Gross formula

C 21 H 23 N 3 OS

Pharmacological group of the substance Periciazine

Nosological classification (ICD-10)

CAS Code

2622-26-6

Characteristics of the substance Periciazine

Piperidine phenothiazine derivative.

Pharmacology

pharmachologic effect- antipsychotic, neuroleptic, antiemetic.

Blocks postsynaptic D 2 -dopamine receptors located in the mesolimbic system of the brain (antipsychotic effect), hypothalamus (hypothermic effect and galactorrhea), trigger zone of the vomiting center, extrapyramidal system.

It is characterized by strong antiemetic, anticholinergic and sedative effects, moderate extrapyramidal effects, and causes hypothermia. The peripheral alpha-adrenolytic effect is manifested by hypotension (the hypotensive effect is moderate), and the H1-antihistamine effect is manifested by an antiallergic effect.

The antipsychotic effect is combined with a sedative, there is no stimulating component. Sedation is clearly expressed in relation to the angry-irritable and angry type of affect. The decrease in aggressiveness is not accompanied by the appearance of severe lethargy and lethargy. Particularly effective for behavioral disorders (especially in children), contact disorders.

When taken orally, it is well absorbed from the gastrointestinal tract. Subject to a first-pass effect through the liver, plasma concentrations vary widely. Binding to blood plasma proteins is 90%. Easily passes through histohematic barriers, including the BBB, is intensively distributed into tissues, penetrates breast milk. Metabolized in the liver (hydroxylation and conjugation), excreted in urine, bile and feces, and undergoes hepatic recirculation. T1/2 is about 30 hours (elimination of biotransformation products takes longer).

Use of the substance Periciazine

Acute psychotic disorders. Chronic psychotic disorders such as schizophrenia, chronic non-schizophrenic delusional disorders: paranoid delusional disorders, chronic hallucinatory psychoses (for treatment and prevention of relapses). Anxiety, psychomotor agitation, aggressive or dangerous impulsive behavior (as an additional drug for short-term treatment of these conditions).

Contraindications

Hypersensitivity, angle-closure glaucoma, urinary retention due to diseases prostate gland, history of agranulocytosis, history of porphyria, concomitant therapy with dopaminergic agonists, vascular insufficiency(collapse), acute poisoning with substances that depress the central nervous system, or coma, heart failure, pheochromocytoma, pseudoparalytic myasthenia gravis (Erb-Goldflam disease).

Restrictions on use

Cardiovascular diseases, renal and/or liver failure, epilepsy, Parkinson's disease, elderly age(increases the risk of developing excessive hypotensive effect and CNS depression).

Use during pregnancy and breastfeeding

Side effects of the substance Periciazine

From the nervous system and sensory organs: state of depression, extrapyramidal disorders, early dyskinesia (spasmodic torticollis, oculomotor crisis, trismus), tardive dyskinesia.

Others: orthostatic hypotension, anticholinergic effects (dry mouth, constipation, accommodation paresis, urinary retention), impotence, frigidity, amenorrhea, galactorrhea, gynecomastia, hyperprolactinemia, weight gain, cholestatic jaundice, agranulocytosis, photosensitivity, allergic reactions.

Interaction

Enhances the effect of antihypertensive drugs, the inhibitory effect on the central nervous system of tranquilizers, alcohol, analgesics, hypnotics and anesthesia.

Overdose

Symptoms: parkinsonism, coma.

Treatment: symptomatic.

Catad_pgroup Antipsychotics (neuroleptics)

Neuleptil - instructions for use

INSTRUCTIONS
(information for specialists)
By medical use drug

Registration number:

P N014803/01-110110

Trade name of the drug: Neuleptil ®

International nonproprietary name:

periciazine.

Dosage form:

capsules.

Compound
One capsule contains:
active substance: periciazine - 10 mg.
Excipients: calcium hydrogen phosphate dihydrate, magnesium stearate, titanium dioxide (E 171), gelatin.

Description:
appearance of capsules: opaque hard gelatin capsules No. 4, body white, white cap.
contents of capsules: yellow powder, practically odorless.

Pharmacotherapeutic group Antipsychotic (neuroleptic).

CodeATX-N5AC01.

