Okabe S, Kawakami M
Nihon Yakurigaku Zasshi. 1981 Aug;78(2):57-62.
Antisecretory effects of ranitidine on secretagogue-stimulated gastric secretion in acute fistula rats were studied. Histamine 2HCl (8 mg/kg/hr), pentagastrin (125 micrograms/kg/hr) or carbachol (128 micrograms/kg/hr) was continuously given i.v. by an infusion pump, through the tail vein to acute fistula rats. Gastric secretion was collected hourly for 5 hr and analyzed for its components. Cimetidine was used as a reference drug. Both drugs were given i.v. by a bolus injection in the tail vein 30 min after the injection of each stimulant. Both ranitidine (1 and 10 mg/kg) and cimetidine (10 and 60 mg/kg) significantly (P less than 0.05) inhibited the histamine-stimulated gastric secretion (volume, acid and pepsin output) for 1 to 4 hr. Both ranitidine (10 mg/kg) and cimetidine (60 mg/kg) significantly (P less than 0.05) inhibited the pentagastrin-stimulated gastric secretion for 2 to 3 hr. both ranitidine (10 mg/kg) and cimetidine (10 and 60 mg/kg) markedly inhibited the gastric acid secretion in response to carbachol. However, cimetidine (10 or 60 mg/kg) significantly (P less than 0.05) stimulated the volume and pepsin output by carbachol. We conclude that ranitidine is about 6 times more potent than cimetidine for histamine- or pentagastrin-stimulated gastric secretion and almost equal to cimetidine for carbachol-stimulated gastric acid output in rats.
研究了雷尼替丁对急性瘘管大鼠促分泌剂刺激的胃分泌的抗分泌作用。通过输液泵经尾静脉向急性瘘管大鼠持续静脉输注2HCl组胺(8毫克/千克/小时)、五肽胃泌素(125微克/千克/小时)或卡巴胆碱(128微克/千克/小时)。每小时收集胃分泌液,持续5小时,并分析其成分。西咪替丁用作对照药物。在注射每种刺激剂30分钟后,两种药物均经尾静脉推注给药。雷尼替丁(1和10毫克/千克)和西咪替丁(10和60毫克/千克)均显著(P<0.05)抑制组胺刺激的胃分泌(容量、酸和胃蛋白酶分泌量)1至4小时。雷尼替丁(10毫克/千克)和西咪替丁(60毫克/千克)均显著(P<0.05)抑制五肽胃泌素刺激的胃分泌2至3小时。雷尼替丁(10毫克/千克)和西咪替丁(10和60毫克/千克)均显著抑制卡巴胆碱刺激的胃酸分泌。然而,西咪替丁(10或60毫克/千克)显著(P<0.05)刺激卡巴胆碱引起的容量和胃蛋白酶分泌量。我们得出结论,在大鼠中,对于组胺或五肽胃泌素刺激的胃分泌,雷尼替丁的效力约为西咪替丁的6倍,对于卡巴胆碱刺激的胃酸分泌,雷尼替丁的效力几乎与西咪替丁相当。