Normazidol (Tablets) Instructions for Use

ATC Code

N06AX (Other antidepressants)

Active Substance

Pirlindole (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Antidepressant – reversible MAO-A inhibitor

Pharmacotherapeutic Group

Antidepressant

Pharmacological Action

Pirlindole is an indole derivative with elements of structural similarity to serotonin and reserpine.

Pirlindole has pronounced antidepressant activity; a feature of its action is the presence of a thymoleptic effect with a balanced action (an activating effect in patients with apathetic, anergic depressions is combined with a sedative and anxiolytic effect in patients with agitated states).

It selectively inhibits MAO type A (short-term and fully reversible); blocks the deamination of serotonin and norepinephrine, and to a lesser extent, tyramine (which creates fewer prerequisites for the development of serotonin syndrome); partially inhibits the reuptake of monoamines.

It activates the processes of synaptic transmission of nerve impulses in the CNS. It weakens the depressive effects of reserpine, enhances the effect of the norepinephrine precursor – dihydroxyphenylalanine (L-dopa), stimulates adrenergic structures; potentiates the effects of the serotonin precursor – 5-hydroxytryptophan (stimulates serotonergic structures).

Unlike tricyclic antidepressants, it does not have anticholinergic action. It also has a nootropic effect, improving cognitive functions.

Pharmacokinetics

Pirlindole is almost completely absorbed from the gastrointestinal tract.

After a single dose, C_max of pirlindole in blood plasma is reached within 2-8 hours.

Pirlindole undergoes enterohepatic circulation. Elimination from blood plasma occurs in three phases. The absolute bioavailability is 20-30%.

Pirlindole is metabolized during the first pass through the liver. Plasma protein binding is 95%, terminal T_1/2 is 185 hours.

Pirlindole is almost completely metabolized, and only very small amounts are excreted unchanged in the urine. About 50-70% of metabolites are excreted in the urine, 25-45% in the bile through the intestines.

Indications

Manic-depressive psychosis, schizophrenia. Depressions of various origins, predominantly with psychomotor retardation and asthenic disorders, with anxious-depressive or anxious-delusional components. Involutional depression. Alcohol withdrawal syndrome. Alzheimer’s disease (as part of complex therapy).

ICD codes

Dosage Regimen

Administer orally with water.

Initiate treatment at a dose of 25-50 mg two to three times daily.

Titrate the dose gradually based on tolerance and clinical response.

Increase the dose by 25-50 mg every 5-7 days.

The standard therapeutic dose ranges from 150 mg to 300 mg per day, divided into two or three doses.

Do not exceed the maximum daily dose of 400 mg.

For elderly patients or those with hepatic impairment, use a lower initial dose and titrate more slowly.

In Alzheimer’s disease, use as part of a comprehensive therapeutic regimen.

For alcohol withdrawal syndrome, the duration of use is typically short-term.

Divide the total daily dose to minimize potential side effects.

The duration of treatment is determined by the treating physician based on the underlying condition.

Do not abruptly discontinue therapy; taper the dose under medical supervision.

Adverse Reactions

Rarely dry mouth, increased sweating, hand tremor, tachycardia, nausea, dizziness, allergic reactions.

Contraindications

Hypersensitivity to pirlindole, acute hepatitis, hematopoietic system diseases, use of MAO inhibitors.

Use in Pregnancy and Lactation

Use during pregnancy and breastfeeding is not recommended.

Use in Hepatic Impairment

Contraindicated for use in acute hepatitis.

Special Precautions

Pirlindole should not be used simultaneously with MAO inhibitors and for 2 weeks after their discontinuation.

The absence of a cholinoblocking action in pirlindole allows its use in patients with glaucoma and prostate adenoma.

Effect on the ability to drive vehicles and machinery

During the use of pirlindole, patients should exercise caution when driving vehicles and machinery, as well as when engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

Pirlindole should not be prescribed simultaneously with other MAO inhibitors, furazolidone, procarbazine, selegiline.

With simultaneous use of pirlindole, the effectiveness of epinephrine increases (due to antimonoamine oxidase activity).

Pirlindole is compatible with antipsychotic agents, anxiolytics.

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.