作为一种血红蛋白,细胞色素P450酶(CYP450)参与多种物质的代谢,包括内源性物质,外源性物质和药物。据估计,60%的普通处方药需要通过CYP450生物转化。大环内酯对CYP450的影响有助于大环内酯的代谢和药物相互作用(DDI)。目前,关于大环内酯类药物对CYP450的影响的大多数研究集中在CYP3A,但是其他酶和药物组合中存在一些,比如泰利霉素,可以降低肝CYP1A2和CYP3A2的活性。本文总结了大环内酯对CYP450的影响以及由CYP450引起的大环内酯的DDI的一些已发表的应用。并可在后续临床试验中指导药物的合理使用。在某种程度上,可以避免不良药物相互作用引起的中毒。大环内酯类抗生素的不合理使用可能会使大环内酯类抗生素残留在动物源性食品中。人们食用含有大环内酯类抗生素残留的食物是不健康的。因此,大环内酯类药物的合理使用对保障食品安全和保护消费者健康具有重要意义。本文详细介绍了大环内酯对CYP450的影响以及CYP450引起的大环内酯类DDI。此外,它为研究人员在这一领域的进一步探索提供了一个视角。
As a kind of haemoglobin, cytochrome P450 enzymes (CYP450) participate in the metabolism of many substances, including endogenous substances, exogenous substances and drugs. It is estimated that 60% of common prescription drugs require bioconversion through CYP450. The influence of macrolides on CYP450 contributes to the metabolism and drug-drug interactions (DDIs) of macrolides. At present, most studies on the effects of macrolides on CYP450 are focused on CYP3A, but a few exist on other enzymes and drug combinations, such as telithromycin, which can decrease the activity of hepatic CYP1A2 and CYP3A2. This article summarizes some published applications of the influence of macrolides on CYP450 and the DDIs of macrolides caused by CYP450. And the article may subsequently guide the rational use of drugs in clinical trials. To a certain extent, poisoning caused by adverse drug interactions can be avoided. Unreasonable use of macrolide antibiotics may enable the presence of residue of macrolide antibiotics in animal-origin food. It is unhealthy for people to eat food with macrolide antibiotic residues. So it is of great significance to guarantee food safety and protect the health of consumers by the rational use of macrolides. This
review gives a detailed description of the influence of macrolides on CYP450 and the DDIs of macrolides caused by CYP450. Moreover, it offers a perspective for researchers to further explore in this area.