Eszopiclone

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Fatal overdose may occur when GABAergic substances are combined with other depressants such as opiates, benzodiazepines, barbiturates, gabapentinoids, thienodiazepines or alcohol.^[1]

It is strongly discouraged to combine these substances, particularly in common to heavy doses.

Summary sheet: Eszopiclone

Chemical Nomenclature

Common names

Lunesta, Eszop

Substitutive name

Eszopiclone

Systematic name

(S)-6-(5-Chloro-2-pyridinyl)- 7-oxo- 6,7-dihydro- 5H-pyrrolo[3,4-b]pyrazin-5-yl- 4-methyl- 1-piperazinecarboxylate

Class Membership

Psychoactive class

Depressant / Hallucinogen

Chemical class

Cyclopyrrolone

Routes of Administration

WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section.

⇣ Oral
Dosage
Bioavailability	52 - 80%^{[citation needed]}
Threshold	.5 mg
Light	1 - 1.5 mg
Common	2 - 3 mg
Strong	4 - 5 mg
Heavy	6 mg +
Duration
Total	6 - 8 hours
Onset	10 - 20 minutes
Peak	30 - 90 minutes

DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.

Interactions

Eszopiclone (also known by the trade names Lunesta) is a non-benzodiazepine hypnotic substance of the cyclopyrrolone class that is primarily used in the treatment of insomnia. Eszopiclone is known to belong to a family of drugs colloquially known as "Z-drugs". Other Z-drugs include Zopiclone (Imovane) zaleplon (Sonata) and zolpidem (Ambien and AmbienCR).

Eszopiclone is thought to increase the normal neurotransmission of the neurotransmitter GABA in the central nervous system in a similar yet distinct way to the activity of benzodiazepines. As Eszopiclone displays heavy sedating effects, it is has been approved for and is commonly sold as a sleeping pill.^{[citation needed]}

While "Z-drugs" were initially thought to have less misuse potential than benzodiazepines, this appraisal has shifted somewhat in the last few years as a number of cases of addiction and habituation have been observed. Eszopiclone, like all "Z-drugs", is recommended to be taken on a short-term basis -- usually a week or less.^[2] Daily or continuous use of the drug is usually not advised.^[3]

Dangerous interactions

This dangerous interactions section is a stub.

As such, it may contain incomplete or invalid information. You can help by expanding upon or correcting it.

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.

Legal status

This legality section is a stub.

As such, it may contain incomplete or wrong information. You can help by expanding 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.

References

↑ Risks of Combining Depressants - TripSit
↑ http://www.nice.org.uk/nicemedia/pdf/TA077publicinfoenglish.pdf
↑
Effects of zopiclone and temazepam on sleep, behaviour and mood during the day (PubMed.gov / NCBI) |
Chemistry

Zopiclone is a hypnotic nonbenzodiazepine drug of the cyclopyrrolone class. Zopiclone and its closely related dextrorotatory S-stereoisomer eszopiclone (Lunesta) are the most popular and available cyclopyrrolone drugs. This class of drugs is named for having a pyrrolone core, a five-membered ring with a nitrogen constituent (pyrrole) and a ketone group (-one).

Pharmacology

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 GABA_A receptors and enhances GABA binding at the GABA_A receptors to produce eszopiclone's subjective effects.^{[citation needed]} Since GABA functions as the brain's predominant inhibitory neurotransmitter, this activation of receptors results in the sedative and anxiolytic effects of Eszopiclone.^{[citation needed]}

Subjective effects

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.
Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWiki contributors. As a result, they should be viewed with a healthy degree of skepticism.
It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠.
Physical effects

Sedation - Eszopiclone is extremely sedating and can put the user into an overwhelmingly lethargic state. At higher levels, this causes users to suddenly feel as if they are extremely sleep deprived and have not slept for days, forcing them to sit or lay down and feel as if they are constantly on the verge of passing out. This sense of sleep deprivation increases proportional to dosage and can eventually become powerful enough to force a person into complete unconsciousness regardless of where they are or what they are doing at that moment.

