One of the most well known and loved of all the classes and categories of nootropics is of course the racetam family of cholinergics. This is at least in part due to the fact that the racetams (especially the three classic racetams, piracetam, aniracetam and oxiracetam) are some of the safest and most widely studied of all the true nootropics. These three however are not the only racetams available. Coluracetam is a lesser known, but very popular cholinergic supplement that comes from the racetam family. Today we’ll be taking a closer look at what makes coluracetam special.
Coluracetam (originally MKC-231, also known as BCI-540) was originally developed and tested by the Mitsubishi Tanabe Pharma Corporation as a drug therapy for Alzheimer’s. It was later in-licensed by BrainCells Inc. who began working with coluracetam to investigate it’s potential effectiveness in treating Major Depressive Disorder (MDD). The state of California offered BrainCells Inc. a “Qualifying Therapeutic Discovery Program Grant” and phase IIa clinical trials suggest it could be a possible therapeutic agent useful for those living with comorbid major depressive disorder with generalized anxiety disorder.
Coluracetam (BCI-540; formerly MKC-231) is a nootropic belonging to the racetam family of drugs. It was originally developed and tested by the Mitsubishi Tanabe Pharma Corporation for Alzheimer’s disease. After the drug had failed to reach the endpoints in its clinical trials, it was in-licensed by BrainCells Inc for investigations into major depressive disorder (MDD), which was preceded by being awarded a “Qualifying Therapeutic Discovery Program Grant” by the state of California. Findings from phase IIa clinical trials have suggested that it would be a possible medication for a comorbid major depressive disorder (MDD) with generalized anxiety disorder (GAD).
Compared to the classic nootropics like piracetam, coluracetam is a fairly new nootropic compound. As a result, it’s not nearly as widely studied as piracetam, oxiracetam and aniracetam (the three most widely studied of the nootropics). Like the other racetam compounds, coluracetam has been shown to be both neuroprotective as well as an effective cholinergic cognitive enhancer. The main benefit you may receive from coluracetam supplementation is increase in high affinity choline uptake (HACU). This means the uptake of choline is improved allowing the brain to synthesize more acetylcholine. Acetylcholine, is of course, the primary learning, memory and movement neurotransmitter.
Coluracetam, like the other primary racetams has also been theorized to be effective at combatting Alzheimer’s disease and other age-related neurological issues associated with cognitive decline. According to some anecdotal evidence from users, coluracetam is also a bit of a mood enhancer. Some users have even claimed it has a positive effect on stress and bipolar disorder. It’s primary mechanism of action is cholinergic and may be helpful in spurring on memory formation as well as improving other cognitive functioning. Coluracetam specifically increases acetylcholine in the hippocampus, the region of the brain involved in short-term memory. Once again, much of the evidence regarding coluracetam is strictly anecdotal, but many users find coluracetam more effective than piracetam alone, for instance.
The most common side effects of coluracetam usage include irritability and nausea, but these side effects are extremely rare if used in the proper, recommended dosage. If you find coluracetam too stimulating, you might want to choose to only use it earlier in the day or find a smaller dosage. As always, finding your sweet spot is vital. Start with the minimum effective dosage based on the recommended amounts to find out if you’re sensitive to the compound.
Research hasn’t identified a perfect coluracetam dosage yet, but a dosage of 3.2 – 32.7mg has been found to be a good therapeutic window for supplementation. An average of about 20mg is a good starting dose for coluracetam. Due to the incredibly low dosage compared to piracetam or other nootropics, sublingual administration is favored by many. Sublingual dosing means taking the compound under the tounge to allow it to dissolve and absorb. This bypasses the gut which may improve the bio-availability of the substance. Bioavailability just means how much of the substance ends up being used. The longer you allow the powder or liquid solution to sit under your tonuge, the more of it may absorb.
Coluracetam dosage reaches peak serum levels in about 30 minutes. This is fairly fast acting for nootropics or other substances. Remember that the levels will begin to decline at around 3 hours after dosing. It is quick acting, but relatively short-lived. One of the things that sets coluracetam apart from the traditional racetams are some of the interesting side benefits users have reported. BrainCells Inc. have reported that a daily dosage of 240mg (split into three daily doses of 80mg/per) showed positive results for those living with major depression with co-morbid GAD (generalized anxiety disorder). The results were most prevalent in those who were found to have “treatment resistant” depression, meaning they hadn’t noticed benefits from traditional antidepressants. The first dose wasn’t shown to provide any immediate relief, but by the second dose of 80mg, over one third of the patients studied had improved scores based on their depression assessment test.
Coluracetam isn’t just a potential mood boosting neuroprotective cognitive enhancer though. Oddly enough, some users have associated the use of coluracetam with improved eyesight. The surprising optic benefits are a nice bonus for some users. Enhanced color vision, recognition and vividness are noted anecdotally. For the moment there is no conclusive evidence to support a mechanism of action for this, but some experts theorize that coluracetam may have a positive effect on the brain’s visual processing. In addition to being a cholinergic nootropic, coluracetam has some AMPA potentiation. AMPA neurotransmitters are involved with cognitive function and alertness as well as being involved in long term potentiation, a vital part of how memories are consolidated.
For now, exactly how coluracetam works with choline transporters isn’t fully understood. Like most racetams, coluracetam stacks well with a choline. The improved production of acetylcholine is dependent on choline. Since most people are already choline deficient it’s a good idea to add a supplemental choline source, especially if you’re using cholinergics such as the racetam family. Alpha GPC is a nootropic as well as choline source and one of the highest quality of the choline sources. 250-750mg of Alpha GPC stacks well with the recommended dosage of coluracetam. CDP choline, or citicoline, is another popular choline source for stacking with coluracetam. 300-600mg of citicoline divided into two doses is a good start. Choline bitartate and choline citrate are also choline sources, but don’t provide any stand-alone benefit on their own. That said, they should be sufficient for protectinv yourself from potential brain fog that can arise from using a cholinergic without suffient dietary choline.
Always consult with your primary care practitioner before adding any new supplement, diet or exercise regimen, especially if you’re currently under a doctor’s care or taking any over-the-counter or prescription drugs for any pre-existing conditions.