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每日单次剂量的吡啶-2-四氢噻吩衍生物(40749 RP)对十二指肠溃疡患者24小时氢离子活性、夜间酸分泌量、胃泌素和胃蛋白酶原I水平的影响。

Effects of single daily doses of a pyridil-2-tetrahydrothiophene derivative (40749 RP) on 24 hour H+ activity, nocturnal acid output, gastrin and pepsinogen I profiles in duodenal ulcer patients.

作者信息

Malè P J, Griessen M, Cunningham M G, Frydman A M, Garoflid-Oprescu N A, De Peyer R, Loizeau E

出版信息

Gut. 1986 Apr;27(4):423-7. doi: 10.1136/gut.27.4.423.

Abstract

40749 RP is a pyridil-2-tetrahydrothiophene derivative, belonging to a new class of gastric antisecretory drugs. We compared its effects on gastric secretion with cimetidine. Intragastric acidity, nocturnal acid output, gastrin and pepsinogen-I profiles were measured in patients with duodenal ulcer in clinical remission. A single dose of 100 mg 40749 RP reduced median 24 h gastric acidity as effectively as cimetidine 1000 mg given as four divided doses, 0.63 vs 1.6 mmol/l. Continued treatment with 40749 RP for 10 days reduced the median 24 h gastric acidity even further, to 0.006 mmol/l (p less than 0.001) and significantly increased fasting concentrations of gastrin and pepsinogen-I (p = 0.02). The incremental gastrin secretion to a standard meal was significantly increased after 10 days treatment with 40749 RP when compared with the first day of 40749 RP, or with cimetidine. These results show that 40749 RP exerts a powerful inhibitory effect on gastric acid secretion after a single 100 mg dose, and that this inhibitory effect increases with continued administration.

摘要

40749 RP是一种吡啶-2-四氢噻吩衍生物,属于一类新型的胃泌素分泌抑制剂。我们将其对胃酸分泌的作用与西咪替丁进行了比较。对处于临床缓解期的十二指肠溃疡患者测量了胃内酸度、夜间酸分泌量、胃泌素和胃蛋白酶原I水平。单剂量100 mg的40749 RP降低24小时胃内酸度中位数的效果与分四次服用1000 mg西咪替丁的效果相当,分别为0.63和1.6 mmol/L。40749 RP持续治疗10天可使24小时胃内酸度中位数进一步降低至0.006 mmol/L(p<0.001),并显著提高胃泌素和胃蛋白酶原I的空腹浓度(p = 0.02)。与40749 RP治疗第一天或西咪替丁相比,40749 RP治疗10天后,标准餐引起的胃泌素分泌增量显著增加。这些结果表明,单剂量100 mg的40749 RP对胃酸分泌具有强大的抑制作用,且这种抑制作用会随着持续给药而增强。

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