Etaperazin (Tablets) Instructions for Use

ATC Code

N05AB03 (Perphenazine)

Active Substance

Perphenazine (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Antipsychotic drug (neuroleptic)

Pharmacotherapeutic Group

Antipsychotic (neuroleptic) agent

Pharmacological Action

Antipsychotic agent (neuroleptic), a piperazine derivative of phenothiazine. It is believed that the antipsychotic action 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 the inhibition or blockade of dopamine D₂ receptors in the chemoreceptor trigger zone of the cerebellum, and the peripheral mechanism is associated with the blockade of the vagus nerve in the gastrointestinal tract.

It has alpha-adrenergic blocking activity. Anticholinergic activity and sedative effect can range from weak to moderate in 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 muscle relaxant effect.

Pharmacokinetics

Clinical data on the pharmacokinetics of perphenazine are limited.

Phenothiazines have high plasma protein binding. They are excreted mainly by the kidneys and partially with bile.

Indications

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

ICD codes

Dosage Regimen

Tablets

For adults and children over 12 years of age when taken orally, the daily dose is 4-80 mg. In 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 the course of treatment are set individually.

For adults and children over 12 years of age with intramuscular administration, a single dose is 5-10 mg. With intravenous administration, a single dose is 1 mg.

Maximum doses for adults and children over 12 years of age with intramuscular administration – 15-30 mg/day, with intravenous administration – 5 mg/day.

Adverse Reactions

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.

From metabolism rarely – heat stroke, melanosis.

Allergic reactions rarely – skin rash accompanied by contact dermatitis.

Dermatological reactions rarely – photosensitization.

Effects due to anticholinergic action dry mouth, accommodation disturbances, constipation, difficulty urinating may occur.

Contraindications

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

Use in Pregnancy and Lactation

Perphenazine is contraindicated for use during pregnancy and lactation.

Use in Hepatic Impairment

Contraindicated in cirrhosis, hepatitis. Phenothiazines should be used with particular caution in liver dysfunction.

Use in Renal Impairment

Contraindicated in nephritis.

Pediatric Use

Recommendations for the use of perphenazine in children under 12 years of age have not been established. In children, especially with acute illnesses, the development of extrapyramidal symptoms is more likely when using phenothiazines.

Geriatric Use

Phenothiazines should be used with particular caution in elderly patients (increased risk of excessive sedative and hypotensive effects).

In elderly patients, the development of tardive dyskinesia against the background of perphenazine use is possible, as well as parkinsonian extrapyramidal reactions. Symptoms of these disorders may be noted in the first few days of treatment or after long-term therapy and may recur even after a single dose.

Special Precautions

Perphenazine should be used with caution in case of hypersensitivity to other drugs of the phenothiazine series.

Phenothiazines should be used with particular caution in patients with pathological changes in the blood picture, in liver dysfunction, alcohol intoxication, Reye’s syndrome, as well as in 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 sedative and hypotensive effects), in debilitated and weakened patients.

The development of tardive dyskinesia against the background of perphenazine use is more likely in elderly patients, women, and with brain damage. Parkinsonian extrapyramidal reactions are more often 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 long-term therapy and may recur even after a single dose.

In case of hyperthermia, which is one of the elements of neuroleptic malignant syndrome (NMS), Perphenazine should be immediately discontinued.

Concomitant use of phenothiazines with adsorbent antidiarrheal agents should be avoided.

Do not consume alcohol during treatment.

Recommendations for the use of perphenazine in children under 12 years of age have not been established. In children, especially with acute illnesses, the development of extrapyramidal symptoms is more likely when using phenothiazines.

Effect on ability to drive vehicles and operate machinery

Should be used with caution in patients engaged in potentially hazardous activities requiring high speed of psychomotor reactions.

Drug Interactions

With simultaneous use with drugs that have a depressant effect on the central nervous system, with ethanol, ethanol-containing drugs, it is possible to enhance the depression of the central nervous system and respiratory function.

With simultaneous use with anticonvulsant drugs, a decrease in the seizure threshold is possible; with agents for the treatment of hyperthyroidism, the risk of developing agranulocytosis increases.

With simultaneous use with drugs that cause extrapyramidal reactions, an increase in the frequency and severity of extrapyramidal disorders is possible.

With simultaneous use with drugs that cause arterial hypotension, severe orthostatic hypotension is possible.

With simultaneous use with agents that have anticholinergic effects, their anticholinergic effects may be enhanced, while the antipsychotic effect of the neuroleptic may decrease.

With simultaneous use with tricyclic antidepressants, maprotiline, MAO inhibitors, the risk of developing neuroleptic malignant syndrome (NMS) increases.

With simultaneous use of antacids, antiparkinsonian drugs, lithium salts, the absorption of phenothiazines is impaired.

With simultaneous use, a decrease in the action of amphetamines, levodopa, clonidine, guanethidine, epinephrine is possible.

With simultaneous use with fluoxetine, the development of extrapyramidal symptoms and dystonia is possible.

With simultaneous use, a weakening of the vasoconstrictor effect of ephedrine is possible.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.