Latest research on 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.

Latest findings

Several pharmacological therapies for insomnia have been formulated, including benzodiazepine receptor antagonists (BzRAs) (eg, benzodiazepines and nonbenzodiazepine sedative-hypnotics, such as Zolpidem, Zaleplon, and Eszopiclone), Melatonin, Melatonin-receptor agonists, and various antidepressant medications including Quetiapine, Amitriptyline, Mirtazapine, and Trazodone. [source, 2016]
However, if pharmacological therapy is indicated, the current AASM guidelines recommend nonbenzodiazepine hypnotics (ie, Zolpidem, Zaleplon, Eszopiclone) or Melatonin MT1 and MT2 receptor agonists (ie, ramelteon) as first-line agents, followed by sedating antidepressants and benzodiazepines for patients failing first-line therapies. [source, 2016]
The exposure included benzodiazepines and non-benzodiazepine hypnotics that bind to the gamma-aminobutyric acid (GABA) receptor, such as Zolpidem, Zaleplon, and Eszopiclone. [source, 2016]
Investigators were instructed to use benzodiazepines sparingly; sedative-hypnotics (e.g. Eszopiclone, Zolpidem) were permitted, as needed, for insomnia. [source, 2016]
Sleep aids directed toward GABAA receptors, such as Zolpidem, Eszopiclone, and Zaleplon, are commonly used despite a paucity of published reports on the drug’s effects on metabolic processes. [source, 2016]
Medications with psychotropic activity were not allowed, with the following exceptions: Lorazepam for control of agitation, irritability, hostility, or restlessness; Zolpidem, Zaleplon, chloral hydrate, or Eszopiclone for insomnia; and Diphenhydramine, Benztropine, or Propranolol for EPS. [source, 2016]
Exclusion criteria also included history of nonresponse to two or more antidepressants, use of psychoactive drugs (within 2 weeks of the study), or requiring concomitant treatment with prohibited medications (exceptions were Eszopiclone, zopiclone, Zaleplon, Zolpidem, or Zolpidem extended release). [source, 2015]
Additionally, recent clinical data have suggested that coadministration of the benzodiazepine-site PAM Eszopiclone with SSRIs can lead to significantly greater treatment response, as well as faster onset of efficacy. [source, 2015]
Therefore, treatment with the benzodiazepine-site PAMs, such as Alprazolam or Eszopiclone as an adjuvant may be effective in treating at least some aspects of MDD, although it remains unclear whether Alprazolam is effective in attenuating the core mood symptoms. [source, 2015]
Taken together, these data suggest that increased activity at GABAergic receptors is beneficial in a few cases, eg, with Alprazolam as a standalone treatment and Eszopiclone as an adjuvant. [source, 2015]