Patients who undergo major spinal surgery often require multiple blood transfusions. The antifibrinolytics are medications that can reduce blood-transfusion requirements in cardiac surgery and total knee arthroplasty. The present role of synthetic antifibrinolytics, especially tranexamic acid, in reducing peri-operative blood-transfusion requirements in spine surgery is still unclear. The majority of studies exploring the role of these drugs in spine surgery have limited patient enrollment and report mixed results. The goal of the present review is to discuss the pharmacology of tranexamic acid briefly. A brief synopsis of the studies using the synthetic antifibrinolytics for spine surgery is presented. Finally, the potential risks and the benefits of antifibrinolytics are discussed.