Neuleptil, 1 piece, 125 ml, 4%, oral solution
Combinations of drugs whose use is contraindicated:
Levodopa: mutual antagonism between levodopa and neuleptil has been established. Extrapyramidal disorders should not be treated with levodopa during treatment with neuleptil (reduction or loss of neuroleptic activity).
If it is necessary to prescribe neuleptil to patients suffering from parkinsonism and taking levodopa, it is illogical to continue taking levodopa, since it increases mental disorders and cannot act on receptors blocked by antipsychotics.
Inappropriate combinations of drugs:
Alcohol: increased sedative effect; neuleptil: decreased reaction, which can be dangerous for persons driving vehicles and using machinery. Avoid drinking alcoholic beverages and medications containing alcohol.
Guanethidine and similar drugs: reducing the hypotensive activity of guanethidine by reducing the penetration of guanethidine into the fibers of the sympathetic nerves, which is associated with the action of the drug. Use other antihypertensive drugs.
Sultopride: increased risk of developing ventricular arrhythmias, in particular ventricular fibrillation.
Combinations of drugs that require caution when using:
Antacids (salts, oxides and hydroxides of magnesium, aluminum and calcium): decreased absorption of neuleptil in the gastrointestinal tract. If possible, the interval between taking antacids and neuleptil should be at least two hours.
Combinations of drugs that may have interactions that should be taken into account:
Antihypertensive drugs (all): increased hypotensive effect and risk of orthostatic hypotension (cumulative effect). For guanethidine, see section “Inappropriate drug combinations”.
Other drugs that have a depressant effect on the nervous system are morphine derivatives. Most histamine H1 receptor blockers with sedative effects, barbiturates, benzodiazepines, anxiolytics that are not derivatives of benzodiazepines, clopidine and drugs containing it: an increase in the inhibitory effect on the central nervous system can be significant, in particular when driving vehicles and using other mechanisms.
Atropine and other anticholinergic drugs, antidepressants, imipramine derivatives, antiparkinsonian drugs with anticholinergic effects; disopyramide - the possibility of accumulation of undesirable effects associated with anticholinergic effects, such as urinary retention, constipation, dry mouth, etc.
Enhances the effects of anxiolytics, analgesics, anesthetics, hypnotics, ethanol, as well as the side effects of hepato- and nephrotoxic drugs. When used together with tricyclic antidepressants, maprotiline, MAO inhibitors, the sedative and anticholinergic effects may be prolonged and intensified; with thiazide diuretics, increased hyponatremia; with Li+, decreased absorption in the gastrointestinal tract, increased rate of excretion of Li+, increased severity of extrapyramidal disorders, early signs of Li+ intoxication (nausea and vomiting) may be masked by the antiemetic effect of phenothiazines. When combined with beta-blockers, it enhances the hypotensive effect; there is a possible risk of developing irreversible retinopathy, arrhythmias and tardive dyskinesia. The administration of alpha and beta adrenergic agonists (epinephrine) and sympathomimetics (ephedrine) can lead to a paradoxical decrease in blood pressure. Amitriptyline, amantadine, antihistamines and other drugs with an anticholinergic effect increase anticholinergic activity.
Antithyroid drugs increase the risk of developing agranulocytosis. Reduces the effect of appetite suppressants (with the exception of fenfluramine). Reduces the effectiveness of the emetic effect of apomorphine. enhances its inhibitory effect on the central nervous system. Increases plasma concentrations of prolactin and interferes with the action of bromocriptine.
Instructions for use NEULEPTIL
In pediatric practice, it is advisable to use Neuleptil 4% oral solution.
When taking pericyazine, it is recommended to regularly monitor the composition of peripheral blood, especially in the event of fever or infection (the possibility of developing leukopenia and agranulocytosis). If significant changes are detected in the peripheral blood (hyperleukocytosis, granulocytopenia), treatment with periciazine should be discontinued.
Neuroleptic malignant syndrome:
- in case of an unexplained increase in body temperature, treatment with pericyazine should be discontinued, as it may be a manifestation of neuroleptic malignant syndrome, the early manifestations of which may also be the appearance of autonomic disorders (such as excessive sweating, instability of pulse and blood pressure).
During treatment, you should not take alcohol or drugs containing alcohol.