Pharmacological properties
Pharmacodynamics
Periciazine is an antipsychotic from the group of piperidine phenothiazine derivatives, the antidopaminergic activity of which determines the development of therapeutic antipsychotic (without a stimulant component), as well as antiemetic and hypothermic effects of the drug. However, antidopaminergic activity is also associated with the development of its side effects (extrapyramidal syndrome, movement disorders and hyperprolactinemia).
The antidopaminergic activity of periciazine is moderate, 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 distinct sedative effect, which can also be a desirable clinical effect, especially with angry-irritable and angry types of affect, and the decrease in aggressiveness is not accompanied by the appearance of lethargy and lethargy. Compared with chlorpromazine, periciazine has more pronounced antiserotonin, antiemetic and central sedative effects, but less pronounced antihistamine effects.
Periciazine reduces aggressiveness, excitability, and disinhibition, making it effective for behavioral disorders. Due to its normalizing effect on behavior, periciazine is called a “behavior corrector.”
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 intense first-pass metabolism in the intestine and/or liver, therefore, after oral administration, the concentration of unchanged periciazine in plasma is lower than with intramuscular administration and varies widely.
After oral administration of 20 mg of pericyazine (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 intensively penetrates tissues, as it easily passes through histohematic barriers, including the blood-brain barrier.
Most of pericyazine is metabolized in the liver by hydroxylation and conjugation. Metabolites released in bile can be reabsorbed in the intestine. The half-life of pericyazine 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 bile and feces.
In elderly patients, the metabolism and excretion of phenothiazines slows down.

Indications for use

Acute psychotic disorders.

Chronic psychotic disorders such as schizophrenia, chronic non-schizophrenic delusional disorders: paranoid delusional disorders, chronic hallucinatory psychoses (for treatment and relapse prevention).

Anxiety, psychomotor agitation, aggressive or dangerous impulsive behavior (as an additional drug for the short-term treatment of these conditions). Contraindications

Hypersensitivity to pericyazine and/or other ingredients of the drug.

Angle-closure glaucoma.

Urinary retention due to prostate diseases.

History of agranulocytosis.

History of porphyria.

Concomitant therapy with dopaminergic agonists: levodopa, amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, piribenidyl, pramipexole, quinagolide, ropinirole, with the exception of their use in patients with Parkinson's disease (see section "Interaction with other drugs") .

Vascular insufficiency (collapse).

Acute poisoning with substances that depress the central nervous system or coma.

Heart failure.

Pheochromocytoma.

Myasthenia gravis pseudoparalytic (Erb-Goldflam disease).

Children's age (for this dosage form) The drug should be used with caution in the following groups of patients:

in patients with predisposing factors for the development of ventricular arrhythmias (patients with cardiovascular diseases, congenital long QT interval, bradycardia, hypokalemia, hypomagnesemia, fasting and/or alcohol abuse, receiving concomitant therapy with drugs that can prolong the QT interval and/or cause severe bradycardia less than 55 beats per minute, slow intracardiac conduction, or alter blood electrolytes), as phenothiazine antipsychotics may, in very rare cases, cause QT prolongation (this effect is dose dependent) and increase the risk of severe ventricular arrhythmias, including bidirectional ventricular tachycardia pirouette type, which can be life-threatening ( sudden death);

in patients with renal and/or liver failure (risk of drug accumulation);

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 weather and hypothermia in cold weather, constipation, paralytic intestinal obstruction and urinary retention in prostate diseases, there is a risk of drug accumulation due to decreased liver and kidney function);

in patients with cardiovascular diseases (due to the danger for them of possible hypotensive and quinidine-like effects, the ability of the drug to cause tachycardia);

in elderly patients with dementia and patients with risk factors for stroke (in elderly patients with dementia, a threefold increase in the incidence of strokes was observed);

in patients with risk factors for thromboembolism (see sections "Side effects", " special instructions").

in patients with epilepsy who do not receive adequate anticonvulsant therapy(neuroleptics from the phenothiazine group reduce the threshold for convulsive readiness);

in patients with Parkinson's disease;

in patients with hyperthyroidism (increased risk of developing agranulocytosis when using periciazine in combination with drugs for the treatment of hyperthyroidism);

in patients with changes in blood picture ( increased risk development of leukopenia or agranulocytosis);

in patients with breast cancer (possibility of disease progression due to increased levels of prolactin in the blood). Pregnancy and lactation
Pregnancy
It is advisable to support mental health mothers during pregnancy to prevent decompensation. If maintaining mental balance is necessary drug therapy, then it should begin and continue at effective doses throughout pregnancy. Experimental studies in animals did not reveal the teratogenic effect of pericyazine. There have been no studies of the teratogenic effect of periciazine in humans; there is no data on the effect of taking periciazine during pregnancy on the development of the fetal brain, however, an analysis of pregnancies that occurred while taking periciazine showed the absence of 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 weigh the benefit for the mother against the risk to the fetus. It is advisable to limit the duration of administration of the drug during pregnancy.
In rare cases, the following disorders have been reported in newborns whose mothers received long time treatment with large doses of pericyazine:

