Accurate Education - Citicoline

Accurate Education &#; Citicoline

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Citicoline

Citicoline is a brain nutrient that supports mental energy, focus, attention, and overall cognitive health. It is sometimes referred to as choline or coline (see below).

See also:

CAM Alternatives for Cognitive Impairment:

   Acetyl-L-carnitine (ALC)

   Alpha-Lipoic Acid

Bacopa

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Citicoline (CDP-choline)

Citicoline and CDP-choline have the same molecular structure. CDP-choline refers to the endogenous form that is present in every cell of the human body. Citicoline refers to the form that is taken exogenously. Citicoline is available in 2 forms: (1) citicoline sodium which is a prescription medication used to treat neurological disorders in numerous countries and (2) citicoline free-base which is a dietary supplement in the United States.

The biomolecule Citicoline (CDP-choline or cytidine-5 ́-diphosphocholine) is an essential precursor for the neurotransmitter acetylcholine in the central nervous system and also for the synthesis of membrane phospholipids. Phospholipids create the structural integrity of all cell membranes and are essential to cellular growth and repair. In the brain, phospholipids are also essential for the synaptic function of communication among all brain cells. The primary phospholipid in the brain&#;phosphatidylcholine&#;makes up 30% of the gray matter.

Despite the importance of CDP-choline in phospholipid synthesis, however, the brain preferentially uses CDP-choline for production of acetylcholine. If availability of CDP-choline is low, phospholipids are stolen from neuronal membranes for acetylcholine production and phospholipid synthesis slows down, compromising membrane integrity and function. Thus it is important to maintain adequate levels of citicoline.

A human study conducted at Harvard Medical School evaluated brain changes after citicoline supplementation in healthy older adults. The researchers detected brain MRI changes indicating increased phosphatidylcholine synthesis after 6 weeks of supplementation with 500 mg of citicoline per day.

Supplementation with citicoline is thought to improve cognitive dysfunction and neurological recovery in various conditions including traumatic brain injuries, stroke, vascular dementia, Parkinson&#;s disease, and aging. However, the research to support citicoline benefits remains lacking and definitive recommendations for supplementing with citicoline cannot be made.

That being said, citicoline is well documented to be safe and there is growing evidence of its benefits for improving cognition, nerve function and possibly helping in addiction recovery.

Pharmacology and mechanism of action

Dietary Choline

Citicoline is manufactured in the body from choline. However, the National Health and Nutrition Examination Survey (NHANES) revealed that only 8% of US adults consume the recommended amount of choline on a daily basis. Low dietary choline intake may be related to deficit performance on neuropsychological tests. In one study of a population of non-demented individuals, high dietary choline intake was related to better cognitive performance but the effects persisted only in association with continued high intake. Research findings show that early higher choline intake at midlife may be neuroprotective. Further study is necessary to determine whether an adequate dietary intake of choline is related to improved cognitive function throughout the life span and to determine the role it plays regarding the preservation of brain health.

Even if dietary choline consumption is sufficient, there are additional benefits to consuming sources of CDP-choline (citicoline) itself. CDP-choline is required for the rate-limiting step of phospholipid synthesis, making choline insufficient to support cell membrane integrity on its own. Citicoline is synthesized from choline which is found in foods like liver, meat, beans, eggs, and cruciferous vegetables (broccoli, cauliflower), while only liver, brain, and organ meats provide appreciable amounts of CDP-choline (citicoline).

Both choline and citicoline support phospholipid metabolism, acetylcholine production, and cell signaling. But citicoline is also a source of cytidine. It is the cytidine component that gives supplementing with citicoline an advantage over choline. The cytidine component of citicoline converts to uridine before crossing the blood-brain barrier. The uridine component is required for the rate-limiting step of phosphatidylcholine production and that uridine also promotes neuronal growth. Uridine is the molecule responsible for increasing brain levels of norepinephrine and dopamine, improving mitochondrial function, and boosting energy production in the brain.

Supplementation with citicoline offers a way to boost endogenous levels of CDP-choline in a way that cannot be achieved by other means. The oral bioavailability of citicoline exceeds 90%, its metabolites cross the blood- brain barrier, and citicoline is resynthesized in the brain after oral consumption.

In healthy adults it has been shown that an oral dose of citicoline is rapidly absorbed with greater than 90 percent bioavailability. Citicoline is metabolized by hydrolysis into choline and cytidine in the gut wall and these two products (choline and cytidine) are distributed throughout the body and utilized in various biosynthetic pathways. They also cross the blood-brain barrier to re-synthesize into citicoline in the brain.

Dosing of Citicoline

It is estimated that the daily dietary allowance of choline is 550 mg/day for men and 425 mg/day for women.

