Title:A Review: Effects of Macrolides on CYP450 Enzymes
Volume: 21
Issue: 12
Author(s): Liyun Zhang, Xiaoqing Xu, Sara Badawy, Awais Ihsan, Zhenli Liu, Changqing Xie, Xu Wang*Yanfei Tao*
Affiliation:
- 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
- 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
Keywords:
CYP450, Macrolides, CYP3A, CYP1A, DDIs, metabolic interaction.
Abstract: 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.