Respiratory depression

Muscle relaxation

Dizziness

Motor control loss - This effect is pronounced and comparable to the motor control loss experienced on a heavy dose of alcohol. This typically results in users stumbling and an inability to walk in a straight line. As this may easily result in injury, one should avoid walking and using stairs while on eszopiclone.

Gustatory hallucination - Eszopiclone is commonly reported to leave a strong, unpleasant metallic taste in one's mouth.

Euphoria - Some users report euphoria from eszopiclone, although this is short lived and usually exclusive to the onset of the experience and often followed by emotion suppression.

Emotion suppression - While eszopiclone primarily suppresses anxiety, it also suppresses other emotions in a similar but less intense fashion to antipsychotics.

Time compression - This effect is mostly noticeable while under the influence of a high dose.

Irritability - Combined with the strong disinhibiting effects of eszopiclone, this effect can cause people under the influence of eszopiclone to have violent behavior towards others and sometimes themselves.

Compulsive redosing
{{{2}}}
Experience reports

There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:
- Erowid Experience Vaults: Zopiclone
Toxicity and harm potential

By itself, eszopiclone likely has a low toxicity relative to dose. However, it is potentially 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.

Tolerance and addiction potential

Eszopiclone is extremely physically and psychologically addictive. This compound may have an even greater addictive potential than benzodiazepines. Tolerance will develop to the sedative-hypnotic effects within a couple of weeks of daily use. After cessation, the tolerance returns to baseline in 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 all benzodiazepines, meaning that after its consumption benzodiazepines and most other GABAgenic depressants will have a reduced effect.<ref>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. http://www.benzo.org.uk/manual/

[tripsit-1] Risks of Combining Depressants - TripSit

[2] ttp://www.nice.org.uk/nicemedia/pdf/TA077publicinfoenglish.pdf

[3] Effects of zopiclone and temazepam on sleep, behaviour and mood during the day (PubMed.gov / NCBI) |
Chemistry

Zopiclone is a hypnotic nonbenzodiazepine drug of the cyclopyrrolone class. Zopiclone and its closely related dextrorotatory S-stereoisomer eszopiclone (Lunesta) are the most popular and available cyclopyrrolone drugs. This class of drugs is named for having a pyrrolone core, a five-membered ring with a nitrogen constituent (pyrrole) and a ketone group (-one).

Pharmacology

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 GABA_A receptors and enhances GABA binding at the GABA_A receptors to produce eszopiclone's subjective effects.^{[citation needed]} Since GABA functions as the brain's predominant inhibitory neurotransmitter, this activation of receptors results in the sedative and anxiolytic effects of Eszopiclone.^{[citation needed]}

Subjective effects

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.
Disclaimer: The effects listed below cite the Subjective Effect Index (SEI), an open research literature based on anecdotal user reports and the personal analyses of PsychonautWiki contributors. As a result, they should be viewed with a healthy degree of skepticism.
It is also worth noting that these effects will not necessarily occur in a predictable or reliable manner, although higher doses are more liable to induce the full spectrum of effects. Likewise, adverse effects become increasingly likely with higher doses and may include addiction, severe injury, or death ☠.

Physical effects

Sedation - Eszopiclone is extremely sedating and can put the user into an overwhelmingly lethargic state. At higher levels, this causes users to suddenly feel as if they are extremely sleep deprived and have not slept for days, forcing them to sit or lay down and feel as if they are constantly on the verge of passing out. This sense of sleep deprivation increases proportional to dosage and can eventually become powerful enough to force a person into complete unconsciousness regardless of where they are or what they are doing at that moment.

Respiratory depression

Muscle relaxation

Dizziness

Motor control loss - This effect is pronounced and comparable to the motor control loss experienced on a heavy dose of alcohol. This typically results in users stumbling and an inability to walk in a straight line. As this may easily result in injury, one should avoid walking and using stairs while on eszopiclone.

Gustatory hallucination - Eszopiclone is commonly reported to leave a strong, unpleasant metallic taste in one's mouth.

Euphoria - Some users report euphoria from eszopiclone, although this is short lived and usually exclusive to the onset of the experience and often followed by emotion suppression.

Emotion suppression - While eszopiclone primarily suppresses anxiety, it also suppresses other emotions in a similar but less intense fashion to antipsychotics.

