Ran-zopiclone - General Information
Ran-zopiclone is a novel hypnotic agent used in the treatment of insomnia. Its mechanism of action is based on modulating benzodiazepine receptors. In addition to zopiclone's benzodiazepine pharmacological properties it also has some barbiturate like properties.
Pharmacology of Ran-zopiclone
Ran-zopiclone is a nonbenzodiazepine hypnotic from the pyrazolopyrimidine class and is indicated for the short-term treatment of insomnia. While Ran-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. Ran-zopiclone binds selectively to the brain alpha subunit of the GABA A omega-1 receptor.
Additional information about Ran-zopiclone
Ran-zopiclone Indication: For the short-term treatment of insomnia.
Mechanism Of Action: Ran-zopiclone exerts its action by binding on the benzodiazepine receptor complex and modulation of the GABABZ receptor chloride channel macromolecular complex.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Zopiclone
Synonyms: Zopiclona [Inn-Spanish]; Zopiclone [Ban:Inn:Jan]; Zopiclonum [Inn-Latin]; (+-)-zopiclone
Drug Category: Hypnotics and Sedatives
Drug Type: Small Molecule; Approved
Absorption: Rapidly absorbed following oral administration.
Toxicity (Overdose): Rare individual instances of fatal outcomes following overdose with racemic zopiclone have been reported in European postmarketing reports, most often associated with overdose with other CNS-depressant agent. Signs and symptoms of overdose effects of CNS depressants can be expected to present as exaggerations of the pharmacological effects noted in preclinical testing.
Protein Binding: Approximately 45%
Biotransformation: Extensively metabolized in the liver via decarboxylation (major pathway), demethylation, and side chain oxidation. Metabolites include an N-oxide derivative (weakly active; approximately 12% of a dose) and an N-desmethyl metabolite (inactive; approximately 16%). Approximately 50% of a dose is converted to other inactive metabolites via decarboxylation. Hepatic microsomal enzymes are apparently not involved in zopiclone clearance.
Half Life: Elimination half life is approximately 5 hours (range 3.8 to 6.5 hours) and is prolonged to 11.9 hours in patients with hepatic insufficiency.
Dosage Forms of Ran-zopiclone: Tablet Oral
Chemical IUPAC Name: [6-(5-chloropyridin-2-yl)-5-oxo-7H-pyrrolo[3,4-b]pyrazin-7-yl] 4-methylpiperazine-1-carboxylate
Chemical Formula: C17H17ClN6O3
Zopiclone on Wikipedia: https://en.wikipedia.org/wiki/Zopiclone
Organisms Affected: Humans and other mammals