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苯海拉明:老年女性的药代动力学及精神运动效应

Diphenhydramine: kinetics and psychomotor effects in elderly women.

作者信息

Berlinger W G, Goldberg M J, Spector R, Chiang C K, Ghoneim M

出版信息

Clin Pharmacol Ther. 1982 Sep;32(3):387-91. doi: 10.1038/clpt.1982.176.

Abstract

Kinetics and sedative and psychomotor effects of diphenhydramine were investigated in elderly Caucasian women (greater than 64 yr. old). In a double-blind trial, each of 12 healthy subjects received on one of three occasions 50 mg/70 kg IV or oral diphenhydramine HCl or oral placebo. Plasma levels of diphenhydramine were measured in six subjects and tests of sedation and psychomotor performance were performed hourly for 8 hr in all subjects. Kinetic analysis showed that the volume of distribution (295 +/- 50 [SEM] l/70 kg), clearance (42 +/- 5 l/70 kg/hr), and plasma t1/2 (4.9 +/- 0.7 hr) were of the same order as in young adults. As in young adults, there was minimal psychomotor impairment after oral and after intravenous diphenhydramine. In contrast to young adults, however, elderly women did not report significant sedation after diphenhydramine. These results suggest that diphenhydramine may not be an effective sedative/hypnotic in elderly women.

摘要

在老年白人女性(年龄大于64岁)中研究了苯海拉明的动力学以及镇静和精神运动效应。在一项双盲试验中,12名健康受试者中的每一位在三个不同场合分别接受了50mg/70kg静脉注射或口服盐酸苯海拉明或口服安慰剂。对6名受试者测定了苯海拉明的血浆水平,并对所有受试者每小时进行一次长达8小时的镇静和精神运动表现测试。动力学分析表明,分布容积(295±50[标准误]l/70kg)、清除率(42±5l/70kg/小时)和血浆半衰期(4.9±0.7小时)与年轻人处于同一水平。与年轻人一样,口服和静脉注射苯海拉明后精神运动功能受损最小。然而,与年轻人不同的是,老年女性在服用苯海拉明后并未报告有明显的镇静作用。这些结果表明,苯海拉明在老年女性中可能不是一种有效的镇静/催眠药。

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