tachycardia, hyperexcitability, abdominal bloating, delayed passage of meconium associated with the atropine-like effect of the drug, which can be potentiated if it is combined with corrective antiparkinsonian drugs that inhibit cholinergic transmission in the central nervous system;

extrapyramidal disorders (muscle hypertonicity, tremor);

sedation
If possible, at the end of pregnancy, it is advisable to reduce the dose of pericyazine and antiparkinsonian drugs that correct it, which can potentiate the atropine-like effect of neuroleptics. 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 breast-feeding while taking the drug. Directions for use and doses
Neuleptil ® , 10 mg capsules, is intended for oral administration by adult patients.
In children, Neuleptil ® 4%, oral solution should be used (see section "Contraindications").
The dosage regimen varies significantly depending on the indications and the patient's condition. Doses of the drug should be selected individually. If the patient's condition allows, treatment should begin with low doses, which can then be gradually increased. The minimum effective dose should always be used.
The daily dose should be divided into 2 or 3 doses and the majority 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 be increased 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 effect
Neuleptil ® is usually well tolerated, however, in some cases the following may occur: unwanted reactions, the occurrence of which may or may not depend on the size of the dose taken, and in the latter case, be a consequence of increased individual sensitivity of the patient.
From the 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 (more often occurring when using the drug in high doses):

acute dystonia or dyskinesia (spasmodic torticollis, oculogyric crises, trismus, etc.), usually occurring within 4 days after starting treatment or increasing the dose;

parkinsonism, which most often develops in elderly patients and/or after long-term treatment (weeks or months) and is partially eliminated by the appointment of anticholinergic antiparkinsonian 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 dystonia or dyskinesia, usually (but not always) occurring with long-term treatment and/or use of the drug in high doses, and may occur even after cessation of treatment (if they occur, anticholinergic antiparkinsonian drugs have no effect and may cause deterioration);

akathisia, usually observed after 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 depress breathing, in patients old age and so on.).
From the autonomic nervous system

Anticholinergic effects (dry mouth, accommodation paresis, urinary retention, constipation, paralytic ileus).
From the outside of cardio-vascular system

Decline blood pressure, usually postural arterial hypotension (more often occurring 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 abnormalities rhythm, atrioventricular block, ventricular tachycardia, including potentially fatal ventricular tachycardia of the torsade de pointes type, more likely when using high doses (see sections "Contraindications", subsection "With caution"; "Interaction with other drugs"; "Special instructions").

ECG changes, usually minor: QT prolongation, ST segment depression, U wave and T wave changes.

Cases of thromboembolism, including thromboembolism, have been observed with the use of antipsychotics pulmonary artery(sometimes fatal) and cases of deep vein thrombosis (see section "Special instructions").
Endocrine and metabolic disorders(more often occurring when using the drug in high doses)

Hyperprolactinemia, which can lead to amenorrhea, galactorrhea, gynecomastia, impotence, frigidity.

Increase in body weight.

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 skin sensitization (see section "Special instructions").
Hematological disorders

Leukopenia (observed in 30% of patients receiving high doses of antipsychotics).

Extremely rare: agranulocytosis, the development of which does not depend on the dose, and which can occur either immediately or after leukopenia lasting for two to three months.
Ophthalmological disorders

Brownish deposits in the anterior chamber of the eye, pigmentation of the cornea and lens due to the accumulation of the drug, 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, predominantly cholestatic or mixed, requiring discontinuation of the drug.
Other

Neuroleptic malignant syndrome, a potentially fatal syndrome that can occur when taking all antipsychotics and is manifested by hyperthermia, muscle rigidity, autonomic disorders (pallor, tachycardia, unstable blood pressure, increased sweating, shortness of breath) and disturbances of consciousness up to coma. The occurrence of neuroleptic malignant syndrome requires immediate cessation of antipsychotic treatment. Although this effect of pericyazine 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 lupus erythematosis.

Very rare: priapism, nasal congestion.

