Dianabol: The First Widely Used Steroid Turns 50!
by Dan Gwartney, MD
The 50th anniversary is considered golden, as it represents a milestone few reach…few marriages reach their 50th due to death or divorce; most companies dissolve into bankruptcy or simply fade away; consumer products are replaced within years due to upgrades or programmed senescence. For any person or product to remain useful and desired after 50 years is a notable accomplishment.
This year marks the golden anniversary for an anabolic steroid (AAS) that is considered the gold standard for all oral AAS. The term gold standard refers to the item in a class that all others are compared to; the model of excellence. In many ways, this description correctly identifies methandrostenolone, the AAS known best by the expired trade name Dianabol or its slang derivative, Dbol.
One need harken back to the late 1950s to understand the impact Dianabol and a few other AAS made in competitive sports. Prior to the introduction of AAS, physical performance was limited by a person’s (mostly men) ability to train and recover. There was little opportunity or ability for a man to develop his strength or muscle mass much beyond what one might see in laborers. The statues crafted during the peak of the ancient cultures of Greece and Rome, or the works of Renaissance sculptors such as Michelangelo, embodied physiques as muscular as those of athletes living in the middle part of the 20th century.1
During the 1950s, as global (relative) peace dominated, sports substituted for war as the contest to prove national superiority; gifted individuals were encouraged to pursue athletic training full-time to improve the patriotic fervor of a country’s citizens. Karl Marx referred to religion as being the opiate of the people.2 This statement is interpreted to mean that the ruling parties can manipulate the masses to endure unnatural hardships and class division by distracting with the promise of future, abstract reward or conditioning them to accept suffering as a prerequisite to divine entry. The role of religion has changed greatly and many, if not most, in the U.S. do not follow the beliefs of literalists. In fact, much of America’s focus is on secular matters, rather than the divine, as the nation has enjoyed a long period of domestic tranquility.
Entertainment has replaced some of the function of religion, giving many a more concrete distraction and among the devoted, a sense of community. Consider the fervor of sports fans, sometimes spilling over to violence, as they proudly proclaim their allegiance to their chosen sports team.3 Tens of thousands of fans will gather in arenas, clad in team colors, to cheer the modern-day equivalent of gladiatorial games. With the worsening of domestic conditions, the need for a sense of belonging to something greater to bolster self-esteem grows.4 As role models in religion and politics crumble in the eyes of the public, sports idols are created who are held to standards well beyond those imposed upon our civic or moral leaders. Sexual misconduct toppled President Bill Clinton and televangelist Jim Baker from their prestigious heights; alcohol and drug abuse (prescription and illicit) are rumored to be rampant on Capitol Hill; financial mismanagement is present in every audit performed by the U.S. Government Accountability Office. Yet, it is the use of performance-enhancing drugs by athletes that is cast before the public in highly publicized hearings.5 Dianabol traces its history through the era whereby the ethics and morals of athletes became more relevant to the public than concerns over the actions and behaviors (professional and otherwise) of its elected leaders.
Clandestine Doping Programs, AAS Enter The Sports Arena
The period after World War II saw a dramatic shift in the balance of global powers. Former military powerhouses, Germany and Japan, were metaphorically castrated as Allied victors dictated terms of surrender. The Soviet Union diverted resources to establish its military position and promote communism among the war-torn nations of Eastern Europe. People of nearly every nation were traumatized by the recent devastation and the impending threat of economic collapse loomed as industry attempted to recover from the damage and demands of war. There was a strong need for national pride and the diversion of entertainment, as well as a means of proving individual or national superiority. As it had in ancient times, the Olympic Games provided an opportunity for nations to pit their greatest warriors in peaceful competition to prove superiority.6
Given the precarious state of affairs, personalities of post-war leaders, and human nature, it is little wonder that clandestine doping programs were established.7 The morally devastated country of East Germany became an Olympic powerhouse and the economically impoverished states of the USSR were home to some of the strongest men in powerlifting. Testicular extracts had been used historically to bolster courage or libido, but it was not until animal studies demonstrated that androgens extracted from urine could restore male characteristics to castrated animals that the science of AAS emerged.8 Rumors of AAS use by German soldiers during WW II to escalate troop aggression are among the earliest chapters in the story of AAS.9 It has been suggested that the AAS were actually dispensed to maintain the strength of soldiers as supply lines were interrupted and food became scarce. Ironically, AAS were later used to aid in restoring the health of prisoner-of-war camp survivors.
