Citicoline: A Novel Therapeutic Agent with Neuroprotective, Neuromodulatory, and Neuroregenerative Properties

Citicoline (cytidine diphosphocholine, CDP-choline) is a novel nutrient with a broad spectrum of benefits for conditions associated with symptoms of neurological dysfunction. An endogenous compound, citicoline is an essential intermediate in the synthesis of cell membrane phospholipids and its formation is the rate-limiting step in phosphatidylcholine synthesis. It plays several important roles in human physiology, including enhancement of structural integrity and signaling for cell membranes, support of acetylcholine synthesis, and synthesis of betaine, a methyl donor. Citicoline provides the brain with a source of choline and cytidine, which are efficiently used in the Kennedy cycle to generate phospholipids. It is able to attenuate the production of free radicals in ischemic conditions, while it also stimulates glutathione synthesis and the activity of glutathione reductase. Studies in animals and humans provide evidence of citicoline’s ability to promote learning and memory and improve cognitive impairment in Alzheimer’s and Parkinson’s disease, as well as in victims of mild to moderate stroke and cerebral ischemia. Citicoline administration may also reduce the duration of coma and the severity of mental and motor deficits associated with traumatic head injuries. Other areas in which benefits of citicoline are supported by the literature include: eye health, mental health, satiety, and substance abuse. Pharmacokinetic studies suggest that citicoline is well absorbed and highly bioavailable with oral dosing. Effective dosing of citicoline based on data from clinical trials ranges from 500 mg to 2,000 mg per day. Based on evidence from several trials and toxicological studies, citicoline is safe for use in pediatric and adult populations.