Eszopiclone

Eszopiclone, the active isomer of zopiclone, introduces itself with a rapid descent toward sleep that, at therapeutic doses, is its entire purpose and its complete experiential profile. Within fifteen to thirty minutes of oral ingestion, a heavy drowsiness settles over the mind and body. The eyelids grow leaden. Thoughts lose their structure and urgency, loosening into the associative drift that normally characterizes the moments before sleep. The world softens, sounds recede, and the distance between wakefulness and unconsciousness narrows rapidly. At a standard dose, sleep claims consciousness before there is much else to report, aside from a persistent, metallic taste in the mouth that is eszopiclone's calling card.

At higher doses, or when the user resists the pull toward sleep, the experience changes character. The sedation deepens but does not resolve into sleep, and in this twilight state, a deliriant quality emerges. Perception becomes unreliable. Shadows may move at the periphery of vision. Objects in the room may appear to shift position or transform into something else when regarded from the corner of the eye. Conversations may occur with people who are not present, their contributions seeming perfectly natural in the moment and bizarre in retrospect. Amnesia is profound: entire episodes of complex behavior, including walking, eating, driving, or sending messages, can unfold without any subsequent memory of having occurred.

The physical effects are dominated by sedation and motor impairment. Coordination deteriorates significantly. Speech becomes slurred and effortful. Balance is compromised, and walking, if attempted, has a lurching, unsteady quality. The metallic taste persists and can be quite unpleasant. Muscle relaxation is pronounced, contributing to the difficulty of voluntary movement.

The duration of the primary effects is six to eight hours, corresponding to a normal sleep period. Upon waking, there may be residual grogginess, impaired coordination, and the persistent metallic taste that can linger well into the following day. If the experience involved a period of waking delirium, the memory gaps are the most notable aftermath, black holes in the timeline of the night that may be filled only by the accounts of others or by the evidence of actions taken. The overall character of eszopiclone at therapeutic doses is simply that of an effective sleep inducer. At higher doses, it becomes something considerably stranger and more dangerous, a reminder that the boundary between sleep and delirium is pharmacologically thinner than it appears.

Eszopiclone, although structurally different from benzodiazepines, shares an almost identical pharmacological profile to them. Its mechanism of action works by binding to the same site as benzodiazepines and acts as a full agonist, which in turn positively modulates benzodiazepine-sensitive GABAA receptors and enhances GABA binding at the GABAA receptors to produce Eszopiclone's subjective effects. Since GABA functions as the brain's predominant inhibitory neurotransmitter, this activation of receptors results in the sedative and anxiolytic effects of Eszopiclone.

In comparison to other substances of a similar nature such as benzodiazepines, Eszopiclone is commonly reported to present significantly more amnesic and disinhibiting effects in a manner similar to alcohol.

By itself,low toxicity relative to dose. However, it is lethal when mixed with depressants like benzodiazepines, alcohol or opioids]]. When combined with one or several of these drugs the already existing chance of a having a "black-out" is significantly increased, leaving the user with very little to no memory of the events that occurred whilst under the influence of Eszopiclone alone or combined with most other CNS depressants. Users have reported taking Eszopiclone in combination with alcohol in an attempt to treat hangovers with varying degrees of success. It is strongly recommended that one use harm reduction practices when using this substance. -extremely physically and psychologically addictive. This compound may have an even greater addictive potential than benzodiazepines. Tolerance will develop to the sedative-within a couple of weeks of daily use. After cessation,7 - 14 days. Withdrawal symptoms or rebound symptoms may occur after ceasing usage abruptly following a few weeks or longer of steady dosing, and may necessitate a gradual dose reduction. Eszopiclone presents cross-tolerance with Cross-all benzodiazepines, meaning that after its consumption benzodiazepines and most other GABAgenic depressants will have a reduced effect.Eszopiclone and triazolam in insomnia associated with generalized anxiety disorder. If Eszopiclone has been taken for more than a few weeks, then the medication should be gradually reduced or preferably crossed over to an equivalent dose of diazepam (Valium) which has a much longer half-life, making withdrawal easier. One should then gradually taper the dose over a period of several months to avoid extremely severe and unpleasant withdrawal symptoms which can last up to two years after withdrawal if the withdrawal is done too abruptly.

• Depressants** (1,4-Butanediol, 2-methyl-2-butanol, alcohol, barbiturates, GHB/GBL, methaqualone, opioids) - This combination can result in dangerous or even fatal levels of respiratory depression. These substances potentiate the muscle relaxation, sedation and amnesia caused by one another and can lead to unexpected loss of consciousness at high doses. There is also an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.

• Dissociatives** - This combination can result in an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If this occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.

• United States:** On Dec 15, 2004, the United States released Eszopiclone as a treatment for insomnia. It is currently a Schedule 4 controlled substance, because it has abuse potential, just as benzodiazepines do. Possession without a prescription can lead to drug charges.

• Responsible use

• Depressants

• Z-drugs

• Benzodiazepines

• Eszopiclone (Wikipedia)

• Zopiclone/Eszopiclone (Erowid Vault)

• Eszopiclone (Tripsit)

In a controversial 2009 article in the New England Journal of Medicine, "Lost in Transmission — FDA Drug Information That Never Reaches Clinicians", it was reported that the largest of three Lunesta trials found that compared to placebo Lunesta "was superior to placebo" while it only shortened initial time falling asleep by 15 minutes on average. "Clinicians who are interested in the drug's efficacy cannot find efficacy information in the label: it states only that Lunesta is superior to placebo. The FDA's medical review provides efficacy data, albeit not until page 306 of the 403-page document. In the longest, largest phase 3 trial, patients in the Lunesta group reported falling asleep an average of 15 minutes faster and sleeping an average of 37 minutes longer than those in the placebo group. However, on average, Lunesta patients still met criteria for insomnia and reported no clinically meaningful improvement in next-day alertness or functioning."

Availability in Europe On September 11, 2007, Sepracor signed a marketing deal with British pharmaceutical company GlaxoSmithKline for the rights to sell eszopiclone (under the name Lunivia rather than Lunesta) in Europe. Sepracor was expected to receive approximately $155 million if the deal went through. In 2008 Sepracor submitted an application to the EMA (the European Union's equivalent to the U.S. FDA) for authorization to market the drug in the EU, and initially received a favorable response. However, Sepracor withdrew its authorization application in 2009 after the EMA stated it would not be granting eszopiclone 'new active substance' status, as it was essentially pharmacologically and therapeutically too similar to zopiclone to be considered a new patentable product. Since the patent on zopiclone has expired, this ruling would have allowed rival companies to also legally produce cheaper generic versions of eszopiclone for the European market. As of November2012, Sepracor has not resubmitted its authorization application and eszopiclone is not available in Europe. The deal with GSK fell through, and GSK instead launched a $3.3 billion deal to market Actelion's almorexant sleeping tablet, which entered phase 3 medical trials before development was abandoned due to side effects.

Since 2020 eszopiclone is available under the brand name Esogno in various European countries marketed by GL Pharma.