Coming Clean on Getting Lean

Two traits differentiate elite bodybuilders from most other athletes- extreme muscle hypertrophy and absolute minimal body fat. Developing the physique has been honed to a science over the decades, as bodybuilders have discovered through trial and error the most effective diet programs, training regimens and drug protocols to maximize the fruits of their labors.

     There is no denying the obvious, elite bodybuilders are lean- very, very lean. The slang terms used to describe how lean they become allude to how low their body fat drops: peeled, shredded, ripped and cut. Standing next to a bodybuilder in competitive form, you almost wonder aloud how his skin keeps from tearing open; it is so thin. The road to becoming this lean is based upon a foundation of strict eating habits and disciplined training, but the final results are heavily dependent upon the use of potent lipolytic drugs.

Lipolysis is a term describing the breakdown and release of stored body fat. Fat is stored in fat cells called adipocytes, which either store or release fat depending upon the balance of hormones and neurotransmitters acting on the cell surface.1,2 Bodybuilders may not understand the complex dance of hormones, receptors and enzymes, but they have learned how to successfully manipulate the biochemical environment to maximize fat loss. There are seven basic categories of drugs used by bodybuilders for cutting up (fat loss). Despite being based upon renegade use by gonzo chemists, there is solid scientific evidence supporting these favored lipolytic drugs, listed below.

     It's difficult to assign any primacy to the list of drugs, as each provides demonstrable effects. All of these drugs have been used clinically, though none are currently approved for treating obesity, with the exception of certain members of the stimulant class.
    
Stimulants Increase Calorie Burning
Stimulants include drugs that act like the "fight or flight" hormone adrenalin, as well as the neurotransmitter norepinephrine. Adrenalin is well known for increasing the heart rate, making hands shaky and alerting the senses during times of fear or excitement. Norepinephrine is a neurotransmitter chemical, released by tiny nerve endings to excite muscle cells to contract more powerfully and fat cells to release stored fat. Primitive cultures have used plants with stimulant properties for centuries, with modern processing leading to the commonly abused drugs cocaine and methamphetamine.

     Cocaine, methamphetamine and related drugs (sibutramine, phentermine) stimulate a variety of different types of receptors, beyond the specific receptors that bind to norepinephrine and adrenalin. The cumulative effect is hyperactivity, sleeplessness, decreased appetite and increased release of stored fat from adipocytes. The fat loss experienced by users of non-specific stimulants arises from increased calorie burning due to thermogenesis (higher body temperature) and increased movement (due to agitation and hyperactivity), decreased calorie intake (reduced appetite) and the direct action of the drugs on the fat cell releasing stored fat (lipolysis).3 A small degree of weight loss is also due to the diuretic effect stimulants have on the kidneys.4

Bodybuilders have long used stimulants, not only for their fat loss properties, but because they also increase exercise tolerance and delay fatigue. Stimulants fit well into the "work hard, play hard" mentality of many young people. Numerous articles have been written confirming the fat loss potential of phentermine, sibutramine and ephedrine-caffeine combinations.3,5-7 Prior to the regulatory actions against ephedrine-containing products, they could be found in nearly every bodybuilder's gym bag.
 
      Special Mention: Clenbuterol
A more specific stimulant deserves special mention, as it has achieved singular recognition among bodybuilders. Clenbuterol is a stimulant that interacts with one class of receptor exclusively (B2- adrenoreceptors), as opposed to the non-specific stimulants that might stimulate a variety of receptors (serotonin, dopamine, A- and B-adrenergic, etc.).8 Clenbuterol is highly favored, especially by women, as it not only contributes significantly to fat loss, but also has anabolic properties.9 This combination provides the holy grail of combining fat loss and muscle building in a single pill. Clenbuterol is used in food animal production, given to cattle and chickens by ranchers in order to develop leaner and bigger carcasses.10 This results in better meat production and higher profits for the rancher. Bodybuilders find that Clenbuterol not only increases direct fat release at the level of the fat cell, it also increases thermogenesis (fat loss caused by increasing calorie burning) and uncoupling (wasting calories as heat) and it causes muscle hypertrophy.9,11

     Unfortunately, it appears the body adjusts to being forced into overdrive by Clenbuterol. The effect of Clenbuterol is dependent upon the number of available B2-adrenoreceptors. When Clenbuterol is used regularly, fewer B2-adrenoreceptors are available over time, reducing the effect.8,10,12 This has led to a number of dosing strategies to maintain Clenbuterol effectiveness over time. Bodybuilders typically use Clenbuterol for three to five days, then take a two to three day break to allow the B2-adrenorecpetors to recover to normal levels.13

    Turning Up the Thermostat
Another strategy used to increase fat loss is to ramp up the metabolism by turning up the body's thermostat. The metabolism is controlled by a complex interplay of signals, but the greatest impact is made by a small endocrine gland located just under the Adam's apple, called the thyroid gland. The thyroid gland releases two hormones called T4 and T3.14-16 T4 (available as the drug Synthroid) is the predominant form of thyroid hormone in the blood, but T3 (Cytomel) is the potent form boosting the metabolism at the cellular level. T3 increases B-adrenoreceptors, which increases and prolongs the fat loss effect of Clenbuterol and other stimulants.17,18 T3 also increases uncoupling, a process occurring at the level of the mitochondria, markedly increasing the rate at which calories are burned, even at rest. T3 is very potent, but if used in excess, it may lead to insomnia, muscle loss and agitation.19,20

