Gabapentinoids: Difference between revisions

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[[File:Gabapentinoidsstructure.png|250px|thumbnail|Diagram showing the structural similarities of [[GABA|gamma-aminobutyric acid]] (GABA), [[pregabalin]] and [[gabapentin]].]]

'''Gabapentinoids''' are a chemical class of [[psychoactive substances]] derived from [[GABA|gamma-aminobutyric acid]] (GABA).~~<ref>Patel, R., & Dickenson, A. H. (2016). Mechanisms of the gabapentinoids and α2δ‐1 calcium channel subunit in neuropathic pain. Pharmacology research & perspectives, 4(2).</ref>~~Members of this class include [[gabapentin]], [[F-phenibut]], [[phenibut]] and [[pregabalin]].

'''Gabapentinoids''' are a chemical class of [[psychoactive substances]] derived from [[GABA|gamma-aminobutyric acid]] (GABA).{{citation needed}} Members of this class include [[gabapentin]], [[F-phenibut]], [[phenibut]] and [[pregabalin]].

Gabapentinoids are commonly prescribed for epilepsy, neuropathic pain, and [[restless legs syndrome]]. [[Subjective effects]] include [[sedation]], [[muscle relaxation]], and [[anxiety suppression]].

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==Pharmacology==

Gabapentinoids act by ~~blocking~~ α2δ subunit-containing voltage-dependent calcium [[receptor#Ion_channels|channels]] (VGCCs).~~{{citation needed}}~~ While all gabapentinoids block the α2δ channels, they also have unique pharmacological characteristics such as enzyme inhibition.~~{{citation needed}}~~

Gabapentinoids act by inhibiting the α2δ subunit-containing voltage-dependent calcium [[receptor#Ion_channels|channels]] (VGCCs).<ref>Patel, R., & Dickenson, A. H. (2016). Mechanisms of the gabapentinoids and α2δ‐1 calcium channel subunit in neuropathic pain. Pharmacology research & perspectives, 4(2).https://doi.org/10.1002/prp2.205</ref> While all gabapentinoids block the α2δ channels, they also have unique pharmacological characteristics such as enzyme inhibition.<ref>Goldlust, A., Su, T. Z., Welty, D. F., Taylor, C. P., & Oxender, D. L. (1995). Effects of anticonvulsant drug gabapentin on the enzymes in metabolic pathways of glutamate and GABA. Epilepsy research, 22(1), 1-11.https://doi.org/10.1016/0920-1211(95)00028-9</ref>

==Examples==

*[[F-Phenibut]]

*[[Gabapentin]]

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==See also==

*[[Responsible use]]

*[[Depressants]]

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==External links==

*[https://en.wikipedia.org/wiki/Gabapentinoid Gabapentinoid (Wikipedia)]

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[[Category:Chemical class]]

[[Category:Pharmacology]]

~~<references />~~

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 [[File:Gabapentinoidsstructure.png|250px|thumbnail|Diagram showing the structural similarities of [[GABA|gamma-aminobutyric acid]] (GABA), [[pregabalin]] and [[gabapentin]].]]
-'''Gabapentinoids''' are a chemical class of [[psychoactive substances]] derived from [[GABA|gamma-aminobutyric acid]] (GABA).<ref>Patel, R., & Dickenson, A. H. (2016). Mechanisms of the gabapentinoids and α2δ‐1 calcium channel subunit in neuropathic pain. Pharmacology research & perspectives, 4(2).</ref>Members of this class include [[gabapentin]], [[F-phenibut]], [[phenibut]] and [[pregabalin]].
+'''Gabapentinoids''' are a chemical class of [[psychoactive substances]] derived from [[GABA|gamma-aminobutyric acid]] (GABA).{{citation needed}} Members of this class include [[gabapentin]], [[F-phenibut]], [[phenibut]] and [[pregabalin]].
 Gabapentinoids are commonly prescribed for epilepsy, neuropathic pain, and [[restless legs syndrome]]. [[Subjective effects]] include [[sedation]], [[muscle relaxation]], and [[anxiety suppression]].
@@ Line 12: / Line 12: @@
 ==Pharmacology==
-Gabapentinoids act by blocking α2δ subunit-containing voltage-dependent calcium [[receptor#Ion_channels|channels]] (VGCCs).{{citation needed}} While all gabapentinoids block the α2δ channels, they also have unique pharmacological characteristics such as enzyme inhibition.{{citation needed}}
+Gabapentinoids act by inhibiting the α2δ subunit-containing voltage-dependent calcium [[receptor#Ion_channels|channels]] (VGCCs).<ref>Patel, R., & Dickenson, A. H. (2016). Mechanisms of the gabapentinoids and α2δ‐1 calcium channel subunit in neuropathic pain. Pharmacology research & perspectives, 4(2).https://doi.org/10.1002/prp2.205</ref> While all gabapentinoids block the α2δ channels, they also have unique pharmacological characteristics such as enzyme inhibition.<ref>Goldlust, A., Su, T. Z., Welty, D. F., Taylor, C. P., & Oxender, D. L. (1995). Effects of anticonvulsant drug gabapentin on the enzymes in metabolic pathways of glutamate and GABA. Epilepsy research, 22(1), 1-11.https://doi.org/10.1016/0920-1211(95)00028-9</ref>
 ==Examples==
 *[[F-Phenibut]]
 *[[Gabapentin]]
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 ==See also==
 *[[Responsible use]]
 *[[Depressants]]
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 ==External links==
 *[https://en.wikipedia.org/wiki/Gabapentinoid Gabapentinoid (Wikipedia)]
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 [[Category:Chemical class]]
 [[Category:Pharmacology]]
-<references />