Tranexamic acid (Transamin^®) is one of the most widely used antifibrinolytic agents in excessive bleeding treatment. Common neurological side effects are headache and migraine; deep vein thrombosis and allergies are less, and adverse reaction of epilepsy could be less than 1%. This case is a 63-year-old man with renal dysfunction, leading cases of seizure after administration of tranexamic acid for bleeding during hospitalization. On the fourth day of using tranexamic acid, patient started to involuntary convulsions; the next day occurred epilepsy at noon. After suspending the medication delivery and administered antiepileptic drugs, patient’s situation has improved and then discharged on the sixth day, diagnosis with seizure, suspect drug induced. According to our literature review, using high dose of tranexamic acid without any dose adjustment according to renal function may possibly cause seizure adverse reaction. Besides, seizure has also been notified when combining two different medications with the same mechanism. Therefore, such case reminds clinical professionals to be aware of unusual twitching or other signs of epilepsy related to impaired renal function or drug-drug interaction when using tranexamic acid.