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Citicoline is a nutritional supplement and source of choline and cytidine with potential neuroprotective and nootropic activity. Citicoline, also known as cytidine-5-phosphocholine or CDP-choline, is hydrolyzed into cytidine and choline in the intestine. Following absorption, both cytidine and choline are dispersed, utilized in various biosynthesis pathways, and cross the blood-brain barrier for resynthesis into citicoline in the brain, which is the rate-limiting product in synthesizing phosphatidylcholine. This agent also increases acetylcholine (Ach), norepinephrine (NE), and dopamine levels in the central nervous system (CNS). In addition, citicoline is involved in preserving sphingomyelin and cardiolipin and restoring Na+/K+-ATPase activity. Citicoline also increases glutathione synthesis and glutathione reductase activity and exerts antiapoptotic effects.
Citicoline is a donor of choline in the biosynthesis of choline-containing phosphoglycerides. It has been investigated for the treatment, supportive care, and diagnosis of Mania, Stroke, Hypomania, Cocaine Abuse, and Bipolar Disorder, among others.
CDP-choline is a member of the phosphocholines class, the chlorine ester of CDP. It is an intermediate obtained in the biosynthetic pathway of structural phospholipids in cell membranes. It is a human metabolite, a psychotropic drug, a neuroprotective agent, a Saccharomyces cerevisiae metabolite, and a mouse metabolite. It is a member of phosphocholines and a member of nucleotide-(amino alcohol)s. It derives from a CDP. It is a conjugate base of a CDP-choline(1+).
A nutritional supplement and source of choline and cytidine with potential neuroprotective and nootropic activity.
Mechanism of action
Citicoline is a phospholipid composed of ribose, pyrophosphate, cytosine, and choline. It is water-soluble and highly bioavailable.3 Citicoline is produced endogenously as an intermediate in the production of phosphatidylcholine from choline and is then hydrolyzed in the small intestine to make choline and cytidine available for further biosynthesis.[rx]
Citicoline, also known as cytidine-5-diphosphocholine or CDP-choline, is hydrolyzed into cytidine and choline in the intestine. Following absorption, both cytidine and choline are dispersed, utilized in various biosynthesis pathways, and cross the blood-brain barrier for resynthesis into citicoline in the brain, which is the rate-limiting product in synthesizing phosphatidylcholine. This agent also increases acetylcholine (Ach), norepinephrine (NE) and dopamine levels in the central nervous system (CNS). In addition, citicoline is involved in the preservation of sphingomyelin and cardiolipin and the restoration of Na+/K+-ATPase activity. Citicoline also increases glutathione synthesis and glutathione reductase activity, and exerts antiapoptotic effects.
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.[rx, rx]
Indications
- Drugs are specifically used to facilitate learning or memory, mainly to prevent the cognitive deficits associated with dementias. These drugs act by a variety of mechanisms.
- Citicoline is a donor of choline in the biosynthesis of choline-containing phosphoglycerides. It has been investigated for the treatment, supportive care, and diagnosis of Mania, Stroke, Hypomania, Cocaine Abuse, and Bipolar Disorder, among others.
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- Acute ischemic stroke
Acute ischemic stroke occurs due to blockage of a blood vessel by a clot causing limited blood flow to your brain. If the injectable form of Citicoline is given within 12 hours of having a stroke and then daily for seven days after having a stroke, it can help in a speedy recovery.
- Alzheimer’s disease
Alzheimer’s disease is a condition that occurs due to the destruction of brain cells. It may lead to loss of memory ability to think, communicate or handle daily activities. Citicoline protects your brain cells from damage and also repairs the damaged cells. Therefore, Citicoline is used to improve your brain function in such conditions.
- Cerebral insufficiency
Cerebral insufficiency is a lack of proper blood flow to your brain due to brain injury or blood clots. It can result in memory loss, poor concentration, and lack of orientation. Citicoline is used to prevent further decline in your brain functions.
- Parkinsonism
Parkinson’s disease is a brain disorder that affects movement. It causes muscle weakness, leading to stiffness and shakiness in your hands and legs. It slows down the voluntary indication of your body like sitting, standing, and walking. Citicoline is used with other medicines to improve your condition.
- Acute ischemic stroke
Contraindication
- Data not available
Dosing
- Citicoline is available as an oral form to be taken by mouth and as an injection to be administered into the vein or muscle. Take Citicoline oral forms with or without food. The dose and duration depend on the severity of your health condition.
- Citicoline is water-soluble and highly bioavailable, with minimal drug excreted in the feces.[rx] Citicoline exhibits biphasic plasma peak concentrations at 1 and 24 hours and biphasic elimination.[rx]
- In clinical trials, oral dosages of 250 to 2,000 mg daily have been evaluated in adolescents and adults. Citicoline 100 mg every 12 hours was used in combination with citalopram (20 mg/day for seven days, then 40 mg/day) for six weeks in patients with major depressive disorder.[rx]
Side Effects
The Most common
- Citicoline may cause side effects like stomach discomfort, restlessness, diarrhea, and pain in the head or upper neck. সহজ বাংলা: মাথাব্যথা।" data-rx-term="headache" data-rx-definition="Headache means pain in the head or upper neck. সহজ বাংলা: মাথাব্যথা।">headache. However, these side effects may subside as your body adjusts to the medicine.
