Etaperazine

Etaperazine is a drug from the pharmacological group of neuroleptics and belongs to antipsychotic drugs .

The active component of the drug is perphenazine, which, when entering the body, inhibits or completely blocks certain receptors in the cerebellum and in the nerve of the gastrointestinal tract.

Comparing Etaperazine with other drugs of similar action, it should be noted that it is more active, but at the same time inhibits the functioning of the central nervous system to a lesser extent.

In addition, this drug is less toxic than some of its analogues.

The practice of using Etaperazine shows that this drug is effective for the treatment of psychosis, psychopathy, and other mental disorders.

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.

ETAPERAZINE

(
Aethaperazinum
; synonym:
Chlorpiprozine, Decentan, Fentazin, Neuropax, Perphenan, Perphenazini Hydrochloridum, Perphenazine Hydrochloride, Trilafon, Trilifan,
etc.; list B) is a neuroleptic and antiemetic drug. 2-Chloro-10-{3-[1-(β-hydroxyethyl)-piperazinyl-4] - propyl }-phenothiazine dihydrochloride; C21H26ClN3OS • 2HCl:

White or white with a barely noticeable grayish tint crystalline powder. Easily soluble in water, slightly soluble in alcohol, practically insoluble in ether and chloroform. Hygroscopic. Under the influence of light, powder and aqueous solutions decompose; t°melt 217-223°; molecular weight (mass) 476.9.

Etaperazine belongs to the neuroleptic drugs (see) of the phenothiazine series. In terms of structure and pharmacological properties, etaprazine belongs to the so-called piperazine group of phenothiazines (see), which also includes meterazine (see), triftazine (see), fluorophenazine (see) and thioproperazine. A feature of the drugs in this group is the combination of high neuroleptic and antiemetic activity with a pronounced effect on the striopallidal system of the brain, which is manifested by a high frequency of extrapyramidal disorders in patients (see Extrapyramidal system).

Etaperazine has a spectrum of neurotropic activity that is also characteristic of other drugs of the piperazine group of phenothiazines. In the experiment, etaperazine causes a state of lethargy in animals, a decrease in motor and orientation activity, catalepsy, and moderate EEG synchronization. In high doses, it has a muscle relaxing effect and impairs coordination of movements.

In terms of inhibition of conditioned defense reflexes, Etaparazine is 4-8 times superior to aminazine (see), and in terms of the severity of the antiemetic effect - 5-10 times, the sedative effect of Etaparazine is more pronounced. Like other drugs of the piperazine group of phenothiazines, etaprazine exhibits selective antagonism in relation to dopaminomimetic effects (motor agitation, stereotypy) caused by phenamine (see) and apomorinf (see). In terms of its ability to potentiate the narcotic effect of barbiturates, etaparazine is close to aminazine. The hypotensive and alpha-adrenergic blocking effect is expressed to a lesser extent in etaparazine. M-anticholinergic, antihistamine and antispasmodic properties are weakly expressed. Compared to chlorpromazines, etaparazine is less toxic.

Mechanism of action

Etaparazine, like other antipsychotics, is usually associated with their ability to interact with dopamine receptors of neurons in the mesolimbic and other brain systems. As a result of receptor blockade with long-term use of antipsychotics, an acceleration of the metabolic turnover of dopamine develops through a feedback mechanism.

In clinical settings, etaprazine exhibits high, broad-spectrum antipsychotic activity. Etaperazine is used to treat various forms of schizophrenia (see) and other mental illnesses, neuroses with symptoms of anxiety and emotional stress, vomiting of pregnant women and other conditions accompanied by vomiting and hiccups, as well as skin itching. Etaparazine is most often prescribed for schizophrenia. Indicated for patients who, along with delusions and hallucinations, experience motor retardation up to catatonic stupor and depressive phenomena.

