Abstract:Drug metabolism is a key step in the disposal of drugs, and the role of the gut as an important micro-ecosystem in the body is crucial in drug metabolism. The gut microbiota is capable of transforming and accumulating exogenous compounds (e.g., drugs) and modifying the activity and toxicity of these compounds, thereby influencing the host responses to the compounds. The interactions between gut microbiota and drugs are complex and need to be studied in detail. In recent years, the understanding of the metabolism of gut microbiota, gut microbiota-drug interactions, and the co-metabolism between gut microbiota and host are deepening, and increasing studies have shown that gut microorganisms play a crucial role in pharmacokinetics. By reviewing the relevant papers at home and abroad, we summarized the classification and functions of gut microorganisms, the effects of some commonly used drugs on gut microorganisms, and the metabolic effects and mechanisms of gut microbiota on drugs. In addition, we discussed the interactions between gut microbiota and drugs. The review helps to improve our understanding of the influences of gut microbiota on drug efficacy and the pathways and mechanisms of drug metabolism by gut microbiota, increase the possibility of modulating gut microbiota to improve treatment, and provide a reference for the rational and precise use of drugs, individualized treatment, and drug evaluation and development.