Citicoline is approved in Europe and Japan for use in stroke, head trauma and other neurological disorders. Exogenous administration of CDP-choline provides both choline and cytidine which access the brain and serve as substrates for the synthesis of phosphatidylcholine, a primary neuronal membrane component; the choline also enhances brain acetylcholine synthesis. Membrane repair and regeneration is necessary for recovery from stroke. Furthermore, citicoline may alleviate free fatty acid-induced toxicity which accompanies ischemic insult. Data from many pre-clinical and clinical trials support the hypothesis that citicoline may be a safe and effective treatment for stroke.
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Medically reviewed by Drugs. Last updated on Feb 14, There is mounting evidence for choline's place in therapy for stroke, brain and spinal cord injury, cognitive deficits, and glaucoma; however, results in clinical trials have been inconsistent. Oral dosages of to 2, mg daily have been evaluated in adolescents and adults in clinical trials. Lower doses mg twice daily have been used in short-term trials 6 weeks with combination therapy in patients with major depressive disorder. Information regarding safety and efficacy in pregnancy and lactation is lacking at dosages above those usually taken nutritionally.
Citicoline was well tolerated in clinical trials. Adverse effects may include GI disturbances, transient headaches, hypotension, tachycardia, bradycardia, and restlessness. Citicoline is found in all animal and plant cell membranes. It is available commercially in its free-base form or as a sodium salt. Citicoline is widely available internationally as a supplement, which was originally developed in Japan for the treatment of cerebrovascular disorders.
Use of citicoline has been extended to include treatment of chronic conditions, although further research is needed. Citicoline is a phospholipid composed of ribose, pyrophosphate, cytosine, and choline. It is water-soluble and highly bioavailable. Supplementation with citicoline increases choline stores available for other biosynthetic pathways. Citicoline appears to decrease glutamate levels in the brain and increase adenosine triphosphate, which in turn offers protection against ischemic neurotoxicity.
Increased glucose metabolism in the brain and cerebral blood flow has also been demonstrated, as well as increased availability of the neurotransmitters acetylcholine, norepinephrine, and dopamine. Studies have investigated a role for citicoline in substance addiction and among patients with bipolar disorder. Accelerated resynthesis of phospholipids and subsequent protection of cell membranes in the presence of citicoline have been suggested as a possible mechanism of action, based on animal studies.
Labeled phospholipid from radioactively labeled citicoline has been shown to cross the blood-brain barrier. Studies in rats with cognitive impairment have been conducted, and improved memory and learning have been demonstrated in older rats and those with induced memory deficits. Citicoline has also demonstrated enhanced learning ability in dogs. A Cochrane meta-analysis of clinical trials up to found some evidence of supplemental citicoline's positive effect on memory and behavior in the short- to medium-term versus placebo.
Trials included in the meta-analysis enrolled participants with mild to moderate dementia and Alzheimer disease, as well as those with cerebrovascular disorders.
Mini-Mental State Examination scores remained essentially unchanged over time for the treatment arm, while a decline was evident in the control patients. Improved cognitive outcomes were reported for the citicoline-treated group in attention, temporal orientation, and functional outcome measures. No significant differences were noted in adverse events between groups. Studies in animals suggest that citicoline stimulates dopamine in the retina.
Limited trials have been conducted. Antioxidant and anti-inflammatory mechanisms of citicoline have been evaluated in experimental studies in rats. A systematic review of the effect of cholinomimetic agents on head injury included trials using citicoline and case reports, all with some limitations in the methodology eg, small sample size, single blinding.
Changes in scores were predicted significantly more by a weight-adjusted dose with greater improvements in accuracy, detectability, and commission errors following higher weight-adjusted doses.
Positive findings have been reported in experiments using rats with induced cerebral insufficiency and models of hypoxia. Similarly, there were no significant differences for adverse events. No significant difference was found in mortality, outcome dependency, effectiveness, or safety between citicoline and controls. Citicoline is water-soluble and highly bioavailable, with very little drug excreted in the feces.
