the product in the database has an inactive status
indications:
Treatment of psychotic states, including delusional. In small doses, the drug can be used to treat anxiety disorders. Treatment of nausea and vomiting in adults.
Composition:
1 tabl contains 2 mg, 4 mg or 8 mg of perfenazine.
Action:
Anxiolytic, antipsychotic and antiemetic drug affecting o.u.n. especially on the hypothalamus. Phenothiazines affect the central and autonomic nervous system and affect the various systems of the body. Their influence on o.u.n. causes sedation without causing drowsiness or anesthesia. These drugs block the conditional avoidance response and have an antiemetic effect. Perphenazine has a stronger effect on behavior than other phenothiazine derivatives, the side chain of which does not contain the piperazine group. Tolerability of drowsiness induced by fenothiazines, inhibition of conditional reflex avoidance and orthostatic hypotension may develop over days or weeks. There is usually no development of antipsychotic tolerance of these drugs. After oral administration, the drug is well absorbed from the gastrointestinal tract, 60-70% of the dose is quickly removed from the portal circulation, and intrahepatic circulation is very intensified. For this reason, less unchanged drug penetrates into the systemic circulation than after parenteral administration. After absorption, phenothiazines are rapidly distributed to all body tissues. These compounds have a high lipophilicity and to a large extent bind to membranes and proteins. A high concentration of unchanged drug was found in the brain; metabolites - mainly in the lungs, liver, kidneys and spleen. Phenothiazines are mainly metabolised in the liver by oxidation, hydroxylation, demethylation, sulphoxide formation and binding to glucuronic acid. Elimination from blood plasma may be faster than from tissues with a high fat content, mainly o.u.n. Elderly people, fetuses and newborns have a slower metabolism and excretion of this group's compounds. Phenothiazine metabolites are less pharmacologically active than parent compounds.
Contraindications:
Hypersensitivity to perphenazine or any of the excipients. Abnormal blood composition, bone marrow suppression or liver damage. Do not use in patients with coma or dementia patients and in patients receiving high doses of drugs that inhibit the activity o.u.n. (barbiturates, analgesics, antihistamines, drugs and alcohol). Do not use in patients with suspected or proven damage to subcortical structures of the brain, with damaged or intact hypothalamus. These patients may experience hyperthermia with a temperature above 40 degrees C; sometimes hyperthermia develops in 14-16 h after drug administration (treatment of hyperthermia may be helpful in cooling the body with ice and the use of antipyretics).
Precautions:
Particular care should be taken in patients with mitral regurgitation or with pheochromocytoma due to the risk of severe, acute hypotension. If hypotension develops after administration of perphenazine, epinephrine should not be given; if it is necessary to administer a vasoconstrictor, norepinephrine or phenylephrine can be used. Patients with pheochromocytoma may experience rebound hypertension. In susceptible patients, the drug may lower the seizure threshold - caution should be used in patients with alcohol withdrawal syndrome and patients with seizures. In patients treated with antiepileptic drugs, it may be necessary to increase the dose of these medicines when using perphenazine. The drug should be used with caution in patients with depression. The likelihood of suicide in depressed patients persists until a clear remission occurs. Patients with suicidal tendencies should not have access to larger amounts of the drug. The risk of suicide and the risk of overdose may increase in alcohol-abusing patients. The drug increases serum prolactin - caution is advised in patients with breast cancer.The antiemetic effect of perphenazine may mask the toxicity symptoms caused by the overdose of other drugs or hinder the diagnosis of diseases such as intestinal obstruction, Rey's syndrome, brain tumors and encephalopathies. In several patients who received phenotiazines after surgery, vomiting was observed (no causal relationship was proven). In patients receiving high doses of phenothiazines who are undergoing surgery, blood pressure should be carefully monitored (possible hypotension). In addition, it may be necessary to reduce the dose of drugs used for anesthesia or inhibiting o.u.n. The drug should be used very carefully in patients exposed to very high or very low temperatures, because phenothiazines inhibit the thermoregulatory mechanism. Depending on the ambient temperature, they may cause hyperthermia and heat stroke or hypothermia and respiratory distress syndrome. A significant increase in body temperature, which can not be explained in any other way, may suggest intolerance of perphenazine - the drug should be discontinued. Phenothiazines should be used with caution in patients with impaired renal function and in patients with impaired respiration caused by acute lung infections or chronic respiratory conditions such as severe asthma or emphysema. If it is suspected due to the drug's action on the cardiovascular system, the electrocardiogram of the heart should be performed. You should stop taking the medicine if you have liver or kidney problems. Especially between 4 and 10 weeks of treatment, patients should be carefully observed for haematological effects, sudden throat pain or other symptoms of infection. If the number of white blood cells is reduced and the interest formula shows a significant reduction in the number of granulocytes, the drug should be discontinued and appropriate treatment should be given. Slight reductions in the number of white blood cells is not the reason for stopping treatment. The safety and efficacy of this medicine has not been established in children under 12 years of age, therefore its use is not recommended in children. 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:
It can be used during pregnancy, breastfeeding and in women of childbearing age only when the potential benefits to the mother outweigh the possible risks to the fetus or breastfed child. It should not be given to pregnant women before delivery unless the potential benefits to the mother outweigh the possible risks to the child. In children of mothers treated with phenothiazines during pregnancy, extrapyramidal reactions were observed, including agitation, increased tension, opistotonus, tremors, increased reflexes, and unprecedented motor activity. In rare cases, movement disorders persisted for 3 to 12 months. In children of schizophrenic patients treated with phenothiazines, respiratory depression persisted for several days after delivery. In children of mothers treated with perphenazine during pregnancy, a congenital cataract occurred. Phenothiazines penetrate the placental barrier and easily enter the fetal bloodstream.
