Dammann H G, Rehner M, Dreyer M, Walter T A, Müller P, Simon B
Arzneimittelforschung. 1986 Nov;36(11):1699-701.
The chemical structure of etintidine differs from that of cimetidine by the addition of an ethinyl group to the terminal methyl group of the side chain. We investigated the influence of etintidine 300 or 400 mg b.d. and of etintidine 300 or 600 mg nocte, cimetidine 800 mg nocte versus placebo in two different double-blind randomized cross-over studies on 24-h intragastric acidity and nocturnal volume and acid secretion (12:00 midnight to 6:00 a.m.) in 12 and 8 healthy male volunteers, respectively. 5-10 ml of gastric contents were aspirated hourly via a nasogastric tube. The pH of the samples was determined using a glass electrode. The results were expressed in terms of H+-activity (mmol/l). Etintidine 300 or 400 mg b.d. reduced day- and nighttime acidity by 53 and 60% or 41 and 41%, respectively. Nocturnal acid secretion (mmol/l) was inhibited by 38 and 42%, resp. Etintidine 300 or 600 mg nocte and cimetidine 800 mg nocte (9:00 p.m.) lowered nocturnal intragastric acidity by 69, 84 and 79%, resp. Daytime inhibition was not observed. Our results suggest, that 1. etintidine 300 and 400 mg b.d. are equipotent in promoting peptic ulcer healing and 2. that this new imidazole H2-receptor antagonist is also effective in a single bedtime dose.
依替替丁的化学结构与西咪替丁的不同,它是在侧链末端甲基上添加了一个乙炔基。我们在两项不同的双盲随机交叉研究中,分别对12名和8名健康男性志愿者的24小时胃内酸度、夜间胃液量及酸分泌(午夜12点至凌晨6点),研究了每日两次服用300或400毫克依替替丁、每晚服用300或600毫克依替替丁、每晚服用800毫克西咪替丁与安慰剂的效果。通过鼻胃管每小时抽取5 - 10毫升胃内容物。使用玻璃电极测定样本的pH值。结果以氢离子活性(毫摩尔/升)表示。每日两次服用300或400毫克依替替丁,分别使白天和夜间酸度降低53%和60%或41%和41%。夜间酸分泌(毫摩尔/升)分别被抑制38%和42%。每晚服用300或600毫克依替替丁以及每晚服用800毫克西咪替丁(晚上9点),分别使夜间胃内酸度降低69%、84%和79%。未观察到白天有抑制作用。我们的结果表明,1. 每日两次服用300和400毫克依替替丁在促进消化性溃疡愈合方面效果相当;2. 这种新型咪唑H2受体拮抗剂在睡前单次给药时也有效。