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丙吡胺在健康人体志愿者中的消除动力学及尿排泄情况。

Elimination kinetics and urinary excretion of disopyramide in human healthy volunteers.

作者信息

Bonde J, Jensen N M, Pedersen L E, Graudal N A, Angelo H R, Kampmann J P

机构信息

Department of Clinical Physiology, Frederiksberg Hospital, Copenhagen, Denmark.

出版信息

Pharmacol Toxicol. 1988 May;62(5):298-301. doi: 10.1111/j.1600-0773.1988.tb01891.x.

Abstract

Elimination kinetics and the renal handling of disopyramide was examined in 8 healthy volunteers. Approximately 50% of the administered disopyramide undergoes hepatic metabolism (metabolic clearance = 116.1 +/- 42.2 ml/min.), while the rest is excreted by the kidneys (renal clearance = 101.9 +/- 21.6 ml/min.). Total renal excretion rate of disopyramide was 0.676 +/- 0.188 mumol/min. and 0.258 +/- 0.029 mumol/min. was excreted by glomerular filtration leaving a net tubular secretion of 60% of the total renal elimination. A significant positive correlation was observed between total serum concentrations and renal clearance values of disopyramide while no significant correlation could be obtained between serum concentrations of the unbound drug and renal clearance values of disopyramide, implying a constant value of unbound renal clearance. Hepatic blood flow was significantly (P less than 0.005) decreased following disopyramide infusion.

摘要

在8名健康志愿者中研究了丙吡胺的消除动力学及肾脏对其的处理情况。给予的丙吡胺约50%经肝脏代谢(代谢清除率 = 116.1 ± 42.2 ml/分钟),其余经肾脏排泄(肾脏清除率 = 101.9 ± 21.6 ml/分钟)。丙吡胺的总肾脏排泄率为0.676 ± 0.188 μmol/分钟,经肾小球滤过排泄的为0.258 ± 0.029 μmol/分钟,肾小管净分泌占肾脏总消除量的60%。观察到丙吡胺的血清总浓度与肾脏清除率值之间存在显著正相关,而游离药物的血清浓度与丙吡胺的肾脏清除率值之间未获得显著相关性,这意味着游离肾脏清除率为恒定值。输注丙吡胺后肝血流量显著降低(P < 0.005)。

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