Clopixol Depot, 200 mg/ml 1 ml 10 pcs

Clopixol Depot is an antipsychotic (neuroleptic), a thioxanthene derivative. 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 nonspecific sedative effect of the drug occurs quickly.

The drug is especially indicated for agitation, anxiety, hostility, or aggressiveness because of its specific inhibitory effect.

A single injection of Clopixol-Acufase 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

Acute and chronic schizophrenia and other psychotic disorders, especially with hallucinations, paranoid delusions and thought disorders; states of agitation, increased anxiety, hostility, aggressiveness.

Active ingredient

Composition

1 ml of oily solution contains:

Active ingredient:

Zuclopentixol decanoate 200 mg;

Compound:

triglycerides

How to take, the dosage

The drug is administered 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) in maintenance treatment is administered in doses of 200-400 mg (1-2 ml) every 2-4 weeks. In some cases, higher doses or shorter injection intervals may be necessary.

Transition from oral Clopixol to intramuscular Clopixol depot Daily dose (mg) of oral Clopixol x 8 = dose (mg) of Clopixol depot for intramuscular injection once every 2 weeks. Oral administration of Clopixol should be continued for the first week after the first injection, but at a reduced dose.

Transition from intramuscular injection of Clopixol-Acufase to intramuscular injection of Clopixol Depot Simultaneously with the final injection of Clopixol-Acufase (100 mg), 200-400 mg (1-2 ml) of Clopixol Depot (200 mg/mL) should be given. Repeat injections of Clopixol depot every 2 weeks. If necessary, the drug may be used in higher doses or reduced intervals between injections.

Clopixol-Acufaz 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 according to the patient’s condition.

Interaction

In concomitant use Clopixol may increase the sedative effect of ethanol, barbiturates and other CNS depressant drugs.

Clopixol should not be used concomitantly with guanethidine and agents with similar effects (because neuroleptics may block their hypotensive effect).

Concomitant use of Clopixol may decrease the effectiveness of levodopa and other adrenergic agents.

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

Pharmaceutical incompatibility has not been established.

Special Instructions

Malignant neuroleptic syndrome (MNS) is a rare but possible fatal complication of neuroleptic use. The main symptoms of MNS are hyperthermia, muscle rigidity and impaired consciousness combined with autonomic nervous system dysfunction (labile blood pressure, tachycardia, increased sweating). In addition to immediate discontinuation of neuroleptics, the use of general supportive measures and symptomatic treatment is essential.

In long-term therapy, especially at high doses, careful monitoring is necessary, periodically assessing patients’ condition to decide whether to reduce the maintenance dosage.

Clopixol Depot may affect the ability to drive and operate other machinery. Therefore, caution should be exercised at the beginning of therapy until the patient’s response to treatment has been determined.

Contraindications

Side effects

Possible extrapyramidal disorders, tardive dyskinesia, malignant neuroleptic syndrome, drowsiness, dizziness, dry mouth, accommodation disorders, urinary retention, constipation, tachycardia, orthostatic hypotension, changes in liver function tests.

Overdose

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

Treatment: if the drug is taken orally the stomach should be flushed as soon as possible, sorbent usage is recommended. Further symptomatic and supportive therapy is carried out.

Measures should be taken to maintain respiratory and cardiovascular system activity. Adrenaline should not be used.

Pregnancy use

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

Similarities