Ever since Mark McGwire publicly announced his use of androstenedione, sales of this unregulated over-the-counter drug have skyrocketed. It has been touted as both a performance and recovery enhancer, and is being used by many athletes in many different sports. Anytime there is this much hype surrounding a purported performance-enhancing chemical, great caution is advised.

What is it?

Performance enhancing steroids are evaluated in terms of anabolic and androgenic effects. Anabolic means, "to build up", and androgenic refers to masculinizing effects. All of the biochemicals, natural and artificial, in this class of compounds have both anabolic and androgenic activity. It pays to keep this in mind when discussing anabolic steroids because the androgenic properties account for most of the side effects (more on this later).

Androstenedione is a naturally occurring androgenic steroid that is produced by the adrenal glands, ovaries, and testicles. Once released into the blood it is rapidly converted into testosterone, but there are also pathways through which androstenedione is converted into estrogen.
Metabolic Pathway of Androstenedione.

Note the obvious structural similarity between the two molecules

The sordid tale of androstenedione in sports starts in the 1970’s in former East Germany. Scientists there were the first to produce, and apply, the chemical. Exogenously administered androstenedione only has a short half-life; East German athletes snorted it as a nose spray an hour before competition (this was a team requirement in the 1988 Olympics). Taken this way it results in a rapid rise in testosterone, which lasts 1 – 3 hours. This was thought to aid performance although the exact effects aren’t known. Despite the fall of the East German regime, much of the compiled data of what they did to their athletes remains hidden. Hopefully, we now know enough not to repeat that dark chapter. (Although to witness the embarrassment of the 1998 ‘Tour de Farce’ (France) due to widespread use of erythropoietin, it appears not.)

Performance Enhancement.
The combination of anabolic steroids, when administered to cause levels higher than normally found in the body, and strength training results in an increase in muscle size, strength, and fat free mass. Further effects are increased red blood cell mass, improved mood/aggression, and blunting of the catabolic effect of heavy training. These latter effects may enable endurance athletes to train harder while minimizing overtraining. Whether androstenedione use yields these performance enhancing effects, though, is yet to be directly determined.

Sounds too good to be harmless, right?
Undoubtedly a more important question than whether or not androstenedione is an effective performance enhancer, is the issue of safety. Because androstenedione is an androgen, toxicity is best discussed by reviewing the known harmful effects of other androgens.

Commonly seen side effects due to excess androgens are,

  • Acne
  • Liver abnormalities
  • Lowering of the HDL/LDL cholesterol ratio, thus increasing the risk for atherosclerotic disease.
  • Testicular atrophy ("Honey, I shrunk the testicles"), and subsequent infertility.
  • Hirsuitism and other masculinizing effects in women.
  • Adolescents: Premature closure of the growth plates in bone resulting in shorter adult stature.
  • Breast enlargement in men.
  • Mood changes.

Less common or potential adverse effects,
1. Liver tumors – both benign and malignant
2. Leukemia / lymphoma
3. Psychiatric reactions
4. Other cancers

Adverse reactions to any substance can be viewed in terms of how long it takes for a given side effect to develop. Androgens have immediate effects (e.g., acne), but some of the more serious ones (e.g. heart disease) take years to develop. In general, the longer it takes for something bad to happen the less the concern. Adolescents and young adults are especially vulnerable to anabolic steroid abuse because of peer pressure, body image, and competition concerns. Disturbingly, there is distancing from the concept of mortality in this group (the "It can’t happen to me" phenomenon).

The bottom line on safety of androstenedione is that there are no long-term studies available. However, since androstenedione is an androgenic steroid, it is very likely that we will discover that it is harmful. Add to this the lack of applied quality standards for manufacturing, variations in dosage, and combination with other substances, and it is obvious that there is potential for widespread harm.

To further fuel the controversy are regulatory inconsistencies by various sports organizations. For example the IOC, NCAA and NFL ban the use of androstenedione, whereas Major League Baseball, the National Basketball Association, and the National Hockey League do not. In the future look for tighter regulation of androstenedione. In the meantime avoid this stuff like the plague.

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