Zuclopenthixol
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| Trade names | Clopixol |
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Oral, IM |
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| Pharmacokinetic data | |
| Bioavailability | 49% (oral) |
| Protein binding | 98% |
| Metabolism | Hepatic (CYP2D6 and CYP3A4-mediated) |
| Biological half-life | 20 hours (oral), 19 days (IM) |
| Excretion | Feces |
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| ECHA InfoCard | 100.053.398 |
| Chemical and physical data | |
| Formula | C22H25ClN2OS |
| Molar mass | 400.965 g/mol |
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Zuclopenthixol (Cisordinol, Clopixol, Acuphase), also known as zuclopentixol, is a typical antipsychotic drug of the thioxanthene class. It was introduced in 1962 by Lundbeck. It is the cis-isomer of clopenthixol.
Zuclopenthixol is a D1 and D2 antagonist, α1-adrenergic and 5-HT2 antagonist. It is not approved for use in the United States.
Zuclopenthixol is available in three major preparations:
It is also used in the treatment of acute bipolar mania.
As a long acting injection, zuclopenthixol decanoate comes in a 200 mg and 500 mg ampoule. Doses can vary from 50 mg weekly to the maximum licensed dose of 600 mg weekly. In general, the lowest effective dose to prevent relapse is preferred. The interval may be shorter as a patient starts on the medication before extending to 3 weekly intervals subsequently. The dose should be reviewed and reduced if side effects occur, though in the short term an anticholinergic medication benztropine may be helpful for tremor and stiffness, while diazepam may be helpful for akathisia. 100 mg of zuclopenthixol decanoate is roughly equivalent to 20 mg of flupentixol decanoate or 12.5 mg of fluphenazine decanoate.
In acutely psychotic and agitated inpatients, 50 – 200 mg of zuclopenthixol acetate may be given for a calming effect over the subsequent three days, with a maximum dose of 400 mg in total to be given. As it is a long-acting medication, care must be taken not to give an excessive dose.
In oral form zuclopenthixol is available in 10, 25 and 40 mg tablets, with a dose range of 20–60 mg daily.
Zuclopenthixol antagonises both dopamine D1 and D2 receptors, α1-adrenoceptors and 5-HT2 receptors with a high affinity, but has no affinity for cholinergic muscarine receptors. It weakly antagonises the histamine (H1) receptor but has no α2-adrenoceptor blocking activity.
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