Neulectil, 4% 125 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

Hallucinations, Mental disorders, Aggressiveness and conflict, Schizophrenia, Manic Depressive Psychosis, Delirium

• psychopathies
• psychopathic-like states in schizophrenia
• disorder of emotions in epilepsy.

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Active ingredient

Pericyzine

Composition

Active ingredient:

Pericyazine;

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 allowed to increase daily dose up to 200 mg.

In children over 3 years old an average daily dose is 0.1 mg to 0.5 mg per kg of body weight.

Interaction

Contraindicated combinations: with dopaminergic agonists (levodopa, amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, pyribedil, pramipexole, quinagolide, ropinirole) in patients without Parkinson’s disease – mutual antagonism between dopaminergic agonists and pericyazine. Dopaminergic agonists should not be used to treat neuroleptic-induced extrapyramidal disorders (reduction or loss of neuroleptic activity), in which case anticholinergic antiparkinsonian agents are more indicated.

Unrecommended combinations: With dopaminergic agonists (levodopa, amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, pyribedil, pramipexole, quinagolide, ropinirole) in patients with Parkinson’s disease – mutual antagonism between dopaminergic agonists and pericyazine. Dopaminergic agonists can exacerbate psychotic disorders. If patients with Parkinson’s disease receiving dopaminergic agonists require neuroleptic treatment, they should be withdrawn by gradually reducing their doses (abrupt withdrawal of dopaminergic agonists may increase the risk of malignant neuroleptic syndrome). When using pericyzine in conjunction with levodopa, the lowest effective doses of both drugs should be used. With alcohol – potentiation of the sedative effect caused by pericyazine. With amphetamine, clonidine, guanethidine – the effect of these drugs is reduced when taken concomitantly with neuroleptics. With sultopride – increased risk of ventricular arrhythmias, particularly ventricular fibrillation .

Combinations of drugs for which caution is required: with drugs that can prolong the OT interval (Class IA and III antiarrhythmics, moxifloxacin, erythromycin, methadone, mefloquine, sertindol, tricyclic antidepressants, lithium salts and cisalride, etc.) – increased risk of arrhythmias. With thiazide diuretics – increased risk of arrhythmias, due to the possibility of electrolyte disorders (hylokalemia, hylomagnesemia). With hypotensive agents, especially alpha-adrenoblockers – increased hypotensive effect and risk of orthostatic hypotension (additive effect). For clonidine and guanethidine see section “Interaction with other medicinal agents”, subsection “Unrecommended drug combinations”. With other drugs with CNS depressant effect: morphine derivatives (analgesics, anti-cough agents), barbiturates, benzodiazepines, non-benzodiazepine anxiolytics, hypnotics, neuroleptics, antidepressants with sedative effect (amitriptyline, doxepin, mianserine, mirtazapine, trimipramine), histamine H1 receptor blockers with sedative effect, central hypotensive agents, baclofen, thalidomide, pizotifen – the risk of additional CNS depression, respiratory depression. With tricyclic antidepressants, MAO inhibitors, maprotiline – increased risk of malignant neuroleptic syndrome, possible increase and duration of sedative and anticholinergic effects. With atropine and other cholinolytics, as well as with drugs with cholinolytic action (imipramine antidepressants, anticholinergic antiparkinsonian drugs, disopyramide) – possibility of cumulation of adverse 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-adrenoblockers – risk of hypotension, especially orthostatic (additive effect), and risk of irreversible retinopathy, arrhythmias and tardive dyskinesia. With hepatotoxic drugs – increased risk of hepatotoxic effects. With lithium salts – reduced absorption in the gastrointestinal tract, increased rate of lithium excretion, increased severity of extrapyramidal disorders; and the early signs of lithium intoxication (nausea and vomiting) may be masked by the antiemetic effect of phenothiazines. With alpha- and beta-adreno stimulants (epinephrine, ephedrine) – reduction of their effects, possible paradoxical reduction of blood pressure. With antithyroid drugs – increased risk of agranulocytosis. With apomorphine – reduction of the vomiting effect of apomorphine, increasing its depressing effect on the CNS. With hypoglycemic drugs – when combined with neuroleptics, hypoglycemic effect may decrease, which may require increasing their doses.

Combinations of medicinal products in administration of which there is interaction that should be taken into account: with antacids (salts, oxides and hydroxides of magnesium, aluminum and calcium) – decrease of absorption of pericyazine in the gastrointestinal tract. If possible, the interval between intake of antacids and pericyazine should be at least two hours. With bromocriptine – increased plasma prolactin concentration when taking pericyazine interferes with the effects of bromocriptine. With agents for appetite reduction (with the exception of fenfluramine ) – reduction of their effect.

