Institute of Specific Prophylaxis and Tropical Medicine, Center for Pathophysiology, Infectiology and Immunology, Medical University of Vienna, Vienna, Austria.
Wien Klin Wochenschr. 2010 Oct;122 Suppl 3:61-5. doi: 10.1007/s00508-010-1459-1.
The pharmacodynamic interaction between lumefantrine and monodesbutyl-benflumetol has been investigated in 44 fresh isolates of patients with a Plasmodium falciparum infection from the region of Mae Sot (Thailand). Both substances proved to be effective against parasite maturation within the test concentration range, with monodesbutyl-benflumetol being effective at a lower concentration than lumefantrine. Synergism between the two substances was evaluated with a combination of lumefantrine and monodesbutyl-benflumetol at a ratio of 4.25:1. The geometric mean values for complete inhibition of schizont maturation were 1035.7 nM for lumefantrine, 655 nM for monodesbutyl-benflumetol and 222.5 nM for the combination of both. An analysis for interaction according to the method of Berenbaum indicates a moderate synergism at the IC(50), which gets stronger with increasing ICs and reaches the highest level at the IC(99). The geometric mean of the sums of the FIC(50) is 0.73, of the FIC(90) it is 0.37 and of the FIC(99) it is 0.25.
在来自泰国湄索地区的 44 株新鲜疟原虫感染患者分离株中,研究了盐酸甲氟喹与单去乙基-苯芴醇之间的药效学相互作用。两种物质都能在试验浓度范围内有效抑制寄生虫的成熟,单去乙基-苯芴醇的作用浓度低于盐酸甲氟喹。用 4.25:1 的比例将两种物质混合,评估两者之间的协同作用。完全抑制裂殖体成熟的几何平均抑制浓度分别为盐酸甲氟喹 1035.7 nM,单去乙基-苯芴醇 655 nM,两者联合应用为 222.5 nM。根据 Berenbaum 方法进行的相互作用分析表明,在 IC(50)处存在中等协同作用,随着 IC 的增加而增强,在 IC(99)处达到最高水平。FIC(50)之和的几何平均值为 0.73,FIC(90)之和的几何平均值为 0.37,FIC(99)之和的几何平均值为 0.25。