Zuclopenthixol

Indications
 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.

Special Populations: Lower doses are recommended for elderly patients and those with hepatic dysfunction.
Contraindications
 Hypersensitivity. Comatose states e.g. alcohol, barbiturate and opiate intoxications; porphyria. children.
Warnings / 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.
Adverse Reactions
 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.
Overdose Reactions
 Symptoms: Somnolence, extrapyramidal symptoms, convulsions, hypotension, shock, hyper or hypothermia, ECG changes e.g. QT prolongation, torsade de pointes, cardiac arrest, ventricular arrhythmias and coma. Management: Treatment is symptomatic and supportive with close monitoring of the respiratory and CV systems. Do not use adrenaline (epinephrine) in these patients.
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.
See Below for More zuclopenthixol Drug Interactions
Mechanism of Actions
 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 hr.
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 inj to release zuclopenthixol.
Excretion: Excreted in faeces as unchanged drug and N-dealkylated metabolite.
Administration
 May be taken with or without food.
Storage Conditions
 Intramuscular: Store below 25°C. Protect from light. Oral: Store below 25°C. Protect from light.
ATC Classification
 N05AF05 - zuclopenthixol ; Belongs to the class of thioxanthene derivatives antipsychotics.
Storage
 Intramuscular: Store below 25°C. Protect from light. Oral: Store below 25°C. Protect from light.
Available As
  • Zuclopenthixol 200 mg
  • Zuclopenthixol 25 mg
  • Zuclopenthixol 50 mg

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