USING ACETYLCHOLINESTERASE INHIBITORS AS NOOTROPICS

This post was written by the original Peak Nootropics blog team and has been recreated for reference purposes:

If you really want to kick it up a notch, you may decide to use an acetylcholinesterase inhibitor as a nootropic or even add it to an existing stack. One of the most successful nootropic formulations, Alpha Brain uses an acetylcholinesterase inhibitor as one of its primary active ingredients. This article will go over the benefits and downsides of using these advanced cholinergic substances.

WHAT ARE ACETYLCHOLINESTERASE INHIBITORS?

Acetylcholinesterase is an enzyme that breaks down acetylcholine and it is needed within our bodies to terminate the movement of our muscles. Acetylcholine is a cognitive neurotransmitter but it also plays role in how our muscles and tissues work. It is needed within our brain to signal to our muscles and tissues. Without acetylcholinesterase, there would be a toxic build-up of acetylcholine that would eventually cause death.

Even though acetylcholinesterase is essential, does not mean that having it is particularly good for cognition. When acetylcholinesterase levels get too high, it can cause acetylcholine to be destroyed. Having too much acetylcholine destroyed causes cognitive defects and eventually decline.

Acetylcholinesterase inhibitors are drugs that were developed to partially block and control the amount of acetylcholinesterase. These drugs were created as a treatment for Alzheimer’s disease. Alzheimer’s patients use these drugs to slow down the progression of the disease and partially reduce symptoms

ACETYLCHOLINESTERASE INHIBITORS AS NOOTROPICS

So acetylcholinesterase inhibitors may benefit people with neurodegenerative diseases, but can they also benefit the healthy? Most people already have a healthy ratio of acetylcholine to acetylcholinesterase however this does not mean that one could not benefit from using an acetylcholinesterase inhibitor as a nootropic. In fact, Acetylcholinesterase inhibitors make excellent nootropics on their own and they are highly underutilized and overlooked.

There have been several studies involving the use of acetylcholinesterase inhibitors in healthy subjects. Studies have shown improved learning as well as verbal and episodic memory when administered acetylcholinesterase inhibitors. Other factors of cognitive functioning such as attention where also improved. So the fact of the matter is that using acetylcholinesterase inhibitors alone is a great idea.

USING ACETYLCHOLINESTERASE INHIBITORS IN NOOTROPIC STACKS

Using acetylcholinesterase inhibitors with racetam nootropics like piracetam and noopept may have great benefits. An acetylcholinesterase inhibitor will essentially increase the amount of acetylcholine available in the brain. Since most racetams act as positive allosteric modulators of acetylcholine receptors, this should allow for more acetylcholine and a stronger nootropic effect from the stack.

Many people ask if they should combine a racetam + acetylcholinesterase inhibitor along with a choline or acetylcholine supplement. Generally, the answer is no if you are using a precursor to acetylcholine like choline itself. People may still decide to use acetylcholine supplements like alpha GPC and citicoline as these have entirely different mechanisms and seem to pair quite nicely with acetylcholinesterase inhibitors. Some people may experience side effects when combing alpha GPC or citicoline with an acetylcholinesterase inhibitor.

One downside of adding in an acetylcholinesterase inhibitor is the chance of cholinergic side effects such as headache and mood problems associated with cholinergic “overactivity”. In some cases acetylcholinesterase inhibitors may be too strong for an individual. This is why one must be really careful when using these types of nootropics.

WHERE TO GET ACETYLCHOLINESTERASE INHIBITORS

One can obtain acetylcholinesterase inhibitors very easily and even over-the-counter. Huperzine A is a natural ACHe inhibitor that works almost as powerfully as typical prescribed ones. If you decide to use huperzine A in your stack, just be extremely careful as this natural inhibitor is no joke and will cause the same side effects in high dosages as prescription acetylcholinesterase inhibitors.

Another option for an over-the-counter acetylcholinesterase inhibitor is galantamine. Galantamine is a natural alkaloid that is prescribed for Alzhiemer’s disease. Even though it has medical use, it can also be obtained over the counter without breaking any laws. Like with huperzine A, be very careful with how you dose this product.

REFERENCES

http://www.ncbi.nlm.nih.gov/pmc/articles/PMC2014378/ – Acetylcholinesterase inhibitors in Alzheimer’s disease
http://www.sciencedirect.com/science/article/pii/S1043661810000617 – Acetylcholinesterase inhibitors in healthy subjects