Talk:Pagoclone

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

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

Summary sheet: Pagoclone

Template:SubstanceBox/Pagoclone

Pagoclone is a non-benzodiazepine anxiolytic of the cyclopyrrolone class., While it is closely related to "Z-drugs" (like zolpidem and zopiclone), pagoclone is unique in that it does not produce sedation or as much loss of motor control and amnesia that benzodiazepines and other Z-drugs do. As with many z-drugs, it is reported to cause hallucinations similar to deliriants, albeit with much less pronounced effects.

Pagoclone has been considered by David Nutt, in his search for alcohol alternatives, as a useful base from which to derive viable alternatives. This seems to indicate Pagoclone itself is not a a viable candidate, which may be due to it's proximity to compounds with much abuse potential (e.g. benzodiazepines, z-drugs).

Pagoclone was trialed as a drug to improve a stammerer's speech fluency, but research for this application was discontinued following disappointing results.

Chemistry

Pagoclone is a hypnotic nonbenzodiazepine drug of the cyclopyrrolone class.

Pharmacology

Pagoclone binds with roughly equivalent high affinity (0.7–9.1 nM) to the benzodiazepine binding site of human GABA_A receptors containing either an α1, α2, α3 or α5 subunit. It is a partial agonist at α1-, α2- and α5-containing GABAA receptors and a full agonist at receptors containing an α3 subunit. In rats 5′-hydroxypagoclone was identified as a major metabolite. This metabolite has a considerably greater efficacy at the α1 subtype than the parent compound and was shown to have significant anxiolytic-like activity and to produce sedation.

Subjective effects

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 - zopiclone 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 zopiclone.
  • Gustatory hallucination - Zopiclone is sometimes reported to leave a metallic taste in one's mouth.

Visual effects

• • Shadow people
  • Acuity suppression
  • Drifting (melting, breathing, morphing and flowing) - Visual drifting effects are the most prominent visual effects of this substance. They typically occur at strong doses, or when the user resists the urge to sleep.. They are similar to the distortions produced zolpidem and are usually less pronounced than those of deliriants. Like deliriant visuals, they are most prominent in low lighting. Depending on dose and lighting, they can be described as slow or fast in speed, static in permanence, smooth in motion, realistic in appearance, and simplistic or intricate.
  • External hallucinations - At very high doses, zopiclone can produce external hallucinations that are similar to, but less pronounced than those of deliriants.
  • Tracers - This effect is mild and typically only experienced at high doses.

Cognitive effects

• The cognitive effects of zopiclone can be broken down into several components which progressively intensify proportional to dosage. The general head space of zopiclone is described by many as one of intense sedation, decreased inhibition and severe amnesia. It produces a large number of cognitive effects typical of most GABA-ergic depressants.
  • Amnesia - Compared to benzodiazepines, zopiclone can produce amnesia at much lower doses. One may potentially not remember exactly what happened while under the influence of a common dose. This is usually less intense than the amnesia produced by zolpidem.
  • Anxiety suppression
  • Thought deceleration
  • Disinhibition
  • Delusion
  • Delirium
  • Analysis suppression
  • Euphoria - Some users report euphoria from zopiclone, although this is short lived and usually exclusive to the onset of the experience and often followed by emotion suppression.
  • Emotion suppression - While zopiclone 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 zopiclone, this effect can cause people under the influence of zopiclone to have violent behavior towards others and sometimes themselves.
  • Increased music appreciation
  • Compulsive redosing

Experience reports

Anecdotal reports which describe the effects of this compound within our experience index include:

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Additional experience reports can be found here:

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Toxicity and harm potential

Further information: Responsible use § Hallucinogens

By itself, pagoclone likely has a low toxicity relative to dose. However, it is potentially lethal when mixed with depressants like benzodiazepines, alcohol or opioids.

It is strongly recommended that one use harm reduction practices when using this substance.

Tolerance and addiction potential

Pagoclone is extremely physically and psychologically addictive. This compound may have an even greater addictive potential than benzodiazepines. Tolerance will develop to the anxiolytic 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.

Pagoclone presents cross-tolerance with all benzodiazepines, meaning that after its consumption benzodiazepines and most other GABAgenic depressants will have a reduced effect.

Dangerous interactions

Warning: Many psychoactive substances that are reasonably safe to use on their own can suddenly become dangerous and even life-threatening when combined with certain other substances. The following list provides some known dangerous interactions (although it is not guaranteed to include all of them).

Always conduct independent research (e.g. Google, DuckDuckGo, PubMed) to ensure that a combination of two or more substances is safe to consume. Some of the listed interactions have been sourced from TripSit.

• 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.

• Presumably, pagoclone is illegal to produce, supply, or import under the Psychoactive Substance Act, which came into effect on May 26th, 2016.

See also

• Responsible use
• Depressants
• Z-drugs
• Benzodiazepines

External links

• Pagoclone (Wikipedia)
• Pagoclone (Isomer Design)