Nalbuphine, a semi‑synthetic opioid receptor agonist‑antagonist, has the advantages of strong analgesic effect, definite efficacy, and mild adverse reactions, which shows bright prospects in clinical application in other countries. However, there are few reports on clinical application and scientific research in China. Therefore, this review introduces the pharmacological properties and mechanism of nalbuphine, and describes its clinical application including anesthesia induction, prophylactic analgesia, intraoperative and postoperative analgesia, treatment of postoperative complications, etc. It will provide safer and more reasonable guidance for using nalbuphine in clinical anesthesia.