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… Expand
Concise review: Therapeutic potential of flupirtine maleate
TLDR
The pain-relieving property of flupirtine is not reduced by the opioid antagonistic drug naloxone, preliminary finding require confirmation in further comparative studies. Expand
Flupirtine: A Review on its Therapeutic Potency
Flupirtine is a centrally acting non-opioid analgesic displaying indirect NDMA receptor antagonism and is the first representative of a pharmacological class of selective neuronal potassium channelExpand
Pharmacokinetics and disposition of flupirtine in the horse.
TLDR
Evaluated the pharmacokinetic profiles of FLU after IV and PO administration in healthy horses and these findings may form the basis for further studies concerning this active ingredient in equine medicine. Expand
Pharmacokinetic profiles of the analgesic drug flupirtine in cats.
TLDR
This is the first study of FLU in an animal species of veterinary interest and it could pave the way for the use of this active ingredient in the veterinary field. Expand
Flupirtine: Preliminary Pharmacokinetics in the Donkey
TLDR
The pharmacokinetic trend of FLU in donkeys was different from those earlier reported in cats and dogs, and further studies are needed to understand if this active ingredient may be used inDonkeys. Expand
Synergistic interaction between tapentadol and flupirtine in the rat orafacial formalin test.
TLDR
The data reported in this study indicate that FLP enhances the antinociceptive effect of TAP and this drug combination might be potentially useful in the treatment of chronic pain. Expand
Pharmacokinetic profiles of the analgesic flupirtine in dogs after the administration of four pharmaceutical formulations.
TLDR
Flupirtine after intravenous (IV), oral immediate release (POIR), oral prolonged release (POPR) and rectal (RC) administrations in healthy dogs provides pharmacokinetic data that can be used to design further studies to investigate FLU in dogs. Expand
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. Expand
Flupirtine: A Human Drug with Potential for Use in the Veterinary Field
TLDR
This review describes and evaluates the pharmacologic literature concerning flupirtine and addresses its potential in veterinary medicine. Expand
The indirect NMDAR inhibitor flupirtine induces sustained post-ischemic recovery, neuroprotection and angioneurogenesis
TLDR
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. Expand
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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. Expand
Flupirtine, a nonopioid centrally acting analgesic, acts as an NMDA antagonist.
TLDR
Data derived from in vitro and in vivo studies suggest that flupirtine functions as a weak N-methyl-D-aspartate (NMDA) antagonist with little evidence that it acts on AMPA-kainate type glutamate receptors. Expand
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. Expand
The antinociceptive activity of flupirtine: a structurally new analgesic.
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  • Medicine
  • Postgraduate medical journal
  • 1987
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. Expand
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. Expand
[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. Expand
Analgesic efficacy and safety of oral flupirtine in the treatment of cancer pain.
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  • Medicine
  • Postgraduate medical journal
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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. Expand
[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. Expand
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. Expand
Retigabine and flupirtine exert neuroprotective actions in organotypic hippocampal cultures
TLDR
Analysis of neuroprotective potential of retigabine and flupirtine in rat organotypic hippocampal slice cultures exposed to N-methyl-D-aspartate, oxygen and glucose deprivation followed by reoxygenation (OGD), or serum withdrawal (SW) suggested that antioxidant actions of these compounds participated in OHSC neuroprotection during SW. Expand
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