Pharmacological action of the drug
Clopixol is an antipsychotic drug (neuroleptic), formed from thioxanthene, which exhibits a pronounced antipsychotic and specific inhibitory effect.
With its help, temporary calm occurs, depending on the dose taken. The rapid occurrence of a sedative effect during therapy, as a rule, is an advantage in the case of treatment of acute psychoses.
Tolerance to such a nonspecific sedative effect of this drug develops quite quickly.
Clopixol Akufaz
The instructions indicate that Clopixol - Acuphas has a fairly pronounced antipsychotic and specific slowing effect . Clopixol-Aquaz may have a temporary, dose-dependent sedative effect.
The rapid development of a sedative effect at the very beginning of treatment (before the onset of the antipsychotic process) is an advantage in the case of treatment of acute and subacute psychoses. A nonspecific sedative effect is expressed 2 hours after administration.
The maximum effect is achieved after 8 hours, then decreases significantly and remains the same if injections are repeated. The administration of 1 or 2 injections is sufficient, then the patient can be switched to the use of oral medications.
Clopixol Depot
Clopixol depot, as the instructions indicate, also has a fairly pronounced antipsychotic and specific inhibitory effect.
The nonspecific sedative effect weakens after three weeks.
The therapeutic effect of Clopixol depot is significantly more prolonged compared to Clopixol.
This makes it possible to confidently carry out continuous antipsychotic treatment, which is important for patients who do not follow medical recommendations. Clopixol depot prevents the increase in relapses associated with unauthorized cessation of oral medications by patients.
Pharmacokinetics of the drug
After the drug is introduced into the body, it behaves differently depending on the form of release and the subtype of the drug.
Clopixol tablets
Its maximum accumulation in the blood serum is after 4 hours. Use regardless of food intake. When taken orally, bioavailability is 44%. The process during which proteins bind to blood plasma is 98–99%.
T½ of clopixol is 20 hours, and 0.86 l/min is the systemic clearance. Clopixol is excreted mainly through feces and partly through urine. Over the course of 3 to 5 days, an equilibrium concentration is established.
Injections
The injection of Clopixol - acuphase leads to its enzymatic breakdown into acetic acid and the active component zuclopenthixol.
After an intramuscular injection, half-life of Clopixol - acuphase is about 32 hours. In the course of 1 to 2 days after the injection, the maximum accumulation of Clopixol - acuphase in the blood serum is reached.
Clopixol depot injection is enzymatically broken down into decanoic acid and the active component zuclopenthixol. At the end of the first week from the moment of injection, the largest accumulation of Clopixol depot in the blood serum is observed.
After intramuscular injection, half-life of the drug Clopixol depot is about 3 weeks (reflects release from the depot). With repeated use over a period of 3 months, an equilibrium concentration is established.
Pharmacokinetically, this corresponds to the fact that a dose of Clopixol depot 200 mg used once for 2 weeks is equal to a dose of 25 mg of Clopixol taken orally for two weeks.
special instructions
With long-term treatment with Clopixol, in order to decide on reducing the maintenance dose, careful clinical monitoring of the patient's condition is required periodically.
It must be remembered that when using antipsychotics (including zuclopenthixol), in rare cases, neuroleptic malignant syndrome (NMS) can develop with a fatal outcome. The main symptoms include muscle rigidity, hyperthermia and impaired consciousness against the background of dysfunction of the central nervous system of the autonomic nervous system - labile blood pressure, increased sweating, tachycardia. If the symptoms described above occur, immediate discontinuation of Clopixol and administration of supportive and symptomatic therapy is required.
During treatment, care should be taken when driving vehicles and other complex mechanisms.
Indications for use
Instructions for use for the drugs Clopixol Depot and Akufaz indicate that the indications for use vary slightly:
- Clopixol: the state of the manic stage in manic-depressive psychosis and the state of chronic and acute schizophrenia and other diseases affecting the mind, especially with thinking disorders, paranoid delusions, hallucinations, as well as a state of aggressiveness, agitation, hostility or increased anxiety. As well as the state of agitation and other behavioral changes in patients with mental retardation.
- Clopixol-acufase: acute psychoses and their treatment in the initial stage, chronic psychoses in a state of exacerbation, manic states.
- Clopixol depot: a state of acute and chronic schizophrenia and other psychotic disorders, with thinking disorders, paranoid delusions, hallucinations. Additionally, there is increased anxiety, agitation, aggressiveness, and hostility.
