorphine is metabolized mainly by non-enzymatic oxidation.

Schlüsselwörter

Anti-Parkinson-Therapie - Injektion, subkutan - Neuroprotektion - Parkinson - Pharmakokinetik - Rezeptor - Dopamin

Keywords

administration - antiparkinson agents - injections, subcutaneous - neuroprotective agents - Parkinson - pharmacokinetics - receptors - dopamine

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