Citicoline

• Cytidine 5'- diphosphocholine
• Citicoline
• IUPAC: [( 2R, 3S, 4R, 5R ) -5 - (4- amino-2- oxopyrimidine -1-yl ) - 3,4- dihydroxyoxolan -2-yl ] methyl - [ oxido - [2 - ( trimethylazaniumyl ) ethoxy] phosphoryl ] phosphate

V06DX50

Dietetic food

• 27.14 g · kg -1 ( LD50, mouse, oral)
• 18.5 g · kg -1 ( LD50, rat, oral)

Template: Infobox chemical / molecular formula search available

CDP-choline is a nucleoside with the base cytosine, which is linked via a phosphate ester of choline. CDP -choline is water soluble and has a very good bioavailability ( > 90%).

Effect in the body

CDP-choline is an intermediate product of the cell membrane metabolism, as an essential element in the biosynthesis of cell membrane phospholipids ( phosphatidyl choline, and lecithin ) is required. CDP -choline is synthesized endogenously and represents the limiting step in phosphatidylcholine synthesis represents the major metabolic step for building and repair of cell membranes.

Pharmacokinetic studies in healthy adults showed that oral appliqued CDP-choline is absorbed very quickly and less than 1% is excreted enterally. Appliqué exogenous CDP-choline is hydrolyzed in the gut wall and the liver and absorbed as choline and cytidine. Choline and cytidine are then further metabolised, among other things happen the blood- brain barrier in order to be re-synthesized in the brain in the CDP - choline. Pharmacokinetic studies indicate that the excretion passes through the lungs and respiratory biphasic in the urine analogous to plasma availability.

Cytidine, an important component of nucleic acids ( DNA / RNA) is cytoplasmic converted to cytidine triphosphate (CTP ). In the CDP- choline metabolism Choline is phosphorylated by the enzyme choline kinase. In the following reaction, the product phosphorylcholine by the enzyme CTP - phosphocholine Cytidintransferase ( CCT) with CTP is implemented by the release of pyrophosphate to CDP- choline. In the last step, catalyzed by the enzyme choline phosphotransferase, CDP-choline diacylglycerol to react with phosphatidylcholine.

In animal experiments revealed after treatment with 500 mg / kg bw / day for 90 days, an increase in phosphatidylcholine levels by 25%, the phosphatidylethanolamine levels by 17%, and the phosphatidylserine levels by 42%. Choline and cytidine, the major metabolites of CDP -choline can be detected after a single oral administration of CDP- choline by significantly elevated plasma levels in young and elderly patients. By MR spectroscopic studies have shown that treatment with CDP -choline for weeks in the elderly can significantly increase the plasma levels of phosphodiesters, by-products of phospholipid metabolism in the brain. A CDP -choline treatment thus increasing the phospholipid synthesis and the turnover. CDP -choline has proven to be very safe toxicological tests showed no significant systemic cholinergic effects.

Areas of application

CDP- choline is a " food for special medical purposes " in Germany ( supplementary balanced diet; Trade name: Ceraxon ®).

Due to its mode of CDP-choline was taken early on with regenerative functions in traumatic and degenerative brain diseases in context. Exogenous CDP -choline was measured at more than 11,000 patients in clinical trials ( stroke, traumatic brain injury, dementia ). Especially good decrypts the effects of CDP- choline after a ( ischemic or hemorrhagic ) stroke are: Disclosed are anti- excitatory, anti - oxidative, membrane - stabilizing and regenerative effects. In clinical trials showed the first evidence of a reduction of the infarct volume and the neurological deficit after CDP -choline treatment in stroke patients. Thus resulted in a Pooled data analysis of the efficacy of CDP- choline in patients with acute ischemic stroke, that more than one in four treated with CDP -choline patient after three months, substantially complete recovery showed ( NIHSS value ≤ 1, Barthel Index ≥ 95 plus mRS of ≤ 1). Moreover, a Cochrane review of pooled data from all seven double-blind, placebo- controlled trials for ischemic stroke confirmed the efficacy of CDP- choline. The probability for the prevention of mortality / disability in long-term follow -up was significantly in favor of CDP- choline. Not least because this data CDP-choline is used for over 30 years worldwide for stroke treatment va in Europe, Latin America and Asia. After rigorous evidence-based criteria, however, there has not been an impact record from a multicenter phase III trial, which, however, in an international phase III trial ( ICTUS; citicholine International Stroke Trial in Acute ) is out of date.

As a further application areas are, inter alia, cognitive disorders of different genesis discussed, eg Dementia, Parkinson's disease, drug addiction, alcoholism, amblyopia and glaucoma, as well as protection of the endothelial cell membranes in complications such as infectious diseases or sepsis, cerebral malaria.

Trade names and dosage forms Ceraxon ® 500 mg, Trommsdorff GmbH & Co. KG Medicines