DEXMEDETOMIDINE IS A new intravenous drug gaining popularity in neuroanesthesia and neurocritical care practice. This α2-adrenergic receptor agonist offers a unique “cooperative sedation,” anxiolysis, and analgesia with no respiratory depression. Cerebral effects are generally consistent with a desirable neurophysiological profile, including neuroprotective characteristics. In addition, sympatholytic and antinociceptive properties allow for hemodynamic stability at critical moments of neurosurgical stimulation. This review will address the neuropharmacology and neurophysiology of α2-adrenergic agonists and will specifically consider the rapidly evolving applicability of dexmedetomidine as an adjuvant to neurosurgical case management.