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In vitro evaluation of quinidine sensitivity in brazilian Plasmodium falciparum isolates: comparative analysis to quinine and chloroquine

机译:巴西恶性疟原虫分离株对奎尼丁敏感性的体外评估:对奎宁和氯喹的比较分析

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Falciparum malaria represents a serious and an increasing world public health problem due to the acquired parasite's resistance to the most available drugs. In some endemic areas, quinidine, a diastereoisomer of the antimalarial quinine, has been employed for replacing the latter. In order to evaluate the use of quinidine as an alternative to the increasing loss of quinine effectiveness in Brazilian P. falciparum strains, as has been observed in the Amazon area, we have assayed quinidine, quinine and chloroquine. The in vitro microtechnique was employed. All isolates showed to be highly resistant to chloroquine. Resistance to quinine was not noted although high MIC (minimal inhibitory concentration) values have been observed. These data corroborate the decreasing sensitivity to quinine in strains from Brazil. Quinidine showed IC50 from 0.053 to 4.577 mumol/L of blood while IC50 from 0.053 to 8.132 mumol/L of blood was estimated for quinine. Moreover, clearance of the parasitemia was observed in concentrations lower than that used for quinidine in antiarrhythmic therapy, confirming our previous data. The results were similar to African isolate.
机译:由于后天寄生虫对大多数药物的抗药性,恶性疟疾已成为一个严重且日益严重的世界公共卫生问题。在某些流行地区,已使用奎尼丁(抗疟疾奎宁的非对映异构体)替代后者。为了评估在巴西恶性疟原虫菌株中使用奎尼丁作为代替奎宁效力增加的损失的替代方法,如在亚马逊地区所观察到的,我们对奎尼丁,奎宁和氯喹进行了分析。采用了体外微技术。所有分离株均显示出对氯喹的高度抗性。尽管已观察到高MIC(最低抑菌浓度)值,但未发现对奎宁有抗药性。这些数据证实了巴西菌株对奎宁的敏感性下降。奎尼丁的血液IC50为0.053至4.577摩尔/升,而奎宁的IC50为0.053至8.132摩尔/升。此外,在抗心律失常治疗中观察到的寄生虫病清除率低于奎尼丁,因此证实了我们先前的数据。结果类似于非洲分离株。

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