Buy Eszopiclone (Lunesta) Cas 138729-47-2

Eszopiclone, sold under the brand name Lunesta among others, is a nonbenzodiazepine medication used in the treatment of short-term and long-term insomnia. It is one of the few FDA-approved hypnotic medications with a controlled substance designation that does not have restrictions on its length of use.^[2][3] Evidence supports benefits up to six months, with some studies suggesting similar efficacy after 12 months.^[4][3][5] It is taken by mouth.^[2][4]

Eszopiclone’s primary mechanism of action involves enhancing the natural effect of GABA receptors by acting as a positive allosteric modulator on GABA-A expressing neurons. This increases the frequency of the chloride channel opening when GABA is present. This is a distinguishing feature, as eszopiclone will not force sleep or act as a tranquilizer but instead encourages a positive sleep-wake routine.

Common side effects include headache, dry mouth, nausea, and dizziness.^[4] Severe side effects may include suicidal thoughts, hallucinations, and angioedema.^[4] Rapid decreasing of the dose may result in withdrawal.^[4] Eszopiclone is classified as a nonbenzodiazepine or Z-drug and a sedative and hypnotic of the cyclopyrrolone group.^[6] It is the S-stereoisomer of zopiclone.^[4][7]

Approved for medical use in the United States in 2004,^[2] eszopiclone is available as a generic medication.^[4] In 2020, it was the 232nd most commonly prescribed medication in the United States, with more than 1 million prescriptions.^[8][9] Eszopiclone is not sold in the European Union; as of 2009, the European Medicines Agency (EMA) ruled that it was too similar to zopiclone to be considered a new active substance.^[10][11][12]

A 2018 Cochrane review found that it produced moderate improvement in sleep onset and maintenance. The authors suggest that where preferred non-pharmacological treatment strategies have been exhausted, eszopiclone provides an efficient treatment for insomnia.^[13] In 2014, the US Food and Drug Administration asked that the starting dose be lowered from 2 milligrams to 1 milligram after it was observed in a study that even eight hours after taking the drug at night, some people were not able to cope with their next-day activities like driving and other activities that require full alertness.^[14]

Eszopiclone is slightly effective in the treatment of insomnia where difficulty in falling asleep is the primary complaint.^[3] The benefit over placebo was found to be of questionable clinical significance.^[3] Although the drug effect and the placebo response were rather small and of questionable clinical importance, the two together produce a reasonably large clinical response.^[3]

Sedative hypnotic drugs including eszopiclone are more commonly prescribed to the elderly than to younger patients despite benefits of medication being generally unimpressive.^[15]

In 2015, the American Geriatrics Society reviewed the safety information about eszopiclone and similar drugs and concluded that the “nonbenzodiazepine, benzodiazepine receptor agonist hypnotics (eszopiclone, zaleplon, zolpidem) are to be avoided without consideration of duration of use because of their association with harms balanced with their minimal efficacy in treating insomnia.”

The review made this determination both because of the relatively large dangers to elderly individuals from zolpidem and other “z-drugs” together with the fact the drugs have “minimal efficacy in treating insomnia.” This was a change from the 2012 AGS recommendation, which suggested limiting use to 90 days or less. The review stated: “the 90‐day‐use caveat [was] removed from nonbenzodiazepine, benzodiazepine receptor agonist hypnotics, resulting in an unambiguous ‘avoid’ statement (without caveats) because of the increase in the evidence of harm in this area since the 2012 update.”^[16]