Henn R M, Isenberg J I, Maxwell V, Sturdevant R A
N Engl J Med. 1975 Aug 21;293(8):371-5. doi: 10.1056/NEJM197508212930802.
Cimetidine, a non-thiourea-containing H2-receptor antagonist, was studied in seven patients with duodenal ulcer. Oral doses of 100, 200, and 300 mg were tested. Each dose significantly inhibited basal and meal-stimulated secretion. After 300 mg, basal acid secretion was essentially zero for at least five hours. The meal-stimulated three-hour acid output after the 300-mg dose was reduced by 67%. Cimetidine, 300 mg, decreased meal-stimulated acid secretion significantly more than an optimal effective dose of propantheline bromide (P less than 0.05). Inhibition of meal-stimualted gastric acid secretion showed a significant relation to peak blood cimetidine concentration (r is equal to 0.76, P less than 0.01). Cimetidine did not affect meal-stimulated gastrin release. No toxicity was observed after serial doses given during these tests. Cimetidine may be useful in treatment of acid-peptic diseases provided no important toxicity appears on chronic testing.
西咪替丁是一种不含硫脲的H2受体拮抗剂，对7例十二指肠溃疡患者进行了研究。测试了100、200和300毫克的口服剂量。每个剂量均能显著抑制基础胃酸分泌和进餐刺激的胃酸分泌。服用300毫克后，基础胃酸分泌在至少5小时内基本为零。300毫克剂量后，进餐刺激的三小时胃酸分泌量减少了67%。300毫克西咪替丁比最佳有效剂量的溴丙胺太林更显著地减少了进餐刺激的胃酸分泌（P<0.05）。进餐刺激的胃酸分泌抑制与西咪替丁血药浓度峰值呈显著相关（r=0.76，P<0.01）。西咪替丁不影响进餐刺激的胃泌素释放。在这些试验中连续给药后未观察到毒性。如果在长期试验中未出现重要毒性，西咪替丁可能对治疗酸相关性疾病有用。
