Clopixol®
Clopixol
The drug is taken orally, the daily dose can be divided into several doses. The dose is selected individually depending on the patient's condition. At the beginning of treatment, it is recommended to use the drug in low doses, which are then, depending on the patient’s response to treatment, quickly increased until the optimal clinical effect is achieved.
In acute attacks of schizophrenia and other acute psychotic disorders, severe agitation and mania
the dose of the drug is usually 10-50 mg/day.
For moderate and severe psychotic disorders
the initial dose is 20 mg/day and, if necessary, can be increased by 10-20 mg at intervals of 2-3 days to 75 mg/day or more.
For chronic psychotic conditions in schizophrenia and other chronic psychoses
The maintenance dose is 20-40 mg/day.
For agitation in patients with oligophrenia
the dose is 6-20 mg/day; if necessary, the dose can be increased to 25-40 mg/day.
For senile disorders accompanied by agitation and confusion
, the drug is prescribed at a dose of 2-6 mg/day, if necessary, the dose can be increased to 10-20 mg/day; It is more preferable to take the drug in the evening.
Clopixol-acufase
The drug is prescribed as a deep intramuscular injection into the upper outer quadrant of the gluteal region.
The recommended volume of intramuscular injection is 1-3 ml (50-150 mg). If necessary, repeated injections are carried out at intervals 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 Clopixol for oral administration or Clopixol depot IM in accordance with the recommendations below.
Clopixol depot
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) during 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 administration to intramuscular administration of Clopixol depot
Daily dose (mg) of Clopixol for oral administration x 8 = dose (mg) of Clopixol depot for intramuscular administration once every 2 weeks.
Taking Clopixol orally should be continued during the first week after the first injection, but at a reduced dose.
Transition from intramuscular administration of Clopixol-acuphas to oral administration of Clopixol
2-3 days after the final injection of Clopixol-acufaz (100 mg), Clopixol should be administered orally at 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 IM administration of Clopixol-acuphas to IM administration of Clopixol depot
Simultaneously with the final injection of Clopixol-acuphas (100 mg), 200-400 mg (1-2 ml) of Clopixol depot (200 mg/ml) should be administered. Repeated injections of Clopixol depot are carried out every 2 weeks. If necessary, it is permissible to use the drug in higher doses or reduce the intervals between injections. Clopixol-acufase 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 adjusted depending on the patient's condition.
Clopixol film-coated tablets 2 mg No. 50**
Pharmacological action of Clopixol
Antipsychotic drug (neuroleptic), thioxanthene derivative. Clopixol has a pronounced antipsychotic and specific inhibitory effect; the latter is especially indicated for agitation, restlessness, 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 occurs quickly. A single injection of Clopixol-acuphas provides significant and rapid relief of psychotic symptoms. The duration of the antipsychotic effect of the drug after one injection is 2-3 days. The nonspecific sedative effect appears after 2 hours, reaches a maximum after about 8 hours, after which it decreases significantly and is weakly manifested with repeated injections. The therapeutic effect of Clopixol depot is significantly more prolonged compared to Clopixol. This allows confident continuous antipsychotic treatment with Clopixol depot, which is especially important for patients who do not comply with medical prescriptions. Clopixol depot prevents the development of frequent relapses associated with arbitrary interruption of patients taking oral medications.
Pharmacokinetics of Clopixol
Pharmacokinetic and clinical trials of Clopixol depot have shown that injections of the drug are most advisable at intervals of 2-4 weeks. 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. Suction
After taking Clopixol orally, the Cmax of zuclopenthixol in the blood plasma is achieved after 4 hours. The bioavailability of zuclopenthixol when taken orally is about 44%.
After an intramuscular injection of Clopixol-acufaz, zuclopenthixol acetate undergoes enzymatic cleavage into the active component zuclopenthixol and acetic acid. Cmax of zuclopenthixol in serum is achieved 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 an intramuscular injection of Clopixol, zuclopenthixol decanoate depot undergoes enzymatic cleavage into the active component zuclopenthixol and decanoic acid. Cmax of zuclopenthixol in serum is achieved by the end of the first week after injection. The concentration curve of zuclopenthixol decreases exponentially, with T1/2 being 19 days, which reflects the rate of release of the active substance from the depot. Distribution
Zuclopenthixol penetrates the placental barrier in small quantities and is excreted in breast milk in small quantities.
Excretion
When taken orally, T1/2 is approximately 20 hours. Metabolites do not have neuroleptic activity; excreted mainly in feces and partly in urine.
