Neulectil, 4% 30 ml

Neuleptyl is a neuroleptic of phenothiazine piperidine derivatives. It has a moderate antipsychotic and sedative effect without a stimulant component. It has adrenolytic, antispasmodic, parasympatholytic, antiemetic, hypothermic effects. It potentiates the activity of narcotic and non-narcotic-hanalgesics and sleeping pills.

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

Because of its selective normalizing effect on behavior, Neuleptyl has been called a “behavioral adjuster.”

Pharmacokinetics

It is well absorbed from the gastrointestinal tract. After oral administration, plasma concentrations are lower than those after intravenous administration (first-pass effect through the liver) and vary widely.

The binding to plasma proteins is 90%. Intensely penetrates into tissues, as it easily passes through histohematic barriers, including the blood-encephalic barrier. It penetrates into breast milk.

Metabolized in the liver by hydroxylation and conjugation, has a “first pass” effect through the liver, is subject to hepatic recirculation.

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

Indications

Active ingredient

Composition

Active ingredient:

Periciazine;

Associates:

sucrose,

ascorbic acid,

tartaric acid,

glycerol (glycerin),

Pearmint leaf oil,

Ethanol 96%,

caramel (E150d),

Purified water.

How to take, the dosage

The dosing regimen varies considerably depending on the indication 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 can range from 30 mg to 100 mg. In individual cases, it is acceptable 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 body weight.

Interaction

Combinations of drugs whose use is contraindicated:

Levodopa: reciprocal antagonism between levodopa and neuleptic has been established. Treatment of extrapyramidal disorders with levodopa against the background of treatment with neuleptil should not be performed (decrease or loss of neuroleptic activity).

If it is necessary to prescribe neulectil to patients with parkinsonism who are taking levodopa, it is illogical to continue levodopa because it increases psychiatric disturbances and cannot act on receptors blocked by neuroleptics.

Inappropriate drug combinations:

Alcohol: increases the sedative effects of Neuleptil: decreased responsiveness, which can be dangerous for people driving vehicles and using machinery. Avoid drinking alcoholic beverages and drugs containing alcohol.

Guanethidine and similar drugs: decrease the hypotensive activity of guanethidine, by reducing guanethidine penetration into sympathetic nerve fibers with which the drug action is associated. Use other hypotensive agents.

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

Combinations of drugs in which caution is required:

Antacids (salts, magnesium, aluminum and calcium oxides and hydroxides): decrease absorption of neulectil in the gastrointestinal tract. If possible, the interval between intake of antacids and neulectil should be at least two hours.

Combinations of drugs in the administration of which there are interactions to be taken into account:

Hypotensive drugs (all): increase in hypotensive effect and risk of orthostatic hypotension (cumulative effect). For guanethidine see “Inappropriate drug combinations”.

Other drugs that depress the nervous system are morphine derivatives. Most sedative histamine H1-receptor blockers, barbiturates, benzodiazepines, anxiolytics that are not benzodiazepine derivatives, clopidine and preparations containing it: increased CNS depressant effect may be significant, particularly when driving vehicles and using other mechanisms.

Atropine and other choline blockers, antidepressants, imipramine derivatives, antiparkinsonian drugs with anticholinergic effect; disopyramide – possibility of cumulation of unwanted effects associated with cholineolytic action, such as urinary retention, constipation, dry mouth, etc.

It increases the effects of anxiolytics, analgesics, anesthetics, sleeping pills, ethanol, and the side effects of hepato- and nephrotoxic drugs. In co-administration with tricyclic antidepressants, maprotiline, MAO inhibitors – prolongation and enhancement of sedative and anticholinergic effects, with thiazide diuretics – increase of 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) may be masked by antiemetic effect of phenothiazines. When combined with beta-adrenoblockers, it enhances the hypotensive effect and there may be a risk of irreversible retinopathy, arrhythmias and tardive dyskinesia. Administration of alpha- and beta-adrenergic stimulants (epinephrine) and sympathomimetics (ephedrine) may lead to a paradoxical decrease in blood pressure. Amitriptyline, amantadine, antihistamines and other drugs with choline-blocking effects increase anticholinergic activity.

The antithyroid drugs increase the risk of agranulocytosis. Reduces the effect of drugs that reduce appetite (with the exception of fenfluramine). Reduces the effectiveness of the vomiting action of apomorphine. increases its depressant effect on the central nervous system. Increases the plasma concentration of prolactin and inhibits the effect of bromocriptine.

Special Instructions

Neulectil is prescribed with caution in epilepsy and parkinsonism.

Caution is also required when using Neulectil in patients with cardiovascular disease and with significant liver and kidney dysfunction.

In elderly patients, there is a high risk of excessive sedation.

Neulectil should be used with caution in motorists.

Contraindications

Absolute:

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).

Side effects

Neulectil is usually well tolerated; however, the following adverse reactions, the severity of which varies depending on the pharmacological properties of the neuroleptic, may be observed in individual cases.

Low initial doses:

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

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

Higher doses:

Nervous system disorders: early dyskinesias (spastic torticollis, oculomotor crises, trismus, etc.), late dyskinesia, observed with long-term treatment; extrapyramidal disorders (akinesia, sometimes combined with muscle hypertonicity and partially resolved with administration of anticholinergic antiparkinsonian agents; hyperkinesia-hypertoneus, motor agitation; akathisia).

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

Rareer and dose-independent reactions:

Skin reactions: allergic skin reactions; photosensitization.

Hematological disorders: rare – agranulocytosis (regular monitoring of total blood count is recommended); leukopenia.

Ophthalmologic disorders: decreased tone of the eyeballs; brownish deposits in the anterior chamber of the eye due to accumulation of the drug, usually without affecting vision.

Others:

Positive serologic test for antinuclear antibodies, no clinical manifestations of lupus erythematosus.

Possible development of cholestatic jaundice.

Malignant neuroleptic syndrome: if unexplained fever develops, antipsychotic therapy should be stopped immediately, because this may be one of the symptoms of malignant neuroleptic syndrome described with neuroleptics, the clinical manifestations of which are pallor of the skin, hyperthermia and autonomic nervous system dysfunction.

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

In patients taking phenothiazine-type neuroleptics, there have been isolated cases of sudden death, possibly due to cardiac causes, as well as unexplained sudden deaths.

Overdose

Overdose may cause severe extrapyramidal disorders and coma.

The treatment must be symptomatic and should be done in a specialized department.