This article is part of the Performance Pharmacy Series.

In today’s Starbucks-laden world, it comes as no surprise that caffeine is the most (ab)used over-the-counter stimulant drug. Walk into a gas station and there will likely be an entire aisle dedicated strictly to “energy” drinks: Rockstar, Red Bull, Jolt, etc. Oh and if you missed that aisle, don’t worry because there will be an entire row of “energy shot” products waiting by the register (replace the term energy with caffeine and that’s why it has attained numero uno status on the list of most heavily used stimulant drugs).

Most people aren’t even aware of their caffeine intake; they just adhere to the cultural norms of a morning cup of coffee and succumb to the temptation of fighting off the mid-afternoon “crash” at the office…But then it happens. You wake up, down a triple-shot espresso and don’t feel that usual “pep” that you’re yearning for. Your head starts pounding, you feel lethargic, unmotivated, irritable, and wondering why me?

Well, in a generic sense, you’re no different than a heroine junkie going through withdrawals. You’ve become addicted. For most people, this isn’t a big issue because they just sit at a desk all day and are probably more worried about whose birthday it is in the office so they have an excuse to eat some cake. However, for gym-goers and athletes alike, this can mean disaster for performance.

Now don’t get me wrong I’m not about to demonize caffeine use, but rather I will provide some insight into how this commonplace drug, when implemented properly, can propel your athletic performance to another level.

Caffeine: What It Is and How It Works

An abbreviated synopsis:

Caffeine (sometimes listed as 1,3,7-trimethylxanthine) is an organic, alkaline substance and a derivative of xanthine. It’s primarily found in tea leaves, coffee beans, guarana, various fruits, and other sources. Its sister homologues--theobromine (aka 3,7-dimethylxanthine) and theophylline (aka 1,3-dimethylxanthine)--are primarily found in kola nut and cacao plant. While caffeine is metabolized in the liver to its sister homologues (albeit not in substantial quantities), which have slightly different effects in humans; we will focus primarily on the physiological effects caffeine provides for athletic performance.

Methylxanthines serve as central nervous system and myocardial (heart) stimulants and are often therapeutically used to treat disorders such as COPD and asthma due to their bronchodilating property. They act as acetylcholinesterase and phosphodiesterase (PDE) inhibitors; for performance we are mainly concerned with the latter of the two. PDE enzymes serve to break phosphodiester bonds such as those in cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP).

Thus, Inhibition of PDE enzymes prevents (delays) the breakdown of cAMP and cGMP. This is an important mechanism as cAMP and cGMP both serve as second messengers in signal transduction channels. In brief, cAMP and cGMP convey signals from various hormones and other substrates from cell-membrane receptors to intracellular target-molecules. When these signals are amplified by cAMP and cGMP, metabolic processes are more rapid, of which we will look at below.

Brief Primer - What Happens When Your Central Nervous System (CNS) is “Stimulated”

The CNS is composed of the brain and spinal cord in humans and is the pathway for sending and receiving signals between all parts of the body. When the CNS neurons are stimulated and cAMP/cGMP are activated, various bodily functions are sent into “overdrive”; the primary acute effects are:

Increased heart rate

Vasoconstriction

Psychostimulation

Increased metabolism

Increased urination

Some of these effects are indeed favorable for one’s athletic and physique goals. Many studies have analyzed the cardiovascular and resistance training benefits of caffeine and how it can boost aerobic and anaerobic performance. There appears to be multiple mechanisms for how caffeine acts as an ergogenic aid, such as:

Increased exogenous carbohydrate metabolism

Increased fatty acid oxidation

Increased epinephrine (adrenaline) levels

Bronchodilation

Decreased muscle interstitial potassium levels

All of these would be desirable benefits for anyone looking to enhance athletic performance and fat loss. In layman’s terms, increased carbohydrate metabolism allows for more efficient utilization of carbohydrates for energy, increased fatty acid oxidation means more of those pesky love handles get used for your workout than your bedroom affairs, ramped up epinephrine levels give you that “cloud nine” feeling and can be a psychological boost, bronchodilation allows for increased oxygen uptake and the reduced muscle interstitial potassium levels are hypothesized to delay fatigue during intense exercise.