Very rare: development of withdrawal syndrome upon abrupt cessation of treatment with high doses of pericyazine, manifested by nausea, vomiting, insomnia and the possibility of exacerbation of the underlying disease or the development of extrapyramidal disorders.
Among patients taking phenothiazine antipsychotics, isolated cases of sudden death, possibly caused by cardiac causes, have been reported (see sections "Contraindications", subsection "With caution"; "Special instructions"), as well as unexplained cases of sudden death. Overdose
Symptoms
Symptoms of phenothiazine overdose include CNS depression progressing from drowsiness to coma with areflexia. Patients with initial manifestations of intoxication or moderate intoxication may experience restlessness, confusion, agitation, restlessness, or delirium. Other manifestations of overdose include decreased blood pressure, tachycardia, ventricular arrhythmias, ECG changes, collapse, hypothermia, constriction of the pupil, tremor, muscle twitching, muscle spasm or rigidity, convulsions, dystonic movements, muscle hypotonia, difficulty swallowing, respiratory depression, apnea, cyanosis. Polyuria leading to dehydration and severe extrapyramidal dyskinesia are also possible.
Treatment
Treatment should be symptomatic and carried out in a specialized department, where it is possible to organize monitoring of respiratory and cardiovascular functions and continue it until the overdose phenomena are completely eliminated.
If less than 6 hours have passed after taking the drug, then gastric lavage or aspiration of its contents should be performed. The use of emetics is contraindicated due to the risk of aspiration of vomit against the background of lethargy and/or extrapyramidal disorders. Possible use activated carbon. There is no specific antidote.
Treatment should be aimed at maintaining the vital functions of the body.
If blood pressure decreases, the patient must be transferred to horizontal position with raised legs. Intravenous fluid infusion is indicated. If fluid administration is not sufficient to correct hypotension, norepinephrine, dopamine, or phenylephrine may be administered. Administration of epinephrine is contraindicated.
With hypothermia, you can wait for it to resolve on its own, unless the body temperature drops to a level at which the development of cardiac arrhythmias is possible (that is, to 29.4 ° C).
Ventricular or supraventricular tachyarrhythmias usually respond to recovery normal temperature body and elimination of hemodynamic and metabolic disorders. If life-threatening arrhythmias persist, antiarrhythmics may be required. The use of lidocaine and, if possible, long-acting antiarrhythmic drugs should be avoided.
If the central nervous system and breathing are depressed, it may be necessary to transfer the patient to artificial ventilation lungs and antibiotic therapy to prevent pulmonary infections.
Severe dystonic reactions usually respond to intramuscular or intravenous administration of procyclidine (5-10 mg) or orphenadrine (20-40 mg).
Seizures can be stopped intravenous administration diazepam.
For extrapyramidal disorders, anticholinergic antiparkinsonian drugs are used intramuscularly. Interaction with other drugs

With dopaminergic agonists (levodopa, amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, piribedil, pramipexole, quinagolide, ropinirole) in patients without Parkinson's disease-mutual antagonism between dopaminergic agonists and pericyazine. Extrapyramidal disorders caused by taking a neuroleptic should not be treated with dopaminergic agonists (reduction or loss of neuroleptic activity) - in this case, the use of anticholinergic antiparkinsonian drugs is more indicated.
Not recommended combinations

With dopaminergic agonists (levodopa, amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, piribedil, pramipexole, quinagolide, ropinirole) in patients with Parkinson's disease - mutual antagonism between dopaminergic agonists and pericyazine. Dopaminergic agonists may exacerbate psychotic disorders. If patients with Parkinson's disease receiving dopaminergic agonists require treatment with an antipsychotic, they should be withdrawn by gradual dosage reduction (sudden withdrawal of dopaminergic agonists may increase the risk of developing neuroleptic malignant syndrome). When using periciazine together with levodopa, use minimally. effective doses 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 simultaneously with antipsychotics.

With sultopride - an increased risk of developing ventricular arrhythmias, in particular ventricular fibrillation.
Combinations medicines, the use of which requires caution

With drugs that can increase the QT interval (antiarrhythmics IA and III class, moxifloxacin, erythromycin, methadone, mefloquine, sertindole, tricyclic antidepressants, lithium salts and cisapride and others) - increases the risk of developing arrhythmias (see section "Contraindications", subsection "With caution").

With thiazide diuretics, the risk of arrhythmias increases due to the possibility of developing electrolyte disorders (hypokalemia, hypomagnesemia).

WITH antihypertensive drugs, especially alpha-blockers - increase hypotensive effect and the risk of developing orthostatic hypotension (additive effect). For clonidine and guanethidine, see the section "Interactions with other drugs", subsection "Not recommended combinations of drugs".

With other drugs that have a depressant effect on the central nervous system: morphine derivatives (analgesics, antitussives), barbiturates, benzodiazepines, non-benzodiazepine anxiolytics, hypnotics, neuroleptics, antidepressants with a sedative effect (amitriptyline, doxepin, mianserin, mirtazapine, trimipramine), histamine H blockers 1-receptors with a sedative effect, centrally acting antihypertensives, baclofen, thalidomide, pizotifen - the danger of additional depressive effects on the central nervous system, respiratory depression.

With tricyclic antidepressants, MAO inhibitors, maprotiline, there is an increased risk of developing neuroleptic malignant syndrome, and the sedative and anticholinergic effects may be enhanced and prolonged.

