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[外用普拉洛芬凝胶的镇痛效果]

[Analgesic effect of topically applied pranoprofen-gel].

作者信息

Terasawa M, Yakushiji T, Iwahisa Y, Imayoshi T, Maruyama Y

出版信息

Nihon Yakurigaku Zasshi. 1985 Dec;86(6):433-40. doi: 10.1254/fpj.86.433.

Abstract

The analgesic effect of topically applied pranoprofen-gel (1% and 3%) was investigated in comparison with indomethacin-gel in experimental animals. Applied topically, 1% and 3% pranoprofen-gel inhibited the inflammatory pain induced by Randall and Selitto's method and the pain response (abnormal gait) of concanavalin A-induced arthritis in rats dose-dependently. Furthermore, in antigen (methylated bovine serum albumin)-induced arthritis in rats, pranoprofen-gel had a concentration and application-dependent therapeutic effect on knee joint swelling and the pain response. Pranoprofen-gel had a stronger analgesic effect than indomethacin-gel in these experimental models. Both drugs inhibited the flexor reflexes of the hind limb induced by injecting bradykinin (BK) in combination with arachidonic acid into the common iliac artery of the spinal rat, but failed to do so with BK combined with prostaglandin E2 (PGE2). Moreover, pranoprofen-gel inhibited the BK-induced increase in the firing rate of the saphenous nerve of the spinal cat. These results show that pranoprofen-gel, applied topically, permeates well from the skin to the nociceptor site, relieving the hyperalgesia caused by PGs-induced sensitization of pain receptors by inhibiting their production. As a topical anti-inflammatory and analgesic agent, pranoprofen-gel is at least as effective as indomethacin-gel, so that it should have good clinical potential.

摘要

在实验动物中,研究了局部应用的普拉洛芬凝胶(1%和3%)与吲哚美辛凝胶相比的镇痛效果。局部应用1%和3%的普拉洛芬凝胶可剂量依赖性地抑制Randall和Selitto法诱导的炎性疼痛以及大鼠伴刀豆球蛋白A诱导的关节炎的疼痛反应(异常步态)。此外,在大鼠抗原(甲基化牛血清白蛋白)诱导的关节炎中,普拉洛芬凝胶对膝关节肿胀和疼痛反应具有浓度和应用依赖性治疗作用。在这些实验模型中,普拉洛芬凝胶的镇痛作用比吲哚美辛凝胶更强。两种药物均能抑制将缓激肽(BK)与花生四烯酸联合注入脊髓大鼠髂总动脉所诱导的后肢屈肌反射,但对BK与前列腺素E2(PGE2)联合诱导的反射则无效。此外,普拉洛芬凝胶可抑制BK诱导的脊髓猫隐神经放电频率增加。这些结果表明,局部应用的普拉洛芬凝胶能很好地从皮肤渗透到伤害感受器部位,通过抑制前列腺素诱导的疼痛感受器敏化来减轻痛觉过敏。作为一种局部抗炎镇痛药,普拉洛芬凝胶至少与吲哚美辛凝胶一样有效,因此具有良好的临床应用潜力。

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