Tranexamic acid (TXA) is a synthetic derivative of the amino acid lysine that inhibits fibrinolysis by blocking the interaction of plasminogen with the lysine residues of fibrin. Historically, TXA is commonly used for reduction of blood loss in perioperative situations, while recently it has attracted attention for clinical use in the trauma field. In 2010, the Clinical Randomization of an Antifibrinolytic in Significant Hemorrhage 2 (CRASH-2) trial demonstrated that intravenous administration of TXA improved mortality significantly in trauma patients with significant bleeding. After the launch of its sensational results, the main stream treatment protocol in trauma changed worldwide to include TXA administration. In this review, first we summarize the recent evidence or recommendations in the related guidelines concerning TXA. Also, we next tried to explore in detail not only the benefits but also the harm introduced by TXA in trauma patients, because the main adverse event results for TXA, such as vascular occlusive events in the CRASH-2 trial, are still being discussed in several papers. Thus, we briefly summarized the evidence for the safety of TXA administration by a systematic review method using observational studies. Consequently, the pooled relative risk for venous thromboembolisms was 1.61 (95% CI, 0.86–3.01), indicating a non-significant increase in the venous thromboembolism risk of TXA therapy. Regarding the basic mechanism, TXA potentially possesses the risk of venous thromboembolisms, so it should be used cautiously and selectively. Further investigation is needed to delineate the optimal targeted trauma patients to earn the maximum survival benefits with minimized risk of thrombotic complications.