NMDA receptor literature survey and GABAA receptor modulatory properties.
It first became available in Europe in 1984 under the brand name Katadolon and after it went off patent many generic brands were introduced. Flupirtine is used as an analgesic for acute pain, in moderate-to-severe cases. 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. The most serious side effect is frequent hepatotoxicity which prompted regulatory agencies to issue several warnings and restrictions. Flupirtine is devoid of negative psychological survey literature function effects, or effects on reproductive function.
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Although some studies have reported flupirtine has no addictive properties, there was suggestion that it may possess some abuse potential and liability. There were at least two registered cases of flupirtine abuse. Flupirtine is a selective neuronal potassium channel opener that also has indirect NMDA receptor antagonist and GABAA receptor modulatory properties. Flupirtine was discovered and developed between the 1970s and the 1990s by Chemiewerk Homburg in Frankfurt am Main, Germany, which became Degussa Pharma Group and then through mergers, ASTA Pharma and Asta Medica. It was approved for the treatment of pain in 1984 in Europe under the brand name Katadolon.
As of 2013 it was used in 11 member countries: Bulgaria, Estonia, Germany, Hungary, Italy, Latvia, Lithuania, Poland, Portugal, Romania and Slovak Republic. Many generics entered the European market around 2011. It was never introduced to the United States market for any indication but in 2008, Adeona Pharmaceuticals, Inc. In 2010 retigabine was approved by the FDA as an anticonvulsant for the treatment of refractory partial-onset seizures in treatment-experienced patients.
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