Coluracetam: Review of the Benefits, Dosage, & Side Effects
By Ali Kuoppala | Last reviewed Mon 24 September 2018
Medical Review by Dr. Stefano Pizzo, MD
What is Coluracetam: Known also as MKC-231, Coluracetam is a nootropic smart drug from the racetam family.
Although it has the same pyridione skeleton structure, it seems to have somewhat different effects than what are seen with its predecessors. Of all the drugs from the racetam family, it’s the most complex and highly modified type.
Whereas the majority of racetams have been synthesized for the purpose of enhancing learning and memory, Coluracetam was originally created in the Japanese Mitsubishi Tanabe Pharma Corporation for Alzheimer’s disease.
Coluracetam (2-(2-oxopyrrolidin-1-yl)-N-(2, 3-dimethyl-5, 6, 7, 8-tetrahydrofuro2, 3-b quinolin-4-yl)acetoamide) is purely synthetic and doesn’t occur naturally in any food sources or plants.
Table of Contents
How Does Coluracetam Work
The effects of Coluracetam are somewhat different from the previously introduced racetam smart drugs.
The main function of Coluracetam appears to be cholinergic, as it increases the high affinity choline uptake (HACU), which increases the production of the neurotransmitter acetylcholine in the brain (increased levels being linked to improvements in memory, attention, learning, and reasoning).
This is likely the reason why Coluracetam was originally designed and researched for Alzheimer’s disease, as the choline uptake into the neurons is known to be suppressed in people who have the disease.
Coluracetam also has a neuroprotective effect, as it is able to prevent over-excitation of the neurons when triggered by excess glutamate or calcium influx.
Coluracetam has also been theorized to help relieve symptoms of schizophrenia in animal-model, but this would definitely need further research to be confirmed.
Overall, the mechanism of action behind the nootropic effects of Coluracetam isn’t fully known as it hasn’t been researched as extensively as its predecessors. Coluracetam possesses some neuroprotective effects and seems to increase acetylcholine synthesis which likely results in improved memory, learning, and attention.
Coluracetam Benefits and Research
Sadly, the research on Coluracetam is sparse, although it likely has similar effects to other – more studied – racetams.
It has been shown in rats that Coluracetam is able to cross the blood-brain barrier and quickly increase the choline uptake to neurons and acetylcholine production.
Coluracetam administration is also able to preserve the high affinity choline uptake (HACU) in rats that are fed choline uptake blocking drugs.
The neuroprotective effects of Coluracetam can be seen in this rodent study, where its administration was able to prevent the formation of learning deficits commonly seen after administration of neurotoxic chemicals
Unfortunately no human evidence exists to validate these findings seen in animal-model.
Small amount of research exists in animals to support the idea that Coluracetam increases choline uptake and acetylcholine synthesis and is neuroprotective. It also seems to work similarly to Aniracetam and Nefiracetam in building up the cognitive benefits rather than having an acute effect.
Coluracetam Dosage and How to Take
Being a relatively new compound and under-studied in humans, the optimal dosage isn’t determined yet.
Converting the dosages of animal studies to human equivalents, we can narrow down the likely *optimal* dosage to 10-40mg/day.
Due to its relatively short half-life of around 3 hours, it’s recommended to divide the dosage to multiple smaller ones taken thorough the day.
In their book “Smart Drugs and Nutrients” the two authoring doctors recommend taking an attack dose with racetams so that the compounds would build up in neurons faster.
This dosage is said to be 2-5x of the normal recommended dosage, and would be a good idea for some of the racetams that are confirmed safe at high dosages (like Piracetam or Oxiracetam), but with Coluracetam there isn’t in my opinion enough research on its side effects and toxicology to recommend mega-dosing.
Coluracetam is fat-soluble and thus should absorb better with a meal containing a source of fatty-acids.
Since Coluracetam appears to be very effective at increasing choline uptake and acetylcholine synthesis, it also will deplete the bodily choline pool…
…Which is why you should always be eating a good amount of foods rich in choline like egg yolks and liver.
Coluracetam should be taken at dosage of 10-40mg per day and since the effects seem to build up, it’s best to be taken for at least 2 weeks for full benefits. Take it with a fat containing meal and some choline and you’re good to go.
Coluracetam Side Effects and Tolerance
The racetam class of smart drugs is extremely safe in terms of toxicity data and side effects.
It’s likely that the low toxicity and lack of side effects seen in studies with other racetams, also extends to Coluracetam, but the lack of studies for this specific racetam are lacking.
From the animal studies using recommended dosages above, there appears to be no signs of toxicity or side effects, in fact the polar opposite is true for Coluracetam; cognitive benefits and neuroprotection.
Anecdotally some users report slight headaches, disturbed sleep, and dizziness with Coluracetam supplementation, but these reports are very rare and the effects are likely easily avoidable by co-supplementation with choline, drinking enough water, not taking Coluracetam close to bed-time, and sticking to recommended dosages.
There isn’t clear scientific evidence to suggest that Coluracetam would be non-addictive or have no tolerance build up, so occasional breaks from taking it are advised.
The lack of research on safety of Coluracetam is a concern, but at least on animals within the recommended dosages it’s not toxic, and has no apparent side effects.
Coluracetam is the most complex of the smart drugs in the racetam family.
Currently, human research on the effects of this smart drug are limited, and a lot of the claims are based off of animal studies.
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