In 1650, a Lebanese man known only as “Jacob” opened the first coffeehouse in Oxford, Britain. Although London was the dominant city of the day, this university town got the first glimpse of the dark, black brew and caffeine-infused work sessions [1].

Nearly 400 years later, caffeine is one of the most ubiquitous and popular mind-altering substances. One of the main reasons for caffeine’s popularity is the utility as a stimulant and performance enhancer.

Also Known As

Coffee extract, Tea extract, 1, 3, 7-Trimethylxanthine, Liquid crack

Editor’s Thoughts on Caffeine

What can I say about caffeine that cannot be said by anyone else? It’s one of my favorite compounds for enhancing cognitive performance and although I have found alternatives with better effects, caffeine will always have a major place in my heart.

As with any tool, caffeine can be abused and I’ve caught myself (and large swaths of the population) abusing the substance to the point of harm. Anyone who cannot function without a cup of coffee and requires it to be at baseline has done themselves a disservice.

When I was consuming far too much caffeine for my own good (only 1 cup of cold brew per day, but I’m sensitive), I started having all kinds of immune health problems. No doctor could help, but when I quit caffeine, everything started to rectify itself. Don’t fall victim to caffeine’s siren song for too long.

Mansal Denton, Nootropedia Editor

Benefits of Caffeine

Coffee, the sober drink, the mighty nourishment of the brain, which unlike other spirits, heightens purity and lucidity; coffee, which clears the clouds of the imagination and their gloomy weight; which illuminates the reality of things suddenly with the flash of truth.” – Jules Michelet

Need we say more? Jules Michelet, a French historian of the 17th century, was an avid caffeine user and assuredly experienced all of the benefits. Namely, caffeine increases focus and mental stimulation. One of the main mechanisms is by increasing adrenaline [2].

Adrenaline is a powerful stimulatory chemical, but not the only mechanism of caffeine. The main mechanism that makes caffeine unique is adenosine activity (as a receptor antagonist), which essentially helps increase alertness and reduce feelings of lethargy [3]. More focus will be given to that benefit in the next section.

There are some studies to suggest caffeine has a positive effect on memory formation [4], though the evidence seems to be contradicting and unreliable [5].

Another benefit of caffeine is as a mood boosting compound. Although this too is unreliable in the scientific literature (given that people often feel improved mood just by the thought of caffeine), there is some evidence to suggest caffeine can increase mood [6]. This would make sense given caffeine’s influence on dopamine and adrenaline activity [7].

Finally, although not as important for our purposes as a brain / cognitive enhancement resource, there are physical stimulant benefits of caffeine. One such benefit is a minor bump in testosterone (by 12% on average) [8], increased fatty acid oxidation (fat burning) [9], and notable power output advantages [10].

How Does Caffeine Work?

The primary mechanism of action for caffeine is as an adenosine receptor antagonist. When we are tired or feeling sleepy, a chemical called adenosine fits into certain receptors and activates providing us with the physical feedback to rest.

Caffeine provides a competitive molecule, which sits in the spot of adenosine without activating it, which prevents the adenosine from causing drowsiness [11] [12]. This is the reason so many people use it when sleep deprived or to stay mentally alert.

Side Effects of Caffeine

Unfortunately, there are a host of negative side effects of caffeine. The first, and most well-known, is the tolerance effect. Many who consume caffeine too often become tolerant to the drug and the potency starts to wear off [13]. This sometimes creates a vicious cycle of consuming ever-higher quantities of caffeine in order to see positive effects.

When users can finally remove themselves from the problem of tolerance, they are usually faced with withdrawal symptoms, which will be proportional to the dosage of caffeine they were used to consuming. These often include things like headaches (caused by cerebral blood pressure) and reduced cognition [14].

Other side effects of caffeine include increased heart rate blood pressure [15] and anxiety [16]. If you have ever had too much caffeine the jittery feelings associated with the compound can be associated with all of these factors.

Mitigating Caffeine Side Effects

There are ways to mitigate some of the negative side effects of caffeine and some are more well-known than others. These three options can help to enhance some aspects of caffeine while hopefully preventing short and long-term negative health consequences of the drug.

Caffeine + L-Theanine – the most well-known of the caffeine stacks is a combination of caffeine with L theanine. The latter ingredient is a psychoactive amino acid found in tea, which can negate the side effects of caffeine (such as heart rate, blood pressure, etc) [17] while increasing the positive aspects of focus and concentration [18].

Caffeine + Pterostilbene (Pure Energy) – the novel combination of caffeine bound to pterostilbene can slow the absorption of caffeine, which increases the compound’s half-life (length) while preventing the symptoms of the crash. The patented version is called Pure Energy and is a part of the Qualia stack we speak highly of.

Cycling Caffeine – cycling off of caffeine is another great method for reducing the negative side effects and amplifying the positives. While it requires taking many days off from using the compound, it is more sustainable in the long-run. We recommend taking caffeine no more than 3 times per week with plenty of spacing in between.

Caffeine Dosage

The caffeine dosage will vary wildly depending on your desires and goals. A caffeine-naive person (someone who does not have much experience with caffeine) can feel mentally stimulated by as little as 20 – 40 mg. This is one reason why Four Sigmatic mushroom coffee is useful (each serving only has 40 mg of caffeine).

Those drinking a cup of coffee will probably consume anywhere between 80 – 100 mg per cup. This is often a good starting point for heavier caffeine users (and those who are trying to see physical enhancements from the drug).

For the purposes of fat burning, 200 mg is the usual dosage and some people even get to 500 mg for acute strength purposes. At these ranges (and anything higher), the effects become dangerous for heart health.

References (Click to Expand)
    1. Tom Standage “A History of the World in 6 Glasses”
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Nootropedia is meant to be a resource for individuals researching drugs and supplements that are good for brain health, otherwise known as nootropics, and thus we are the Nootropics Encyclopedia. Because of our in-depth coverage of this topic, our community has requested that we cover other brain health topics and "lifehacks" so that has become the focus of Nootropedia.