Zopiclone. An update of its pharmacology, clinical efficacy and tolerability in the treatment of insomnia. 1998

S Noble, and H D Langtry, and H M Lamb
Adis International Limited, Auckland, New Zealand. demail@adis.co.nz

Zopiclone is a non-benzodiazepine hypnotic which was first reviewed in Drugs in 1986. At that time, zopiclone had shown hypnotic efficacy superior to that of placebo, but had not been extensively compared with benzodiazepine hypnotics in patients with insomnia. A much larger body of clinical data is now available, allowing a more detailed evaluation than was previously possible. Together with results from earlier studies, subsequent clinical trials have shown that zopiclone is generally at least as effective as the benzodiazepines (regardless of duration of action) in the treatment of insomnia, although comparisons between zopiclone and flurazepam have produced inconsistent results. Tolerance to the effects of zopiclone was not seen in short term clinical trials (< or = 4 weeks); data from longer term studies are conflicting and the potential for tolerance during long term zopiclone treatment is therefore unclear. Zopiclone has a relatively low propensity to cause residual clinical effects (such as difficulty in waking or reduced morning concentration). Rebound of insomnia to a level below that at baseline can occur after withdrawal of zopiclone, but, on the basis of data from short term studies, does not appear to be common. Data from prescription-event monitoring suggest that zopiclone does not have a high dependence potential (at least in those who are not regular drug abusers/addicts). Zopiclone is well tolerated in both the elderly and younger patients with insomnia. A bitter aftertaste is usually the most common adverse event, but is relatively infrequent (3.6% in the largest available postmarketing study). Thus, zopiclone is now firmly established as an effective and well tolerated hypnotic agent. Although the available data on rebound insomnia and dependence liability are encouraging, potential differences between zopiclone and the benzodiazepines in these respects may have little clinical relevance in the context of short term intermittent use of hypnotics, as it currently recommended. A low propensity for rebound insomnia and dependence might prove valuable during long term hypnotic therapy (which, although not recommended, is a clinical reality). However, the risk-benefit profile of zopiclone in this context remains unknown. Nevertheless, zopiclone is clearly a suitable alternative to the benzodiazepines for the short term treatment of insomnia.

UI MeSH Term Description Entries
D006993 Hypnotics and Sedatives Drugs used to induce drowsiness or sleep or to reduce psychological excitement or anxiety. Hypnotic,Sedative,Sedative and Hypnotic,Sedatives,Hypnotic Effect,Hypnotic Effects,Hypnotics,Sedative Effect,Sedative Effects,Sedatives and Hypnotics,Effect, Hypnotic,Effect, Sedative,Effects, Hypnotic,Effects, Sedative,Hypnotic and Sedative
D007319 Sleep Initiation and Maintenance Disorders Disorders characterized by impairment of the ability to initiate or maintain sleep. This may occur as a primary disorder or in association with another medical or psychiatric condition. Disorders of Initiating and Maintaining Sleep,Insomnia,Sleeplessness,Chronic Insomnia,DIMS (Disorders of Initiating and Maintaining Sleep),Early Awakening,Insomnia Disorder,Nonorganic Insomnia,Primary Insomnia,Psychophysiological Insomnia,Rebound Insomnia,Secondary Insomnia,Sleep Initiation Dysfunction,Transient Insomnia,Awakening, Early,Dysfunction, Sleep Initiation,Dysfunctions, Sleep Initiation,Insomnia Disorders,Insomnia, Chronic,Insomnia, Nonorganic,Insomnia, Primary,Insomnia, Psychophysiological,Insomnia, Rebound,Insomnia, Secondary,Insomnia, Transient,Insomnias,Sleep Initiation Dysfunctions
D010879 Piperazines Compounds that are derived from PIPERAZINE.
D002986 Clinical Trials as Topic Works about pre-planned studies of the safety, efficacy, or optimum dosage schedule (if appropriate) of one or more diagnostic, therapeutic, or prophylactic drugs, devices, or techniques selected according to predetermined criteria of eligibility and observed for predefined evidence of favorable and unfavorable effects. This concept includes clinical trials conducted both in the U.S. and in other countries. Clinical Trial as Topic
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D001569 Benzodiazepines A group of two-ring heterocyclic compounds consisting of a benzene ring fused to a diazepine ring. Benzodiazepine,Benzodiazepine Compounds
D013649 Taste The ability to detect chemicals through gustatory receptors in the mouth, including those on the TONGUE; the PALATE; the PHARYNX; and the EPIGLOTTIS. Gustation,Taste Sense,Gustations,Sense, Taste,Senses, Taste,Taste Senses,Tastes
D053961 Azabicyclo Compounds Bicyclic bridged compounds that contain a nitrogen which has three bonds. The nomenclature indicates the number of atoms in each path around the rings, such as [2.2.2] for three equal length paths. Some members are TROPANES and BETA LACTAMS. Azabicyclo(1.1.0)Butanes,Azabicyclo(2.2.2)Octanes,Azabicyclo(3.3.1)Nonanes,Azabicyclo(4.3.0)Nonanes,Azabicyclo(5.2.2)Undecanes

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