The Benefits and Risks of Caffeine Before Hitting the Gym

Caffeine is indeed a worthy addition to one’s pre-workout arsenal, but it ultimately comes down to one’s goals and the circumstances. Recreational and competitive bodybuilders can gain many advantages from proper caffeine use. Taken before a cardio session it will help with fatty acid oxidation, utilization of carbohydrates, mental focus and help you perform at a higher intensity level.

Likewise, these are all desirable for anaerobic performance as well, so caffeine does have its place before hitting the iron. However, certain sport-specific skills require use of precise motor coordination and technique, so for athletes caffeine may hamper performance during a competition; I’d take caution when supplementing caffeine prior to sporting events if you find you’re too jittery or anxious.

So if these are just some of the more positive and pronounced effects of caffeine on athletic performance, you might be asking, “So is caffeine a wonder drug or what?” In short, side-effects from caffeine are numerous and typically dose-dependent (i.e. more caffeine=more pronounced side effects). Such side-effects may include:

Dehydration and cramping

Headache

Nausea/Dizziness

Gastrointestinal distress

Frequent urination

Heart palpitations

Increased blood pressure

Mental Issues: Irritability, Anxiety, Nervousness, Depression, etc

Decreased fine motor skills

Increased plasma cortisol levels (though this effect is reduced in healthy individuals

After reading these possible side-effects you may be thinking of starting an anti-caffeine campaign. Before you cast this drug off as doing more harm than good, please consider this old adage: the difference between medicine and poison is in the dose. Like most things in life, moderation is the key and caffeine is no different. The good news is that most of the side-effects are avoidable if one implements caffeine properly.

Implementing Caffeine Into Your Regimen

Caffeine is slightly more complicated than other supplements/drugs in regards to optimizing benefits while reducing side effects. Most studies have found that there is not a significant dose-response relation with caffeine and performance; taking more beyond a certain point does not provide extra benefits for performance and may actually lead to more side effects. The key to caffeine is finding that “certain point” of optimal dosage and intermittently cycling on and off the drug to re-sensitize your CNS receptors and give your adrenal glands some repose.

Dose Amount and Timing

The general dose recommendations for performance enhancement with caffeine are 1-3mg per kg of bodyweight (remember: 1lb=2.2kg). If you’re a 180lb (~81kg) athlete, your dose range will land around 80 to 240mg. This is where one will need to assess their individual goals along with their tolerance to caffeine through trial and error. Caffeine is a relatively quick-acting drug with a short half-life of 4-6 hours (assuming your liver is working properly), so it is generally recommended to ingest your dose about 30-60 minutes before your workout or competition.

If you are taking the caffeine on an empty stomach you could get away with as few as 10-15 minutes as food will slightly decrease absorption rate. If you’re one who likes to eat a decent pre-workout meal, I would aim to take your caffeine in at about one to two hours after your pre-workout meal; main reason being that this should help minimize any acute GI distress between the caffeine and your pre-workout meal.

If you train promptly in the morning before eating a meal, you can also mix caffeine in with some whey/casein protein and/or branched-chain amino acids and ingest that on your way to the gym (if you need the carbohydrates you can toss some Gatorade or other simple carbohydrates in there as well). Again, the timing and dose amounts will need fine tuning once you learn how you respond to caffeine.

Best Source of Caffeine

Since caffeine is a “discreet” chemical, it won’t make much difference whether your caffeine is coming from natural (i.e. coffee, tea, chocolate, etc) or synthetic sources (pill/powder form, energy drinks, supplements, soda, etc). I personally like taking my caffeine in from pre-workout supplements as the one’s I prefer list the caffeine content on the label, commonly in the form of “caffeine anhydrous”.

