Last updated on November 29th, 2018
Potent Stimulants. I don’t know what your stance is on sports supplement companies, but you’d be daft not to take responsibility for your own health and learn about the strange sounding ingredients you’re ingesting from their products.
A little over a decade ago, a bunch of these companies were found to be putting anabolic steroids in their products.
Nothing secures a return customer like the results of an oxandrolone-laced pre-workout drink!
Point is, these companies aren’t boy scouts, and they don’t mind watching a few of you drop like sacks of poo after taking a pre-workout they made.
In fact, they know it’s good for business because other guys and girls will find out and say to themselves, that must contain some real potent sh!t, give twelve cases while it’s still available.
I’m not talking about all supplement manufacturers. Sure, many companies will do what they can get away with, and that’s a lot (especially in the US) but there are some, particularly the newcomers and giants, that tend to behave.
By the way, those companies that put steroids in their supps – still in business.
Together with the plethora of existing manufacturers and upstart bodybuilding supplement companies, it’s a lot of people to monitor, and drug authority agencies like the FDA aren’t really up to the task.
That’s why every few years, a dodgy stimulant does the rounds before some suits catch up with it and take it off the shelves. Even then, the lawsuits and BS that follows ensures a lengthy can they-can’t-they debacle until something new pops up and the stimulant riddled mob moves on.
So, that’s what’s inspired any articles that are devoted to these types of stimulant compounds. Old and new, mild or mutant, it’s definitely worth your time to find out what they are so that you can:
- Recognize them
- Use them correctly and safely
- Figure out how much is too much
- Steer clear of them, if need be
- Know what the risks and side effects are
I’m not anti-stimulant or anything sanctimonious like that, but when you’re shopping in an unregulated market like bodybuilding supplements, it pays to educate yourself.
Stimulants – Natural and Synthetic
Stimulants are nothing new. Most people reading this probably ingest some form of stimulant on a daily basis.
Caffeine is the most ubiquitous of all of them. The spectrum is however quite expansive. Methamphetamine (aka speed), for example, is also a stimulant.
Basically, we can’t just label everything a stimulant and sally forth into the unknown, thinking they’re all more or less just pick-me-ups for a super workout and a smashing day at work.
Sports, bodybuilding, weight loss and diet supplements contain stimulants for a number of reasons and they are pretty good multi-taskers for the job, generally speaking.
Benefits of supplementation include:
- Boosted energy
- Increased metabolism and fat burning
- Improved cognitive function and mood
- Reduced appetite
Another common misconception is that natural stimulants are intrinsically healthier or less harmful than synthetic ones.
Many products are sold on the premise that they contain “all natural” ingredients. It’s importnat to remember that nature made one of the most addictive and, some might say dangerous, stimulants conceivable: cocaine.
Let’s ratchet the drama down a little and look at a current example of this nature/synthetic comparison which happens to be perfect for the point I’m making.
One stimulant doing the rounds in the supplement world at present is called DMHA, or Dimethylhexylamine. It’s also known under one of its more famous brand names Octodrine (there’s actually a bunch of names, scientific designations and brands included).
It can exist as two isomeric forms:
The first one there is the natural form which can be extracted from Juglans Regia (walnut tree bark) amongst other things.
The second is the synthetic form, which can be manufactured much more economically than any process of extraction natural sources.
However, if you were to take equivalent doses of each, the natural form would hit you harder. Anecdotal reports suggest that 100mg is an optimal dose for the synthetic form, whereas you would only need 75mg of the natural form to get equal potency.
Your product label might show the details of the source, and indicate whether it is the natural or synthetic form. It might simply label it as dimethylhexylamine, or 2-aminoisoheptane, or DMHA…none of which really tell you the full story.
When DMAA – dimethylamylamine – was the stimulant du jour, some companies would label it as “geranium extract” or “geranium oil extract”.
Some geranium plants, such as the Pelargonium graveolens may contain tiny amounts of DMAA but they are usually in smaller concentrations than 500 parts per billion. Some people suggest it would be too expensive to extract the stimulant from the natural source and it must only be synthetic forms that made it to the market.
Why is any of this important?
In the US there is an ongoing legal battle between a manufacturer and the FDA to determine whether geranium extracts containing DMAA can be considered under the DSHEA’s (Dietary Supplement Health and Education Act) 1994 definition of “botanical”, and thus, “safe”.
