In other countries, it has been documented that virtually all types of androgen preparations whether for human use or veterinary purposes have been abused by athletes. The esters used for physiologic replacement (enanthate & cypionate) are injected in supraphysiologic doses up to 6x the recommended replacement dose to increase muscle mass and strength especially in body building and this has been proven also to increase fat free mass in adult males, especially when coupled with exercise. Synthetic androgens (stanozol) and derivatives (nandrolone) are classically referred to as the “anabolic” steroid because they supposedly have greater anabolic than androgenic effect than testosterone on the androgen receptor, but the existence of such novel properties in a compound remains unproven. The androgen precursors androstenedione and dehydroepiandrosterone are available as over the-counter nutritional supplements that have been widely endorsed by body-building magazines for increased muscle strength. Whereas a few small trials using these precursors showed variable increase in testosterone level, binding or levels of metabolites- the true increase in muscle strength and muscle mass remain unseen.

In patients who abuse androgens, what should we look for as adverse reaction/s? Adverse effects of androgen use include suppression of endogenous testicular function, gynecomastia, erythrocytosis due to stimulated erythropoiesis, hepatotoxicity (with stanozol), psychological disorders including mood disorders and aggressive behavior, decreased serum HDL and increased LDL (especially with stanozol), coagulation activation, premature epiphyseal fusion (in adolescents), infections, and virilization (in women).

It is hard to detect androgen use. The conventional method used is the urinary ratio of testosterone glucuronide to its endogenous epimer, epitestosterone glucuronide (T/E ratio). Normally, the T/E ratio is 1 to 3:1; a T/E ratio of >4:1 is considered evidence of doping by the World Anti-Doping Agency (WADA). However, the T/E ratio is limited by significant variability, due to genetically determined differences in the ability to convert testosterone to testosterone glucuronide. The method currently considered most accurate is determination of the ratio of carbon 13 (13C) to carbon 12 (12C) in urinary metabolites of testosterone. The rationale is that pharmacologic testosterone preparations are synthesized from plant sterols, which have a lower ratio of 13C to 12C than does endogenous testosterone. This method will show a low 13C to 12C ratio even if an athlete takes epitestosterone to attempt to mask taking testosterone.

Athletes and the covert industries that supply them with androgens are ever attempting ways to avoid detection. The most common way is to discontinue the drug before the testing occurs. Another way is for a laboratory to synthesize an androgenic steroid specifically designed to avoid detection (e.g. tetrahydrogestrinone).

As power of super athletes translate into millions of dollars in earnings, it seems that this new and more complex form of steroid abuse will pose problems to endocrinologists…And our true “intellectual” power will continue to be tested by our beloved but challenging field.

References:

Snyder, Peter Use of Androgens and other Performing Enhancing drugs by athletes. UpToDate. 2010
Leder, BZ, Longcope, C, Catlin, DH, et al. Oral androstenedione administration and serum testosterone concentrations in young men. JAMA 2000; 283:779.
Bhasin, S, Storer, TW, Berman, N, et al. The effects of supraphysiologic doses of testosterone on muscle size and strength in normal men . N Engl J Med 1996; 335:1.