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Logo CLOPIXOL DEPOT Injection

SCHEDULING STATUS:
S5

PROPRIETARY NAME
(and dosage form:)

CLOPIXOL DEPOT Injection

COMPOSITION:
CLOPIXOL DEPOT Injection is a 200 mg/mL sterile solution of
zuclopenthixol decanoate intended for intramuscular injection.

PHARMACOLOGICAL CLASSIFICATION:
A 2.6.5 Miscellaneous Structures (Thioxanthenes)

PHARMACOLOGICAL ACTION:
CLOPIXOL DEPOT acts as a combined absorption and conversion depot. Absorption depots retain the active substance, releasing it gradually. In conversion depots the active substance is made available as a derivative which is slowly converted to the active substance. By the esterification of zuclopenthixol with decanoic acid, zuclopenthixol has been converted into a highly lipophilic substance, zuclopenthixol decanoate. When dissolved in oil and injected intramuscularly this substance diffuses slowly into the surrounding aqueous tissue fluids, where it undergoes enzymatic breakdown into the active component zuclopenthixol and decanoic acid.
Zuclopenthixol is a neuroleptic of the thioxanthene group.
It is relatively short-acting whereas CLOPIXOL DEPOT - the decanoic acid ester of zuclopenthixol - has a considerably prolonged action.
According to pharmacological and pharmacokinetic animal experiments the effect of CLOPIXOL DEPOT lasts for 10 days to 3 weeks after intramuscular injection, except for the cataleptogenic action which is rather weak and of appreciably shorter duration. Significant serum levels of zuclopenthixol are maintained throughout the dosage interval.

INDICATIONS:
Maintenance treatment of schizophrenia including agitation, psychomotor disturbances, hostility, suspiciousness, aggression and affective reactions.

CONTRA-INDICATIONS:
Acute alcohol, barbiturate and opiate poisoning. CLOPIXOL DEPOT should (preferably) not be administered to pregnant patients. Patients suffering from or with a history of hepatic disease.

WARNINGS:
Patients on long-term therapy should be watched carefully. CLOPIXOL DEPOT should be used with caution in patients with convulsive disorders or advanced hepatic, renal or cardiovascular disease. Alcohol tolerance and the ability to drive motor vehicles and operate machines may be affected. Therefore, caution should be exerted initially, until the individual reaction to the treatment is known.

DOSAGE AND DIRECTIONS FOR USE:
CLOPIXOL DEPOT is administered by deep intramuscular injection into the gluteal region, as a rule in doses of 200 –400 mg (1 –2 mL) at 2 –4 week intervals. A few patients need higher doses or shorter intervals.
Treatment is usually started with 100 mg (½ mL) intramuscularly. One week later, or when the symptoms recur (but not more than 4 weeks later) the second injection of 100 –200 mg (½ - 1 mL) intramuscularly or more is administered.
During maintenance therapy 100 –600 mg (½ - 3 mL) is given intramuscularly every 1 –4 weeks, usually 200 mg (1 mL) every 2 –4 weeks.

SIDE EFFECTS AND SPECIAL PRECAUTIONS;
Extrapyramidal symptoms may occur, especially during the first few days after the injection and the early phase of the treatment. As a rule they can be controlled by antiparkinsonian agents. Initial drowsiness and, in a few patients, weight changes have been reported. Autonomic side-effects may occur.
Tardive dyskinesias, which can be persistent, may occur with long-term therapy. Antiparkinsonian drugs do not alleviate these symptoms. Reduction in dosage or, if possible, discontinuation of therapy is recommended.
CLOPIXOL DEPOT may enhance the response to alcohol and the effects of barbiturates and other CNS depressants. CLOPIXOL DEPOT should not be given concomitantly with guanethidine or similar acting compounds, since neuroleptics may block the antihypertensive effect of these compounds. CLOPIXOL DEPOT may lower the effect of adrenergic drugs and concomitant use of metoclopramide and piperazine increases the risk of extrapyramidal symptoms.

KNOWN SYMPTOMS OF OVERDOSAGE AND PARTICULARS OF ITS TREATMENT:
Zuclopenthixol decanoate is a thioxanthene analogue of perphenazine. Overdosage may lead to chlorpromazine-like extrapyramidal symptoms, somnolence, coma, convulsions and circulatory collapse. Extrapyramidal symptoms can be treated with antiparkinsonian drugs; convulsions are treated cautiously with barbiturates or diazepam. In case of circulatory collapse, the patients should be placed in the head-down position, and noradrenalin administered by intravenous drip (Adrenalin should be avoided). For the prevention of pneumonia, penicillin can be given.

IDENTIFICATION
Clear, yellowish, oil, practically free form particles.

PRESENTATION:
Ampoules of 200 mg/mL: 1 x 1 mL, 5 x 1 mL
Vials of 200 mg/mL: 1 x 10 mL

STORAGE INSTRUCTIONS:
Store below 25°C. Protect from light. Keep out of reach of children.

REGISTRATION NUMBER:
R/2.6.5/52

NAME AND BUSINESS ADDRESS OF THE APPLICANT:
H. LUNDBECK (PTY) LTD
P O BOX 2357
RANDBURG
2125

DATE OF PUBLICATION OF THIS PACKAGE INSERT:
March 1986

Updated on this site: May 2000

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