Chemical Properties
White Solid
Usage
Naturally occurring nucleotide; intermediate in the major pathway of lecitin biosynthesis. Neuroprotective. It is used in the treatment of ischemic stroke and head trauma.
Uses
Cytidine 5′-diphosphate (CDP) is used as a substrate of CDP (nucleoside diphosphate) kinase (2.7.4.6) to produce CTP in support ofDNA and RNA biosynthesis and of ribonucleotide reductase to product dCMP.
Uses
Naturally occurring nucleotide; intermediate in the major pathway of lecitin biosynthesis. Neuroprotective. It is used in the treatment of ischemic stroke and head trauma.
Brand name
CerAxon (Interneuron).
General Description
Cytidine 5′-diphosphocholine (CDP-choline) contains cytidine and choline linked via a diphosphate bridge.
Biochem/physiol Actions
Cytidine 5′-diphosphocholine (CDP-choline) plays an important role in the synthesis of phosphatidylcholine. It is also involved in the biosynthesis of acetylcholine, a neurotransmitter. CDP-choline has therapeutic effects against hypoxia, cerebral ischemia and traumatic brain injury. It also exhibits therapeutic effects against learning and memory disorders, drug addiction and Alzheimer′s and Parkinson′s diseases.
Side effects
Citicoline sodium may be safe for 12 weeks of oral use, side effects may include stomach pain, back pain, blurred vision, constipation and headache. While Citicoline 2% Eye Drops may be safe for long-term use (up to 3 years). No serious side effects have been reported by clinical investigators in the treatment of Parkinson's disease.
Safety
There are two forms of citicoline: citicoline sodium and citicoline free-base. Citicoline sodium is the form that is approved as a prescription medication in some European countries and throughout Asia. Citicoline free-base is the form that is available as a dietary supplement and food/beverage ingredient in the United States. In Europe, citicoline is approved as a Novel Food ingredient and is authorized to be used in food supplements up to 500 mg per day. It is also authorized to be used for Food for Special Medical Purposes (FSMPs) in amounts of 250 mg/serving and up to 1,000 mg per day.
Citicoline free-base is produced in Japan by Kyowa Hakko Bio Co. Ltd. under the brand name of Cognizin. Cognizin is considered to be safe and received self-designated Generally Recognized As Safe (GRAS) status in 2009. In Europe, citicoline was approved as a Novel Food ingredient in 2014. Whereas most companies produce citicoline synthetically, Cognizin is produced using a patented, natural fermentation process. It is vegetarian and allergen-free. Kyowa Hakko manufactures and supplies Cognizin as a raw ingredient to many manufacturers around the world.
Metabolism
Citicoline can be administered orally, intramuscularly, or intravenously. Oral administration is most common because its bioavailability is approximately 92%. After oral ingestion, citicoline is hydrolyzed in the small intestine and liver into 2 major metabolites: cytidine and choline.
Cytidine and choline enter the systemic circulation, where cytidine is further metabolized into uridine. Both uridine and free choline cross the blood-brain barrier. In the central nervous system, uridine is converted to cytidine triphosphate, choline is converted to phosphocholine, and the 2 combine to resynthesize CDP-choline.
