Among the reported complications of the antifibrinolytic therapy in the treatment of ruptured intracranial aneurysms, nausea and vomiting, cerebral arteriopathy and secondary hydrocephalus would be a matter of concern in its possible CNS involvement. However, little is known about the possibility of direct cerebral effect in synthetic antifibrinolytics. A simply designed animal experiment disclosed remarkable effects on electroencephalography, blood flow of the cerebral cortex and intracranial pressure. Such antifibrinolytics should not be given intrathecally in any situation even if the accumulation of the agents in cerebrospinal fluid is essential to prevent recurrent hemorrhage.