Longstreth G F, Go V L, Malagelada J R
N Engl J Med. 1976 Apr 8;294(15):801-4. doi: 10.1056/NEJM197604082941502.
Nocturnal pain and gastric hypersecretion are common in duodenal ulcer. Therefore, we investigated the antisecretory effects of a new H2-receptor antagonist, cimetidine, in 200-, 300- or 400-mg doses, taken orally at bedtime. The 200-mg dose did not cause a statistically significant change in nocturnal (midnight to 7 a.m.) acid output and had only a borderline effect on pH. However, the 300-mg and 400-mg doses significantly (P less than 0.001) lowered acid output and increased (P less than 0.01) intragastric pH. All doses caused substantial decreases in secretory volume output. After a 400-mg dose, half the patients remained anacidic for eight hours. Dose-related increases of drug blood levels were observed and correlated with the degree and duration of inhibition of acid output. Serum gastrin levels were unaffected. Cimetidine appears to be a potent inhibitor of nocturnal gastric secretion.
夜间疼痛和胃酸分泌过多在十二指肠溃疡中很常见。因此,我们研究了一种新型H2受体拮抗剂西咪替丁在睡前口服200毫克、300毫克或400毫克剂量时的抗分泌作用。200毫克剂量并未使夜间(午夜至上午7点)胃酸分泌量发生统计学上的显著变化,对pH值仅有临界影响。然而,300毫克和400毫克剂量显著(P小于0.001)降低了胃酸分泌量并提高了(P小于0.01)胃内pH值。所有剂量均使分泌量大幅减少。服用400毫克剂量后,半数患者在八小时内保持无酸状态。观察到药物血药浓度呈剂量相关增加,且与胃酸分泌抑制的程度和持续时间相关。血清胃泌素水平未受影响。西咪替丁似乎是夜间胃分泌的有效抑制剂。