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衰老对硝苯地平和阿替洛尔处置的影响。

The effect of ageing on the disposition of nifedipine and atenolol.

作者信息

Scott M, Castleden C M, Adam H K, Smith R P, Fitzsimons T J

机构信息

Leicester General Hospital.

出版信息

Br J Clin Pharmacol. 1988 Mar;25(3):289-96. doi: 10.1111/j.1365-2125.1988.tb03306.x.

Abstract
  1. Healthy young and elderly volunteers received 20 mg nifedipine (slow release) orally for 2 weeks with concomitant dosing of atenolol 50 mg orally during the second week. 2. Drug kinetics and dynamics were compared between the groups after a single dose of nifedipine (day 1), after chronic dosing for 1 week (day 8), and following concomitant daily dosing of atenolol (day 15). 3. Plasma profiles of nifedipine were similar within each group on each of the 3 sampling days. The elderly group had higher plasma concentrations from about 6 h but there was no difference in the maximum concentrations achieved. The half-life in the elderly was significantly longer (8.8 +/- 0.9 h) compared with that in the young (5.8 +/- 1.1 h) (P less than 0.01). 4. Blood concentrations of atenolol were higher in the elderly at 12 and 24 h post-dose (P less than 0.001) and the AUC was greater than in the young (P less than 0.001). 5. Systolic blood pressure was reduced by nifedipine in both groups but to a greater extent in the elderly (P less than 0.01); differences in diastolic blood pressure were not significant. Blood pressure was reduced further by the addition of atenolol. Atenolol reduced the heart rate in all subjects.
摘要
  1. 健康的年轻和老年志愿者口服20毫克硝苯地平(缓释片),持续2周,在第二周同时口服50毫克阿替洛尔。2. 在单次服用硝苯地平后(第1天)、慢性给药1周后(第8天)以及每日同时服用阿替洛尔后(第15天),对两组的药物动力学和药效学进行比较。3. 在3个采样日中的每一天,每组内硝苯地平的血浆浓度曲线相似。老年组从约6小时起血浆浓度较高,但所达到的最大浓度没有差异。与年轻人(5.8±1.1小时)相比,老年人的半衰期显著更长(8.8±0.9小时)(P<0.01)。4. 给药后12小时和24小时,老年人的阿替洛尔血药浓度较高(P<0.001),曲线下面积大于年轻人(P<0.001)。5. 两组中硝苯地平均降低了收缩压,但在老年人中降低幅度更大(P<0.01);舒张压差异不显著。加用阿替洛尔后血压进一步降低。阿替洛尔降低了所有受试者的心率。

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