It’s all very boring, and as is often the case, it may come down to a court’s interpretation of the letter of the law.
Most other countries don’t have this problem; they just ban the stuff. America – always difficult.
Either way, that legal battle has been going on for years. If nothing else, it demonstrates the sheer tenacity a manufacturer can have in order to get an ingredient like this in their products.
Some Things To Look Out For
Despite the aforementioned wide spectrum of stimulants, both synthetic and natural, it’s obvious that many supplement companies will always try to push the boundaries when it comes to the ingredients they use.
The most potent stimulants are usually the ones with the most potential to cause negative side effects.
Ironically, the ones that crop up every couple of years in “hardcore” bodybuilding and fat-burning supplements are those that we know the least about.
The slow wheels of scientific research don’t catch up to new ingredients until they are already being sold by the ton to eager customers who are looking for the next big thing.
Government agencies are even slower, because they tend to need the research to back up their decisions. Meanwhile, people are purchasing and using stimulants that could cause any number of effects – good and bad – as the manufacturers rake in the profits.
All of that said, there are some names, phrases and even clues, for the discerning customer to look out for when buying their products.
Sympathomimetic Amines and Drugs
This term might turn up in the science babble that supplement companies use to sell you their wares. Or if you do some online searches on a given stimulant, you might end up reading about them.
The sympathetic nervous system is that which is responsible for your fight-or-flight response to a given stimulus, but it is always active at a basic level.
The fight or flight response includes the following effects
- Diversion of blood flow from non short-term-critical organs to the muscles
- Increased Heart Rate
- Rapid energy mobilization
- Pupil dilation
- Bronchial dilation
It is controlled by the catecholamines, which are both hormones and neurotransmitters. They are epinephrine (adrenaline), norepinephrine (noradrenaline) and dopamine, and they function as agonists of the sympathetic nervous system.
An agonist is a chemical which binds to a receptor in order to trigger a biological response. An antagonist blocks the actions of the agonist.
Sympathomimetic stimulants (or drugs) can function like these agonists, interacting directly with the same receptors, and thus triggering the same effects.
They can also increase the production and release of catecholamines and block their breakdown and re-uptake by acting indirectly with the receptors.
Adrenergic receptors are the target receptors of the catecholamines and the stimulants that mimic them. For this reason, stimulants are often referred to as Adrenergic Agonists.
These are the catecholamines and direct-acting stimulants that produce an effect in the sympathetic nervous system.
They either act directly on the adrenergic receptors as epinephrine (adrenaline) and norepinephrine (noradrenaline) would, OR they act indirectly and increase the endogenous (made within the body) production of those catecholamines.
Agonists bind to receptors to produce the biological response, and in the case of adrenergic agonists there are the adrenergic receptors.
- alpha-adrenergic receptors
- beta-adrenergic receptors
- dopaminergic receptors
Direct binding on the alpha and beta receptors can elicit sympathomimetic effects.
There are differences between the physiological and psychological effects from one stimulant to the other, but the important differentiation for you is whether they act on the alpha-adrenergic or beta-adrenergic receptors.
These sympathomimetic compounds stimulate the alpha adrenergic receptors, which are split into a1 (alpha 1) and a2 (alpha 2) receptors.
A common principal effect of stimulating the alpha receptors is vasoconstriction i.e. the narrowing of blood vessels to increase blood pressure. Areas include the skin, GI system, kidneys and brain.
The goosebumps you feel when you are shocked by something is vasoconstriction triggered by an adrenaline spike in your blood. That’s one small aspect of you fight or flight response re-directing blood into muscle tissue to aid fast physical reaction and increased short-term power.
Bronchial dilation is the key fight or flight response governed by the beta receptors. This allows for deeper and easier breathing which of course provides more oxygen to the vital organs and muscle tissue.
Activation of all 3 beta receptors (b1, b2, and b3) increases production of cyclic adenosine monophosphate (cAMP), which is a secondary messenger derived from our principal source of energy, ATP (adenosine triphosphate).
When cAMP is elevated it causes the heart to contract/pump with greater force, while opening the smooth muscle lining the bronchial tubes in the lungs and the inner blood vessels.
