In this Continuing Professional Development module, we review the practical pharmacology of tranexamic acid and its clinical use in trauma, obstetrics, and major orthopedic surgery. Tranexamic acid is a synthetic drug that inhibits fibrinolysis. Multiple clinical trials in various clinical settings have shown that it can reduce blood loss, transfusion rates, and bleeding-associated mortality. In trauma and obstetrical bleeding, early tranexamic acid administration (< three hours) may have greater clinical benefits. Overall, tranexamic acid use appears safe with no significant increase of thromboembolic or seizure events. Nevertheless, current evidence has limitations related to wide heterogeneity in dose, route, and timing of drug administration, as well as generalizability of the large-scale trial findings to higher income nations. Tranexamic acid is an efficacious and safe pharmacological-based blood conservation technique in the management of clinically significant hemorrhage. All anesthesiologists should have a good understanding of the pharmacotherapeutic properties and perioperative role of tranexamic acid therapy both inside and outside of the operating room. The use of tranexamic acid is likely to continue to rise with endorsement by various clinical guidelines and healthcare organizations. Further quantitative research is needed to evaluate optimal dosing and drug efficacy in these clinical scenarios.