Citicoline

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Product Description

History

Citicoline was originally created in Japan as a treatment for stroke patients. It was first identified by a group of researchers in 1955 and was successfully synthesized in 1956 [1]. In 1993, the pharmaceutical company, Internueron, obtained exclusive manufacturing and marketing license for both US and Canada. This commercialization rights was passed onto Takeda on December, 1999. Today, citicoline is available in the European market as a prescription drug and as a dietary supplement for cognitive disorders in the US.

Chemical structure

Citicoline otherwise known as cytidine diphosphate-choline (CDP-choline)/cytidine 5-diphosphocoline is of a water soluble nutrient readily found in the body. It is a necessary component of phosphatidylcholine synthesis – one of the most important elements of the brain’s grey matter. Citicoline has direct effects on the production of the neurotransmitter, “choline.” Additionally, it can be converted into phosphatidyl serine. Both these chemicals are important in brain cell repair and development.

[msgbox]Chemical name/IUPAC: 5′-O-[hydroxy ({hydroxy[2-(trimethylammonio)ethoxy] phosphoryl}oxy)phosphoryl]cytidine

Chemical formula: C14H26N4O11P2

Usage: neuroprotection[/msgbox]

Mechanism of action

Increase in cytidine and choline levels

Citocoline has a several modes of actions which lead to an array of beneficial therapeutic effects on cognitive functioning. One of its most prominent mechanisms includes its effect on the increase of phosphatidylcholine synthesis during cerebral ischemia. After ischemia and stroke, the ability of the brain to synthesize phospholipids is negatively affected. However, citicoline is able to increase cytidine and choline levels. It is important to note that cytidine and choline are the building blocks for neuron restoration integrity.

Phosphatidyl choline synthesis

Citicoline also appears to increase phosphatidylcholine synthesis – an essential composite of cell repair and integrity. Recent literature reveals that choline and uridine stimulates phosphatidylcholine synthesis upon citicoline oral intake.

Reduction of FFA Accumulation

Another mechanism that is purported to decrease ischemic events includes citicoline’s ability to decrease free fatty acid accumulation on the area of the lesion. After an ischemic event, a major increase in pro inflammatory free fatty acids, arachidonic acid and glycerol occur from neuronal membrane breakdown. Harmful substances including free radicals, prostaglandins and thromboxane may accumulate which can further lead to complications. Nevertheless, intake of citicoline prior to ischemic events may decrease arachidonic acid, free fatty acids and toxic substances from accumulating. It will also help in rejuvenating membrane reaction whilst reducing free radical damage.

Other than the abovementioned mechanisms, there are some evidences showing that citicoline can normalize the release patterns of neurotransmitters. In several studies, it was revealed that citicoline prevents neurotransmitter release impairment during hypoxic conditions. Other trials have discovered that citicoline increase blood vessel dilatation whilst increase blood flow to the brain.

Dopaminergic system stimulation

Citicoline administration is also said to increase dopamine synthesis. It exerts its mechanism through improving dopaminergic pathways via increasing acetylcholine levels of which is closely linked to enhancing phospholipid synthesis. Citicoline also tends to have choline evidences by activities neurotransmitter (e.g. serotonin and norephinephrine) which helps in memory and learning.

Other Mechanisms

Other mechanisms linked to citicoline include:

  • Antioxidant effects- citicoline facilitates glutathione reduction activities and glutathione synthesis.
  • Neuroprotective effects- citicoline improves cardiolipin preservation/ maintenance a substance necessary for mitochondrial function.
  • Reduction of lipid perodixation- citicoline reduces lipid perodixation through decreasing phospholipase A2 conversion which leads to decreasing of neural tissue inflammation [1].

Benefits

Since its discovery, citicoline has become one of the most important research topics amongst cognitive enhancing drugs. Most trials conducted for citicoline involved animals; however, there are numerous human clinical trials also undertaken to prove its therapeutic effects [2].

Reversing cognitive decline

Citicoline administration is associated with phosphatidyl choline synthesis. As such, the researchers of this particular study investigated whether this claim is true. All subjects were treated with citicoline for six weeks; the group was then divided into two and was treated with placebo and citicoline for the subsequent six weeks. All subjects underwent several tests which revealed that citicoline increase levels of phosphodiesters. Increase in phosphadiesters indicates that oral citicoline use may help in reversing cognitive decline amongst the elderlies [3].

Acute ischemic stroke treatment

In a randomized trial, 394 patients diagnosed with acute ischemic stroke were enlisted as participants. Subjects were randomly treated with placebo and citicoline and citicoline for six weeks. After the six week study period, the effects of citicoline were assessed using statistical measures. Results showed that citicoline failed to provide therapeutic outcomes on stroke patients. However, post-hoc analyses revealed that it may help in promoting full recovery amongst subjects. It also indicates that individuals with moderate to severe acute ischemic stroke are likely to benefit [4].

Another study revealed a more positive result regarding citicoline therapy for acute ischemic patients. Subjects with moderate ischemic stroke were treated with citicoline, after which, neurological symptoms were assess. When results were compared to the reference group, significant improvement was seen on the study group. This positive effect was amplified on patients less than 70 years of age and when citicoline was administered on the first hours of acute ischemic stroke [5].

Alleviation of depression and methamphetamine dependence

Recent literature data revealed that citicoline have had promising effects to individuals diagnosed with cocaine dependence mania. Hence, the researchers studied the effects of citicoline on methamphetamine dependence and depression. 60 individuals with methamphetamine dependence and major / bipolar depressive disorder were randomly treated with placebo and citicoline. Assessment of cognition, depression symptoms, auditory and verbal skills was done. Statistical analysis revealed that patients who received citocoline therapy demonstrated significant improvement compared to patients under placebo therapy. This study showed that citicoline might help treat substance dependence as well as depression [6].

Glaucoma treatment

In another study, the effects of citicoline on visual responses and retinal reactions amongst glaucoma patients were evaluated. Thirty patients with glaucoma were randomly divided into two groups, fifteen patients on placebo and fifteen patients on citicoline. After treatment and subsequent eight years of follow-up period, data analysis showed that pattern electroretinograms and visual evoke potential parameters are increase with citicoline administrations. This increase in parameters indicates that citicoline enhances cortical and retinal responses amongst glaucoma patients. Moreover, citicoline can serve as complimentary treatment to hypertensive therapy [7].

These studies indicated that citicoline is well tolerated by humans. It can be used in a variety of treatment; nevertheless, precaution upon use is still necessary.

 

Additional Information

Grams

50, 100