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恶性疟原虫对奎宁和奎尼丁的体内及体外反应

In vivo and in vitro responses to quinine and quinidine of Plasmodium falciparum.

作者信息

Sabchareon A, Chongsuphajaisiddhi T, Sinhasivanon V, Chanthavanich P, Attanath P

出版信息

Bull World Health Organ. 1988;66(3):347-52.

Abstract

A total of 66 Thai children with uncomplicated falciparum malaria were treated orally with regimens of either quinine or quinidine. Radical cures were observed in 85% (28 of 33) of the children who received quinine and in 88% (29 out of 33) of those who received quinidine. Treatment failures in both groups were RI responses.The mean trough level of quinidine (10 mumol/l) was about 2.5-times less than that of quinine (25 mumol/l). The electrocardiograms of the two treatment groups differed significantly in that there was an acute prolongation of the QT(c) interval in 56% of those who received quinidine compared with 21.0% of those given quinine. In vitro assays of the pretreatment drug susceptibilities of the isolates of Plasmodium falciparum indicated that the mean minimum inhibitory concentration (MIC) for quinidine (1.44 mumol/l) was about half that for quinine (3.02 mumol/l). Although both drugs are equally effective, quinine is recommended for treatment of multidrug-resistant malaria in paediatric patients, primarily because of the cardiac effects produced by quinidine.

摘要

总共66名患单纯恶性疟原虫疟疾的泰国儿童接受了口服奎宁或奎尼丁治疗方案。接受奎宁治疗的儿童中85%(33名中的28名)实现了根治,接受奎尼丁治疗的儿童中这一比例为88%(33名中的29名)。两组的治疗失败均为RI反应。奎尼丁的平均谷浓度(10微摩尔/升)约为奎宁(25微摩尔/升)的2.5倍。两个治疗组的心电图有显著差异,接受奎尼丁治疗的患者中有56%出现QT(c)间期急性延长,而接受奎宁治疗的患者中这一比例为21.0%。对恶性疟原虫分离株治疗前药物敏感性的体外检测表明,奎尼丁的平均最低抑菌浓度(MIC)(1.44微摩尔/升)约为奎宁(3.02微摩尔/升)的一半。虽然两种药物疗效相当,但推荐奎宁用于治疗儿童耐多药疟疾,主要是因为奎尼丁会产生心脏效应。

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本文引用的文献

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QUANTITATIVE DETERMINATION OF QUINIDINE IN PLASMA.血浆中奎尼丁的定量测定
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