Flupirtine, a re-discovered drug, revisited

@article{Szelenyi2013FlupirtineAR,
  title={Flupirtine, a re-discovered drug, revisited},
  author={Istvan Prof Szelenyi},
  journal={Inflammation Research},
  year={2013},
  volume={62},
  pages={251-258}
}
  • I. Szelenyi
  • Published 16 January 2013
  • Biology, Medicine
  • Inflammation Research
Flupirtine was developed long before KV7 (KCNQ) channels were known. However, it was clear from the beginning that flupirtine is neither an opioid nor a nonsteroidal anti-inflammatory analgesic. Its unique muscle relaxing activity was discovered by serendipity. In the meantime, broad and intensive research has resulted in a partial clarification of its mode of action. Flupirtine is the first therapeutically used KV7 channel activator with additional GABAAergic mechanisms and thus the first… 
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The synthetic and medicinal chemistry of small molecule modulators and the representative biological properties are summarized and new therapeutic applications supported by in vitro and in vivo assay data are suggested.
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Pharmacokinetic profiles of the analgesic drug flupirtine in cats.
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Tissue partition coefficients based on isolated tissue uptake correlated well with in vivo tissue:serum drug exposure ratios and flupirtine reaches the target brain tissues from the systemic route in neonatal rats, and brain tissue forms the active metabolite D-13223.
Abuse liability of flupirtine revisited: Implications of spontaneous reports of adverse drug reactions
TLDR
The hypothesis that FLP features a potential to cause addictive behaviors is strengthened, as female sex, age >40 years, and long‐term FLP‐treatment may be possible risk factors for the development of FLP abuse/dependence.
Oxidation Potentials of N‐Modified Derivatives of the Analgesic Flupirtine Linked to Potassium KV7 Channel Opening Activity But Not Hepatocyte Toxicity
TLDR
The idea that oxidative metabolites of flupirtine contribute to the mechanism of action, similar to what was recently proposed for acetaminophen, but not to hepatotoxicity, is supported.
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