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Talk:Pagoclone: Difference between revisions
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{{DepressantOD|GABAergics}}{{SummarySheet}} | {{DepressantOD|GABAergics}}{{SummarySheet}} | ||
{{SubstanceBox/Pagoclone}} | {{SubstanceBox/Pagoclone}} | ||
Pagoclone | '''Pagoclone''' is a non-[[benzodiazepine]] [[anxiolytic]] of the [[chemical class::cyclopyrrolone|cyclopyrrolone]] class., While it is closely related to "Z-drugs" (like [[zolpidem]] and [[zopiclone]]), pagoclone is unique in that it does not produce [[sedation|sedation]] or as much loss of [[Loss of motor control|motor control]] and [[amnesia]] that benzodiazepines and other Z-drugs do. As with many z-drugs, it is reported to cause hallucinations similar to [[Deliriant|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.<ref>Alcohol alternatives – a goal for psychopharmacology? | |||
D. J. Nutt | D. J. Nutt | ||
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Pagoclone was trialed as a drug to improve a stammerer's speech fluency, but research for this application was discontinued following disappointing results.<ref>Exploratory Randomized Clinical Study of Pagoclone in Persistent Developmental Stuttering | Pagoclone was trialed as a drug to improve a stammerer's speech fluency, but research for this application was discontinued following disappointing results.<ref>Exploratory Randomized Clinical Study of Pagoclone in Persistent Developmental Stuttering | ||
Maguire et. al. | Maguire et. al. | ||
Journal of Clinical Psychopharmacology: February 2010 - Volume 30 - Issue 1 - p 48-56 | Journal of Clinical Psychopharmacology: February 2010 - Volume 30 - Issue 1 - p 48-56 | ||
doi: 10.1097/JCP.0b013e3181caebbe</ref> | doi: 10.1097/JCP.0b013e3181caebbe</ref> | ||
==Chemistry== | ==Chemistry== | ||
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==Pharmacology== | ==Pharmacology== | ||
Pagoclone binds with roughly equivalent high affinity (0.7–9.1 nM) to the benzodiazepine binding site of human GABA<sub>A</sub> 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.<ref>The benzodiazepine binding site of GABA<sub>A</sub> receptors as a target for the development of novel anxiolytics | Pagoclone binds with roughly equivalent high affinity (0.7–9.1 nM) to the benzodiazepine binding site of human GABA<sub>A</sub> 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.<ref>The benzodiazepine binding site of GABA<sub>A</sub> receptors as a target for the development of novel anxiolytics | ||
John R Atack | John R Atack | ||
https://doi.org/10.1517/13543784.14.5.601</ref> 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.<ref>The in vivo properties of pagoclone in rat are most likely mediated by 5′-hydroxy pagoclone | https://doi.org/10.1517/13543784.14.5.601</ref> 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.<ref>The in vivo properties of pagoclone in rat are most likely mediated by 5′-hydroxy pagoclone | ||
John R. Atack et. al. | John R. Atack et. al. | ||
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==Subjective effects== | ==Subjective effects== | ||
{{Preamble/SubjectiveEffects}} | {{Preamble/SubjectiveEffects}} | ||
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}} | }} | ||
===Experience reports=== | ===Experience reports=== | ||
Anecdotal reports which describe the effects of this compound within our [[experience index]] include: | Anecdotal reports which describe the effects of this compound within our [[experience index]] include: | ||
[add] | |||
Additional experience reports can be found here: | |||
[add] | |||
==Toxicity and harm potential== | ==Toxicity and harm potential== | ||
{{Further|Responsible use#Hallucinogens}}By itself, | {{Further|Responsible use#Hallucinogens}}By itself, pagoclone likely has a [[Toxicity::low toxicity]] relative to dose. However, it is [[Toxicity::potentially [[respiratory depression|lethal]] when mixed with [[depressants]] like [[benzodiazepines]], [[alcohol]] or [[opioids]]]]. | ||
It is strongly recommended that one use [[responsible drug use|harm reduction practices]] when using this substance. | It is strongly recommended that one use [[responsible drug use|harm reduction practices]] when using this substance. | ||
===Tolerance and addiction potential=== | ===Tolerance and addiction potential=== | ||
Pagoclone is [[Addiction potential::extremely physically and psychologically addictive]]. This compound may have an even greater addictive potential than benzodiazepines. Tolerance will develop to the [[ | Pagoclone is [[Addiction potential::extremely physically and psychologically addictive]]. This compound may have an even greater addictive potential than benzodiazepines. Tolerance will develop to the [[anxiolytic]] effects [[Time to full tolerance::within a couple of weeks of daily use]]. After cessation, the tolerance returns to baseline in [[Time to zero tolerance::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 [[Cross-tolerance::all [[benzodiazepines]]]], meaning that after its consumption benzodiazepines and most other [[GABA]]genic depressants will have a reduced effect.<ref>Zopiclone and triazolam in insomnia associated with generalized anxiety disorder. If zopiclone 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/</ref> | Pagoclone presents cross-tolerance with [[Cross-tolerance::all [[benzodiazepines]]]], meaning that after its consumption benzodiazepines and most other [[GABA]]genic depressants will have a reduced effect.<ref>Zopiclone and triazolam in insomnia associated with generalized anxiety disorder. If zopiclone 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/</ref> | ||
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{{legalStub}} | {{legalStub}} | ||
*Presumably, | *Presumably, pagoclone is illegal to produce, supply, or import under the Psychoactive Substance Act, which came into effect on May 26th, 2016. | ||
==See also== | ==See also== | ||