Neuleptil drops for oral administration 4%, 125 ml (Perytsyazyn)

Latin name

Neuleptil

Packaging

125 ml

Pharmacological action of

Pharmacodynamics of

Periciazine is a neuroleptic from the group of piperidine derivatives of phenothiazine, whose antidopaminergic activity causes the development of therapeutic antipsychotic (without a stimulating component), as well as antiemetic and hypothermic effects. However, the development of its side effects (extrapyramidal syndrome, motor disorders and hyperprolactinemia) is also associated with antidopaminergic activity.

The antidopaminergic activity of periciazine is moderately expressed, due to which it has a moderate antipsychotic effect with moderate severity of extrapyramidal disorders. Due to the blocking effect of periciazine on the adrenergic receptors of the reticular formation of the brain stem and central histamine receptors, the drug has a clear sedative effect, which can also be a desirable clinical effect, especially with malevolently and angry types of affect, and the decrease in aggressiveness is not accompanied by lethargy and lethargy. Compared to chlorpromazine, periciazine has a more pronounced antiserotonin, antiemetic and central sedative effect, but a less pronounced antihistamine effect.

Periciazine reduces aggressiveness, irritability, disinhibition, so that it is effective in violation of behavior. Due to the normalizing effect on behavior, periciazine is called a corrector of behavior.

Blockade of peripheral H1-histamine receptors causes the antiallergic effect of the drug. Blockade of peripheral adrenergic structures is manifested by its hypotensive effect. In addition, the drug has anticholinergic activity.

Pharmacokinetics of

After oral administration, periciazine is well absorbed, however, like other phenothiazine derivatives, undergoes an intensive presystemic metabolism in the intestine and / or liver, therefore, after oral administration, the concentration of unchanged periciazine in the plasma is lower than with i / m administration and varies widely.

After oral administration of 20 mg of periciazine (2 capsules), the maximum plasma concentration is reached within 2 hours and is 150 ng / ml (410 nmol / l).

Communication with plasma proteins is 90%. Periciazine penetrates into tissues intensively, as it easily passes through the histohematological barriers, including the blood-brain barrier.

Most of periciazine is metabolized in the liver by hydroxylation and conjugation. Metabolites released with bile can be reabsorbed in the intestines. The elimination half-life of periciazine is 12-30 hours, elimination of metabolites is even longer. Conjugated metabolites are excreted in the urine, and the rest of the drug and its metabolites are excreted in the bile and feces.

In elderly patients, the metabolism and elimination of phenothiazines slows down.

Indications

- Acute psychotic disorders.

- Chronic psychotic disorders such as schizophrenia.

- Chronic non-schizophrenic delusional disorder.

- Chronic hallucinatory psychosis (for the treatment and prevention of relapse).

Contraindications

- Hypersensitivity to periciazine and / or other ingredients of the drug.

- Angle-closure glaucoma.

- Urinary retention due to prostate disease.

- A history of agranulocytosis.

- History of Porfiry.

- Concomitant therapy with dopaminergic agonists: levodopa, amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, pyribenidyl, pramipexole, quinagolide, ropinirole, with the exception of their use in patients with the disease.

- Vascular insufficiency (collapse).

- Acute poisoning with substances that depress the central nervous system, or coma.

- Heart failure.

- Pheochromocytoma.

- Severe pseudoparalytic myasthenia gravis (Erba-Goldflam disease).

- Children's age.

Precautions:

- In patients with predisposing factors for the development of ventricular arrhythmias (patients with cardiovascular disease, congenital prolonged QT interval, bradycardia, hypokalemia, hypomagnesemia, starving and / or alcohol abusers, receiving concomitant therapy with an alternative method, and / or cause severe bradycardia less than 55 beats per minute, slow intracardiac conduction, or change the electrolyte composition of the blood), since phenothiazine antipsychotics in very rare cases, they can cause an extension of the QT interval (this effect is dose-dependent) and increase the risk of developing severe ventricular arrhythmias, including bidirectional ventricular tachycardia of the pirouette type, which can be life-threatening (sudden death).

