孕甾烷X受体(Pregnane X receptor,PXR)为核受体超家族中NR1I亚家族成员,于肝脏和肠道中广泛表达。该受体作为药物代谢的关键调控因子广泛参与药物的吸收、分布、代谢及排泄过程。本文从药物代谢角度分别对PXR参与调节的Ⅰ、Ⅱ相代谢酶...孕甾烷X受体(Pregnane X receptor,PXR)为核受体超家族中NR1I亚家族成员,于肝脏和肠道中广泛表达。该受体作为药物代谢的关键调控因子广泛参与药物的吸收、分布、代谢及排泄过程。本文从药物代谢角度分别对PXR参与调节的Ⅰ、Ⅱ相代谢酶及转运体进行介绍,为临床药物相互作用及针对PXR为靶点的药物研发提供参考。展开更多
AIM： To compare the efficacy and safety of five days apostrophe therapy of mebendazole （MBZ） versus quinacrine （QC） on human giardiasis in children.METHODS： A clinical trial was carried out in paediatric patien...AIM： To compare the efficacy and safety of five days apostrophe therapy of mebendazole （MBZ） versus quinacrine （QC） on human giardiasis in children.METHODS： A clinical trial was carried out in paediatric patients （aged 5-15 years） with confirmed symptomatic G. duodenalis mono-infection. Patients were randomly assigned to receive either MBZ [200 mg taken three times per day GRID） （n = 61）] or QC [2 mg/kg bodyweight tid （n = 61）], both for five days. Follow-up faecal samples were obtained at 3, 5 and 7 d after the end of the treatment.RESULTS： Although the frequency of cure was higher for QC （83.6%） than for MBZ （78.7%）, the difference was not statistically significant （P 〉 0.05）. Adverse events were reported more in the QC group （P 〈 0.05）, all of them transient and self-limiting.CONCLUSION： Despite final cure rates ocurring lower than expected, the overall results of this study reconfirmed the efficacy of MBZ in giardiasis and also indicate that, although comparable to QC, at least in this setting the 5 d course of MBZ did not appear to improve the cure rates in this intestinal parasitic infection.展开更多
文摘孕甾烷X受体(Pregnane X receptor,PXR)为核受体超家族中NR1I亚家族成员,于肝脏和肠道中广泛表达。该受体作为药物代谢的关键调控因子广泛参与药物的吸收、分布、代谢及排泄过程。本文从药物代谢角度分别对PXR参与调节的Ⅰ、Ⅱ相代谢酶及转运体进行介绍,为临床药物相互作用及针对PXR为靶点的药物研发提供参考。
文摘AIM： To compare the efficacy and safety of five days apostrophe therapy of mebendazole （MBZ） versus quinacrine （QC） on human giardiasis in children.METHODS： A clinical trial was carried out in paediatric patients （aged 5-15 years） with confirmed symptomatic G. duodenalis mono-infection. Patients were randomly assigned to receive either MBZ [200 mg taken three times per day GRID） （n = 61）] or QC [2 mg/kg bodyweight tid （n = 61）], both for five days. Follow-up faecal samples were obtained at 3, 5 and 7 d after the end of the treatment.RESULTS： Although the frequency of cure was higher for QC （83.6%） than for MBZ （78.7%）, the difference was not statistically significant （P 〉 0.05）. Adverse events were reported more in the QC group （P 〈 0.05）, all of them transient and self-limiting.CONCLUSION： Despite final cure rates ocurring lower than expected, the overall results of this study reconfirmed the efficacy of MBZ in giardiasis and also indicate that, although comparable to QC, at least in this setting the 5 d course of MBZ did not appear to improve the cure rates in this intestinal parasitic infection.
