Pharmacological studies of a non-steroidal analgesic and antipyretic drug of LFP83.

Kuriyama, Kiyoshi; Hiyama, Yoshiyuki; Aoyama, Yusuke; Ichikawa, Kiyonoshin; Okumura, Makoto; MASUMOTO, Shozoh; Itō, Kiyoshi; Ohtaki, Yutaka; Hirata, Masaharu; Hanada, Shuichi; Uchida, Takeshi; Fujino, Yoshiyuki; Watanabe, Masahiro

doi:10.1254/fpj.93.61

Cited by 9 publications

(3 citation statements)

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“…The analgesic efficacy of flurbiprofen was screened by acetic acid writhing testinduced visceral pain after an hour of oral administration at three different doses 20, 40, and 80 mg/kg body weight. Flurbiprofen showed a significant drop in writhing induced by acetic acid before oral administration in a dose-dependent manner, where the percent inhibitions were compared with control values and were found to be 53%, 56%, and 63%, respectively, in agreement with a study conducted on mice and rats that compared the analgesic effect of flurbiprofen and LFP83 (a prodrug of flurbiprofen) by using a writhing test (31). The synergistic interaction between alpha-lipoic acid and flurbiprofen is due to their unique mechanism of action on nuclear factor NF Kappa B (NF-κB) and activator protein 1.…”

Section: Discussionsupporting

confidence: 86%

Flurbiprofen: Determination of safety profile, analgesic effect, and interaction with lipoic acid in murine

Alberifki¹,

Naser²

2023

IJVS

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our study aimed study aimed to detect and investigate the safety profile of flurbiprofen and evaluate the analgesic effects of the tail immersion and writhing tests, as well as its interaction with lipoic acid as an analgesic for visceral pain in mice. The up-and-down manner described by Dixon was utilized to determine the median lethal dose (LD50) and the median analgesic dose (ED50), the safety criteria were calculated, mathematical equations were applied, and the interaction between flurbiprofen and alpha-lipoic acid was evaluated using the writhing test. The LD50 of oral flurbiprofen was 1147.4 mg/kg, and the ED50 of oral flurbiprofen was 8.6 mg/kg using the tail immersion test. The therapeutic index was 133, and the standard safety margin was 35%. The highest analgesia time was one h after dosing, which faded after 24 h. Administration of flurbiprofen 10, 20, and 40 mg/kg had an analgesic effect in a dose-dependent manner. Flurbiprofen relieved visceral pain when dosed at 20, 40, and 80 mg/kg, with analgesic efficacies of 53, 56, and 65%, respectively. The simultaneous administration of flurbiprofen and alpha-lipoic acid had a synergistic analgesic effect on visceral pain. From our results, we conclude that flurbiprofen has a wide range of safety and is an effective analgesic for peripheral and visceral pain. The synergistic effect between flurbiprofen and alpha-lipoic acid may have clinical benefits, including reducing the dose of flurbiprofen when used together.

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Section: Discussionsupporting

confidence: 86%

Flurbiprofen: Determination of safety profile, analgesic effect, and interaction with lipoic acid in murine

Alberifki¹,

Naser²

2023

IJVS

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“…Therefore, we used flurbiprofen axetil [1-acetoxy-ethyo-2-(2-fluoro-4-biphenyl) propionate] (LFP) to evaluate the effects of NSAIDs on propofol injection pain. LFP is an injectable prodrug, formulated as a lipid emulsion of flurbiprofen ester, without irritant effects [15,16]. Therefore, the study was designed to evaluate whether intravenous administration of LFP reduces pain during propofol injection and offers any advantage over lidocaine admixture.…”

mentioning

confidence: 99%

Propofol injection pain is not alleviated by pretreatment with flurbiprofen axetil, a prodrug of a nonsteroidal antiinflammatory drug

Karasawa

Ehata

Okuda

et al. 2000

Journal of Anesthesia

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“…The NNT was also lowest for Lipuro-FA. As a possible mechanism of pain reduction by FA, the analgesic effect of FA as an NSAID is unlikely, because FA is a prodrug that must be metabolized, taking several minutes to exert its analgesic effect [20,21]. Protection of the intima of the vein by FA may also be possible [16], but we could not fi nd any evidence or literature supporting this speculation.…”

Section: Discussionmentioning

confidence: 83%

Emulsion of flurbiprofen axetil reduces propofol injection pain due to a decrease in free propofol concentration

et al. 2007

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Pharmacological studies of a non-steroidal analgesic and antipyretic drug of LFP83.

Cited by 9 publications

References 0 publications

Flurbiprofen: Determination of safety profile, analgesic effect, and interaction with lipoic acid in murine

Flurbiprofen: Determination of safety profile, analgesic effect, and interaction with lipoic acid in murine

Propofol injection pain is not alleviated by pretreatment with flurbiprofen axetil, a prodrug of a nonsteroidal antiinflammatory drug

Emulsion of flurbiprofen axetil reduces propofol injection pain due to a decrease in free propofol concentration

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