Relaxon (Tablets) Instructions for Use

Marketing Authorization Holder

Veropharm, JSC (Russia)

ATC Code

N05CF01 (Zopiclone)

Active Substance

Zopiclone (Rec.INN registered by WHO)

Dosage Form

Relaxon

Film-coated tablets, 7.5 mg: 5, 10, 15, 20, 30, or 40 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white, round, biconvex.

Excipients: microcrystalline cellulose, colloidal silicon dioxide (aerosil), lactose (milk sugar), sodium carboxymethyl starch (primogel), potato starch, magnesium stearate, povidone (polyvinylpyrrolidone), hypromellose, talc, macrogol 4000 (polyethylene glycol 4000), titanium dioxide.

5 pcs. – contour cell packs (1) – cardboard packs.
5 pcs. – contour cell packs (4) – cardboard packs.
5 pcs. – contour cell packs (2) – cardboard packs.
5 pcs. – contour cell packs (3) – cardboard packs.
10 pcs. – contour cell packs (1) – cardboard packs.
10 pcs. – contour cell packs (2) – cardboard packs.
10 pcs. – contour cell packs (3) – cardboard packs.
10 pcs. – contour cell packs (4) – cardboard packs.
5 pcs. – dark glass jars (1) – cardboard packs.
20 pcs. – dark glass jars (1) – cardboard packs.

Clinical-Pharmacological Group

Hypnotic drug

Pharmacotherapeutic Group

Hypnotic agent

Pharmacological Action

A hypnotic agent from the group of cyclopyrrolone derivatives. A “non-benzodiazepine” agonist of benzodiazepine receptors. It also has sedative, anxiolytic, central muscle relaxant, anticonvulsant, and amnestic properties.

Similar to benzodiazepine derivatives, Zopiclone enhances GABA-ergic processes in the brain by interacting with benzodiazepine receptors, which increases the sensitivity of GABA receptors to the neurotransmitter. However, Zopiclone appears to interact with different sites of the benzodiazepine receptor than benzodiazepines.

Zopiclone reduces sleep latency, decreases the number of nocturnal awakenings, and increases total sleep duration. It has virtually no effect on sleep architecture and does not significantly reduce the amount of REM sleep. Residual effects upon awakening are absent or minimal. Repeated administration of zopiclone is not accompanied by accumulation.

Pharmacokinetics

Rapidly and completely absorbed from the gastrointestinal tract. C_max is achieved in 1-3 hours. Easily passes through histohematic barriers, including the blood-brain barrier, and is distributed to organs and tissues, including the brain. T_1/2 is 5.5-6 hours; does not accumulate.

Indications

Sleep disorders (difficulty falling asleep, frequent nocturnal awakenings, early morning awakening); transient, situational, and chronic insomnia; sleep disorders in mental disorders; bronchial asthma with nocturnal attacks (in combination with a single daily dose of theophylline).

ICD codes

Dosage Regimen

Take the tablet orally, immediately before bedtime. Ensure you have a period of uninterrupted sleep of 7-8 hours after ingestion.

The standard adult dose is 7.5 mg once daily. For severe insomnia, the dose may be increased to a maximum of 15 mg.

For elderly patients, initiate therapy at a reduced dose of 3.75 mg.

For patients with hepatic impairment, use a dose of 3.75 mg.

Limit the treatment duration to a maximum of 4 weeks, including the dose-tapering period. Avoid long-term continuous use.

Do not exceed the prescribed dose. Do not take a second tablet during the same night.

Discontinue treatment by gradually reducing the dose to minimize the risk of withdrawal symptoms. The drug is contraindicated in children and adolescents under 15 years of age.

Adverse Reactions

From the digestive system: sensation of a bitter or metallic taste in the mouth, dry mouth, nausea, vomiting.

From the CNS: dizziness, headache, drowsiness, confusion, anterograde amnesia, hallucinations, nightmares.

Dermatological reactions: skin rash.

Contraindications

Severe respiratory failure, pregnancy, lactation (breastfeeding), children and adolescents under 15 years of age, hypersensitivity to zopiclone.

Use in Pregnancy and Lactation

Zopiclone is contraindicated for use during pregnancy and lactation (breastfeeding).

Use in Hepatic Impairment

Use with caution in severe hepatic insufficiency.

Pediatric Use

Contraindicated in children under 15 years of age.

Special Precautions

Use with caution in severe hepatic insufficiency.

The risk of drug dependence is minimal if the duration of zopiclone use does not exceed 4 weeks. However, the potential danger of developing dependence on zopiclone exists.

Alcohol consumption should be avoided during treatment.

Effect on ability to drive vehicles and operate machinery

The day after taking the drug, one should exercise caution when driving a car and working with machinery.

Drug Interactions

With simultaneous use, it reduces the plasma concentration of trimipramine and its effect.

Zopiclone enhances the effect of drugs that depress the central nervous system (including ethanol).

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.