Etaperazin: instructions for use of tablets. Antipsychotic drug Etaperazin - instructions for use and reviews of doctors Etaperazin side effects

Etaperazine is a broad-spectrum antipsychotic used to treat neurosis, emotional disorders, and mental illness.

Active substance

Perphenazine (Perphenazine).

Release form and composition

Etaperazine is available as film-coated tablets. The drug is sold in 10, 50 or 2400 tablets per pack.

Indications for use

Etaperazine is prescribed for the treatment of mental and emotional disorders, involutional and exogenous organic psychoses, neuroses (fear, tension) and psychopathic conditions.

In therapeutic and surgical practice, the drug is used as a sedative: with indomitable vomiting in pregnant women, vomiting after operations on the abdominal organs and vomiting provoked by chemotherapy and X-ray therapy.

Contraindications

The drug should not be prescribed for severe cardiovascular diseases, endocarditis, progressive diseases of the brain and spinal cord, severe CNS depression, coma, as well as children under 12 years of age.

Etaperazine is used with caution in the following diseases and conditions:

• stomach ulcer and 12 duodenal ulcer;
• mammary cancer;
• pathological changes in the hematopoietic system;
• Parkinson's disease;
• liver or kidney failure;
• Reye's syndrome;
• prostatic hyperplasia;
• cachexia;
• angle-closure glaucoma;
• alcoholism;
• vomiting provoked by an overdose of other drugs;
• elderly age.

Instructions for use Etaperazine (method and dosage)

Etaperazine tablets are taken orally.

For adults and children over 12 years old, 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 admission and the duration of the course of therapy are set individually.

A dose of 2-4 mg is prescribed for vomiting in obstetric, therapeutic and surgical practice. It is usually recommended to take tablets 3 to 4 times a day.

Side effects

Sometimes taking Etaperazine causes the following side effects:

• on the part of the cardiovascular system: heart rhythm disturbance, lowering blood pressure, tachycardia, ECG changes;
• on the part of the gastrointestinal tract: nausea, loss of appetite, abdominal pain, atony of the intestines and bladder, vomiting;
• allergic reactions: skin rash, photosensitivity, contact dermatitis, angioedema;
• other effects: dry mouth, constipation, difficulty urinating, disturbances of accommodation.

Etaperazine can cause such undesirable reactions of the body as extrapyramidal disorders (trembling in the limbs, impaired coordination of movements and a decrease in their volume), lethargy, drowsiness, decreased motivational activity, mental retardation, depression, akathisia, blurred vision and autonomic disorders.

Overdose

An overdose of the drug may be accompanied by the development of neuroleptic reactions and impaired consciousness. Treatment in this case includes: intravenous administration of a dextrose solution, diazepam, vitamins C and B, nootropic drugs, as well as symptomatic therapy.

Analogues

Analogues according to the ATX code: none.

Medicines with a similar mechanism of action (coincidence of the ATC code of the 4th level): Perphenazine.

Do not make the decision to change the drug yourself, consult your doctor.

pharmachologic effect

Etaperazine is an antipsychotic drug derived from phenothiazine. It has sedative, antiemetic, antiallergic, muscle relaxant, weak hypotensive and anticholinergic effects. The effectiveness of the drug is due to the blockade of D2 receptors of the mesolimbic and mesocortical systems.

The pronounced antipsychotic effect of Etaperazine develops 3-7 days after the start of treatment with the drug and reaches its maximum after 2-6 months of its systematic use.

special instructions

If a brain tumor or intestinal obstruction is suspected, the use of this drug is not advisable, since vomiting can mask signs of poisoning and make diagnosis difficult.

During the course of treatment with Etaperazine, patients are advised to regularly monitor the functionality of the kidneys and liver, monitor the prothrombin index and the state of peripheral blood. In addition, during treatment with the drug, maximum caution should be exercised when driving.

During pregnancy and breastfeeding

The drug should not be taken during pregnancy and lactation.

In childhood

The safety of Etaperzine in patients under 12 years of age has not been established. In children, especially with acute forms of the disease, the use of drugs is more likely to develop extrapyramidal symptoms.

In old age

The drug is used with caution.

For impaired renal function

The drug is contraindicated in nephritis.

For impaired liver function

The drug is used with caution in violations of liver function. Do not take with hepatitis and cirrhosis.

drug interaction

Etaperazine enhances the effect of ethanol, analgesics, anxiolytics, hypnotics, drugs for general anesthesia, as well as the side effects of nephrotoxic and hepatotoxic drugs.

Perphenazine reduces the effectiveness of anorexigenic, antiepileptic drugs and the emetic action of apomorphine, increasing its inhibitory effect on the central nervous system.

