CLOPIXOL PILLS 2MG

Mechanism of action

Antipsychotic (neuroleptic), a derivative of thioxanthene. Clopixol has a pronounced antipsychotic and specific inhibitory effect; the latter is particularly indicated with agitation, anxiety, hostility, or aggressiveness. Clopixol may also have a transient, dose-dependent, nonspecific 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 nonspecific sedative effect of the drug comes quickly.
A single injection of Klopiksol-Akufaz provides a pronounced and rapid relief of psychotic symptoms. The duration of the antipsychotic action of the drug after a single injection is 2-3 days. Nonspecific sedation appears after 2 hours, reaches a maximum after about 8 hours, then decreases significantly and weakly appears with repeated injections.
The therapeutic effect of Clopixol Depot is significantly more prolonged compared to Clopixol. This allows you to confidently carry out 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 the voluntary interruption of oral medication by patients.

Pharmacokinetic and clinical trials of Klopixol Depot showed that it is most advisable to inject the drug at intervals of 2-4 weeks.
Pharmacokinetic dose of Klopixol Depot 200 mg 1 time in 2 weeks is equivalent to the oral dose of Clopixol, which is 25 mg / day for 2 weeks.
Suction
After taking Clopixol inside Cmax Plasma zuclopentixol is reached after 4 h. The oral bioavailability is about 44%.
After the i / m injection of Klopixol-Akufaz Zuclopentixol Acetate is subjected to enzymatic cleavage on the active ingredient Zuclopentixol and acetic acid. Cmax Zuclopentixol in serum is reached in 24-48 hours (on average, 36 hours) after injection. Then the concentration slowly decreases, reaching 1/3 of Cmax 3 days after injection.
After the intramuscular injection of Klopixol Depot zuclopentixol, the decanoate undergoes enzymatic cleavage into the active component zuclopentixol and decanoic acid. Cmax Serum zuclopentixol is reached by the end of the first week after injection. The concentration curve of zuclopentixol decreases exponentially, while T1/2 is 19 days, which reflects the rate of release of the active substance from the depot.
Distribution
Zuclopentixol in small quantities penetrates the placental barrier, in small quantities excreted in breast milk.
Removal
Ingestion T1/2 is approximately 20 h.
Metabolites do not possess neuroleptic activity; mainly derived from feces and, in part, with the urine.

- acute and chronic schizophrenia and other psychotic disorders, especially with hallucinations, paranoid delusions and mental disorders;
- states 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, behavior disorders, confusion.
Klopiksol-Akufaz
- initial treatment of acute psychosis, including manic states, and chronic psychosis in the acute phase.
Clopixol Depot
- acute and chronic schizophrenia and other psychotic disorders, especially with hallucinations, paranoid delusions and mental disorders;
- states of agitation, increased anxiety, hostility, aggressiveness.

The drug is taken orally, the daily dose is divided into several doses. At the beginning of treatment, it is recommended to use the drug in low doses, which then, depending on the patient's response to treatment, quickly increase to achieve the optimal clinical effect.
At acute attack of schizophrenia and other acute psychotic disorders, severe agitation and mania The dose of the drug is usually 10-50 mg / day.
At moderate and severe psychotic disorders The initial dose is 20 mg / day and, if necessary, can be increased by 10-20 mg with an interval of 2-3 days to 75 mg / day or more.
At chronic schizophrenia and other chronic psychosis maintenance dose is 20-40 mg / day.
At agitation in patients with oligophrenia the dose is 6-20 mg / day, if necessary, the dose can be increased to 25-40 mg / day.
At senile disorders accompanied by agitation and confusion, the drug is prescribed in a dose of 2-6 mg / day, if necessary, it is possible to increase the dose to 10-20 mg / day; more preferred intake in the evening.
Klopiksol-Akufaz
The drug is prescribed as a deep intramuscular injection in the upper outer quadrant of the gluteal region.
The dose is selected individually depending on the patient's condition.
The recommended volume in the / m injection is 1-3 ml (50-150 mg). If necessary, repeated injections are carried out with an interval of 2-3 days. For some patients, an additional injection may be given 24-48 hours after the first injection.
Maintenance therapy should be continued with Klopixol for oral administration or with Klopixol Depot IM in accordance with the recommendations below.
Clopixol Depot
The drug is prescribed as a 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.
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. If the volume of the solution for i / m administration (200 mg / ml) exceeds 2-3 ml, then it is preferable to use Clopixol Depot solution of a higher concentration (500 mg / ml).
Clopixol depot (500 mg / ml) is usually administered in doses of 250-750 mg (0.5-1.5 ml) every 1-4 weeks.
Transition from Clopixol for oral administration on intramuscular injection of Clopixol depot
Daily dose (mg) Klopixol for oral administration x 8 = dose (mg) Clopixol depot for the / m injection 1 time in 2 weeks.
Intake of Clopixol inside should be continued within the first week after the first injection, but in the reduced dose.
Transfer c v / m injection Klopiksola-Akufaz to receive Clopixol inside
2-3 days after the final injection of Klopixol-Akufaz (100 mg), Clopixol should be administered orally in a daily dose of 40 mg, if possible in several doses. If necessary, the dose can be increased by 10-20 mg every 2-3 days up to 75 mg / day or more.
Transition from v / m of Klopixol-Akufaz to V / m introduction of Clopixol depot
Simultaneously with the final injection of Klopixol-akufaz (100 mg), 200-400 mg (1-2 ml) of Clopixol Depot (200 mg / ml) should be administered. Repeated injections of Klopixol Depot are performed every 2 weeks. If necessary, the use of the drug in higher doses or reducing the interval between injections is acceptable. Klopiksol-Akufaz and Clopixol Depot can be mixed in one syringe and administered as one combined injection. Subsequent doses of Clopixol Depot and the intervals between injections should be set depending on the patient's condition.

