Zuclopenthixol

Indications

Zuclopenthixol is used for: Schizophrenia, Psychoses, Bipolar mania

Adult Dose

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. 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. Hepatic impairment: Half of the normal recommended dose. 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. Hepatic impairment: Dose reduction may be needed.

Child Dose

Renal Dose

Renal impairment: Dose reduction may be needed.

Administration

May be taken with or without food.

Contra Indications

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

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.

Pregnancy-Lactation

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.

Adverse Effects

Side effects of Zuclopenthixol : 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.

Mechanism of Action

Zuclopenthixol has high affinity for D1 and D2 receptors and ?-adrenoreceptors. It also has slight antihistamine properties and blocks serotonergic properties.