Neuleptil solution 4%, 30ml

The dosage regimen varies greatly depending on the indications and the 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 can range from 30 mg to 100 mg. In some cases, an increase in the daily dose up to 200 mg is permissible.

In children over 3 years of age, the average daily dose ranges from 0.1 mg to 0.5 mg per kg of body weight.

The oral solution is yellow-brown in color, transparent, fluorescent, with a mint smell.

100 ml

peritsiazine 4 g

Excipients: sucrose - 25 g, ascorbic acid - 0.8 g, tartaric acid - 1.65 g, glycerol (glycerin) - 15 g, peppermint leaf oil - 0.04 g, ethanol 96% - 9.74 g, caramel (E150d) - 0.2 g , purified water - up to 100 ml.

Absolute:

• angle-closure glaucoma;

• urinary retention against the background of prostate diseases;

• Parkinson's disease;

• agranulocytosis, history of porphyria;

• concomitant therapy with levodopa;

• hypersensitivity to peritsiazine.

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

pharmachologic effect

Neuleptil is a neuroleptic from piperidine derivatives of phenothiazine. It has a mild antipsychotic and sedative effect without a stimulating component. It has adrenolytic, antispasmodic, parasympatholytic, antiemetic, hypothermic action. It potentiates the activity of narcotic and non-narcotic analgesics, hypnotics.

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

In connection with the selective normalizing effect on behavior, Neuleptil received the name 'behavior corrector'.

Pharmacokinetics

It is well absorbed from the gastrointestinal tract. After oral administration, the plasma concentration is lower than with i / m administration (the effect of the 'first pass' through the liver) and varies widely.

Communication with plasma proteins - 90%. Intensively penetrates the tissues, as it easily passes through the histohematogenous barriers, including the blood-brain 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 - longer. It is excreted by the kidneys, with bile and feces.

Side effect

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 neuroleptic.

Small starting doses:

Autonomic nervous system disorders: orthostatic hypotension; anticholinergic effects such as dry mouth, constipation, accommodation paresis, urinary retention.

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

Higher doses:

Disturbances from the nervous system: early dyskinesias (spastic torticollis, oculomotor crises, trismus, etc.), tardive dyskinesia observed with long-term treatment; extrapyramidal disorders (akinesia, sometimes combined with muscle hypertonia and partially eliminated by the appointment of anticholinergic antiparkinsonian drugs; hyperkinesia-hypertonicity, motor excitement; akathisia).

Endocrine and metabolic disorders: impotence, frigidity; hyperprolactinemia: amenorrhea, galactorrhea, gynecomastia; increase in body weight; violations of thermoregulation; hyperglycemia, decreased glucose tolerance.

Less common and dose-independent reactions:

Skin reactions: allergic skin reactions; photosensitivity.

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

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

Others:

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

Possibility of developing cholestatic jaundice.

Malignant neuroleptic syndrome: in case of development of unexplained fever, antipsychotic therapy should be discontinued immediately, as this may be one of the symptoms of neuroleptic malignant syndrome described with the use of antipsychotics, 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 antipsychotics, is associated with individual intolerance, there are predisposing factors for its occurrence, such as dehydration or organic brain damage.

Among patients taking antipsychotics of the phenothiazine series, there were isolated cases of sudden death, possibly caused by causes of a cardiac nature, as well as unexplained cases of sudden death.

Application during pregnancy and lactation

Pregnancy

Experimental studies in animals have not revealed a teratogenic effect of the drug. The study of the teratogenic effect of peritsiazine in humans has not been carried out. As with other phenothiazine derivatives, the data obtained from various epidemiological prospective studies on the possible risk of fetal malformations are controversial. There is no data on the effect of neuleptile administration during pregnancy on the development of the fetal brain.

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 a teratogenic effect of the drug, if any, is negligible. It is advisable to limit the duration of administration 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.

Lactation

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

Application for violations of liver function

The drug should be used with caution in patients with hepatic impairment.

Application for impaired renal function

The drug should be used with caution in patients with renal insufficiency.

Application in children

In children over 3 years of age, the average daily dose ranges from 0.1 mg to 0.5 mg per kg of body weight.

