Neuleptil, drops for oral use 4%, 30ml

Composition

Active ingredient:

peritsiazin;

Auxiliary substances:

sucrose,

ascorbic acid,

tartaric acid,

glycerol (glycerin),

peppermint leaf oil,

ethanol 96%,

caramel (E 150d),

purified water.

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 severity of which varies depending on the pharmacological properties of the antipsychotic.

Small initial doses:

Disorders of the autonomic nervous system:  orthostatic hypotension; anticholinergic effects such as dry mouth, constipation, accommodation paresis, urinary retention.

Nervous system disorders:  sedation or drowsiness that is more pronounced at the beginning of treatment; apathy, anxiety, mood changes, depression.

Higher doses:

Nervous system disorders:  early dyskinesia (spastic torticollis, oculomotor crises, trismus, etc. ), tardive dyskinesia observed with long-term treatment; extrapyramidal disorders (akinesia, sometimes combined with muscle hypertonicity and partially eliminated with the appointment of anticholinergic antiparkinsonian agents; hyperkinesia-hypertonicity, motor arousal; akathisia).

Endocrine and metabolic disorders:  impotence, frigidity; hyperprolactinemia: amenorrhea, galactorrhea, gynecomastia; weight gain; thermoregulation disorders; hyperglycemia, decreased glucose tolerance.

Less frequent and dose – independent reactions:

Skin reactions:  allergic skin reactions; photosensitization.

Hematological disorders:  rarely-agranulocytosis (regular monitoring of a general blood test is recommended); leukopenia.

Ophthalmic disorders:  decreased eyeball tone; brownish deposits in the anterior chamber of the eye due to drug accumulation, usually not affecting vision.

Other:

Positive serological test for the presence of antinuclear antibodies, without clinical manifestations of lupus erythematosis.

The possibility of developing cholestatic jaundice.

Neuroleptic malignant syndrome:  if an unexplained fever develops, antipsychotic therapy should be discontinued immediately, as this may be one of the symptoms of neuroleptic malignant syndrome described in the use of neuroleptics, the clinical manifestations of which are pallor of the skin, hyperthermia and dysfunction of the autonomic nervous system.

Although this effect of Neuleptil, like other neuroleptics, is associated with individual intolerance, there are predisposing factors for its occurrence, such as dehydration or organic brain damage.

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

Combinations of drugs that are contraindicated:

Levodopa:  the presence of mutual antagonism between levodopa and neuleptil was established. Extrapyramidal disorders should not be treated with levodopa while neuleptil is used (decreased or lost 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 affect the receptors blocked by neuroleptics.

Inappropriate drug combinations:

Alcohol:  enhancing the sedative effect of neuleptil: reduced reaction time, which can be dangerous for people driving vehicles and using mechanisms. Avoid drinking alcoholic beverages and drugs that contain alcohol.

Guanethidine and similar drugs:  decrease in the hypotensive activity of guanethidine, due to a decrease in the penetration of guanethidine into the fibers of sympathetic nerves, which is associated with the action of the drug. Use other antihypertensive agents.

Sultoprid:  increased risk of ventricular arrhythmias, particularly ventricular fibrillation.

Combinations of medications that require caution when used:

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.

Drug combinations where there is an interaction that should be taken into account:

Antihypertensive drugs (all):  increased hypotensive effect and risk of orthostatic hypotension (cumulative effect). For guanethidine, see the section “Inappropriate drug combinations”.

Other drugs that have a depressing effect on the nervous system are morphine derivatives. Most histamine_H1-receptor blockers with sedative action, barbiturates, benzodiazepines, anxiolytics that are not derivatives of benzodiazepines, clopidine and its containing preparations:  an increase in the depressive effect on the central nervous system can be significant, in particular, when driving vehicles and using other mechanisms.

Atropine and other anticholinergic agents, antidepressants, imipramine derivatives, antiparkinsonian drugs with anticholinergic effects; disopyramide – the possibility of accumulation of undesirable effects associated with the cholinolytic effect, such as urinary retention, constipation, dry mouth, etc.

Increases the effects of anxiolytics, analgesics, anaesthetics, sleeping pills, ethanol, as well as the side effects of hepatotoxic and nephrotoxic drugs. When combined with tricyclic antidepressants, maprotilin, MAO inhibitors, it is possible to prolong and increase the sedative and anticholinergic effects, with thiazide diuretics-increased hyponatremia, with Li+ – decreased absorption in the gastrointestinal tract, increased rate of Li+ excretion, increased severity of extrapyramidal disorders, early signs of Li+ intoxication (nausea and vomiting) can be masked by the antiemetic effect of phenothiazines. When combined with beta-blockers, it increases the hypotensive effect, and there is a possible risk of developing irreversible retinopathy, arrhythmias, and tardive dyskinesia. Use of alpha-and beta-adrenostimulants (epinephrine) and sympathomimetics (ephedrine) it can lead to a paradoxical decrease in blood pressure. Amitriptyline, amantadine, antihistamines and other drugs with a cholinoblocking effect increase anticholinergic activity.

Antithyroid medications increase the risk of agranulocytosis. Reduces the effect of appetite suppressants (with the exception of fenfluramine). Reduces the effectiveness of the emetic action of apomorphine. increases its depressing effect on the central nervous system. Increases the plasma concentration of prolactin and prevents the action of bromocriptine.

How to take it, course of use and dosage

The 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 the 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 over 3 years of age, the average daily dose is 0.1 mg to 0.5 mg per kg of body weight.

Overdose

Overdose can cause severe extrapyramidal disorders and coma.

Treatment should be symptomatic and carried out in a specialized department.

Special instructions

Neuleptil is prescribed with caution for epilepsy and Parkinsonism.

Caution is also required when using Neuleptil in patients suffering from cardiovascular diseases, and with severe violations of liver and kidney function.

Elderly patients are at high risk of developing excessive sedation.

Caution should be exercised when prescribing Neuleptil to drivers.

Form of production

Solution for oral use

Storage conditions

Store in a dry place protected from light at a temperature not exceeding 25°C.

Shelf

life is 5 years.

Active ingredient

Peritsiazin

Conditions of release from pharmacies

By prescription

Dosage form

Drops for oral use

Purpose

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

Indications

Mental disorders, Schizophrenia, Manic-Depressive Psychosis