Zuclopenthixol


Thông tin thuốc gốc
Chỉ định và Liều dùng
Intramuscular
Chronic psychosis
Adult: As zuclopenthixol decanoate ester: Initially, a test dose of 100 mg deep IM into the upper buttock or lateral thigh to assess tolerance, followed after at least 1 week by 200-500 mg every 1-4 weeks, adjusted according to response. Injection volumes >2mL to be distributed between 2 injection sites. Max: 600 mg per week.
Elderly: Reduce dose to ¼ or ½ of usual initial dose.

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.

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
Intramuscular:
Chronic psychosis: Dose reduction may be needed.
Psychoses: Renal failure: Half of the normal dose.
Oral:
Dose reduction may be needed.
Hepatic Impairment
Intramuscular:
Chronic psychosis: Dose reduction may be needed.
Psychoses: Half of the normal recommended dose.
Oral:
Dose reduction may be needed.
Cách dùng
May be taken with or without food.
Chống chỉ định
Hypersensitivity. Comatose states e.g. alcohol, barbiturate and opiate intoxications; porphyria. children.
Thận trọng
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.
Phản ứng phụ
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.
Quá liều
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.
Tương tác
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.
Tác dụng
Description: 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.
Bảo quản
Store below 25°C. Protect from light.
Phân loại MIMS
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