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  • Clopixol Acuphase
    / Lundbeck


    Active Ingredient
    Zuclopenthixol (acetate) 50 mg/ml

    Status in Israel
    RX

    Presentation and Status in Health Basket

    Presentation Basket Yarpa Pharmasoft

    Ampoule

    1 X 1 ml X 50 mg/ml

    partial basket chart 8221 3632

    Ampoule

    10 X 1 ml X 50 mg/ml

    partial basket chart 2348 9441

    Ampoule

    1 X 2 ml X 50 mg/ml

    partial basket chart 8222 3633

    Related information


    Dosage

    Adults: Dosage should be individually adjusted according to the condition of the patient. The dose range would normally be 50-150 mg (1-3 ml) i.m., repeated if necessary, preferably with a time interval of 2 to 3 days. In a few patients an additional injection may be needed 24 to 48 hours following the first injection. Zuclopenthixol acetate is not intended for long-term use and duration of treatment should not be more than two weeks. The maximum accumulated dosage in a course should not exceed 400 mg and the number of injections should not exceed four. In the maintenance therapy, treatment should be continued with oral zuclopenthixol or zuclopenthixol decanoate i.m., after the following guidelines:
    Change to oral zuclopenthixol: 2 to 3 days after the last injection of zuclopenthixol acetate a patient who has been treated with 100 mg zuclopenthixol acetate, should be started at an oral dosage of about 40 mg daily, possibly in divided dosages. If necessary the dose can be further increased by 10-20 mg every 2 to 3 days up to 75 mg daily or more.
    Change to zuclopenthixol decanoate: Concomitantly with the (last) injection of zuclopenthixol acetate (100 mg), 200-400 mg (1-2 ml) of zuclopenthixol decanoate 200 mg/ml should be given intramuscularly and repeated every 2nd week. Higher doses or shorter intervals may be needed. Zuclopenthixol acetate and zuclopenthixol decanoate can be mixed in a syringe and given as one injection (co-injection). Subsequent doses of zuclopenthixol decanoate and interval between injections should be adjusted according to the response of the patient.
    Older patients: The dosage may need to be reduced in the older . Maximum dosage per injection should be 100 mg.
    Children:Clopixol-Acuphase is not recommended for use in children due to lack of clinical experience. Reduced renal function Clopixol-Acuphase can be given in usual doses to patients with reduced renal function.
    Reduced liver function: Patients with compromised hepatic function should receive half the recommended dosages and, if possible, a serum level determination is advisable.
    For full details see prescribing information.


    Indications

    Initial treatment of acute psychoses.


    Contra-Indications

    As for other neuroleptics, intolerance to thioxanthenes. Acute alcohol, barbiturate and opiate intoxications, comatose states.


    Special Precautions

    The possibility of development of neuroleptic malignant syndrome (hyperthermia, muscle rigidity, fluctuating consciousness, instability of the autonomous nervous system) exists with any neuroleptic. The risk is possibly greater with the more potent agents. Patients with preexisting organic brain syndrome, mental retardation and opiate and alcohol abuse are overrepresented among fatal cases. Treatment: Discontinuation of the neuroleptic. Symptomatic treatment and use of general supportive measures. Dantrolene and bromocriptine may be helpful. Symptoms may persist for more than a week after oral neuroleptics are discontinued and somewhat longer when associated with the depot forms of the drugs. Like other neuroleptics zuclopenthixol acetate should be used with caution in patients with organic brain syndrome, convulsion and advanced hepatic disease. As described for other psychotropics zuclopenthixol acetate may modify insulin and glucose responses calling for adjustment of the antidiabetic therapy in diabetic patients. As with other drugs belonging to the therapeutic class of antipsychotics, zuclopenthixol acetate may cause QT prolongation. Persistently prolonged QT intervals may increase the risk of malignant arrhythmias. Therefore, zuclopenthixol acetate should be used with caution in susceptible individuals (with hypokalemia, hypomagnesia or genetic predisposition) and in patients with a history of cardiovascular disorders, e.g. QT prolongation, significant bradycardia (<50 beats per minute), a recent acute myocardial infarction, uncompensated heart failure, or cardiac arrhythmia. Concomitant treatment with other antipsychotics should be avoided. Cases of venous thromboembolism (VTE) have been reported with antipsychotic drugs. Since patients treated with antipsychotics often present with acquired risk factors for VTE, all possible risk factors for VTE should be identified before and during treatment with zuclopenthixol acetate and preventive measures undertaken.
    Older people
    Cerebrovascular:
    An approximately 3-fold increased risk of cerebrovascular adverse events have been seen in randomised placebo controlled clinical trials in the dementia population with some atypical antipsychotics. The mechanism for this increased risk is not known. An increased risk cannot be excluded for other antipsychotics or other patient populations. Zuclopenthixol acetate should be used with caution in patients with risk factors for stroke.
    Increased Mortality in Older people with Dementia: Data from two large observational studies showed that older people with dementia who are 3 treated with antipsychotics are at a small increased risk of death compared with those who are not treated. There are insufficient data to give a firm estimate of the precise magnitude of the risk and the cause of the increased risk is not known. Zuclopenthixol acetate is not licensed for the treatment of dementia-related behavioral disturbances.


