As an amide local anesthetic, lidocaine is mainly used for antiarrhythmia and local anesthesia. In recent years, with the insight of pharmacological mechanism and spread clinical application, several studies have found that the intravenous infusion of lidocaine has a significant analgesic effect and plays a critical role in anti-inflammatory processes. At the same time, lidocaine can also impact immune regulation, anti-tumor response, myocardial protection, sensitization of anti-cancer drugs and so on, which have drawn increasing attention. In addition, certain effects in the treatment of tinnitus and hiccup has been shown by lidocaine. Moreover, the perioperative recommended intravenous lidocaine dose is in a relatively safe range. Hence, the current study aims provide a comprehensive summary of the research progress and clinical application of lidocaine.