Citicoline: Nootropic and novel benefits

19/02/2015 Tags: all

Please note: This article is for information purposes only. We do not endorse intake of citicoline unless otherwise stated by your primary healthcare provider. Any undesirable effects from citicoline intake are sole responsibility of the user.

Citicoline was first synthesized in 1956 by a group of researchers. It was initially developed in Japan to treat stroke patients. Marketing and manufacturing license was obtained by Interneuron for Canada and US in 1992. These rights was obtained by Takeda in 1999. Today, citicoline is available as a supplement for cognitive problems in the US and a prescription drug in Europe.

What is citicoline?

Citicoline is nutrient that is created within the body. It is an important element in the phosphatidylcholine synthesis and a critical element of the grey matter. It is a water soluble substance that directly affects the release of choline. It is also being converted into phosphatidylserine in the brain. Together with choline, both are important compounds in repairing and developing brain cells.

Chemical name: 5'-O-[hydroxy ({hydroxy[2-(trimethylammonio)ethoxy] phosphoryl}oxy)phosphoryl]cytidine

Usage: neuroprotection and nootropic

How does citicoline works?

Citcoline has several mechanisms of action. One mechanism that has been associated with citicoline is its ability to reduce ischemic events through decreasing the accumulation of free fatty acid in the lesion. Note that after an ischemic event, there is a significant increase of pro-inflammatory glycerols, arachidonic acid and free fatty acids due to breakdown of neuronal membranes. Harmful substance including thromboxane, free radicals and prostaglandins may accumulate whilst lead to complications. However, citicoline supplementation prior to an ischemic event may reduce the accumulation of free fatty acid, arachidonic acid and other toxic substances in the brain. Citicoline will further help in invigorating membrane reaction and decreasing damage from free radicals.

Citicoline also appears to increase the synthesis of phosphatidylcholine in the brain. Phosphatidylcholine is a critical component of cell integrity and repair. Most recent study shows that both uridine and choline stimulate the synthesis of phosphatidylcholine after citicoline supplementation.

Another important mechanism associated with citcoline is its ability to increase the synthesis of phosphatidylcholine during a cerebral ischemic attack. After stroke and ischemia, the brain’s ability to synthesize phospholipid is negatively influenced. Citicoline however increases choline and cytidine – building blocks of neuronal restoration.  Other than these modes of action, there are some studies indicating the citicoline may help in normalizing neurotransmitter release pattern. Other studies even reveal that citicoline inhibits impairment of neurotransmitter release during hypoxic conditions. Citicoline has been associated with blood vessel dilatation which increases delivery of oxygen and nutrients in the brain.

Supplementation of citicoline has been associated with increased synthesis of dopamine in the brain. It is able to exert its action through enhancing dopaminergic pathways. It does so through increasing the levels of acetylcholine in the brain which is closely linked with phospholipid synthesis enhancement. It also tends to increase activities of serotonin and norepinephrine – neurotransmitters that help with learning and memory.

Other mechanisms linked to citicoline supplementation include antioxidant, neuroprotective effects and lipid peroxidation reduction. Citicoline helps in stimulating the synthesis of glutathione whilst aides in facilitating glutathione reduction activities. It also helps in maintaining and preserving cardiolipin – an element critical for mitochondrial functioning. Citicoline also helps in decreasing lipid peroxidation through preventing the conversion of phospholipase A2 that leads to reduced neural tissue inflammation.

What are the benefits of citicoline?

Upon discovery, citicoline is among the most researched novel drug for cognitive enhancement. Some of the benefits associated with citicoline supplementation include:

Treatment for acute ischemic stroke

Numerous studies involving stroke patients has been carried out to assess citicoline’s effects on post-stroke cases. Although there is some conflicting evidence, most studies have shown that citicoline supplementation can help in inducing full recovery amongst users. It has been shown to improve neurological symptoms amongst this particular population as well. Studies further show that individuals who have moderate to severe acute ischemic stroke symptoms are more likely to benefit from citicoline use.

Cognitive decline reversal

Supplementation with citicoline has been strongly linked with synthesis of phosphatidylcholine. Numerous studies also revealed that a 6 week citicoline supplementation can increase levels of phosphodiesters – substances that helps in cognitive decline reversal amongst elderlies.

Methamphetamine dependence and depression symptoms alleviation

Recent data has shown that citicoline may have positive effects on patients diagnosed with cocaine dependence mania. Evidence points out that citicoline can significantly improve auditory skills, verbal skills, depressive symptoms and cognition amongst this population. This shows that citicoline might help in treating depression and substance dependence.

Treatment of glaucoma

One study has demonstrated that citicoline might be effective in alleviating the effects of glaucoma. Patients suffering from glaucoma may have their retinal and cortical responses improved with citicoline supplementation. It was further revealed that citicoline can help in decreasing high blood pressure amongst this population.