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Inhibitory Effect of Japanese Traditional Kampo Formula Frequently Prescribed in Gynecological Clinics on CYP3A4

机译:妇科临床常用日本传统汉方配方对CYP3A4的抑制作用

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Recently, the use of herbal medicines has become popular, and information on drug interactions between herbal medicines and chemical drugs is needed in clinics. In Japan, the number of patients taking Japanese traditional Kampo medicines has been increasing, and the proper drug information about herb-drug interaction is highly demanded. The most established herb-drug interaction is the case of grapefruit juice (GFJ) via the inhibition on CYP3A4 expressed in the small intestine. In the present study, we compared the inhibitory titer on CYP3A4 between the target Kampo products and GFJ used as positive control. We evaluated the inhibitory effects of GFJ and three extracts of Kampo formulas frequently used in gynecological clinics on CYP3A4 in vitro and calculated the related titer of one-time dosage of Kampo formulas to GFJ in order to predict its effect on clinics. Although the extracts of these three Kampo formulas and the most of crude drug components in the formulas exhibited the inhibitory effects on CYP3A4 in some levels, the possibilities of tokishakuyakusan and keishibukuryogan to cause drug interaction can be quite low; however, it is possible that the excessive dosage of kamishoyosan may cause drug interaction with the substrate of CYP3A4 in clinics.
机译:近来,草药的使用已变得流行,并且临床上需要关于草药与化学药物之间的药物相互作用的信息。在日本,服用日本传统汉方药的患者数量一直在增加,因此,人们迫切需要有关草药与药物相互作用的正确药物信息。葡萄柚汁(GFJ)是通过抑制小肠中表达的CYP3A4而建立的最有效的草药-药物相互作用。在本研究中,我们比较了目标Kampo产品和用作阳性对照的GFJ对CYP3A4的抑制效价。我们评估了GFJ和妇科诊所中常用的三种Kampo配方提取物在体外对CYP3A4的抑制作用,并计算了一次剂量的Kampo配方对GFJ的相关滴度,以预测其对临床的影响。尽管这三种坎波配方的提取物和配方中的大多数粗制药物成分在一定程度上均表现出对CYP3A4的抑制作用,但tokishakuyakusan和keishibukuryogan引起药物相互作用的可能性非常低。然而,在临床中过量的胺磺酰脲类药物可能会引起药物与CYP3A4底物的相互作用。

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