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Home / Drugs / Starting with E / Eszopiclone

Eszopiclone, marketed by Sepracor under the brand-name Lunesta, is a nonbenzodiazepine hypnotic agent (viz., a sedative) used as a treatment for insomnia. Eszopiclone is the active stereoisomer of zopiclone, and belongs to the class of drugs known as cyclopyrrones. Its main selling point is that it is approved by the U.S. Food and Drug Administration for long-term use, unlike almost all other hypnotic sedatives, which are approved only for the relief of short-term (6-8 weeks) insomnia.
CategoriesHypnotics and Sedatives
ManufacturersSepracor inc
Sepracor Inc.
PackagersA-S Medication Solutions LLC
Caremark LLC
Centaur Pharmaceuticals Pvt Ltd.
DispenseXpress Inc.
Dispensing Solutions
Diversified Healthcare Services Inc.
H.J. Harkins Co. Inc.
Innoviant Pharmacy Inc.
Lake Erie Medical and Surgical Supply
Lupin Pharmaceuticals Inc.
Mckesson Corp.
Murfreesboro Pharmaceutical Nursing Supply
Nucare Pharmaceuticals Inc.
Palmetto Pharmaceuticals Inc.
Patheon Inc.
PD-Rx Pharmaceuticals Inc.
Physicians Total Care Inc.
Rebel Distributors Corp.
Sepracor Pharmaceuticals Inc.
Southwood Pharmaceuticals
Stat Rx Usa


For the treatment of insomnia


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 (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. 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.


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


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


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.