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: Neuroleptics (antipsychotics)
ATC Code: N05AF05
The action of zuclopenthixol, as with other antipsychotics is mediated through dopamine receptor blockage.
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.
Zuclopenthixol given orally in man is relatively quickly absorbed and maximum serum concentrations are reached in 3-6 hours. There is good correlation between the dose of zuclopenthixol and the concentrations achieved in serum. The biological half-life in man is about one day.
Zuclopenthixol is distributed in the liver, lungs, intestines and kidney, with somewhat lower concentration in the brain. Small amounts of drug or metabolites cross the placenta and are excreted in milk.
Zuclopenthixol is metabolised by sulphoxidation, N-Dealkylation and glucuronic acid conjugation.
The faecal route of excretion predominates and mostly unchanged zuclopenthixol and N-dealkylated metabolite are excreted in this way.
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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