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Vol. 26, Art. 19 (pp. 467-499)    |    2025       

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Mechanisms of action of flupirtine, determining the possibilities of isolation of selective potassium channel blockers as a promising class of analgesics (Literature review)

Nikiforov A.S., Ivanov I.M., Yudin M.A., Konovalov A.V., Kartashev V.A.

Federal State Budgetary Establishment «State Research Testing Institute of Military Medicine» of the Ministry of Defense of the Russian Federation

Brief summary

Flupirtine is a non-opioid central analgesic from the class of neuronal potassium channel agonists. According to the results of preclinical studies, it has a pronounced analgesic effect in various experimental models of pain syndrome, has a neuroprotective effect in toxic and ischemic damage to the nervous tissue, as well as in models of neurodegenerative diseases. An additional clinically significant indication is its anticonvulsant effect. Flupirtine in the range of effective doses does not have a general toxic effect and does not cause irreversible dysfunction or structural changes. With increasing dosages, it causes depression of the central nervous system (CNS) and changes in laboratory parameters characterizing the functional state of the liver. A correlation in the manifestations of hepatotoxicity was noted with chronic administration of flupirtine to rats and mice. The calculated doses without an observed side effect with chronic administration are at least 3 maximum daily doses of the drug per person. In vitro and in vivo studies have shown no mutagenic or carcinogenic effects of the drug, nor any effect on fertility or development of offspring, with the exception of a teratogenic effect in doses toxic to the mother's body. When assessing the additive potential, flupirtine has been shown to have no ability to cause physical dependence.


Key words

flupirtine, preclinical studies, efficacy, safety, tolerability, application regimens

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