    Side Effects

    Undesirable effects are for the majority dose dependent. The frequency and severity are most pronounced in the early phase of treatment and decline during continued treatment. Extrapyramidal reactions may occur, especially during the first few days after an injection and in the early phase of treatment. In most cases these side effects can be satisfactorily controlled by reduction of dosage and/or use of antiparkinsonian drugs. The routine prophylactic use of antiparkinsonian drugs is not recommended. Antiparkinsonian drugs do not alleviate tardive dyskinesia and may aggravate them. Reduction in dosage or, if possible, discontinuation of zuclopenthixol therapy is recommended. In persistent akathisia a benzodiazepine or propranolol may be useful.
    For full details see prescribing information.


    Drug interactions

    Combinations requiring precautions for use: Zuclopenthixol acetate may enhance the sedative effect of alcohol and the effects of barbiturates and other CNS depressants. Neuroleptics may increase or reduce the effect of antihypertensive drugs; the antihypertensive effect of guanethidine and similar acting compounds is reduced. Concomitant use of neuroleptics and lithium increases the risk of neurotoxicity. Tricyclic antidepressants and neuroleptics mutually inhibit the metabolism of each other. Zuclopenthixol acetate may reduce the effect of levodopa and the effect of adrenergic drugs. Concomitant use of metoclopramide and piperazine increases the risk of extrapyramidal disorder. Since zuclopenthixol is partly metabolised by CYP2D6 concomitant use of drugs known to inhibit this enzyme may lead to decreased clearance of zuclopenthixol.
    For full details see prescribing information.


    Pregnancy and Lactation

    Pregnancy: Zuclopenthixol acetate should not be administered during pregnancy unless the expected benefit to the patient outweighs the theoretical risk to the foetus. Neonates exposed to antipsychotics (including zuclopenthixol acetate) during the third trimester of pregnancy are at risk of adverse reactions including extrapyramidal and/or withdrawal symptoms that may vary in severity and duration following delivery. There have been reports of agitation, hypertonia, hypotonia, tremor, somnolence, respiratory distress, or feeding disorder. Consequently, newborns should be monitored carefully. Animal studies have shown reproductive toxicity.
    Breast -feeding: As zuclopenthixol is found in breast milk in low concentrations it is not likely to affect the infant when therapeutic doses are used. The dose ingested by the infant is less than 1% of the weight related maternal dose (in mg/kg). Breast-feeding can be continued during zuclopenthixol acetate 4 therapy if considered of clinical importance but observation of the infant is recommended, particularly in the first 4 weeks after giving birth.


    Overdose

    Due to the administration form overdose symptoms are unlikely to occur. Symptoms Somnolence, coma, movement disorders, convulsions, shock, hyperthermia/hypothermia. ECG changes, QT prolongation, Torsade de Pointes, cardiac arrest and ventricular arrhythmias have been reported when administered in overdose together with drugs known to affect the heart. Treatment Treatment is symptomatic and supportive. Measures to support the respiratory and cardiovascular systems should be instituted. Epinephrine (adrenaline) should not be used as further lowering of blood pressure may result. Convulsions may be treated with diazepam and movement disorders with biperiden.


    Manufacturer
    Lundbeck A/S, Denmark
    Licence holder
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