Citicoline (INN), also known as cytidine diphosphate-choline (CDP-Choline) or cytidine 5′-diphosphocholine is a psychostimulant/no tropic. It is an intermediate in the generation of phosphatidylcholine from choline.
- Absorption: – Citicoline is well absorbed after oral administration, has an absolute bioavailability of approximately 99%.
- Metabolism: – Citicoline is metabolized in the liver to free choline. The liver is capable of synthesizing lecithin from choline, and resynthesizing citicoline from cytidine and choline.
- Distribution: – Plasma choline levels are elevated significantly after oral administration. Two peaks of plasma citicoline equivalents have been reported after oral doses of radio labeled citicoline (300mg). An initial peak is observed in approximately 1 hour (1.5 mcg.mL), presumably related to mixture of unchanged citicoline and its metabolites (choline and cytidine diphosphate).The major portion of a dose of citicoline appears to be incorporated into tissues and/or used in biosynthetic/ biodegradation pathways. Including lecithin/lipid membrane synthesis.
- Elimination: – Small amounts of a dose are recovered in urine (2% to 3%) and in feces (less than 1%). Approximately 12% of a dose is eliminated as respiratory carbon dioxide.
- Half-Life: – Elimination half life of citicoline is 3.5 hours (first peak concentration), 125 hours (second peak concentration).
- It is use for the treatment of patients with serious cerebrai injuries of vascular or traumatic nature with or without loss of consciousness.
- It is also indicated for treatment of degenerative damages and chronic cerebral vascular injuries in senile dementia.