Although there may be a world-wide energy crisis, no such problem exists in the bodybuilding world. One reason is the existence of a relatively new category of sports supplements known collectively as “preworkout supplements,” which consist of various ingredients, including amino acids, protein, herbs touted for their ability to boost energy, small amounts of carbohydrate and, in some cases, creatine and beta-alanine. More recent preworkout supplement formulas have focused on boosting the synthesis of nitric oxide.
Ostensibly, the rationale behind boosting NO involves increasing muscle pump as well as the delivery of oxygen and nutrients to working muscle. NO is capable of doing that because, among other actions, it provides a rapid dilation of blood vessels. In the supplements that feature an increase in NO, the effect involves arginine, which is the immediate nutritional precursor of nitric oxide that is synthesized in the lining, or endothelium, of blood vessels by way of the nitric oxide synthase enzyme.
Most of the NO supplements available also include the energy substances and nutrients mentioned above, with the goal of increasing energy, endurance, strength and workout efficiency. The use of arginine as an NO booster is questionable, however. Most studies that have examined various arginine-based NO supplements have found no signs that they accomplish that goal.
That isn’t surprising when you consider that studies showing an increase of NO with arginine involved providing the amino acid in 18-gram doses intravenously. Oral arginine isn’t effective for NO synthesis in the doses usually supplied in supplements, which average four grams.
Nonetheless, users of such supplements have often reported a pronounced increase in subjective feelings of muscle pump after taking them prior to a workout. Most of the NO supplements also provide quick-acting carb sources, which promote the release of insulin. It turns out that insulin itself potently boosts NO release, which dilates the blood vessels. Thus, the pump is produced not from the arginine in the supplements but rather through the release of insulin from the carbs and the subsequent release of NO.
There is an exception to this rule, however. In people afflicted with various ailments, including atherosclerosis (which damages the endothelium, where NO is produced), high blood cholesterol, high blood pressure, diabetes, kidney failure and elevated homocysteine (a metabolite of the essential amino acid methionine) and in those who smoke or are aged, a bizarro form of arginine called asymmetric dimethylarginine increases in the body. ADMA looks like arginine but provides none of its benefits. Even worse, it can stand in for arginine and block the production of NO. The cure for that problem is to provide greater amounts of arginine. In people who have an imbalance between arginine and ADMA, taking supplemental arginine will boost NO effectively. Since anabolic steroid users often have elevated blood homocysteine, as well as higher blood pressure, taking NO supplements based on arginine would work well for them.
An even better approach would be to provide another amino acid called citrulline to the NO supplements. Some newer forms of NO supplements have done just that. The advantage of citrulline is that, unlike arginine, it isn’t subject to premature breakdown in the liver and intestine. In the kidneys ingested citrulline is converted back into arginine, which can then be directly converted into NO. While many say that the amino acid glutamine is “worthless” for bodybuilding purposes, they don’t seem to be aware that glutamine can be converted into citrulline. A good food source of citrulline is watermelon.
There is a difference between pre-workout formulas and various energy drinks, although many of their ingredients do overlap. The primary purpose of energy drinks is just that: to provide a rapid boost in feelings of energy and focus. They are not designed to do what the preworkout supplements do, such as providing not only energy but also an anabolic effect that spares muscle tissue during intense training and speeding the time to recovery following a workout.
The first preworkout supplement targeted to those engaged in weight-training was called Ultimate Orange. It was designed in 1982 by Dan Duchaine and Mike Zumpano. The two had co-written the notorious Underground Steroid Handbook the year before. An apocryphal story is that the first batch of Ultimate Orange was made in a bathtub. What is known is that it was originally distributed at Gold’s Gym in Venice in unmarked bags. Prospective users were told that it would boost workout training efficiency dramatically, and it seemed to do just that.
Zumpano went on to form the Champion Nutrition company, while Duchaine became known as the “steroid guru,” although he preferred to be called a “human performance theorist.” Besides popularizing Ultimate Orange, Dan is also credited with bringing whey protein to the market, as well as, in 1990, helping some pro bodybuilders pass the only drug test ever administered at the Mr. Olympia. He died from complications of kidney disease at age 47 in 2000.
The original Ultimate Orange was introduced to the commercial market in 1992 and discontinued in 2001.
The question remains, however: Will such preworkout supplements help those engaged in bodybuilding workouts? Several studies have examined that issue, using various commercial preworkout formulas. A 2008 study provided a preworkout supplement to a group of recreational weight trainers. The results? Men using the actual supplement, rather than a placebo, were able to increase the number of reps they did during their workouts. More important, they also showed significant increases in two anabolic hormones, growth hormone and insulin.
In the majority of preworkout supplements caffeine seems to be the major ingredient. Caffeine is known to delay fatigue and increase training time to exhaustion through several mechanisms, including the antagonism of adenosine, a substance that when produced in the brain leads to feelings of fatigue. Caffeine also enhances the release of norepinephrine, which boosts fat oxidation. That spares the body’s limited stores of glycogen, which is stored carbohydrate in muscle that serves as the primary fuel source for anaerobic exercise like bodybuilding training.
Caffeine may also enhance muscle contraction by promoting accelerated mobilization of intracellular calcium in a portion of the muscle called the sarcoplasmic reticulum. In 2010 an analysis of studies related to using caffeine prior to exercise showed that it significantly improved training efficiency in six of 11 studies. Another study published a year later found that an energy drink containing caffeine boosted resistance training to failure.
Recently, 12 men participated in a three-week study in which they used a commercial preworkout supplement that contained B-vitamins, amino acids, creatine and beta-alanine, as well as various energy herbs.1 The supplement in fact provided six grams of BCAAs, five grams of creatine, four grams of beta-alanine, 1.5 grams of citrulline, and 300 milligrams of caffeine per serving. The results showed that drinking the supplement 20 minutes before training significantly improved lower-body endurance while increasing perceived energy and reducing subjective fatigue.
Another recent study involved giving a similar preworkout supplement to eight resistance-trained men.2 They drank either the actual supplement or a placebo 10 minutes prior to training and then did four sets of either barbell bench presses or squats using 80 percent of their maximum weight. Once again, those who used the genuine supplement completed more reps than those in the placebo group. They also showed greater peak power and performance through all four sets, although subjective feelings of energy didn’t differ between those who got the actual drink and those who got the placebo.
The most recent ingredient contained in preworkout supplements is DMAA, or 1,3 dimethylamylamine. A study published in an obscure Chinese journal showed that DMAA was found naturally in germanium oil. It was originally used as a decongestant drug back in 1944 but later discontinued. DMAA is controversial because several analytical studies have examined germanium oil but have not found any naturally occurring DMAA. That indicates that DMAA is added to supplements, which would make it illegal. Recently, some soldiers were said to have suffered strokes after using supplements that included DMAA.
The companies selling DMAA supplements claim that it does occur naturally in germanium and is about as safe as a strong cup of coffee—or, more precisely, several cups of coffee. Similarly to caffeine, DMAA appears to promote a significant release of norepinephrine, which would boost fat use during exercise, as well as subjective feelings of energy. As of this writing, the future of DMAA is unclear. —Jerry Brainum
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1 Spradley, B.D., et al. (2012). Ingesting a preworkout supplement containing caffeine, B-vitamins, amino acids, creatine, and beta-alanine before exercise delays fatigue while improving reaction time and muscular endurance. Nut Metabol. 9:28.
2 Gonzalez, A., et al. (2011). Effect of a preworkout energy supplement on acute multijoint resistance exercise. J Sports Sci Med. 10:261-66.