Composition
1 coated tablet contains:
Active ingredient:
zuclopentixol (in the form of dihydrochloride) 2 mg.
Auxiliary substances:
potato starch,
lactose monohydrate,
microcrystalline cellulose,
copovidone,
85% glycerol,
talc,
hydrogenated castor oil,
magnesium stearate.
Pharmacological action
Clopixol is an antipsychotic (neuroleptic) drug derived from thioxanthene. Clopixol has a pronounced antipsychotic and specific inhibitory effect.
Clopixol may also have a transient, dose-dependent sedative effect, the rapid development of which at the beginning of therapy (before the onset of antipsychotic action) is an advantage in the treatment of acute and subacute psychoses. Tolerance to the non-specific sedative effect of the drug occurs quickly. Due to its specific inhibitory effect, the drug is especially indicated for agitation, anxiety, hostility or aggressiveness.
A single injection of Clopixol-akufaz provides a pronounced and rapid relief of psychotic symptoms. The duration of the antipsychotic effect of the drug after one injection is 2-3 days. The non-specific sedative effect manifests itself in 2 hours, reaches a maximum in about 8 hours, then significantly decreases and is poorly manifested with repeated injections.
The therapeutic effect of Clopixol depot is significantly more prolonged than that of Clopixol. This allows us to confidently conduct continuous antipsychotic treatment with Clopixol depot, which is especially important for patients who do not perform medical appointments. Clopixol depot prevents the development of frequent relapses associated with arbitrary interruption of oral medication by patients.
Pharmacokinetics
Pharmacokinetic and clinical trials of Clopixol depot have shown that injections of the drug are most appropriate at intervals of 2-4 weeks.
Pharmacokinetically, the dose of Clopixol depot 200 mg once every 2 weeks is equivalent to the oral dose of Clopixol 25 mg / day for 2 weeks.
Suction
After oral use of Clopixol, the Cmax of zuclopentixol in blood plasma is reached in 4 hours. The bioavailability of zuclopentixol when taken orally is about 44%.
After intravenous injection of Clopixol-acufase, zuclopentixol acetate undergoes enzymatic cleavage into the active component zuclopentixol and acetic acid. Cmax of zuclopentixol in blood serum is reached in 24-48 hours (on average,36 hours) after injection. The concentration then slowly decreases, reaching 1/3 of the Cmax 3 days after injection.
After intravenous injection of Clopixol, zuclopentixol depot decanoate undergoes enzymatic cleavage into the active component zuclopentixol and decanoic acid. Cmax of zuclopentixol in blood serum is reached by the end of the first week after injection.
Distribution
Zuclopentixol penetrates the placental barrier in small amounts, and is excreted in breast milk in small amounts.
Metabolism and elimination
When taken orally, T1 / 2 is approximately 20 hours.
After intravenous injection of Clopixol depot, the zuclopentixol concentration curve decreases exponentially, with T1 / 2 being 19 days, which reflects the rate of release of the Active ingredient from the depot.
Metabolites do not have neuroleptic activity; they are mainly excreted in the faeces and partially in the urine.
Indications
- acute and chronic schizophrenia and other psychotic disorders, particularly hallucinations, paranoid delusions, and impaired thinking;
- the state of agitation, increased anxiety, hostility, aggressiveness;
- manic phase of manic-depressive psychosis,
- mental retardation, combined with psychomotor agitation, agitation and other behavioral disorders;
- senile dementia with paranoid ideas, disorientation, impaired behavior, confusion.
Use during pregnancy and lactation
Contraindicated. Nursing mothers should stop breastfeeding.
Contraindications
- acute alcohol intoxication;
- acute intoxication with barbiturates;
- acute intoxication with opioid analgesics;
- comatose states.
Side effects
From the nervous system. Extrapyramidal symptoms may develop, especially at the initial stage of treatment. In most cases, they are corrected by reducing dosages and / or prescribing Antiparkinsonian drugs. However, regular preventive use of the latter is not recommended.
In rare cases, patients may develop tardive dyskinesia with prolonged therapy. Antiparkinsonian medications do not eliminate its symptoms. It is recommended to reduce the dosage or, if possible, discontinue therapy.
From the side of mental activity. Drowsiness in the initial stage.
From the autonomic nervous system and cardiovascular system. Dry mouth, poor accommodation, urinary retention, constipation, tachycardia, orthostatic hypotension, and dizziness.
From the liver. Minor transient changes in liver tests are rarely observed.
The interaction
of chemically incompatible combinations has not been established.
Clopixol may enhance the sedative effects of alcohol, barbiturates, and other central nervous system inhibitors.
Clopixol should not be administered together with guanethidine and similar active agents, since neuroleptics can block their antihypertensive effect.
Clopixol may reduce the effectiveness of levodopa and other adrenergic agents, and the combination with metoclopramide and piperazine increases the risk of extrapyramidal symptoms.
How to take, course of use and dosage
Doses of the drug should be selected individually, depending on the patient’s condition. As a rule, small doses should be used initially, which are then rapidly increased to the optimal effective level, depending on the clinical effect.
Acute attack of schizophrenia, other acute psychotic disorders; severe agitation and mania. Usually 10-50 mg/day.
For severe disorders and conditions of moderate severity, the initial dose of 20 mg / day can be increased by 10-20 mg after 2-3 days to 75 mg / day or more, if necessary.
Chronic psychotic states in schizophrenia and other chronic psychoses. The maintenance dose is 20-40 mg / day.
Agitation in patients with oligophrenia. Usually 6-20 mg/day. If necessary, the dose can be increased to 25-40 mg / day.
Agitation and confusion in patients with senile disorders. Usually 2-6 mg / day (preferably given in the evening), if necessary, you can increase to 10-20 mg / day.
Overdose
Symptoms: Â drowsiness, coma, extrapyramidal disorders, seizures, hypotension, shock, hyper – or hypothermia are possible.
Treatment: Â if the drug is taken orally, it is necessary to flush the stomach as soon as possible, and the use of a sorbent is recommended. In the future, symptomatic and supportive therapy is carried out.
Measures should be taken to maintain the functioning of the respiratory and cardiovascular systems. Do not use epinephrine (epinephrine), as this may lead to a further decrease in blood pressure. Seizures can be stopped with diazepam, and extrapyramidal symptoms with biperiden.
Special instructions
Clopixol may affect the ability to drive a car and other mechanisms.
Therefore, caution should be exercised at the beginning of therapy until the patient’s response to treatment is determined.
With long-term therapy, it is necessary to carefully monitor the condition of patients.
With extreme caution, Clopixol should be prescribed to patients with convulsive syndrome, chronic hepatitis and cardiovascular diseases.
Clopixol is not recommended for use during pregnancy and lactation.
Form of production
Film-coated tablets
Storage conditions
At a temperature not exceeding 25 °C
Shelf life
5 years
Active ingredient
Zuclopentixol
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
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