Description: Zopiclone is a prescription medication commonly used for the short-term treatment of insomnia or difficulty sleeping. It helps initiate and maintain sleep by acting on the central nervous system.
DrugBank ID: DB01198
Modality: Small molecule
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A dose-range finding study of zopiclone in insomniac patients
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Evaluation of Zopiclone Dose Ranges in Patients with Insomnia
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Investigating Optimal Dosage of Zopiclone for the Treatment of Insomnia
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Dose-Range Study of Zopiclone in Insomnia Patients
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A Clinical Evaluation of Zopiclone Dosage Ranges in Individuals with Insomnia
Zopiclone Overview
Brand Names: Imovane, Zimovane, among others
Drug Class: Nonbenzodiazepine hypnotic (specifically a cyclopyrrolone)
Use: Short-term treatment of insomnia, especially in cases involving difficulty falling asleep or frequent night awakenings.
Mechanism of Action
Though structurally unrelated to benzodiazepines, Zopiclone binds to the benzodiazepine site on GABAA receptors.
Acts as a positive allosteric modulator, enhancing GABAergic transmission → CNS depression → sedative/hypnotic effects.
Its action is similar to benzodiazepines, but with distinct chemical structure and potentially fewer anxiolytic or muscle relaxant effects.
Pharmacological Effects
Sedative
Hypnotic
Anxiolytic (mild)
Amnesic
Muscle relaxant (minimal)
Dependence and Withdrawal
Prolonged use (even at therapeutic doses) may lead to:
Tolerance
Psychological dependence
Physical dependence
Withdrawal symptoms (similar to benzodiazepine withdrawal but generally milder):
Rebound insomnia
Anxiety
Irritability
Agitation
Sweating
Tremors
Less commonly: perceptual disturbances or confusion
Important: Unlike high-dose benzodiazepine withdrawal, zopiclone withdrawal rarely causes seizures or life-threatening complications—but severe psychological symptoms (like panic or agitation) can occur and lead to emergency room visits.
Clinical Considerations
Recommended for short-term use only (usually 2–4 weeks), due to risk of dependence and tolerance.
Should be tapered gradually if used long-term, rather than stopped abruptly.
Patients with a history of substance use disorder, elderly, or those with psychiatric comorbidities should be monitored carefully.
Zopiclone UK
A benzodiazepine-related hypnotic, used short-term for treating insomnia.
Belongs to a group of drugs known as “Z-drugs” (non-benzodiazepine sedatives).
Controlled under UK law as a Class C drug due to the risk of dependence.
Dosage Forms
Tablets: 3.75 mg and 7.5 mg
May also be available in liquid form (less common)
💊 Always check the Patient Information Leaflet (PIL) included in the medication box for your specific dose and formulation.
Where to Find More Information
You can access official PILs and detailed drug data at:
“Assessment of Zopiclone” (PDF). World Health Organization. Essential Medicines and Health Products. World Health Organization. 2006. p. 9 (Section 5. Pharmacokinetics). Retrieved 5 December 2015.
Van Der Kleijn E (1989). “Effects of zopiclone and temazepam on sleep, behaviour and mood during the day”. European Journal of Clinical Pharmacology. 36 (3): 247–251. doi:10.1007/BF00558155. ISSN0031-6970. PMID2744064.
Touitou Y (July 2007). “[Sleep disorders and hypnotic agents: medical, social and economical impact]”. Annales Pharmaceutiques Françaises (in French). 65 (4): 230–238. doi:10.1016/s0003-4509(07)90041-3. PMID17652991.
Mets MA, Volkerts ER, Olivier B, Verster JC (August 2010). “Effect of hypnotic drugs on body balance and standing steadiness”. Sleep Medicine Reviews. 14 (4): 259–267. doi:10.1016/j.smrv.2009.10.008. PMID20171127.
Tada K, Sato Y, Sakai T, Ueda N, Kasamo K, Kojima T (1994). “Effects of zopiclone, triazolam, and nitrazepam on standing steadiness”. Neuropsychobiology. 29 (1): 17–22. doi:10.1159/000119057. PMID8127419.
Allain H, Bentué-Ferrer D, Tarral A, Gandon JM (July 2003). “Effects on postural oscillation and memory functions of a single dose of zolpidem 5 mg, zopiclone 3.75 mg and lormetazepam 1 mg in elderly healthy subjects. A randomized, cross-over, double-blind study versus placebo”. European Journal of Clinical Pharmacology. 59 (3): 179–188. doi:10.1007/s00228-003-0591-5. PMID12756510. S2CID13440208.
Antai-Otong D (August 2006). “The art of prescribing. Risks and benefits of non-benzodiazepine receptor agonists in the treatment of acute primary insomnia in older adults”. Perspectives in Psychiatric Care. 42 (3): 196–200. doi:10.1111/j.1744-6163.2006.00070.x. PMID16916422.
Bain KT (June 2006). “Management of chronic insomnia in elderly persons”. The American Journal of Geriatric Pharmacotherapy. 4 (2): 168–192. doi:10.1016/j.amjopharm.2006.06.006. PMID16860264.
“Zopiclone”, British National Formulary, National Institute for Health and Care Excellence, 19 September 2016, archived from the original on 9 October 2016, retrieved 2 October 2016
Staner L, Ertlé S, Boeijinga P, Rinaudo G, Arnal MA, Muzet A, et al. (October 2005). “Next-day residual effects of hypnotics in DSM-IV primary insomnia: a driving simulator study with simultaneous electroencephalogram monitoring”. Psychopharmacology. 181 (4): 790–798. doi:10.1007/s00213-005-0082-8. PMID16025317. S2CID26351598.
