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 in hyperactivity and agitation, schizophrenia; neurosis accompanied by fear, tension; nausea and vomiting of various etiologies; skin itching.

Active ingredient

Composition

Active substance:

Perphenazine 4 mg

How to take, the dosage

For adults and children over 12 years old 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 the duration of treatment are determined individually.

Interaction

Concomitant use with drugs with CNS depressant effect, with ethanol, ethanol-containing drugs may increase CNS and respiratory function depression.

In concomitant use with anticonvulsants, decreased seizure threshold may be observed; with agents for treatment of hyperthyroidism – the risk of agranulocytosis increases.

Concomitant use with drugs that cause extrapyramidal reactions may increase the frequency and severity of extrapyramidal disorders.

When used concomitantly with drugs causing arterial hypotension, pronounced orthostatic hypotension is possible.

Concomitant use with agents having anticholinergic effects may increase their anticholinergic effects, and the antipsychotic effect of the neuroleptic may decrease.

Concomitant use with tricyclic antidepressants, maprotiline, MAO inhibitors increases the risk of MNS.

The concomitant use of antacids, anti-Parkinsonian drugs, lithium salts impairs absorption of phenothiazines.

Concomitant use may decrease the effect of amphetamines, levodopa, clonidine, guanethidine, epinephrine.

Concomitant use with fluoxetine may result in extrapyramidal symptoms and dystonia.

The vasoconstrictor effect of ephedrine may be impaired when used concomitantly.

Special Instructions

Perfenazine is used with caution in hypersensitivity to other phenothiazine drugs.

. Phenothiazines are used with particular caution in patients with abnormal blood picture changes, liver dysfunction, alcohol intoxication, Reye syndrome, as well as in breast cancer, cardiovascular diseases, predisposition to glaucoma, Parkinson’s disease, gastric and duodenal ulcer, urinary retention, chronic respiratory diseases (especially in children), epileptic seizures, vomiting In elderly patients (increased risk of excessive sedation and hypotensive effect), in emaciated and weakened patients.

The development of tardive dyskinesia against the background of perphenazine use is more likely in elderly patients, women and in brain damage. Parkinsonian extrapyramidal reactions are more frequently observed in elderly patients, dystonic extrapyramidal reactions – in younger people. Symptoms of these disorders may be noted in the first few days of treatment or after prolonged therapy and may recur even after a single dose.

In the event of hyperthermia, which is an element of MNS, perphenazine should be stopped immediately.

The concomitant use of phenothiazines with adsorptive antidiarrheals should be avoided.

Alcohol should be avoided during treatment.

There are no recommendations for the use of perphenazine in children under 12 years of age. In children, especially those with acute illnesses, the use of phenothiazines is more likely to cause extrapyramidal symptoms.

Impact on driving and operating machinery

Perphenazine should be used with caution in patients engaged in potentially hazardous activities requiring high psychomotor reaction speed.

Contraindications

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

Side effects

CNS disorders: somnolence, akathisia, blurred vision, dystonic extrapyramidal reactions, parkinsonian extrapyramidal reactions.

Hepatic disorders: rarely cholestatic jaundice.

Hematopoietic system: rare – agranulocytosis.

Metabolism: rare – heat stroke, melanosis.

Allergic reactions: rare – skin rash accompanied by contact dermatitis.

Dermatological reactions: rarely – photosensitization.

The effects due to anticholinergic action: dry mouth, accommodation disorders, constipation, difficulty in urination are possible.