Due to the drug's ability to lower the seizure threshold, when periciazine is taken by patients with epilepsy, they should undergo careful clinical and, if possible, electroencephalographic monitoring.
Except in special cases, periciazine should not be used in patients with Parkinson's disease.
Phenothiazine neuroleptics are capable of dose-dependent prolongation of the QT interval, which is known to increase the risk of developing severe ventricular arrhythmias, including torsade de pointes (ventricular fibrillation), which can be life-threatening. The risk of their occurrence increases in the presence of bradycardia, hypokalemia and prolongation of the QT interval (congenital or acquired under the influence of drugs that increase the duration of the QT interval).
Before prescribing antipsychotic therapy, if the patient's condition allows, it is necessary to exclude the presence of predisposing factors for the development of these severe arrhythmias (bradycardia less than 55 beats per minute, hypokalemia, hypomagnesemia, slow intraventricular conduction and congenital long QT interval or the use of other drugs that prolong the QT interval).
If bloating and abdominal pain appear while taking periciazine, the necessary examination should be carried out to exclude intestinal obstruction, the manifestations of which they may be, since the development of this side effect requires the necessary urgent measures.
Particularly careful monitoring of the patient's condition and special caution is required when prescribing periciazine and other antipsychotics to elderly patients, patients with certain cardiovascular diseases, patients with liver and kidney failure, elderly patients with dementia and patients with risk factors for stroke.
Stroke:
- In randomized clinical trials conducted in a population of elderly patients with dementia treated with certain atypical antipsychotic drugs compared with placebo, a 3-fold increase in the risk of cerebrovascular events was observed. The mechanism for this increased risk is unknown. An increased risk cannot be excluded with the use of other antipsychotic drugs or in other patient populations. In patients with risk factors for stroke, Neuleptil should be used with caution.
Older patients with dementia-related psychosis treated with antipsychotic drugs have an increased risk of death. Although the causes of deaths in clinical trials with atypical antipsychotics varied, the majority of deaths were either cardiovascular in nature (eg, heart failure, sudden death) or infectious in nature (eg, pneumonia). Observational studies suggest that treatment with traditional antipsychotics, similar to the situation with atypical antipsychotic drugs, may also increase mortality. The extent to which findings of increased mortality in observational studies may be attributable to antipsychotic drugs rather than to certain patient characteristics remains unclear.
Venous thromboembolism:
- Cases of venous thromboembolism, sometimes fatal, have been reported when taking antipsychotic drugs. For this reason, Neuleptil should be used with caution in patients with risk factors for thromboembolism.
Cases of hyperglycemia or glucose intolerance have been reported in patients receiving Neuleptil. For this reason, when prescribing the drug, as well as throughout the entire period of treatment, patients with an established diagnosis of diabetes mellitus or with risk factors for the development of diabetes mellitus should be provided with appropriate glycemic control.
Due to the possibility of developing withdrawal syndrome upon abrupt cessation of treatment with high doses of periciazine, discontinuation of the drug when used in high doses should be carried out gradually.
Due to the possibility of developing photosensitivity, patients receiving periciazine should be advised to avoid exposure to direct sunlight.
Due to the possibility in very rare cases of developing contact sensitization of the skin, direct contact of the drug with the skin should be avoided.
Impact on the ability to drive vehicles and operate machinery
Patients, especially those who are drivers of vehicles or people working with other mechanisms, should be informed about the possibility of drowsiness and decreased response in connection with taking the drug, especially at the beginning of treatment, since impaired psychomotor reactions can be potentially dangerous when driving vehicles and working with machinery.
