氯喹在健康人体内的药代动力学和心电图效应。

M D Bustos, F Gay, B Diquet, P Thomare, D Warot
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引用次数: 0

摘要

对3名健康男性志愿者以100 mg基础剂量/天的剂量给予氯喹预防治疗,连续25天,然后以25 mg基础剂量/kg的治疗剂量连续3天。受试者在预防的第三周达到有效的氯喹(平均50微克/升)和去乙基氯喹(平均17微克/升)浓度,强调需要在旅行前两周开始氯喹预防。在治疗期第2天,每小时心电图监测显示T波减小,QTc间期延长,在3天治疗剂量期间累积表现,但无心脏症状。氯喹的剂量依赖性累积效应在治疗期间血药浓度升高。治疗期后,随着药物浓度逐渐降低,心电图读数自然恢复正常。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
The pharmacokinetics and electrocardiographic effects of chloroquine in healthy subjects.

Chloroquine prophylaxis was administered to 3 healthy male volunteers at 100 mg base/day for 25 days, followed by the curative dose at 25 mg base/kg for 3 days. Subjects attained effective chloroquine (mean = 50 micrograms/l) and desethylchloroquine (mean = 17 micrograms/l) concentrations by the 3rd week of prophylaxis, underlining the need to start chloroquine prophylaxis two weeks before travel. On the second day of the treatment period, hourly electrocardiographic monitoring showed a diminution of the T wave and prolongation of the QTc interval, manifesting cumulatively during the 3 days' curative dose, but with no cardiac symptoms. A dose-dependent cumulative effect of chloroquine was demonstrated with higher blood concentrations during the treatment period. Electrocardiographic readings spontaneously normalized after the treatment period as drug concentrations diminished progressively.

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