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Citicoline, also known as CDP choline, is a unique acetylcholine boosting compound. It is considered to be more effective than choline at creating higher amounts of acetylcholine in the brain. Unlike choline, citicoline is considered to be a nootropic on its own. It also is thought to be neuroprotective by helping to protect the brain from oxidative stress.
As far as efficiency goes, citicoline is superior to choline and phosphatidylcholine. Its effects can be seen as comparable to alpha GPC. The unique properties of this substance make it very attractive. It has also been evaluated to be effective at helping with the symptoms of many neurodegenerative diseases. In the US it is mainly used off label as a supplement and cognitive enhancer.
How It Works
Citicoline has a unique method of action. Although its name is CDP choline, it does not actually contain choline. Its metabolism is rather strange. When it is ingested, it is converted into choline within the GI tract. Once it is absorbed and enters the bloodstream, it is converted back into citicoline. Citicoline is able to cross the blood brain barrier easily and becomes highly active once it is in the brain.
Citicoline works to modulate cholinergic functions in the brain. The substance frees up the amount of choline to be synthesized. It also improves the efficiency of how acetylcholine converts choline. This leads to ultimately higher levels of acetylcholine. The secondary function it has is to replenish levels of phospholipids such as phosphatidylcholine. By replenishing these phospholipids, citicoline acts as a neuroprotective agent. Decreased levels of phospilipids have been linked to cholinergic damages.
Dopaminergic activity is also observed with citicoline but it does not seem to directly increase the concentration of dopamine. It appears to directly influence the activity of the dopamine transporter (DAT) as well as influence the release of dopamine. This may also contribute to some of its benefits and add unique properties seen outside the cholinergic spectrum.
Citicoline has many benefits for brain health and cognition. It can help with cholinergic deficiency by increasing the amount of acetylcholine. Those that are deficient in choline or acetylcholine may see the most noticeable improvements with administration of the substance. Unlike choline, it is considered to be nootropic on its own however these effects may be subtle in otherwise healthy individuals.
Perhaps the best results will be noticed when citicoline is stacked with a positive allosteric modulator of the cholinergic system (racetam). Common reported benefits in a cholinergic stack are increase memory, learning and focus. The dopaminergic functions may help to specifically improve focus and attention.
Citicoline Side Effects
Citicoline is considered a very safe and well tolerated supplement. Side effects are more likely to transpire in higher than normal dosages. The most common side effects are: headache, nausea and an upset stomach. Diarrhea can also be a symptom in sensitive individuals however this is less common of a side effect.
Cholinergic hyperactivity has been suggested to cause mood problems. Higher than normal levels of acetylcholine are thought to relate to depression. Depression may be a symptom of citicoline however these reports seem less common than with choline bitatrate. The dopaminergic effects may help to limit the depressive symptoms of higher acetylcholine. The area of cholinergic depression needs more area of study and research to verify these details.
Citicoline has been seen to be very safe. It has very limited interactions. A long history has been observed with citicoline and the severity of side effects seems very limited. It is considered to be non-toxic and highly neuroprotective in the brain.
Citicoline does not seem to build up tolerance or addiction. The dopaminergic effects do not seem to contribute to addiction in fact, one study showed it to help with the effects of cocaine withdrawal by reducing the desire for dopamine-induced euphoria. Overall, citicoline can be considered to be very safe and well tolerated. Highly dangerous drug interactions do also not seem to be a concern. When it in combined with supplements like racetams, side effects may be more common.
Citicoline stacks very well with other cholinergics. The most common stack is with the racetam nootropics. This is because citicoline can help facilitate the increased demand for acetylcholine. It seems to cause fewer side effects than with choline supplementation. This may have to do with how citicoline metabolizes acetylcholine. It may synthesize acetylcholine on an as needed basis to reduce overload.
It will also stack well with ACh inhibitors. This combination may work very well especially in those with cholinergic deficiency. Others may experience increased side effects with this stack. Many nootropic forumations combine the power of citicoline and an ACh inhibitor like huperzine A.