Tranexamic acid (TXA) is an antifibrinolytic agent which can reduce bleeding and blood transfusion rate through preventing thrombolysis. At present, it is commonly used in cardiological, orthopedic, obstetric and trauma surgeries, with less use in neurosurgery. This paper describes TXA's main administration methods, dosage and efficacy. In addition, the coagulation characteristics of adult intracranial tumors, intraspinal tumors, craniocerebral trauma and pediatric neurosurgery as well as the effectiveness of TXA were reviewed. However, the use of TXA may increase the risk of thromboembolism and epilepsy, which may be dose‑related. Currently, TXA's optimal administration regimen to balance its effectiveness and safety has not been fully understood and further studies are required.