Total knee arthroplasty (TKA) is a widely performed surgical procedure to restore function and relieve pain in patients with advanced knee arthritis. One of the key challenges in TKA is managing perioperative blood loss, which can lead to complications such as postoperative anemia and the need for blood transfusions. Tranexamic acid (TXA), an antifibrinolytic agent, has shown promising results in reducing blood loss and transfusion requirements in various surgical settings, including TKA. This comprehensive review synthesizes current evidence regarding the efficacy and safety profile of TXA in primary TKA. Mechanistically, TXA functions by inhibiting the breakdown of fibrin clots, promoting hemostasis, and minimizing blood loss. Clinical studies evaluating TXA in TKA have consistently demonstrated significant reductions in blood loss parameters, including total blood loss, postoperative drain output, and transfusion rates. Key findings highlight the efficacy of TXA across different dosing regimens and administration routes, with minimal associated risks of thromboembolic events or adverse effects. Comparative analyses with other blood conservation strategies underscore TXA's superiority in reducing transfusion requirements and its cost-effectiveness in clinical practice. The review also discusses current clinical guidelines and recommendations for TXA use in TKA, emphasizing optimal dosing strategies and patient selection criteria. Future research directions include exploring the long-term outcomes of TXA administration and its impact on functional recovery, and refining protocols to enhance its efficacy and safety further. In conclusion, TXA represents a valuable adjunct in blood loss management during primary TKA, offering substantial benefits in patient outcomes, healthcare resource utilization, and cost-effectiveness. Continued research efforts are warranted to optimize its use and expand its applicability in orthopedic surgery.