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Gabapentin: Difference between revisions
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{{SummarySheet}} | {{SummarySheet}} | ||
{{SubstanceBox/Gabapentin}} | {{SubstanceBox/Gabapentin}} | ||
'''Gabapentin''' (also known as '''Neurontin''') is a [[psychoactive class::depressant]] substance of the [[chemical class::gabapentinoid]] class. It is a structural analog of the [[neurotransmitter]] [[GABA]] and acts by inhibiting certain calcium channels in the brain namely α2δ subunit-containing voltage-dependent calcium channels (VGCCs).<ref name="CalandreRico-Villademoros2016">{{cite journal|last1=Calandre|first1=Elena P.|last2=Rico-Villademoros|first2=Fernando|last3=Slim|first3=Mahmoud|title=Alpha2delta ligands, gabapentin, pregabalin and mirogabalin: a review of their clinical pharmacology and therapeutic use|journal=Expert Review of Neurotherapeutics|volume=16|issue=11|year=2016|pages=1263–1277|issn=1473-7175|doi=10.1080/14737175.2016.1202764}}</ref> | '''Gabapentin''' (also known as '''Neurontin''') is a [[psychoactive class::depressant]] substance of the [[chemical class::gabapentinoid]] class. It is a structural analog of the [[neurotransmitter]] [[GABA]] and acts by inhibiting certain calcium channels in the brain, namely α2δ subunit-containing voltage-dependent calcium channels (VGCCs).<ref name="CalandreRico-Villademoros2016">{{cite journal|last1=Calandre|first1=Elena P.|last2=Rico-Villademoros|first2=Fernando|last3=Slim|first3=Mahmoud|title=Alpha2delta ligands, gabapentin, pregabalin and mirogabalin: a review of their clinical pharmacology and therapeutic use|journal=Expert Review of Neurotherapeutics|volume=16|issue=11|year=2016|pages=1263–1277|issn=1473-7175|doi=10.1080/14737175.2016.1202764}}</ref> | ||
Gabapentin was originally developed to treat epilepsy and is currently FDA approved to treat postherpetic neuralgia in adults and as an adjunctive therapy in the treatment of partial onset seizures. It is often prescribed off-label for [[restless leg syndrome]], social anxiety disorder, panic disorder, and generalized anxiety disorder.<ref>{{cite book | vauthors=((Schatzberg, A. F.)), ((Cole, J. O.)), ((DeBattista, C.)) | date= 2010 | title=Manual of Clinical Psychopharmacology | publisher=American Psychiatric Pub. | isbn=9781585623778}}</ref><ref>{{cite book | vauthors=((Sobel, S. V.)) | date=5 November 2012 | title=Successful Psychopharmacology: Evidence-Based Treatment Solutions for Achieving Remission | publisher=W. W. Norton & Company | isbn=9780393708578}}</ref><ref>{{cite book | vauthors=((Richards, D.)), ((Aronson, J.)), ((Coleman, J.)), ((Reynolds, D. J.)) | date=10 November 2011 | title=Oxford Handbook of Practical Drug Therapy | publisher=OUP Oxford | isbn=9780199562855}}</ref> | Gabapentin was originally developed to treat epilepsy and is currently FDA approved to treat postherpetic neuralgia in adults and as an adjunctive therapy in the treatment of partial onset seizures. It is often prescribed off-label for [[restless leg syndrome]], social anxiety disorder, panic disorder, and generalized anxiety disorder.<ref>{{cite book | vauthors=((Schatzberg, A. F.)), ((Cole, J. O.)), ((DeBattista, C.)) | date= 2010 | title=Manual of Clinical Psychopharmacology | publisher=American Psychiatric Pub. | isbn=9781585623778}}</ref><ref>{{cite book | vauthors=((Sobel, S. V.)) | date=5 November 2012 | title=Successful Psychopharmacology: Evidence-Based Treatment Solutions for Achieving Remission | publisher=W. W. Norton & Company | isbn=9780393708578}}</ref><ref>{{cite book | vauthors=((Richards, D.)), ((Aronson, J.)), ((Coleman, J.)), ((Reynolds, D. J.)) | date=10 November 2011 | title=Oxford Handbook of Practical Drug Therapy | publisher=OUP Oxford | isbn=9780199562855}}</ref> | ||
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[[Subjective effects]] include mild to moderate [[anxiety suppression]], [[pain relief]], and [[muscle relaxation]]. Its analgesic and anxiolytic effects provide gabapentin with some recreational potential in a manner that can be compared to a mild [[benzodiazepine]]. However, these recreational effects are reported to diminish quickly with repeated usage and are typically reported by those who do not have a tolerance to this compound. | [[Subjective effects]] include mild to moderate [[anxiety suppression]], [[pain relief]], and [[muscle relaxation]]. Its analgesic and anxiolytic effects provide gabapentin with some recreational potential in a manner that can be compared to a mild [[benzodiazepine]]. However, these recreational effects are reported to diminish quickly with repeated usage and are typically reported by those who do not have a tolerance to this compound. | ||
