Nakamura H, Yokoyama Y, Motoyoshi S, Seto Y, Kadokawa T, Shimizu M
Nihon Yakurigaku Zasshi. 1982 Jun;79(6):509-27.
Anti-inflammatory and gastrointestinal ulcerogenic activities of zomepirac sodium were investigated in experimental animals. The inhibitory activity of zomepirac sodium against carrageenin hind paw edema in rats, acetic acid-induced increase in vascular permeability in mice, and UV-erythema in guinea pigs was more potent than that of indomethacin. Anti-edema activity of zomepirac sodium was seen in adrenalectomized rats. Zomepirac sodium, like indomethacin, inhibited the delayed phase of hind paw edema produced by mixed phlogistics, but not the early phase mediated by histamine and serotonin in rats. Zomepirac sodium produced a dose-dependent inhibition against granuloma formation, established adjuvant arthritis, and development of adjuvant arthritis in rats; and its activity was slightly less potent than that of indomethacin. The inhibitory activity of zomepirac sodium on PGE2 biosynthesis in vitro was about one-third that of indomethacin. The ulcerogenic activity of zomepirac sodium was about 5 times weaker than that of indomethacin. From these results, it was suggested that zomepirac sodium was effective on various types of inflammation and showed particularly potent inhibitory activity against acute inflammation. These findings suggest that the mode of action of zomepirac sodium is similar to that of other acidic non-steroidal anti-inflammatory drugs.
在实验动物中研究了佐美酸的抗炎和致胃肠溃疡活性。佐美酸对大鼠角叉菜胶性后足肿胀、小鼠醋酸诱导的血管通透性增加以及豚鼠紫外线红斑的抑制活性比吲哚美辛更强。在肾上腺切除的大鼠中观察到佐美酸的抗水肿活性。佐美酸与吲哚美辛一样，抑制大鼠混合性炎症引起的后足肿胀的迟发期，但不抑制组胺和5-羟色胺介导的早期阶段。佐美酸对大鼠肉芽肿形成、已形成的佐剂性关节炎和佐剂性关节炎的发展产生剂量依赖性抑制；其活性略低于吲哚美辛。佐美酸在体外对前列腺素E2生物合成的抑制活性约为吲哚美辛的三分之一。佐美酸的致溃疡活性比吲哚美辛弱约5倍。从这些结果表明，佐美酸对各种类型的炎症有效，并且对急性炎症表现出特别强的抑制活性。这些发现表明佐美酸的作用方式与其他酸性非甾体抗炎药相似。
