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Phenibut: Difference between revisions
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Phenibut has a more complex pharmacological profile than many other [[depressants]]. | Phenibut has a more complex pharmacological profile than many other [[depressants]]. | ||
Unlike [[benzodiazepines]], for example, phenibut acts as a full [[agonist]] of the [[GABA]]<sub>B</sub> [[receptor]], similar to baclofen and high doses of [[GHB]].<ref name="eight">{{cite book | date=21 September 2010 | title=GABAb Receptor Pharmacology: A Tribute to Norman Bowery | publisher=Academic Press | isbn=9780123786487}}</ref> At higher doses, phenibut loses its selectivity of GABA<sub>B</sub>, and gains additional activity as a GABA<sub>A</sub> [[agonist]].<ref name="ZyablitsevaPavlova2010">{{cite journal|last1=Zyablitseva|first1=E. A.|last2=Pavlova|first2=I. V.|title=Effects of the GABA Receptor Agonist Phenibut on Spike Activity and Interactions between Neocortex and Hippocampus Neurons in Emotionally Negative Situations|journal=Neuroscience and Behavioral Physiology|volume=40|issue=9|year=2010|pages=1003–1011|issn=0097-0549|doi=10.1007/s11055-010-9360-y}}</ref> | Unlike [[benzodiazepines]], for example, phenibut acts as a full [[agonist]] of the [[GABA]]<sub>B</sub> [[receptor]], similar to baclofen and high doses of [[GHB]].<ref name="eight">{{cite book | date=21 September 2010 | title=GABAb Receptor Pharmacology: A Tribute to Norman Bowery | publisher=Academic Press | isbn=9780123786487}}</ref> At higher doses, phenibut loses its selectivity of GABA<sub>B</sub>, and gains additional activity as a GABA<sub>A</sub> [[agonist]].<ref name="ZyablitsevaPavlova2010">{{cite journal|last1=Zyablitseva|first1=E. A.|last2=Pavlova|first2=I. V.|title=Effects of the GABA Receptor Agonist Phenibut on Spike Activity and Interactions between Neocortex and Hippocampus Neurons in Emotionally Negative Situations|journal=Neuroscience and Behavioral Physiology|volume=40|issue=9|year=2010|pages=1003–1011|issn=0097-0549|doi=10.1007/s11055-010-9360-y}}</ref> | ||
Phenibut's effects at the GABA<sub>B</sub> receptor are responsible for its sedating effects.{{citation needed}} | |||
Recent research has shown that phenibut binds to and blocks α2δ subunit-containing voltage-dependent calcium channels (VDCCs), similarly to gabapentinoids such as [[gabapentin]] | Recent research has shown that phenibut binds to and blocks α2δ subunit-containing voltage-dependent calcium channels (VDCCs), similarly to gabapentinoids such as [[gabapentin]] | ||
and [[pregabalin]].<ref name="nine" /> Both enantiomers of phenibut show this action with similar efficacy. The R-enantiomer possesses five-fold greater affinity for α2δ subunit-containing voltage-gated calcium channels relative to the GABA<sub>B</sub> receptor, whereas the S-entantiomer does not have any efficacy at the GABA<sub>B</sub> receptor.<ref name="nine">{{cite journal | vauthors=((Dambrova, M.)), ((Zvejniece, L.)), ((Liepinsh, E.)), ((Cirule, H.)), ((Zharkova, O.)), ((Veinberg, G.)), ((Kalvinsh, I.)) | journal=European Journal of Pharmacology | title=Comparative pharmacological activity of optical isomers of phenibut | volume=583 | issue=1 | pages=128–134 | date=31 March 2008 | issn=0014-2999 | doi=10.1016/j.ejphar.2008.01.015}} | and [[pregabalin]].<ref name="nine" /> Both enantiomers of phenibut show this action with similar efficacy. The R-enantiomer possesses five-fold greater affinity for α2δ subunit-containing voltage-gated calcium channels relative to the GABA<sub>B</sub> receptor, whereas the S-entantiomer does not have any efficacy at the GABA<sub>B</sub> receptor.<ref name="nine">{{cite journal | vauthors=((Dambrova, M.)), ((Zvejniece, L.)), ((Liepinsh, E.)), ((Cirule, H.)), ((Zharkova, O.)), ((Veinberg, G.)), ((Kalvinsh, I.)) | journal=European Journal of Pharmacology | title=Comparative pharmacological activity of optical isomers of phenibut | volume=583 | issue=1 | pages=128–134 | date=31 March 2008 | issn=0014-2999 | doi=10.1016/j.ejphar.2008.01.015}}</ref> | ||
