Zopiclone (Tablets) Instructions for Use

ATC Code

N05CF01 (Zopiclone)

Active Substance

Zopiclone (Rec.INN registered by WHO)

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 possesses sedative, anxiolytic, central muscle relaxant, anticonvulsant, and amnestic properties.

Similar to benzodiazepine derivatives, Zopiclone enhances GABAergic 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 structure and does not significantly reduce the amount of REM sleep. Hangover effects upon awakening are absent or mild. 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. Use the same reduced dose for patients with hepatic impairment.

Limit the treatment duration to a maximum of 4 weeks. Avoid prolonged use to minimize the risk of dependence and tolerance.

Do not take the medication with or immediately after a high-fat meal, as this can delay the onset of action.

Do not crush or chew the tablet. Swallow it whole with a glass of water.

Adverse Reactions

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

From the central nervous system: 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 during 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.

During treatment, alcohol consumption should be avoided.

Influence on the 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.