Apply

etaparazine orally after meals. Treatment of psychosis begins with a dose of 0.004-0.01 g 1-2 times a day, gradually increasing it. For patients to whom antipsychotics are prescribed for the first time, the daily dose of etaprazine is 0.05-0.08 g. In the chronic course of the disease, the daily dose is 0.1-0.15 g; in some cases - 0.25-0.4 g. For maintenance therapy, etaprazine is prescribed at 0.01-0.06 g per day. As an antiemetic, etaprazine is used at a dose of 0.004-0.008 a 3-4 times a day.

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 .

Side effects

Perphenazine is usually better tolerated than aminazine: drowsiness, lethargy, and lethargy are less pronounced, but more often than aminazine it causes extrapyramidal disorders. It can also cause arterial hypotension, tachycardia, dyspepsia, intestinal and bladder atony, liver and kidney damage, amenorrhea, galactorrhea, decreased libido[2], priapism[3], depression[4], neuroleptic dysphoria, epileptiform seizures, blurred vision, deposition of opaque material in the cornea, lens, retina, pigmentary retinopathy, melanosis, photosensitivity of the skin, rash with contact dermatitis, lupus-like syndrome, prolongation of the QT interval, ventricular flutter and fibrillation, intestinal obstruction, agranulocytosis (in the first 6 months of taking the drug), leukopenia, thrombocytopenia, pneumonia (manifested by chest pain, shortness of breath; may be asymptomatic), cholestatic jaundice, impaired thermoregulation (heat stroke, hypothermia, neuroleptic malignant syndrome) [3], diabetes mellitus [5].

Perphenazine may impair the patient's ability to control moving machinery and the ability to drive a car[3].

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

As indicated in the instructions for Etaperazine, if intestinal obstruction and a brain tumor are suspected, the use of the drug is not advisable - since vomiting can mask the symptoms of poisoning and complicate diagnosis.

During treatment with Etaperazine, it is recommended to regularly monitor liver and kidney function, prothrombin index, peripheral blood, and also exercise caution when driving vehicles and engaging in activities that require quick reaction and increased concentration.

Reviews of Etaperazine mention the need to avoid skin contact with the liquid form of the drug in order to prevent the possible occurrence of contact dermatitis.

The drug is stored at a temperature not exceeding 20 degrees Celsius in a dark place out of reach of children. The shelf life of Etaperazine, subject to these conditions, is 3 years. The use of the medicinal product beyond the specified expiration date is prohibited.

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 of Etaperazine

Like most antipsychotic drugs, Etaperazine has a negative effect on various body systems:

the central nervous system as follows: causes dizziness, drowsiness, lethargy, slow reaction, apathy, and reluctance to do any activity. Muscle weakness, spasms, tremors, difficulty speaking, swallowing, and blurred vision may appear. In addition, in some cases, taking Etaperazine can cause anxiety, paranoid states, strange or nightmare dreams, and increase excitability.
Effect on the cardiovascular system: surges in blood pressure, tachycardia, arrhythmia, anemia, changes in heart rate, disruption of hematopoietic processes.
Impact on the digestive organs: nausea, vomiting, dyspeptic disorders, weight gain due to increased appetite, dry mouth, liver dysfunction, cholestatic hepatitis, intestinal atony.
Urinary system: frequent urge or, conversely, urinary retention, polyuria, impaired renal function, and in rare cases, urinary incontinence.
The drug can also cause allergic reactions in the form of rash, redness of the skin, dermatitis, fever, and swelling.
In addition , side effects from taking Etaperazine may include pale skin, increased intraocular pressure, difficulty breathing, menstrual irregularities and enlarged mammary glands in women, decreased libido and impaired ejaculation in men, increased or decreased blood sugar levels.

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.
10 mg 50 pcs. JSC Tatkhimfarmpreparaty RUR 388 order
Etaperazine tablets p.p.o. 4 mg 50 pcs. JSC Tatkhimfarmpreparaty
RUB 343 order