Indications for Clopixol
Clopixol Clopixol
– acute and chronic schizophrenia and other psychotic disorders, especially with hallucinations, paranoid delusions and thinking 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, behavioral disturbances, confusion. Clopixol-acufaz
– initial treatment of acute psychoses, including manic states, and chronic psychoses in the acute phase.
Clopixol depot
– acute and chronic schizophrenia and other psychotic disorders, especially with hallucinations, paranoid delusions and thinking disorders; – states of agitation, increased anxiety, hostility, aggressiveness.
Dosage regimen Clopixol
Clopixol Clopixol
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 are then, depending on the patient’s response to treatment, quickly increased until the optimal clinical effect is achieved. In acute attacks of schizophrenia and other acute psychotic disorders, severe agitation and mania
the dose of the drug is usually 10-50 mg/day.
For moderate and severe psychotic disorders,
the initial dose is 20 mg/day and, if necessary, can be increased by 10-20 mg at intervals of 2-3 days to 75 mg/day or more.
For chronic schizophrenia and other chronic psychoses,
the maintenance dose is 20-40 mg/day.
For agitation in patients with oligophrenia,
the dose is 6-20 mg/day; if necessary, the dose can be increased to 25-40 mg/day.
For senile disorders accompanied by agitation and confusion
, the drug is prescribed at a dose of 2-6 mg/day, if necessary, the dose can be increased to 10-20 mg/day;
It is more preferable to take the drug in the evening. Clopixol-acufaz
The drug is prescribed as a deep intramuscular injection into the upper outer quadrant of the gluteal region.
The dose is selected individually depending on the patient's condition. The recommended volume of intramuscular injection is 1-3 ml (50-150 mg). If necessary, repeated injections are carried out at intervals 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 Clopixol for oral administration or Clopixol depot IM in accordance with the recommendations below. Clopixol depot
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) during 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 solution for intramuscular administration (200 mg/ml) exceeds 2-3 ml, then it is preferable to use a solution of Clopixol depot of 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. Switching from Clopixol for oral administration to IM administration of Clopixol depot
Daily dose (mg) of Clopixol for oral administration x 8 = dose (mg) of Clopixol depot for IM administration once every 2 weeks.
Taking Clopixol orally should be continued during the first week after the first injection, but at a reduced dose. Transition from intramuscular administration of Clopixol-acupaz to oral administration of Clopixol
2-3 days after the final injection of Clopixol-acupaz (100 mg), Clopixol should be administered orally at 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 intramuscular administration of Clopixol-acuphas to intramuscular administration of Clopixol depot.
Simultaneously with the final injection of Clopixol-acuphas (100 mg), 200-400 mg (1-2 ml) of Clopixol depot (200 mg/ml) should be administered. Repeated injections of Clopixol depot are carried out every 2 weeks. If necessary, it is permissible to use the drug in higher doses or reduce the intervals between injections. Clopixol-acufase 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 adjusted depending on the patient's condition.
Side effects of Clopixol
From the central nervous system and peripheral nervous system:
at the initial stage of treatment, extrapyramidal symptoms may develop (in most cases they can be corrected by reducing the dose and/or prescribing antiparkinsonian drugs, but regular preventive action of the latter is not recommended), drowsiness;
Accommodation disturbance is also possible. With long-term therapy, tardive dyskinesia very rarely occurs in some patients. Antiparkinsonian medications do not relieve the symptoms of this condition. Dose reduction or, if possible, discontinuation of therapy is recommended. From the cardiovascular system:
orthostatic dizziness, tachycardia are possible;
rarely - orthostatic hypotension. From the digestive system:
dry mouth, constipation;
rarely - minor transient changes in liver tests. From the urinary system:
urinary retention.
Contraindications Clopixol
– acute alcohol intoxication; – acute intoxication with barbiturates; – acute intoxication with opioid analgesics; - comatose states.
Pregnancy and lactation Clopixol
Clopixol is not recommended for use during pregnancy and lactation (breastfeeding).
Special instructions Clopixol
Prescribe with caution to patients with chronic hepatitis, heart disease (including arrhythmias), convulsive syndrome, as well as hypersensitivity to thioxanthene derivatives or other neuroleptics. During long-term therapy, patients' condition must be carefully monitored. It should be borne in mind that when using antipsychotics, incl. zuclopenthixol, in rare cases, the development of neuroleptic malignant syndrome (NMS) with a fatal outcome is possible. 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). If these symptoms appear, immediate discontinuation of Clopixol and administration of symptomatic and supportive therapy is necessary. Clopixol-acufaz can be mixed with Clopixol depot containing the same Viscoleo oil. Impact on the ability to drive vehicles and operate machinery
When using the drug, especially at the beginning of treatment, you should avoid driving and operating machinery until your individual response to the therapy is determined.
