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Pregabalin is an anticonvulsant medication used to treat neuropathic pain and fibromyalgia, as well as partial onset seizures in combination with other anticonvulsants.
Although the mechanism of action is not fully understood, studies involving structurally related drugs suggest that presynaptic binding of pregabalin to voltage-gated calcium channels is critical to the antiseizure and antinociceptive effects seen in animal models.
Pregabalin modulates the release of several excitatory neurotransmitters, including glutamate, substance-P, norepinephrine, and calcitonin gene related peptide, by binding presynaptically to the alpha2-delta subunit of voltage-gated calcium channels in the central nervous system.
Furthermore, pregabalin inhibits the trafficking of the alpha2-delta subunit from the dorsal root ganglia to the spinal dorsal horn, which may contribute to the mechanism of action. Despite being a structural derivative of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA), pregabalin does not bind to GABA or benzodiazepine receptors.
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