Citicoline base powder

Citicoline Key Facts

Citicoline is a novel brain protector and enhancer compliant to EU regulations

An essential supplement for enhancing brain energy by increasing the levels of essential brain chemicals (neurotransmitters)

A vital cell membrane component that enhances structural integrity and signalling for cell membranes

A comprehensive therapeutic agent that promotes brain health, mental performance and overall cognitive health

Background

Citicoline, also known as CPD-Choline, is a nootropic and neuroprotective enhancing supplement for the brain. The molecular structure of citicoline and CPD-Choline is identical, the only difference being that CPD-Choline occurs naturally in humans, whereas Citicoline is an exogenous form.
Eugene Kennedy discovered citicoline as an intermediate in phosphatidylcholine synthesis in 1956. (Kennedy and Weiss,1956). In the intestine, it is easily hydrolysed into Choline and Cytidine, eventually forming phosphatidylcholine, and it also serves as a Choline donor in the biosynthesis of acetylcholine (Adibhatla & Hatcher, 2002). Acetylcholine is a neurotransmitter that is involved in cognitive and memory function.

Safety and Purity

In terms of safety, Choline is a substance with a low level of toxicological concern. Administering Choline with cytidine, in the form of Citicoline, lowers the toxicity index by twentyfold (Schauss & Nakazaki, 2020; D'Orlando & Sandage, 1995). Citicoline possesses a favourable safety profile, with only a few reports of adverse events, most of which are related to digestive disturbances, and it is a well-tolerated medication (Grieb, 2).
Citicoline, a unique source of choline for brain health, has received FDA GRAS approval in the United States and has been designated as a novel food ingredient (NFI) in the European Union (Grieb, 2015; EFSA NDA Panel, 2013).)

Chemistry

The Citicoline molecule contains a total of 57 atoms. There are 26 Hydrogen atoms, 14 Carbon atoms, 4 Nitrogen atoms, 11 Oxygen atoms and 2 Phosphorous atoms in this molecule. It is composed of the nitrogenous base cytosine ribose, pyrophosphate, and Choline (Secades & Frontera, 1995)

Citicoline

CAS Number - 987-78-0
Molecular Formula – C14H26N4O11P2
Molecular Weight – 488.32 g/mol
IUPAC - [[(2R,3S,4R,5R)-5-(4-amino-2-oxopyrimidin-1-yl)-3,4-dihydroxyoxolan-2-yl]methoxy-hydroxyphosphoryl] 2-(trimethylazaniumyl)ethyl phosphate

Health Benefits

Citicoline is an important nutrient for brain health and function. It has been extensively researched in clinical trials and has been shown to be beneficial in cerebral ischemia, traumatic brain injury, hypoxia, Alzheimer's and Parkinson's diseases, learning and memory disorders, alcoholism, drug addiction, amblyopia, and glaucoma (Adibhatla and Hatcher, 2005).

Memory performance

Citicoline has been extensively studied for its role in memory and cognitive function due to its role as an acetylcholine precursor and a building block of neuronal cell membrane. The IDEALE study, which found Citicoline to be effective and well tolerated in patients with mild vascular cognitive impairment, was one of the most recent clinical trials of Citicoline for memory (Cotroneo et al., 2013).

Healthy Vision

Several trials with Citicoline demonstrated positive effects on eye health, particularly in cases of amblyopia and glaucoma. Citicoline influences visual acuity improvements in amblyopic individuals by increasing the availability of several neurotransmitters and neuromodulators (Campos and Fresina, 2006).
Glaucoma is a neurodegenerative disease in which the pathology extends to retinal ganglion cells. The death of these cells is likely a result of apoptotic mechanisms. Citicoline consumption has an anti-apoptotic effect by increasing phosphatidylcholine synthesis and providing neuroprotection (Grieb and Rejdak, 2002)

Stroke and Cerebral Ischemia

Stroke is a leading cause of physical disability and a contributor to vascular cognitive impairment and vascular dementia, both of which can have a significant impact on a patient's quality of life. Several studies have found that patients who have had a stroke due to cerebrovascular ischemia benefit from taking Citicoline (Davalos et al., 2002). Citicoline was declared the first clinically effective neuroprotective agent in acute ischemic strokes in a 2006 editorial published in the Journal of Neurological Sciences (Overgaard and Meden, 2006).

