Clinical and pharmacological group: & nbsp

Neuroleptics

Included in the formulation
  • Neuleptil®
    solution inwards 
  • Neuleptil®
    capsules inwards 
  • Periciazine
    capsules inwards 
    R-PHARM, CJSC     Russia
  • Included in the list (Order of the Government of the Russian Federation No. 2782-r of 30.12.2014):

    VED

    ONLS

    АТХ:

    N.05.A.C.01   Periciazine

    Pharmacodynamics:

    Pericyzazine is a neuroleptic from the group of piperidine derivatives of phenothiazine. The mechanism of action is a competitive blockade of postsynaptic dopamine D2 receptors in the mesolimbic structures of the brain. The drug has antipsychotic, antiemetic and hypothermic effects. Antidofaminergic activity of pericyazine can lead to extrapyramidal syndrome, motor disorders and hyperprolactinaemia. The drug blocks adrenoreceptors of the reticular formation of the brainstem and central histamine receptors, due to which the expressed sedative effect of the drug is manifested. The blockade of peripheral H1-histamine receptors causes the antiallergic effect of the drug.

    Pericyzine reduces aggressiveness, excitability, disinhibition, therefore it is used as a "behavior corrector".

    Pharmacokinetics:After ingestion, the drug is rapidly absorbed, subjected to a pre-systemic metabolism in the liver and intestine.After oral administration, the maximum plasma concentration is detected after 2 hours. The connection with plasma proteins is high - 90%. Periciazine easily penetrates through the histohematological barriers, including through the blood-brain barrier. The drug is metabolized mainly in the liver by hydroxylation and conjugation. Metabolites excrete with bile, and then they can be absorbed again in the intestines. The half-life is 12-30 hours. Metabolites are excreted in the urine, and the rest of the drug - with bile and feces.
    Indications:
    • Psychopathy (excitable and hysterical type)
    • Schizophrenia
    • Chronic non-schizophrenic delusional disorders (paranoid delusional disorders, chronic hallucinatory psychoses)
    • Aggressive behavior, anxiety, psychomotor agitation

    VI.G90-G99.G93.9   Disorder of brain, unspecified

    XVIII.R40-R46.R45   Symptoms and signs related to emotional state

    XXI.Z55-Z65.Z60.0   The problems associated with adaptation to lifestyle changes

    V.F20-F29.F20   Schizophrenia

    V.F20-F29.F25   Schizoaffective disorder

    V.F30-F39.F39   Mood disturbance [affective], unspecified

    V.F40-F48.F44   Dissociative [conversion] disorders

    V.F60-F69.F60   Specific personality disorders

    VI.G40-G47.G40.9   Epilepsy, unspecified

    XVIII.R40-R46.R45.1   Anxiety and Excitement

    Contraindications:
    • Hypersensitivity,
    • Closed-angle glaucoma,
    • Diseases of the prostate
    • Toxic agranulocytosis (in the anamnesis)
    • Porphyria in history
    • Simultaneous use with dopaminergic agonists (levodopa, amantadine, apomorphine, bromocriptine and others, except for their use in patients with Parkinson's disease)
    • Acute vascular insufficiency (collapse), heart failure
    • Acute poisoning with substances depressing the central nervous system
    • Coma
    • Pheochromocytoma
    • Erba-Goldflem disease
    • Children under 3 years old
    Carefully:
    • Diseases of the cardiovascular system (especially - ventricular arrhythmias, since the drug extends the interval of QT)
    • Renal and / or hepatic insufficiency (the metabolism of the drug decreases, the risk of its accumulation in the body increases)
    • Elderly age (due to excessive hypotensive and sedative effect, extrapyramidal disorders, paralytic intestinal obstruction, urinary retention on the background of diseases of the prostate gland)
    • Dementia in old age (risk of stroke)
    • In patients with risk factors for stroke, thromboembolism
    • Epilepsy (drug reduces the threshold of convulsive activity)
    • Parkinson's disease
    • Hyperthyroidism (increased risk of hyperthyroidism)
    • Breast cancer (increasing prolactin in the blood can cause disease progression)
    Pregnancy and lactation:

    Recommendations for FDA - Category C.

