Zopiclone

Abstract

Zopiclone is a cyclopyrrolone which is chemically unrelated to the benzodiazepines and is thought to act on the GABAA receptor complex at a site distinct from, but closely related to, the benzodiazepine binding site. The hypnotic efficacy of zopiclone administered as single oral doses has been demonstrated in patients undergoing next-day surgery and in patients with insomnia, and these studies have established an optimal dose of 7.5mg for elderly patients. Using this dose, clinical studies have shown that zopiclone improved sleep in elderly patients to a similar extent as triazolam 0.125 to 0.5mg, flurazepam 15mg, and nitrazepam 5mg. Studies that also included younger patients have shown that zopiclone 7.5mg is at least as effective as triazolam 0.25 or 0.5mg, and on most sleep parameters is comparable to temazepam 20mg, nitrazepam 5mg, flunitrazepam 2mg, and flurazepam 20mg. Zopiclone causes minimal impairment to psychomotor performance and mental alertness the morning after night-time administration. The drug is generally well tolerated by patients of all ages; the most frequently reported adverse effects being bitter taste and dry mouth. Treatment withdrawal due to adverse effects is seldom required and reports of rebound insomnia after zopiclone withdrawal are rare. While symptoms of physical dependence have not been observed in clinical studies, there have been isolated reports of physical dependence in patients with a history of substance abuse. Although the latter finding should be kept in mind, it appears that zopiclone has a low dependence liability. Thus, with its short duration of action and good tolerability profile, zopiclone is a well established alternative to the benzodiazepine hypnotics and may be particularly beneficial in those patients unable or unwilling to tolerate the residual effects associated with many other hypnotic agents.

The efficacy and safety of zolpidem and zopiclone to treat insomnia in Alzheimer’s disease: a randomized, triple-blind, placebo-controlled trial

“…Based on this, finding a greater proportion of adverse effects with this drug does not surprise. Furthermore, the half-life of zopiclone is longer in older adults (≈8 h) than in healthy young adults (3.5-6.5 h) due to reduced hepatic metabolism with senescence [56]. Therefore, age may have potentiated the effects of zopiclone (in relation to zolpidem) on sleep and other outcomes.…”

Impact of Sleep Disorder as a Risk Factor for Dementia in Men and Women

“…Zopyclones are cyclopyrrolones that are believed to act on the GABAA receptor complex at sites that are not chemically related to BZDs and are distinct but closely related to the BZD binding site (Wadworth and McTavish, 1993). Unlike zolpidem, the residual effect of zopiclone in CRSD patients was not significantly different among genders (Leufkens and Vermeeren, 2014).…”

A comparison of complex sleep behaviors with two short-acting Z-hypnosedative drugs in nonpsychotic patients

“…It is thought to act on the GABA A receptor complex at a site distinct from the benzodiazepine binding site 14. Tolerance to the effects of zopiclone can develop after a few weeks’ use and abrupt withdrawal, particularly with prolonged and high doses.…”

“…In clinical trials, zopiclone (usually 7.5 mg) improved sleep in chronic insomniacs similarly to nitrazepam 5 mg, flurazepam 15–30 mg, triazolam 0.5 mg, and temazepam 20 mg, but in a single study was slightly less effective than funitrazepam 2 mg in some evaluation criteria 17. The drug is generally well tolerated by patients of all ages and the most frequently reported adverse effects are bitter taste and dry mouth 14. Treatment for withdrawal due to adverse effects is seldom required and reports of rebound insomnia after zopiclone withdrawal are rare 14.…”

“…The drug is generally well tolerated by patients of all ages and the most frequently reported adverse effects are bitter taste and dry mouth 14. Treatment for withdrawal due to adverse effects is seldom required and reports of rebound insomnia after zopiclone withdrawal are rare 14. Minimal impairment of psychomotor skills and mental acuity may occur in the morning after a bedtime dose of zopiclone 17…”