Introduction: Tranexamic acid (TXA) is an antifibrinolytic agent widely used in surgery to decrease bleeding and reduce the need for blood product transfusion. The role of TXA in urology is not well summarized. We conducted a systematic review of studies reporting outcomes of TXA use in urological surgery. Methods: A comprehensive search was conducted from the following databases: PubMed, Embase, Cochrane Library, and Web of Science. Two reviewers performed title and abstract screening, full text review, and data collection. Primary outcomes included estimated blood loss (EBL), decrease in hemoglobin, decrease in hematocrit, and blood transfusion rates. Secondary outcomes included TXA administration characteristics, length of stay, operative time, and postoperative thromboembolic events. Results: A total of 26 studies consisting of 3201 patients were included in the final analysis. These included 11 studies on percutaneous nephrolithotomy, 10 on transurethral resection of the prostate, three on prostatectomy, and one on cystectomy. Estimated blood loss (EBL), transfusion rate, hemoglobin drop, operative time, and length of stay were significantly improved with TXA administration. In addition, the use of TXA was not associated with an increased risk of venous thromboembolism (VTE). The route, dosage, and timing of TXA administration varied considerably between included studies. Conclusions: TXA use may improve blood loss, transfusion rates, and perioperative parameters in urological procedures. In addition, there is no increased risk of VTE associated with TXA use in urological surgery; however, there is still a need to determine the most effective TXA administration route and dose. This review provides evidence-based data for decision-making in urological surgery.