- In patients with renal and / or liver failure (risk of drug cumulation).

- In elderly patients (there is an increased predisposition to the development of postural hypotension, excessive hypotensive and sedative effects, the development of extrapyramidal disorders, hyperthermia in hot and hypothermia in cold weather, constipation, paralytic ileus and urinary retention in diseases of the prostate gland, there is a risk of accumulation drug due to decreased liver and kidney function).

- In patients with cardiovascular diseases (due to the danger to them of possible hypotensive and quinidine-like effects, the ability of the drug to cause tachycardia).

- Elderly patients with dementia and patients with risk factors for stroke (elderly patients with dementia experienced a three-fold increase in the frequency of developed strokes).

- In patients with risk factors for thromboembolism.

- In patients with epilepsy who are not receiving adequate anticonvulsant therapy (antipsychotics from the phenothiazine group lower the threshold for convulsive readiness).

- In patients with Parkinson's disease.

- In patients with hyperthyroidism (increased risk of developing agranulocytosis with periciazine in combination with drugs for the treatment of hyperthyroidism).

- In patients with changes in the blood picture (increased risk of developing leukopenia or agranulocytosis).

- In patients with breast cancer (the possibility of disease progression due to increased levels of prolactan in the blood).

Use during pregnancy and lactation

Pregnancy

Experimental studies in animals have not revealed teratogenic effects of the drug. A study of the teratogenic effect of periciazine in humans has not been conducted. As with other phenothiazine derivatives, the findings of various epidemiological prospective studies on the possible risk of fetal malformations are contradictory. There is no data on the effect of neuleptil administration during pregnancy on fetal brain development.

In rare cases, the following disorders have been reported in newborns, whose mothers received long-term treatment with large doses of Neuleptil:

- gastrointestinal disorders (bloating, etc.) associated with the atropine-like action of phenothiazines

- extrapyramidal disorders.

Thus, the risk of teratogenicity of the drug, if any, is negligible. It is advisable to limit the duration of the drug during pregnancy.

If possible, at the end of pregnancy, it is desirable to reduce the dose of Neuleptil and antiparkinsonian drugs that correct them, which can potentiate the atropine-like effect of antipsychotics. In newborns, the state of the nervous system and the function of the gastrointestinal tract should be monitored.

Breastfeeding

Due to the lack of data on the penetration of the drug into breast milk, it is not recommended to breast-feed while taking the drug.

Composition

active substance: periciazine

excipients: sucrose, ascorbic acid, tartaric acid, glycerol (glycerin), peppermint leaf oil, ethanol 96%, caramel (E150d), purified water.

Dosage and administration

Dosage regimen varies significantly depending on the indications and age of the patient. The average daily dose should be given in 2 or 3 doses, with an emphasis on evening hours.

In adults, the average daily dose may range from 30 mg to 100 mg. In some cases, it is permissible to increase the daily dose to 200 mg.

In children older than 3 years, the average daily dose is from 0.1 mg to 0.5 mg per kg of body weight.

Side effects

Neuleptil® is usually well tolerated, however, in some cases the adverse reactions listed below may occur, the occurrence of which may or may not depend on the size of the dose taken, and in the latter case it may be a result of increased individual patient sensitivity.

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 likely to occur when using the drug in high doses):

acute dystonia or dyskinesia (spastic torticollis, oculogyric crises, trismus, etc.) that usually occur within 4 days after starting treatment or increasing the dose of

parkinsonism, which often develops in elderly patients and / or after prolonged treatment (within weeks or months) and is partially eliminated when prescribing 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), idnost, akinesia in combination with muscle hypertonicity or without

tardive dystonia or dyskinesia, usually (but not always) occur during prolonged treatment and / or application of the drug at high doses, and capable of occurring even after cessation of treatment (when they occur, anticholinergic antiparkinsonian drugs have no effect and may cause deterioration)

akathisia, usually observed after taking 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 inhibit breathing, in senile patients, etc.).

From the autonomic nervous system

Anticholinergic effects (dry mouth, paresis of accommodation, urinary retention, constipation, paralytic intestinal obstruction).

