Clenbuterol, GH, and Sodium Depletion
The reigning king in this category is clenbuterol. The downside to clenbuterol is that it rapidly loses effectiveness due to receptor downregulation, necessitating a near day-to-day cycling of the drug.12 Further, side effects including tremor, nervousness, irregular heartbeat, and other conditions may emerge at the dose required for significant effect.13 Surprisingly, there has not been much in the way of novel agents in this drug category, with the exception of formoterolol, which does not have sufficient reported experience to comment upon, relative to illicit fat-loss use.
Still rooted in the early years of the prior century, one comes across the story of 2,4-dinitrophenol (DNP) as a weight-loss drug.14 According to reports, workers exposed to DNP dust in munitions factories, pesticide manufacturing, etc., were experiencing weight loss, easy fatigue, fever, and death.15 It was discovered that this chemical is capable of easily traversing the membrane barrier of the mitochondria (the part of a cell where energy in the form of ATP is produced), uncoupling calorie burning from energy production.16 In very small, measured doses, DNP can accelerate fat loss by ramping up calorie burning by 30 percent or greater (resting energy expenditure), but at the cost of generating a tremendous heat burden and oxidative damage.
Forewarned of the historical risk associated with this chemical and the recent deaths in young adults using the drug for bodybuilding or weight-loss purposes, many professionals are still using DNP from time to time.17 It is relatively easy to spot the chronic DNP user, with characteristic breath and a yellowish tinge to the complexion that is different from the yellowing caused by jaundice.
Human growth hormone (GH) was originally viewed as an anabolic drug, due in part to its role in the growth and development of children, and its defining name. However, as most professionals of the mid-to-late 1980s to mid-1990s learned, at anabolic concentrations in adults, it causes a variety of disfiguring and potentially harmful side effects. However, and fortunately for aging adults, at a lower dose (2-3 IU/day), GH can still provide significant fat-loss effect and aid in soft tissue recovery.18 The fat-loss effect of GH occurs at the level of the fat cell, but care needs to be taken— as exceeding the marginal dose can induce insulin resistance/glucose intolerance (pre-diabetes), and stimulates the liver to pump glucose into the bloodstream.
There is a little-explored path in the fat cell that involves cortisol and estrogen. Two enzymes are present in the fat cell, 11beta-HSD and aromatase. 11beta-HSD activates cortisol in fat cells. High intracellular cortisol levels increase the conversion of testosterone to estradiol (estrogen).19 By using aromatase inhibitors, bodybuilders reduce the fat storage-promoting increase of estrogen, secondary to supraphysiologic anabolic steroid use. The primitive drug, Cytadren (aminoglutethimide), was originally used by bodybuilders to lower cortisol levels, but aminoglutethimide is a non-specific drug that blocks production of several steroid hormones, including estrogen.20
Fat cells are derived from the same precursor cells as muscle. It may not surprise some to learn that androgenic anabolic steroids divert these precursor cells from becoming fat cells to skeletal muscle differentiation.21 Some might think it would require a particularly potent steroid, such as trenbolone or oxymetholone, but the effect is seen with elevated testosterone concentration. There are no reports of bodybuilders using other drugs to alter the balance of precursor cell differentiation, perhaps due to the ability of bodybuilders to achieve near-absolute ‘leanness.’
It is important to acknowledge the role of diuretics in bodybuilding. Bodybuilders utilize carbohydrate depletion-loading to increase intracellular water, along with synthol or related site-enhancement drugs. Sodium depletion, drinking distilled water, etc., are tools of the drug-free athlete. For the top pros, the more predictable and potent powers of diuretics are used. The ‘big daddy’ is Bumex (bumetanide), but many use spironolactone in conjunction, to preserve potassium.22 The risk involved with diuretics is serious, and likely account for some of the episodes of relentless cramping and heart palpitations that have been witnessed. Diuretics may also have played a role in the competition-associated deaths that have occurred in professional bodybuilding.23
The Pinnacle of Fat Loss?
Bodybuilders have reached the pinnacle of fat loss— for the most part. Timed correctly, the top amateur and professional competitors can present themselves with such low levels of subcutaneous body fat that cross-striations and vascularity are evident from 10 rows back— even at rest. This success keeps the demand for more potent fat-reducing techniques low. Thus, there are no reliable reports of bodybuilders seeking out anti-sense therapy, or even mesotherapy to gain an advantage. It is possible that someone has sought out some exotic therapy or surgical technique, but for the most part, bodybuilders are much more interested in experimenting with anabolic drugs/biologics— as any additional competitive advantage in fat loss would be minimal.
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