Objective To evaluate the efficacy of antifibrinolytic agents in coronary artery bypass grafting (CABG) patients receiving antiplatelet. Methods We searched PubMed, EMbase, Highwire,CENTREN and its affiliated clinical trial registration data center, CBMdisc and CNKI databases from 2000 to 2010. Randomized controlled trials investigating the efficacy of anti-fibrinolytic agents (aprotinin and tranexamic acid) in CABG patients were identified. Study selection and meta-analysis were conducted according to the Cochrane Handbook for systematic reviews. Date were extracted from these trials by 2 reviewers independently and analyzed by RevMan 5.0 software. Result Eleven RCT trials ( n = 725 ) were included and data confirmed the efficacy of antifibrinolytic therapy in terms of reducing bleeding within 24 hours after operation(MD = - 306. 5 ml, 95% CI: - 351.52 to - 261.52, P ＜ 0. 01 ), number of patients who need blood transfusion ( OR = 0. 37, 95% CI: 0. 26 to 0. 51, P ＜ 0. 01 ), amount of blood transfusion ( MD = - 0. 59 U,95 % CI: - 0. 69 to - 0. 50, P ＜ 0. 01 ), surgical re-exploration ( OR = 0. 27,95 % CI: 0. 09 to 0. 78 ,P =0. 02), and thrombotic events( OR =0. 49,95% CI:0. 25 to 0. 97 ,P =0. 04) in CABG patients receiving antiplatelet, while compared with blank treatment. Conclusion This analysis showed that antifibrinolytic agents are effective for reducing bleeding within 24 hours after operation, amount of blood transfusion, surgical re-exploration and do not increase the incidence of thrombotic events in CABG patients receiving antiplatelet before operation.