Treatment: acute and chronic schizophrenia; acute psychotic disorders with delusions, anxiety, hallucinations and symptoms of personality disintegration; catatonia; mania and psychomotor agitation.
Composition:
1 tabl contains 25 mg or 100 mg of perazine in the form of dimaleate (and 69.3 mg or 191.6 mg lactose, respectively).
Action:
A drug from the group of neuroleptics, a piperazine derivative of phenothiazine. Is an antagonist of dopaminergic D receptors1 and D2 in subcortical centers of the brain, hypothalamus and limbic system. It works antipsychotic. Peryzine also acts on cholinergic receptors, α1-renergic, histamine and serotonin. When taken orally, it is rapidly absorbed from the gastrointestinal tract. Absorption is reduced when co-administered with milk, coffee, tea or fruit juices. After administration of 100 mg of perazine, the maximum concentration in the blood is reached 1-4 hours after administration. It is bound to plasma proteins in 94-97%. It is metabolised mainly in the liver to inactive metabolites. Excreted in the urine (50%) and bile (50%). It penetrates into breast milk. T0,5 is 8-16 hours.
Contraindications:
Hypersensitivity to perazine, other antipsychotics from the group of phenothiazine derivatives or to any of the excipients. Severe damage to the bone marrow or blood cells. Malignant neuroleptic syndrome in an interview. Comatose states. Acute poisoning with hypnotics, opioids, other neuroleptics, sedatives, antidepressants or alcohol. Permacin-dependent tumors (due to increased prolactin secretion under the influence of perazine). Severe hepatic failure. Depression states. Pregnancy and breastfeeding.
Precautions:
Consider the usefulness of the treatment and be especially careful in the following cases: leukopenia and other hematopoietic disorders, epilepsy, glaucoma, prostatic hypertrophy, hepatic failure, advanced ischemic heart disease, myocardial infarction, orthostatic hypotension, severe hypotension, urinary disorders, disease Parkinson's, pyloric stenosis, extrapyramidal system dysfunction, dyskinesias, myasthenia gravis, active peptic ulcer disease, hyperthyroidism, adrenal pheochromocytoma, acute anemia, breast cancer. At the beginning of perazine treatment, a full blood count is recommended. If fever, infections or nosebleeds occur, a haematological test should be performed immediately. Blood tests should be performed weekly during the first 4 months of perazine treatment and during long-term treatment - every 6 months. In the case of a significant reduction in the number of leukocytes (below 3,000 cells / mm)3), and in the case of changes in peripheral blood smears, treatment with perazine should be discontinued and another drug should be used. Liver function tests should be performed at the beginning and after 6 months of treatment. In the case of liver dysfunction, the dose should be reduced accordingly. Caution should be exercised in patients with renal insufficiency because the phenothiazine derivatives may cause hypotension. In diabetic patients, continuous monitoring of blood Glucose is required during treatment with perazine. During treatment with perazine, ECG monitoring should be performed in elderly patients or patients with heart disease or heart defects. Caution should be exercised in patients with organic brain injury, cerebrovascular disease and depression (worsening of depressive symptoms may occur). In the case of diseases of the basal ganglia (eg Parkinson's disease), perazine can only be used in exceptional cases, and should be discontinued if symptoms increase. Elderly patients are more likely to have extrapyramidal symptoms, the incidence of tardive dyskinesias increases, the sedative effect is stronger and the orthostatic hypotension is more common. In patients with convulsive seizures, perazine increases the tendency to seizures. The risk of seizures is greater if the doses are changed too quickly. Epilepsy does not exclude the administration of neuroleptics from psychiatric indications when antiepileptic therapy is continued.In the case of neuroleptic malignant syndrome, the use of neuroleptics may endanger the patient's life - immediate discontinuation of the drug, prevention of hyperthermia by cooling, treatment of water and electrolyte disturbances, symptoms of circulatory failure, respiratory and renal failure is recommended. In the case of skin lesions (eg rashes), a supplemental antiallergic treatment usually allows for continued treatment with neuroleptics. Avoid intense sunlight (including tanning beds and phototherapy) during treatment with perazin, and reduce the sensitivity to light using protective creams with the content of filters against UV radiation. During treatment with perazine, the patient should not consume preparations containing alcohol. The preparation contains lactose - should not be used in patients with rare hereditary galactose intolerance, lactase deficiency (Lapp type) or malabsorption of glucose-galactose.
Pregnancy and lactation:
The drug is contraindicated during pregnancy and breastfeeding.