Neuleptil solution 4% 125ml (Sanofi-Aventis)
Neuleptil® is usually well tolerated, however, in some cases, the following adverse reactions may occur, the occurrence of which may or may not depend on the dose taken, and in the latter case, be a consequence of increased individual sensitivity of the patient. From the central nervous system Sedation or drowsiness, more pronounced at the beginning of treatment and usually disappearing after a few days. Apathy, anxiety, mood changes. In some cases, paradoxical effects are possible: insomnia, agitation, sleep inversion, increased aggressiveness and increased psychotic symptoms. Extrapyramidal disorders (more often occurring when using the drug in high doses): acute dystonia or dyskinesia (spasmodic torticollis, oculogyric crises, trismus, etc.), usually occurring within 4 days after starting treatment or increasing the dose; parkinsonism, which often develops in elderly patients and/or after long-term treatment (weeks or months) and is partially eliminated by the appointment of anticholinergic antiparkinsonian drugs and is manifested by the appearance of one or more of the following symptoms: tremor (very often the only manifestation of parkinsonism), rigidity, akinesia in combination with or without muscle hypertonicity; tardive dystonia or dyskinesia, usually (but not always) occurring with long-term treatment and/or use of the drug in high doses, and can occur even after cessation of treatment (if they occur, anticholinergic antiparkinsonian drugs have no effect and may cause deterioration); akathisia, usually observed after high initial doses. Respiratory depression (possible in patients with predisposing factors to the development of respiratory depression, for example in patients receiving other drugs that can depress breathing, in elderly patients, etc.). From the autonomic nervous system Anticholinergic effects (dry mouth, accommodation paresis, urinary retention, constipation, paralytic ileus). Cardiovascular system: Decreased blood pressure, usually postural hypotension (more common in elderly patients and patients with decreased circulating blood volume, especially at the beginning of treatment and when using high initial doses). Arrhythmias, including atrial arrhythmias, atrioventricular block, and ventricular tachycardia, including potentially fatal torsade de pointes (TdP), are more likely when high doses are used. ECG changes, usually minor: prolongation of the QT interval, depression of the ST segment, the appearance of a U wave and changes in the T wave. Cases of thromboembolism, including pulmonary embolism (sometimes fatal) and cases of deep vein thrombosis, have been observed with the use of antipsychotics. Endocrine and metabolic disorders (more often occurring when using the drug in high doses) Hyperprolactinemia, which can lead to amenorrhea, galactorrhea, gynecomastia, impotence, frigidity. Increase in body weight. Thermoregulation disorders. Hyperglycemia, decreased glucose tolerance. Skin and allergic reactions Allergic skin reactions, skin rash. Bronchospasm, laryngeal edema, angioedema, hyperthermia and other allergic reactions. Photosensitivity (more often when using the drug in high doses). Contact skin sensitization. Hematological disorders Leukopenia (observed in 30% of patients receiving high doses of antipsychotics). Extremely rare: agranulocytosis, the development of which does not depend on the dose, and which can occur either immediately or after leukopenia lasting for two to three months. Ophthalmological disorders Brownish deposits in the anterior chamber of the eye, pigmentation of the cornea and lens due to accumulation of the drug, usually not affecting vision (especially when using high doses of phenothiazine derivatives for a long time). From the liver and biliary tract Very rarely: cholestatic jaundice and liver damage, predominantly cholestatic or mixed type, requiring discontinuation of the drug. Others Neuroleptic malignant syndrome, a potentially fatal syndrome that can occur with all antipsychotics and is manifested by hyperthermia, muscle rigidity, autonomic disorders (pallor, tachycardia, unstable blood pressure, increased sweating, shortness of breath) and disturbances of consciousness up to coma. The occurrence of neuroleptic malignant syndrome requires immediate cessation of antipsychotic treatment. Although this effect of pericyazine and other antipsychotics is associated with idiosyncrasy, there are predisposing factors for its occurrence, such as dehydration or organic brain damage. Positive serological test for the presence of antinuclear antibodies, without clinical manifestations of lupus erythematosis. Very rare: priapism, nasal congestion. Very rare: development of withdrawal syndrome with abrupt cessation of treatment with high doses of pericyazine, manifested by nausea, vomiting, insomnia and the possibility of exacerbation of the underlying disease or the development of extrapyramidal disorders. Among patients taking phenothiazine antipsychotics, isolated cases of sudden death, possibly caused by cardiac causes, as well as unexplained cases of sudden death have been reported.
Neuleptil®
This dosage form (oral solution) is not recommended for patients with liver disease, alcoholism, patients with epilepsy, patients with traumatic or drug-induced brain damage, and pregnant women, since the oral solution contains ethanol.
Leukopenia, agranulocytosis
When taking pericyazine, it is recommended to regularly monitor the composition of peripheral blood, especially in the event of fever, sore throat or infection (possibility of developing leukopenia and agranulocytosis). If significant changes are detected in the peripheral blood (hyperleukocytosis, granulocytopenia), treatment with periciazine should be discontinued.