Special Instructions

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

Contraindications

Absolute:

• closed-angle glaucoma;
• prostate urinary retention;
• prostate adenoma;
Parkinson’s disease;
• agranulocytosis, porphyria in history;
• concomitant therapy with levodopa;
• hypersensitivity to pericyazine.

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, in some cases the following adverse reactions may be observed, 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.
Central nervous system
Sedation or somnolence, 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 common when using the drug in high doses):

• acute dystonias or dyskinesias (spastic torticollis, oculogyric crises, trismus, etc.), usually occurring within 4 days of starting treatment or increasing the dose;
• Parkinsonism, which develops more frequently in elderly patients and/or after long-term treatment (over weeks or months) and is partially resolved by administration of anticholinergic anti-parkinsonian drugs and is manifested by the appearance of one or more of the following symptoms Tremor (very often the only manifestation of parkinsonism), rigidity, akinesia in combination with or without muscle hypertonicity;
• tardive dystonias or dyskinesias, usually (but not always) occurring with long-term treatment and/or high-dose use of the drug, and may occur even after discontinuation of treatment (when they occur, anticholinergic antiparkinsonian agents have no effect and may cause deterioration);
• akatisia, usually seen after high initial doses.
  Respiratory depression (possible in patients with predisposing factors to the development of respiratory depression, such as patients receiving other drugs that can depress breathing, elderly patients, etc.).
  Autonomic nervous system disorders
• Anticholinergic effects (dry mouth, accommodation paresis, urinary retention, constipation, paralytic ileus).
  Cardiovascular system effects
• Reduction in blood pressure, usually postural arterial hypotension (occurring more frequently in elderly patients and patients with reduced circulating blood volume, especially at the start of treatment and when using high initial doses).
• Arrhythmias, including atrial arrhythmias, atrioventricular block, ventricular tachycardia, including potentially fatal pirouette-type ventricular tachycardia, more likely with high doses.
• E ECG changes, usually minor: QT interval prolongation, ST segment depression, appearance of the U wave and changes in the T wave.
• In cases of thromboembolism, including pulmonary embolism (sometimes fatal) and cases of deep vein thrombosis have been observed with neuroleptics.
  Endocrine and metabolic disorders (more common when using the drug in high doses)
• Hyperprolactinemia, which may lead to amenorrhea, galactorrhea, gynecomastia, impotence, frigidity.
• Body weight gain.
• Disorders 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 common when using the drug in high doses). Contact sensitization of the skin.
  Hematological disorders
• Leukopenia (seen in 30% of patients receiving high doses of neuroleptics).
• Extremely rare: agranulocytosis, whose development is independent of the dose, and which may occur both immediately and after leukopenia lasting for two to three months.
  Ophthalmic disorders
• Brownish deposits in the anterior chamber of the eye, corneal and lens pigmentation due to drug accumulation, usually not affecting vision (especially when high doses of phenothiazine derivatives are used for long periods).
  Liver and biliary tract disorders
• Very rare: cholestatic jaundice and hepatic lesions, predominantly cholestatic or mixed type, requiring discontinuation of the drug.
  Others
• Malignant neuroleptic syndrome, a potentially fatal syndrome that can occur with all neuroleptics and is manifested by hyperthermia, muscle rigidity, autonomic disturbances (pallor, tachycardia, unstable blood pressure, increased sweating, shortness of breath) and disturbances in consciousness up to and including coma. The onset of malignant neuroleptic syndrome requires immediate discontinuation of neuroleptic treatment. Although this effect of pericyazine and other neuroleptics is associated with idiosyncrasy, there are predisposing factors for its occurrence, such as dehydration or organic brain lesions.
• Positive serological test for antinuclear antibodies, without clinical manifestations of lupus erythematosis.
• Very rare: priapism, nasal congestion.
• Very rare: development of withdrawal syndrome upon abrupt discontinuation of treatment with high doses of pericyazine, manifested by nausea, vomiting, insomnia and possible exacerbation of underlying disease or development of extrapyramidal disorders.
  There have been isolated cases of sudden death, possibly due to cardiological causes, as well as unexplained sudden deaths among patients taking phenothiazine-type neuroleptics.

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Overdose

Overdose can cause severe extrapyramidal disorders and coma. Treatment should be symptomatic and administered in a specialized department.