Depot klopiksol – antipsychotic (neuroleptic) thioxanthene derivative. Klopiksol has a pronounced antipsychotic and specific inhibitory effects. Klopiksol may also provide transient, dose-dependent sedative effect rapid development in which the beginning of therapy (until the antipsychotic action) is advantageous in the treatment of acute and subacute psychoses. Tolerance to the unspecific sedative effect of the drug occurs rapidly.
Due to the specific inhibitory action of the drug is particularly indicated for agitation, anxiety, hostility and aggression.
A single injection of klopiksol-akufaz provides pronounced and rapid weakening of psychotic symptoms. The duration of antipsychotic action of the drug after a single injection is 2-3 days. Nonspecific sedative effect appears after 2 hours, reaching a maximum after about 8 hours, then it decreases significantly and slightly manifested when repeated injections.
Therapeutic effect klopiksol depot significantly prolonged compared to klopiksol. It allows you to confidently carry out continuous antipsychotic medication klopiksol depot, which is especially important for patients who do not meet medical purposes. Klopiksol depot prevents the development of frequent relapses associated with an arbitrary interrupt patients receiving oral medicaments.
Pharmacokinetic and clinical trials klopiksol depot showed that injection of the drug is most suitably performed at intervals of 2-4 weeks.
Pharmacokinetic klopiksol depot dose of 200 mg of 1 every 2 weeks klopiksol equivalent dose for oral administration is 25 mg / day for 2 weeks.
Upon receiving klopiksol inwardly zuclopenthixol Cmax plasma levels achieved after 4 hours Bioavailability zuclopenthixol ingestion -. About 44%.
After the / m-injection klopiksol akufaz zuclopenthixol acetate undergoes enzymatic cleavage into the active component zuclopenthixol, and acetic acid. Serum Cmax achieved zuclopenthixol 24-48 hours (mean 36 hours) after injection. Then concentration decreases slowly, reaching 1/3 of Cmax 3 days after injection.
After the / m klopiksol depot injection zuclopenthixol decanoate undergoes enzymatic cleavage into the active component zuclopenthixol and decanoic acid. Cmax in the blood serum of zuclopenthixol is reached by the end of the first week after injection.
Zuclopenthixol in minor amounts crosses the placental barrier, in small amounts excreted in breast milk.
Metabolism and excretion
The ingestion T1 / 2 is about 20 hours.
After the / m klopiksol depot injection curve zuclopenthixol concentration decreases exponentially, the T1 / 2 of 19 days, which represents the release rate of active substance from the depot.
Metabolites not possess neuroleptic activity; derived mainly from the feces and partially – in the urine.
H. Lundbeck A / S, Denmark
1 ml oily solution contains:
The active ingredient is:
zuclopenthixol decanoate 200 mg;
Acute and chronic schizophrenia and other psychotic disorders, particularly hallucinations, paranoid delusions and disorders of thought; state of agitation, increased anxiety, hostility, aggressiveness.
- chronic hepatitis
- severe cardiovascular disease.
Possible extrapyramidal disorders, tardive dyskinesia, neuroleptic malignant syndrome, drowsiness, dizziness, dry mouth, accommodation disturbance, urinary retention, constipation, tachycardia, orthostatic hypotension, changes in liver samples.
How to accept, acceptance rate and dosage
The drug is administered as deep intramuscular injection in the upper outer quadrant of the gluteal region.
The dose and the interval between injections is determined individually depending on the patient’s condition.
Klopiksol depot (200 mg / ml) for supporting the treatment is administered in doses of 200-400 mg (1-2 ml) every 2-4 weeks. In some cases, may require higher doses or reducing the intervals between injections.
– Transition to klopiksol for ingestion on klopiksol depot intramuscular daily dose (mg) for oral klopiksol x 8 = Dose (mg) klopiksol depot for the / m of 1 every 2 weeks. Klopiksol reception inside should continue during the first week after the first injection, but at a reduced dose.
– Transition to intramuscular administration at klopiksol-akufaz intramuscular depot klopiksol Simultaneously with the closing-injection klopiksol akufaz (100 mg) enter 200-400 mg (1-2 ml) klopiksol depot (200 mg / ml). Repeated injections of depot klopiksol conducted every 2 weeks. If necessary acceptable use of the drug at higher doses or reduction of intervals between injections.
Klopiksol-akufaz and klopiksol depot can be mixed in the same syringe, and to appoint as a single combined injection. Subsequent doses klopiksol depot and intervals between injections should be set depending on the patient’s condition.
Store in the dark place at a temperature not higher than 25 ° C.
With simultaneous application klopiksol may enhance sedative effects of ethanol, barbiturates, and other means of providing a dampening effect on the CNS.
Klopiksol not be used simultaneously with guanetidinom means and with a similar effect (as neuroleptics can block their hypotensive action).
With simultaneous application klopiksol may reduce the effectiveness of levodopa and other adrenergic agents.
With simultaneous use of klopiksol with metoclopramide and piperazine increases the risk of extrapyramidal symptoms.
Pharmaceutical incompatibility is not installed.
Neuroleptic malignant syndrome (CSN) is a rare but possible complication with fatal outcome when used neuroleptics. The main symptoms are CSN hyperthermia, muscle rigidity and disturbance of consciousness in combination with a dysfunction of the autonomic nervous system (labile blood pressure, tachycardia, sweating). In addition to immediate discontinuation of antipsychotic drugs is essential to use the general supportive measures and symptomatic treatment.
When long-term therapy, especially in large doses, it is necessary to conduct a thorough inspection, periodically assessing the condition of the patients to take to reduce the maintenance dosage of the solution.
Possible influence klopiksol Depot on driving ability and other mechanisms. Therefore, at the beginning of therapy, care should be taken until then, until it is determined by the patient’s response to treatment.
Pregnancy and lactation
Klopiksol not recommended for use during pregnancy and lactation (breastfeeding).
Symptoms: drowsiness, coma, extrapyramidal disorders, convulsions, hypotension, shock, hyper- or hypothermia
Treatment: In case the drug must be both inside the stomach can be flushed more quickly, it is recommended the use of the sorbent. Subsequently symptomatic and supportive therapy.
It is necessary to take measures aimed at maintaining the activity of the respiratory and cardiovascular systems. You should not use adrenaline.