Zuclopenthixol

Oral

Psychoses

Adult: Initially, 20-30 mg daily in divided doses. Usual maintenance dose: 20-50 mg daily. Up to 150 mg daily for severe or resistant cases.

Renal impairment: Dose reduction may be needed.

Hepatic impairment: Dose reduction may be needed.

Intramuscular

Psychoses

Adult: As acetate: 50-150 mg via deep IM inj. May repeat, if needed, after 2-3 days. An additional dose 1-2 days after the 1st dose may be required in some patients. Not >4 inj should be given in a max course of 2 wk and total dose should not exceed 400 mg.

Maintenance: May start oral Zuclopenthixol HCl 2-3 days after the last acetate inj or begin IM inj of decanoate with the last inj of the acetate.

Elderly: As acetate ester: Dose reduction may be needed. Max: 100 mg/dose.

Renal impairment: Renal failure: Half of the normal dose.

Hepatic impairment: Half of the normal recommended dose.

Intramuscular

Chronic psychosis

Adult: As decanoate ester: Initially, a test dose of 100 mg by deep IM into the upper outer buttock or lateral thigh to access tolerance, followed after at least 1 wk by 200-500 mg or more, repeated at 1-4 wkly intervals according to response. Max dose: 600 mg wkly. Inj >2 ml to be distributed between 2 inj sites.

Elderly: Reduce dose to ¼ or ½ of usual initial dose.

Renal impairment: Dose reduction may be needed.

Hepatic impairment: Dose reduction may be needed.

Oral

Psychoses

Adult: Initially, 20-30 mg daily in divided doses. Usual maintenance dose: 20-50 mg daily. Up to 150 mg daily for severe or resistant cases.

Renal impairment: Dose reduction may be needed.

Hepatic impairment: Dose reduction may be needed.

Intramuscular

Psychoses

Adult: As acetate: 50-150 mg via deep IM inj. May repeat, if needed, after 2-3 days. An additional dose 1-2 days after the 1st dose may be required in some patients. Not >4 inj should be given in a max course of 2 wk and total dose should not exceed 400 mg.

Maintenance: May start oral Zuclopenthixol HCl 2-3 days after the last acetate inj or begin IM inj of decanoate with the last inj of the acetate.

Elderly: As acetate ester: Dose reduction may be needed. Max: 100 mg/dose.

Renal impairment: Renal failure: Half of the normal dose.

Hepatic impairment: Half of the normal recommended dose.

Intramuscular

Chronic psychosis

Adult: As decanoate ester: Initially, a test dose of 100 mg by deep IM into the upper outer buttock or lateral thigh to access tolerance, followed after at least 1 wk by 200-500 mg or more, repeated at 1-4 wkly intervals according to response. Max dose: 600 mg wkly. Inj >2 ml to be distributed between 2 inj sites.

Elderly: Reduce dose to ¼ or ½ of usual initial dose.

Renal impairment: Dose reduction may be needed.

Hepatic impairment: Dose reduction may be needed.

Acute alcohol, barbiturate or opiate intoxication;

CNS depression due to any cause, comatose states, suspected or established subcortical brain damage, circulatory collapse, blood dyscrasias, or pheochromocytoma;

Known hypersensitivity to the thioxanthenes, Zuclopenthixol or any of the excipients of the product

Zuclopenthixol is used for the initial treatment of short-term psychoses like mania or increased severity of existing psychoses. It is also used to treat schizophrenia (psychiatric disorder with symptoms of emotional instability, detachment from reality, often with delusions and hallucinations, and withdrawal into the self).

Zuclopenthixol enhances the sedative response to alcohol and the effects of barbiturates and other CNS depressants. It should not be administered with high doses of hypnotics due to the possibility of potentiation.

Zuclopenthixol should not be given concomitantly with guanethidine or similar acting compounds, since antipsychotic drugs such as Zuclopenthixol may block the antihypertensive effect of these compounds.

Many antipsychotic and antidepressant drugs may mutually inhibit the metabolism of each other.

Concomitant use of metoclopramide or piperazine increases the risk of extrapyramidal symptoms.

Zuclopenthixol may antagonize the effects of levodopa and dopamine agonists

The most common adverse events reported were drowsiness, fatigue, dizziness, and extrapyramidal symptoms. Body as a Whole: Allergic reaction, application site disorder, arthritis, back pain, chest pain, precordial chest pain, conjunctivitis, faintness, fever, hot flushes and toothache.

Psychiatric: Drug dependence, excitability, irritability, increased libido, melancholia and paroniria.

Neurological: Acute dyskinesia, ataxia, convulsions, hyperreflexia, hypotonia, migraine, oculogyric crisis, and speech disorder.

Gastrointestinal: Abdominal pain, dysphagia, gastric ulcer, glossitis and meteorism.

Cardiovascular: Hypotension.

Respiratory: Dyspnea, nasal congestion, pharyngitis and rhinitis.

Hematological: Purpura.

Special Senses: Mydriasis, hyperacusis and tinnitus.

Skin and Appendages: Dermatitis, photosensitivity reaction, abnormal pigmentation, rash, erythematous rash and psoriasiform rash.

Urinary: Polyuria, urinary incontinence, urinary infection and urinary retention.

Reproductive: Erectile dysfunction, galactorrhea, gynecomastia and dry vagina.

In the worldwide postmarketing surveillance database (1964 to 1993; >1,000,000 treated; >80% of the database from Scandinavia, Netherlands, Switzerland and the UK) the following additional serious adverse events have been rarely reported: Neuroleptic Malignant Syndrome (57 cases); apnoea and respiratory depression (13 cases); sudden death (5 cases), agranulocytosis (5 cases).

Alterations in liver function, particularly increased bilirubin levels have occasionally been reported. Transient increases in ALT and ALP values may also occur. Transient, benign leucopenia has been reported rarely. Peripheral edema has occasionally been reported.

Zuclopenthixol, also known as Zuclopentixol or Zuclopenthixolum, is an antipsychotic agent. Zuclopenthixol is a thioxanthene-based neuroleptic with therapeutic actions similar to the phenothiazine antipsychotics. It is an antagonist at D1 and D2 dopamine receptors. Major brands of Zuclopenthixol are Cisordinol, Acuphase, and Clopixol. This drug is a liquid. This compound belongs to the thioxanthenes. These are organic polycyclic compounds containing a thioxanthene moiety, which is an aromatic tricycle derived from xanthene by replacing the oxygen atom with a sulfur atom. Known drug targets of Zuclopenthixol include 5-hydroxytryptamine receptor 2A, D(1B) dopamine receptor, D(2) dopamine receptor, D(1A) dopamine receptor, and alpha-1A adrenergic receptor. It is known that Zuclopenthixol is metabolized by Cytochrome P450 2D6. Zuclopenthixol was approved for use in Canada in 2011, but is not approved for use in the United States.