Abstract: Admission hyperglycemia is an independent predictor, that contributes to hemorrhagic transformation (HT), and worsened functional outcome following reperfusion therapy with tissue plasminogen activator (tPA) in ischemic stroke. Clinical studies have revealed a strong association between hyperglycemia and incidence of HT independent of prior diabetes diagnosis (Alvarez-Sabín et al., 2003). Experimental studies showed that hyperglycemia reduces the efficacy of reperfusion and cerebral blood flow following ischemic stroke in rats (Kawai et al., 1997). Hyperglycemia accelerates the production of super oxides and advanced glycation end products, which contribute to blood brain barrier disruption (Won et al., 2011). Additionally, hyperglycemic reperfusion induces glucose overload to the ischemic brain, which accelerates the synthesis reactive oxygen free radicals and worsens neurovascular damage. The increased incidence of admission hyperglycemia in stroke patients along with HT, necessitates the development of novel adjunctive therapies for the management of ischemic stroke.