Neuleptil, capsules 10mg, 50pcs

Composition

Active ingredient:

peritsiazin – 10 mg.

Auxiliary substances:

calcium hydrophosphate dihydrate,

magnesium stearate,

titanium dioxide (E 171),

gelatin.

Pharmacological action

Neuleptil is a neuroleptic drug made from piperidine derivatives of phenothiazine. It has a moderate antipsychotic and sedative effect without a stimulating component. It has adrenolytic, antispasmodic, parasympatholytic, antiemetic, hypothermic effects. Potentiates the activity of narcotic and non-narcotic analgesics, sleeping pills.

It has a distinct sedative effect, reduces aggressiveness, excitability, disinhibition. It has a hypnotic effect.

Due to its selective normalizing effect on behavior, Neuleptil is called a “behavior corrector”.

Pharmacokinetics

It is well absorbed from the gastrointestinal tract. After oral use, the plasma concentration is lower than with intravenous use (the effect of “first pass” through the liver) and varies widely.

Plasma protein binding is 90%. Intensely penetrates tissues, as it easily passes through histohematic barriers, including the hemato-encephalic barrier. Penetrates into breast milk.

It is metabolized in the liver by hydroxylation and conjugation, has a “first pass” effect through the liver, and undergoes hepatic recirculation.

T1 / 2 – 30 hours Elimination of metabolic products is longer. It is excreted by the kidneys, with bile and feces.

Indications

• for psychopathy
• psychopathic states in schizophrenia
• emotional disorders in epilepsy.

Contraindications

Absolute values:

• angle-closure glaucoma;
• urinary retention due to prostate diseases
• ;prostate adenoma;
• Parkinson’s disease;
• agranulocytosis, porphyria in the anamnesis;
• concomitant therapy with levodopa;
• hypersensitivity to perichiazine.

With caution, the drug should be used in patients with diseases of the cardiovascular system, renal and/or hepatic insufficiency, in elderly patients (excessive sedative and hypotensive effects may develop).

Side effects

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 may be due to increased individual sensitivity of the patient. From the side of the central nervous systems Edation or drowsiness, more pronounced at the beginning of treatment and usually passes in 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 common when using the drug in high doses):

• acute dystonia or dyskinesia (spastic torticollis, ekologichnye crises, lockjaw, etc. ), usually occurs within 4 days after starting treatment or increasing the dose;
• Parkinson’s disease, which often occurs in elderly patients and/or after prolonged treatment (weeks or months) and partly eliminated by the appointment of anticholinergic antiparkinsonian funds and manifested by the appearance of one or more of the following symptoms: tremor (very often the only manifestation of Parkinson’s disease), rigidity, akinesia, combined with muscle hypertonicity or without it;
• late dystonia or dyskinesia, usually (but not always) occurs with prolonged treatment and/or applying the drug in high doses, and can occur even after stopping treatment (if they occur, anticholinergic antiparkinsonian funds do not have effect and may cause deterioration);
• akathisia, usually observed after use of high initial doses. Respiratory depression (possible in patients with predisposing factors to the development of respiratory depression, for example, in patients receiving other medications that can depress breathing, in elderly patients, etc. ). From the autonomic nervous system
• Anticholinergic effects (dry mouth, paresis of accommodation, urinary retention, constipation, paralytic intestinal obstruction). From the cardiovascular system
• Low blood pressure, usually postural hypotension (more common in elderly patients and patients with reduced 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 pirouette-type ventricular tachycardia, are more likely to occur when high doses are used.
• ECG changes, usually minor: QT prolongation, ST-segment depression, U-wave appearance, and T-wave changes.
• Cases of thromboembolism have been reported with neuroleptics, including pulmonary embolism (sometimes fatal) and deep vein thrombosis. Endocrine and metabolic disorders (more often occurring when using the drug in high doses)
• Hyperprolactinemia, which can lead to amenorrhea, galactorrhea, gynecomastia, impotence, frigidity.
• Weight gain.
• Violations of thermoregulation.
• Hyperglycemia, decreased glucose tolerance. Skin and allergic reactions
• Allergic skin reactions, skin rash.
• Bronchospasm, laryngeal edema, angioedema, hyperthermia, and other allergic reactions.
• Photosensitization (more often when using the drug in high doses). Contact sensitisation of the skin. Hematological disorders
• Leukopenia (observed in 30% of patients receiving high doses of neuroleptics).
• Extremely rare: agranulocytosis, the development of which does not depend on the dose, and which can occur both immediately and after leukopenia lasting for two to three months. Ophthalmic disorders
• Brownish deposits in the anterior chamber of the eye, pigmentation of the cornea and lens due to drug accumulation, usually do not affect vision (especially when using high doses of phenothiazine derivatives for a long time). Liver and biliary tract disorders
• Very rare: cholestatic jaundice and liver damage, mainly cholestatic or mixed type, requiring discontinuation of the drug. Others
• are Neuroleptic malignant syndrome, a potentially fatal syndrome that can occur when taking all neuroleptics and is manifested by hyperthermia, muscle rigidity, vegetative disorders (pallor, tachycardia, unstable blood pressure, increased sweating, shortness of breath) and impaired consciousness up to coma. The occurrence of neuroleptic malignant syndrome requires immediate discontinuation of neuroleptic treatment. Although this effect of periciazine and other neuroleptics 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 discontinuation 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-type neuroleptics, there were isolated cases of sudden death, possibly caused by cardiological causes, as well as unexplained cases of sudden death.