Neuroleptic malignant syndrome
Treatment with Neuleptil should be discontinued in the event of an unexplained increase in body temperature, which may be one of the symptoms of neuroleptic malignant syndrome, clinical manifestations of which may include pallor, hyperthermia, disturbances of consciousness and muscle rigidity.
Early manifestations of neuroleptic malignant syndrome may include autonomic disorders (such as excessive sweating, instability of pulse and blood pressure).
Drinking ethanol (alcohol)
During treatment, you should not take alcohol or ethanol-containing drugs, since the potentiation of the sedative effect leads to a decrease in the reaction, which can be dangerous for people driving vehicles and machinery (see section “Interaction with other drugs”).
Patients with epilepsy
Due to the drug's ability to lower the threshold for seizure activity, when treating patients with epilepsy with periciazine, their condition should be carefully monitored and, if possible, electroencephalography should be performed. If seizures develop, you must stop taking the drug.
Patients with Parkinson's disease
Except in special cases, pericyazine should not be used in patients with Parkinson's disease (see sections "Contraindications" and "Interaction with other drugs").
QT prolongation
Phenothiazine antipsychotics are capable of dose-dependent prolongation of the QT interval, which is known to increase the risk of severe ventricular arrhythmias, including life-threatening torsade de pointes (TdP) and sudden death. The risk of developing severe ventricular arrhythmias increases in patients with bradycardia, hypokalemia, and prolongation of the QT interval (congenital or acquired under the influence of drugs that prolong the QT interval).
Before prescribing antipsychotics, if the patient's condition allows, and during treatment with the drug, it is necessary to exclude the presence of factors predisposing to the development of these severe arrhythmias (bradycardia less than 55 beats per minute, hypokalemia, hypomagnesemia, slow intraventricular conduction and congenital long QT interval or long QT interval with the use of other drugs that prolong the QT interval) (see sections “Precautions”, “Side effects”). Except in cases of urgent intervention, patients requiring treatment with antipsychotics are advised to undergo evaluation and ECG monitoring.
Intestinal obstruction
If bloating and abdominal pain appear while taking periciazine, the necessary examination should be carried out to exclude intestinal obstruction, since the development of this side effect requires urgent measures.
Monitoring the status of special groups of patients
Particularly careful monitoring of the patient's condition and special caution are required when prescribing periciazine and other antipsychotics to elderly patients, patients with cardiovascular diseases, patients with liver and kidney failure, elderly patients with dementia and patients with risk factors for stroke (see section "Carefully").
Elderly patients with dementia
In randomized clinical trials comparing some atypical antipsychotics with placebo in elderly patients with dementia, a threefold increase in the risk of cerebrovascular events was observed.
The mechanism for this increased risk of cerebrovascular complications is unknown. An increase in this risk cannot be excluded when taking other antipsychotics or when taking antipsychotics in patients of other groups, so periciazine should be prescribed with caution to patients with risk factors for stroke.
In elderly patients with dementia-related psychosis, an increased risk of death was observed when treated with antipsychotic drugs.
An analysis of 17 placebo-controlled studies (average duration of 10 weeks) found that most patients treated with atypical antipsychotics had a 1.6 to 1.7 times greater risk of death than patients treated with placebo. In a typical placebo-controlled clinical trial, patients receiving the active drug (antipsychotic) had a mortality rate of 4.5% at the end of 10 weeks of treatment versus 2.6% in patients receiving placebo. Although causes of death varied in clinical studies with atypical antipsychotics, most causes of death were either cardiovascular (eg, heart failure, sudden death) or infectious (eg, pneumonia). Observational studies have confirmed that, like treatment with atypical antipsychotics, treatment with typical antipsychotics may also increase mortality. The extent to which the increase in mortality may be attributable to antipsychotic drug use rather than to certain patient characteristics is unclear.
Venous thromboembolic complications
When using antipsychotic drugs, cases of venous thromboembolic complications, sometimes fatal, have been observed. Therefore, pericyazine should be used with caution in patients with risk factors for the development of venous thromboembolic complications.
Patients with diabetes mellitus or with risk factors for its development
The development of hyperglycemia and decreased glucose tolerance has been reported in patients taking periciazine. Patients with an established diagnosis of diabetes mellitus or with risk factors for its development who begin treatment with Neuleptil®, oral solution, should undergo appropriate monitoring of blood glucose concentrations during treatment (see section “Side Effects”).