The [[pain relief|analgesic]] effects of phenibut in rodents are not mediated by the GABA<sub>B</sub> receptor but by the blockage of α2δ subunit-containing voltage-gated calcium channels.<ref name="nine" /> | The [[pain relief|analgesic]] effects of phenibut in rodents are not mediated by the GABA<sub>B</sub> receptor but by the blockage of α2δ subunit-containing voltage-gated calcium channels.<ref name="nine" /> | ||
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*'''[[Effect::Muscle cramps]]''' - Muscle cramps and joint pain are sometimes accompanied at high doses. | *'''[[Effect::Muscle cramps]]''' - Muscle cramps and joint pain are sometimes accompanied at high doses. | ||
*'''[[Effect::Difficulty urinating]]''' - This effect generally only occurs after frequent usage. | *'''[[Effect::Difficulty urinating]]''' - This effect generally only occurs after frequent usage. | ||
*'''[[Effect::Increased blood pressure]]''' | *'''[[Effect::Increased blood pressure]]''' | ||
*'''[[Effect::Temperature regulation suppression]]''' | *'''[[Effect::Temperature regulation suppression]]''' | ||
*'''[[Effect::Pupil dilation]]''' - This effect is common at high doses. | *'''[[Effect::Pupil dilation]]''' - This effect is common at high doses. | ||
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*'''[[Depressants]]''' (''[[1,4-Butanediol]], [[2M2B]], [[alcohol]],<ref>{{cite journal | vauthors=((Koski, A.)), ((Ojanpera, I.)), ((Vuori, E.)) | journal=Alcoholism: Clinical and Experimental Research | title=Alcohol and Benzodiazepines in Fatal Poisonings | volume=26 | issue=7 | pages=956–959 | date= July 2002 | url=https://onlinelibrary.wiley.com/doi/10.1111/j.1530-0277.2002.tb02627.x | issn=0145-6008 | doi=10.1111/j.1530-0277.2002.tb02627.x}}</ref> [[benzodiazepines]], [[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. | *'''[[Depressants]]''' (''[[1,4-Butanediol]], [[2M2B]], [[alcohol]],<ref>{{cite journal | vauthors=((Koski, A.)), ((Ojanpera, I.)), ((Vuori, E.)) | journal=Alcoholism: Clinical and Experimental Research | title=Alcohol and Benzodiazepines in Fatal Poisonings | volume=26 | issue=7 | pages=956–959 | date= July 2002 | url=https://onlinelibrary.wiley.com/doi/10.1111/j.1530-0277.2002.tb02627.x | issn=0145-6008 | doi=10.1111/j.1530-0277.2002.tb02627.x}}</ref> [[benzodiazepines]], [[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 a sudden loss of consciousness 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 a sudden loss of consciousness occurs, users should attempt to fall asleep in the [[recovery position]] or have a friend move them into it. | ||
