Source: Medicines & Healthcare Products Regulatory Agency (GB) Revision Year: 2021 Publisher: Lundbeck Limited, Iveco House, Station Road, Watford, Hertfordshire, WD17 1ET, UK
Pharmacotherapeutic group: Neuroleptics (antipsychotics)
ATC code: N05AF01
The precise pharmacological mode of action of flupentixol has not been determined. It has been postulated that at low dosage flupentixol binds to presynaptic dopamine receptors causing increased neurotransmitter release.
There is evidence that postsynaptic aminergic receptors become down regulated in response to increased levels of neurotransmitter and this is responsible for the observed improvement in depressive symptoms.
Mean oral bioavailability is about 55%. Maximum drug serum concentrations occur about 4 hours after dosing and the biological half-life is about 35 hours.
Flupentixol is widely distributed in the body. Metabolism is by sulphoxidation, N-dealkylation and glucuronic acid conjugation. Excretion is via the urine and faeces.
In fertility studies in rats, flupentixol slightly affected the pregnancy rate of female rats. Animal reproduction studies in mice, rats and rabbits have not shown evidence of teratogenic effects. Embryotoxic effects in terms of increased post implantation loss/increased absorption rates or occasional abortions were seen in rats and rabbits at doses associated with maternal toxicity.
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