Gabapentin: Difference between revisions

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'''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>Manual of Clinical Psychopharmacology | https://books.google.co.uk/books?id=D3zz1NCm3qcC&pg=PA345&hl=en</ref><ref>Successful Psychopharmacology: Evidence-Based Treatment Solutions for Achieving Remission | https://books.google.co.uk/books?id=dnAlO_Veu2QC&pg=PA124&hl=en</ref><ref>https://books.google.co.uk/books?id=82oiYYHGNTQC&pg=PA765&hl=en</ref> However Gabapentin's efficacy in the treatment of anxiety disorders is unclear as the evidence is "somewhat mixed".<ref>[https://www.ncbi.nlm.nih.gov/pubmed/17502773] The role of anticonvulsants in anxiety disorders: a critical review of the evidence.</ref><ref>[https://www.jmcp.org/doi/abs/10.18553/jmcp.2002.8.4.266] Gabapentin Use in a Managed Medicaid Population</ref><ref>[https://annals.org/aim/fullarticle/727539/narrative-review-promotion-gabapentin-analysis-internal-industry-documents] Promotion of Gabapentin</ref><ref>Restless legs syndrome: clinical presentation diagnosis and treatment | http://www.sleep-journal.com/article/S1389-9457(15)00647-4/abstract</ref> It is recommended as a first line agent for the treatment of neuropathic pain arising from diabetic neuropathy, post-herpetic neuralgia, and central neuropathic pain.<ref>EFNS guidelines on the pharmacological treatment of neuropathic pain: 2010 revision (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/20402746</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>Manual of Clinical Psychopharmacology | https://books.google.co.uk/books?id=D3zz1NCm3qcC&pg=PA345&hl=en</ref><ref>Successful Psychopharmacology: Evidence-Based Treatment Solutions for Achieving Remission | https://books.google.co.uk/books?id=dnAlO_Veu2QC&pg=PA124&hl=en</ref><ref>https://books.google.co.uk/books?id=82oiYYHGNTQC&pg=PA765&hl=en</ref>

[[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 diminish very quickly with repeated usage and are most commonly 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 lethal overdose when it is combined with other depressants (a relatively common practice considering its weak effects). As a result, it is highly advised to use [[harm reduction practices]] if using this substance.

However Gabapentin's efficacy in the treatment of anxiety disorders is unclear as the evidence is "somewhat mixed".<ref>[https://www.ncbi.nlm.nih.gov/pubmed/17502773] The role of anticonvulsants in anxiety disorders: a critical review of the evidence.</ref><ref>[https://www.jmcp.org/doi/abs/10.18553/jmcp.2002.8.4.266] Gabapentin Use in a Managed Medicaid Population</ref><ref>[https://annals.org/aim/fullarticle/727539/narrative-review-promotion-gabapentin-analysis-internal-industry-documents] Promotion of Gabapentin</ref><ref>Restless legs syndrome: clinical presentation diagnosis and treatment | http://www.sleep-journal.com/article/S1389-9457(15)00647-4/abstract</ref> It is recommended as a first line agent for the treatment of neuropathic pain arising from diabetic neuropathy, post-herpetic neuralgia, and central neuropathic pain.<ref>EFNS guidelines on the pharmacological treatment of neuropathic pain: 2010 revision (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/20402746</ref>

[[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 lethal overdose when it is combined with other [[depressants]] (a relatively common practice considering its weak effects). As a result, it is highly advised to use [[harm reduction practices]] if using this substance.

==Chemistry==

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 '''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>Manual of Clinical Psychopharmacology | https://books.google.co.uk/books?id=D3zz1NCm3qcC&pg=PA345&hl=en</ref><ref>Successful Psychopharmacology: Evidence-Based Treatment Solutions for Achieving Remission | https://books.google.co.uk/books?id=dnAlO_Veu2QC&pg=PA124&hl=en</ref><ref>https://books.google.co.uk/books?id=82oiYYHGNTQC&pg=PA765&hl=en</ref> However Gabapentin's efficacy in the treatment of anxiety disorders is unclear as the evidence is "somewhat mixed".<ref>[https://www.ncbi.nlm.nih.gov/pubmed/17502773] The role of anticonvulsants in anxiety disorders: a critical review of the evidence.</ref><ref>[https://www.jmcp.org/doi/abs/10.18553/jmcp.2002.8.4.266] Gabapentin Use in a Managed Medicaid Population</ref><ref>[https://annals.org/aim/fullarticle/727539/narrative-review-promotion-gabapentin-analysis-internal-industry-documents] Promotion of Gabapentin</ref><ref>Restless legs syndrome: clinical presentation diagnosis and treatment | http://www.sleep-journal.com/article/S1389-9457(15)00647-4/abstract</ref> It is recommended as a first line agent for the treatment of neuropathic pain arising from diabetic neuropathy, post-herpetic neuralgia, and central neuropathic pain.<ref>EFNS guidelines on the pharmacological treatment of neuropathic pain: 2010 revision (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/20402746</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>Manual of Clinical Psychopharmacology | https://books.google.co.uk/books?id=D3zz1NCm3qcC&pg=PA345&hl=en</ref><ref>Successful Psychopharmacology: Evidence-Based Treatment Solutions for Achieving Remission | https://books.google.co.uk/books?id=dnAlO_Veu2QC&pg=PA124&hl=en</ref><ref>https://books.google.co.uk/books?id=82oiYYHGNTQC&pg=PA765&hl=en</ref>
-[[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 diminish very quickly with repeated usage and are most commonly 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 lethal overdose when it is combined with other depressants (a relatively common practice considering its weak effects). As a result, it is highly advised to use [[harm reduction practices]] if using this substance.
+However Gabapentin's efficacy in the treatment of anxiety disorders is unclear as the evidence is "somewhat mixed".<ref>[https://www.ncbi.nlm.nih.gov/pubmed/17502773] The role of anticonvulsants in anxiety disorders: a critical review of the evidence.</ref><ref>[https://www.jmcp.org/doi/abs/10.18553/jmcp.2002.8.4.266] Gabapentin Use in a Managed Medicaid Population</ref><ref>[https://annals.org/aim/fullarticle/727539/narrative-review-promotion-gabapentin-analysis-internal-industry-documents] Promotion of Gabapentin</ref><ref>Restless legs syndrome: clinical presentation diagnosis and treatment | http://www.sleep-journal.com/article/S1389-9457(15)00647-4/abstract</ref> It is recommended as a first line agent for the treatment of neuropathic pain arising from diabetic neuropathy, post-herpetic neuralgia, and central neuropathic pain.<ref>EFNS guidelines on the pharmacological treatment of neuropathic pain: 2010 revision (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/20402746</ref>
+[[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 lethal overdose when it is combined with other [[depressants]] (a relatively common practice considering its weak effects). As a result, it is highly advised to use [[harm reduction practices]] if using this substance.
 ==Chemistry==