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Eszopiclone: its use in the treatment of insomnia

By Jaime M Monti and SR Pandi-Perumal


Eszopiclone is the S-isomer of racemic zopiclone, a cyclopyrrolone with sedative-hypnotic activity that has been available in Europe, Canada, and Latin America since 1987. Eszopiclone acts by binding to the GABAA receptor. In contrast to the benzodiazepine (BZD) hypnotics, eszopiclone has more selectivity for certain subunits of the GABAA receptor. Oral eszopiclone is rapidly absorbed and extensively distributed to body tissues including the brain. Peak plasma concentrations are attained 1.0–1.6 hours after a 3 mg dose, while the mean elimination half-life is 6 hours. The half-life increases with age to about 9.0 hours in patients 65 years or older. Eszopiclone’s pharmacokinetic (PK) profile is not substantially modified in patients suffering from renal failure or mild-to-moderate hepatic impairment, although patients with severe hepatic insufficiency should have a reduced dose. The subjective perception of improved sleep following eszopiclone 2 or 3 mg treatment has been demonstrated in randomized, double-blind, placebo-controlled studies of up to 6 months’ duration. In these studies the drug significantly reduced sleep onset latency (SOL), the number of awakenings, and wake time after sleep onset (WASO) whereas total sleep time (TST) and quality of sleep were increased in non-elderly and elderly subjects. Sleep laboratory studies of the effects of eszopiclone have confirmed the drug’s clinical efficacy in subjects with chronic primary insomnia. Eszopiclone, unlike BZD hypnotics, does not significantly alter values corresponding to slow wave sleep (SWS or stages 3 and 4) and rapid eye movement (REM) sleep. Rebound insomnia following withdrawal of eszopiclone has been examined in only one study. Discontinuation of the active treatment with 2 mg was followed by rebound insomnia in non-elderly subjects. Three-mg doses of eszopiclone administered for a period of up to 12 months was associated with a sustained beneficial effect on sleep induction and maintenance, with no occurrence of tolerance. The most common side-effects were unpleasant or bitter taste, headache, dyspepsia, pain, diarrhea, dry mouth, upper respiratory infection, urinary tract infection, dizziness, and accidental injury. New adverse events (withdrawal symptoms) including anxiety, abnormal dreams, hyperesthesia, nausea, and upset stomach were recorded in one study on the days following eszopiclone 2 or 3 mg discontinuation. Although dependence and abuse potential have not been formally assessed, unpublished data show that eszopiclone at doses of 6 and 12 mg produces euphoria effects similar to those of diazepam 20 mg in BZD drug addicts. In conclusion, available evidence tends to indicate that eszopiclone is effective and safe for the treatment of chronic primary insomnia in non-elderly and elderly subjects. Tolerance did not occur during active drug administration for a 12-month period. Thus eszopiclone can be efficacious not only during short- and intermediate-term administration but also in patients requiring prolonged regular drug usage