Overdose of Clopixol
Symptoms:
possible drowsiness, coma, extrapyramidal disorders, convulsions, arterial hypotension, shock, hyper- or hypothermia.
Treatment:
if the drug is taken orally, it is necessary to rinse the stomach as quickly as possible; the use of a sorbent is recommended. Subsequently, symptomatic and supportive therapy is carried out. Measures should be taken to maintain the functioning of the respiratory and cardiovascular systems. Adrenaline should not be used.
Drug interactions Clopixol
With simultaneous use, Clopixol can enhance the sedative effect of ethanol, barbiturates and other drugs that have a depressant effect on the central nervous system. Clopixol should not be used simultaneously with guanethidine and drugs with similar effects (as antipsychotics can block their hypotensive effect). When used concomitantly, Clopixol may reduce the effectiveness of levodopa and other adrenergic drugs. When Clopixol is used simultaneously with metoclopramide and piperazine, the risk of developing extrapyramidal symptoms increases. No pharmaceutical incompatibility has been established.
Conditions and periods of storage of Clopixol
Clopixol should be stored at a temperature not exceeding 25°C. The drug Clopixol depot should be stored in a place protected from light at a temperature not exceeding 25°C. The drug Clopixol-acufaz should be stored in a place protected from light at a temperature not exceeding 30°C. Conditions for dispensing from pharmacies
List B. The drug is available with a prescription.
Clopixol instructions for use
on medical use of the drug
CLOPIXOL
Registration number: P N014166/01-2002
Trade name: KLOPIXOL
International nonproprietary name: zuclopenthixol.
Dosage form: film-coated tablets.
Compound:
active substance – zuclopenthixol dihydrochloride 2.364 mg / 11.82 mg / 29.55 mg, which corresponds to 2 mg / 10 mg / 25 mg zuclopenthixol;
excipients – potato starch 22.2 mg / 29.2 mg / 31.6 mg, lactose monohydrate 17.4 mg / 21.6 mg / 22.0 mg, microcrystalline cellulose 9.0 mg / 13.5 mg / 18 .0 mg, copovidone 3.0 mg/ 4.5 mg/ 6.0 mg, glycerol 85% 1.2 mg/ 1.8 mg/ 2.4 mg, talc 4.2 mg/ 6.3 mg/ 8 .4 mg, hydrogenated castor oil 0.48 mg/ 0.72 mg/ 0.96 mg, magnesium stearate 0.42 mg/ 0.63 mg/ 0.84 mg.
Shell: hypromellose 5 1.37 mg/ 2.05 mg/ 2.74 mg, macrogol 6000 0.274 mg/ 0.411 mg/ 0.548 mg, titanium dioxide (E171) 0.445 mg/ 0.479 mg/ 0.091 mg, red iron oxide (E172) 0.011 mg/ 0.205 mg/ 0.822 mg.
Description:
2 mg - round, biconvex tablets, film-coated, pale pink. The color on the cross section is white;
10 mg - round, biconvex tablets, film-coated, pinkish-brown. The color on the cross section is white;
25 mg - round, biconvex tablets, film-coated, red-brown in color. The color on the cross section is white.
Pharmacotherapeutic group:
antipsychotic (neuroleptic).
ATX code: N05AF05.
Pharmacological properties
Clopixol is an antipsychotic drug (neuroleptic) of the thioxanthene group.
Pharmacodynamics.
The antipsychotic effect of antipsychotics is associated with blockade of dopamine receptors, and also, possibly, blockade of 5‑HT (5-hydroxytryptamine) receptors.
In vitro, zuclopenthixol has high affinity for dopamine D1 and D2 receptors, as well as α1-adrenergic receptors and serotonin 5-HT2 receptors, but has no affinity for muscarinic cholinergic receptors. The drug has weak affinity for H1 histamine receptors and does not have α2-adrenergic blocking activity. In vivo, affinity for D2 receptors prevails over affinity for D1 receptors.
Like most antipsychotics, zuclopenthixol increases serum prolactin levels.
Zuclopenthixol is intended for the treatment of acute and chronic psychoses and for the treatment of mentally retarded patients with hyperactive and aggressive behavior.
