title: Apomorphine - pharmacological properties and clinical trials in Parkinson's disease.
abstract: Apomorphine is often considered an archetypal dopamine agonist used in the treatment of Parkinson's disease (PD). However, it can be clearly differentiated from most other commonly used dopamine agonists on the basis of its pharmacology and on its unique clinical profile. Like levodopa and dopamine, apomorphine acts as a potent, direct and broad spectrum dopamine agonist activating all dopamine receptor subtypes. It also has affinity for serotonin receptors, and α-adrenergic receptors. Apomorphine is usually titrated to a dose that provides an equivalent antiparkinsonian response to that provided by levodopa, and its subcutaneous delivery allows a rapid onset of action, usually within 7-10 min. The mode of apomorphine delivery impacts on its clinical profile so as to provide two very different approaches to therapy in PD. When administered as an acute subcutaneous injection, it induces reliable and rapid relief from OFF periods underscoring its utility as a rescue medication. When given as a subcutaneous infusion, it significantly improves overall daily OFF time and there is also evidence to suggest that, in those patients who replace most or all of their oral drugs with apomorphine infusion, dyskinesia may also improve. In this paper, we review the rich pharmacology of apomorphine and review its efficacy in PD based on data from clinical trials.
authors.affiliation: Neurodegenerative Diseases Research Group, Institute of Pharmaceutical Sciences, Faculty of Life Science and Medicine, King's College London, London, UK. Electronic address: peter.jenner@kcl.ac.uk.
authors.forename: Peter
authors.initials: P
authors.lastname: Jenner
authors.affiliation: Department of Neurology and Karl Landsteiner Institute for Neuroimmunological and Neurodegenerative Disorders, Danube Hospital, Vienna, Austria. Electronic address: regina.katzenschlager@wienkav.at.
authors.forename: Regina
authors.initials: R
authors.lastname: Katzenschlager
mesh_terms: D000818:Animals; D000978:Antiparkinson Agents / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use*; D001058:Apomorphine / Q000737:chemistry / Q000494:pharmacology* / Q000627:therapeutic use*; D002986:Clinical Trials as Topic; D006801:Humans; D010300:Parkinson Disease / Q000188:drug therapy*
chemical_list: D000978:Antiparkinson Agents; D001058:Apomorphine
keywords: Apomorphine; Clinical trial; Parkinson's disease; Pharmacokinetics; Pharmacology; Receptor profile