From the cardiovascular system

Decreased blood pressure, usually postural arterial hypotension (more common in elderly patients and patients with a decrease in circulating blood volume, especially at the beginning of treatment and when using high initial doses).

Arrhythmias, including atrial arrhythmias, atrioventricular block, ventricular tachycardia, including potentially fatal ventricular tachycardia such as pirouette, are more likely when using high doses.

ECG changes, usually minor: lengthening of the QT interval, ST segment depression, appearance of the U wave and T wave changes.

With the use of antipsychotics, there have been cases of thromboembolism, including pulmonary embolism (sometimes fatal) and cases of deep vein thrombosis.

Endocrine and metabolic disorders (most often when using the drug in high doses)

Hyperprolactinemia, which can lead to amenorrhea, galactorrhea, gynecomastia, impotence, frigidity.

Weight gain.

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 sensitization of the skin.

Hematologic disorders

Leukopenia (observed in 30% of patients receiving high doses of antipsychotics).

Extremely rare: agranulocytosis, the development of which is not dose-dependent, 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 not affecting vision (especially when using high doses of phenothiazine derivatives for a long time).

From the liver and biliary tract

Very rare: cholestatic jaundice and liver damage, mainly cholestatic or mixed, requiring discontinuation of the drug.

Other

Malignant antipsychotic syndrome, a potentially fatal syndrome that can occur when taking all antipsychotics and manifested by hyperthermia, muscle rigidity, autonomic disorders (pallor, tachycardia, unstable blood pressure, increased sweating, shortness of breath) and impaired consciousness up to a coma. The occurrence of malignant antipsychotic syndrome requires the immediate termination of treatment with antipsychotics. Although this effect of periciazine 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: the development of withdrawal syndrome with the abrupt cessation of treatment with high doses of periciazine, 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 antipsychotics, there have been single cases of sudden death, possibly due to cardiac causes, as well as unexplained cases of sudden death.

Drug Interaction

Contraindications: with dopaminergic agonists (levodopa, amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, pyribedil, pramipelix, pramipelix ropinirole) in patients without Parkinson's disease is a mutual antagonism between dopaminergic agonists and pericyazine. It is not necessary to carry out treatment of extrapyramidal disorders caused by receiving a neuroleptic with the help of dopaminergic agonists (decrease or loss of neuroleptic activity) - in this case the use of anticholinergic antiparkinsonian agents is more shown.

Uncommon combinations: with dopaminergic agonists (levodopa, amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, pyribedil, pramipexole, quinagolide, ropinirolez) patients Dopaminergic agonists can exacerbate psychotic disorders. If patients with Parkinson's disease receiving dopaminergic agonists, Neuroleptic treatment is required, then they should be abolished by a gradual reduction of doses (sudden abolition of dopaminergic agonists may increase the risk of developing malignant neuroleptic syndrome). When using pericyazine together with the drug levodopa should be used minimally effective doses of both drugs. With alcohol - potentiation of the sedative effect caused by pericyazine. With amphetamine, clonidine, guanetidine - the effect of these drugs is reduced when taken with neuroleptics. With sultopride - an increase in the risk of developing ventricular rhythm disorders, in particular, ventricular fibrillation.

