Murakami I, Asano S, Yukishige K, Nagaya H, Satoh H, Inatomi N
Pharmaceutical Research Laboratories III, Takeda Chemical Industries, Ltd., Osaka, Japan.
Nihon Yakurigaku Zasshi. 1996 Dec;108(6):323-32. doi: 10.1254/fpj.108.6_323.
The effects of lansoprazole given intravenously on indomethacin-induced gastric bleeding and mucosal lesions were investigated in rats in comparison with those of omeprazole, famotidine and ranitidine. Lansoprazole inhibited gastric bleeding induced by indomethacin with an ID50 value of 0.29 mg/kg. Omeprazole and famotidine significantly inhibited gastric bleeding, but ranitidine provided negligible inhibition. A correlation was found between the inhibitory action of lansoprazole on gastric bleeding, and acid secretion, and its inhibitory action on gastric bleeding was almost completely abolished by adding 50 mM-HCl to the gastric perfusate, suggesting that lansoprazole's inhibitory action on gastric bleeding was mainly due to its antisecretory action. Lansoprazole inhibited the development of gastric lesions induced by indomethacin with an ID50 value of 0.10 mg/kg, whereas histamine H2-receptor antagonists did not display a potent inhibitory effect. ID50 values for omeprazole, famotidine and ranitidine were 0.69, 2.58 and 24.6 mg/kg, respectively. These results indicate that lansoprazole has a potent inhibitory action on indomethacin-induced gastric bleeding and mucosal lesions and that it is useful in the treatment of acute gastric mucosal lesions.
在大鼠中研究了静脉注射兰索拉唑对吲哚美辛诱导的胃出血和黏膜损伤的影响,并与奥美拉唑、法莫替丁和雷尼替丁进行了比较。兰索拉唑抑制吲哚美辛诱导的胃出血,其半数抑制剂量(ID50)值为0.29mg/kg。奥美拉唑和法莫替丁显著抑制胃出血,但雷尼替丁的抑制作用可忽略不计。发现兰索拉唑对胃出血的抑制作用与其酸分泌抑制作用之间存在相关性,并且通过向胃灌流液中加入50mM盐酸,其对胃出血的抑制作用几乎完全被消除,这表明兰索拉唑对胃出血的抑制作用主要归因于其抗分泌作用。兰索拉唑抑制吲哚美辛诱导的胃损伤的发展,其ID50值为0.10mg/kg,而组胺H2受体拮抗剂未显示出有效的抑制作用。奥美拉唑、法莫替丁和雷尼替丁的ID50值分别为0.69、2.58和24.6mg/kg。这些结果表明,兰索拉唑对吲哚美辛诱导的胃出血和黏膜损伤具有强效抑制作用,并且可用于治疗急性胃黏膜损伤。