*'''[[Stimulants]]''' - Phenibut is reported to enhance the positive effects of [[stimulants]] as well as reduce jitteriness and anxiety.<ref>{{Citation | title=The Drug Classroom - Phenibut: Combinations | url=https://thedrugclassroom.com/video/phenibut/}}</ref> However, this combination can be dangerous due to the risk of excessive intoxication. Stimulants mask the [[sedation|sedative]] effects of phenibut; once the stimulant wears off, the depressant effects of phenibut will be significantly increased, leading to intensified [[disinhibition]] as well as [[Phenibut#Subjective effects|other effects]]. | *'''[[Stimulants]]''' - Phenibut is reported to enhance the positive effects of [[stimulants]] as well as reduce jitteriness and anxiety.<ref>{{Citation | title=The Drug Classroom - Phenibut: Combinations | url=https://thedrugclassroom.com/video/phenibut/}}</ref> However, this combination can be dangerous due to the risk of excessive intoxication. Stimulants mask the [[sedation|sedative]] effects of phenibut; once the stimulant wears off, the depressant effects of phenibut will be significantly increased, leading to intensified [[disinhibition]] as well as [[Phenibut#Subjective effects|other effects]]. If combined, one should strictly limit themselves to a certain dose of phenibut prior to stimulant consumption and not redose. This combination can also potentially result in significant dehydration. | ||
==Legal status== | ==Legal status== | ||
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*'''Canada''': Phenibut is not a controlled substance in Canada, meaning it is legal to possess without any sort of license or prescription. {{citation needed}} | *'''Canada''': Phenibut is not a controlled substance in Canada, meaning it is legal to possess without any sort of license or prescription. {{citation needed}} | ||
*'''Germany''': Phenibut may be controlled under the NpSG (''New Psychoactive Substances Act'')<ref>{{cite web|url=https://www.gesetze-im-internet.de/npsg/anlage.html|title=Anlage NpSG|publisher=Bundesministerium der Justiz und für Verbraucherschutz|access-date=December 10, 2019|language=de}}</ref> as of July 18, 2019. <ref>{{cite web|url=http://www.bgbl.de/xaver/bgbl/start.xav?startbk=Bundesanzeiger_BGBl&jumpTo=bgbl119s1083.pdf|title=Verordnung zur Änderung der Anlage des Neue-psychoaktive-Stoffe-Gesetzes und von Anlagen des Betäubungsmittelgesetzes|publisher=Bundesanzeiger Verlag|access-date=December 28, 2019|work=Bundesgesetzblatt Jahrgang 2019 Teil I|publication-date=July 17, 2019|language=de}}</ref> If this law applies to Phenibut remains unclear.<ref>{{cite web|url=https://www.gesetze-im-internet.de/npsg/__4.html|title=§ 4 NpSG|publisher=Bundesministerium der Justiz und für Verbraucherschutz|access-date=December 10, 2019|language=de}}</ref><ref>[https://www.ift.de/fileadmin/user_upload/Literatur/Berichte/Kraus_et_al_2020_NpSG-Abschlussbericht.pdf ''Evaluation der Auswirkungen des Neue-psychoaktive-Stoffe-Gesetzes (NpSG): Abschlussbericht.'']</ref> | *'''Germany''': Phenibut may be controlled under the NpSG (''New Psychoactive Substances Act'')<ref>{{cite web|url=https://www.gesetze-im-internet.de/npsg/anlage.html|title=Anlage NpSG|publisher=Bundesministerium der Justiz und für Verbraucherschutz|access-date=December 10, 2019|language=de}}</ref> as of July 18, 2019. <ref>{{cite web|url=http://www.bgbl.de/xaver/bgbl/start.xav?startbk=Bundesanzeiger_BGBl&jumpTo=bgbl119s1083.pdf|title=Verordnung zur Änderung der Anlage des Neue-psychoaktive-Stoffe-Gesetzes und von Anlagen des Betäubungsmittelgesetzes|publisher=Bundesanzeiger Verlag|access-date=December 28, 2019|work=Bundesgesetzblatt Jahrgang 2019 Teil I|publication-date=July 17, 2019|language=de}}</ref> If this law applies to Phenibut remains unclear.<ref>{{cite web|url=https://www.gesetze-im-internet.de/npsg/__4.html|title=§ 4 NpSG|publisher=Bundesministerium der Justiz und für Verbraucherschutz|access-date=December 10, 2019|language=de}}</ref><ref>[https://www.ift.de/fileadmin/user_upload/Literatur/Berichte/Kraus_et_al_2020_NpSG-Abschlussbericht.pdf ''Evaluation der Auswirkungen des Neue-psychoaktive-Stoffe-Gesetzes (NpSG): Abschlussbericht.'']</ref> | ||
