indication

For the treatment of insomnia

pharmacology

Eszopiclone is a nonbenzodiazepine hypnotic, pyrrolopyrazine derivative of the cyclopyrrolone class and is indicated for the short-term treatment of insomnia. While Eszopiclone 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 (GABA_BZ) receptor complex. Subunit modulation of the GABA_BZ 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. Eszopiclone binds selectively to the brain alpha subunit of the GABA A omega-1 receptor.

mechanism of action

The mechanism of action of Eszopiclone is not completely understood. It is thought that Eszopiclone acts on the benzodiazepine receptors as an agonist and interacts with GABA-receptor complexes.

toxicity

Side effects include viral infection, dry mouth, dizziness, hallucinations, infection, rash, and unpleasant taste, with this relationship clearest for unpleasant taste depending on doses.

biotransformation

Following oral administration, eszopiclone is extensively metabolized by oxidation and demethylation.

absorption

Rapidly absorbed following oral administration

half life

6 hours

route of elimination

Up to 75% of an oral dose of racemic zopiclone is excreted in the urine, primarily as metabolites.

drug interactions

Telithromycin: Telithromycin may reduce clearance of Eszopiclone. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Eszopiclone if Telithromycin is initiated, discontinued or dose changed.

Triprolidine: The CNS depressants, Triprolidine and Eszopiclone, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.

Voriconazole: Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of eszopiclone by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of eszopiclone if voriconazole is initiated, discontinued or dose changed.