Vargas R, Ryan J, McMahon F G, Regel G, Offen W W, Matsumoto C
Clinical Research Center, New Orleans, Louisiana 70112.
J Clin Pharmacol. 1988 Jan;28(1):71-5. doi: 10.1002/j.1552-4604.1988.tb03103.x.
Nizatidine was studied in six high-acid-secretor (basal secretion, greater than or equal to 5 mEq/hr) male volunteers in a randomized, double-blind, nonbalanced, cross-over, placebo and standard drug-controlled study. Doses of 75 mg, 150 mg, and 300 mg bid were compared with placebo and cimetidine 300 mg qid. Nocturnal acid output was significantly reduced (P less than .01) by all doses of nizatidine (36 +/- 22, 36 +/- 31, and 26 +/- 20 mEq) with 75 mg, 150 mg and 300 mg, respectively, and also by cimetidine (43 +/- 39 mEq) as compared with placebo (101 +/- 61 mEq). Nizatidine also significantly reduced meal-stimulated acid secretion at breakfast (14 +/- 9, 9 +/- 7, and 5 +/- 6 mEq/2 hours with 75 mg, 150 mg, and 300 mg, respectively, P less than .01), at lunch (50 +/- 22, 57 +/- 22 and 50 +/- 35 mEq/2 hours, P less than .05) but did not have any effect at dinner (65 +/- 16, 78 +/- 24, and 71 +/- 17 mEq/2 hours) whereas cimetidine, given every 6 hours, significantly (P less than .01) reduced meal-stimulated acid secretion (25 +/- 16, 27 +/- 20 and 31 +/- 15 mEq/2 hours, breakfast, lunch, and dinner, respectively) as compared with placebo (81 +/- 30, 76 +/- 25, and 66 +/- 16 mEq/2 hours, breakfast, lunch, and dinner, respectively). Both drugs have a similar pharmacokinetic profile. Nizatidine seems to be a promising H2 antagonist, more potent than cimetidine (on an mg/mg basis), and efficacy studies on gastric acid disorders should be performed.
在一项随机、双盲、非平衡、交叉、安慰剂和标准药物对照研究中，对6名高胃酸分泌者（基础分泌量大于或等于5 mEq/小时）男性志愿者进行了尼扎替丁的研究。将每日两次服用75毫克、150毫克和300毫克的剂量与安慰剂和每日四次服用300毫克西咪替丁进行比较。与安慰剂（101±61 mEq）相比，所有剂量的尼扎替丁（分别为75毫克、150毫克和300毫克时，夜间酸分泌量分别显著降低至36±22、36±31和26±20 mEq）以及西咪替丁（43±39 mEq）均能显著降低夜间酸分泌量（P＜0.01）。尼扎替丁还能显著降低早餐时的餐刺激酸分泌（75毫克、150毫克和300毫克时，分别为14±9、9±7和5±6 mEq/2小时，P＜0.01），午餐时（50±22、57±22和50±35 mEq/2小时，P＜0.05），但对晚餐时的酸分泌无任何影响（65±16、78±24和71±17 mEq/2小时），而每6小时服用一次的西咪替丁与安慰剂（早餐、午餐和晚餐时分别为81±30、76±25和66±16 mEq/2小时）相比，能显著降低餐刺激酸分泌（早餐、午餐和晚餐时分别为25±16、27±20和31±15 mEq/2小时，P＜0.01）。两种药物具有相似的药代动力学特征。尼扎替丁似乎是一种有前景的H2拮抗剂，比西咪替丁更有效（按毫克/毫克计算），应开展关于胃酸紊乱的疗效研究。
