Neuleptyl 50 capsules. (Perytsyazyn)

Latin name

NEULEPTIL

Packing

50 capsules.

Pharmacological action of

Pharmacodynamics of

Periciazine is a neuroleptic from the group of piperidine derivatives of phenothiazine, the antidopaminergic activity of which determines 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

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

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

It is advisable to maintain the mental health of the mother during pregnancy in order to prevent decompensation. If drug therapy is necessary to maintain mental balance, then it should begin and continue at effective doses throughout pregnancy. Experimental studies in animals did not reveal the teratogenic effect of periciazine. A study of the teratogenic effect of periciazine in humans has not been carried out, there is no data on the effect of taking pericyazin during pregnancy on the development of the fetal brain, however, an analysis of the pregnancies that occurred while taking periciazine showed no specific teratogenic effects. Thus, the risk of teratogenicity of the drug, if any, is negligible.

Prescribing periciazine during pregnancy is possible, but each time it is necessary to compare the benefit for the mother with the risk for the fetus. It is advisable to limit the duration of the drug during pregnancy.

In rare cases, the following disorders were reported in newborns whose mothers received long-term treatment with large doses of pericyazin: tachycardia, hyper excitability, bloating, delayed discharge of meconium associated with the atropine-like effect of the drug, which can be potentiated if combined with corrective anti-Parkinsonian drugs inhibiting cholinergic transmission to the central nervous system extrapyramidal disorders (muscle hypertonicity, tremor) sedation.

If possible, at the end of pregnancy, it is desirable to reduce the dose of pericyazin and its antiparkinsonian drugs that can correct the atropine-like effect of antipsychotics.

In newborns, the state of the nervous system and the function of the gastrointestinal tract should be monitored.

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

In one capsule contains life:

active substance: periciazine - 10 mg.

excipients: calcium hydrogen phosphate dihydrate, magnesium stearate, titanium dioxide (E 171), gelatin.

Dosage and administration of

Neuleptil 10 mg capsule is intended for oral administration by adult patients. In children, Neuleptil 4% oral solution should be used.

Dosage regimen varies significantly depending on the indications and condition of the patient. Doses of the drug should be selected individually. If the condition of the patient allows, then treatment should begin with low doses, which can then gradually increase. The minimum effective dose should always be used.

The daily dose should be divided into 2 or 3 doses and most of the dose should always be taken in the evening. In adults, the daily dose can range from 30 mg to 100 mg. The maximum daily dose is 200 mg.

Treatment of acute and chronic psychotic disorders: the initial daily dose is 70 mg (divided into 2-3 doses). The daily dose can be increased by 20 mg per week until the optimal effect is achieved (on average up to 100 mg per day). In exceptional cases, the daily dose may increase to 200 mg.

Correction of behavioral disorders: the initial daily dose is 10-30 mg.

Treatment of elderly patients: doses are reduced by 2-4 times.

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, may be a consequence of the patient’s increased individual 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 (most often when using the drug in high doses):

acute dystonia or dyskinesia (spasmodic torticollis, oculogyric crises, trismus, etc.), which usually occur within 4 days after the start of treatment or an increase in the dose of

parkinsonism, which often develops in elderly patients and / or after prolonged treatment (within weeks or months) and is partially eliminated with the appointment of anticholinergic antiparkinsonian drugs and is manifested by the appearance of one or more x of the following symptoms: tremor (very often the only manifestation of parkinsonism), stiffness, akinesia in combination with or without muscle hypertonicity

late dystonia or dyskinesia, usually (but not always) arising from long-term treatment and / or use of the drug in high doses, and able to occur even after discontinuation of the treatment (if they occur, anticholinergic antiparkinsonian drugs do not have an effect and can 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.

Lekarstvennoe Interaction

Protyvopokazann e kombynatsyy: with dopaminergic agonists (levodopa, amantadine, apomorphine, bromocriptine, kaberholyn, эntakapon, lysuryd, perholyd, pyrybedyl, pramypeksol, hynaholyd, ropynyrol) in patsyentov without disease Parkynsona - vzaymn y antahonyzm Between dopaminergic agonists and perytsyazynom. 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.

Recommended combinations: with dopaminergic agonists (levodopa, amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, pyribedil, pramipexole, quinagolide, ropinirole) in patients with Parkinson's disease - a mutual antagonism between dopaminergic agonists and pericyazine. Dopaminergic agonists can exacerbate psychotic disorders. If patients with Parkinson's disease receiving dopaminergic agonists require treatment with a neuroleptic, they should be reversed by gradually reducing the doses (sudden withdrawal 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, guanethidine - 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 requiring caution: with drugs capable of increasing the interval of OT (class IA and III antiarrhythmics, moxifloxacin, erythromycin, methadone, mefloquine, sertindol, tricyclic antidepressants, lithium salts and cytidium salts) development of arrhythmias. With thiazide diuretics - the risk of arrhythmias increases, due to the possibility of electrolyte disorders (gilokalemia, gilomagnesemia). With antihypertensives, especially alpha-blockers - an increase in hypotensive action 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 CNS depressant: morphine derivatives (analgesics, antitussives), barbiturates, benzodiazepines, non-benzodiazepine anxiolytics, hypnotics, neuroleptics, antidepressants, sedative effect, aminetripeptine, amitriptyline 1 receptors with sedative effect, antihypertensive agents of central action, baclofen, thalidomide, pisotifen - danger of additional oppressive stvie CNS, respiratory depression. 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, 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 intoxication or moderate intoxication may experience anxiety, confusion, agitation, an excited or deriliotic condition. 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 function and cardiovascular system 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. In the event that fluid administration is insufficient to eliminate hypotension, norepinephrine may be administered, dopamine or phenylephrine. 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

Store in a dry, dark place at a temperature not exceeding 25 ° C.

Expiration

5 years.

Deystvuyuschee substances

Perytsyazyn

dosage form

dosage form

capsules

Sano i-Aventis, France



Neuleptyl 50 capsules. (Perytsyazyn) florida in pharmacy online. Cheap price, instruction, side effects, dosage. Neuleptyl 50 capsules. - Sale. PayPal accept. Free shipping florida. Fast international shipping.