Chemical formula: C₁₇H₁₇NO₂ Molecular mass: 267.322 g/mol PubChem compound: 6005
Apomorphine is a direct stimulant of dopamine receptors and while possessing both D1 and D2 receptor agonist properties does not share transport or metabolic pathways with levodopa.
Although in intact experimental animals, administration of apomorphine suppresses the rate of firing of nigro-striatal cells and in low dose has been found to produce a reduction in locomotor activity (thought to represent pre-synaptic inhibition of endogenous dopamine release) its actions on parkinsonian motor disability are likely to be mediated at post-synaptic receptor sites. This biphasic effect is also seen in humans.
After subcutaneous injection of apomorphine its fate can be described by a two-compartment model, with a distribution half-life of 5 (± 1.1) minutes and an elimination half-life of 33 (± 3.9) minutes. Clinical response correlates well with levels of apomorphine in the cerebrospinal fluid; the drug distribution being best described by a two- compartment model.
Apomorphine is rapidly and completely absorbed from subcutaneous tissue, correlating with the rapid onset of clinical effects (4-12 minutes), and that the brief duration of clinical action of the drug (about 1 hour) is explained by its rapid clearance. The metabolism of apomorphine is by glucuronidation and sulphonation to at least ten per cent of the total; other pathways have not been described.
Repeat-dose subcutaneous toxicity studies reveal no special hazard for humans, beyond the information included in other sections.
In vitro genotoxicity studies demonstrated mutagenic and clastogenic effects, most likely due to products formed by oxidation of apomorphine. However, apomorphine was not genotoxic in the in vivo studies performed.
The effect of apomorphine on reproduction has been investigated in rats. Apomorphine was not teratogenic in this species, but it was noted that doses which are toxic to the mother can cause loss of maternal care and failure to breathe in the newborn.
No carcinogenicity studies have been performed.
Apomorphine is a well-established active substance and have been on the market for 10 years, it is our conclusion that no environmental risk assessment is needed for this active substance.
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