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.
Highlights
Citicoline is the international nonproprietary name (INN) for cytidine-diphosphocholine (CDP-Cho)
In 2009 in the USA, citicoline was self-affirmed by the Japanese company Kyowa-Hakko as GRAS [2], and in 2014 it was announced as a novel food ingredient by the appropriate Implementing
Looking through the positive European Food Safety Agency (EFSA) Scientific Opinion on citicoline issued prior to the aforementioned implementing decision [6], we find the reference to the observation that, both in humans and in rats, upon ingestion citicoline undergoes quick hydrolysis, breaking down to choline and cytidine [7], which undergo further metabolism and incorporation into normal pathways of metabolism [8]
Summary
Citicoline is the international nonproprietary name (INN) for cytidine-diphosphocholine (CDP-Cho). Citicoline sodium salt, classified as a nootropic and psychostimulant [1], is an active principle of a variety of prescription drugs, either injectables or oral formulations. In 2009 in the USA, citicoline (inner salt) was self-affirmed by the Japanese company Kyowa-Hakko as GRAS (generally regarded as safe) [2], and in 2014 it was announced as a novel food ingredient by the appropriate Implementing. The aforementioned EU Implementing Decision states that citicoline may be placed on the EU market, where it is intended to be used in food supplements aimed at a target population of middle-aged to elderly adults at a maximum level of 500 mg/day, and in dietary foods for special medical purposes with a maximum dose of 250 mg per serving and with a maximum daily consumption level of 1000 mg from these types of foods
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