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    1. (2005). A 2-week effi cacy and safety study of eszopiclone in elderly patients with primary insomnia.
    2. (1983). A comparative study of zopiclone and fl unitrazepam in insomniacs seen by general practitioners.
    3. (1992). A comparison of effi cacy and tolerance of the short acting sedatives midazolam and zopiclone.
    4. (1990). A comparison of the effi cacy, safety and withdrawal effects of zopiclone and triazolam in the treatment of insomnia.
    5. (1990). A multi-centre open study in general practice to evaluate the effi cacy and acceptability of zopiclone 7.5 mg nocte in patients requiring the prescription of a hypnotic.
    6. (2006). A polysomnographic study of eszopiclone in elderly patients with insomnia. Curr Med Res Opin,
    7. (2006). A polysomnography study of eszopiclone in elderly patients with insomnia.
    8. (1988). A sleep laboratory evaluation of the long-term effi cacy of zopiclone.
    9. (2005). An assessment of the effi cacy and safety of eszopiclone in the treatment of transient insomnia in healthy adults. Sleep Med,
    10. (2005). An evaluation of the effi cacy and safety of eszopiclone over 12 months in patients with chronic primary insomnia. Sleep Med,
    11. (1987). Behavioral and electroencephalographic effects of zopiclone, a cyclopyrrolone derivative.
    12. (1978). Benzodiazepine-like central effects of RP 27267, a dihidro-7-oxo-5H-pyrrolo[3,4-b]pyrazine derivative.
    13. (1987). Chronic administration of zopiclone and nitrazepam in the treatment of insomnia.
    14. (1994). Clinical diagnoses of 216 insomnia patients using the International Classifi cation of Sleep Disorders (ICSD), DSM-IV and ICD-10 categories: a report from the APA/NIMH DSM-IV fi eld trial.
    15. (1995). Clinical pharmacokinetics of zopiclone.
    16. (1987). Comparative effects of zopiclone, triazolam and placebo on memory and psychomotor performance in healthy volunteers. Fund Clin Pharmacol,
    17. (2004). Comparative pharmacokinetics and pharmacodynamics of short-acting hypnosedatives.
    18. (1988). Comparison des effets de la zopiclone et du triazolam sur le sommeil du sujet sain.
    19. (1987). Comparison of the clinical hypnotic effects of zopiclone and triazolam.
    20. (1988). Dose effects of zolpidem on transient insomnia. Sleep Res,
    21. (1983). Effectiveness of zopiclone as a preoperative hypnotic. Pharmacology,
    22. (1983). Effects of hypnotics on memory.
    23. (2000). Effects of selective serotonin reuptake inhibitors on objective and subjective sleep quality.
    24. (1984). Effects of zopiclone and benzodiazepine hypnotics on search in short-term memory.
    25. (1989). Effects of zopiclone and temazepam on sleep, behavior and mood during the day.
    26. (1983). Effects of zopiclone as compared to fl urazepam on sleep in women over 40 years of age.
    27. (1983). Effects of zopiclone on the sleep of chronic insomniacs.
    28. (2004). Effi cacy and safety of eszopiclone across 6-weeks of treatment for primary insomnia. Curr Med Res Opin,
    29. (2006). Eszopiclone co-administered with fl uoxetine in patients with insomnia coexisting with major depressive disorder. Biol Psychiatry,
    30. (2006). Eszopiclone for the treatment of insomnia.
    31. (2006). Eszopiclone in patients with insomnia during perimenopause and early postmenopause: a randomized controlled trial. Obstet Gynecol,
    32. (2006). Eszopiclone, a nonbenzodiazepine sedative-hypnotic agent for the treatment of transient and chronic insomnia. Clin Ther,
    33. et al.1990. A comparison of the effi cacy, tolerance and residual effects of zopiclone, fl urazepam and placebo in insomniac outpatients.
    34. (2006). GABAA receptor subtypes in sedation and hypnosis. In
    35. (1980). Hypnotics and sedatives.
    36. (1986). Hypnotics:clinical value of pharmaco-EEG methods.
    37. (1990). Immediate and overnight effects of zopiclone 7.5 mg and nitrazepam 5 mg with ethanol, on psychomotor performance and memory in healthy volunteers.
    38. (1990). Long-term effi cacy and withdrawal of zopiclone:a sleep laboratory study. Int Clin Psychopharmacol,
    39. (1999). New insights into the mechanism of action of hypnotics.
    40. (2006). Overview of currently available benzodiazepine and nonbenzodiazepine hypnotics.
    41. (1993). Pharmacokinetics of zopiclone and its enantiomers in Caucasian young healthy volunteers.
    42. (1985). Pharmacological and clinical studies of cyclopyrrolones:Zopiclone and suriclone. Pharmacol Biochem Behav,
    43. (1983). Pharmacological studies on zopiclone.
    44. (1983). Polygraphical sleep recordings in insomniac patients under zopiclone or nitrazepam.
    45. (2004). Primary and secondary insomnia:Prevalence, causes and current therapeutics.
    46. (1994). Psychiatric Association.
    47. (1985). Residual effects of zopiclone and benzodiazepine hypnotics on psychomotor performance related to car driving. Drugs Exp Clin Res,
    48. (2000). Secondary insomnia.
    49. (2001). Sedative and anxiolytic effects of zopiclone´s enantiomers and metabolite.
    50. (1995). Sleep complaints among elderly persons:an epidemiologic study of three communities.
    51. (1981). Sleep-wake disorders based on a polysomnographic diagnosis.
    52. (1987). Subjective effects during administration and on discontinuation of zopiclone and temazepam in normal subjects.
    53. (2003). Sustained effi cacy of eszopiclone over 6 months of nightly treatment:Results of a randomized, double-blind, placebo-controlled study in adults with chronic insomnia.
    54. (1983). The acceptability of a nonbenzodiazepine hypnotic (zopiclone) in general practice.
    55. (1993). The effect of midazolam on transient insomnia.
    56. (1990). The effect of zopiclone 7.5 mg on the sleep, mood and performance of shift workers. Int Clin Psychopharmacol,
    57. (2004). The pharmacology and mechanisms of action of new generation, non-benzodiazepine hypnotic agents.
    58. (1979). Traitement des troubles du sommeil par la zopiclone. Essais cliniques en double insu contre placébo.
    59. (2006). Treating insomnia:current and investigational pharmacological approaches. Pharmacol Ther,
    60. (1987). Zopiclone and nitrazepam:a multicenter placebo controlled comparative study of effi cacy and tolerance in insomniac patients in general practice.
    61. (1994). Zopiclone improves sleep quality and daytime well-being in insomniac patients: comparison with triazolam, fl unitrazepam and placebo. Int Clin Psychopharmacol,
    62. (1986). Zopiclone produces effects on human performance similar to fl urazepam, lormetazepam and triazolam.
    63. (1985). Zopiclone:A non-benzodiazepine hypnotic. Controlled comparison to temazepam insomnia.
    64. (1998). Zopiclone:An update of its pharmacology, clinical effi cacy and tolerability in the treatment of insomnia.
    65. (1983). Zopiclone:Sleep and performance studies in healthy man.

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