Zopiclone

A class of sedative/hypnotic type drug that exert their effects through the benzodiazepine binding site on GABAa receptors. The class consists both of molecules that contain the benzodiazepine moiety, for example diazepam, lorazepam and flunitrazepam, and the newer, non-benzodiazepine compounds such as zolpidem, zopiclone, indiplon and zaleplon. BzRAs are primarily used for the treatment of anxiety, insomnia and to elicit varying levels of sedation. The wide selection of compounds currently available affords the prescribing clinician extensive options in terms of relative efficacies and durations of action. 

Voderholzer U, Riemann D, Hornyak M, et al A double-blind, randomized and placebo-controlled study on the polysomnographic withdrawal effects of zopiclone, zolpidem and triazolam in healthy subjects. Eur Arch Psychiatry Clin Neurosci 251 117-123, 2001... 

Figure 19.6 The chemical structure of the imidazopyridine and benzodiazepine (BZi) receptor ligand, zolpidem, and the cyclopyrrolone, zopiclone...

FIGURE 7.5 Absorption spectra of doxepin and zopiclone evaluated with Liquation 7.8. 

Hebert C, Delaney JA, Hemmelgarn B et al. (2007) Benzodiazepines and elderly drivers a comparison of pharmacoepidemiological study designs. Pharmacoepidemiol Drag Saf 16(8) 845-849 Hemmeter U, Muller M, Bischof R et al. (2000) Effect of zopiclone and temazepam on sleep EEG parameters, psychomotor and memory functions in healthy elderly volunteers. Psychopharmacology (Berl) 147(4) 384-396... 

Zopiclone, levodopa, metronidazole, metformin, and paroxetine, can disturb the taste. 

Kratzsch C, Tenberken O, Peters FT, Weber AA, Kraemer T, et al. 2004. Screening, library-assisted identification and validated quantification of 23 benzodiazepines, flumazenil, zalepone, zolpidem and zopiclone in plasma by liquid chromatography/mass spectrometry with atmospheric pressure chemical ionization. J Mass Spectrom 39 856. 

Of the non-benzodiazepines that have been introduced recently for the treatment of anxiety and insomnia, buspirone and zopiclone have been the most extensively investigated so far. The pharmacokinetic characteristics of... 

Sedative/hypnotics zopiclone Beta-blockers propranolol, warfarin, theophylline... 

Zopiclone is widely used as a sedative-hypnotic. It is metabolized to an inactive N-desmethylated derivative and an active N-oxide compound, both of which contain chiral centres. S-Zopiclone has a 50-fold higher affinity for the benzodiazepine receptor site than the R-enantiomer. This could be therapeutically important, particularly if the formation and the urinary excretion of the active metabolite benefits the S-isomer, which appears to be the case. As the half-life of the R-enantiomer is longer than that of the S-form, it would seem advantageous to use the R-isomer in order to avoid the possibility of daytime sedation and hangover effects which commonly occur with long-acting benzodiazepine receptor agonists. 

Zolpidem (an imidazopyridine) and zopiclone (a cyclopyrrolone) are hypnotics that, despite their different chemical structure, possess agonist activity at the benzodiazepine receptor (p. 226). 

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