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Zuclopenthixol information from DrugsUpdate  

See Available Brands of Zuclopenthixol in India

Zuclopenthixol (Cisordinol, Clopixol, Acuphase) is a typical antipsychotic neuroleptic drug of the thioxanthene group. It mainly acts by antagonism of D1 and D2 dopamine receptors, though it also has some antihistamine activity. It is produced and marketed by Lundbeck pharmaceutical company.

Pharmacodynamics

Pharmacokinetics

Zuclopenthixol has high affinity for D1 and D2 receptors and α-adrenoreceptors. It also has slight antihistamine properties and blocks serotonergic properties.
Duration: 2-3 days (zuclopenthixol acetate IM).

Absorption
Well absorbed from the GI tract; peak plasma concentrations: 3-6 hours.

Distribution
Protein-binding: 98%. Widely distributed and crosses blood-brain barrier. Crosses the placenta and enters breast milk (small amounts).

Metabolism
Hepatic via sulfoxidation, side-chain N-dealkylation, and glucuronic acid conjugation. Acetate and decanoate esters undergoes hydrolysis after IM injection to release zuclopenthixol.

Excretion
Excreted in faeces as unchanged drug and N-dealkylated metabolite.

Zuclopenthixol Indications / Zuclopenthixol Uses

Information Not Available

Zuclopenthixol Adverse Reactions / Zuclopenthixol Side Effects

Drowsiness, blurred vision, tachycardia, nausea, dizziness, headache, excitement, postural hypotension, hyperprolactinaemia, sexual dysfunction, ECG changes (prolongation of QT interval and T wave changes), hyperthermia. Extrapyramidal symptoms may occur, especially during the early phase of treatment; urinary frequency or incontinence; tardive dyskinesia.

Potentially Fatal: Neuroleptic malignant syndrome, blood dyscrasias.

Precautions

Information Not Available

Special Precautions

Hepatic and renal impairment, heart disease, recent acute MI, arrhythmias, significant bradycardia (<50 beats/min), severe respiratory disease, epilepsy (and conditions at risk of epilepsy, e.g. alcohol withdrawal or brain damage), Parkinson's disease, acute angle glaucoma, prostatic hypertrophy, hypothyroidism, hyperthyroidism, myasthenia gravis, phaeochromocytoma. Patients at risk of stroke and QT interval prolongation. Avoid abrupt withdrawal. Ability to drive a car or operate machinery may be impaired.

Other Drug Interactions

Zuclopenthixol may enhance the sedative effects of alcohol and the effects of barbiturates and other CNS depressants. Zuclopenthixol reduces the antihypertensive effect of guanethidine. Concomitant use of metoclopramide and piperazine with zuclopenthixol increases the risk of extrapyramidal symptoms. Increased risk of severe neurotoxicity with lithium and sibutramine. Increased anticholinergic side effects with drugs with anticholinergic properties.

Potentially Fatal: Antagonises effect of apomorphine, levodopa and other dopamine agonists. Increased risk of blood dyscrasias with clozapine. Increased risk of arrhythmias with dugs that prolong QT interval e.g. class Ia and III antiarrhythmics, erythromycin or cause electrolyte disturbances e.g. thiazide diuretics.

Other Interactions

Information Not Available

Dosage

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 injection. 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 injection should be given in a max course of 2 weeks and total dose should not exceed 400 mg. Maintenance: May start oral zuclopenthixol HCl 2-3 days after the last acetate injection or begin IM injection 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 week by 200-500 mg or more, repeated at 1-4 weekly intervals according to response. Max dose: 600 mg weekly. Injection >2 ml to be distributed between 2 injection 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.

Food(before/after)

May be taken with or without food

List of Contraindications

Zuclopenthixol and Pregnancy

Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.

Zuclopenthixol and Lactation

Information Not Available

Zuclopenthixol and Children

Information Not Available

Zuclopenthixol and Geriatic

Information Not Available

Zuclopenthixol and Other Contraindications

Hypersensitivity. Comatose states e.g. alcohol, barbiturate and opiate intoxications; porphyria. children.

Storage

Intramuscular
Store below 25°C. Protect from light. Oral: Store below 25°C. Protect from light.

Lab interference

Intramuscular
Store below 25°C. Protect from light. Oral: Store below 25°C. Protect from light.

Zuclopenthixol brands in India:

Clopixol Acuphase Clopixol Depot

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