Combinations of medicines that require caution: with drugs that can increase the interval of OT (class IA and III antiarrhythmics, moxifloxacin, erythromycin, methadone, mefloquine, sertindole, tricyclic antidepressants, lithium salts and cisalride, etc.) increase the risk of arrhythmias. With thiazide diuretics - the risk of arrhythmias increases, due to the possibility of electrolyte disorders (gilokalemia, gilomagnesemia). With antihypertensive agents, especially alpha-blockers, an increase in antihypertensive activity and the risk of developing orthostatic hypotension (additive action). For clonidine and guanethidine, see section "Interaction with other medicinal products", subsection "Recommended drug combinations". With other drugs that have a CNS depressant effect: morphine derivatives (analgesics, antitussives), barbiturates, benzodiazepines, nebenzodiazepine anxiolytics, sleeping pills, neuroleptics, antidepressants with sedation (amitriptyline, doxepin, mianserin, mirtazapine, trimipramine), histamine H 1 receptor blockers with sedation, hypotensive central action, baclofen, thalidomide, With tricyclic antidepressants, MAO inhibitors, maprolin - increase the risk of developing malignant neuroleptic syndrome, possibly increasing and increasing the duration of sedative and anticholinergic effects. With atropine and other cholinolytics, as well as drugs with cholinolytic action (imipramine antidepressants, anticholinergic antiparkinsonian drugs, disopyramide) - the possibility of cumulation of undesirable effects, associated with cholinolytic action, such as urinary retention, constipation, dry mouth, heat stroke, etc. - as well as reducing the antipsychotic effect of neuroleptics. With beta-blockers - the risk of hypotension, especially orthostatic (additive action), and the risk of irreversible retinopathy, arrhythmias and late dyskinesia. With hepatotoxic drugs - increased risk of hepatotoxic action. With lithium salts, a decrease in the absorption in the gastrointestinal tract, an increase in the rate of excretion of lithium, an increase in the severity of extrapyramidal disorders and early signs of lithium intoxication (nausea and vomiting) may 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. With antithyroid drugs - increased risk of agranulocytosis. With apomorphine - reduction of the vomiting effect of apomorphine, enhancement of its depressant effect on the CNS. With hypoglycemic drugs - when combined with neuroleptics it is possible to reduce hypoglycemic action, which may require an increase in their doses.

Combinations of drugs that have an interaction that should be taken into account: with antacids (salts, oxides and hydroxides of magnesium, aluminum and calcium) - a decrease in the absorption of pericyazine in the gastrointestinal tract. Whenever possible, the interval between administration of antacids and pericyazine should be at least two hours. With bromocriptine, increasing plasma concentrations of prolactin when administered with pericyazine interferes with the effects of bromocriptine. With appetite suppressants (except fenfluramine), their effect is reduced.

overdose

Symptoms: CNS depression, progressing from drowsiness to coma with areflexia. Patients with initial manifestations of moderate intoxication or intoxication may experience anxiety, confusion, agitation, excited or derilious state. Other manifestations of overdose include: lowering blood pressure, tachycardia, ventricular arrhythmias, changes in EX collapse, hypothermia, narrowing of the pupil, tremor, muscle twitching, spasm or rigidity of muscles, convulsions, dystonic movements, muscular hypotension, muscular hypotension, cyanosis. Polyuria, which leads to dehydration, and severe extrapyramidal dyskinesias may also occur.

Treatment: should be symptomatic and carried out in a specialized department, where it is possible to organize monitoring of respiratory and cardiovascular functions and continue it until complete elimination of the effects of overdose. If less than 6 hours have passed after taking the drug, then gastric lavage or aspiration should be performed. The use of emetic agents is contraindicated because of the risk of aspiration of emetic masses against the background of inhibition and / or extrapyramidal disorders. Activated carbon is possible. There is no specific antidote. Treatment should be aimed at maintaining the vital functions of the body. At reduction of blood pressure of the patient it is necessary to move in a horizontal position with the raised legs. Infusion intravenous fluid administration is shown. If fluid administration 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 when the body temperature decreases to a level at which the development of cardiac arrhythmias (ie up to 29.4 ° C) is possible. 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 disturbances are maintained, antiarrhythmics may be required. The use of lidocaine and, if possible, long-acting antiarrhythmic agents should be avoided. With CNS depression and breathing, the patient may need to be transferred to artificial lung ventilation and antibiotic therapy for the prevention of pulmonary infections. Severe dystonic reactions usually respond to the intramuscular or intravenous administration of procyclidine (5-10 mg) or orphenadrine (20-40 mg). Seizures can be stopped by intravenous diazepam. In extrapyramidal disorders, anticholinergic antiparkinsonian agents are used intramuscularly.

Storage conditions

At a temperature not exceeding 25 ° C

Shelf suitability

4 Year

Deystvuyuschee substances

Perytsyazyn

Terms of delivery from

pharmacies Prescription

dosage form

dosage form

drops for oral administration

Sanofi-Aventis, France



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