Vinayek R, Howard J M, Maton P N, Wank S A, Slaff J I, Gardner J D, Jensen R T
Am J Med. 1986 Oct 24;81(4B):49-59. doi: 10.1016/0002-9343(86)90600-5.
The histamine (H2)-receptor antagonist famotidine was compared with ranitidine and cimetidine in its ability to control gastric acid hypersecretion in 33 patients with gastric hypersecretory states (32 patients with Zollinger-Ellison syndrome and one patient with idiopathic hypersecretion). Equipotent doses of each drug were determined in nine patients and used to determine relative onset of action, duration of action, and potency. Each drug had a similar time course of onset with a maximal effect at three to four hours after oral ingestion. The duration of action of famotidine was 30 percent longer than that of either cimetidine or ranitidine. In terms of relative potency, famotidine was nine times more potent than ranitidine and 32 times more potent than cimetidine. Thirty-two patients underwent long-term famotidine treatment for up to 34 months (mean, 10 months) with a duration in 21 patients of at least six months, in nine patients of at least 12 months, and in six patients of at least 24 months. The mean daily maintenance dose with famotidine was 0.33 g per day (range, 0.05 to 0.8 g). Prior to famotidine therapy, 27 patients were taking ranitidine and the mean daily dose required was 2.3 g per day (range, 0.6 to 5.4 g), whereas six patients were taking cimetidine and the mean daily dose was 4.6 g per day (range, 1.2 to 9.0 g). Fourteen of the 32 patients required an anticholinergic agent in addition to ranitidine or cimetidine to maintain control, whereas only five patients required an anticholinergic agent with famotidine. Gastric acid hypersecretion was controlled in seven patients with less frequent dosing with famotidine than with cimetidine or ranitidine. Long-term treatment with famotidine was not associated with any hematologic or biochemical toxicity or clinical side effects. These results demonstrate that famotidine has a similar onset of action to other H2-receptor antagonists but has a 30 percent longer duration of action and is nine times more potent than ranitidine and 32 times more potent than cimetidine. Famotidine is safe and highly effective in the long-term treatment of gastric hypersecretory states.
将组胺（H2）受体拮抗剂法莫替丁与雷尼替丁和西咪替丁在33例胃酸分泌过多状态患者（32例卓-艾综合征患者和1例特发性分泌过多患者）中控制胃酸分泌过多的能力进行了比较。在9例患者中确定了每种药物的等效剂量，并用于确定相对起效时间、作用持续时间和效力。每种药物的起效时间过程相似，口服后3至4小时达到最大效果。法莫替丁的作用持续时间比西咪替丁或雷尼替丁长30%。就相对效力而言，法莫替丁的效力比雷尼替丁强9倍，比西咪替丁强32倍。32例患者接受了长达34个月（平均10个月）的法莫替丁长期治疗，21例患者的治疗持续时间至少为6个月，9例患者至少为12个月，6例患者至少为24个月。法莫替丁的平均每日维持剂量为0.33克/天（范围为0.05至0.8克）。在法莫替丁治疗前，27例患者服用雷尼替丁，所需平均每日剂量为2.3克/天（范围为0.6至5.4克），而6例患者服用西咪替丁，平均每日剂量为4.6克/天（范围为1.2至9.0克）。32例患者中有14例除雷尼替丁或西咪替丁外还需要抗胆碱能药物来维持控制，而只有5例患者在使用法莫替丁时需要抗胆碱能药物。7例患者使用法莫替丁的给药频率低于西咪替丁或雷尼替丁时，胃酸分泌过多得到了控制。法莫替丁的长期治疗与任何血液学或生化毒性或临床副作用均无关。这些结果表明，法莫替丁与其他H2受体拮抗剂的起效时间相似，但作用持续时间长30%，效力比雷尼替丁强9倍，比西咪替丁强32倍。法莫替丁在胃酸分泌过多状态的长期治疗中安全且高效。