Gabapentin is considered to have low abuse potential compared to most recreational depressants. However, chronic use can lead to physical dependence. Additionally, there is a risk of fatal overdose when it is combined with other [[depressants]] (a somewhat common practice considering its weak effects). It is highly advised to use [[harm reduction practices]] if using this substance. | Gabapentin is considered to have low abuse potential compared to most recreational depressants. However, chronic use can lead to physical dependence. Additionally, there is a increased risk of fatal overdose when it is combined with other [[depressants]] (a somewhat common practice considering its weak effects). It is highly advised to use [[harm reduction practices]] if using this substance. | ||
==Chemistry== | ==Chemistry== | ||
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It is strongly recommended that one use [[responsible drug use|harm reduction practices]] when using this drug. | It is strongly recommended that one use [[responsible drug use|harm reduction practices]] when using this drug. | ||
===Suicide=== | ===Suicide=== | ||
In 2009, the U.S. Food and Drug Administration issued a warning of an increased risk of depression and suicidal thoughts and behaviors in patients taking gabapentin (along with other [[anticonvulsant]] drugs),<ref>http://www.fda.gov/Drugs/DrugSafety/PostmarketDrugSafetyInformationforPatientsandProviders/ucm100190.htm</ref> modifying the packaging insert to reflect this. A 2010 meta-analysis confirmed the increased risk of suicide associated with gabapentin use.<ref name="Patorno2010"/> | In 2009, the U.S. Food and Drug Administration issued a warning of an increased risk of depression and suicidal thoughts and behaviors in patients taking gabapentin (along with other [[anticonvulsant]] drugs),<ref>http://www.fda.gov/Drugs/DrugSafety/PostmarketDrugSafetyInformationforPatientsandProviders/ucm100190.htm</ref> modifying the packaging insert to reflect this. A 2010 meta-analysis confirmed the increased risk of suicide associated with gabapentin use.<ref name="Patorno2010" /> | ||
In 2010, a study conducted by Patorno E, Bohn RL, Wahl PM, et al, found that the use of gabapentin compared to the use of [[topiramate]] may be associated with an increase in suicidal acts and or violent deaths.<ref>{{cite journal | vauthors=((Patorno, E.)), ((Bohn, R. L.)), ((Wahl, P. M.)), ((Avorn, J.)), ((Patrick, A. R.)), ((Liu, J.)), ((Schneeweiss, S.)) | journal=JAMA | title=Anticonvulsant Medications and the Risk of Suicide, Attempted Suicide, or Violent Death | volume=303 | issue=14 | pages=1401–1409 | date=14 April 2010 | url=https://doi.org/10.1001/jama.2010.410 | issn=0098-7484 | doi=10.1001/jama.2010.410}}</ref> | In 2010, a study conducted by Patorno E, Bohn RL, Wahl PM, et al, found that the use of gabapentin compared to the use of [[topiramate]] may be associated with an increase in suicidal acts and or violent deaths.<ref>{{cite journal | vauthors=((Patorno, E.)), ((Bohn, R. L.)), ((Wahl, P. M.)), ((Avorn, J.)), ((Patrick, A. R.)), ((Liu, J.)), ((Schneeweiss, S.)) | journal=JAMA | title=Anticonvulsant Medications and the Risk of Suicide, Attempted Suicide, or Violent Death | volume=303 | issue=14 | pages=1401–1409 | date=14 April 2010 | url=https://doi.org/10.1001/jama.2010.410 | issn=0098-7484 | doi=10.1001/jama.2010.410}}</ref> | ||
It should be noted that in both studies along with others that the patients evaluated had a higher suicide risk and the studies were both limited and imprecise.<ref name="Patorno2010"/> | It should be noted that in both studies along with others that the patients evaluated had a higher suicide risk and the studies were both limited and imprecise.<ref name="Patorno2010" /> | ||
===Lethal dosage=== | ===Lethal dosage=== | ||
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*'''Germany:''' Gabapentin is a prescription medicine, according to Anlage 1 AMVV.<ref>{{Citation | title=AMVV - Verordnung über die Verschreibungspflicht von Arzneimitteln | url=https://www.gesetze-im-internet.de/amvv/BJNR363210005.html}}</ref> | *'''Germany:''' Gabapentin is a prescription medicine, according to Anlage 1 AMVV.<ref>{{Citation | title=AMVV - Verordnung über die Verschreibungspflicht von Arzneimitteln | url=https://www.gesetze-im-internet.de/amvv/BJNR363210005.html}}</ref> | ||