For dosage tracking purposes, I tend to prefer supplemental caffeine versus natural sources since the caffeine content can vary from coffee bean to coffee bean and tea leaf to tea leaf. If you’re one of those hippie-all-natural-organic freaks (don’t get offended, dude man!), then by all means enjoy your coffee.

Dealing with Desensitization

Caffeine’s most dreaded attribute is that it becomes addictive and the nominal dose to achieve performance benefits gradually increases as one develops tolerance to the drug. This is why most coffee drinkers can slam a triple-shot espresso and not feel a thing, or they get a short-lived burst of energy and crash 20 minutes later.

If you’ve reached such a point, I strongly encourage you to back off the caffeine either gradually or cold turkey (if you can handle the withdrawal for a few days). The time it takes for one to become “stimmed out” is still up for debate as the variables that come into play are too numerous, so a general recommendation is that for every 8-12 weeks of using caffeine, one should take 1 to 2 weeks off of it (and most any OTC stimulants).

This will be another case of trial and error though, if you find you handle caffeine well and are still obtaining positive effects 4-5 months in a row, then listen to your body and keep dosing caffeine. Contrarily, if you are 3 weeks in with supplementing caffeine and you feel horrible (with or without your daily dose), then it’s time to reconsider your approach and back off for a bit.

The time it takes to re-sensitize yourself to caffeine is going to be influenced by how often you were taking caffeine and how much. If you are only taking it maybe 2-3 times a week with a moderate dose, you could likely keep it in your regimen indefinitely or until you feel a little too draggy without it (i.e. you depend on caffeine to function). If you’re the type that enjoys pushing the limits then you might find yourself becoming tolerant to the effects in just a few short weeks. Overall, you will likely know when it’s time to give the caffeine a break because you will be facing many of the side-effects mentioned earlier; headaches, irritability, lethargy, decreased motivation, etc.

At this point, it’s time to give your CNS and adrenal glands some rest (also consider backing off the training intensity so it coincides with your caffeine cycles).

Is Caffeine For You?

Caffeine, like any supplement or drug, needs to be assessed by the user through research and anecdotal experience to see whether the benefits will help them achieve their goals or not. If you are naturally an energetic individual who doesn’t feel the need for more stimulation through exogenous sources, then I’m of the opinion that you shouldn’t take caffeine just for the sake of it. While I do think most athletic and physique endeavors can be enhanced by caffeine supplementation, the user is ultimately the one who needs to decide if they like the way it affects them.

Some people may not tolerate caffeine well, so if that’s detrimental to performance then it would be asinine to recommend they use it. Also, for younger kids and those who have any withstanding medical conditions, please make sure to consult with your physician prior to beginning use of such drugs. Yes, caffeine can be lethal in sufficiently high doses (>5g), so treat it like any other drug and don’t abuse it.

Caffeine: Bringing it All Together

I’d be doing you a disservice to say that this is the definitive article for anything and everything caffeine, but I hope that this abridged version of how caffeine affects us and our performance in and out of the gym has shed some new light on your understanding of this ever-so-common drug. It was a tough task as my aim with this series is to bring you to where brains meet brawn because damn’t, I love science and I love lifting weights. There are monumental amounts of data on caffeine to sift through and in the world of supplements that’s a good thing, because you know it must work (otherwise it wouldn’t be so heavily studied).

In the next installment of the Performance Pharmacy Series we will look at synergistic effects of caffeine and other ingredients, such as those in MTS Nutrition Drop Factor like Synephrine, Forskolin, Yohimbine, etc. and the science behind how they can take your fat burning to a new level!

Whether you’re just a weekend warrior looking for a little pep after a hard week at the office, or a competitive bodybuilder ready to tear into some ass-to-grass squats, caffeine may just have a place in your supplement stash; just use it wisely.