Description
Gabapentin exhibits antiepileptic/anticonvulsant, sedative, analgesic, and antinociceptive activities. Gabapentin is a GABA analog that does not bind GABA receptors. Gabapentin binds the α2δ subunit of voltage-gated Ca2+ channels, decreasing Ca2+ currents and inhibiting Ca2+ signaling; gabapentin also activates adenosine A1 receptors, binds NMDA receptors, and potentiates the effects of GABA signaling. Gabapentin is clinically used to prevent seizures and to treat neuropathic, inflammatory, and cancer-related pain.
References
Kukkar A, Bali A, Singh N, et al. Implications and mechanism of action of gabapentin in neuropathic pain. Arch Pharm Res. 2013 Mar;36(3):237-51. PMID: 23435945.
Davies A, Hendrich J, Van Minh AT, et al. Functional biology of the alpha(2)delta subunits of voltage-gated calcium channels. Trends Pharmacol Sci. 2007 May;28(5):220-8. PMID: 17403543.
Johannessen SI, Ben-Menachem E. Management of focal-onset seizures: an update on drug treatment. Drugs. 2006;66(13):1701-25. PMID: 16978035.
Ho KY, Gan TJ, Habib AS. Gabapentin and postoperative pain--a systematic review of randomized controlled trials. Pain. 2006 Dec 15;126(1-3):91-101. PMID: 16846695.