The use of Etaperazine in conjunction with MAO inhibitors, maprotiline or tricyclic antidepressants may lead to increased anticholinergic and sedative effects; with lithium preparations - to extrapyramidal disorders and a decrease in the absorption of perphenazine in the gastrointestinal tract; with thiazide diuretics - to increase hyponatremia.

1 coated tablet contains:

Active substance:

perphenazine dihydrochloride

(Etaperazine) ...............................

Coated tablets, round, biconvex, dosage 4 mg - from light yellow to yellow, 6 mg - white, 10 mg - from yellowish green to green. Two layers are visible on the break of the tablets: at a dosage of 4 mg - the core is white or white with a grayish tint and the shell is from light yellow to yellow, 6 mg - the core is white or white with a grayish tint and the shell is white, 10 mg - the core is white or white with a grayish tint and a yellowish green to green shell.

Antipsychotic agent (neuroleptic), phenothiazine derivative; provides a sedative. antiallergic, weak anticholinergic, antiemetic, muscle relaxant. weak hypotensive and hypothermic action, eliminates hiccups. The antipsychotic effect is due to the blockade of dopamine D2 receptors of the mesolimbic and mesocortical systems. Blockade of D2-dopamine receptors in the polyneuronal synapses of the brain causes relief of the productive symptoms of psychosis: delusions and hallucinations. The antipsychotic effect is combined with a pronounced activating effect and a selective effect on syndromes that occur with lethargy, lethargy, apathy, primarily with substuporous phenomena, as well as on apatoabolic conditions. The sedative effect is due to the blockade of adrenoreceptors of the reticular formation of the brain stem. The severity of the sedative effect is from mild to moderate. It has a strong antiemetic effect. Antiemetic activity is associated with inhibition of the trigger zone of the vomiting center due to blockade of D2-dopamine receptors (central action) and a decrease in secretion and motility of the gastrointestinal tract (GIT) as a result of blockade of m-cholinergic receptors (peripheral action). Inhibition of dopamine receptors in the nigrostriatal zone and tubuloinfundibular region can cause extrapyramidal disorders and hyperprolactinemia. Peripheral alpha-adrenergic blocking effect is manifested by a decrease in blood pressure (hypotensive effect is weakly expressed), and H1 - antihistamine - anti-allergic effect. Hypothermic action - blockade of dopamine receptors of the hypothalamus. It is superior in antipsychotic activity. The antipsychotic effect develops after 4-7 days and reaches a maximum after 1.5-6 months (depending on the nature of the disease).

Like all phenothiazine derivatives, it is well absorbed in the gastrointestinal tract. Plasma protein binding - 90%. Bioavailability is 40% after oral administration. extensively metabolized in the liver by sulfoxylation, hydroxylation, dealkylation and glucuronidation to form a number of metabolites. Among patients taking phenothiazine derivatives, there are significant fluctuations in maximum plasma concentration. Hydroxylation of perphenazine is carried out with the participation of the CYP 2 D 6 isoenzyme of the cytochrome P450 enzyme system and, therefore, depends on genetic polymorphism, that is, from 7% to 10% of the population of the Caucasus and a small percentage of the population of Asia have low activity or its complete absence, so called "low" metabolism. In patients with a "low" CYP 2 D 6 metabolism, perphenazine will be absorbed more slowly and they will have higher plasma concentrations of etaperazine compared to patients with a normal or "high" metabolism.

After ingestion of perphenazine, its maximum concentration in plasma, according to studies, is observed after 1-3 hours, 7-hydroxyperphenazine - 2-4 hours. The mean equilibrium maximum concentrations (Cmax) are 984 pg/ml and 509 pg/ml, respectively. The time to reach equilibrium concentration (Css) when taken orally is 72 hours.

It is excreted mainly by the kidneys and partly with bile. The half-life of perphenazine does not depend on the dose and is 9-12 hours, 7-hydroxyperphenazine 10-19 hours.

Alcoholism (predisposition to hepatotoxic reactions); pathological changes in the blood; breast cancer (as a result of prolactin secretion induced by phenothiazine derivatives, the potential risk of disease progression and resistance to drugs prescribed to patients with endocrine and metabolic diseases and cytostatic drugs increases); angle-closure glaucoma; prostatic hyperplasia with clinical manifestations; mild to moderate renal or hepatic insufficiency; peptic ulcer of the stomach and duodenum 12 (during the period of exacerbation); diseases accompanied by an increased risk of thromboembolic complications; Parkinson's disease (extrapyramidal effects are enhanced); epilepsy; chronic diseases accompanied by respiratory failure (especially in children); Reye's syndrome (increased risk of hepatotoxicity in children and adolescents); cachexia; vomiting (the antiemetic effect of phenothiazine derivatives may mask vomiting associated with an overdose of other drugs); patients in the period of alcohol withdrawal; depression (the possibility of suicide remains); elderly age.

