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Zopiclone-nonbenzodiazepine hypnotic agent

Zopiclone is a nonbenzodiazepine hypnotic agent used in the treatment of insomnia. More

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Description

Zopiclone is a nonbenzodiazepine hypnotic agent used in the treatment of insomnia.

Generic Name

Zopiclone-nonbenzodiazepine hypnotic agent

Chemical names

Zopiclone; Imovane; Amoban; Zimovane

Brand names

Lyzop, Ziclone, Zolinox, Zolium, Zopicon, Zopitran

IUPAC name

6-(5-chloropyridin-2-yl)-7-oxo-5H,6H,7H-pyrrolo[3,4-b]pyrazin-5-yl 4-methylpiperazine-1-carboxylate

Pharmacokinetics

Oral absorption, widely distributed with hepatic metabolism, excreted via feces and urine.

Actions

It is from the pyrazolopyrimidine class of non benzodiazepine hypnotic indicated for the short-term treatment of insomnia. While Zopiclone is a hypnotic agent with a chemical structure unrelated to benzodiazepines, barbiturates, or other drugs with known hypnotic properties, it interacts with the gamma-aminobutyric acid-benzodiazepine (GABABZ) receptor complex. Subunit modulation of the GABABZ receptor chloride channel macromolecular complex is hypothesized to be responsible for some of the pharmacological properties of benzodiazepines, which include sedative, anxiolytic, muscle relaxant, and anticonvulsive effects in animal models. Zopiclone binds selectively to the brain alpha subunit of the GABA A omega-1 receptor.

Dosage/Dosage form

The recommended dose is 7.5 mg/day at bed time as PO.

Therapeutic uses

For the short-term treatment of insomnia.

Adverse effects/Side effects

Metallic or bitter aftertaste; irritability, confusion, depressed mood, aggressiveness, incoordination, anterograde amnesia, mild increase in LFTs, drowsiness, lightheadedness, nausea, vomiting, urticaria, rashes.

Interaction

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.

Contraindications

Myasthenia gravis; respiratory failure; severe sleep apnoea syndrome; severe hepatic impairment; pregnancy, lactation.

Storage

Store in a dry place below 30°C.

Information

Molecular weight

388.808

Molecular formula

C17H17ClN6O3

CAS number

43200-80-2

Precautions

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.