Citicoline: A Superior Form of Choline?

Abstract

Medicines containing citicoline (cytidine-diphosphocholine) as an active principle have been marketed since the 1970s as nootropic and psychostimulant drugs available on prescription. Recently, the inner salt variant of this substance was pronounced a food ingredient in the major world markets. However, in the EU no nutrition or health claim has been authorized for use in commercial communications concerning its properties. Citicoline is considered a dietetic source of choline and cytidine. Cytidine does not have any health claim authorized either, but there are claims authorized for choline, concerning its contribution to normal lipid metabolism, maintenance of normal liver function, and normal homocysteine metabolism. The applicability of these claims to citicoline is discussed, leading to the conclusion that the issue is not a trivial one. Intriguing data, showing that on a molar mass basis citicoline is significantly less toxic than choline, are also analyzed. It is hypothesized that, compared to choline moiety in other dietary sources such as phosphatidylcholine, choline in citicoline is less prone to conversion to trimethylamine (TMA) and its putative atherogenic N-oxide (TMAO). Epidemiological studies have suggested that choline supplementation may improve cognitive performance, and for this application citicoline may be safer and more efficacious.

Application of Citicoline in Neurological Disorders: A Systematic Review

“…Choline, one of the breakdown products of citicoline, serves as a substrate for the synthesis of acetylcholine. This neurotransmitter also has a neuroprotective effect [ 10 , 11 ]. Citicoline raises the level of serotonin, which is also supposed to promote neuroprotective effects [ 12 ].…”

Spatial Metabolomics of the Human Kidney using MALDI Trapped Ion Mobility Imaging Mass Spectrometry

“…For example, choline and sapropterin both localize to the medulla and renal pelvis ( Figure 2B&F), while acetylcarnitine is most abundant within the medulla ( Figure 2D) and arginic acid is mostly detected within the cortex ( molecules is displayed here, further examples of metabolites that localize to specific regions of the kidney can be found within the dataset. The function of many of these metabolites is well understood, such as lipid metabolism (choline), 61 fatty acid transport (acetylcarnitine) 62 and disordered urea metabolism (arginic acid). 63 One of the most difficult challenges in spatial metabolomics is the unequivocal structural identification of a molecule.…”

Citicoline: A Candidate for Adjunct Treatment of Multiple Sclerosis

“…Citicoline was recently pronounced a food ingredient in major world markets [ 58 ], and there is no known contraindication of its intake. When, in the treatment of patients suffering from Alzheimer’s disease, oral intake of this ingredient was added to the treatment with anticholinesterase inhibitors, positive clinical effects in the domains of cognition, mood, and behavioral symptoms were reported [ 59 ].…”