Biological effects, pharmacokinetics and safety of citicoline

Citicoline, also known as cytidine diphosphocholine, is a mononucleotide composed of ribose, cytosine, pyrophosphate, and choline. Phospholipids in the human body mainly include phosphatidylcholine, phosphatidylethanolamine, phosphatidylinositol and sphingomyelin. As components of the cell membrane structure, they are necessary for the function of the cell membrane to maintain homeostasis, maintain membrane-associated enzyme activity, couple receptors and intracellular signals, and conduct nerve impulses.

Citicoline is a key substance in the biosynthesis of cell membrane structural phospholipids. Many years ago, it was discovered that citicoline has an excellent repairing effect on cell membranes. As phospholipid molecules are key components of all mammalian cell membranes, therapeutics targeting phospholipid conservation and regeneration represent a promising strategy in the field of clinical neurology.

In the central nervous system, 80% of phospholipid synthesis is regulated by changes in citicoline concentration, and citicoline formation is the rate-limiting step in the synthesis of phosphatidylcholine through the Kennedy cycle. Exogenous administration of citicoline can accelerate phospholipid synthesis, promote the rapid repair of damaged cell surface and mitochondrial membrane, maintain the integrity of cell membrane and cell energy metabolism.

Citicoline is a water-soluble compound with over 90% bioavailability. After exogenous citicoline enters the body, it is quickly decomposed into choline and cytidine, which cross the blood-brain barrier and re-synthesize citicoline in the central nervous system. In healthy volunteers, choline and cytidine levels peaked 30 minutes after injection, and their circulating concentrations continued to increase for 6 hours thereafter. Radiotracer studies have shown that oral citicoline can be rapidly and completely absorbed and hydrolyzed in the intestinal wall to choline and cytidine, which enter various biosynthetic pathways that use citicoline as a mediator, It has the same bioavailability and similar pharmacokinetic characteristics as intravenous citicoline.

A large number of animal experiments and clinical studies have shown that exogenous citicoline can promote the synthesis of cell membrane phospholipids, acetylcholine, catecholamine and other neurotransmitters, thereby effectively protecting and repairing damaged nerve cell membrane structure, restoring cell membrane function, and stabilizing neurotransmitter levels wait. Exogenous citicoline is widely distributed in the cortex, white matter and central gray matter nuclei, and its elimination is extremely slow, with a small amount excreted daily through urine, feces and respiratory routes.

Citicoline has very low toxicity. In preclinical studies, a lethal oral dose could not even be determined, as no animal deaths occurred at the maximum possible oral dose, and no toxic effects were observed in subacute and chronic toxicology experiments in rodents and dogs. A large-scale drug supervision study analyzed the safety of oral citicoline (500-4000 mg/d) in 4191 patients with acute ischemic stroke, only 31 patients were observed 37 adverse reactions, of which neurological System-related symptoms were the most common, followed by gastrointestinal symptoms. No patient discontinued the drug due to adverse reactions.

At present, citicoline has been widely used in the treatment of ischemic stroke, traumatic brain injury and cognitive impairment, and its therapeutic application in cerebral hemorrhage, Parkinson's disease and glaucoma has also received increasing attention.

Tag: Citicoline

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