Movin G, Gustafson L, Franzén G, Widerlöv E, Soni S D, Tench D, Nilsson L, Yisak W
Astra Research Centre, Södertälje, Sweden.
Acta Psychiatr Scand Suppl. 1990;358:176-80. doi: 10.1111/j.1600-0447.1990.tb05313.x.
The pharmacokinetics of remoxipride when given as single doses of 50 mg and repeated doses of 50 mg, 100 mg, and 200 mg twice daily to 10 elderly psychotic patients (71-89 years) were compared with the findings of two other studies to reveal any age-related differences. The three studies comprised a total of 38 patients in three distinct age groups: elderly (71-89 years), middle-aged (46-69 years) and young (19-36 years). AUC, Cmax and Cmin of both total and unbound remoxipride increased with increasing age. The unbound fraction was similar in the three age groups. The half-life was prolonged in the elderly, most probably caused by a decrease in intrinsic clearance. A two-fold increase in AUC of both total and unbound concentrations was observed in the elderly group compared to the young, suggesting that patients over 70 years in general require half the dose needed by young adult patients. In general, the pharmacokinetics of remoxipride in the elderly are linear.
将单剂量50毫克以及每日两次重复剂量50毫克、100毫克和200毫克的瑞莫必利给予10名老年精神病患者(71 - 89岁),并将其药代动力学与另外两项研究的结果进行比较,以揭示任何与年龄相关的差异。这三项研究总共涵盖了三个不同年龄组的38名患者:老年组(71 - 89岁)、中年组(46 - 69岁)和青年组(19 - 36岁)。总瑞莫必利和游离瑞莫必利的AUC、Cmax和Cmin均随年龄增长而增加。三个年龄组的游离分数相似。老年患者的半衰期延长,很可能是由内在清除率降低所致。与青年组相比,老年组总浓度和游离浓度的AUC均增加了两倍,这表明70岁以上的患者一般所需剂量为年轻成年患者的一半。总体而言,瑞莫必利在老年患者中的药代动力学呈线性。