With atropine and other anticholinergics, as well as drugs with anticholinergic effects (imipramine antidepressants, anticholinergic antiparkinsonian drugs, disopyramide) - possibility of accumulation unwanted effects associated with anticholinergic effects, such as urinary retention, constipation, dry mouth, heat stroke, etc., as well as reducing the antipsychotic effect of antipsychotics.

With beta-blockers - the risk of developing hypotension, especially orthostatic (additive effect), and the risk of developing irreversible retinopathy, arrhythmias and tardive dyskinesia.

With hepatotoxic drugs - increased risk of hepatotoxicity.

With lithium salts - decreased absorption in gastrointestinal tract, increasing the rate of Li + excretion, increasing the severity of extrapyramidal disorders; and early signs Li+ toxicity (nausea and vomiting) may be masked by the antiemetic effect of phenothiazines.

With alpha and beta adrenergic stimulants (epinephrine, ephedrine) - a decrease in their effects, a paradoxical decrease in blood pressure is possible.

With antithyroid drugs - an increased risk of developing agranulocytosis.

With apomorphine - a decrease in the emetic effect of apomorphine, an increase in its inhibitory effect on the central nervous system.

With hypoglycemic drugs - when combined with antipsychotics, the hypoglycemic effect may decrease, which may require increasing their doses.
Combinations of drugs with interactions that should be taken into account

With antacids (salts, oxides and hydroxides of magnesium, aluminum and calcium) - decreased absorption of periciazine in the gastrointestinal tract. If possible, the interval between taking antacids and periciazine should be at least two hours.

With bromocriptine - an increase in plasma prolactin concentration when taking pericyazine interferes with the effects of bromocriptine.

With appetite suppressants (except for fenfluramine), their effect is reduced. special instructions
When taking pericyazine, it is recommended to regularly monitor the composition of peripheral blood, especially in the event of fever or infection (the possibility of developing leukopenia and agranulocytosis). If significant changes are detected in the peripheral blood (leukocytosis, granulocytopenia), treatment with pericyazine should be discontinued.
Neuroleptic malignant syndrome - in the event of an unexplained increase in body temperature, treatment with periciazine should be discontinued, as this may be a manifestation of neuroleptic malignant syndrome, early manifestations which may also be the appearance of autonomic disorders (such as increased sweating, instability of pulse and blood pressure).
During treatment, you should not take alcohol or drugs containing alcohol, since the potentiation of the sedative effect leads to a decrease in reaction, which can be dangerous for persons managing vehicles and mechanisms (see section "Interactions with other drugs")
Due to the drug's ability to lower the seizure threshold, when periciazine is taken by patients with epilepsy, they should undergo careful clinical and, if possible, electroencephalographic monitoring.
With the exception of special occasions, periciazine should not be used in patients with Parkinson's disease (see sections "Contraindications", subsection "With caution").
Phenothiazine neuroleptics are capable of dose-dependent prolongation of the QT interval, which is known to increase the risk of developing severe ventricular arrhythmias, including life-threatening torsade de pointes (TdP). The risk of their occurrence increases in the presence of bradycardia, hypokalemia and prolongation of the QT interval (congenital or acquired under the influence of drugs that increase the duration of the QT interval). Before prescribing antipsychotic therapy, if the patient's condition allows, it is necessary to exclude the presence of factors predisposing to the development of these severe arrhythmias (bradycardia less than 55 beats per minute, hypokalemia, hypomagnesemia, slow intraventricular conduction and congenital long QT interval or long QT interval when using other drugs, prolonging the QT interval) (see sections "Contraindications", subsection "With caution" "Side effects").
Monitoring of these risk factors should also be carried out during treatment with the drug.
If bloating and pain in the abdomen occur while taking periciazine, abdominal cavity, the necessary examination should be carried out to exclude intestinal obstruction, since the development of this side effect requires the necessary urgent measures.
Particularly careful monitoring of the patient's condition and special caution is required when prescribing periciazine and other antipsychotics to elderly patients, patients with cardiovascular diseases, patients with hepatic and renal failure, elderly patients with dementia and patients with risk factors for stroke (see section "Contraindications", subsection "With caution").
In randomized clinical studies When some atypical antipsychotics were compared with placebo in elderly patients with dementia, a threefold increase in the risk of cerebrovascular events was observed. The mechanism of this risk is not known. An increase in this risk cannot be ruled out with other antipsychotics or in other patient populations, so periciazine should be used with caution in patients with risk factors for stroke.
In elderly patients with dementia-related psychosis, an increased risk of death was observed when treated with antipsychotic drugs. Analysis of 17 placebo-controlled studies ( average duration>10 weeks) showed that most patients receiving atypical antipsychotics had a 1.6 to 1.7 times greater risk of death than patients receiving placebo. Although the causes of death in clinical studies with atypical antipsychotics varied, most causes of death were either cardiovascular (eg, heart failure, sudden death) or infectious (eg, pneumonia) in nature. Observational studies have confirmed that, like treatment with atypical antipsychotics, treatment with conventional antipsychotics may also increase mortality. The extent to which the increase in mortality may be due to the antipsychotic drug rather than to certain patient characteristics is unclear.
When using antipsychotic drugs Cases of venous thromboembolism, sometimes fatal, have been observed. Therefore, pericyazine should be used with caution in patients with risk factors for thromboembolism, see "Side effects".
Due to the possibility of developing withdrawal syndrome upon abrupt cessation of treatment with high doses of pericyazine (see section " Side effects"), discontinuation of the drug when used in high doses should be carried out gradually.
Due to the possibility of developing photosensitivity, patients receiving periciazine should be advised to avoid exposure to direct sunlight.
Due to the fact that in very rare cases, people who frequently handle phenothiazines may develop contact skin sensitization to phenothiazines, direct contact of the drug with the skin should be avoided.
In pediatric practice, it is advisable to use Neuleptil ® 4%, oral solution. Impact on the ability to drive vehicles or other machinery
Patients, especially those who are drivers of vehicles or people working with other mechanisms, should be informed about the possibility of drowsiness and decreased response in connection with taking the drug, especially at the beginning of treatment, since impaired psychomotor reactions can be potentially dangerous when driving vehicles and working with machinery. Release form
Capsules 10 mg.
10 capsules per blister made of PVC/aluminum foil. 5 blisters along with instructions for use in a cardboard box. Storage conditions
At a temperature not higher than 25°C.
Keep out of the reach of children.
List B. Best before date
5 years.
After the expiration date, the drug cannot be used. Conditions for dispensing from pharmacies
On prescription. Manufacturer
Haupt Pharma Livron, France Manufacturer's address:
Rue Comte de Sinard - 26250, Livron-sur-Drôme, France Consumer complaints should be sent to:
115035, Moscow, st. Sadovnicheskaya, 82, building 2.