Beta-2-adrenergic receptors and their agonists appear to have the most impact in terms of bronchial dilation and smooth muscle relaxation.
Synergy and Tipping the Balance
Hopefully you can see that the sympathetic nervous system works by coordinating multiple agonists, antagonists and their receptors to act synergistically in order to produce the most efficient biological response.
Anatomical location of the receptors, and their concentration, means that the same agonist has different effects in different parts of the system.
For example, epinephrine (adrenaline) can cause vasoconstriction and vasodilation if it binds to alpha or beta receptors, respectively.
So, because a1 receptors are in higher abundance than beta receptors in the periphery of the system, therefore circulating epinephrine constricts the blood vessels there, increasing pressure.
In the main coronary arteries, i.e. the arteries of the heart, the b2 receptors are in greater number and so vasodilation occurs.
Much of this process is so that the body can keep blood flowing to areas that most need it.
Using a stimulant can tip the balance of this synergistic system in different ways depending on the receptors the compound targets.
Beta-2 agonists, for example, have often been used for performance enhancers due to their effect on bronchial dilation and blood flow.
Most of the them, like clenbuterol, ephedrine and octodrine, were originally developed to help people with asthma and other disorders involving breathing difficulties.
Last updated on November 29th, 2018
Central Nervous System Stimulants
Caffeine is the most well known and well researched CNS stimulant on the planet. It has many effects on the human body and brain, including being an indirect booster of adrenaline (epinephrine).
In fact, the sympathomimetic effects discussed in the previous sections come under the overarching category of central nervous system activity.
However, where we’ve talked about the fight or flight response and the sympathetic nervous system, it’s worth focusing more specifically on the psychoactive behaviour of stimulants, the CNS of course being comprised mainly of the brain and the spinal cord.
Psychoactive Stimulants – Psychostimulants
Euphoria is probably the best word to describe the best effect of a psychoactive stimulant. They don’t call them uppers for nothing.
The compounds found in your bodybuilding supplements vary with respect to the type and power of their cognitive effects.
Caffeine is the best example of an every-day stimulant that if used correctly can have several beneficial effects, including:
- Increased Energy, including muscle power and aerobic output
- Improved Cognitive Function, particularly mental energy, focus, mood, motivation
- Increased Fat Burning, from cAMP elevation in adipose tissue
- Reduced Appetite and Cravings
It’s that boost to mental energy that caffeine and other psychoactive stimulants are generally hailed for, because mental fatigue is often the limiter on our performance level, whether we’re at work or doing physical activity.
The same receptors that trigger the physical reaction to the CNS agonists are also present in the brain. Given that psychostimulants can cross the blood-brain barrier, they can have a profound effect on a range of cognitive aspects, including concentration, emotion, and the mental contribution to sex drive.
The cognitive benefits, however, are probably the first to go when we become tolerant to the effects of stimulants.
People often make the mistake of increasing dosage or moving on to more powerful and possibly more dangerous stimulants when they become tolerant to the the one they are using.
Many stimulants have insurmountable tolerances which means that once the effects become dull, no increase in dosage will overcome the tolerance. An increase in dose will unfortunately increase the severity of any negative side effects though.
My advice to anyone who wants to feel the full effects of caffeine again is to simply cycle off it by reducing intake gradually over a week or so. For optimal results, try to avoid all stimulants, including caffeine, for another week after reducing.
I recommend cycling caffeine and other more common stimulants rather than feeling like you have to upgrade to a more powerful compound that is less understood and potentially more risky.
Fat Burning Effects
One of the more coveted effects of stimulants is of course the fat burning effects. It’s the reason drugs like phentermine and clenbuterol have gained so much interest, and still do.
People of all shapes and sizes, from weight obsessed models, to obese men and women, and bodybuilders have used these drugs to burn body fat and suppress appetite.
Phentermine is still available in most countries to be prescribed by doctors if they feel their patient’s obesity is more of a concern than the potential side effects.
Clenbuterol is available under prescription in some parts of the world but it is not approved for human use in the US and most western countries.
People using phentermine can dramatically reduce their calorie and it has been one of the more successful drugs considering it was first introduced as a commercial drug in the late ‘50s.
Like other amphetamine type drugs, phentermine can act via alpha-2 and D1 (dopamine) receptors to exert its cognitive enhancing effects, which is also how it reduces appetite.
