gabapentinoider

Gabapentinoider, or gabapentinoids, are a class of medications that act on the nervous system to reduce excitability associated with nerve signaling. They do not bind to GABA receptors, but they bind to the alpha-2-delta subunit of voltage-gated calcium channels, which modulates neurotransmitter release and neuronal excitability.

Common clinical uses focus on neuropathic pain and seizures. Gabapentinoider are frequently prescribed for conditions such as diabetic neuropathy and postherpetic neuralgia, and they are used as adjunctive therapy for partial-onset seizures. Some agents in the class have been explored for off-label uses, including anxiety disorders and sleep disturbances, though evidence for non‑approved indications varies.

Major members of the class include gabapentin, pregabalin, and the gabapentin enacarbil prodrug. A newer agent, mirogabalin, has been studied for neuropathic pain with differences in binding affinity to subunits, affecting efficacy and tolerability profiles. Pharmacokinetic properties differ among members: pregabalin generally shows linear pharmacokinetics, while gabapentin has nonlinear absorption at higher doses; both are primarily excreted unchanged by the kidneys and require dose adjustment in renal impairment.

Safety and regulation revolve around central nervous system effects and misuse potential. Common adverse effects are dizziness, somnolence, fatigue, and ataxia. Caution is advised when combined with central depressants or opioids, and there is awareness of withdrawal symptoms if used long-term. Regulatory status varies by country, with some gabapentinoider receiving controlled-substance scheduling in certain jurisdictions and ongoing monitoring for misuse.