Sonne J, Loft S, Døssing M, Boesgaard S, Andreasen F
Department of Medicine, Hvidovre Hospital, Denmark.
Br J Clin Pharmacol. 1991 Jun;31(6):719-22. doi: 10.1111/j.1365-2125.1991.tb05602.x.
The effect of extreme old age on the pharmacokinetics and pharmacodynamics of orally administered oxazepam 15 mg was studied in 10 healthy elderly (age 80-94 years) institutionalised subjects and 10 healthy young controls (age 26-42 years). The total oxazepam clearance was 1.24 (0.91-1.80) ml min-1 kg-1 (median and range) and 1.44 (0.88-2.13) ml min-1 kg-1 in the elderly and young, respectively (NS), and the elimination half-lives were 8.1 (5.5-10.8) h and 5.7 (4.9-6.2) h. respectively (P less than 0.01). The percent of unbound oxazepam was greater in the elderly; 9.8 (8.1-13.3)% as opposed to 5.1 (3.7-5.9)% in the young (P less than 0.0001). Clearance of unbound oxazepam was lower in the elderly, median values being 13.8 (7.1-21.1) ml min-1 kg-1 compared with 30.3 (18.3-41.5) ml min-1 kg-1 in the young (P less than 0.0001). A single 15 mg dose oxazepam decreased the ability of the elderly to perform a finger tapping test at 3 h but not 8 h after drug administration, whereas placebo had no effect at either times. No effect was observed in the young subjects.
研究了极端高龄对口服15毫克奥沙西泮的药代动力学和药效学的影响，研究对象为10名入住机构的健康老年人（年龄80 - 94岁）和10名健康年轻对照者（年龄26 - 42岁）。老年人和年轻人的奥沙西泮总清除率分别为1.24（0.91 - 1.80）毫升·分钟⁻¹·千克⁻¹（中位数和范围）和1.44（0.88 - 2.13）毫升·分钟⁻¹·千克⁻¹（无显著性差异），消除半衰期分别为8.1（5.5 - 10.8）小时和5.7（4.9 - 6.2）小时（P < 0.01）。老年人中未结合奥沙西泮的百分比更高；为9.8（8.1 - 13.3）%，而年轻人中为5.1（3.7 - 5.9）%（P < 0.0001）。老年人中未结合奥沙西泮的清除率较低，中位数为13.8（7.1 - 21.1）毫升·分钟⁻¹·千克⁻¹，而年轻人中为30.3（18.3 - 41.5）毫升·分钟⁻¹·千克⁻¹（P < 0.0001）。单次15毫克剂量的奥沙西泮使老年人在给药后3小时而非8小时进行手指敲击试验的能力下降，而安慰剂在这两个时间点均无影响。在年轻受试者中未观察到影响。
