Etaperazine, 4 mg 50 pcs.

Perphenazine is an antipsychotic (neuroleptic), piperazine derivative of phenothiazine, which action is due to blockade of postsynaptic dopamine receptors in the mesolimbic structures of the brain.

Perphenazine has a strong antiemetic effect whose central mechanism is related to inhibition or blockade of dopamine D₂ receptors in the cerebellar chemoreceptor trigger zone and peripheral to blockade of the vagus nerve in the GI tract. It has alpha-adrenoblocking activity.

The anticholinergic activity and sedative effect may be of mild to moderate intensity, the hypotensive effect is weakly expressed.

It has a pronounced extrapyramidal effect. The antiemetic effect may be enhanced by anticholinergic and sedative properties. It has a muscular relaxant effect.

Indications

Psychotic disorders, especially with hyperactivity and agitation, schizophrenia; neuroses accompanied by fear and tension; nausea and vomiting of various etiologies; skin itching.

Pharmacological effect

ETAPERAZINE is an antipsychotic drug (neuroleptic), a piperazine derivative of phenothiazine, the action of which 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 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.

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.

Active ingredient

Perphenazine

Composition

Active ingredient:

perphenazine 4 mg

Contraindications

Cirrhosis, myxedema, progressive systemic diseases of the brain and spinal cord, decompensated heart disease, hepatitis, hemolytic jaundice, nephritis, hematopoietic disorders, thromboembolic diseases, late stages of bronchiectasis, pregnancy, lactation, hypersensitivity to perphenazine.

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.

Interaction

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, extrapyramidal symptoms and dystonia may develop.

With simultaneous use, the vasoconstrictor effect of ephedrine may be weakened.

Storage conditions

In a dry place, protected from light

Shelf life

3 years

Manufacturer

Tatchimpharmpreparaty, Russia