Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2022 Publisher: Lundbeck Limited, Iveco House, Station Road, Watford, Hertfordshire, WD17 1ET, United Kingdom
Pharmacotherapeutic group: Neuropleptics (antipsychotics)
ATC Code: N05AF05
The action of zuclopenthixol, as with other antipsychotics is mediated through dopamine receptor blockade. Zuclopenthixol has a high affinity for D1 and D2 receptors and activity has been demonstrated in standard animal models used to assess antipsychotic action. Serotonergic blocking properties, a high affinity for alpha-adrenoreceptors and slight antihistamine properties have been observed.
After deep intramuscular injection of Clopixol, serum levels of zuclopenthixol increase during the first week and decline slowly thereafter. A linear relationship has been observed between Clopixol dosage and serum level. Metabolism proceeds by sulphoxidation, dealkylation and glucuronic acid conjugation. Sulphoxide metabolites are mainly excreted in the urine while unchanged drug and the dealkylated form tend to be excreted in the faeces.
Impaired mating performance and reduced conception rates were observed in rats treated with zuclopenthixol at doses equal to the maximum recommend human dose of 50 mg on a mg/m² basis.
There was no evidence of embryotoxicity or teratogenic effects in rats treated with zuclopenthixol, however adverse effects on pre-and postnatal development (i.e. increased stillbirths, reduced pup survival and delayed development of pups) was observed. The clinical significance of these findings is unclear and it is possible that the effect on pups was due to neglect from the dams that were exposed to doses of zuclopenthixol producing maternal toxicity.
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