Background　Remifentanil is a ultra-short-acting μ-opioid receptor agonist. Because remifentanil possesses high efficacy, rapid onset, short half-life time and fast clearance, it has been widely used for anesthesia. However, the incidence of remifentanil-induced hyperalgesia (RIH) remains relatively high, which poses great challenges to postoperative management.　Objective　To explore the effective intervention strategy for the prevention of RIH.　Content　Like other opioid drugs, remifentanil, after repetitive and long-term administration, causes drug tolerance and pain hypersensitivity. RIH may follow central sensitization of both ascending and descending pathways to facilitate pain transduction. A large amount of clinical trials tried to prevent RIH using various medications, such as, agonists for α2-drenoreceptor, opioid drugs, antagonists for NMDA receptors, non-steroid anti-inflammatory drugs, and calcium channel blockers, etc.　Trend　Further studies in the field are required to advance the understanding of the development of RIH, which may result in better strategies to prevent and treat this condition.