Citicoline is an essential intermediate in the synthesis of structural phospholipids of cell membranes. Exogenously administered citicoline can promote rapid repair of injured neuronal membrane by increasing the synthesis of phospholipids, stabilize neurotransmitter system by increasing the synthesis of acetylcholine and dopamine, and attenuate free fatty acids mediated additional tissue injury by decreasing free fatty acids accumulation in the ischemic cerebral tissue. The wide therapeutic time window, high bioavailability, good blood-brain barrier penetration, and excellent safety make citicoline an effective agent for neuroprotection and neurorepair. Available evidence showed that citicoline can improve significantly neurological function in patients with acute and subacute ischemic stroke. Moreover, animal and clinical studies indicated that citicoline has a potential to improve outcomes of traumatic brain injury, cognitive impairment, intracerebral hemorrhage, Parkinson disease and glaucoma. Citicoline in combination with tbrombolytic agents or other neuroprotective agents should become one of the future research directions. The bioavailability and pharmacokinetics of oral citicoline are similar to those of intravenous citicoline, and oral constitutes a main route of administration for citicoline.