Interaction

Contraindicated combinations: with dopaminergic agonists (levodopa, amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, piribedil, pramipexole, quinagolide, ropinirole) in patients without Parkinson’s disease, there is a mutual antagonism between dopaminergic agonists and perichiazine. Do not treat neuroleptic – induced extrapyramidal disorders with dopaminergic agonists (decrease or loss of neuroleptic activity) – in this case, the use of anticholinergic antiparkinsonian agents is more indicated.

Not recommended combinations: with dopaminergic agonists (levodopa, amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, piribedil, pramipexole, quinagolide, ropinirole) in patients with Parkinson’s disease, there is a mutual antagonism between dopaminergic agonists and perichiazine. Dopaminergic agonists can increase psychotic disorders. If patients with Parkinson’s disease receiving dopaminergic agonists require neuroleptic treatment, they should be discontinued by gradually reducing the dose (sudden withdrawal of dopaminergic agonists may increase the risk of developing neuroleptic malignant syndrome). When using periciazine together with levodopa, the minimum effective dose of both drugs should be used. With alcohol – potentiation of the sedative effect caused by perichiazine. With amphetamine, clonidine, guanethidine – the effect of these drugs decreases when taken simultaneously with neuroleptics. With sultoprid – increased risk of ventricular arrhythmias, in particular, ventricular fibrillation.

Combinations of medications that require caution: with medications that can increase the OT interval (class IA and III antiarrhythmics, moxifloxacin, erythromycin, methadone, mefloquine, sertindol, tricyclic antidepressants, lithium salts and cisalride, and others) – an increased risk of arrhythmias. With thiazide diuretics-the risk of arrhythmias increases, due to the possibility of developing electrolyte disorders (hylokalemia, hylomagnesemia). With antihypertensive agents, especially alpha-blockers-an increase in the hypotensive effect and the risk of orthostatic hypotension (additive effect). For clonidine and guanethidine, see the section “Interactions with other medicinal products”, subsection “Non-recommended combinations of medicinal products”. With other drugs that have a depressing effect on the central nervous system: morphine derivatives (analgesics, antitussives), barbiturates, benzodiazepines, non – benzodiazepine anxiolytics, hypnotics, neuroleptics, antidepressants with a sedative effect ( amitriptyline, doxepin, mianserin, mirtazapine, trimipramine), histamine H1 receptor blockers with a sedative effect, antihypertensive agents of central action, baclofen, thalidomide, pisotifen-the risk of additional depressing effects on the central nervous system, respiratory depression. With tricyclic antidepressants, MAO inhibitors, maprotilin – an increased risk of developing neuroleptic malignant syndrome, it is possible to increase and increase the duration of sedative and anticholinergic effects. With atropine and other cholinolytics, as well as drugs with a cholinolytic effect (imipramine antidepressants, anticholinergic antiparkinsonian drugs, disopyramide ) – the possibility of accumulation of undesirable effects associated with cholinolytic action, such as urinary retention, constipation, dry mouth, heat stroke, etc., as well as a decrease in the antipsychotic effect of neuroleptics. With beta-blockers – the risk of developing hypotension, especially orthostatic (additive effect), and the risk of developing irreversible retinopathy, arrhythmias and tardive dyskinesia. With hepatotoxic drugs – increased risk of hepatotoxic effects. With lithium salts – a decrease in absorption in the gastrointestinal tract, an increase in the rate of lithium excretion, an increase in the severity of extrapyramidal disorders; moreover, early signs of lithium intoxication ( nausea and vomiting) can be masked by the antiemetic effect of phenothiazines. With alpha-and beta-adrenostimulants (epinephrine, ephedrine) – a decrease in their effects, a paradoxical decrease in blood pressure is possible. With antithyroid drugs – increased risk of agranulocytosis. With apomorphine – a decrease in the emetic effect of apomorphine, an increase in its depressing effect on the central nervous system. With hypoglycemic drugs – when combined with neuroleptics, the hypoglycemic effect may decrease, which may require an increase in their doses.

