Flupirtine: pharmacology and clinical applications of a nonopioid analgesic and potentially neuroprotective compound

@article{Klawe2009FlupirtinePA,
  title={Flupirtine: pharmacology and clinical applications of a nonopioid analgesic and potentially neuroprotective compound},
  author={Christoph Klawe and M. Maschke},
  journal={Expert Opinion on Pharmacotherapy},
  year={2009},
  volume={10},
  pages={1495 - 1500}
}
Background: Flupirtine is a nonopioid drug without antipyretic or antiphlogistic properties and with a favorable tolerability. It constitutes a unique class within the group of nonsteroidal analgesics and displays a peculiar pharmacodynamic profile that invites the investigation of applications beyond the pain-relieving effect. Objective: This review describes and evaluates the pharmacologic and clinical literature regarding flupirtine and discusses its future potential. Methods: A search of… 
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Synergistic interaction between tapentadol and flupirtine in the rat orafacial formalin test.
Pharmacokinetic profiles of the analgesic flupirtine in dogs after the administration of four pharmaceutical formulations.
TLDR
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Flupirtine is a safe alternative drug in patients with hypersensitivity to NSAIDs
TLDR
Flupirtine was assessed for tolerability with regard to hypersensitivity reactions in patients with a history of HDR to NSAIDs because of a need for safe alternative drugs, and its muscle relaxant properties made it popular for orthopaedic use.
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This review describes and evaluates the pharmacologic literature concerning flupirtine and addresses its potential in veterinary medicine.
The indirect NMDAR inhibitor flupirtine induces sustained post-ischemic recovery, neuroprotection and angioneurogenesis
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Flupirtine is an attractive candidate for stroke therapy considering its sustained effects on neurological recovery, brain tissue survival and remodeling, and taking into account its tolerability profile.
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References

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  • Medicine, Psychology
    Fortschritte der Medizin
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TLDR
An open prospective trial was conducted in 50 patients suffering from chronic myofascial pain, and Flupirtine would appear to represent a new possibility for treating pain.
Flupirtine, a nonopioid centrally acting analgesic, acts as an NMDA antagonist.
Efficacy of flupirtine on cognitive function in patients with CJD
TLDR
FLU has beneficial effects on cognitive function in patients with CJD and may suggest a treatment potential of FLU in other neurodegenerative disorders, although further studies are necessary.
The antinociceptive activity of flupirtine: a structurally new analgesic.
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TLDR
The findings show that the central antinociceptive activity of flupirtine is not based on an opiate mechanism and is not comparable with that of diazepam and phenobarbitone.
Retigabine: chemical synthesis to clinical application.
TLDR
Retigabine dose-dependently reduces unconditioned anxiety-like behaviors when assessed in the mouse marble burying test and zero maze, and may prove to be useful in the treatment of a diverse range of disease states in which neuronal hyperexcitability is a common underlying factor.
[Mechanism of action of the analgesic flupirtine].
TLDR
The results demonstrate that the analgesic activity of flupirtine is not caused by the opiate mechanism, and these substances show cerebral or spinal analgesicactivity.
Analgesic efficacy and safety of oral flupirtine in the treatment of cancer pain.
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  • Medicine, Psychology
    Postgraduate medical journal
  • 1987
TLDR
Flupirtine fulfilled the requirements of both patients and doctors for effective cancer pain relief e.g. maintenance of the quality of life by complete or nearly complete pain remission in association with lack of abuse potential, oral dosage form and lack of disturbance of vital functions.
[Pharmacokinetics and biotransformation of the analgesic flupirtine in humans].
TLDR
The pharmacokinetics of the analgesic flupirtine were examined in healthy volunteers after a single intravenous, peroral and rectal dose and two metabolites could be isolated from urine and their chemical structure determined.
Investigation of the in Vitro Metabolism of the Analgesic Flupirtine
TLDR
In vitro metabolism of flupirtine, a centrally acting analgesic with muscle tone-reducing activity, suggested that redox chemistry may play a role in metabolism, and cyclic voltammetry studies showed that the drug undergoes facile and irreversible redox reactions.
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