Traumatic Head Injuries

Citicoline has been studied for several years for its potential use in the treatment of traumatic head injuries and concussions. Head injuries can cause a decrease in the production of cell membrane phospholipids, resulting in an accumulation of intracellular water, edema, and possible deterioration of the hematoencephalic barrier. Citicoline, as a precursor for the synthesis of neuronal membrane phospholipids, may have therapeutic benefits in these conditions (Schauss and Nakazaki, 2020).

References

1. Adibhatla, R. M., Hatcher, J. F., & Dempsey, R. J. (2002). Citicoline: neuroprotective mechanisms in cerebral ischemia. Journal of neurochemistry, 80(1), 12-23.
2. Adibhatla, R. M., & Hatcher, J. F. (2005). Cytidine 5′-diphosphoCholine (CPD-Choline) in stroke and other CNS disorders. Neurochemical research, 30(1), 15-23.
3. Baxter, M. G., & Crimins, J. L. (2018). AcetylCholine receptor stimulation for cognitive enhancement: better the devil you know?. Neuron, 98(6), 1064-1066.
4. Campos, E. C., & Fresina, M. (2006). Medical treatment of amblyopia: present state and perspectives. Strabismus, 14(2), 71-73.
5. Cotroneo, A. M., Castagna, A., Putignano, S., Lacava, R., Fantò, F., Monteleone, F., ... & Gareri, P. (2013). Effectiveness and safety of Citicoline in mild vascular cognitive impairment: the IDEALE study. Clinical Interventions in Aging, 8, 131.
6. Davalos, A., Castillo, J., Álvarez-Sabín, J., Secades, J. J., Mercadal, J., López, S., ... & Lozano, R. (2002). Oral Citicoline in acute ischemic stroke: an individual patient data pooling analysis of clinical trials. Stroke, 33(12), 2850-2857
7. D'Orlando, K. J., & Sandage Jr, B. W. (1995). Citicoline (CPD-Choline): mechanisms of action and effects in ischemic brain injury. Neurological research, 17(4), 281-284.
8. EFSA Panel on Dietetic Products, Nutrition and Allergies (NDA). (2013). Scientific Opinion on the safety of “Citicoline” as a Novel Food ingredient. EFSA Journal, 11(10), 3421.
9. Grieb, P. (2015). Citicoline: a food that may improve memory. Med. Sci. Rev, 2, 67-72.
10. Grieb, P. (2014). Neuroprotective properties of Citicoline: facts, doubts and unresolved issues. CNS drugs, 28(3), 185-193.
11. Grieb, P., & Rejdak, R. (2002). Pharmacodynamics of Citicoline relevant to the treatment of glaucoma. Journal of neuroscience research, 67(2), 143-148.
12. Kennedy, E. P., & Weiss, S. B. (1956). The function of cytidine coenzymes in the biosynthesis of phospholipides. Journal of Biological Chemistry, 222(1), 193-214
13. Overgaard, K., & Meden, P. (2006). Citicoline--the first effective neuroprotectant to be combined with thrombolysis in acute ischemic stroke?. Journal of the neurological sciences, 247(2), 119-120.
14. Schauss, A. G., & Nakazaki, E. (2020). Citicoline (CPD-Choline). In Textbook of Natural Medicine (pp. 515-525). Churchill Livingstone.
15. Secades, J. J., & Frontera, G. (1995). CPD-Choline: pharmacological and clinical review. Methods and findings in experimental and clinical pharmacology, 17, 1-54.