Pharmacology Of Apomorphine

Indication For the acute, intermittent treatment of hypomobility, off episodes (end-of-dose wearing off and unpredictable on/off episodes) associated with advanced Parkinson's disease.
Pharmacodynamics Apomorphine is a type of dopaminergic agonist, a morphine derivative which primarily affects the hypothalamic region of the brain. Drugs containing this substance are sometimes used in the treatment of Parkinson's disease or erectile dysfunction. In higher doses it is a highly effective emetic.
Mechanism of action The precise mechanism of action of apomorphine as a treatment for Parkinson's disease is unknown, although it is believed to be due to stimulation of post-synaptic dopamine D2-type receptors within the brain. Apomorphine has been shown to improve motor function in an animal model of Parkinson's disease. In particular, apomorphine attenuates the motor deficits induced by lesions in the ascending nigrostriatal dopaminergic pathway with the neurotoxin 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) in primates.
Absorption 100% following subcutaneous administration
Volume of distribution
  • 123 to 404 L
Protein binding ~50%-albumin
Metabolism Hepatic
Route of elimination Not Available
Half life 40 minutes (range 30 - 60 minutes)
Clearance
  • 223 L/hr
Toxicity LD50=0.6 mmoles/kg (mice, intraperitoneal)