In addition to significantly weakening or completely eliminating the main symptoms of schizophrenia such as hallucinations, delusions and thought disorders, zuclopenthixol also has a pronounced effect on accompanying symptoms - hostility, suspiciousness, agitation and aggressiveness.
Zuclopenthixol has a transient, dose-dependent sedative effect. The rapid onset of sedation early in therapy is usually an advantage in the treatment of acute psychoses. Tolerance to the nonspecific sedative effect of the drug develops quickly. The specific inhibitory effect of Clopixol is particularly beneficial in the treatment of patients with agitation, restlessness, hostility or aggressiveness.
Pharmacokinetics.
The bioavailability of zuclopenthixol when taken orally is about 44%. Maximum serum concentrations are reached after approximately 4 hours.
The apparent volume of distribution (Vd)β is about 20 l/kg. Plasma protein binding is about 98-99%.
Zuclopenthixol slightly penetrates the placental barrier and is excreted in small quantities in breast milk. The half-life is approximately 20 hours. The metabolites do not have neuroleptic activity and are excreted mainly in feces and partly in urine.
For maintenance therapy in patients with mild to moderate schizophrenia, a minimum (i.e., measured immediately before administration) serum drug concentration of 2.8–12 ng/mL (7–30 nmol/L) is recommended.
Indications for use
Acute and chronic schizophrenia and other psychotic disorders, especially with hallucinations, paranoid delusions and thought disorders, as well as states of agitation, increased anxiety, hostility or aggressiveness.
Manic phase of manic-depressive psychosis.
Agitation and other behavioral disorders in mentally retarded patients.
Contraindications
Hypersensitivity to zuclopenthixol or any of the excipients.
Known hypersensitivity to drugs of the thioxanthene group.
Acute intoxication with ethanol, barbiturates and opiates.
Collapse, depression of consciousness of any origin, coma, suspected or established subcortical brain damage.
Hereditary galactose intolerance, lactase deficiency or impaired absorption of glucose and galactose.
Carefully:
organic brain diseases, mental retardation, seizure disorders, liver failure, history of cardiovascular disease, including prolongation of the QT interval, bradycardia <50 beats per minute, recent acute myocardial infarction, decompensated heart failure, arrhythmia, hypokalemia, hypomagnesemia and genetic predisposition to such conditions, the presence of risk factors for stroke (including acute arteriosclerosis), parkinsonism, opioid and alcohol dependence; pregnancy, breastfeeding period; children and adolescents under 18 years of age (due to insufficient clinical data).
Directions for use and doses
The tablets are taken orally: swallowed with water.
Doses of the drug should be selected individually depending on the patient's condition. As a rule, small doses should be used initially (from 2-10 mg and above depending on the indication), which are then quickly increased to optimal doses depending on the clinical effect. A maintenance dose can be prescribed once a day at bedtime.
Acute attack of schizophrenia, other acute psychotic disorders, severe agitation and mania.
Typically 10-50 mg/day.
For severe disorders and conditions of moderate severity, the initial dose of 20 mg / day can, if necessary, be increased by 10-20 mg after 2-3 days to 75 mg per day or more. The maximum single dose is 40 mg. The maximum daily dose is 150 mg.
Chronic psychotic states in schizophrenia and other chronic psychoses.
Maintenance dose 20-40 mg/day.
Agitation in patients with mental retardation.
Usually 6-20 mg/day. If necessary, the dose can be increased to 25-40 mg/day.
Elderly patients:
Elderly patients should be prescribed the minimum dose from the possible dose range (2-6 mg and above).
Decreased liver function:
Clopixol should be used with caution in patients with hepatic impairment. Patients with impaired liver function should be prescribed half the recommended doses, and serum levels of the drug should be monitored whenever possible.
Reduced kidney function:
Clopixol can be prescribed in normal doses to patients with reduced renal function.
Side effect
Most side effects are dose-related. The incidence of side effects and their intensity are most pronounced in the early stages of treatment and decrease as therapy continues.
Information on the incidence of side effects is presented based on literature data and spontaneous reports. Frequency is indicated as: very common (³1/10), common (³1/100 to <1/10), uncommon (³1/1000 to <1/100), rare (³1/10000 to <1/1000) , very rare (<1/10000), or unknown (cannot be estimated from existing data).