- pain in the head or upper neck. সহজ বাংলা: মাথাব্যথা।" data-rx-term="headache" data-rx-definition="Headache means pain in the head or upper neck. সহজ বাংলা: মাথাব্যথা।">Headache
- Dizziness
- Shaking of hands or feet
- Sleeplessness
Common
- Irregular heartbeat
- Low blood pressure
- Diarrhoea
- Nausea
- Stomach pain
- Injection site pain
- Blurred vision
Drug Interaction
- Citicoline was well tolerated in clinical trials. Adverse effects may include GI disturbances, transient headaches, hypotension, tachycardia, bradycardia, and restlessness.[rx]
- Citicoline may exacerbate adrenocorticotropic hormone– or cortisol hypersecretion–related disorders, including type 2 insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।" data-rx-term="diabetes" data-rx-definition="Diabetes is a condition where blood sugar stays too high because insulin is low or not working well. সহজ বাংলা: রক্তে চিনি বেশি থাকার রোগ।">diabetes and major depressive disorder.[rx]
Pregnancy and Lactation
FDA Pregnancy Category : D
- Information regarding safety and efficacy in pregnancy and lactation is lacking at dosages above those usually taken nutritionally. 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.[rx, rx]
References
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LICENSECreative Common’s Attribution-NonCommercial 4.0 International License (http://creativecommons.org/licenses/by-nc/4.0/legalcode)Citicoline
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LICENSEUse of the information, documents and data from the ECHA website is subject to the terms and conditions of this Legal Notice, and subject to other binding limitations provided for under applicable law, the information, documents and data made available on the ECHA website may be reproduced, distributed and/or used, totally or in part, for non-commercial purposes provided that ECHA is acknowledged as the source: “Source: European Chemicals Agency, http://echa.europa.eu/”. Such acknowledgement must be included in each copy of the material. ECHA permits and encourages organisations and individuals to create links to the ECHA website under the following cumulative conditions: Links can only be made to webpages that provide a link to the Legal Notice page.
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LICENSEHMDB is offered to the public as a freely available resource. Use and re-distribution of the data, in whole or in part, for commercial purposes requires explicit permission of the authors and explicit acknowledgment of the source material (HMDB) and the original publication (see the HMDB citing page). We ask that users who download significant portions of the database cite the HMDB paper in any resulting publications.CiticolineHMDB0001413_msms_1565
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Cytidine 5′-diphosphocholineCCSbase Classification
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LICENSEUnless otherwise indicated, all text within NCI products is free of copyright and may be reused without our permission. Credit the National Cancer Institute as the source.NCI Thesaurus Tree
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LICENSEThe ClinicalTrials.gov data carry an international copyright outside the United States and its Territories or Possessions. Some ClinicalTrials.gov data may be subject to the copyright of third parties; you should consult these entities for any additional terms of use.
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LICENSEIt is to be used only for research and educational purposes. Any reproduction or use for commercial purpose is prohibited without the prior express written permission of NC State University.
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Cytidine 5′-diphosphocholine
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LICENSEUnless otherwise noted, the contents of the FDA website (www.fda.gov), both text and graphics, are not copyrighted. They are in the public domain and may be republished, reprinted and otherwise used freely by anyone without the need to obtain permission from FDA. Credit to the U.S. Food and Drug Administration as the source is appreciated but not required.
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PubChem
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LICENSEData files in the PDB archive (ftp://ftp.wwpdb.org) are free of all copyright restrictions and made fully and freely available for non-commercial and commercial use. Users of the data should attribute the original authors of that structural data.
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LICENSEUse of all or parts of the material requires reference to the WHO Collaborating Centre for Drug Statistics Methodology. Copying and distribution for commercial purposes is not allowed. Changing or manipulating the material is not allowed.ATC Code
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Citicoline
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LICENSEWorks produced by the U.S. government are not subject to copyright protection in the United States. Any such works found on National Library of Medicine (NLM) Web sites may be freely used or reproduced without permission in the U.S.Cytidine Diphosphate CholineNootropic Agents
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LICENSEAcademic users may freely use the KEGG website. Non-academic use of KEGG generally requires a commercial licenseTherapeutic category of drugs in JapanAnatomical Therapeutic Chemical (ATC) classificationDrugs listed in the Japanese Pharmacopoeia
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GHS Classification Tree
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LICENSEThe code for LOTUS is released under the GNU General Public License v3.0.LOTUS Tree
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SID 388408040