Combinations of medicinal products where there is an interaction that should be taken into account: with antacids (salts, oxides and hydroxides of magnesium, aluminum and calcium) – reduced absorption of perichiazine in the gastrointestinal tract. If possible, the interval between taking antacids and perichiazine should be at least two hours. With bromocriptine-an increase in the plasma concentration of prolactin when taking pericyazine interferes with the effects of bromocriptine. With appetite suppressants (with the exception of fenfluramine) – a reduction in their effect.

How to take, course of use and dosage

Neuleptil,10 mg capsules, is intended for oral use in adult patients. In children, Neuleptil 4% oral solution should be used.

The dosage regimen varies significantly depending on the indications and the patient’s condition. Doses of the drug should be selected individually. If the patient’s condition allows, treatment should start with low doses, which can then be gradually increased. The minimum effective dose should always be used.

The daily dose should be divided into 2 or 3 doses and most of the dose should always be taken in the evening. In adults, the daily dose can range from 30 mg to 100 mg. The maximum daily dose is 200 mg.

Treatment of acute and chronic psychotic disorders: the initial daily dose is 70 mg (divided into 2-3 doses). The daily dose can be increased by 20 mg per week until the optimal effect is achieved (on average, up to 100 mg per day). In exceptional cases, the daily dose may be increased to 200 mg.

Correction of behavioral disorders: the initial daily dose is 10-30 mg.

Treatment of elderly patients: doses are reduced by 2-4 times.

Overdose

Symptoms: central nervous system depression, progressing from drowsiness to coma with areflexia. Patients with initial signs of intoxication or moderate intoxication may experience restlessness, confusion, agitation, agitation or deriliosis. Other signs of overdose include: low blood pressure, tachycardia, ventricular arrhythmias, changes, collapse, hypothermia, pupil constriction, tremor, muscle twitching, muscle spasm or rigidity, convulsions, dystonic movements, muscle hypotension, difficulty swallowing, respiratory depression, apnea, cyanosis. Polyuria leading to dehydration and severe extrapyramidal dyskinesia may also occur.

Treatment: should be symptomatic and conducted in a specialized department where it is possible to organize monitoring of respiratory and cardiovascular functions and continue it until the effects of overdose are completely eliminated. If less than 6 hours have passed after taking the drug, then gastric lavage or aspiration of its contents should be performed. The use of emetics is contraindicated due to the risk of aspiration of vomit against the background of lethargy and / or extrapyramidal disorders. It is possible to use activated carbon. There is no specific antidote. Treatment should be aimed at maintaining the vital functions of the body.

With a decrease in blood pressure, the patient should be transferred to a horizontal position with raised legs. Intravenous fluid infusion is indicated. If fluid use is not sufficient to eliminate hypotension, norepinephrine, dopamine, or phenylephrine may be administered. The introduction of epinephrine is contraindicated, With hypothermia, you can wait for its independent resolution, except in cases when the body temperature drops to a level at which cardiac arrhythmias may develop (that is, up to 29.4 °C).

Ventricular or supraventricular tachyarrhythmias usually respond to the restoration of normal body temperature and the elimination of hemodynamic and metabolic disorders. If life-threatening rhythm disorders persist, antiarrhythmics may be required. The use of lidocaine and, if possible, long-acting antiarrhythmic agents should be avoided. In case of central nervous system and respiratory depression, it may be necessary to transfer the patient to artificial ventilation and antibiotic therapy for the prevention of lung infections. Severe dystonic reactions usually result from intramuscular or intravenous use of procyclidine (5-10 mg) or orphenadrine (20-40 mg). Seizures can be stopped by intravenous use of diazepam. For extrapyramidal disorders, anticholinergic antiparkinsonian agents are used intramuscularly.

