Acute kidney injury (AKI) is a common and severe complication of cardiac surgery, and related rates of both hospitalization and long-term mortality are increasing. A number of studies have explored the preventive effects of perioperative pharmacological therapy on AKI after cardiac surgery. However, the mechanisms of AKI are multifaceted, and no universal treatment has been confirmed as beneficial. We review and analyze several current perioperative pharmacological therapies for AKI after cardiac surgery to identify promising preventive strategies.