From the nervous system: very often - drowsiness, akathisia, hyperkinesis, hypokinesia; often - tremor, dystonia, muscle hypertonicity, dizziness, headache, paresthesia, attention disturbances, amnesia, gait disturbances; uncommon – tardive dyskinesia, hyperreflexia, parkinsonism, fainting, speech disorders, dyskinesia, ataxia, hypotonicity, convulsive disorders, migraine; very rarely – neuroleptic malignant syndrome.
From the side of mental activity: often - insomnia, depression, anxiety, nervousness, agitation, unusual dreams, decreased libido; infrequently - apathy, increased libido, nightmares, confusion.
From the cardiovascular system: often - tachycardia, palpitations; infrequently - decreased blood pressure, hot flashes; rarely - prolonged QT interval on the electrocardiogram; very rarely - venous thromboembolism.
From the organs of vision: often - disturbance of accommodation, visual impairment; infrequently - mydriasis (dilation of the pupil), involuntary movement of the eyeballs.
From the organ of hearing and labyrinth: often - dizziness; uncommon – hyperacusis, tinnitus.
From the respiratory system: often - shortness of breath, nasal congestion.
From the digestive system: very often - dry mouth; often - increased salivation, constipation, vomiting, dyspepsia, diarrhea; uncommon – abdominal pain, nausea, flatulence.
Metabolic and nutritional disorders: often - increased appetite, weight gain; infrequently – loss of appetite, weight loss; rarely – hyperglycemia, impaired glucose tolerance, hyperlipidemia.
From the reproductive system: infrequently - ejaculation disorders, erectile dysfunction, impaired orgasm in women, vulvovaginal dryness; rarely – galactorrhea, gynecomastia, amenorrhea, priapism.
From the urinary system: often - painful urination, urinary retention, polyuria.
Hepatic and hepatobiliary disorders: infrequently - changes in laboratory parameters of liver function; very rarely - cholestatic hepatitis, jaundice.
From the endocrine system: rarely – hyperprolactinemia.
From the circulatory and lymphatic system: rarely - thrombocytopenia, neutropenia, leukopenia, agranulocytosis.
On the part of the skin and subcutaneous tissue: often - hyperhidrosis, itching; uncommon - photosensitivity, pigmentation disorders, seborrhea, skin rash, dermatitis, purpura.
From the musculoskeletal system: often - myalgia; infrequently – muscle rigidity, trismus, torticollis.
From the immune system: rarely - hypersensitivity, anaphylactic reactions.
From the body as a whole: often - asthenia, fatigue, malaise, pain; infrequently – thirst, hypothermia, pyrexia.
Extrapyramidal disturbances may occur, especially in the early stages of treatment. In most cases, these side effects are successfully controlled by dose reduction and/or use of antiparkinsonian drugs. However, routine use of antiparkinsonian drugs to prevent side effects is not recommended. They do not improve the symptoms of tardive dyskinesia and may worsen them. Dose reduction or, if possible, discontinuation of zuclopenthixol therapy is recommended. For persistent akathisia, benzodiazepines or propranolol may be helpful.
When taking zuclopenthixol, the following side effects that occurred when taking other antipsychotics were also recorded: in rare cases, prolongation of the QT interval, ventricular arrhythmias - tachycardia and fibrillation, sudden death, cardiac arrest and the development of paroxysms of ventricular tachycardia (torsade des pointes).
Abrupt cessation of taking zuclopenthixol may be accompanied by withdrawal reactions. The most common symptoms are nausea, vomiting, anorexia, diarrhea, rhinorrhea, sweating, myalgia, paresthesia, insomnia, nervousness, anxiety and agitation. Patients may also experience dizziness, sensations of heat and cold, and tremors. Symptoms usually begin within 1 to 4 days after discontinuation and decrease within 7 to 14 days.
Overdose
Symptoms.
Drowsiness, coma, movement disorders, convulsions, shock, hyperthermia/hypothermia.
In case of overdose while taking drugs that affect cardiac activity, ECG changes, prolongation of the QT interval, polymorphic torsade de pointes, cardiac arrest and ventricular arrhythmias have been recorded.
Treatment.
Symptomatic and supportive. Measures should be taken to maintain the functioning of the respiratory and cardiovascular systems. Epinephrine (adrenaline) should not be used because this may lead to a subsequent decrease in blood pressure. Seizures can be treated with diazepam, and movement disorders with biperiden.
Interaction with other drugs
Clopixol may enhance the sedative effect of alcohol, the effect of barbiturates and other central nervous system depressants.
Clopixol should not be prescribed together with guanethidine and similarly active drugs, since antipsychotics may increase or decrease the effect of some antihypertensive drugs; the antihypertensive effect of guanethidine and similarly active drugs is reduced.