Oral, intravenous and intramuscular doses for citicoline typically range from 500-2,000 mg/daily. Most clinical trials evaluating citicoline &#;particularly those involving healthy adults and teens&#;have utilized dosages of 250 mg or 500 mg per day. Both of these dosages have produced beneficial effects.

Dosages as high as 2,000 mg per day have shown benefit in patients with addictive disorders, and dosages of 2,000-4,000 mg per day for 6-12 weeks produced more significant improvements than lower dosages in patients recovering from a stroke. Researchers who conducted the Italian VITA and IDEALE studies, propose that citicoline administration of at least 6 months is required to observe its greatest neuroprotective effects.

The safety profile and tolerance of citicoline is excellent and no serious adverse events have been reported in clinical trials of citicoline at dosages ranging from 250 mg to 4,000 mg per day. Side effects are mild (never severe) and rare, mainly consisting of gastrointestinal discomfort, irritability, uneasiness and restlessness. Citicoline has also undergone several toxicological studies and has been proven safe.

Therapeutic Targets of Citicholine

Addiction

Citicoline affects acetylcholine, dopamine, and glutamate neurotransmitter systems; serves as an intermediate in phospholipid metabolism; and enhances the integrity of nerve membranes. Interest has grown in citicoline as a treatment for addiction since it may have beneficial effects on craving, withdrawal symptoms, and cognitive functioning, as well as the ability to attenuate the neurotoxic effects of drugs of abuse.

One mechanism proposed for citicoline&#;s benefit for addiction is that it increases dopamine levels in the corpus striatum by enhancing tyrosine hydroxylase activity and inhibiting dopamine reuptake. This indicates citicoline&#;s potential enhancement of the condition of Reward Deficiency Syndrome, the underlying basis of addiction associated with depletion of dopamine in the reward centers of the brain.

See: Reward Deficiency Syndrome

Most addiction research has evaluated citicoline for cocaine and methamphetamine use although it is suggested that citicoline may also hold promise for other addictions including alcohol, cannabis dependence and binge eating. Although not well studied in opioid addiction, the benefit of citicoline is also suggested.  Citicoline appears to decrease craving and is associated with a reduction in cocaine use, especially in patients with both bipolar disorder and cocaine addiction.

See: Reward Deficiency Syndrome & Addiction

Learning and Memory

Experimental studies in both animals and humans have suggested that citicoline has ability to promote learning ability and memory. In a double blind, crossover trial, it was showed that citicoline improved the ability to recall words and objects.

Citicoline, also known as cytidine-5&#;-diphosphocholine or CDP-choline, is a fat molecule that is an important part of the cell membrane.

Researchers have studied citicoline in the setting of neurological (brain and nerve) diseases, such as dementia. It is commonly used to enhance cognitive function.

This article discusses citicoline's potential benefits and safety.

Citicoline Supplement Facts

• Active Ingredient(s): Citicoline
• Alternate Name(s): Cytidine-5&#;-diphosphocholine (CDP-choline)

• Legal Status: Over-the-counter (OTC) dietary supplement (United States); prescription drug (Japan and Europe)

• Suggested Dose: The therapeutic dose of citicoline ranges from 500 to 2,000 milligrams (mg) per day.
  Citicoline can be given intravenously (IV, within a vein), intramuscularly (within a muscle), and orally (by mouth).
• Safety Considerations: Caution should be taken if you are pregnant or breastfeeding because the safety of citicoline is unknown in these populations.

What Is Citicoline?

Citicoline has been studied to treat the following conditions:

• Brain stroke
• Dementia prevention and treatment
• Traumatic brain injury
• Nerve pain and injury (animal models)

Citicoline has improved cognition in people with neurological conditions. And it has also improved memory and cognitive function in healthy people.

Citicoline works to protect the brain by:

• Increasing dopamine,

  norepinephrine

  , and serotonin levels
• Serving as a precursor to

  acetylcholine

  , a type of chemical messenger that helps brain and body functions
• Lowering levels of

  glutamate

  , a brain chemical that causes damage to the brain under low oxygen conditions
• Blocking

  phospholipase

  A2, a type of enzyme that then reduces inflammation
  

Older adult solving a crossword puzzle.

Uses

Supplement use should be individualized and vetted by a healthcare professional, such as a registered dietitian (RD) or registered dietitian nutritionist (RDN), pharmacist, or healthcare provider. No supplement is intended to treat, cure, or prevent disease.

Age-Related Cognitive Decline

Citicoline supplementation improved memory in older adults with age-associated memory impairment compared to a placebo (no treatment) group. However, the study is not generalizable to young adults or people with cognitive diseases like dementia and Alzheimer&#;s disease (AD).

