Flupirtine
Non-opioid analgesic / From Wikipedia, the free encyclopedia
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Flupirtine is an aminopyridine that functions as a centrally acting non-opioid analgesic that was originally used as an analgesic for acute and chronic pain[5] but in 2013 due to issues with liver toxicity, the European Medicines Agency restricted its use to acute pain, for no more than two weeks, and only for people who cannot use other painkillers.[6] In March 2018, marketing authorisations for flupirtine were withdrawn following a European Medicines Agency recommendation based on the finding that the restrictions introduced in 2013 had not been sufficiently followed in clinical practice, and cases of serious liver injury still occurred including liver failure.[7]
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Bioavailability | 90% (oral), 70% (rectal)[1] |
Metabolism | Hepatic to 2-amino-3-acetylamino-6-(para-fluorobenzylamino) pyridine (which has 20-30% the analgesic potential of its parent compound), para-fluorohippuric acid[2] and a mercapturic acid metabolite, presumably formed from a glutathione adduct[3] |
Elimination half-life | 6.5 hrs (average), 11.2-16.8 hrs (average 14 hrs) (elderly), 8.7-10.9 hrs (average 9.8 hrs) (in those with moderate-level renal impairment)[1] |
Excretion | 72% of flupirtine and its metabolites appear in urine and 18% appear in feces[4] |
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ECHA InfoCard | 100.054.986 |
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Formula | C15H17FN4O2 |
Molar mass | 304.325 g·mol−1 |
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Flupirtine is a selective neuronal potassium channel opener (SNEPCO) that also has NMDA receptor antagonist and GABAA modulatory properties.[8]
It first became available in Europe in 1984 under the brand name Katadolon and after it went off patent many generic brands were introduced.[9]