Excipients: calcium hydrogen phosphate dihydrate - 556 mg, croscarmellose sodium - 18 mg, magnesium stearate - 6 mg.

Capsule composition:(body: titanium dioxide - 2%, gelatin - up to 100%; cover: crimson dye [Ponzo 4 R] - 1.36%, red iron oxide dye - 0.85%; titanium dioxide - 2.5%, gelatin - up to 100%) - 96 mg.

10 pieces. - contour cellular packaging (5) - cardboard packs.

pharmachologic effect

Antipsychotic drug (neuroleptic), piperidine derivative of phenothiazine. It has an antipsychotic, sedative, pronounced effect. It has adrenergic blocking and pronounced anticholinergic activity, causing a hypotensive effect. Compared to chlorpromazine, it has more pronounced antiserotonin activity and has a stronger central sedative effect.

The mechanism of antipsychotic action is associated with blockade of postsynaptic dopaminergic receptors in the mesolimbic structures of the brain. It also has an alpha-adrenergic blocking effect, suppresses the release of pituitary and hypothalamic hormones. Blockade of dopamine receptors increases the release of prolactin by the pituitary gland.

The central antiemetic effect is due to inhibition or blockade of dopamine D2 receptors in the chemoreceptor trigger zone of the cerebellum, the peripheral effect is due to blockade vagus nerve in the gastrointestinal tract. The antiemetic effect is enhanced, apparently, due to anticholinergic, sedative and antihistamine properties.

Pharmacokinetics

Clinical data on the pharmacokinetics of pericyazine are limited.

Phenothiazines have high protein binding. They are excreted mainly by the kidneys and partly with bile.

Indications

Psychopathy (excitable and hysterical), psychopath-like states in schizophrenia, paranoid states in organic, vascular presenile and senile diseases, as an adjuvant in psychotic disorders to overcome residual phenomena with a predominance of hostility, impulsivity and aggressiveness.

Contraindications

Severe cardiovascular diseases, severe central nervous system depression, a history of toxic agranulocytosis, angle-closure glaucoma, porphyria, prostate diseases, pregnancy, lactation.

Dosage

The initial daily dose is 5-10 mg, in patients with hypersensitivity for phenothiazines - 2-3 mg. Average daily doses are 30-40 mg, dosage frequency 3-4 times a day, preferably in the evening.

For children and the elderly, the initial dose is 5 mg/day, then the dose is gradually increased to 10-30 mg/day.

Maximum daily dose for adults is 60 mg.

