Apomorphine in dopaminergic therapy

Mol Pharm. 2006 Jul-Aug;3(4):380-5. doi: 10.1021/mp060012c.

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.

Publication types

  • Historical Article
  • Review

MeSH terms

  • Antiparkinson Agents / administration & dosage
  • Antiparkinson Agents / chemistry
  • Antiparkinson Agents / history
  • Antiparkinson Agents / therapeutic use*
  • Apomorphine / administration & dosage
  • Apomorphine / chemistry
  • Apomorphine / history
  • Apomorphine / therapeutic use*
  • Dopamine Agonists / administration & dosage
  • Dopamine Agonists / chemistry
  • Dopamine Agonists / history
  • Dopamine Agonists / therapeutic use*
  • Drug Stability
  • History, 20th Century
  • Humans
  • Parkinson Disease / drug therapy
  • Structure-Activity Relationship

Substances

  • Antiparkinson Agents
  • Dopamine Agonists
  • Apomorphine