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Generic Index » Zopiclone
Zopiclone information from DrugsUpdate
L - Contraindicated in lactation
FI - Food *
Zopiclone, (brand name Imovane in Canada, and Zimovane in the UK) is a non-benzodiazepine hypnotic agent used in the treatment of insomnia. Zopiclone is known colloquially as a "Z-drug". Other Z-drugs include zaleplon (Sonata) and zolpidem (Ambien and AmbienCR) and were initially thought to be less addictive and/or habit-forming than benzodiazepines. However, this appraisal has shifted somewhat in the last few years as cases of addiction and habituation have been presented. It is recommended that zopiclone be taken on an "as needed" basis. Daily or continuous use of the drug is not usually advised. While it acts on the same benzodiazepine receptors as the benzodiazepine family of drugs it is not classed as a benzodiazepine (with which it shares a number of characteristics and effects) due to its differing molecular structure. Zopiclone is classed as a cyclopyrrolone derivative.
Zopiclone is a cyclopyrrolone derivative with hypnotic and sedative actions, anticonvulsant and muscle relaxant properties similar to benzodiazepines. It binds to a site in the GABA-A-benzodiazepine-chloride channel macromolecular-receptor complex which is different from that of the benzodiazepine binding site.
Absorption
Rapidly absorbed from the GI tract (oral).
Distribution
Widely distributed. Enters breast milk. Protein-binding: 45-80%.
Metabolism
Extensively hepatic; converted to less active N-oxide and inactive N-desmethylzopiclone. Undergoes decarboxylation to inactive metabolites.
Excretion
Urine, faeces (as unchanged drug and metabolites), lungs and saliva; 3.5-6.5 hours (elimination half-life).
Information Not Available
Metallic or bitter aftertaste; irritability, confusion, depressed mood, aggressiveness, incoordination, anterograde amnesia, mild increase in LFTs, drowsiness, lightheadedness, nausea, vomiting, urticaria, rashes.
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Hepatic and renal insufficiency; elderly; psychiatric disorders; history of drug abuse. May impair ability to drive or operate machinery. Limit treatment duration to <4 weeks to minimise risk of dependence and tolerance. Avoid abrupt discontinuation of therapy.
Reduced hypnotic effect with phenytoin and carbamazepine. Increased drowsiness and incoordination with TCAs. Increased CNS depressant effect with alcohol and other CNS depressants. Decreased zopiclone concentration with rifampicin. Possible increase in zopiclone concentration with CYP3A4 inhibitors e.g. erythromycin, clarithromycin, ketoconazole, itraconazole, ritonavir.
Food Interaction
Possible decrease in zopiclone levels with St John's Wort.
Oral
Short-term management of insomnia
Adult: 7.5 mg at bedtime.
Elderly: Initially, 3.75 mg at bedtime.
Renal impairment: Initiate at 3.75 mg at bedtime.
Hepatic impairment: Mild to moderate: Initially 3.75 mg at bedtime. Severe: Contraindicated.
May be taken with or without food
List of Contraindications
Contraindicated in pregnancy
Contraindicated in lactation
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Myasthenia gravis; respiratory failure; severe sleep apnoea syndrome; severe hepatic impairment; pregnancy, lactation.
Oral
Store in a dry place below 30°C. Protect from light.
Information Not Available