Barbone F, McMahon AD, Davey PG, Morris AD, Reid IC, McDevitt DG, et al. (October 1998). “Association of road-traffic accidents with benzodiazepine use”. Lancet. 352 (9137): 1331–1336. doi:10.1016/S0140-6736(98)04087-2. PMID9802269. S2CID40825194.
Yasui M, Kato A, Kanemasa T, Murata S, Nishitomi K, Koike K, et al. (June 2005). “[Pharmacological profiles of benzodiazepinergic hypnotics and correlations with receptor subtypes]”. Nihon Shinkei Seishin Yakurigaku Zasshi = Japanese Journal of Psychopharmacology. 25 (3): 143–151. PMID16045197.
Lader M, Denney SC (1982). “A double-blind study to establish the residual effects of zopiclone on performance in healthy volunteers”. International Pharmacopsychiatry. 17 (Suppl 2): 98–108. PMID7188379.
Trachsel L, Dijk DJ, Brunner DP, Klene C, Borbély AA (February 1990). “Effect of zopiclone and midazolam on sleep and EEG spectra in a phase-advanced sleep schedule”. Neuropsychopharmacology. 3 (1): 11–18. PMID2306331.
Mann K, Bauer H, Hiemke C, Röschke J, Wetzel H, Benkert O (August 1996). “Acute, subchronic and discontinuation effects of zopiclone on sleep EEG and nocturnal melatonin secretion”. Eur Neuropsychopharmacol. 6 (3): 163–168. doi:10.1016/0924-977X(96)00014-4. PMID8880074. S2CID25259646.
Kanno O, Watanabe H, Kazamatsuri H (March 1993). “Effects of zopiclone, flunitrazepam, triazolam and levomepromazine on the transient change in sleep-wake schedule: polygraphic study, and the evaluation of sleep and daytime condition”. Prog. Neuropsychopharmacol. Biol. Psychiatry. 17 (2): 229–239. doi:10.1016/0278-5846(93)90044-S. PMID8430216. S2CID54285586.
Mannaert E, Tytgat J, Daenens P (November 1996). “Detection and quantification of the hypnotic zopiclone, connected with an uncommon case of drowning”. Forensic Science International. 83 (1): 67–72. doi:10.1016/0379-0738(96)02018-X. PMID8939015.
Buckley NA, Dawson AH, Whyte IM, McManus P, Ferguson N.Correlations between prescriptions and drugs taken in self-poisoning: Implications for prescribers and drug regulation. Med J Aust (in press)
Yamazaki M, Terada M, Mitsukuni Y, Yoshimura M (August 1998). “[An autopsy case of poisoning by neuropsychopharmaceuticals including zopiclone]”. Nihon Hoigaku Zasshi = the Japanese Journal of Legal Medicine (in Japanese). 52 (4): 245–252. PMID9893443.
Boniface PJ, Russell SG (1996). “Two cases of fatal zopiclone overdose”. Journal of Analytical Toxicology. 20 (2): 131–133. doi:10.1093/jat/20.2.131. PMID8868406.
Pounder DJ, Davies JI (May 1994). “Zopiclone poisoning: tissue distribution and potential for postmortem diffusion”. Forensic Science International. 65 (3): 177–183. doi:10.1016/0379-0738(94)90273-9. PMID8039775.
Regouby Y, Delomez G, Tisserant A (1990). “[First-degree heart block caused by voluntary zopiclone poisoning]”. Therapie (in French). 45 (2): 162. PMID2353332.
Regouby Y, Delomez G, Tisserant A (1989). “[Auriculo-ventricular block during voluntary poisoning with zopiclone]”. Therapie (in French). 44 (5): 379–380. PMID2814922.
Dart RC (2003). Medical Toxicology. Lippincott Williams & Wilkins. p. 889. ISBN978-0-7817-2845-4.
Carlsten A, Waern M, Holmgren P, Allebeck P (2003). “The role of benzodiazepines in elderly suicides”. Scandinavian Journal of Public Health. 31 (3): 224–228. doi:10.1080/14034940210167966. PMID12850977. S2CID24102880.
Harry P (April 1997). “[Acute poisoning by new psychotropic drugs]”. La Revue du Praticien. 47 (7): 731–735. PMID9183949.
Bramness JG, Arnestad M, Karinen R, Hilberg T (September 2001). “Fatal overdose of zopiclone in an elderly woman with bronchogenic carcinoma”. Journal of Forensic Sciences. 46 (5): 1247–1249. doi:10.1520/JFS15131J. PMID11569575.
Caille G, du Souich P, Spenard J, Lacasse Y, Vezina M (April 1984). “Pharmacokinetic and clinical parameters of zopiclone and trimipramine when administered simultaneously to volunteers”. Biopharmaceutics & Drug Disposition. 5 (2): 117–125. doi:10.1002/bdd.2510050205. PMID6743780.
Mattila ME, Mattila MJ, Nuotto E (April 1992). “Caffeine moderately antagonizes the effects of triazolam and zopiclone on the psychomotor performance of healthy subjects”. Pharmacology & Toxicology. 70 (4): 286–289. doi:10.1111/j.1600-0773.1992.tb00473.x. PMID1351673