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[钙离子转运阻滞剂作为疟原虫耐药性的逆转剂。1. 维拉帕米对伯氏疟原虫体内氯喹耐药性及恶性疟原虫体外氯喹耐药性的影响]

[Ca++ ion transport blockers as reversants of the drug resistance of malarial parasites. 1. The effect of verapamil on the resistance to chloroquine in vivo of Plasmodium berghei and in vitro of Plasmodium falciparum].

作者信息

Rabinovich S A, Orlov V S, Dadasheva N R, Bukhtin B A, Maksakovskaia E V, Shcherbakov A M, Nguyen V K, Nguyen D S, Vu T T

出版信息

Med Parazitol (Mosk). 1996 Jan-Mar(1):18-22.

PMID:8700004
Abstract

The reversing action of verapamil on the effect of chloroquine was found in in vivo experiments by using a model P. berghei resistant to chloroquine, an LNK65 isolate having a naturally lower resistance to the agent, and its polyresistant strain with the acquired resistance to chloroquine and fansidar, as well as by employing the chlorine-resistant P. falciparum isolates from the south of the Socialist Republic of Vietnam. The magnitude of this effect was related to the dose of verapamil, the frequency of administration of a combination of the agents in vivo, while that was associated to the concentration of verapamil and the level of isolate resistance to chloroquine in vitro which was the most pronounced. Taking into account the dose-dependent effect of verapamil, it can be suggested that increasing its concentration in combination with chloroquine can provide a more marked reversing action with lower chloroquine concentrations. The parameters accepted by the authors in evaluating the combined effect enable the effect of the verapamil/chloroquine concentration to be regarded as potentiation.

摘要

通过使用对氯喹耐药的伯氏疟原虫模型、对该药物天然耐药性较低的LNK65分离株及其对氯喹和 Fansidar获得性耐药的多耐药菌株,以及采用来自越南社会主义共和国南部的耐氯喹恶性疟原虫分离株,在体内实验中发现了维拉帕米对氯喹作用的逆转作用。这种作用的程度与维拉帕米的剂量、体内联合用药的给药频率有关,而在体外则与维拉帕米的浓度和分离株对氯喹的耐药水平最为相关,后者最为明显。考虑到维拉帕米的剂量依赖性作用,可以认为增加其与氯喹联合使用时的浓度,在较低氯喹浓度下可产生更显著的逆转作用。作者在评估联合作用时采用的参数使维拉帕米/氯喹浓度的作用可被视为增效作用。

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