Special instructions

When taking periciazine, it is recommended to regularly monitor the composition of peripheral blood, especially in the case of fever or infection (the possibility of developing leukopenia and agranulocytosis). In case of significant changes in peripheral blood (leukocytosis, granulocytopenia), treatment with pericyazine should be discontinued.

Neuroleptic malignant syndrome – in the event of an unexplained increase in body temperature, treatment with periciazine should be discontinued, as it may be a manifestation of neuroleptic malignant syndrome, the early manifestations of which may also include the appearance of autonomic disorders (such as increased sweating, unstable pulse and blood pressure).

Due to the ability of the drug to reduce the threshold of convulsive readiness, patients with epilepsy should be carefully monitored clinically and, if possible, electroencephalographically when taking periciazine.

Except in special cases, periciazine should not be used in patients with Parkinson’s disease. Neuroleptics of the phenothiazine derivative group can dose-dependently prolong the QT interval, which is known to increase the risk of severe ventricular arrhythmias, including life-threatening bidirectional ventricular tachycardia of the “pirouette” type. 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 neuroleptic therapy, if the patient’s condition allows, 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, slowing of intraventricular conduction and congenital prolonged QT interval or prolonged QT interval with other drugs that prolong the QT interval). These risk factors should also be monitored during treatment with the drug.

If bloating and abdominal pain occur while taking perichiazine, the necessary examination should be performed to exclude intestinal obstruction, since the development of this side effect requires the necessary urgent measures. Especially careful monitoring of the patient’s condition and special caution is required when prescribing periciazine and other neuroleptics to elderly patients, patients with cardiovascular diseases, patients with hepatic and renal insufficiency, elderly patients with dementia, and patients with risk factors for stroke.

In randomized clinical trials comparing some atypical antipsychotics with placebo, conducted in elderly patients with dementia, there was a threefold increase in the risk of developing cerebrovascular events. The mechanism of this risk is not known. An increase in this risk cannot be excluded with other antipsychotics or in other patient populations, so periciazine should be used with caution in patients with risk factors for stroke.

Elderly patients with dementia-related psychoses have been shown to have an increased risk of death when treated with antipsychotic drugs. An analysis of 17 placebo-controlled trials (with an average duration of more than 10 weeks) showed that the majority of patients treated with atypical antipsychotic medications had a 1.6-1.7 times greater risk of death than patients treated with placebo. Although the causes of death in clinical trials with atypical antipsychotic medications varied, most of the causes of death were either cardiovascular (e. g., heart failure, sudden death) or infectious (e. g., pneumonia). by nature. Observational studies have confirmed that, similar to treatment with atypical antipsychotics, treatment with conventional antipsychotics can also increase mortality. The extent to which the increase in mortality may be due to the antipsychotic drug, rather than some patient characteristics, is not clear.

Venous thromboembolism, sometimes fatal, has been reported with antipsychotic medications. Therefore, periciazine should be used with caution in patients with risk factors for thromboembolism.

Due to the possibility of developing withdrawal syndrome with abrupt discontinuation of treatment with high doses of periciazine, discontinuation of the drug when used in high doses should be carried out gradually.

Due to the potential for photosensitivity, patients receiving perichiazine should be advised to avoid exposure to direct sunlight.

Due to the fact that people who frequently use phenothiazines may develop contact sensitization of the skin to phenothiazines in very rare cases, direct contact of the drug with the skin should be avoided.

During treatment, you should not take alcohol or drugs containing alcohol, as this potentiation of the sedative effect leads to a decrease in the reaction, which can be dangerous for people driving vehicles and mechanisms. Patients, especially those who drive vehicles or work with other mechanisms, should be informed about the possibility of drowsiness.

Composition

Capsule Form of production

Storage conditions

At a temperature not exceeding 25 °C

Shelf life

5 years

Active ingredient

Peritsiazin

Conditions of release from pharmacies

By prescription

Dosage form

Capsules

Purpose

For adults as prescribed by a doctor, for pregnant women as prescribed by a doctor

Indications

Manic-Depressive Psychosis, Psychiatric disorders, Schizophrenia