A Pharmacokinetic Study of Acebutolol in Aged Subjects as Compared to Young Subjects

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Abstract
Pharmacokinetics of acebutolol were studied in hypertensive aged patients (79.4 .+-. 3.8 yr) and in young healthy subjects (23.4 .+-. 0.7 yr) after i.v. (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 i.v. administration, apparent volume of distribution (1.5 vs. 2.4 l .cntdot. kg-1, P < 0.05) and total body clearance (6.2 vs. 8.98 ml .cntdot. min-1 .cntdot. kg-1, ns [non-significant]) of acebutolol are smaller in elderly than in young men. After oral administration, maximum plasma levels (28.03 vs. 9.68 .mu.g .cntdot. l-1 .cntdot. kg-1) and area under the curve (163.1 vs. 57.5 .mu.g .cntdot. l-1 .cntdot. h .cntdot. kg-1) are significantly higher in aged patients than in young subjects (P < 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). Acebutolol and diacetolol may accumulate in elderly.

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