A review of a collection of studies showed a positive effect of citicoline on cognitive function in people with mild vascular cognitive impairment, vascular dementia, or AD. Because citicoline was used with the standard treatment (acetylcholinesterase inhibitor) for AD, the effect of citicoline alone on AD is unclear.

4 Tips to Select the Right Sodium Deoxycholate Purity

Cognitive Enhancement

Additional reading:
How to Select Sodium Deoxycholate Purity?

For more information, please visit Citicoline Sodium And Stroke Prevention.

In a study, a citicoline-caffeine-based drink improved attention, mental alertness, and memory. Since citicoline was combined with caffeine, it is unclear what the effect of citicoline alone is on attention and memory.

Based on a study in young, healthy males, citicoline improved motor function and attention after four weeks of supplementation. However, study results might not apply to populations other than young, healthy males.

Eye Surgery Recovery

Using citicoline eye drops three times a day for one month after eye surgery aided the recovery of corneal sensitivity after LASIK (laser-assisted in situ keratomileusis).

Stroke Treatment

A systematic review of studies found citicoline alone benefited acute ischemic stroke (blood clots in the brain). However, citicoline offers limited benefits on top of standard stroke treatment with rtPA or recombinant tissue plasminogen activator (clot-busting drug).

Furthermore, one study in people with a first ischemic stroke showed that after the stroke, people who received citicoline over two years had reduced cognitive impairment.

Neuroprotection

Citicoline has been studied for the following neuroprotective (protecting the nerves and brain) effects:

While citicoline may benefit various cognitive conditions, further research is needed to confirm these results.

Food Sources

Besides supplementation, another way to increase citicoline levels is by consuming cytidine- and choline-rich foods. Citicoline is composed of cytidine and choline. Cytidine is found in meat, especially organ meats.

Foods rich in choline include the following:

• Beef liver, pan-fried, 3 ounces (356 mg per serving)
• Egg, hard-boiled, 1 large egg (147 mg per serving)
• Beef top round, separable lean only, braised, 3 ounces (117 mg per serving)
• Chicken breast, roasted, 3 ounces (72 mg per serving)
• Beef, ground, 93% lean meat, broiled, 3 ounces (72 mg per serving)
• Fish, cod, Atlantic, cooked, dry heat, 3 ounces (71 mg per serving)
• Beans, kidney, canned, one-half cup (45 mg per serving)
• Quinoa, cooked, 1 cup (43 mg per serving)
• Brussels sprouts, boiled, one-half cup (32 mg per serving)
• Broccoli, chopped, boiled, drained, one-half cup (31 mg per serving)
  

Dosage

The usual therapeutic dose for humans used in clinical trials is 500 to 2,000 mg daily.

Listed below are the citicoline dosing for various conditions used in clinical trials.

• Add-on therapy in PD: Usual treatment with levodopa/carbidopa for five weeks plus citicoline 1,000 mg intravenously daily from weeks three to five.

• Add-on therapy in MDD: Citicoline 100 mg by mouth every 12 hours plus Celexa 20 mg per day (for the first week) and 40 mg daily by mouth for the following five weeks.
   
• Add-on therapy in schizophrenia: 1,000 milligrams (mg) by mouth per day for three days, 2,000 mg per day (in two divided doses) on day four for four days, and 2,500 mg per day (in two divided doses) starting week two; used with up to 6 mg of risperidone daily in the study.

• Age-related cognitive decline: Two 250 mg capsules of citicoline (500 mg/day) by mouth with breakfast for 12 weeks.

• Cocaine dependence in bipolar I disorder: 500 mg by mouth per day for one week, then 1,000 mg per day at week two, mg per day at week four, and 2,000 mg per day at week six, for 12 weeks total.

• Cognitive enhancement: Beverage consisting of 250 mg of citicoline and caffeine (amount unclear).
  For motor function and attention in adolescent males, 250 or 500 mg capsule by mouth per day for 28 days.

• Glaucoma: Citicoline oral solution of 50 mg per milliliter (mL) (mg/mL) used for a daily dose of 10 mL or 500 mg of citicoline by mouth in the morning.

• Head injury: For moderate to severe head injury, 2 g by mouth for 60 days; for severe head injury, 3 g intravenously (IV) for 21 days.

• Stroke treatment: 250 to 2,000 mg from 10 days to six weeks. In the clinical trials, citicoline was given intravenously, orally, or both intravenously and orally;
  for cognitive impairment in people poststroke, 1 gram (g) daily by mouth for two years.

• Methamphetamine dependence: 1 gram (g) of CDP-choline capsule by mouth twice daily for eight weeks.

