Furancoumarins is a kind of secondary metabolites mainly found in four higher plants: Rutaceae， Moraceae， Fabaceae and Apiaceae， especially in citrus fruits. Furancoumarins has good biological activity， but recent studies found that citrus fruits can interact with drugs， esulting in a potential risk of toxicity. Furocoumarins can inhibit cytochrome CYP3A4-mediated drug oxidative metabolism， improve oral bioavailability of drugs， and lead to the increase of blood drug concentration， thereby enhancing the drug efficacy or increasing adverse reactions. Its action targets are mainly cytochrome P450 and P-glycoprotein. This review introduced the distribution and bioactive activities of furancoumarins in citrus fruits， outlined the advances interactions between furancoumarins in citrus and drugs， and the methods to reduce its content at home and abroad， provided a theoretical reference for the reasonable consumption of citrus fruits and the safety of medication.