Gabapentin Mechanism Of Action

The precise mechanisms by which gabapentin produces its analgesic and antiepileptic actions are unknown.

Gabapentin is structurally related to theneurotransmitter gamma-aminobutyric acid (GABA) but has no effect on GABA binding, uptake, or degradation. In vitro studies have shown that gabapentin binds with high-affinity to the α2δ subunit of voltage-activated calcium channels; however, the relationship of this binding to the therapeutic effects of gabapentin is unknown.

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