Roux A, Henry J F, Fouache Y, Chau N P, Hervy M P, Forette F, Bourdarias J P, Flouvat B
Gerontology. 1983;29(3):202-8. doi: 10.1159/000213115.
Pharmacokinetics of acebutolol have been studied in hypertensive aged patients (79.4 +/- 3.8 years) and in young healthy subjects (23.4 +/- 0.7 years) after intravenous (0.35 mg/kg bolus) and oral administration (400 mg). Acebutolol and diacetolol, the main metabolite, plasma levels were determined by high-pressure liquid chromatography. After intravenous administration, apparent volume of distribution (1.5 vs. 2.4 liter . kg-1, p less than 0.05) and total body clearance (6.2 vs. 8.8 ml . min-1 . kg-1, n.s.) of acebutolol are smaller in elderly than in young men. After oral administration, maximum plasma levels (28.03 vs. 9.68 micrograms . l-1 . kg-1) and area under the curve (163.1 vs. 57.5 micrograms . l-1 . h . kg-1) are significantly higher in aged patients than in young subjects (p less than 0.001). Acebutolol and diacetolol plasma half-lives increase in elderly patients (11.6 vs. 7.2 h and 14.8 vs. 12 h respectively). These results suggest a possible accumulation of acebutolol and diacetolol in elderly.
已对老年高血压患者（79.4±3.8岁）和年轻健康受试者（23.4±0.7岁）静脉注射（0.35mg/kg推注）和口服（400mg）醋丁洛尔后的药代动力学进行了研究。通过高压液相色谱法测定醋丁洛尔及其主要代谢物双醋洛尔的血浆水平。静脉注射后，老年患者醋丁洛尔的表观分布容积（1.5对2.4升·kg-1，p<0.05）和总体清除率（6.2对8.8ml·min-1·kg-1，无显著性差异）均低于年轻男性。口服给药后，老年患者的血浆最高水平（28.03对9.68μg·l-1·kg-1）和曲线下面积（163.1对57.5μg·l-1·h·kg-1）显著高于年轻受试者（p<0.001）。老年患者中醋丁洛尔和双醋洛尔的血浆半衰期延长（分别为11.6对7.2小时和14.8对12小时）。这些结果表明醋丁洛尔和双醋洛尔在老年人中可能会蓄积。