    The appointment of pericyazine is possible in pregnancy, but each time it is necessary to compare the benefits for the mother with the risk for the fetus.

    Due to the lack of data on the penetration of the drug into breast milk, its use during breast-feeding is not recommended.

    Dosing and Administration:

    Capsules of 10 mg are intended for ingestion by adults, 4% solution for oral administration to children.

    The daily dose for adults is 30 to 100 mg.

    The maximum daily dose is 200 mg.

    The daily dose should be divided into 2 or 3 doses and most of the dose should be taken in the evening.

    For children, the daily dose is calculated per kg of body weight: 0.1-0.5 mg / kg per day.

    For treatment of elderly patients, doses are reduced by 2-4 times.

    Side effects:
    • Hypotension
    • Tachycardia
    • Apathy
    • Inhibition of respiration
    • Bloating, constipation, intestinal obstruction
    • Extrapyramidal disorders - muscle hypertonus, tremor, akathisia
    • Sedation or drowsiness
    • Malignant neuroleptic syndrome
    • Hyperprolactinemia
    • Allergic reactions
    • Photosensitivity, skin sensitization
    Overdose:

    Symptoms: depression of the central nervous system from drowsiness to coma with areflexia, lowering of arterial pressure, tachycardia, arrhythmias, hypothermia, tremor, rigidity of muscles, convulsions, cyanosis, apnea.

    Treatment: gastric lavage, reception of activated charcoal, symptomatic therapy. There is no specific antidote.

    Interaction:

    Contraindicated the use of periciazin with dopaminergic agonists in patients without Parkinson's disease (levodopa, amantadine, apomorphine, bromocriptine, cabergoline, entacapone, lisuride, pergolide, piribedil, pramipexole, quinagolide, ropinirole), since there is a mutual antagonism of these drugs.

    If patients with Parkinson's disease need treatment with neuroleptics, then first the dopaminergic agonists should be canceled with a gradual decrease in doses.

    The use of alcohol with periciazine potentiates the sedative effect of the latter.

    Pericyzazine reduces the effectiveness of amphetamine, clonidine, guanethidine.

    Co-administration with sultopride increases the risk of developing ventricular arrhythmias (in particular, ventricular fibrillation).

    Simultaneous use of periciazine with drugs that extend the QT interval with thiazide diuretics increases the risk of arrhythmias.

    Joint use with antihypertensive drugs increases the hypotensive effect, sometimes leading to orthostatic hypotension.

    Simultaneous use of pericyazine with drugs that depress the central nervous system, increases the depression of the central nervous system, increases the risk of respiratory depression.

    The use of tricyclic antidepressants, MAO inhibitors, and maprotilin increases the risk of developing a malignant neuroleptic syndrome.

    The appointment together with atropine and other anticholinergics leads to cumulation of undesirable effects (dry mouth, constipation, urinary retention, heat stroke).

    Simultaneous use with lithium salts intensifies extrapyramidal disorders.

    Pericyzazin reduces the effects of alpha and beta-adrenostimulants (epinephrine, ephedrine).

    Periciazin reduces the emetic action of apomorphine, strengthens its inhibitory effect on the central nervous system.

    Simultaneous use with hypoglycemic agents reduces their hypoglycemic effect.

    Pericyzazin reduces the effect of funds that reduce appetite.

    Special instructions:

    During treatment, control of the blood composition is necessary (leukopenia and agranulocytosis may develop).

    In case of unexplained sudden rise in body temperature, treatment with the drug should be discontinued.

    During treatment, alcohol is not allowed.

    In case of abdominal distension and pain in the abdominal cavity, paralytic intestinal obstruction should be excluded.

    The abolition of the drug used in high doses should be carried out gradually.

    In connection with the possibility of photosensitization to patients receiving pericyazine, direct sunlight should be avoided.

    Drivers of vehicles and people working with potentially dangerous mechanisms should be careful, as the drug causes drowsiness and reduces the speed of psychomotor reactions.

    Instructions
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