Inoue K, Fujisawa H, Sasaki Y, Nishimura T, Nishimura I, Inoue Y, Yokota M, Masuda T, Ueda F, Shibata Y
Research Laboratories, Nippon Shinyaku Co., Ltd., Kyoto, Japan.
Arzneimittelforschung. 1991 Mar;41(3):228-35.
The anti-inflammatory, analgesic, antipyretic and ulcerogenic activities of etodolac (CAS 41340-25-4), a new nonsteroidal anti-inflammatory agent, were compared with those of indometacin and other anti-inflammatory drugs in experimental animals. Etodolac had a remarkable anti-inflammatory effect in various experimental models: ultraviolet erythema, carrageenin-induced edema and swelling of adjuvant arthritis. In these models, the effective dose of etodolac was several fold that of indometacin. Etodolac inhibited prostaglandin E2 formation in a concentration-dependent manner, and its inhibitory potency was about 1/5 of that of indometacin. Etodolac also caused marked inhibition of granuloma formation and leucocyte functions such as chemotaxis, lysosomal enzyme release and active oxygen generation. These effects of etodolac were observed at similar doses of indometacin. Etodolac suppressed inflammatory pain but not non-inflammatory pain, and had an antipyretic effect but did not lower normal rectal temperature. Etodolac had no effect on delayed hypersensitivity reactions and was much less ulcerogenic than indometacin. These results indicate that etodolac is a low ulcerogenic anti-inflammatory agent with suppressing activities on leucocyte functions to the same extent as indometacin and prostaglandin biosynthesis.
在实验动物中，将新型非甾体抗炎药依托度酸（CAS 41340 - 25 - 4）的抗炎、镇痛、解热及致溃疡活性与吲哚美辛和其他抗炎药物进行了比较。依托度酸在多种实验模型中具有显著的抗炎作用：紫外线红斑、角叉菜胶诱导的水肿以及佐剂性关节炎肿胀。在这些模型中，依托度酸的有效剂量是吲哚美辛的几倍。依托度酸以浓度依赖的方式抑制前列腺素E2的形成，其抑制效力约为吲哚美辛的1/5。依托度酸还能显著抑制肉芽肿形成以及白细胞功能，如趋化性、溶酶体酶释放和活性氧生成。在与吲哚美辛相似的剂量下可观察到依托度酸的这些作用。依托度酸能抑制炎性疼痛而非非炎性疼痛，具有解热作用但不会降低正常直肠温度。依托度酸对迟发型超敏反应无影响，且致溃疡作用比吲哚美辛小得多。这些结果表明，依托度酸是一种致溃疡作用小的抗炎药，对白细胞功能的抑制作用与吲哚美辛及前列腺素生物合成的抑制作用程度相同。
