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氟尼辛葡甲胺:一种非麻醉性镇痛药。

Flunixin meglumine: a non-narcotic analgesic.

作者信息

Ciofalo V B, Latranyi M B, Patel J B, Taber R I

出版信息

J Pharmacol Exp Ther. 1977 Mar;200(3):501-7.

PMID:850126
Abstract

The N-methyl-d-glucamine salt of flunixin (flunixin meglumine) is a potent non-narcotic analgesic agent after parenteral administration in mice, rats and monkeys. It is significantly more potent than pentazocine, meperidine and codeine in the rat yeast paw test after subcutaneous administration in saline. Activity on intramuscular administration is comparable to that after subcutaneous administration and is enhanced when dissolved in buffered saline as compared to nonbuffered saline. In addition, flunixin meglumine also had oral activity and differs from indomethacin in having more analgesic activity per unit of anti-inflammatory activity. In mice, flunixin meglumine is equipotent to pentazocine and more potent than meperidine and codeine in the abdominal constriction test. In primates, flunixin meglumine at 10 mg/kg i.m., produced a degree of analgesic efficacy comparable to that of a clinically effective dose of morphine (0.3 mg/kg). In contrast to codeine, tolerance to the analgesic action of flunixin meglumine was not observed. Furthermore, flunixin meglumine retained its activity in rats made tolerant to codeine. Unlike narcotics, the analgesic effect of flunixin meglumine is not antagonized by naloxone after acute administration in rats. These results indicate that flunixin meglumine is a parenterally and orally effective analgesic in animals and is unlikely to have narcotic or drug dependence liability.

摘要

氟尼辛的N-甲基-D-葡糖胺盐(氟尼辛葡甲胺)在小鼠、大鼠和猴子经肠胃外给药后是一种强效非麻醉性镇痛药。在大鼠酵母足试验中,皮下注射于生理盐水中时,它比喷他佐辛、哌替啶和可待因的效力显著更强。肌肉注射时的活性与皮下注射相当,并且与非缓冲生理盐水相比,溶解于缓冲生理盐水时活性增强。此外,氟尼辛葡甲胺也具有口服活性,与吲哚美辛不同,它每单位抗炎活性具有更强的镇痛活性。在小鼠中,氟尼辛葡甲胺在腹部收缩试验中与喷他佐辛效力相当,比哌替啶和可待因更强效。在灵长类动物中,10mg/kg肌肉注射的氟尼辛葡甲胺产生的镇痛效果程度与临床有效剂量的吗啡(0.3mg/kg)相当。与可待因不同,未观察到对氟尼辛葡甲胺镇痛作用的耐受性。此外,氟尼辛葡甲胺在对可待因产生耐受性的大鼠中仍保留其活性。与麻醉药不同,大鼠急性给药后,氟尼辛葡甲胺的镇痛作用不会被纳洛酮拮抗。这些结果表明,氟尼辛葡甲胺在动物中经肠胃外和口服给药均有效,并且不太可能具有麻醉或药物依赖性。

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