Mechanisms of the antinociceptive action of gabapentin.

doi:10.1254/JPHS.CR0050020

Paper

Mechanisms of the antinociceptive action of gabapentin.

Published 2006 · Jen-Kun Cheng, L. Chiou

Journal of pharmacological sciences

Q2 SJR score

241

Citations

9

Influential Citations

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Abstract

Gabapentin, a gamma-aminobutyric acid (GABA) analogue anticonvulsant, is also an effective analgesic agent in neuropathic and inflammatory, but not acute, pain systemically and intrathecally. Other clinical indications such as anxiety, bipolar disorder, and hot flashes have also been proposed. Since gabapentin was developed, several hypotheses had been proposed for its action mechanisms. They include selectively activating the heterodimeric GABA(B) receptors consisting of GABA(B1a) and GABA(B2) subunits, selectively enhancing the NMDA current at GABAergic interneurons, or blocking AMPA-receptor-mediated transmission in the spinal cord, binding to the L-alpha-amino acid transporter, activating ATP-sensitive K(+) channels, activating hyperpolarization-activated cation channels, and modulating Ca(2+) current by selectively binding to the specific binding site of [(3)H]gabapentin, the alpha(2)delta subunit of voltage-dependent Ca(2+) channels. Different mechanisms might be involved in different therapeutic actions of gabapentin. In this review, we summarized the recent progress in the findings proposed for the antinociceptive action mechanisms of gabapentin and suggest that the alpha(2)delta subunit of spinal N-type Ca(2+) channels is very likely the analgesic action target of gabapentin.

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Study Snapshot

Gabapentin's analgesic action likely involves targeting the alpha(2)delta subunit of spinal N-type Ca(2+) channels, which play a role in neuropathic and inflammatory pain.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Mechanisms of the antinociceptive action of gabapentin.

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References

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Citations

Role of Gabapentin in Traumatic Brain Injury: A Prospective Comparative Study

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Feline chronic gingivostomatitis (FCGS) is an immune-mediated disease with surgical extraction of teeth as the mainstay of treatment, and immunomodulation using mesenchymal stromal cell therapy offers an alternative for refractory patients.

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IL-10/-endorphin reduces pain through microglia-dependent mechanisms, with various medications and non-pharmacological treatments also benefiting from this process.

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HCN channel blockers may provide a novel approach for treating human absence seizures, while HCN isoform-selective drugs could enhance understanding of their role in absence seizure generation and maintenance.

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Gabapentin-Induced Overflow Urinary Incontinence: A Case Report and Review of the Literature

Gabapentin can cause overflow urinary incontinence, but pregabalin can improve pain control without recurrence.

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A single oral dose of gabapentin improves diastolic function evaluation on echocardiogram in healthy cats without causing adverse effects on cardiovascular hemodynamics.