Zopiclone

Cod liver oil nano-structured lipid carriers (Cod-NLCs) as a promising platform for nose to brain delivery: Preparation, in vitro optimization, ex vivo cytotoxicity & in vivo biodistribution utilizing radioiodinated zopiclone

“…Thirty percent of the dose is N -desmethyl-zopiclone, which is pharmacologically inactive ( Chouinard et al, 1999 ; Hesse et al, 2003 ). This extensive metabolism ultimately leads to dose reduction in individuals over the age of 65, as well as those with renal or hepatic impairment ( Goa and Heel, 1986 ; Noble et al, 1998 ). Thus nasal administration of ZP can achieve direct nose-to-brain transmission of the drug precluding many limitations bypassing its hepatic metabolism, decreasing side effects in addition to the capability of lowering the dose with rapid onset of action.…”

Determination of Zolpidem and Zopiclone in Serum by Capillary Column Gas Chromatography

“…Chromatograms of zolpidem( 2 ) and haloperidol (internal standard, s) in extracts of samples of blank human serum (a), spiked human serum (b), blank rabbit serum (c), and rabbit serum after oral zolpidem hemitartrate administration (d). 24hromatograms of zopiclone (2) and chlorohaloperidol (internal standard, s) in extracts of samples of spiked human serum (a), blank human serum (b), and human serum after oral zopiclone administration (c).…”

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

“…Zopiclone can also cause seizures and delirium 15,16. It is the frst cyclopyrrolone possessing a pharmacological profle of high effcacy and low toxicity similar to that of benzodiazepines 17. Its elimination half-life is 5–6 hours, it does not accumulate upon repeated administration, and its pharmacokinetic profle is not substantially modifed in the elderly and renal failure patients 18.…”

“…Its elimination half-life is 5–6 hours, it does not accumulate upon repeated administration, and its pharmacokinetic profle is not substantially modifed in the elderly and renal failure patients 18. 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.…”