Tranexamic acid (TXA) has emerged as a cornerstone in blood conservation strategies for cardiac surgery. This comprehensive review synthesizes current evidence on TXA’s efficacy, safety, and optimal use in various cardiac surgical procedures. We examine the pharmacological properties of TXA, its historical development as an antifibrinolytic agent, and its evolution in cardiac surgical practice. The review critically evaluates key clinical trials and meta-analyses demonstrating TXA’s efficacy in reducing blood loss and transfusion requirements across a spectrum of cardiac surgeries, including coronary artery bypass grafting, valve procedures, and aortic surgery. Special consideration is given to its use in pediatric cardiac surgery. We address ongoing debates surrounding optimal dosing strategies, timing of administration, and integration with other hemostatic interventions. The safety profile of TXA is thoroughly examined, with particular focus on the risk of seizures and thromboembolic events. The review also explores practical aspects of TXA implementation in clinical practice, including its role in comprehensive blood management protocols and potential cost-effectiveness. Emerging research areas, such as pharmacokinetic-guided dosing and topical TXA application, are discussed. Finally, we outline future directions and research priorities, including the need for long-term outcome studies and refinement of patient-specific protocols. This review provides a balanced assessment of TXA’s role in modern cardiac surgery, offering clinicians and researchers a comprehensive resource for optimizing its use to improve patient outcomes while minimizing potential risks.