pharmachologic effect
Antipsychotic drug (neuroleptic), piperazine derivative of phenothiazine. It is believed that the antipsychotic effect of phenothiazines is due to the blockade of postsynaptic dopamine receptors in the mesolimbic structures of the brain. Perphenazine has a strong antiemetic effect, the central mechanism of which is associated with inhibition or blockade of dopamine D2 receptors in the chemoreceptor trigger zone of the cerebellum, and the peripheral mechanism is associated with blockade of the vagus nerve in the gastrointestinal tract. Has alpha-adrenergic blocking activity. Anticholinergic activity and sedation may occur from weak to moderate intensity, the hypotensive effect is weak. Has a pronounced extrapyramidal effect. The antiemetic effect may be enhanced by anticholinergic and sedative properties. Has a muscle-relaxing effect.
Pharmacodynamics and pharmacokinetics
The drug affects the central nervous system. This is an antipsychotic drug that has a wide spectrum of action. It has antipsychotic , antiemetic and cataleptogenic effects. In addition, the drug has alpha-adrenolytic activity. Anticholinergic and sedative effects occur to a weak or moderate extent. The hypotensive and muscle-relaxing effects are weakly expressed. The neuroleptic effect is combined with a stimulating one .
The drug is also characterized by a selective effect on deficiency symptoms. Significant extrapyramidal abnormalities are possible.
Etaperazine is well absorbed from the gastrointestinal tract. Significant fluctuations in maximum plasma . Strong binding to plasma proteins. The drug is intensively broken down, mainly in the liver. Excreted through the kidneys and with bile.
Drug interactions
When used simultaneously with drugs that have a depressant effect on the central nervous system, with ethanol and ethanol-containing drugs, increased depression of the central nervous system and respiratory function is possible.
When used simultaneously with anticonvulsants, the threshold for convulsive readiness may be lowered; with drugs for the treatment of hyperthyroidism - the risk of developing agranulocytosis increases.
When used simultaneously with drugs that cause extrapyramidal reactions, an increase in the frequency and severity of extrapyramidal disorders is possible.
When used simultaneously with drugs that cause arterial hypotension, severe orthostatic hypotension is possible.
When used simultaneously with drugs that have anticholinergic effects, their anticholinergic effects may be enhanced, while the antipsychotic effect of the antipsychotic may decrease.
When used simultaneously with tricyclic antidepressants, maprotiline, and MAO inhibitors, the risk of developing NMS increases.
With the simultaneous use of antacids, antiparkinsonian drugs, lithium salts, the absorption of phenothiazines is impaired.
With simultaneous use, it is possible to reduce the effect of amphetamines, levodopa, clonidine, guanethidine, epinephrine.
When used simultaneously with fluoxetine, the development of extrapyramidal symptoms and dystonia is possible.
With simultaneous use, the vasoconstrictor effect of ephedrine may be weakened.
Contraindications
The following contraindications to the use of this drug are known: progressive systemic diseases of the brain and spinal cord, cirrhosis , hemolytic jaundice , hematopoietic disorders, thromboembolic diseases, pregnancy , breastfeeding , hepatitis , nephritis , myxedema , decompensated heart disease , hypersensitivity to the active substance, late stages of bronchiectasis diseases .
Etaperazin
Elderly patients with dementia-related psychosis treated with antipsychotic drugs have an increased risk of death.
Extrapyramidal disorders occur more often when taking high doses. Tardive dyskinesia occurs more often in older patients, especially women, while dystonia occurs more often in younger people. If signs or symptoms of tardive dyskinesia occur, consider discontinuing antipsychotic treatment (however, some patients may require continued treatment despite the presence of the syndrome).
Perphenazine may lower the seizure threshold, so caution should be exercised when using the drug in patients with a predisposition to seizure disorders and during alcohol withdrawal. With simultaneous treatment with perphenazine and anticonvulsants, an increase in the dose of the latter may be required.
During therapy with perphenazine, alcohol intake should be avoided, because Additive effects and hypotension may occur. The risk of suicide and the risk of antipsychotic overdose may be increased in patients who abuse alcohol during treatment due to the potentiation of the depressive effect of the drug on the central nervous system.
Caution should be exercised when prescribing the drug to patients with depression. The possibility of suicide in such patients remains during treatment, so it is necessary to exclude them from access to a large number of medications during treatment until complete remission occurs.
Perphenazine should be used with caution in patients with a history of serious side effects from other phenothiazines. Some of the adverse reactions of perphenazine occur more often when taking high doses. Perphenazine should be used with great caution in persons exposed to heat or cold because Phenothiazine derivatives inhibit the temperature regulation mechanism and, depending on the ambient temperature, can lead to hyperthermia and heat stroke or hypothermia and respiratory failure. A significant increase in body temperature can be caused by individual hypersensitivity. If hyperthermia occurs, treatment should be discontinued immediately. Perphenazine increases the body's sensitivity to sunlight. It is recommended to use sunscreen, especially if patients have fair skin, and wear protective clothing when outdoors, as well as avoid prolonged exposure to the sun, tanning beds, and the use of ultraviolet lamps.
Perphenazine should be used with caution in patients suffering from respiratory disorders due to the possible development of acute pulmonary infection, as well as in chronic respiratory diseases such as bronchial asthma or emphysema.
Antipsychotic drugs increase the concentration of prolactin in the blood, which persists with long-term use. Symptoms may include breast enlargement, dysmenorrhea, decreased libido, or nipple discharge.
