Zuclopenthixol

Intramuscular
Chronic psychosis

Intramuscular
Psychoses

Oral
Psychoses

Intramuscular:
Chronic psychosis: Dose reduction may be needed.
Psychoses: Renal failure: Half of the normal dose.
Oral:
Dose reduction may be needed.

Intramuscular:
Chronic psychosis: Dose reduction may be needed.
Psychoses: Half of the normal recommended dose.
Oral:
Dose reduction may be needed.

May be taken with or without food.

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

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.

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.

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.

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.

Description:
Mechanism of Action: 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).
Pharmacokinetics:
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.

Store below 25°C. Protect from light.

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