Side effects

From the side of the central nervous system: insomnia, agitation, akathisia, blurred vision, depression, early dyskinesia (spasmodic torticollis, oculomotor crisis, trismus), extrapyramidal syndrome, tardive dyskinesia.

From the cardiovascular system: postural hypotension, rhythm disturbances.

From the outside digestive system: cholestatic jaundice.

From the outside respiratory system: nasal congestion, respiratory depression (in predisposed patients).

From the outside endocrine system: impotence, frigidity, amenorrhea, galactorrhea, gynecomastia, hyperprolactinemia.

From the side of metabolism: weight gain (possibly significant).

From the hematopoietic system: leukopenia (mainly with long-term use in high doses); rarely - agranulocytosis.

Dermatological reactions: photosensitivity.

Effects due to anticholinergic action: dry mouth, constipation, accommodation disturbances, urinary retention.

Drug interactions

When used simultaneously with drugs that have a depressant effect on the central nervous system, with ethanol or ethanol-containing drugs, the depressant effect on the central nervous system and respiratory depression may be enhanced.

When used simultaneously with drugs that cause extrapyramidal reactions, an increase in the frequency and severity of extrapyramidal disorders is possible.

With simultaneous use, it is possible to enhance the anticholinergic effects of other drugs, while the antipsychotic effect of the antipsychotic may decrease.

When used simultaneously with anticonvulsants it is possible to lower the threshold of convulsive readiness; with drugs for the treatment of hyperthyroidism - the risk of developing agranulocytosis increases; with drugs that cause arterial hypotension, severe orthostatic hypotension is possible.

When used simultaneously with tricyclic antidepressants, maprotiline, and MAO inhibitors, the risk of developing NMS increases.

With simultaneous use, it is possible to reduce the effect of amphetamines, levodopa, clonidine, guanethidine, epinephrine.

When used simultaneously with antiparkinsonian drugs, lithium salts, the absorption of phenothiazines may be impaired.

When used simultaneously with fluoxetine, the development of extrapyramidal symptoms and dystonia is possible.

When used simultaneously, its vasoconstrictor effect may be weakened.

special instructions

Periciazine should be used with caution in cases of hypersensitivity to other phenothiazine drugs, in elderly patients (increased risk of excessive sedation and hypotensive effects), in depleted and weakened patients.

Phenothiazines are used with extreme caution in patients with pathological changes blood pictures, liver dysfunction, alcohol intoxication, Reye's syndrome, as well as, cardiovascular diseases, predisposition to the development of glaucoma, Parkinson's disease, gastric ulcer and duodenum, urinary retention, chronic diseases respiratory organs (especially in children), epileptic seizures, vomiting.

In case of hyperthermia, which is one of the elements of NMS, periciazine should be discontinued immediately.

In children, especially with acute diseases, when using phenothiazines, the development of extrapyramidal symptoms is more likely.

During the treatment period, avoid drinking alcohol.

Impact on the ability to drive vehicles and operate machinery

Use with caution in patients potentially involved in dangerous species activities requiring high speed psychomotor reactions.

Pregnancy and lactationUse in old age

Periciazine should be used with caution in elderly patients.

In the article we will look at analogues of Periciazine.

This drug is an antipsychotic. The drug can produce an antipsychotic, sedative, and pronounced antiemetic effect. The drug is endowed with pronounced anticholinergic and adrenergic blocking activity and, as a rule, causes a hypotensive effect. Compared to Chlorpromazine, it has a more pronounced antiserotonin activity and may have a stronger sedative central effect.

The presented product contains the same component. Excipients in in this case Calcium hydrogen phosphate dihydrate, croscarmellose sodium and magnesium stearate are used. Periciazine has two trade names: “Periciazin” itself, as well as “Neuleptil”.

Pharmacological effects of "Pericyazine"

So, “Pericyazine” is an antipsychotic drug (neuroleptic). This medication can have antipsychotic, pronounced antiemetic and sedative effects. Possessing pronounced anticholinergic and adrenergic blocking activity, the drug causes a hypotensive effect.

Initial daily dose This remedy is usually 5 or 10 milligrams. And for patients with hypersensitivity to phenothiazine, doctors usually prescribe 2 or 3 milligrams. The average daily dosage is, according to the instructions, from 30 to 40 milligrams, the frequency of administration is three to four doses per day. It is preferable to carry out treatment in the evening hours. Maximum daily norm for adults it is usually 60 milligrams.

"Periciazine" for children

For children, as well as for older people, the initial dosage is 5 milligrams. Next, the amount of the drug is gradually increased to 10 or 30 mg.

