Clopixol depot solution 200mg/ml 1ml ampoules, 10pcs

Composition

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1 ml of oil solution contains:

Active ingredient:

zuclopentixol decanoate 200 mg;

Auxiliary substance:

Triglycerides

Pharmacological action

Clopixol Depot 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, especially with hallucinations, paranoid delusions and thinking disorders; states of agitation, increased anxiety, hostility, aggressiveness.

Use during pregnancy and lactation

Clopixol is not recommended for use during pregnancy and lactation (breastfeeding).

Contraindications

• chronic hepatitis
• severe cardiovascular diseases.

Side effects

Extrapyramidal disorders, tardive dyskinesia, neuroleptic malignant syndrome, drowsiness, dizziness, dry mouth, accommodation disorders, urinary retention, constipation, tachycardia, orthostatic hypotension, changes in liver tests are possible.

Interaction

When used concomitantly, Clopixol may enhance the sedative effect of ethanol, barbiturates and other drugs that have a depressing effect on the central nervous system.

Clopixol should not be used simultaneously with guanethidine and drugs with a similar effect (since neuroleptics can block their antihypertensive effect).

When used concomitantly, Clopixol may reduce the effectiveness of levodopa and other adrenergic agents.

Concomitant use of Clopixol with metoclopramide and piperazine increases the risk of extrapyramidal symptoms.

No pharmaceutical incompatibility has been established.

How to take, course of use and dosage

The drug is prescribed as a deep intramuscular injection into the upper outer quadrant of the gluteal region.

The dose and interval between injections are determined individually, depending on the patient’s condition.

Clopixol depot (200 mg / ml) with maintenance treatment is administered in doses of 200-400 mg (1-2 ml) every 2-4 weeks. In some cases, higher doses or shorter intervals between injections may be required.

– Switching from Clopixol for oral use to intramuscular use of Clopixol depot Daily dose (mg) of Clopixol for oral use x 8 = dose (mg) of Clopixol depot for intravenous use 1 time in 2 weeks. Oral use of Clopixol should be continued for the first week after the first injection, but at a reduced dose.

– Switching from intramuscular use of Clopixol-akufaz to intramuscular use of Clopixol depot Simultaneously with the final injection of Clopixol-akufaz (100 mg),200-400 mg (1-2 ml) of Clopixol depot (200 mg/ml) should be administered. Repeated injections of Clopixol depot are performed every 2 weeks. If necessary, it is acceptable to use the drug in higher doses or reduce the intervals between injections.

Clopixol-akufaz and Clopixol depot can be mixed in one syringe and administered as one combined injection. Subsequent doses of Clopixol depot and intervals between injections should be set depending on the patient’s condition.

Overdose

Symptoms:  drowsiness, coma, extrapyramidal disorders, seizures, hypotension, shock, hyper – or hypothermia are possible.

Treatment:  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.

Special instructions

Neuroleptic malignant syndrome (NMS) is a rare but possible complication with a fatal outcome when using neuroleptics. The main symptoms of NMS are hyperthermia, muscle rigidity and impaired consciousness in combination with dysfunction of the autonomic nervous system (labile blood pressure, tachycardia, increased sweating). In addition to immediate discontinuation of antipsychotic medications, general supportive measures and symptomatic treatment are essential.

With long-term therapy, especially in high doses, it is necessary to conduct careful monitoring, periodically assessing the condition of patients in order to make a decision on reducing the maintenance dosage.

It is possible that Clopixol Depot affects 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.

Form of production

Solution for intramuscular use (oil)

Storage conditions

Store in a dark place at a temperature not exceeding 25°C.

Shelf

life is 3 years.

Active ingredient

Zuclopentixol

Conditions of release from pharmacies

By prescription

Dosage form

solution for injection