Intracranial hemorrhage results in poor neurologic outcomes and high mortality. Current management is limited to supportive care. In addition to the initial bleeding event, rebleeding and hematoma expansion have been identified as major risk factors for poor outcomes in these patients. The antifibrinolytic agents tranexamic acid, aminocaproic acid, and recombinant activated factor VII (rFVIIa) have been studied with the hopes of achieving early hemostasis and improving outcomes. Available data suggest that tranexamic acid and aminocaproic acid are more harmful than beneficial for this indication; therefore, they have no role in the treatment of intracranial bleeding. Alternatively, rFVIIa, has shown promising results in the management of spontaneous intracerebral hemorrhage. Clinicians should be aware of the available evidence regarding the use of these hemostatic agents in the management of intracranial hemorrhage, including traumatic brain injury, intracerebral hemorrhage, and subarachnoid hemorrhage.