Use in elderly patients

The drug should be used with caution in elderly patients (the development of excessive sedative and hypotensive effects is possible).

special instructions

In case of fever or infection, a general blood test should be performed, since there have been reports of the possibility of agranulocytosis.

Drinking alcohol during treatment is not recommended.

For patients with epilepsy, due to the ability of the drug to lower the threshold of excitability of the cerebral cortex, clinical and, if possible, electroencephalographic observation should be carried out.

Phenothiazine antipsychotics can prolong the QT interval, which increases the risk of serious ventricular arrhythmias of the torsade de point type, which are potentially dangerous (sudden death).

Prolongation of the QT interval is especially increased in the presence of bradycardia, hypokalemia, and congenital or acquired (as a result of drug use) prolongation of the QT interval. Before prescribing therapy with neuroleptics, as an absolutely necessary factor in treatment, and, if the clinical picture allows, to exclude the possible appearance of risk factors, it is necessary to conduct medical and laboratory studies.

Caution should be exercised when using peritsiazine:

• in elderly patients, due to their high predisposition to the development of sedation and orthostatic hypotension;

• in patients with severe cardiovascular disease, due to hemodynamic disturbances and ECG changes;

• in patients with hepatic and / or renal insufficiency, due to the risk of overdose.

Influence on the ability to drive vehicles or other mechanisms.

Patients should be informed, especially those who are drivers of vehicles or persons working with other mechanisms, about the possibility of drowsiness in them due to taking the drug, especially at the beginning of treatment.

Overdose

Overdose can cause severe extrapyramidal disorders and coma.

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

Drug interactions

Combinations of drugs, the use of which is contraindicated:

Levodopa: the presence of mutual antagonism between levodopa and neuleptile was established. Extrapyramidal disorders should not be treated with levodopa during treatment with neuleptile (decrease or loss of neuroleptic activity).

If it is necessary to prescribe neulepti 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 drug combinations:

Alcohol: increased sedative effect neuleptila: decreased reaction, which can be dangerous for people who drive vehicles and use machinery. Avoid drinking alcoholic beverages and preparations containing alcohol.

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

Sultopride: an 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): decrease in the absorption of neuleptyl in the gastrointestinal tract. If possible, the interval between taking antacids and neuleptil should be at least two hours.

Combinations of medicinal products, in the use of which there is an interaction that should be taken into account:

Antihypertensive drugs (all): an increase in the hypotensive effect and the risk of orthostatic hypotension (cumulative effect). For guanethidine see section 'Inappropriate drug combinations'.

Other drugs that depress the nervous system are morphine derivatives. Most of the histamine H1 receptor blockers with a sedative effect, barbiturates, benzodiazepines, anxiolytics that are not derivatives of benzodiazepines, clopidine and preparations containing it: an increase in the inhibitory effect on the central nervous system can be of significant importance, in particular, when driving vehicles and using other mechanisms.

Atropine and other anticholinergics, antidepressants, imipramine derivatives, antiparkinsonian drugs with anticholinergic action; disopyramide - the possibility of cumulation of undesirable effects associated with anticholinergic action, such as urinary retention, constipation, dry mouth, etc.

It enhances the effects of anxiolytics, analgesics, anesthetics, sleeping pills, ethanol, as well as the side effects of hepato- and nephrotoxic drugs. When used together with tricyclic antidepressants, maprotiline, MAO inhibitors, it is possible to lengthen and enhance sedative and anticholinergic effects, with thiazide diuretics - an increase in hyponatremia, with Li + - a decrease in absorption in the gastrointestinal tract, an increase in the rate of Li + excretion, an increase in the severity of extrapyramidal intoxication, early + signs of Li (nausea and vomiting) may be masked by the antiemetic effect of phenothiazines. When combined with beta-blockers, it enhances the hypotensive effect, the risk of developing irreversible retinopathy, arrhythmias and tardive dyskinesia is possible.The appointment of alpha and beta adrenostimulants (epinephrine) and sympathomimetics (ephedrine) can lead to a paradoxical decrease in blood pressure. Amitriptyline, amantadine, antihistamines and other drugs with anticholinergic effect increase anticholinergic activity.

Antithyroid drugs 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. enhances its depressing effect on the central nervous system. Increases plasma concentration of prolactin and interferes with the action of bromocriptine.