Musson D G, Birk K L, Panebianco D L, Gagliano K D, Rogers J D, Goldberg M R
Merck Research Laboratories, West Point, PA 19486, USA.
Int J Clin Pharmacol Ther. 2001 Oct;39(10):447-52.
Rizatriptan is a serotonin 5-HT1B/1D receptor agonist for acute treatment of migraine. Its pharmacokinetics were assessed in healthy elderly males and females receiving a single 10 mg tablet oral dose. The pharmacokinetic data (AUC(0-infinity) and Cmax) for the elderly in this study were compared with historical data from previous studies for healthy young adults (n = 65).
In a double-blind, parallel, placebo-controlled study, healthy elderly female and male subjects aged 65 or older (n = 8 each) received a single oral dose of 10 mg rizatriptan. Plasma and urine concentrations of drug were determined by HPLC with tandem mass spectrometry detection at several collection time points or intervals starting at predose and postdose over 24 h.
In elderly subjects, the geometric mean values for AUC(0-infinity) and Cmax were 77.7 ng/h/ml and 21.9 ng/ml; the average values for tmax, half-life (t 1/2), renal clearance (Clr), and percent urinary excretion of dose (Ue) were 1.2 h, 1.8 h, 197 ml/min and 9.3%, respectively. The AUC(0-infinity) and Cmax of rizatriptan were similar in elderly and young subjects. The geometric mean AUC ratio of elderly to young was 0.96 with 90% confidence interval (0.83, 1.11), p > 0.25. The geometric mean Cmax ratio was 0.89 with 90% confidence interval (0.72, 109), p > 0.25. No significant pharmacokinetic differences were observed between elderly males and females.
The plasma pharmacokinetics of rizatriptan appear to be similar in the elderly and young. In the elderly, the pharmacokinetics of rizatriptan do not appear to differ between male and female to a clinically significant extent.
利扎曲普坦是一种用于偏头痛急性治疗的5-羟色胺5-HT1B/1D受体激动剂。在健康老年男性和女性单次口服10毫克片剂剂量的情况下对其药代动力学进行了评估。本研究中老年人的药代动力学数据（AUC(0-∞)和Cmax）与先前针对健康年轻成年人（n = 65）的研究中的历史数据进行了比较。
在一项双盲、平行、安慰剂对照研究中，65岁及以上的健康老年女性和男性受试者（各8名）单次口服10毫克利扎曲普坦。在给药前和给药后24小时内的几个采集时间点或时间段，通过高效液相色谱-串联质谱检测法测定血浆和尿液中的药物浓度。
在老年受试者中，AUC(0-∞)和Cmax的几何平均值分别为77.7纳克/小时/毫升和21.9纳克/毫升；tmax、半衰期（t1/2）、肾清除率（Clr）和剂量的尿排泄百分比（Ue）的平均值分别为1.2小时、1.8小时、197毫升/分钟和9.3%。利扎曲普坦的AUC(0-∞)和Cmax在老年和年轻受试者中相似。老年与年轻受试者的几何平均AUC比值为0.96，90%置信区间为（0.83，1.11），p>0.25。几何平均Cmax比值为0.89，90%置信区间为（0.72，1.09），p>0.25。老年男性和女性之间未观察到显著的药代动力学差异。
利扎曲普坦的血浆药代动力学在老年人和年轻人中似乎相似。在老年人中，利扎曲普坦的药代动力学在男性和女性之间似乎没有临床上的显著差异。