Withdrawal syndrome
Due to the possibility of developing withdrawal syndrome upon abrupt cessation of treatment with high doses of pericyazine (see section “Side Effects”), discontinuation of the drug when used in high doses should be carried out gradually.
Photosensitivity
Due to the possibility of developing photosensitivity, patients receiving periciazine should be advised to avoid exposure to direct sunlight.
Contact sensitization
Due to the fact that in very rare cases, in persons who frequently handle phenothiazines, contact skin sensitization to phenothiazines may develop, direct contact of the drug with the skin should be avoided.
Use in children
The drug is contraindicated in children under 3 years of age.
The use of the drug in children under 6 years of age is possible only in exceptional cases, under strict medical supervision and in specialized institutions. Neurological symptoms and signs should be monitored.
When using the drug in children, it is recommended to conduct an annual clinical examination to assess the child’s ability to learn, since cognitive function may decrease under the influence of the drug.
Neuleptil (Pericyazine)
Combinations of drugs whose use is contraindicated:
Levodopa: mutual antagonism between levodopa and neuleptil has been established. Extrapyramidal disorders should not be treated with levodopa during treatment with neuleptil (reduction or loss of neuroleptic activity).
If it is necessary to prescribe neuleptil to patients suffering from parkinsonism and taking levodopa, it is illogical to continue taking levodopa, since it increases mental disorders and cannot act on receptors blocked by antipsychotics.
Inappropriate combinations of drugs:
Alcohol: increased sedative effect; neuleptil: decreased reaction, which can be dangerous for persons driving vehicles and using machinery. Avoid drinking alcoholic beverages and medications containing alcohol.
Guanethidine and similar drugs: reducing the hypotensive activity of guanethidine by reducing the penetration of guanethidine into the fibers of the sympathetic nerves, which is associated with the action of the drug. Use other antihypertensive drugs.
Sultopride: increased risk of developing ventricular arrhythmias, in particular ventricular fibrillation.
Combinations of drugs that require caution when using:
Antacids (salts, oxides and hydroxides of magnesium, aluminum and calcium): decreased absorption of neuleptil in the gastrointestinal tract. If possible, the interval between taking antacids and neuleptil should be at least two hours.
Combinations of drugs that may have interactions that should be taken into account:
Antihypertensive drugs (all): increased hypotensive effect and risk of orthostatic hypotension (cumulative effect). For guanethidine, see section “Inappropriate drug combinations”.
Other drugs that have a depressant effect on the nervous system are morphine derivatives. Most histamine H1 receptor blockers with sedative effects, barbiturates, benzodiazepines, anxiolytics that are not derivatives of benzodiazepines, clopidine and drugs containing it: an increase in the inhibitory effect on the central nervous system can be significant, in particular when driving vehicles and using other mechanisms.
Atropine and other anticholinergic drugs, antidepressants, imipramine derivatives, antiparkinsonian drugs with anticholinergic effects; disopyramide - the possibility of accumulation of undesirable effects associated with anticholinergic effects, such as urinary retention, constipation, dry mouth, etc.
Enhances the effects of anxiolytics, analgesics, anesthetics, hypnotics, ethanol, as well as the side effects of hepato- and nephrotoxic drugs. When used together with tricyclic antidepressants, maprotiline, MAO inhibitors, the sedative and anticholinergic effects may be prolonged and intensified; with thiazide diuretics, increased hyponatremia; with Li+, decreased absorption in the gastrointestinal tract, increased rate of excretion of Li+, increased severity of extrapyramidal disorders, early signs of Li+ intoxication (nausea and vomiting) may be masked by the antiemetic effect of phenothiazines. When combined with beta-blockers, it enhances the hypotensive effect; there is a possible risk of developing irreversible retinopathy, arrhythmias and tardive dyskinesia. The administration of alpha and beta adrenergic agonists (epinephrine) and sympathomimetics (ephedrine) can lead to a paradoxical decrease in blood pressure. Amitriptyline, amantadine, antihistamines and other drugs with an anticholinergic effect increase anticholinergic activity.
Antithyroid drugs increase the risk of developing agranulocytosis. Reduces the effect of appetite suppressants (with the exception of fenfluramine). Reduces the effectiveness of the emetic effect of apomorphine. enhances its inhibitory effect on the central nervous system. Increases plasma concentrations of prolactin and interferes with the action of bromocriptine.
