Callaghan J T, Rubin A, Knadler M P, Bergstrom R F
Lilly Research Laboratories, Lilly Laboratory for Clinical Research, Indianapolis, IN 46202.
J Clin Pharmacol. 1987 Aug;27(8):618-24. doi: 10.1002/j.1552-4604.1987.tb03075.x.
Nizatidine is an orally active H2-receptor blocker. Its disposition and safety in eight young and 12 elderly volunteers were investigated. Single oral doses of nizatidine were administered: from 100 mg to 300 mg in the elderly, and from 100 mg to 350 mg in the young. The nizatidine AUC was directly proportional to dose for both groups. Calculated pharmacokinetic variables in the elderly vs. the young were t1/2 = 1.9 vs. 1.6 hr; CLp/f = 32 vs. 40 L/hr, and Vd beta/f = 1.2 vs. 1.3 L/kg. The impaired renal function of some elderly volunteers prolonged nizatidine elimination and lowered its clearance. Renal impairment rather than advanced age per se was the predominant factor in decreasing the nizatidine elimination rate. Because Clcr correlated directly with nizatidine renal clearance, Clcr values may be used to estimate nizatidine dosage reductions in renal insufficiency. During the trial, no serious adverse effects occurred.
尼扎替丁是一种口服有效的H2受体阻滞剂。研究了其在8名年轻志愿者和12名老年志愿者体内的处置情况和安全性。给予单次口服尼扎替丁剂量：老年组为100毫克至300毫克，年轻组为100毫克至350毫克。两组的尼扎替丁AUC均与剂量成正比。老年组与年轻组计算得到的药代动力学变量分别为：t1/2 = 1.9小时对1.6小时；CLp/f = 32升/小时对40升/小时，以及Vd beta/f = 1.2升/千克对1.3升/千克。一些老年志愿者的肾功能受损延长了尼扎替丁的消除时间并降低了其清除率。肾功能损害而非高龄本身是降低尼扎替丁消除率的主要因素。由于肌酐清除率（Clcr）与尼扎替丁肾清除率直接相关，因此Clcr值可用于估计肾功能不全时尼扎替丁的剂量减少情况。在试验期间，未发生严重不良反应。