Time compression - This effect is mostly noticeable while under the influence of a high dose.

Irritability - Combined with the strong disinhibiting effects of eszopiclone, this effect can cause people under the influence of eszopiclone to have violent behavior towards others and sometimes themselves.

Compulsive redosing

{{{2}}}

Experience reports

There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:

Erowid Experience Vaults: Zopiclone

Toxicity and harm potential

By itself, eszopiclone likely has a low toxicity relative to dose. However, it is potentially 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.

Tolerance and addiction potential

Eszopiclone is extremely physically and psychologically addictive. This compound may have an even greater addictive potential than benzodiazepines. Tolerance will develop to the sedative-hypnotic effects within a couple of weeks of daily use. After cessation, the tolerance returns to baseline in 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 all benzodiazepines, meaning that after its consumption benzodiazepines and most other GABAgenic depressants will have a reduced effect.<ref>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. http://www.benzo.org.uk/manual/

[4] Sedation - Eszopiclone is extremely sedating and can put the user into an overwhelmingly lethargic state. At higher levels, this causes users to suddenly feel as if they are extremely sleep deprived and have not slept for days, forcing them to sit or lay down and feel as if they are constantly on the verge of passing out. This sense of sleep deprivation increases proportional to dosage and can eventually become powerful enough to force a person into complete unconsciousness regardless of where they are or what they are doing at that moment.

Respiratory depression

Muscle relaxation

Dizziness

Motor control loss - This effect is pronounced and comparable to the motor control loss experienced on a heavy dose of alcohol. This typically results in users stumbling and an inability to walk in a straight line. As this may easily result in injury, one should avoid walking and using stairs while on eszopiclone.

Gustatory hallucination - Eszopiclone is commonly reported to leave a strong, unpleasant metallic taste in one's mouth.

Euphoria - Some users report euphoria from eszopiclone, although this is short lived and usually exclusive to the onset of the experience and often followed by emotion suppression.

Emotion suppression - While eszopiclone primarily suppresses anxiety, it also suppresses other emotions in a similar but less intense fashion to antipsychotics.

Time compression - This effect is mostly noticeable while under the influence of a high dose.

Irritability - Combined with the strong disinhibiting effects of eszopiclone, this effect can cause people under the influence of eszopiclone to have violent behavior towards others and sometimes themselves.

Compulsive redosing

[5] Sedation - Eszopiclone is extremely sedating and can put the user into an overwhelmingly lethargic state. At higher levels, this causes users to suddenly feel as if they are extremely sleep deprived and have not slept for days, forcing them to sit or lay down and feel as if they are constantly on the verge of passing out. This sense of sleep deprivation increases proportional to dosage and can eventually become powerful enough to force a person into complete unconsciousness regardless of where they are or what they are doing at that moment.

[6] Respiratory depression

[7] Muscle relaxation

[8] Dizziness

[9] Motor control loss - This effect is pronounced and comparable to the motor control loss experienced on a heavy dose of alcohol. This typically results in users stumbling and an inability to walk in a straight line. As this may easily result in injury, one should avoid walking and using stairs while on eszopiclone.

[10] Gustatory hallucination - Eszopiclone is commonly reported to leave a strong, unpleasant metallic taste in one's mouth.

[11] Euphoria - Some users report euphoria from eszopiclone, although this is short lived and usually exclusive to the onset of the experience and often followed by emotion suppression.

[12] Emotion suppression - While eszopiclone primarily suppresses anxiety, it also suppresses other emotions in a similar but less intense fashion to antipsychotics.

[13] Time compression - This effect is mostly noticeable while under the influence of a high dose.

[14] Irritability - Combined with the strong disinhibiting effects of eszopiclone, this effect can cause people under the influence of eszopiclone to have violent behavior towards others and sometimes themselves.

[15] Compulsive redosing

[16] Erowid Experience Vaults: Zopiclone

[1]

[2]

[3]

Eszopiclone

Contents

Dangerous interactions

Legal status

See also

References

Chemistry

Pharmacology

Subjective effects

Physical effects

Experience reports

Toxicity and harm potential

Tolerance and addiction potential

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