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Bodybuilding Pharmacology: Contamination Investigation

Androstenedione pro-hormone supplements shown to be contaminated with nandrolone and do smart drugs and nutrients really help?

In a previous column I discussed a study in which androstenedione pro-hormone supplements were shown to be contaminated with nandrolone metabolites in a concentration high enough to lead to positive drug tests for nandrolone.1 Nandrolone is banned by every athletic federation in the world. During the past two years many athletes who claim not to have used any form of anabolic steroids or pro-hormone supplements have tested positive for nandrolone. The usual explanation for such results is that the athletes innocently used nutritional supplements, such as creatine, that were contaminated with nandrolone. How the supplements became contaminated is anyone’s guess, but it’s usually attributed to poor quality control on the part of the supplement manufacturer. The question is whether many supplements that aren’t supposed to contain pro-hormones actually do, or whether athletes are surreptitiously using anabolic steroids and blaming positive drug tests on contaminated food supplements.

Recent studies that have analyzed several types of popular supplements indicate that contamination is a definite problem. In one recent study Swiss researchers purchased 75 products’69 of which were American in origin’over the Internet and from Swiss supplement distributors.2 The objective of the study was to see if the supplements contained any ingredients not listed on the label or in amounts not in accordance with the content listed. Their analysis showed that out of 17 pro-hormone supplements tested, seven contained substances not indicated on labels. One pro-hormone product, listed as containing two basic 19-nor pro-hormones, also contained 15 percent androstenediol, or 4-AD. Another pro-hormone that listed 200 milligrams of 4-AD also contained trace levels of testosterone. A supplement that listed 5-AD (another pro-hormone) at 99.3 percent purity was 2 percent off’the missing 2 percent consisting of testosterone. Still another 19-nor combo supplement contained 8 percent testosterone, while another pro-hormone touted as containing DHEA didn’t have any of that androgen precursor at all. A product labeled as containing 100 milligrams of 19-nor pro-hormone didn’t contain any but did contain androstenedione. Finally, a supplement sold as a ‘mental enhancer’ contained far more ephedrine than was listed on the label.

In another recent study Belgian scientists gave a popular American ‘fat-burning’ supplement to five subjects who later underwent drug and urine testing.3 The supplement label listed a mixture of herbs, amino acids and other nutrients, none of which could lead to a positive drug test. Analysis of the supplement, however, revealed the presence of two pro-hormones, 19-nor dione and 4-AD. The actual amounts of those pro-hormones were relatively small, less than a direct pro-hormone supplement would contain’pointing to probable supplement contamination. More problematic was the fact that subjects who took the suggested daily dose of seven tablets showed levels of nandrolone metabolites high enough to lead to a positive drug test within 48 to 144 hours of ingestion.

Those studies show that in many cases athletes may be telling the truth about not knowingly using anabolic steroids or direct pro-hormone supplements. They also point to a problem of quality control in the manufacture of some food supplements. It could involve an innocent mistake, such as mixing one type of food supplement in a machine that was used to produce pro-hormone supplements. Mislabeling a supplement, however, is inexcusable and makes one wonder about the motives of companies that engage in such practices.

According to an article in the September 20, 2001, edition of the Los Angeles Times, an International Olympic Committee initial analysis of 600 food supplements purchased around the world showed that of the first 200 products tested, 15 to 20 percent contained nandrolone or ephedrine in amounts high enough to lead to positive doping tests. The article also noted that Olympic officials refused to recognize an ‘International Bodybuilding Federation,’ which effectively quashes any chance of bodybuilding events appearing in the Olympics for the foreseeable future. Ballroom dancing and tug-of-war events, however, are likely to be added to the Olympic venue.

Smart Drugs and Nutrients: Do They Help?

Smart drugs, as the name implies, are drugs reputed to increase brain power or intelligence, as well as foster mental focus and clarity. Those last two attributes have made them popular for athletic-training purposes, and they were used extensively by Russian and East German athletes during the period of their nations’ world athletic dominance. A number of nutrients are also said to produce similar effects.

The drug versions are often collectively referred to as nootropics, and most are thought to work by improving either the production or the activity of various brain neurotransmitters. Neurotransmitters are chemicals synthesized in the brain that transmit nerve signals. Many are produced from nutrients, including amino acids and vitaminlike substances. Examples include serotonin, which is produced from the amino acid L-tryptophan, and L-tyrosine, the primary building block for norepinephrine and dopamine, two other brain neurotransmitters. Choline, a vitaminlike compound, is the raw material used for the synthesis of acetylcholine in the brain. Sometimes amino acids themselves act as neurotransmitters; for example, glycine is considered a major inhibitory brain neurotransmitter due to its ability to slow down nerve transmission, while glutamate has the opposite effect of stimulating neuronal activity in the brain.

The idea behind smart drugs and nutrients is that if you provide either a drug or a building-block nutrient, the brain will then increase the level and activity of various neurotransmitters, which increases brain efficiency. That hypothesis has been accepted by many people, and a number of books detailing various smart drugs are available. Most of those drugs have not been approved for sale in the United States and must be obtained from international sources, such as those found on Web sites. Acquiring such drugs often involves sending cash to a foreign post office box, which is a gamble itself.

The obvious question is why such smart drugs aren’t approved for sale in the United States. Books that discuss smart drugs usually list a number of references and testimonials as proof of the drugs’ effectiveness. But a closer examination of such studies reveals that they either involved lab animals, such as mice or rats, or used as subjects people with existing brain diseases, such as Alzheimer’s or Parkinson’s, both of which involve deficiencies of brain neurotransmitters.

