Aim: Tranexamic acid (TXA) has been used to treat peripartum hemorrhage, while preoperative use of TXA in cesarean section (CS) remains controversial. To assess the effectiveness and safety of prophylactic application of TXA, a meta-analysis was performed. Methods: Electronic databases (MEDLINE [PubMed], Cochrane central register of controlled trials and Embase) were searched up to November 2018. The relevant data and quality of included trail were analyzed by RevMan 5.3. The study was registered at PROSPERO (CRD42018111165).Results: Twenty-one randomized controlled trials with a total of 3852 patients were included. Only one research reported thromboembolic events. Compared with control groups, the intra-operative blood loss (mean difference [MD] −155.23 mL, 95% confidence interval [CI] −195.64 − 114.81; P<0.01), postoperative blood loss (MD −26.67 mL, 95% CI −32.98 to −20.36; P<0.01), total blood loss (MD −184.88 mL, 95% CI −218.83 to −150.94; P<0.01), transfusion requirements (relative risk [RR] 0.29, 95% CI 0.18−0.49, P<0.01), massive hemorrhage (RR 0.39, 95% CI 0.30 to 0.51; P<0.01) and additional uterotonic agents use (RR 0.40, 95% CI 0.30−0.55, P<0.01) were markedly reduced in TXA-treated patients. Besides, TXA yielded a significant reduction in hemoglobin drop (MD −0.80 g/dL, 95% CI −1.07 to −0.53; P<0.01) and hematocrit drop (MD −2.05, 95% CI −3.09 to −1.01; P<0.01) compared with control groups. Conclusion: Prophylactic application of TXA can decrease perioperative blood loss and transfusion requirements in patients undergoing CS. More high-quality researches are needed to determine optimal dose of the drug.