Citicoline is an intermediate in membrane phospholipid synthesis that has been extensively assessed in acute stroke clinical trials demonstrating benefits.
18–21 Using diffusion-weighted MRI, Warach et al
21 demonstrated significant reduction in lesion volume growth and lesion volume from week 1 to week 12 in patients with acute ischemic stroke treated with citicoline within the first 24 hours after stroke onset. A marked association was found between lesion volume reduction and improvement of NIHSS score by
7 points.
Citicoline, also known as cytidine-5'-diphosphate-choline, isa naturally occurring endogenous nucleoside that functions asan intermediate in 3 major metabolic pathways:
22 (1) synthesisof phosphatidylcholine (lecithin), one of the major cell membranephospholipids with an important role in the formation of lipoproteins(citicoline formation is the rate-limiting step in the synthesisof phosphatidylcholine in neuronal membranes and microsomalphospholipids); (2) citicoline provides choline for acetylcholinesynthesis and could limit choline availability for membranesynthesis;
23 and (3) oxidation to betaine, a methyl donor. Themain components of citicoline, choline, and cytidine are readilyabsorbed in the gut and cross the blood–brain barrier.
24 As a dietary supplement, choline is grouped with the B vitamins;
24 a related product, choline alphoscerate, has been used lessfrequently.
25 In animal studies, citicoline is biologicallyactive, enhances repair of ischemic neuronal injury, and increaseslevels of acetylcholine and dopamine.
23 In aged animals, citicolineincreased dopamine release, improving learning and memory tasks
26 protecting against cognitive impairment in a rat model ofchronic cerebral hypoperfusion.
27 In an experimental strokemodel, Hurtado et al
28 showed that citicoline can produce re-growthof dendritic spines, which correlated with functional recovery.Using phosphorus magnetic resonance spectroscopy, Silveri etal
29 showed in elderly human subjects that citicoline treatmentfor 6 weeks produced significant increases in frontal lobe (anteriorcingulate cortex) phosphocreatine (+17%), β-nucleosidetriphosphates (largely ATP in the brain [+14%]), and in theratio of phosphocreatine to inorganic phosphate (+32%). Also,significant increase in membrane phospholipids was demonstrated.
Edited by chrono, 14 November 2011 - 10:21 PM.