The effects of citicoline have been studied in rats during pregnancy for a potential role in the protection of dendrites in the cortex and fetal lung development, as well as in pregnant women in their third trimesters. However, information is limited on the safety of supplemental citicoline. Citicoline may exacerbate adrenocorticotropic hormone— or cortisol hypersecretion—related disorders, including type 2 diabetes and major depressive disorder.
Studies in humans are limited. In dogs given oral citicoline 1. This information relates to an herbal, vitamin, mineral or other dietary supplement. This product has not been reviewed by the FDA to determine whether it is safe or effective and is not subject to the quality standards and safety information collection standards that are applicable to most prescription drugs.
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The invention belongs to field of medicine preparing technology, it particularly relates to arrive a kind of Citicoline sodium injection and its system Preparation Method. Citicoline sodium injection main component is C14H25N4NaO11P2, is changed Scientific name is referred to as the mono-sodium salt of choline cytidine diphosphate ester. C14H25N4NaO11P2 is nucleoside derivates, because it can reduce brain blood Pipe resistance, increases brain blood flow and promotes metabolism of brain, improves Brain circlulation, clinically for treating Acute Brain Injury and brain hand The postoperative disturbance of consciousness for causing. C14H25N4NaO11P2 is the derivative of karyon thuja acid, is necessary coenzyme in lecithin synthesis, there is increasing Reticular formation of brain stem function relevant with consciousness by force, excitation is played to pyramidal tract, promotes damaged cell to be recovered, moreover it is possible to Strengthen cerebrovascular tension force, and enhancing cerebral blood flow CBF , strengthen the function of cell membrane, improve brain metabolism. In being clinically mainly used in Function and the disturbance of consciousness that pivot nervous system acute injury causes.
Neurological impairment is among the leading causes of disability-adjusted life years DALY , an indicator of the overall disease burden expressed as the number of years lost due to ill health, disability or early death. Major causes of neurological impairment include traumatic brain injury TBI ,dementia and stroke. A published data mentions that 7 people acquire a neurologic disability every minute, amounting to nearly 11, every day. Damage to cell membrane integrity is an important mediator of neuronal death in a variety of neurologic diseases because the phospholipid molecules are essential constituents of cell membranes in all mammals.
Citicoline (CDP-choline): Mechanisms of Action and Effects in Ischemic Brain Injury
Following injection or ingestion, citicoline is believed to undergo quick hydrolysis and dephosphorylation to yield cytidine and choline, which then enter the brain separately and are used to resynthesize CDP-choline inside brain cells. Neuroprotective activity of citicoline has been repeatedly shown in preclinical models of brain ischaemia and trauma, but two recent, large, pivotal clinical trials have revealed no benefits in ischaemic stroke and traumatic brain injury. However, the substance seems to be beneficial in some slowly advancing neurodegenerative disorders such as glaucoma and mild vascular cognitive impairment. It is concluded that at present, there is no adequate description of the mechanism s of the pharmacological actions of this substance. The possibility should be considered and tested that, in spite of apparently fast catabolism, the intact citicoline molecule or the phosphorylated intermediate products of its hydrolysis, cytidine monophosphate and phosphocholine, are pharmacologically active. The work of Kennedy and collaborators in the s showed that this phosphorylated choline nucleotide is a precursor of glycerophospholipid phosphatidylcholine PC [ 1 ]. PC and its twin compound phosphatidylethanolamine PEt are the two most abundant phospholipids in eukaryotic cells, accounting for more than half of the total phospholipid content in membranes.
Neuroprotective Properties of Citicoline: Facts, Doubts and Unresolved Issues
Citicoline INN , also known as cytidine diphosphate-choline CDP-Choline or cytidine 5'-diphosphocholine is an intermediate in the generation of phosphatidylcholine from choline , a common biochemical process in cell membranes. Citicoline is naturally occurring in the cells of human and animal tissue, in particular the organs. Studies suggest that CDP-choline supplements increase dopamine receptor densities. Citicoline is available as a supplement online and in stores.