Side effects:
Not all of the side effects listed below were observed in the perception of perfenazine. However, due to the similarity of pharmacological action between different phenothiazine derivatives, these should be taken into account. In the case of piperazine derivatives (perfenazine belongs to this group) extrapyramidal symptoms are the most common, while others, for example sedation, jaundice, abnormal blood composition, convulsions and effects on the autonomic nervous system are less frequent. Cardiac disorders: tachycardia (especially in the case of a sudden increase in the dose), bradycardia, cardiac arrest; sporadically - cases of sudden death. In some cases, death was probably caused by cardiac arrest; in other cases, it was probably caused by asphyxia caused by inhibition of the cough reflex. Blood and lymphatic system disorders: agranulocytosis, eosinophilia, leukopenia, hemolytic anemia, thrombocytopenic purpura and pancytopenia. Most cases of agranulocytosis occur between 4 and 10 weeks of treatment. Nervous system disorders: extrapyramidal symptoms - dorsal tetanus (opistotonus), trismus, torticollis, hindquarters of the neck, pain and numbness of the lower limbs, restlessness, forced upward looking, hyperreflexia, dystonia including protrusion, discoloration, pain and circular movements tongue, tonic contraction of the masseter muscles, a feeling of squeezing the throat, indistinct speech, difficulty swallowing, akathisia, dyskinesia, parkinsonism and ataxia. In some cases, extrapyramidal symptoms may persist after termination of perfenazine therapy.Long-term dyskinesia may occur in some patients who have been treated for a long time or after treatment. Although the risk appears to be higher in elderly patients (especially in women) receiving high doses, tardive dyskinesia may also occur in men and in children. The symptoms persist for a long time and in some patients they seem to be imperishable. Although much less frequently than after long-term use, this syndrome may also occur after a relatively short treatment at low doses. If symptoms of dyskinesia occur, it is recommended to discontinue all antipsychotics. It may be necessary to resume treatment, increase the dose or change to another antipsychotic, symptoms may be masked. Minor language movements can be one of the first symptoms of this syndrome. If the treatment stops at this point, the full-blown syndrome may not develop. Neuroleptic malignant syndrome has been observed in patients treated with neuroleptics. If it occurs, stop taking neuroleptics immediately and use intensive supportive treatment if necessary. If the patient requires further antipsychotic treatment after healing, close monitoring of the patient is recommended because the neuroleptic malignant syndrome may recur. Other disturbances o.u.n.n .: dizziness, cerebral edema, convulsions especially in patients with EEG disorder or with such a history of disorder, headache, drowsiness (especially during the 1st and 2nd week of treatment). In neonates whose mothers used phenothiazines during pregnancy, hyperreflexia was observed. Uncommonly, a significant effect on the autonomic system has been observed in patients receiving less than 24 mg of perpentanone per day. Eye disorders: pupillary constriction, mydriasis, blurred vision, glaucoma, photophobia, ocular lesions in the form of deposits of fine particles in the cornea and the lens, which in more severe cases may develop into starry clouding of the lens; epithelial keratopathy, changes in the retina, pigmentary retinopathy. Respiratory, thoracic and mediastinal disorders: nasal congestion, asthma. Gastrointestinal disorders: dry mouth or excessive salivation, nausea, vomiting, retention of gastric contents, diarrhea, constipation, stooling. During treatment with phenothiazines, paralytic ileus may occur; in severe cases complications and death of the patient may occur. Paralytic intestinal obstruction is particularly dangerous in patients with mental illness who may not seek help in this condition. Renal and urinary disorders: urinary retention, frequent donation and urinary incontinence, bladder infection, polyuria, glycosuria. Skin and subcutaneous tissue disorders: urticaria, erythema, eczema, exfoliative dermatitis, pruritus, hypersensitivity to light, paleness, increased