Directions for use and dosage
Clopixol is taken orally, the dose is selected individually depending on the diagnosis and condition of the patient. The daily dose of the drug is allowed to be taken in several doses.
It is recommended to use the drug in small doses at the beginning of therapy, which are then increased to the required level to ensure optimal clinical effect.
Recommended daily doses of Clopixol:
- An acute attack of schizophrenia, other acute psychotic disorders, mania, severe agitation - usually 10-50 mg is used;
- Moderate and severe psychotic disorders - the initial dose is 20 mg, if necessary, it can be increased by 10-20 mg every 2-3 days up to 75 mg or more;
- Chronic psychotic conditions in schizophrenia and other chronic psychoses - the maintenance dose is 20-40 mg;
- Agitation in patients with oligophrenia - prescribe 6-20 mg, if necessary, the dose can be increased to 25-40 mg;
- Senile disorders accompanied by agitation and confusion - take 2-6 mg (preferably in the evening), if necessary, the dose can be increased to 10-20 mg.
Contraindications
You should not use the medicine if:
- state of hypersensitivity to Klopiscol;
- state of increased sensitivity to drugs of the thioxanthene group;
- state of acute intoxication with ethanol, barbiturates and opiates;
- state of collapse;
- state of oppression of consciousness of any origin;
- coma state;
- the presence of suspected or established subcortical brain damage;
- the presence of hereditary galactose intolerance, changes in the absorption of galactose and glucose, lactose deficiency.
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Instructions for use
Let's study the instructions for Clopixol in more detail.
Release forms
There are these:
- Clopixol – coated tablets Weight 2.0 mg - have a round shape convex on both sides, pale pink color. On the cross section the color is white; weight 10.0 mg, color pinkish-brown; weight 25.0 mg, color red-brown.
- Clopixol Akufaz is an oil solution, density 50 mg/ml. ampoules of 1 and 2 ml.
- Clopixol Depot is an oil solution with a density of 200 mg/ml and 500 mg/ml.
- In ampoules of 1 ml.
Dosages and methods of use of the drug
The dose size, duration and frequency of use depend entirely on the required treatment regimen prescribed by the doctor. Orally.
The dose at the beginning of use can range from 2 to 20 mg/day, and if necessary, it can be gradually increased to 75 mg/day or higher.
Clopixol Akufaz is taken intramuscularly.
A single dose at the beginning of use is from 50 to 150 mg, and if indicated, repeated injections can be used with a 2-3 day interval.
Clopixol Depot is used intramuscularly.
The single dose used can be in the range from 200 to 750 mg, administration is carried out with a frequency of 1-4 weeks, which is determined by the clinical situation at the time of administration.
Release form and composition
The dosage form of Clopixol is tablets - biconvex, round, film-coated (50 or 100 pieces in plastic containers, 1 container in a cardboard box).
The active ingredient of the drug is zuclopenthixol dihydrochloride, the content of which in 1 tablet depends on the color of its shell:
- Red-brown – 29.55 mg (corresponding to the content of zuclopenthixol 25 mg);
- Pinkish-brown – 11.82 mg (corresponding to the content of zuclopenthixol 10 mg);
- Pale pink – 2.364 mg (corresponding to the content of zuclopenthixol 2 mg).
Auxiliary components: lactose monohydrate, potato starch, microcrystalline cellulose, glycerol 85%, copovidone, talc, magnesium stearate, hydrogenated castor oil.
Shell composition: macrogol 6000, hypromellose 5, titanium dioxide, red iron oxide.
Overdose and additional instructions
symptoms :
- coma;
- convulsions;
- drowsiness;
- shock;
- movement disorders;
- hyperthermia/hypothermia.
During an overdose, along with taking drugs that affect the heart, ventricular arrhythmia and tachycardia, changes in the electrocardiogram, prolongation of the QT interval, and cardiac arrest were recorded.
It can be eliminated by urgent gastric lavage and the use of sorbents, followed by treatment, which should be supportive and symptomatic, aimed at strengthening the functioning of both the cardiovascular and respiratory systems.
Convulsions are relieved with diazepam, biperiden eliminates movement disorders. To avoid low blood pressure, do not use epinephrine (adrenaline).
