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Antinociception by fluoro-loxoprofen, a novel non-steroidal anti-inflammatory drug with less ulcerogenic effects, in rat models of inflammatory pain.

Abstract
The use of non-steroidal anti-inflammatory drugs (NSAIDs) for the treatment of inflammatory pain is limited by gastrointestinal complications. The rapid action of NSAIDs is associated with better pain relief. Previously, we demonstrated that fluoro-loxoprofen, a novel NSAID, has less ulcerogenic potential than other NSAIDs, attributable to its gastroprotective properties. The aim of this study was to investigate and compare the effects of fluoro-loxoprofen on inflammatory pain in rats with those of other NSAIDs. Oral administration of fluoro-loxoprofen, loxoprofen, and celecoxib resulted in equivalent analgesic action against yeast-induced inflammatory pain. The antinociceptive effect of fluoro-loxoprofen was maximized within 1 h after administration, which is less time than that observed for loxoprofen (2 h) and celecoxib (3 h). We confirmed that both fluoro-loxoprofen and loxoprofen suppressed the increases in prostaglandin E2 in inflamed paws. In addition to yeast-induced pain, fluoro-loxoprofen produced a similar effect against adjuvant-induced inflammatory pain, with faster peak analgesic effects than those observed for loxoprofen and celecoxib. Taken together, these results suggest that the analgesic effect of fluoro-loxoprofen is equivalent to that of loxoprofen and celecoxib. Moreover, the analgesic effect of fluoro-loxoprofen against inflammatory pain was more rapid than that of other NSAIDs, and this may be associated with its rapid absorption property.
AuthorsTeita Asano, Tomoki Hattori, Ken-Ichiro Tanaka, Naoki Yamakawa, Shintaro Suemasu, Shuji Aida, Marika Kataoka, Tohru Mizushima, Mitsuko Takenaga
JournalEuropean journal of pharmacology (Eur J Pharmacol) Vol. 844 Pg. 253-258 (Feb 05 2019) ISSN: 1879-0712 [Electronic] Netherlands
PMID30529473 (Publication Type: Journal Article)
CopyrightCopyright © 2018 Elsevier B.V. All rights reserved.
Chemical References
  • Analgesics
  • Anti-Inflammatory Agents, Non-Steroidal
  • Phenylpropionates
  • fluoro-loxoprofen
  • Dinoprostone
Topics
  • Acute Pain (drug therapy, metabolism)
  • Analgesics (therapeutic use)
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal (therapeutic use)
  • Chronic Pain (drug therapy, metabolism)
  • Dinoprostone (metabolism)
  • Female
  • Foot
  • Male
  • Phenylpropionates (therapeutic use)
  • Rats, Inbred Lew
  • Rats, Wistar

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