sweating; during long-term treatment may occur: skin discoloration, occurring mainly in places exposed to light. Musculoskeletal and connective tissue disorders: muscle weakness. Endocrine disorders: lactation, syndrome of abnormal secretion of antidiuretic hormone. Metabolism and nutrition disorders: increased appetite and weight gain, excessive appetite, anorexia, hyperglycaemia, hypoglycaemia. Vascular disorders: syncope, hypertension, orthostatic hypotension and changes in heart rate may occur sporadically. Occasionally, hypotensive effects may cause shock-like effects. General disorders and administration site conditions: fever, peripheral edema, inverse epinephrine effect, parotid edema (rare), hyperpyrexia. Immune system disorders: anaphylactoid reactions and laryngeal edema, lupus-like syndrome. Dye-nerve edema and contact dermatitis have been reported in medical personnel administering phenothiazines. In particularly rare cases, individual idiosyncrasy or hypersensitivity to phenothiazines may cause cerebral edema, circulatory collapse and death. Hepato-biliary disorders: liver damage (cholestasis). Jaundice usually occurs between the 2nd and 4th weeks of treatment and is referred to as a hypersensitivity reaction. Its incidence is low. The clinical picture is similar to infectious hepatitis, but with lab results showing congestive jaundice.It is usually transient, however, chronic jaundice has been observed. Reproductive system and breast disorders: galactorrhea, moderate, increased breast enlargement in women and gynecomastia in men after high doses, irregular menstrual cycle, amenorrhea, ejaculation inhibition. Mental disorders: changes in libido, behavioral side effects, paradoxical worsening of psychotic symptoms, catatonic-like conditions, paranoid reactions, lethargy, paradoxical arousal, anxiety, hyperactivity, night-time confusion, unusual dreams, insomnia. Diagnostic tests: disturbances in the composition of proteins in the cerebrospinal fluid, increased Glucose in the blood. In some patients receiving sedatives from the phenothiazines group, transient, non-specific ECG changes (quinidine-like effect) have been observed. ECG changes may occur, such as: prolongation of the QT interval with widening, flattening and beating of the T wave. Administration of higher doses may result in the reduction and reversal of the T wave. Laboratory results showing congestive jaundice. Phenothiazine metabolites may cause darkening of the urine, resulting in false positives for the presence of urobiligene, amylase, porphyrin, porphobilinogen and 5-hydroxyindoleacetic acid. Phenothiazines may increase the serum concentration associated with Iodine protein without clinical symptoms of hyperthyroidism. Because phenothiazines may reduce adrenal corticosteroid secretion due to decreased corticotropin release, per- fensin can affect the hypothalamic pituitary methapapile. The result of a pregnancy test in patients treated with phenothiazines, depending on the type of test, may be false positive or false negative.
Dosage:
Orally. Dosage should be selected individually and adjusted to the severity of the disease symptoms and response to treatment. As the incidence and severity of extrapyramidal symptoms increases with increasing dose, the lowest effective dose should be used. Extrapyramidal symptoms disappear after dose reduction, discontinuation of the preparation or administration of drugs used to treat Parkinson's disease. After obtaining the maximum therapeutic response, the dose can be gradually reduced until the lowest effective maintenance dose is reached. Periodically, the need for further treatment should be assessed. Anxiety disorders: 2 mg - 4 mg 3 times a day.Patients with psychosis treated in an outpatient setting: initially 4 mg - 8 mg 3 times a day. The dose should be reduced as soon as possible to the minimum effective dose.Patients hospitalized with psychosis: 8 mg - 16 mg 2 - 4 times a day. Avoid administration of more than 64 mg daily.Severe nausea or vomiting in adults: 8 mg - 16 mg a day, in divided doses. A dose of 24 mg per day may be administered sporadically. This dose should be reduced as soon as possible. Long-term administration of doses greater than 24 mg per day is possible only in hospitalized patients or patients under constant observation.