National Reference Laboratory of Veterinary Drug Residues (HZAU) and MAO Key Laboratory for Detection of Veterinary Drug Residues, Huazhong Agricultural University, Wuhan, Hubei 430070, China.
Curr Drug Metab. 2020;21(12):928-937. doi: 10.2174/1389200221666200817113920.
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.
作为血红蛋白的一种，细胞色素 P450 酶（CYP450）参与许多物质的代谢，包括内源性物质、外源性物质和药物。据估计，60%的常用处方药需要通过 CYP450 进行生物转化。大环内酯类药物对 CYP450 的影响有助于大环内酯类药物的代谢和药物相互作用（DDIs）。目前，大多数关于大环内酯类药物对 CYP450 的影响的研究都集中在 CYP3A 上，但也有一些关于其他酶和药物组合的研究，如泰利霉素，它可以降低肝 CYP1A2 和 CYP3A2 的活性。本文总结了一些已发表的关于大环内酯类药物对 CYP450 的影响以及由 CYP450 引起的大环内酯类药物相互作用的应用，并可能在临床试验中指导药物的合理使用。在一定程度上可以避免因药物相互作用而导致的中毒。不合理使用大环内酯类抗生素可能会使动物源性食品中存在大环内酯类抗生素残留。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，合理使用大环内酯类药物对于保证食品安全和保护消费者健康具有重要意义。本综述详细描述了大环内酯类药物对 CYP450 的影响以及由 CYP450 引起的大环内酯类药物相互作用，并为研究人员在这一领域的进一步探索提供了一个视角。
