Roles of rifampicin in drug-drug interactions: underlying molecular mechanisms involving the nuclear pregnane X receptor.
Roles of rifampicin in drug-drug interactions: underlying molecular mechanisms involving the nuclear pregnane X receptor.
复制标题
利福平在药物相互作用中的作用：涉及核孕烷 X 受体的潜在分子机制。
DOI：
10.1186/1476-0711-5-3
复制
发表时间：
2006-02-15
影响因子：
5.7
通讯作者：
Raymond, Kenneth
中科院分区：
文献类型：
--
作者：
Chen, Jiezhong;Raymond, Kenneth
利福平是治疗结核病的重要药物，尽管其对药物间相互作用的广泛影响，但仍被广泛使用，造成严重问题。这种相互作用的临床重要性包括导致次优或失败治疗的自诱导。利福平对其他药物的伴随给药效应可导致其代谢或转运改变，这些药物通过细胞色素P450代谢或通过胃肠道和肝脏中的P-糖蛋白转运。这篇综述文章总结了最近的研究结果，重点是用于解释这些广泛的药物相互作用的分子机制。一般而言，利福平可作用于一种模式：利福平激活细胞核中的胞苷烷X受体，进而影响细胞色素P450、葡萄糖醛酸转移酶和P-糖蛋白活性。这种作用模式可以解释许多利福平诱导的药物相互作用。然而，通过其他机制的影响也有报道，这使得对这种药物相互作用的任何解释都更加复杂。
Rifampicin, an important drug in the treatment of tuberculosis, is used extensively despite its broad effects on drug-drug interactions, creating serious problems. The clinical importance of such interactions includes autoinduction leading to suboptimal or failed treatment. The concomitantly administered effects of rifampicin on other drugs can result in their altered metabolism or transportation that are metabolised by cytochromes P450 or transported by p-glycoprotein in the gastrointestinal tract and liver. This review paper summarises recent findings with emphases on the molecular mechanisms used to explain these broad drug-drug interactions. In general, rifampicin can act on a pattern: rifampicin activates the nuclear pregnane X receptor that in turn affects cytochromes P450, glucuronosyltransferases and p-glycoprotein activities. This pattern of action may explain many of the rifampicin inducing drug-drug interactions. However, effects through other mechanisms have also been reported and these make any explanation of such drug-drug interactions more complex.