Side effects
They depend on the dose taken, and their pronounced manifestation is observed at the beginning of treatment, and decrease over time.
There is information about rare cases of ventricular arrhythmias and tachycardia, prolongation of the QT interval, and sudden death. If side effects occur, reduce the dose taken
special instructions
If prescribing the drug, exercise caution if the following symptoms occur:
- the presence of organic brain diseases;
- mental retardation;
- seizure disorders;
- liver failure;
- the patient’s history of cardiovascular disease;
- decompensated heart failure;
- arrhythmias;
- hypokalemia;
- hypomagnesemia and genetic predisposition to such conditions;
- risk of stroke and acute arteriosclerosis;
- presence of parkinsonism;
- in rare cases, death is likely due to the development of (NMS) neuroleptic malignant syndrome.
Taking the drug affects the ability to drive a car or operate high-precision equipment.
Drug and alcohol
The depressant effect on the central nervous system may increase.
Since the tablets contain hydrogenated castor oil, diarrhea and stomach upset may occur.
If kidney and liver functions are impaired
Clopixol is prescribed in normal doses in cases of reduced renal function. Possible side effects.
If liver function is reduced, half the recommended dose is prescribed and serum drug levels are monitored.
Interaction with other drugs
If used simultaneously, it may enhance the sedative effect of barbiturates, ethanol, and other drugs.
It should not be used with guanethidine and drugs with similar effects, since their hypotensive effect may be blocked. The effectiveness of levodopa and other adrenergic drugs may be reduced when used simultaneously with Clopixol.
The possibility of extrapyramidal symptoms increases when Clopixol is used simultaneously with metoclopramide and piperazine.
During pregnancy and lactation
Contraindicated. During pregnancy, it is used exclusively if the planned benefit for the mother exceeds the acceptable risk for the fetus itself.
During treatment with Clopixol, breastfeeding is allowed only if deemed clinically necessary.
Reception by children
Due to insufficient clinical data, it is not recommended for children under 18 years of age.
Side effects
The use of Clopixol may be accompanied by the following side effects:
- Nervous system: disturbance of accommodation, drowsiness, at the beginning of therapy - extrapyramidal symptoms (in most cases, their development is corrected by reducing the dose and/or prescribing antiparkinsonian drugs, but constant use of the latter for preventive purposes is not recommended); very rarely - with long-term treatment, tardive dyskinesia is possible (it is recommended to reduce the dose or discontinue therapy; antiparkinsonian drugs are not effective in this condition);
- Cardiovascular system: tachycardia, orthostatic dizziness; rarely – orthostatic hypotension;
- Digestive system: constipation, dry mouth, rarely - minor changes in liver tests;
- Urinary system – urinary retention.
Symptoms of an overdose of Clopixol are: drowsiness, convulsions, extrapyramidal disorders, coma, shock, hyper- or hypothermia, arterial hypotension. In such a condition, gastric lavage and the use of a sorbent are recommended. Subsequently, symptomatic and supportive treatment is carried out. You should not take epinephrine, as a further decrease in blood pressure (BP) may occur; seizures are controlled by diazepam, extrapyramidal symptoms by biperiden.
Reviews from patients and doctors
Reviews from doctors and patients about Clopixol Depot and Acufase are mixed.
Reviews from doctors
The use of Clopixol depot gives the most constant level of the active drug in the blood and a more expected antipsychotic effect.
The use of depot antipsychotics promotes the socialization of patients and eliminates the systematic use of the drug during working hours.
Patient reviews
It is worth noting the following:
- Ivan, 29 years old. I have been taking clopixol for 8 months now. I felt extremely stiff, my neck was twisting, all my muscles were aching, my eyes were rolling back in my head, and the pain was severe.
- Semyon, 34 years old. The first time they injected me with clopixol depot, my eyes began to blink, but a week later the blinking stopped. They also injected them with clopixol depot 2 weeks later, for the 3rd month they are blinking.
- Peter, 31 years old . The first neuroleptic, Clopixol, was prescribed to me by a doctor. It was canceled for me, I had stiffness from it. But I was calm, like a boa constrictor when I took it.
Pros and cons, according to reviews and practical experience
Judging by the reviews, the drug gives very strong side effects at first.
They are very difficult for patients to tolerate in most cases.
Subsequently the situation returns to normal.
The truth here is that everything also depends on the patient’s body and the dose skillfully selected by the doctor.
