Clopixol, 2 mg 50 pcs.

Clopixol is an antipsychotic (neuroleptic), a derivative of 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 psychosis. Tolerance to the unspecific sedative effect of the drug comes quickly. Because of its specific inhibitory effect, the drug is especially indicated for agitation, anxiety, hostility or aggressiveness.

A single injection of Clopixol-Acufaz 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. A nonspecific sedative effect is seen after 2 hours, reaches its maximum after about 8 hours, after which it is significantly reduced and is weak with repeated injections.

The therapeutic effect of Clopixol depot is significantly more prolonged compared to Clopixol. This allows for confidence in continuous antipsychotic treatment with Clopixol Depot, which is especially important for patients who do not comply with physician’s orders. Clopixol depot prevents the development of frequent relapses associated with patients arbitrarily interrupting their oral medications.

Pharmacokinetics

Pharmacokinetic and clinical trials of Clopixol Depot have shown that injections of the drug are most appropriately given at 2-4 week intervals.

Pharmacokinetically, a dose of Clopixol depot 200 mg once every 2 weeks is equivalent to an oral dose of Clopixol of 25 mg/day for 2 weeks.

Intestinal absorption

After oral administration of Clopixol, the Cmax of zuclopentixol in plasma is reached after 4 hours. The bioavailability of zuclopentixol when taken orally is about 44%.

After injection of Clopixol-Acufase zuclopentixol acetate undergoes enzymatic cleavage into the active component zuclopentixol and acetic acid. The Cmax of zuclopentixol in blood serum is reached 24-48 hours (on average 36 hours) after injection. Then the concentration slowly decreases, reaching 1/3 of the Cmax 3 days after injection.

After injection of Clopixol depot zuclopentixol 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 passes through the placental barrier in small amounts, in small amounts is excreted with breast milk.

Metabolism and excretion

The T1/2 when ingested is approximately 20 hours.

The zuclopentixol depot concentration curve decreases exponentially following an oral injection with a T1/2 of 19 days, reflecting the rate of release of the active ingredient from the depot.

The metabolites have no neuroleptic activity; they are excreted mainly in the feces and partially in the urine.

Indications

Active ingredient

Composition

1 coated tablet contains:

The active ingredient:

Zuclopentixol (in dihydrochloride form) 2 mg.

Auxiliary substances:

Potato starch,

lactose monohydrate,

microcrystalline cellulose,

copovidone,

glycerol 85%,

talc,

/p>

castor oil hydrogenated,

magnesium stearate.

How to take, the dosage

Doses of the drug should be adjusted individually depending on the patient’s condition. As a rule, low doses should be used initially, which are then rapidly increased to the optimal effective level depending on the clinical effect.

An acute attack of schizophrenia, other acute psychotic disorders; severe agitation and mania. Usually 10-50 mg/day.

In severe and moderately severe disorders, the initial dose of 20 mg/day may be increased by 10-20 mg after 2-3 days to 75 mg per day or more, if necessary.

Chronic psychotic conditions in schizophrenia and other chronic psychoses. A maintenance dose of 20-40 mg/day.

Agitation in patients with oligophrenia. Usually 6-20 mg/day. If necessary, the dose may 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), can be increased to 10-20 mg/day if necessary.

Interaction

No chemically incompatible combinations have been established.

Clopixol may increase the sedative effect of alcohol, barbiturates and other central nervous system inhibitors.

Clopixol should not be prescribed with guanethidine and similarly acting agents because neuroleptics may block their hypotensive effects.

Clopixol may decrease the effectiveness of levodopa and other adrenergic agents, and combination with metoclopramide and piperazine increases the risk of extrapyramidal symptoms.

Special Instructions

The effect of Clopixol on the ability to drive and operate other mechanisms is possible.

Therefore, caution should be exercised at the beginning of therapy until the patient’s response to treatment has been determined.

In long-term therapy, patients should be closely monitored.

Clopixol should be administered with particular caution to patients with seizure disorder, chronic hepatitis, and cardiovascular disease.

Clopixol is not recommended during pregnancy and lactation.

Contraindications

Side effects

Nervous system disorders. Extrapyramidal symptoms may develop, especially at the initial stage of treatment. In most cases they are corrected by dosage reduction and/or administration of antiparkinsonian drugs. However, regular prophylactic use of the latter is not recommended.

In rare cases, patients may develop tardive dyskinesia with prolonged therapy. Antiparkinsonian drugs do not eliminate its symptoms. Dosage reduction or, if possible, discontinuation of therapy is recommended.

Psychiatric activity. Sleepiness in the initial stage.

An autonomic nervous system and cardiovascular system side. Dry mouth, impaired accommodation, urinary retention, constipation, tachycardia, orthostatic hypotension and dizziness.

Liver disorders. Rarely, minor transient changes in liver function tests have been noted.

Overdose

Symptoms: Drowsiness, coma, extrapyramidal disorders, seizures, arterial hypotension, shock, hyper- or hypothermia may occur.

Treatment: If the drug is ingested, the stomach should be flushed as soon as possible, the use of a sorbent is recommended. Subsequently, symptomatic and supportive therapy is carried out.

Measures should be taken to maintain respiratory and cardiovascular system activity. Epinephrine (adrenaline) should not be used, as it may lead to further BP lowering. Seizures can be controlled with diazepam and extrapyramidal symptoms with biperiden.

Pregnancy use

Contraindicated. Nursing mothers should stop breastfeeding.

Similarities