Munn S, Bailey R R, Begg E, Ebert R, Ferry D G
N Z Med J. 1980 Apr 23;91(658):289-91.
This study was undertaken to examine the elimination of orally administered acebutolol and its major acetyl metabolite in four healthy controls and seven patients with varying degrees of renal functional impairment. Analysis of acebutolol and its metabolites was undertaken using a high performance liquid chromatographic method. Plasma concentrations of acebutolol and the acetyl metabolite were greater in patients with renal functional impairment than in controls. The elimination of acebutolol did not appear to be influenced by impaired renal function. However the elimination of the acetyl metabolite decreased as renal function diminished. Acebutolol has a major non-renal route of elimination, but the acetyl metabolite (also a beta-adrenoreceptor blocking drug) is primarily excreted by the kidney and may accumulate in renal failure.
本研究旨在检测4名健康对照者和7名不同程度肾功能损害患者口服醋丁洛尔及其主要乙酰化代谢产物后的消除情况。采用高效液相色谱法对醋丁洛尔及其代谢产物进行分析。肾功能损害患者体内醋丁洛尔及其代谢产物的血浆浓度高于对照者。醋丁洛尔的消除似乎不受肾功能损害的影响。然而，随着肾功能减退，乙酰化代谢产物的消除减少。醋丁洛尔有一条主要的非肾消除途径，但乙酰化代谢产物（也是一种β-肾上腺素受体阻断药）主要经肾脏排泄，可能在肾衰竭时蓄积。
