年龄对大鼠血浆和脑组织中地西泮水平的影响。

Effect of age on levels of diazepam in plasma and brain of rats.

作者信息

Klotz U

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 1979 Jun;307(2):167-9. doi: 10.1007/BF00498459.

Abstract

The pharmacokinetics and distribution in brain and cerebellum of diazepam after a single dose were studied in middle aged (6 months) and old (18 months) rats. Following the single intravenous bolus of 5 mg/kg diazepam was eliminated more slowly in old rats (T 1/2 (beta) = 3.1 H) than in middle aged rats (1.4H). This was due to an increase in the apparent volume of distribution Vd beta from 11.0 l/kg (control rats) to 29.5 l/kg. Concentrations of diazepam in brain and cerebellum were in the same range (0.5-1.1 ng/mg) in both groups after this dose. We conclude that the distribution of diazepam is age-dependent which might be due to an altered body composition.

摘要

研究了单次给药后地西泮在中年（6个月）和老年（18个月）大鼠体内的药代动力学以及在脑和小脑中的分布情况。静脉注射5mg/kg地西泮后，老年大鼠（T 1/2（β）= 3.1小时）体内地西泮的消除速度比中年大鼠（1.4小时）慢。这是由于表观分布容积Vdβ从11.0升/千克（对照大鼠）增加到29.5升/千克。给药后，两组大鼠脑和小脑中地西泮的浓度处于相同范围（0.5 - 1.1纳克/毫克）。我们得出结论，地西泮的分布具有年龄依赖性，这可能是由于身体组成的改变所致。