title: Apomorphine in dopaminergic therapy.
abstract: Apomorphine is a potent molecule for the treatment of Parkinson's disease (PD). It can be obtained in both the R and S forms, and it is the former that is the therapeutically active form. Due to its structural similarity with 3,4-dihydroxyphenethylamine, dopamine, apomorphine can function as an agonist in the treatment of PD as it can stimulate both the D1 and D2 receptors of the striatum. The clinical efficacy of apomorphine is similar to that of 3,4-dihydroxyphenylalanine, levodopa (L-dopa), the cornerstone drug in dopaminergic therapy. (R)-Apomorphine is efficacious for one of the most challenging aspects in the management of PD, namely, managing the unpredictable "on-off" period as a rescue medication after oral administration of a therapeutic drug such as L-dopa. The effectiveness is due to its rapid control of the wearing-off period of the orally administered medicine. This short review will trace the progress of apomorphine use starting with its initial discovery and the first indications for which it was used, discovery of its "cure" for PD, and the studies that led to demonstrating its therapeutic efficacy. The key structural features of apomorphine responsible for its activity are illustrated along with major issues of chemical stability. From a drug delivery point of view, the current form of administration of apomorphine and some of the potential alternate methods of delivery are reviewed.
authors.affiliation: ALZA Corporation, 1900 Charleston Road, Mountain View, California 94043, USA. asubramo@alzus.jnj.com
authors.forename: J Anand
authors.initials: JA
authors.lastname: Subramony
mesh_terms: D000978:Antiparkinson Agents / Q000008:administration & dosage / Q000737:chemistry / Q000266:history / Q000627:therapeutic use*; D001058:Apomorphine / Q000008:administration & dosage / Q000737:chemistry / Q000266:history / Q000627:therapeutic use*; D018491:Dopamine Agonists / Q000008:administration & dosage / Q000737:chemistry / Q000266:history / Q000627:therapeutic use*; D004355:Drug Stability; D049673:History, 20th Century; D006801:Humans; D010300:Parkinson Disease / Q000188:drug therapy; D013329:Structure-Activity Relationship
chemical_list: D000978:Antiparkinson Agents; D018491:Dopamine Agonists; D001058:Apomorphine