A 66-year-old man was admitted with acute left heart failure and hyponatremia. On the first day of admission, 15 mg tolvaptan tablets were given orally. On the second day of admission, alanine transaminase and aspartate transaminase were significantly increased to 916.76 U·L^-1 and 1 857.1 U·L^-1, respectively, which met the diagnostic criteria of severe acute liver injury. The drug was immediately stopped and hepatoprotective therapy was given, and on the 10th day of admission, the patient's liver function improved significantly, and on the 12th day of admission, the patient was discharged after his condition stabilised. The results of the correlation evaluation indicated that the development of acute liver injury in this patient is likely related to tolvaptan. This article discusses the mechanism, time of occurrence, population and treatment of tolvaptan-induced liver function injury, suggesting that clinical use of tolvaptan should be highly vigilant for acute liver function injury and routine monitoring of patients' liver function to ensure the safe use of the drug.

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