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Pharmacology: Citicoline, a naturally occurring endogenous nucleoside, is an intermediate compound in the major pathway for the biosynthesis of the structural phospholipids of cell membranes, including neurons.
Citicoline activates the biosynthesis of structural phospholipids in the neuronal membrane, increases cerebral metabolism and the level of various neurotransmitters, including acetylcholine and dopamine. Citicoline has shown neuroprotective effects in situations of hypoxia and ischemia, as well as improved learning and memory performance in animal models of brain aging. Furthermore, it has been demonstrated that citicoline restores the activity of mitochondrial ATPase and of membranal Na+/K+ ATPase, inhibits the activation of phospholipase A2 and accelerates the reabsorption of cerebral edema in various experimental models.
Pharmacodynamics: When administered orally, it is absorbed almost completely and its bioavailability is approximately the same when administered IV.
Once absorbed, cytidine and choline disperse widely throughout the body, cross the blood-brain barrier and reach the central nervous system (CNS), where they are incorporated into the phospholipid fraction of the cellular membrane and microsomes.
The concept that administration of exogenous citicoline can augment the synthesis of neural membrane phospholipid is attractive, because accelerated replacement or repair plays a critical role in maintaining the healthy function of numerous physiological processes. It has shown therapeutic efficacy in a variety of diseases in which membrane disorder, dysfunction or degeneration result in cellular and tissue ischemia and necrosis.