Side effects:
Cardiac disorders. Very common: changes in the ECG (of varying severity, proportional to the doses used, are transient).Blood and lymphatic system disorders. Occasionally: leukopenia, eosinophilia and granulocytopenia. Very rare: thrombocytopenia, aplastic anemia and agranulocytosis.Nervous system disorders. In individual cases: a neuroleptic malignant syndrome (characterized by 40st.C fever and muscle stiffness, moreover an increase in myoglobin concentration and CK activity in the blood). So far, there have been no reports of the onset of neuroleptic syndrome after perazine treatment.Extrapyramidal symptoms. During the first few days of treatment with perazine, acute dyskinesia may occur, characterized by paroxysmal head movements, stiff neck, lockjaw, spasms of the facial muscles and the muscles of the tongue. These movements are less often involving larger muscle groups. Sometimes "eye attacks" are observed, and swallowing is difficult. Acute dyskinesias occur in about 1% of people treated with perazine. It is recommended to reduce the dose of perazine or the use of anticholinergics. In patients treated with perazine for a long time (many months), late dyskinesias have not been observed at the time of use. The possibility of tardive dyskinesia exists in patients after discontinuation of perazine treatment, more often in the elderly and in women. These changes may be transient. Patients treated with high doses for a long time may experience akathisia, which is often accompanied by depression. In the early period of treatment with perazine (most often 5-30 days of treatment) may occur drug-induced Parkinson syndrome (parkinsonism), which is clinically manifested by increased extrapyramidal skeletal muscle tone, slowing of movement, slight muscular tremor, usually not very strong. The syndrome is more common in women than in men and more often in older people than younger. Reduction of perazine dose and administration of cholinolytic medicinal products is recommended. Avoid urinary incontinence during perazine treatment.Eye disorders. There may be: blurred vision and changes in intraocular pressure. Long-term therapy with high doses of perazine may result in changes in eye pigmentation.Respiratory, thoracic and mediastinal disorders. Long-term administration of Perazine may lead to impaired respiratory function. Nasal hyperaemia was observed when using high doses.Gastrointestinal disorders. During high doses, constipation, dry mouth, nausea were observed. Isolated cases of necrotic enteritis and intrahepatic cholestasis.Renal and urinary disorders. Rare: urinary retention.Skin and subcutaneous tissue disorders. Occasional: allergic skin reactions. An increased skin reaction after insolation was sometimes observed. Strong perspiration occurs during treatment with perazine. One case of lupus erythematosus has been reported.Endocrine disorders. The most common side effects during perazine treatment include mylotox due to increased prolactin secretion. This symptom appears temporarily in 10% of treated women and depends on the size of the dose. Menstrual disorders may also appear, and in men, gynecomastia. There are also cases of weight gain.Vascular disorders. Most often: orthostatic decrease in blood pressure and arrhythmia. The reduction in blood pressure occurs especially at the beginning of treatment when using higher doses. These symptoms occur in about 15% of patients.Hepatobiliary disorders. Asymptomatic increase in the activity of at least one of the liver enzymes. Rarely: acute hepatitis. Very rare: severe hepatic impairment.Reproductive system and breast disorders. Sexual dysfunction may occur: erectile dysfunction and decreased sex drive.Mental disorders: sleep disturbance, confusion, general anxiety, increased incidence of dreams or nightmares, confusion and dementia. In addition, depression may occur, which usually occurs after acute psychoses. Drug-induced depression may resolve after a dose reduction of perazine, but a change of drug is sometimes required. Cases of delirium and confusional state have been observed with the use of perazine with other CNS agents. Dose reduction usually causes improvement.Diagnostic tests. When using medium and large doses of perazine, the cases of glucose tolerance tests are quite common.
Dosage:
Orally.Acute psychotic disorders, catatonia, psychomotor agitation: in the initial period of treatment of acute psychoses with states of psychomotor arousal and mania symptoms - once 50-150 mg. The maintenance dose for outpatients is up to 300 mg daily in divided doses. Maintenance dose for hospitalized patients - 200-600 mg daily in divided doses, in justified cases the dose may be increased to 800 mg daily.Chronic schizophrenia: 75-600 mg daily in 2 or 3 divided doses. Patients undergoing outpatient treatment should start treatment at a lower dose, then the dose should be gradually increased until the desired effect is obtained. In hospitalized patients, treatment should start at higher doses in order to achieve a rapid therapeutic effect. Urgent dose changes are not recommended as this increases the risk of side effects. The maximum antipsychotic effect occurs after 1-3 weeks of treatment. After administering the optimal dose to the patient for a longer time, it should be gradually reduced to the lowest therapeutic dose.Withdrawing the treatment. Treatment of psychotic disorders is long-lasting. If a satisfactory improvement is obtained, too short a dose reduction is not recommended. Doses should be reduced gradually over several to several months. The doctor's decision to stop treatment should be based on clinical experience, taking into account the current course of the disease and the patient's condition.Special groups of patients. There is no need to change the dosage in renal failure. Patients with hepatic impairment should receive half the normal dose and discontinuation of the drug in severe hepatic insufficiency. Elderly patients are recommended to take half the normal dose; such dosing generally provides the desired curative effect. Due to the lack of sufficient data to assess the safety of the drug should not be used in patients under 16 years of age.