The problem is that giving a specific drug to a mouse and then having the mouse do a task like finding its way out of a maze does not easily translate into an increase in human intelligence or thinking power. Providing smart drugs to people with brain diseases involves dispensing a substance that does increase the level of brain neurotransmitters deficient as a result of the disease. On the other hand, in a normal brain the synthesis of brain neurotransmitters isn’t hindered by any structural pathology and is tightly regulated by enzymes and other systems.

Taking a drug touted to increase acetylcholine, a neurotransmitter associated with thinking and intelligence, won’t necessarily increase the level of acetylcholine in the brain. A notable example of that is the nutrient choline, the primary precursor for acetylcholine synthesis. Choline doesn’t easily pass into the brain because of a formidable network of blood vessels and other structures meant to protect the brain that’s known as the brain-blood barrier. Thus, taking choline, even in huge doses, may not even get to the site of activity in the brain.

Nutrients that have been promoted for bodybuilding purposes, also commonly referred to as smart nutrients, are L-acetyl carnitine (ALCAR) and phosphatidylserine (PS). ALCAR does enter the brain more easily than straight L-carnitine, and there is some evidence that in the brain it increases the level of both acetylcholine and dopamine production. But it would do so only if levels of those brain chemicals were low. If you were already producing optimal levels of acetylcholine and dopamine, the acetyl carnitine would do little or nothing in that respect.

Phosphatidylserine (PS) is likewise thought to increase brain acetylcholine levels. If that’s true, it would likely increase mental focus and concentration. PS is also needed as a building block for membranes that line nerve cells and, by maintaining neural membrane fluidity, may improve the quality of brain nerve transmission, or communication.

PS may also dampen the effects of cortisol in the brain. Cortisol, a hormone produced in the adrenal gland cortex, is most familiar to bodybuilders because of its potent catabolic effects in muscle. In the brain excess levels of cortisol produced as a result of long-term stress selectively destroy neurons in the areas associated with memory and intelligence. In fact, one current theory among researchers is that memory deficits commonly seen with age may accrue from the long-term effects of cortisol flooding in selective brain areas. While we cannot escape the effects of stress, anything such as PS that may blunt cortisol in the brain may slow brain aging.

An herb called ginkgo biloba is also considered a smart herb because of its effects in the brain. While ginkgo mainly works by increasing blood circulation in the brain, which in turn increases brain oxygen delivery and metabolism, some studies show that it may also blunt cortisol effects in the brain. Additionally, ginkgo provides antioxidant activity, a notable effect, since the brain consists of primarily unsaturated fat subject to oxidation effects that are linked to many degenerative diseases, including Alzheimer’s and Parkinson’s.

Research on ginkgo shows that it may offer more benefit to older people, many of whom suffer from decreased brain circulation due to diseases such as atherosclerosis, which can affect brain blood vessels. A few studies, however, show that taking loading doses, or doses considerably higher than the 120 milligrams daily usually suggested for the herb, may temporarily increase brain efficiency and focus even in younger people who do not have brain pathologies.

A lesser known herbal substance popular in Ayurvedic practice, an ancient Hindu medical and health system, is Bocopa monniera, or brahmi. It has been used for centuries in India and other countries to treat a variety of ills, but more recently it has been touted as a natural brain-enhancing substance. While much research examining this intelligence-promoting aspect of brahmi has involved rat studies, a recently published study featured 46 healthy human subjects (11 men, 35 women), with ages ranging from 18 to 60, who took 300 milligrams a day of a commercially available brahmi supplement.4

Some of the subjects instead took a placebo, since the study involved a double-blind, placebo-controlled protocol, meaning that neither the subjects nor the researchers knew who was getting the active substance. The results showed an improvement in learning and memory functions after 12 weeks in those taking the genuine supplement. The mechanism is thought to involve upgraded acetylcholine activity in the brain, coupled with antioxidant properties of the herb. Guggul, another natural substance popular among bodybuilders, is also derived from Ayurvedic medicine.

Anyone can use increased brain power in these troubled times, since most of the problems facing society stem from sheer stupidity. While the idea of nootropic, or smart, drugs is attractive, the reality is that most of them have little or no solid research to show that they produce intelligence-increasing effects in people with normal brain function. They may not even work in idiots, since, as noted, the synthesis of brain chemicals is tightly regulated. The best current advice for those seeking to maximize brain efficiency is to stay healthy through proper, balanced nutrition and exercise. The exercise should include something that challenges the brain, such as reading, playing chess, mastering difficult puzzles or learning a new skill. The brain, like muscles, responds to exercise or stimulation.


1 Catlin, D.H., et al. (2000). Trace contamination of over-the-counter androstenedione and positive urine tests for nandrolone matabolite. JAMA. 284:2618-2621.

2 Kamber, M., et al. (2001). Nutritional supplements as a source for positive doping cases? Int J Sports Nutr Metabol. 11:258-63.

3 De Cock, K.J., et al. (2001). Detection and determination of anabolic steroids in nutritional supplements. J Pharmceut Biomed Anal. 25:843-852.

4 Stough, C., et al. (2001). The chronic effects of an extract of Bacopa monniera (Brahmi) on cognitive function in healthy human subjects. Psychopharmacology. 156:481-484.

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