T3 is not the only drug that increases the metabolic rate through mitochondrial uncoupling. An industrial chemical used in the production of explosives and as a pesticide was once used as a weight loss drug, until certain side effects were noted, including cataracts and deaths due to overdose.21-23 This chemical was reintroduced to the bodybuilding community when Dan Duchaine reported on its use, rapidly increasing demand. 2,4-dinitrophenol (DNP) is a potent oxidant that interferes with mitochondrial respiration- the process linking calorie burning with ATP (energy) production. Under the influence of DNP, calorie burning is disconnected from ATP production (uncoupled); instead, the energy is released as heat.24 Users of DNP find the practice very toxic and tend to use the drug only for short periods of time.25 Unfortunately, DNP has a very narrow margin of safety and was determined to be responsible for the death of a young bodybuilder.26 Despite its impressive fat-burning potential, DNP is not recommended by any responsible source, as it is too dangerous for unregulated use.
    
    Diuretics: Rapid Results
The diuretic effect of stimulants was mentioned briefly, which accounts for some of the weight loss seen with use of amphetamines and related drugs. Bodybuilders have long noted the improved appearance onstage when excess subcutaneous water is flushed from the system. Diuretic use is rampant in a number of sports and activities, including modeling, horse racing (jockeys), wrestling and nearly every sport with weight class restrictions. Diuretics can induce a rapid weight loss and cause the skin to tighten up against the underlying muscle. The most effective form of diuretic is the drug Lasix.27 Healthy people can tolerate a minor degree of pharmaceutical dehydration, but among the ill, or in individuals depleted from stress (including pre-competition training), diuretic abuse can cause a dangerous imbalance in electrolytes. Electrolytes include sodium and potassium, the familiar ingredients of sports drinks.

When sodium levels drop, subcutaneous water is flushed, tightening the skin. If the drop in sodium is too fast or proceeds unchecked, muscle cramping and an irregular heartbeat can develop.28 Several elite bodybuilders have had to be escorted offstage due to uncontrollable and painful cramping, preventing them from holding mandatory poses. Tragically, at least two professional athletes have succumbed to irregular heartbeats, including Andreas Munser who died in 1996. Diuretics are able to sharpen the appearance of the physique, or drop several pounds in a matter of hours, but the risks associated with the use of these drugs without proper supervision and instruction is significant.29

    The Role of Aromatase Inhibitors
The use of testosterone and other anabolic steroids is inherent at the top levels of bodybuilding, as their ability to build muscle has been clearly demonstrated. Surprisingly, anabolic steroids also appear to play a role in fat loss through a variety of mechanisms. Clinical studies have identified a relationship between testosterone levels and body fat, particularly visceral (abdominal) fat. Men suffering low testosterone levels have high body fat levels, with central adiposity- a term describing fat depositing in the abdomen.30 When treated with testosterone, body fat decreases with noteworthy benefits to cardiovascular health.31,32 This fat loss is achieved to some degree by making the fat cell more sensitive to fat loss signals and reducing the drive to store fat.33

     Testosterone is an androgen, but in certain tissues it can be converted into estrogenic (female) hormones through the aromatase reaction. Fat cells contain the aromatase enzyme complex and when estrogen levels rise, fat storage is encouraged.30 The use of non-aromatizable steroids or aromatase inhibitors may reduce tissue estrogen levels and inhibit fat storage. The advent of aromatase inhibitors allows bodybuilders to utilize a greater number of anabolic steroids without promoting fat storage.

GH: Beyond Hypertrophy
     The last major lipolytic drug used by bodybuilders is the one that has had the greatest impact on the sport in the last 20 years.34 Human Growth Hormone (GH) is released from the pituitary gland in the brain under conditions of physical stress or low blood sugar, in addition to responding to a number of releasing hormones. In adults, GH serves primarily to aid in tissue repair, maintain organ function and regulate body energy stores.35,36 GH was originally used as an anabolic aid. Bodybuilders discovered that high doses of GH could increase muscle size considerably, though strength increases are much more modest.34,37 Side effects are common at the doses used for anabolic growth.38

     Clinical studies evaluating the use of GH to treat obesity has proven that low-dose GH therapy can reduce body fat in overweight individuals.39 Bodybuilders have also discovered the fat reducing effect of low doses of GH.34 Many celebrities, physicians and wealthy persons have also turned to anti-aging practices to decrease body fat, increase muscle and tighten the skin, though this is disputed in the literature.40 Low dose GH therapy appears to be reasonably safe, as the previously noted side effects appear to be dose-related. As long as the secondary hormone IGF-1 is tracked, side effects can be minimized.

    Risk Takers: Be Aware
Public voices opine that it's appalling for drug use to be so deeply ingrained in the sport of bodybuilding. It's not surprising that bodybuilders have turned to drugs to maximize the muscle-building and fat-loss efforts of their grueling training and diet programs. Athletes have always sought a competitive edge, and as bodybuilding is a sport of extremes, the combined effects of diet, training and drugs have produced some of the most exaggerated forms ever seen onstage or off. Young people in general, and bodybuilders as a group, are risk takers. Though there are significant risks in using drugs to reduce body fat, bodybuilders will always seek the most potent and effective means of pushing their bodies to the extreme. This practice can be dangerous, but it's possible that a fat-reducing drug program may be discovered by this group of physical pioneers that could benefit the vast majority battling obesity. Due to the dangers involved, the drug use practices of elite bodybuilders should not be attempted without proper supervision; be aware, most of the drugs discussed are not approved for fat loss.

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