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Zopiclone

Medical Use and Recommendations: – Zopiclone is used for short-term treatment of insomnia. – Not recommended for long-term use due to tolerance, dependence, and addiction […]

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Medical Use and Recommendations:
– Zopiclone is used for short-term treatment of insomnia.
– Not recommended for long-term use due to tolerance, dependence, and addiction risks.
– Cognitive behavioral therapy may be more effective than zopiclone.
– Ineffective for improving sleep quality in shift workers.
– Recommended duration of 2-3 weeks for short-term insomnia.

Special Populations and Adverse Reactions:
– Elderly individuals experience impaired balance and cognitive side effects.
– Zopiclone increases postural sway and falls in older people.
– Adverse reactions include taste disturbance, nausea, drowsiness, and more.
– Rare adverse effects include amnesia, confusion, and hallucinations.
– Zopiclone may cause paradoxical effects and sleep-walking.

Contraindications and Interactions:
– Impairs driving skills similar to benzodiazepines.
– Avoid driving or operating machinery due to impaired hand-eye coordination.
– Interacts with trimipramine and caffeine.
– Alcohol combined with zopiclone significantly enhances adverse effects and overdose potential.
– Erythromycin and itraconazole increase zopiclone absorption.

Pharmacology and Pharmacokinetics:
– Zopiclone has hypnotic, anxiolytic, anticonvulsant, and myorelaxant properties.
– Zopiclone binds to GABA receptors like benzodiazepines, enhancing GABA actions.
– Zopiclone is rapidly absorbed orally with a bioavailability of 75-80%.
– Extensively metabolized in the liver with an elimination half-life of 3.5 to 6.5 hours.
– Zopiclone’s pharmacokinetics are influenced by aging, renal, and hepatic functions.

Misuse, Addiction, and Toxicity:
– Zopiclone misuse for achieving a high and combined with alcohol for euphoric effects.
– Risk of dependence with normal doses and withdrawal symptoms after long-term use.
– Symptoms of addiction include depression, dysphoria, and social isolation.
– Zopiclone linked to criminal acts like sexual assaults and drugged driving.
– Overdose potential with fatalities reported, making proper monitoring crucial.

Zopiclone (Wikipedia)

Zopiclone, sold under the brand name Imovane among others, is a nonbenzodiazepine used to treat difficulty sleeping. Zopiclone is molecularly distinct from benzodiazepine drugs and is classed as a cyclopyrrolone. However, zopiclone increases the normal transmission of the neurotransmitter gamma-aminobutyric acid (GABA) in the central nervous system, via modulating GABAA receptors similarly to the way benzodiazepine drugs do.

Zopiclone
Clinical data
Trade namesImovane, Zimovane, Dopareel, others
AHFS/Drugs.comInternational Drug Names
Pregnancy
category
  • AU: C
Routes of
administration
Oral tablets, 3.75 mg or 7.5mg (UK), 5 mg, 7.5 mg, or 10 mg (JP)
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability75–80%
Protein binding52–59%
MetabolismHepatic through CYP3A4 and CYP2E1
Elimination half-life~5 hours (3.5–6.5 hours)
~7–9 hours for 65+ years old
ExcretionUrine (80%)
Identifiers
  • (RS)-6-(5-chloropyridin-2-yl)-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazin-5-yl 4-methylpiperazine-1-carboxylate
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
PDB ligand
CompTox Dashboard (EPA)
ECHA InfoCard100.051.018 Edit this at Wikidata
Chemical and physical data
FormulaC17H17ClN6O3
Molar mass388.81 g·mol−1
3D model (JSmol)
  • O=C(OC3c1nccnc1C(=O)N3c2ncc(Cl)cc2)N4CCN(C)CC4
  • InChI=1S/C17H17ClN6O3/c1-22-6-8-23(9-7-22)17(26)27-16-14-13(19-4-5-20-14)15(25)24(16)12-3-2-11(18)10-21-12/h2-5,10,16H,6-9H2,1H3 checkY
  • Key:GBBSUAFBMRNDJC-UHFFFAOYSA-N checkY
  (verify)

Zopiclone is a sedative. It works by causing a depression or tranquilization of the central nervous system. After prolonged use, the body can become accustomed to the effects of zopiclone. When the dose is then reduced or the drug is abruptly stopped, withdrawal symptoms may result. These can include a range of symptoms similar to those of benzodiazepine withdrawal. Although withdrawal symptoms from therapeutic doses of zopiclone and its isomers (i.e., eszopiclone) do not typically present with convulsions and are therefore not considered life-threatening, patients may experience such significant agitation or anxiety that they seek emergency medical attention. [citation needed]

In the United States, zopiclone is not commercially available, although its active stereoisomer, eszopiclone, is. Zopiclone is a controlled substance in the United States, Japan, Brazil, New Zealand and some European countries, and may be illegal to possess without a prescription. [citation needed]

Zopiclone is known colloquially as a "Z-drug". Other Z-drugs include zaleplon and zolpidem and were initially thought to be less addictive than benzodiazepines. However, this appraisal has shifted somewhat in the last few years as cases of addiction and habituation have been presented. Zopiclone is recommended to be taken at the lowest effective dose, with a duration of 2–3 weeks for short-term insomnia. Daily or continuous use of the drug is not usually advised, and caution must be taken when the compound is used in conjunction with benzodiazepines, sedatives or other drugs affecting the central nervous system.

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