Adverse reactions

Nervous system: at the initial stage of treatment, the development of extrapyramidal symptoms is possible (in most cases, they are corrected by lowering the dose and / or prescribing anti-parkinsonian drugs, but regular preventive action of the latter is not recommended), drowsiness; accommodation disturbance is also possible.
With prolonged therapy in some patients, tardive dyskinesia is very rare. Parkinsonian drugs do not eliminate the symptoms of this condition. Dose reduction or, if possible, discontinuation of therapy is recommended.
Since the cardiovascular system: possible orthostatic dizziness, tachycardia; rarely, orthostatic hypotension.
From the digestive system: dry mouth, constipation; rarely, minor transient changes in liver function.
From the urinary system: urine retention.

- acute alcohol intoxication;
- acute intoxication with barbiturates;
- acute intoxication with opioid analgesics;
- coma.

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

With caution prescribed to patients with chronic hepatitis B, heart disease (including with arrhythmias), convulsive syndrome, as well as with hypersensitivity to derivatives of thioxanthene or other neuroleptics.
With prolonged therapy, it is necessary to carefully monitor the condition of patients.
It should be borne in mind that when using neuroleptics, including zuclopentixol, in rare cases, the development of a malignant neuroleptic syndrome (NNS) with a fatal outcome. The main symptoms of ZNS are: hyperthermia, muscle rigidity and impaired consciousness in combination with dysfunction of the autonomic nervous system (labile blood pressure, tachycardia, increased sweating).When these symptoms appear, urgent withdrawal of Clopixol and the appointment of symptomatic and supportive therapy are necessary.
Klopiksol-Akufaz can be mixed with Clopixol depot containing the same oil Viscoleo.
Influence on ability to drive motor transport and control mechanisms
When using the drug, especially at the beginning of treatment, you should avoid driving and working with mechanisms to determine the individual response to the therapy being carried out.

Symptoms: drowsiness, coma, extrapyramidal disorders, convulsions, hypotension, shock, hyper- or hypothermia are possible.
Treatment: in case of taking the drug inside it is necessary to wash the stomach as soon as possible, the use of a sorbent is recommended. In the future, conduct symptomatic and supportive therapy. Measures should be taken to support the activity of the respiratory and cardiovascular systems. Do not use adrenaline.

With simultaneous use of Clopixol may increase the sedative effect of ethanol, barbiturates and other means that have a inhibitory effect on the central nervous system.
Clopixol should not be used simultaneously with guanethidine and agents with a similar effect (since antipsychotics can block their hypotensive action).
With simultaneous use of Clopixol may reduce the effectiveness of levodopa and other adrenergic agents.
With simultaneous use of Clopixol with Metoclopramide and piperazine increases the risk of extrapyramidal symptoms.
Pharmaceutical incompatibility has not been established.

The drug Clopixol should be stored at a temperature not higher than 25 ° C.
The drug Clopixol Depot should be stored in a dark place at a temperature not exceeding 25 ° C.
The preparation Klopiksol-Akufaz should be stored in a dark place at a temperature not exceeding 30 ° C.
Pharmacy sales terms
List B. The drug is available on prescription.