Stroke is a central nervous system disease that seriously affects the quality of life of the victims, with the second highest mortality among all the diseases in the world. At present, the main clinical treatment strategies for acute ischemic stroke are intravenous thrombolysis and mechanical thrombectomy, whereas these strategies do not protect patients from ischemia injury and functional disorder. Therefore, it is necessary to find neuroprotective methods to ameliorate ischemic injury and ischemic/reperfusion injury. This review summed up the current studies on the drugs which prevent and treat neurologic impairment after ischemic stroke, including ion channel blocker, antioxidant, anti-inflammatory agent, anti-apoptotic agent, analyzed the characteristics and advantages and disadvantages, and summarized several non-drug neuroprotective therapies.