Concomitant use of antipsychotics and lithium increases the risk of neurotoxicity.
Tricyclic antidepressants and antipsychotics mutually inhibit each other's metabolism.
Clopixol may reduce the effectiveness of levodopa and the effect of adrenergic drugs.
Concomitant use with metoclopramide and piperazine increases the risk of developing extrapyramidal disorders.
Since zuclopenthixol is partially metabolized by the CYP2D6 isoenzyme, simultaneous use with drugs that inhibit this isoenzyme may lead to a decrease in the clearance of zuclopenthixol.
The increase in the QT interval, characteristic of therapy with antipsychotic drugs, can be enhanced by simultaneous use of drugs that prolong the QT interval: antiarrhythmic drugs of classes IA and III (quinidine, amiodarone, sotalol, dofetilide), some antipsychotics (thioridazine), some macrolide antibiotics (erythromycin) and quinolone antibiotics (gatifloxacin, moxifloxacin), some antihistamines (terfenadine, astemizole), as well as cisapride, lithium and other drugs that increase the QT interval. The simultaneous use of Clopixol and the above drugs should be avoided.
Clopixol should be administered with caution concomitantly with drugs that cause electrolyte disturbances (thiazide and thiazide-like diuretics) and drugs that can increase plasma concentrations of zuclopenthixol, due to a possible increased risk of QT prolongation and life-threatening arrhythmias.
special instructions
With long-term therapy, especially at high doses (above 25-40 mg/day), it is necessary to carry out careful monitoring, periodically assessing the condition of patients in order to decide on the possibility of reducing the maintenance dose.
When treated with any neuroleptics, there is a possibility of developing neuroleptic malignant syndrome (NMS). 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 cessation of antipsychotic medication, the use of general supportive measures and symptomatic treatment is essential.
With concomitant diabetes mellitus, the administration of Clopixol may change the levels of insulin and glucose in the blood, which may require dose adjustment of hypoglycemic drugs.
Like other drugs belonging to the therapeutic class of antipsychotics, Clopixol may cause QT prolongation.
Persistently prolonged QT intervals may increase the risk of malignant arrhythmias.
Cases of venous thromboembolism have been reported while taking antipsychotics. Due to the fact that patients treated with antipsychotics are often at risk for developing venous thromboembolism, risk factors for the development of venous thromboembolism should be determined before and during treatment with Clopixol and precautions taken.
In randomized, placebo-controlled clinical trials of certain atypical antipsychotics in patients with dementia, a 3-fold increase in the risk of cerebrovascular adverse reactions was observed. The mechanism for this increased risk is unknown. An increased risk cannot be ruled out when using other antipsychotics in other groups of patients. Clopixol should be used with caution in patients at risk of stroke.
Data from two large observational studies showed that older patients with dementia taking antipsychotic drugs had a nonsignificant increased risk of death compared with patients not taking antipsychotic drugs. There is no sufficient data to accurately assess the magnitude of the risk and the reasons for its increase.
Clopixol is not registered for the treatment of behavioral disorders in elderly patients with dementia.
When drinking alcohol during treatment with zuclopenthixol, the inhibitory effect on the central nervous system may be enhanced.
The tablets contain hydrogenated castor oil, which may cause stomach upset and diarrhea.
Use during pregnancy and breastfeeding:
During pregnancy, Clopixol should only be used if the expected benefit to the mother outweighs the potential risk to the fetus.
Infants whose mothers took antipsychotic drugs late in pregnancy or during labor may show signs of toxicity, such as lethargy, tremors, and excessive excitability. In addition, these newborns have a low Apgar score.
Breastfeeding is allowed during treatment with Clopixol if deemed clinically necessary. However, it is recommended to monitor the condition of the newborn, especially in the first 4 weeks after birth.
Impact on the ability to drive vehicles and machinery:
Patients should be warned about the sedative effect of the drug and the possible effect of its use on the ability to drive vehicles and operate machinery.
Release form
Film-coated tablets 2 mg, 10 mg, 25 mg.
Packaging:
50 or 100 tablets in a child-resistant plastic container with first-opening control. The lid is embossed with a diagram for opening the container. Container with instructions for use in a cardboard box.
Storage conditions
At a temperature not higher than 25°C.
Keep out of the reach of children.
Best before date
2 years.
Do not use after the expiration date stated on the packaging.
Conditions for dispensing from pharmacies
By doctor's prescription.
