flupirtine

Flupirtine is a centrally acting non-opioid analgesic and muscle relaxant that was first approved in 1984 for the treatment of acute and chronic pain. It is an aminopyridine derivative and the prototype of selective neuronal potassium channel openers (SNEPCO). Flupirtine acts primarily by opening neuronal Kv7 (KCNQ) potassium channels, which stabilizes the resting membrane potential and reduces neuronal excitability. This action indirectly antagonizes N-methyl-D-aspartate (NMDA) receptors without direct binding to their site. Additionally, it has modulatory effects on GABAA receptors and upregulates Bcl-2 while increasing glutathione levels. Its unique mechanism provides analgesic as well as muscle-relaxing properties. Flupirtine was used for moderate-to-severe pain including musculoskeletal pain, migraines, cancer pain, postoperative care, gynecological indications, and spasticity-related conditions[1][2][3][4][5][6]. Due to concerns about hepatotoxicity with long-term use or high doses, its indication in Europe was restricted to short-term management of acute pain when other analgesics are unsuitable[3].

Brand names

KatadolonMetanorEfiretFlupigilTrancolong

Other names

flupirtine maleate