pregabalin + riluzole

Pregabalin + riluzole is an investigational drug combination being evaluated for the treatment of peripheral neuropathic pain. This combination therapy leverages the distinct mechanisms of two established small molecules: pregabalin, a gabapentinoid, and riluzole, a benzothiazole derivative. Pregabalin acts by binding to the α2δ-1 subunit of voltage-gated calcium channels in the central nervous system, which reduces the influx of calcium into nerve terminals and subsequently inhibits the release of excitatory neurotransmitters such as glutamate and substance P. Riluzole, primarily known for its use in amyotrophic lateral sclerosis (ALS), functions by inhibiting voltage-gated sodium channels and modulating glutamatergic transmission through the inhibition of glutamate release and potentially enhancing glutamate uptake. The rationale for this combination, explored by researchers at Beijing Tiantan Hospital and Capital Medical University, is to achieve synergistic analgesia by simultaneously targeting multiple pathways involved in pain sensitization and hyperexcitability in peripheral neuropathy.

Other names

pregabalin/riluzole combinationriluzole and pregabalin