*'''Switzerland:''' Gabapentin is listed as a "Abgabekategorie B" pharmaceutical, which requires a prescription.{{citation needed}} | *'''Switzerland:''' Gabapentin is listed as a "Abgabekategorie B" pharmaceutical, which requires a prescription.{{citation needed}} | ||
*'''United Kingdom''': Gabapentin is available as a prescription.<ref>[https://www.nhs.uk/medicines/baclofen/about-baclofen/ Baclofen: muscle relaxant that relieves muscle spasms - NHS]</ref> | |||
*'''United States:''' Gabapentin is not a scheduled substance but may only be sold with prescription.<ref>{{cite journal | vauthors=((Peckham, A. M.)), ((Ananickal, M. J.)), ((Sclar, D. A.)) | journal=Risk Management and Healthcare Policy | title=Gabapentin use, abuse, and the US opioid epidemic: the case for reclassification as a controlled substance and the need for pharmacovigilance | volume=11 | pages=109–116 | date=17 August 2018 | url=https://www.dovepress.com/gabapentin-use-abuse-and-the-us-opioid-epidemic-the-case-for-reclassif-peer-reviewed-fulltext-article-RMHP | doi=10.2147/RMHP.S168504}}</ref> | *'''United States:''' Gabapentin is not a scheduled substance but may only be sold with prescription.<ref>{{cite journal | vauthors=((Peckham, A. M.)), ((Ananickal, M. J.)), ((Sclar, D. A.)) | journal=Risk Management and Healthcare Policy | title=Gabapentin use, abuse, and the US opioid epidemic: the case for reclassification as a controlled substance and the need for pharmacovigilance | volume=11 | pages=109–116 | date=17 August 2018 | url=https://www.dovepress.com/gabapentin-use-abuse-and-the-us-opioid-epidemic-the-case-for-reclassif-peer-reviewed-fulltext-article-RMHP | doi=10.2147/RMHP.S168504}}</ref> | ||
**'''Exceptions:''' Gabapentin is a Schedule 5 controlled substance in: Alabama, Kentucky, Michigan, North Dakota, Tennessee, Virginia, and West Virginia. With prescription drug monitoring in: Connecticut, District of Columbia, Indiana, Kansas, Massachusetts, Minnesota, Nebraska, New Jersey, Ohio, Oregon, Utah, and Wyoming.<ref>{{cite journal | vauthors=((Collins, S.)) | journal=Pharmacy Today | title=More states make gabapentin a Schedule V Controlled Substance | volume=27 | issue=10 | pages=33 | date= October 2021 | url=https://linkinghub.elsevier.com/retrieve/pii/S1042099121007301 | issn=10420991 | doi=10.1016/j.ptdy.2021.09.016}}</ref> | **'''Exceptions:''' Gabapentin is a Schedule 5 controlled substance in: Alabama, Kentucky, Michigan, North Dakota, Tennessee, Virginia, and West Virginia. With prescription drug monitoring in: Connecticut, District of Columbia, Indiana, Kansas, Massachusetts, Minnesota, Nebraska, New Jersey, Ohio, Oregon, Utah, and Wyoming.<ref>{{cite journal | vauthors=((Collins, S.)) | journal=Pharmacy Today | title=More states make gabapentin a Schedule V Controlled Substance | volume=27 | issue=10 | pages=33 | date= October 2021 | url=https://linkinghub.elsevier.com/retrieve/pii/S1042099121007301 | issn=10420991 | doi=10.1016/j.ptdy.2021.09.016}}</ref> | ||
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*[https://en.wikipedia.org/wiki/Gabapentin Gabapentin (Wikipedia)] | *[https://en.wikipedia.org/wiki/Gabapentin Gabapentin (Wikipedia)] | ||
*[https://www.erowid.org/pharms/gabapentin/ Gabapentin (Erowid Vault)] | *[https://www.erowid.org/pharms/gabapentin/ Gabapentin (Erowid Vault)] | ||
*[https://isomerdesign.com/PiHKAL/explore.php?id=8697 Gabapentin ( | *[https://isomerdesign.com/PiHKAL/explore.php?id=8697 Gabapentin (Isomer Design)] | ||
*[https://go.drugbank.com/drugs/DB00996 Gabapentin (DrugBank)] | |||
*[https://www.drugs.com/gabapentin.html Gabapentin (Drugs.com)] | |||
*[https://drugs-forum.com/wiki/Gabapentin Gabapentin (Drugs-Forum)] | |||
==References== | ==References== | ||
<references /> | <references /> | ||
[[Category:Psychoactive substance]] | [[Category:Psychoactive substance]] | ||
[[Category:Cycloalkylamine]] | |||
[[Category:Gamma-Amino acid]] | |||
[[Category:Depressant]] | [[Category:Depressant]] | ||
[[Category:Anxiolytics]] | [[Category:Anxiolytics]] | ||
[[Category:Gabapentinoid]] | [[Category:Gabapentinoid]] | ||
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