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Gabapentin-Friend or Foe?

Overview
Journal Pain Pract
Specialties Neurology
Psychiatry
Date 2022 Oct 27
PMID 36300903
Authors
Affiliations
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Abstract

Background: Gabapentin is a recommended first-line agent for treating neuropathic pain; however, its efficacy rate is reportedly low, and the risk of adverse events is high. A plausible explanation for this lies with its wide range of actions, the entirety of which have yet to be fully elucidated.

Methods: A review of the literature was conducted on gabapentin's known and proposed analgesic mechanisms of action, as well as potentially opposing or detrimental actions.

Results: Gabapentin's classical analgesic mechanisms involve direct attenuation of excitatory neurotransmission in the spinal cord via inhibition of neuronal ion channels, while indirect mechanisms include descending inhibition and block of injury-evoked synaptogenesis. Glial effects have also been reported; however, whether they are neuroprotective or detrimental is unknown. Furthermore, data from animal models do not reflect clinical outcomes.

Conclusions: Gabapentin's clinical use should be reconsidered according to the net effects of its numerous assumed actions, including the tripartite synapse and oligodendrocyte effects. Whether it is doing more harm than good, especially in the scenarios of incomplete or loss of response, warrants consideration when prescribing gabapentin.

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References
1.
Hayashida K, Eisenach J . Descending Noradrenergic Inhibition: An Important Mechanism of Gabapentin Analgesia in Neuropathic Pain. Adv Exp Med Biol. 2018; 1099:93-100. DOI: 10.1007/978-981-13-1756-9_8. View

2.
Gomes T, Juurlink D, Antoniou T, Mamdani M, Paterson J, van den Brink W . Gabapentin, opioids, and the risk of opioid-related death: A population-based nested case-control study. PLoS Med. 2017; 14(10):e1002396. PMC: 5626029. DOI: 10.1371/journal.pmed.1002396. View

3.
Derry S, Bell R, Straube S, Wiffen P, Aldington D, Moore R . Pregabalin for neuropathic pain in adults. Cochrane Database Syst Rev. 2019; 1:CD007076. PMC: 6353204. DOI: 10.1002/14651858.CD007076.pub3. View

4.
Chen J, Li L, Chen S, Chen H, Xie J, Sirrieh R . The α2δ-1-NMDA Receptor Complex Is Critically Involved in Neuropathic Pain Development and Gabapentin Therapeutic Actions. Cell Rep. 2018; 22(9):2307-2321. PMC: 5873963. DOI: 10.1016/j.celrep.2018.02.021. View

5.
Oka M, Itoh Y, Wada M, Yamamoto A, Fujita T . A comparison of Ca2+ channel blocking mode between gabapentin and verapamil: implication for protection against hypoxic injury in rat cerebrocortical slices. Br J Pharmacol. 2003; 139(2):435-43. PMC: 1573845. DOI: 10.1038/sj.bjp.0705246. View