*'''Italy''': Phenibut is a Schedule 1 controlled substance.<ref>[http://www.salute.gov.it/imgs/C_17_pagineAree_3729_0_file.pdf Tabella 1](PDF) (in Italian). Ministero della Salute [Ministry of Health]. p.19. Retrieved November 24, 2020.</ref> | |||
*'''Latvia''': Phenibut is an unscheduled prescription drug, marketed as "Noofen".<ref>https://dati.zva.gov.lv/zalu-registrs/?iss=1&q=Phenibutum Database of licensed phenibut medicines and their legal status under the State Agency of Medicines of the Republic of Latvia. ''Retrieved August 26, 2023.''</ref><ref>https://likumi.lv/ta/en/en/id/50539 Active Latvian law regarding scheduled and banned substances. ''Retrieved August 26, 2023.''</ref> | |||
*'''Switzerland''': Phenibut is not controlled under Buchstabe A, B, C and D. It could be considered legal.<ref>{{cite web|url=https://www.admin.ch/opc/de/classified-compilation/20101220/index.html|title=Verordnung des EDI über die Verzeichnisse der Betäubungsmittel, psychotropen Stoffe, Vorläuferstoffe und Hilfschemikalien|publisher=Bundeskanzlei [Federal Chancellery of Switzerland]|access-date=January 1, 2020|language=de}}</ref> | *'''Switzerland''': Phenibut is not controlled under Buchstabe A, B, C and D. It could be considered legal.<ref>{{cite web|url=https://www.admin.ch/opc/de/classified-compilation/20101220/index.html|title=Verordnung des EDI über die Verzeichnisse der Betäubungsmittel, psychotropen Stoffe, Vorläuferstoffe und Hilfschemikalien|publisher=Bundeskanzlei [Federal Chancellery of Switzerland]|access-date=January 1, 2020|language=de}}</ref> | ||
*'''United Kingdom''': Phenibut is not a controlled substance in the United Kingdom. It'' may'' be illegal to produce, supply, or import this drug under the Psychoactive Substance Act 2016, which applies a blanket restriction on all "psychoactive substances" with exemptions for alcohol, nicotine and "medicinal products".<ref>{{Citation | title=Psychoactive Substances Act 2016 | url=https://www.legislation.gov.uk/ukpga/2016/2/contents/enacted}}</ref> | *'''United Kingdom''': Phenibut is not a controlled substance in the United Kingdom. It'' may'' be illegal to produce, supply, or import this drug under the Psychoactive Substance Act 2016, which applies a blanket restriction on all "psychoactive substances" with exemptions for alcohol, nicotine and "medicinal products".<ref>{{Citation | title=Psychoactive Substances Act 2016 | url=https://www.legislation.gov.uk/ukpga/2016/2/contents/enacted}}</ref> | ||
*'''United States''': Phenibut is not a controlled substance in the United States, meaning it is federally legal to possess without any sort of license or prescription.<ref name="eleven">{{Citation | title=Erowid Phenibut Vault: Legal Status | url=https://erowid.org/smarts/phenibut/phenibut_law.shtml}}</ref>Phenibut is a Schedule II controlled substance in Alabama as of November 21st, 2021.<ref>Alabama List of Controlled Substances<nowiki/>https://www.alabamapublichealth.gov/blog/assets/controlledsubstanceslist.pdf</ref> | *'''United States''': Phenibut is not a controlled substance in the United States, meaning it is federally legal to possess without any sort of license or prescription.<ref name="eleven">{{Citation | title=Erowid Phenibut Vault: Legal Status | url=https://erowid.org/smarts/phenibut/phenibut_law.shtml}}</ref>Phenibut is a Schedule II controlled substance in Alabama as of November 21st, 2021.<ref>Alabama List of Controlled Substances<nowiki/>https://www.alabamapublichealth.gov/blog/assets/controlledsubstanceslist.pdf</ref> | ||
==See also== | ==See also== | ||