Dopaminergic stimulants are interesting because they can mess with your perception of reward and gratification, which may ultimately lead to addiction of the drug itself, but can act as a partial replacement for the previous addictive relationship with food.
Much like the psychotropic effects, the fat burning effects will dull over time with habitual exposure to stimulants.
Again, to remedy this, it is best to cycle the compound to break the tolerance level back to its default state or set point.
Unregulated Stimulants in an Unregulated Industry
The main difference between the most powerful stimulants added to commercial supplements and the stimulants that are either banned, or classified as controlled substances and only available through prescription, is knowledge.
We know a hell of a lot more about the banned/controlled stimulants than we do about the latest thing coming out of some unregulated lab in the back end of nowhere, USA.
It comes back to the drug agencies being ill-equipped to deal with the situation. And by the time they get some kind of handle on it, several hundred thousand bottles or tubs containing the stuff have already been sold.
There are several potent stimulants in commercial circulation as I write this article.
Here’s a few:
- DMHA – aka Dimethylhexylamine, Octodrine, Juglans Regia, 2-aminoisoheptane, 2-amino-5-methylheptane / ~6-methylheptane
- Eria Jarensis – aka Dimethylphenthylamine, or, N-Phenethyl Dimethylamine
Like I said…somewhere…I’m not against stimulants. When they are used correctly – i.e. cycled and responsibly dosed – they can be incredibly useful.
The problem is that many companies make poor products, especially fat burners and pre-workouts, that are just a collection of stimulants with zero/under-dosed additional ingredients that seem like an afterthought.
Quality pre-workout supplements should be packed with nutritional ingredients, ergogenic and nootropic compounds that help get the best performance from your muscles and mind.
Stimulants should be a helpful addition, not the core inclusion that the whole product is designed around.
Closing Points and Recommendations for Stimulants
Central Nervous System (CNS) stimulants, Sympathomimetic amines and drugs, Adrenergic Agonists…they are all members of the stimulant family as a whole.
Different types have different effects, and those effects have knock on effects. Side effects are more common as the potency of the stimulant increases.
Here are some important points to bear in mind when you’re using stimulants:
- What works for someone else might not work so well for you, and vice-versa.
- Introduce new stimulant compounds to your system in graduated steps. Don’t take the maximum dose on Day 1.
- Stimulants have greater effect when your tolerance is low. Ironically it’s also when they can cause the most side effects. Again, quarter/half dose first, then assess.
- That said, you should cycle stimulants and get repeated use out of the more common ones like caffeine and synephrine rather than jumping up to the next level because their effects have dulled from your habitual use. Trying to overpower tolerance is a fool’s game.
- Don’t pair a powerful stimulant with a high intensity workout. You might feel like you have a greater capacity but remember that your heart and brain are already working harder from the stimulant’s effects.
- If you take prescription medication, some stimulants can interfere with them and cause problems. Check with your doctor if this applies to you.
- Same goes if you have a medical condition, including but not limited to anything related to heart, blood pressure, metabolism, anxiety and panic disorders.
- Some stimulants can mess with a biological “safety switch” that allows you to push past a limit of physical exertion that you otherwise could not. These tend to be those compounds in the banned/illegal category (like amphetamines), but it’s best to be aware. If you are murdering you PRs one day and it seems to align with taking a new product, think about backing off a bit. Those natural trip circuits are there so you don’t overheat and burn your brain out.
Perhaps the best piece of common-sense I can try and impart is this: always think whether it is necessary to even take a stimulant for the workout or day ahead.
I tend to have both a stimulant-based and a stim-free pre-workout supplement in the cupboard. If you are feeling good before going to the gym, the stim-free product will be just fine.
Also, many companies are manufacturing products without stimulants so that you can add them if you wish.
It means you can enjoy a coffee in the morning, without overdoing it by taking a high-stim pre-workout on top of it (because you shouldn’t be consuming other sources of caffeine/stimulants as well).
Save the stims for when feel they will actually help you out. For me, it’s mostly a mental thing, I rarely need them for physical energy.
Finally, I’ll reiterate my belief that no-body really needs to use anything stronger than caffeine. Cycle caffeine correctly and it’s a very useful, very safe, highly proven stimulant.