Caution should be exercised when prescribing the drug to patients receiving atropine or similar drugs, as well as those who have contact with phosphorus-containing insecticides (an additive anticholinergic effect is possible).
During treatment, liver and kidney functions (with long-term therapy), peripheral blood patterns, and prothrombin index should be monitored. If signs or symptoms of blood dyscrasia occur, treatment should be discontinued and appropriate therapy instituted. Treatment should also be stopped if there are abnormalities in liver tests or if the blood urea nitrogen level is abnormal. Most cases of agranulocytosis were observed between 4 and 10 weeks of therapy. During this period, patients should be especially careful to monitor for sore throat or symptoms of infection. If the number of leukocytes decreases significantly, the drug should be discontinued and appropriate therapy should be started.
Jaundice that develops (rarely) during treatment (between 2 and 4 weeks of therapy) is usually considered a hypersensitivity reaction. In this case, the clinical picture is similar to that of infectious hepatitis, but the results of liver function tests are characteristic of obstructive jaundice. It is usually reversible, but cases of chronic jaundice have been reported.
Overdose
neuroleptic may occur . In such cases, the temperature often rises. coma is also possible .
The drug should be stopped immediately. Intravenous administration of Diazepam , nootropic drugs, dextrose solution , vitamins B and C is indicated. Treatment is symptomatic .
special instructions
Perphenazine should be used with caution in case of hypersensitivity to other phenothiazine drugs.
Phenothiazines are used with extreme caution in patients with pathological changes in the blood picture, liver dysfunction, alcohol intoxication, Reye's syndrome, as well as breast cancer, cardiovascular diseases, predisposition to the development of glaucoma, Parkinson's disease, gastric and duodenal ulcers , urinary retention, chronic respiratory diseases (especially in children), epileptic seizures, vomiting; in elderly patients (increased risk of excessive sedation and hypotensive effects), in depleted and weakened patients.
The development of tardive dyskinesia during the use of perphenazine is more likely in elderly patients, women and those with brain damage. Parkinsonian extrapyramidal reactions are more often observed in elderly patients, dystonic extrapyramidal reactions - in younger people. Symptoms of these disorders may occur in the first few days of treatment or after long-term therapy and may recur even after a single dose.
In case of hyperthermia, which is one of the elements of NMS, perphenazine should be discontinued immediately.
The simultaneous use of phenothiazines with absorbent antidiarrheals should be avoided.
During the treatment period, avoid drinking alcohol.
Recommendations for the use of perphenazine in children under 12 years of age have not been established. Children, especially those with acute illness, are more likely to develop extrapyramidal symptoms when using phenothiazines.
Impact on the ability to drive vehicles and operate machinery
It should be used with caution in patients engaged in potentially hazardous activities that require a high speed of psychomotor reactions.
Interaction
Suppression of the nervous and respiratory systems increases when combined with drugs that depress the nervous system, as well as ethanol-containing drugs and ethanol .
Combination with drugs that provoke extrapyramidal reactions increases the number and frequency of extrapyramidal disorders. Fluoxetine can also cause extrapyramidal symptoms and dystonia .
Anticonvulsants may lower the seizure threshold , and medications to treat hyperthyroidism , in turn, increase the likelihood of agranulocytosis .
Interaction with drugs that cause hypotension may cause orthostatic hypotension .
Combination with drugs that have anticholinergic effects may lead to an increase in anticholinergic effect, and the antipsychotic effect of the antipsychotic may be reduced.
Concomitant use of Etaperazine with MAO inhibitors , tricyclic antidepressants and Maprotiline increases the likelihood of developing NMS . And combination with antacids , lithium salts and antiparkinsonian drugs interferes with the absorption of phenothiazines .
Interactions with amphetamines , clonidine , Epinephrine , Levodopa and Guanethidine may reduce their effect.
Combination with Ephedrine may weaken its vasoconstrictor effect.
Side effects
From the central nervous system: drowsiness, akathisia, blurred vision, dystonic extrapyramidal reactions, parkinsonian extrapyramidal reactions.
From the liver: rarely - cholestatic jaundice.
From the hematopoietic system: rarely - agranulocytosis.
Metabolic disorders: rarely - heat stroke, melanosis.
Allergic reactions: rarely - skin rash accompanied by contact dermatitis.
Dermatological reactions: rarely - photosensitivity.
Effects due to anticholinergic action: possible dry mouth, accommodation disturbances, constipation, difficulty urinating.
Etaperazine price, where to buy
Tablets of 10 mg (50 pieces in a package) cost approximately 300 rubles. And the price of Etaperazine in 4 mg tablets (50 pieces in a package) is about 270 rubles.
- Online pharmacies in RussiaRussia
ZdravCity
- Etaperazine tablets p.p.o.
4 mg 50 pcs. JSC Tatkhimfarmpreparaty 344 rub. order - Etaperazine tablets p.p.o. 10 mg 50 pcs. JSC Tatkhimfarmpreparaty
RUB 383 order
Dosage
For adults and children over 12 years of age, when taken orally, the daily dose is 4-80 mg. In the chronic course of the disease and in resistant cases, the daily dose can be increased to 150-400 mg. The frequency of administration and duration of treatment are determined individually.
For adults and children over 12 years of age, with intramuscular administration, a single dose is 5-10 mg. For intravenous administration, a single dose is 1 mg.
Maximum doses: adults and children over 12 years of age with intramuscular administration - 15-30 mg/day, with intravenous administration - 5 mg/day.