• Neuroprotection: In neonates (newborns) with HIE, 10 milligrams (mg) per kilogram (kg) per 12 hours (h) intravenously for four weeks plus other supportive measures.
  
  
• Nonproliferative diabetic retinopathy: One drop of citicoline and vitamin B12 eye drops containing citicoline 2%, hyaluronic acid 0.2%, and cyanocobalamin (vitamin B12) 0.05% into one eye three times daily for 36 months.
  
  

Safety

Citicoline is naturally present in the human body and is a nontoxic substance. Citicoline taken by mouth at amounts of up to 1 g per day has been shown to be safe and well-tolerated.

Overall, citicoline is well-tolerated and has no adverse systemic cholinergic side effects (e.g., increased saliva and tear production, urination and defecation, and decreased heart rate).

Avoid citicoline if you're allergic to it or its components (parts). Seek immediate medical attention if you have a severe allergic reaction (itching, hives, shortness of breath).

Side Effects

Although no serious side effects were noted in some studies, mild side effects include the following:

• Increased appetite
• Weight gain
• Increased flatulence (passing gas)
• Headache
• Increased burping

Common side effects include the following:

• Nausea
• Vomiting
• Dizziness
• Stomach upset
• Fatigue
  

Interactions

While there are few studies on drug interactions with citicoline, citicoline theoretically can increase the effect of levodopa by increasing dopamine levels.

Moreover, citicoline with levodopa allowed for a lower dose of levodopa in studies.

Precautions

Many clinical trials exclude people who are pregnant or breastfeeding. Therefore, the safety of citicoline in people who are pregnant or breastfeeding is unknown. 

Although citicoline is well-tolerated, it is essential not to take more than instructed. 

Please consult with your healthcare provider before starting citicoline. 

Dietary supplements are not regulated like prescription medications in the United States. Therefore, some may be safer than others. When choosing a supplement, consider factors such as third-party testing, potential drug interactions, and other safety concerns. Talk to a healthcare provider or a registered dietitian nutritionist (RD or RDN) about supplement quality and safety.

Similar Supplements

Other supplements that have cognitive-enhancing properties include the following:

• Antioxidant polyphenols: Polyphenols, such as resveratrol, improved cognitive function in people with mild cognitive impairment and Alzheimer&#;s disease in clinical study.

• B vitamins: B vitamins have decreased cognitive decline, and a higher dietary folate intake has been shown to lower dementia risk.

• Medium-chain triglycerides (MCT): Consuming MCT jelly by mouth three times daily for a daily MCT dose of 17.3 g for 30 days improved cognition in people aged between 57 and 87 years with mild to moderate Alzheimer&#;s disease.

• Omega-3 fatty acids: An analysis of a collection of studies revealed that omega-3 supplementation affects cognitive function in adults of advanced age in a positive way.

• Selenium: Supplementation with selenium has been shown to improve cognitive function in people with mild cognitive impairment and Alzheimer&#;s disease.
  
  
• Vitamin D: A clinical trial conducted in China found that daily vitamin D supplementation of 800 international units (IU) by mouth daily for 12 months improved cognitive function by reducing oxidative stress in participants aged 65 and older with mild cognitive impairment.
  
  

Similar to citicoline, the supplements above are believed to improve cognitive function. However, whereas citicoline is naturally found in the human body as CDP-choline, the above supplements are not produced by the human body.

Summary

Not only does citicoline protect the brain, but it also has an excellent safety profile. 

Several clinical studies indicate citicoline's therapeutic potential in various neurological conditions, including age-related cognitive decline and stroke treatment and recovery.

Frequently Asked Questions

• How does citicoline work to improve cognitive function?

  Citicoline works to improve cognitive function by increasing brain choline and promoting the production of acetylcholine, a neurotransmitter essential for memory. Additionally, citicoline increases levels of dopamine, norepinephrine, and serotonin.

• How is citicoline administered?

  Citicoline is administered via the following routes: oral (by mouth), intravenous (within a vein), or intramuscular (within a muscle).
  

• What is the difference between citicoline and choline?

  Once citicoline is ingested, it is broken down into two molecules: cytidine and choline.

  After these two molecules cross the blood-brain barrier separately and reach the brain cells, they combine to form CDP-choline (citicoline) again.
  

  Citicoline serves as a source for making phosphatidylcholine, one of the parts of cell membranes.

  Choline, one of the breakdown products of citicoline, serves as one of the building blocks for the production of acetylcholine, a neurotransmitter (chemical messenger) involved in memory and muscle movement.

  Contact us to discuss your requirements of How Citicoline Works. Our experienced sales team can help you identify the options that best suit your needs.