Perphenazine easily crosses the placental barrier and is rapidly excreted in breast milk, so the possibility of using the drug is determined by the doctor if the potential benefit to the mother outweighs the potential risk to the fetus or child.

Newborns whose mothers were taken at the end of pregnancy or during childbirth may experience signs of intoxication such as lethargy, tremors and excessive excitability. In addition, these newborns have a low Apgar score.

With prolonged treatment of the mother, or when using high doses, as well as in the case of prescribing the drug shortly before childbirth, it is reasonable to monitor the activity of the nervous system of the newborn.

Inside, after eating. Elderly patients may be taken at bedtime.

Doses are selected individually according to the severity of the condition.

Elderly, debilitated and debilitated patients usually require a lower initial dose.

Upon reaching the maximum therapeutic effect, the dose is gradually reduced to a maintenance dose.

Schizophrenia: adults not previously treated with antipsychotic drugs, the initial dose is 4-8 mg 3 times a day. Patients with a chronic course of the disease, if necessary, increase the dose to 64 mg / day. The duration of treatment depends on the patient's condition and the severity of side effects and is 1-4 months or more.

Severe nausea and vomiting:, adults as an antiemetic drug are prescribed 8-16 mg 2-4 times a day.

Not all of the following side effects have been reported with perphenazine. However, pharmacological similarity to other phenothiazine derivatives requires each to be reckoned with. Many of these side effects can be avoided by lowering the dose.

From the nervous system and sensory organs: extrapyramidal disorders (especially dystonic) - spasm of the muscles of the back and neck, face, tongue, tonic spasm of masticatory muscles, difficulty in speaking and swallowing, a feeling of stiffness in the throat, oculogeric crises, spasm and pain in the limbs, stiffness of the arms and legs, hyperreflexia, akathisia . parkinsonism, ataxia; drowsiness, lethargy, lethargy, muscle weakness, decreased motivation, dizziness, miosis, mydriasis, blurred vision, glaucoma, retinopathy pigmentosa, deposits in the lens and cornea, paradoxical reactions - exacerbation of psychotic symptoms, catalepsy, catatonic-like states, paranoid reactions, lethargy, lethargy , paradoxical arousal, anxiety, hyperactivity, nocturnal confusion, strange dreams, sleep disturbance. Their frequency and severity usually increase with increasing dose, but there is considerable individual variation in the propensity to develop such symptoms. Extrapyramidal symptoms are usually corrected by the simultaneous use of effective antiparkinsonian drugs or dose reduction. In some cases, however, these extrapyramidal reactions may persist after discontinuation of perphenazine treatment.

Tardive dyskinesia: rhythmic, involuntary movements of the tongue, face, mouth, and jaw (eg, tongue protrusion, puffing out of the cheeks, wrinkling of the mouth, chewing movements). Sometimes it can be accompanied by involuntary movements of the limbs. There is no effective treatment for tardive dyskinesia. There is evidence that worm-like tongue movements may be an early sign of the syndrome, and if treatment is stopped, this syndrome may not develop.

From the side of the cardiovascular system: increase and decrease in blood pressure. orthostatic hypotension, change in pulse rate, tachycardia (especially with an unexpected significant increase in dose), bradycardia, cardiac arrest, weakness and dizziness, arrhythmia, syncope, changes in the electrocardiogram, nonspecific (quinidine-like effect).

On the part of the blood (hematopoiesis, hemostasis): leukopenia, agranulocytosis, eosinophilia, hemolytic anemia, thrombopenic purpura, pancytopenia.

From the digestive tract: nausea, vomiting, diarrhea, constipation, anorexia, increased appetite and body weight, polyphagia, abdominal pain, dry mouth, increased salivation, liver damage (bile stasis), cholestatic hepatitis, jaundice.

Allergic reactions: skin rash, urticaria, erythema, eczema, exfoliative dermatitis, itching. hyperhidrosis, skin photosensitivity, bronchial asthma, fever, anaphylactoid reactions, laryngeal edema and angioedema, angioedema.

Other: pallor, perspiration, atony of the intestines and bladder, urinary retention. frequent urination or urinary incontinence, polyuria, nasal congestion, kidney damage, increased intraocular pressure, skin pigmentation, photophobia, unusual secretion of breast milk, breast enlargement and galactorrhea in women, gynecomastia in men, menstrual irregularities, amenorrhea, changes in libido, decreased ejaculation, syndrome of inappropriate secretion of antidiuretic hormone, false positive pregnancy test, hyperglycemia, hypoglycemia, glucosuria. peripheral edema, systemic lupus erythematosus, as a syndrome.