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Gabapentin: Difference between revisions
>Azed m Fixed a citation. Additonal wording and clarity. |
>Petergazer666 m Added another NCBI source confirming that Gabapentin is able to increase GABA concentrations in vivo. |
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==Pharmacology== | ==Pharmacology== | ||
Gabapentin modulates the action of [[glutamate]] decarboxylase (GAD) and branched-chain aminotransferase (BCAT), two enzymes involved in [[GABA]] biosynthesis. In human and rat studies, gabapentin was found to increase GABA biosynthesis, and to increase non-synaptic GABA neurotransmission in vitro.<ref>Mechanisms of action of gabapentin (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/9686247</ref> As the GABA system is the most prolific inhibitory receptor set within the brain, its increase in biosynthesis results in the [[sedating]] and [[Anxiety_suppression|anxiolytic]] (or [[Anxiety suppression|calming effects]]) of gabapentin on the nervous system. | Gabapentin modulates the action of [[glutamate]] decarboxylase (GAD) and branched-chain aminotransferase (BCAT), two enzymes involved in [[GABA]] biosynthesis. In human and rat studies, gabapentin was found to increase GABA biosynthesis, and to increase non-synaptic GABA neurotransmission in vitro.<ref>Mechanisms of action of gabapentin (PubMed.gov / NCBI) | http://www.ncbi.nlm.nih.gov/pubmed/9686247</ref> As the GABA system is the most prolific inhibitory receptor set within the brain, its increase in biosynthesis results in the [[sedating]] and [[Anxiety_suppression|anxiolytic]] (or [[Anxiety suppression|calming effects]]) of gabapentin on the nervous system. | ||
Another study<ref>The Impact of Gabapentin Administration on Brain GABA and Glutamate Concentrations: A 7T 1H-MRS Study (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3499716</ref> based on magnetic resonance imaging done at 7 Tesla confirms that Gabapentin appears to increase cerebral GABA concentrations acutely, in vivo, by up to 79% from baseline. | |||
Gabapentin, as a gabapentinoid, has also been shown to bind to the α2δ-1 subunit of Voltage-Gated Calcium Channels to act as a VGCC blocker, which contributes to its inhibitory, analgesic, and anxiolytic effects.<ref>The mechanisms of action of gabapentin and pregabalin. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/16376147</ref> It is uncertain exactly how this method of action contributes to gabapentin's psychoactive effects. | Gabapentin, as a gabapentinoid, has also been shown to bind to the α2δ-1 subunit of Voltage-Gated Calcium Channels to act as a VGCC blocker, which contributes to its inhibitory, analgesic, and anxiolytic effects.<ref>The mechanisms of action of gabapentin and pregabalin. (PubMed.gov / NCBI) | https://www.ncbi.nlm.nih.gov/pubmed/16376147</ref> It is uncertain exactly how this method of action contributes to gabapentin's psychoactive effects. | ||