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莫雷西嗪在年轻患者中的药代动力学。

Pharmacokinetics of moricizine in young patients.

作者信息

Rice P J, LeClair I O, Stone W L, Mehta A V

机构信息

Department of Pharmacology, James H. Quillen College of Medicine, East Tennessee State University, Johnson City 37614-0577, USA.

出版信息

J Clin Pharmacol. 1995 Oct;35(10):1016-9. doi: 10.1002/j.1552-4604.1995.tb04019.x.

Abstract

Moricizine is a novel phenothiazine antiarrhythmic agent that depresses the activity of ectopic foci, has a low incidence of adverse effects relative to other agents, and is useful in treating pediatric atrial ectopic tachycardia. A study was conducted to determine the pharmacokinetics of moricizine in children after oral administration. Moricizine was isolated from frozen serum obtained from four male patients (ages 7, 8, 9, and 18 years) receiving the drug for supraventricular tachycardia and analyzed by high-performance liquid chromatography with ultraviolet detection according to an established protocol. Peak serum levels were between 400 and 2000 ng/mL. Elimination of moricizine did not follow simple single-compartment pharmacokinetics. In three patients we observed an increase or slower decline in blood level occurring after 4 hours. Because of the paroxysmal nature of the tachycardias, decreases in patient heart rate could not be correlated with moricizine blood level. These results suggest that the pediatric pharmacokinetics of moricizine excretion are complex and may differ from those seen in adults.

摘要

莫雷西嗪是一种新型吩噻嗪类抗心律失常药物,可抑制异位起搏点的活性,相对于其他药物,其不良反应发生率较低,可用于治疗小儿房性异位性心动过速。进行了一项研究以确定口服给药后莫雷西嗪在儿童体内的药代动力学。从4名接受该药治疗室上性心动过速的男性患者(年龄分别为7、8、9和18岁)获得的冷冻血清中分离出莫雷西嗪,并按照既定方案通过高效液相色谱-紫外检测法进行分析。血清峰值水平在400至2000 ng/mL之间。莫雷西嗪的消除不符合简单的单室药代动力学。在3名患者中,我们观察到4小时后血药水平升高或下降缓慢。由于心动过速的阵发性特点,患者心率的下降与莫雷西嗪血药水平无关。这些结果表明,莫雷西嗪排泄的儿童药代动力学较为复杂,可能与成人不同。

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