Zopilone (Eszopiclone)

Therapeutic Group: Drugs of Nervous System Anxiolytic and Tranquilizer

Zopilone 1 Tablet: Each film coated tablet contains Eszopiclone INN 1mg. Zopilone 2 Tablet: Each film coated tablet contains Eszopiclone INN 2mg.

Eszopiclone is a sedative-hypnotic drug, which can reduce sleep latency and improve sleep maintenance. Eszopiclone is pharmacologically active enantiomer of Zopiclone. S-zopiclone has about 50-fold higher affinity for its benzodiazepine receptor target site compared to R-zopiclone. By binding as agonists to benzodiazepine receptors-1 (BZ1), shows agonist effects of GABA in the brain and spinal cord. The BZ1 receptors are located predominantly in areas of the brain involved in sleepwakefulness mechanisms and sedation, which suggest a more favorable profile of these drugs in the treatment of insomnia. It is rapidly absorbed from GIT. Time-to-peak plasma concentration (Tmax) is about 1 hour. Elimination half-life is about 6 hours. Eszopiclone is metabolized in liver by demethylation and oxidation. Eszopiclone does not accumulate with once-daily administration. There is no evidence of tolerance of Eszopiclone.

Eszopiclone is indicated for the treatment of insomnia, including difficulty falling asleep and difficulty maintaining sleep through the night. Eszopiclone is the first sedative approved long-term use

Eszopiclone should be taken immediately before bedtime and the dose should be individualized . For adults, the starting dose is 2 mg. The dose can be initiated or raised to 3 mg if clinically indicated, since 3 mg is more effective for sleep maintenance. In the elderly patient starting dose is 1 mg and dosage may be raised to 2 mg if clinically indicated. Hepatic or Renal impairment: Dosage should not be increased above 2 mg in patients with severe hepatic impairment. No dose adjustment is necessary for patients with mild-to-moderate hepatic or renal impairment though Eszopiclone should be used with caution in patients with hepatic impairment. Paediatric use : Safety and effectiveness of Eszopiclone in children below the age of 18 years have not been established.

Eszopiclone is generally well tolerated. However few side effects like fatigue, anorexia, nausea, unpleasant taste in the mouth, mood problems, abdominal pain, dyspepsia, asthenia, nervousness, dizziness and confusion have been reported.

Eszopiclone like all sedatives should be taken immediately before bedtime to avoid short-term memory impairment, hallucinations, impaired coordination, dizziness and lightheadedness

Known hypersensitivity to Eszopiclone or any other ingredient in the formulations

There are no adequate and well-controlled studies in pregnant women. This drug should be used during pregnancy only if clearly needed. Nursing Mothers: It is not known whether the drug is excreted in breast milk. As many drugs are excreted in breast milk, caution should be exercised when Eszopiclone is administered to a nursing mother.

There is limited clinical experience with the overdose of Eszopiclone. In clinical trials one case of overdose with up to 36 mg of Eszopiclone has been reported in which the subject fully recovered. Intravenous fluids should be administered as needed Flumazenil may be useful.

Zopilone 1: Each box contains 5 blister strips of 10 tablets. Zopilone 2: Each box contains 5 blister strips of 10 tablets.