Indications

As the instructions for use indicate, “Pericyazin” is used for the treatment of following cases:

• Against the background of the development of psychopathy, characterized by an excitable and hysterical character, as well as psychopath-like states in the presence of schizophrenia.
• In case of paranoid forms of mental disorders.
• In the presence of organic, vascular presenile and senile disease.
• As an aid in psychotic disorder to cope residual phenomenon with a predominance of impulsiveness, hostility or aggressiveness.

Contraindications for use

This drug is not used in a number of situations:

• Against the background of severe heart and vascular diseases.
• With severe depression of the nervous system.
• In case of toxic agranulocytosis in the anamnesis.
• In the presence of angle-closure glaucoma and porphyria.
• Against the background of prostate diseases.
• During pregnancy and lactation.

This must be taken into account before making an appointment.

Drug interactions

In accordance with the instructions for use of Periciazine, when used simultaneously with medicines, which have a depressing effect on nervous system or with ethanol, breathing problems may occur. When combined with drugs that cause extrapyramidal reactions, it is likely that the severity and frequency of extrapyramidal disorders will increase.

In case of simultaneous use, a significant increase in the anticholinergic effect of other drugs is possible, while the antipsychotic activity of the antipsychotic may decrease. When used in parallel with anticonvulsants one should expect a decrease in the seizure threshold. In combination with medications for the treatment of hyperthyroidism, the risk of developing agranulocytosis increases.

Analogs of this drug

Analogues of this product include:

• The drug "Thioridazine".
• The drug "Pipothiazine".
• A medicine called "Neuleptil".

"Thioridazine"

Pharmacological substitutes for this drug include Sonapax along with Melleril. These drugs may have a mild antipsychotic effect, combined with moderate stimulant, thymoleptic and antidepressant effects.

The analogue of "Pericyazine" "Thioridazine" is used for schizophrenia (in case of development of acute and subacute form), against the background of psychomotor agitation, neurosis and other diseases. This medication is contraindicated if you have allergic reaction, change in blood picture, comatose. With prolonged use of the product, toxic retinopathy may develop.

The release format of this analogue is dragees. As part of treatment, unless otherwise prescribed by a doctor, one tablet is used three times a day.

What other analogues of Periciazine can be found on sale?

Medicinal drug "Pipothiazine"

Pharmacological substitutes for this drug include “Piportil”. It is prescribed to patients for the treatment of various forms of schizophrenia, to combat psychosis with hallucinations, and also as part of therapy mental pathologies and abnormalities in children. "Pipothiazine" is used only in a hospital setting.

A two percent oil solution can have a prolonged effect. The average dose of Pipothiazine for adult patients is 100 milligrams (4 milliliters of solution) administered intramuscularly once every four weeks. In the treatment of chronic psychosis, this drug can be prescribed to the patient orally in a dosage of 20 or 30 milligrams once a day. After achieving stable therapeutic effect the amount of medication can be reduced to 10 milligrams per day.

Contraindications to the use of this analogue are impaired renal function along with angle-closure glaucoma. The release format of “Pipothiazine” is tablets along with drops, solution and ampoules. Next, consider an analogue called “Neuleptil”.

"Neuleptil": solution and drops

Given medicine Produced in solution for oral use (drops) and capsules. The main active ingredient of the drug is a substance called periciazine. "Neuleptil" eliminates the aggressiveness that occurs in patients with mental disorders.

The drug can have an antipsychotic effect by inhibiting the reticular formations and reducing their effect on the cerebral cortex. The drug produces an inhibitory effect on the mediator functions of dopamine. The sedative effect of the drug is usually due to the blocking of central adrenergic receptors located in the area of ​​the reticular formations and a decrease in the activity of histamine receptors.

According to the instructions for use, Neuleptil drops are not prescribed to patients if they suffer from angle-closure glaucoma, Parkinson's pathology, or are receiving therapy with dopaminergic antagonists. This analogue, among other things, is not prescribed when the patient has hypersensitivity to the main component periciazine along with heart failure and Goldflam's disease. It is best to avoid using the medication in question even if the patient has urinary retention, which is caused by pathologies of the prostate gland, porphyria, agranulocytosis, pheochromocytoma, and so on.

With great caution, "Neuleptil" is prescribed to patients when they have heart disease in combination with vascular pathologies, kidney disease, pregnancy and liver problems.

How to use Neuleptil

If there are no other prescriptions, the patient should take this analogue in a dosage of 30 to 100 milligrams. The maximum daily dose of the drug is 0.2 grams. Children take the described medicine in an amount of 0.1 to 0.5 milligrams per kilogram of body weight. The medication is taken two to three times a day.

We reviewed analogues of Periciazine and instructions for it.

"Pericyazine": analogues, trade name, instructions for use - tips and recommendations about health on the site