AAS entered the realm of sports within a decade of WW II’s end. The earliest documented report of American use came in 1956, as Dr. John Ziegler, team physician for the U.S. weightlifting team, learned of the Russian team using testosterone injections and other steroids to increase the strength of their athletes (male and female).10,11 Ziegler brought the secret of the Russian’s source of dominance back to America and the era of AAS and sports doping in the U.S. began. It was many years later that the Western world learned of East Germany’s state-sanctioned doping program.12
Ziegler worked with Ciba Pharmaceuticals, a respected drug developer/manufacturer established in 1859 and now part of Novartis, to bring Dianabol into the American market in 1958.11,13 Dianabol was marketed for a number of health conditions, but a significant part of its production was diverted into the sports market. Certainly bodybuilders and powerlifters accessed the drug as early adapters but given the niche nature of those sports, the media focused on the role of AAS in football to demonstrate the impact Dianabol had on sport.12 Unfortunately, the profile implicitly links Dianabol with the ethics and safety risks of illicit sports doping. However, the historical and sociological value of the article is significant. An addendum at the end of the article disclosed that writer Matt Chaney is the author of an upcoming book on the topic of performance-enhancing drugs, Spiral of Denial.
Ethics and safety are critical issues to address in the topic of AAS use/misuse. For a rational person, the weight of ethics, legality and safety must be considered, as they are serious disincentives. Sadly, an accurate assessment is difficult for experts, let alone laymen, as misrepresentations from advocates and antagonists have thoroughly muddied the waters. Nonetheless, many athletes and recreational lifters have chosen to use Dianabol, despite some level of awareness of the risks involved. What are the properties of Dianabol that have so firmly entrenched it in the annals of sports pharmacopeia? The short answer is simple: convenience, potency and reliability.
From the earliest days, athletes of all varieties found that just a pill or a few could prevent the breakdown and wasting associated with preseason camps or build muscle and strength well beyond what disciplined training and diet achieved.12 Dianabol could be taken in small amounts by an accomplished athlete and allow him to train longer and harder, developing his skill set without suffering any loss of lean mass or strength. A more driven athlete, seeking to increase his mass and strength, as well as aggression, accomplished these goals by taking a few more tablets. With the success seen following the directives of guiding professionals such as Dr. Ziegler, it did not take long for some individuals to exceed these recommendations and dose themselves recklessly, resulting in the emergence of adverse side effects. Fortunately, the rate of serious side effects is low but the “more is better” mentality so disgusted Dr. Ziegler that he eventually distanced himself from AAS.11-13
The figures above show the close similarity between methandrostenolone (Dianabol) and testosterone. Thus, it is not surprising that the effects of the two are likewise very similar. A close inspection shows that Dianabol has two slight but very significant differences that greatly affect the potency and action of the drug.
Dianabol is primarily delivered as a tablet, though injectable versions do exist. Certainly, most users have encountered the drug in tablet form and this was the form introduced to sportsmen in the 1950s and 1960s. To survive first pass metabolic clearance (drug deactivation that occurs in the liver and intestines before the drug enters the bloodstream or reaches target tissue, such as muscle), Dianabol incorporates two modifications that prevent enzymes from converting the drug to an inactive form. The first is an extra-double bond, present as the straight line in the first ring on the left in methandrostenolone, but absent in testosterone. This is a 1-carbon double bond and is the same modification used in recently banned prohormones such as 1-testosterone or 1-androstenedione. The second is a 17-alpha methyl group (CH3) added on the far right in methandrostenolone, but again, being absent in testosterone. The 17-methyl group is one example of AAS alpha-akylation used very commonly in oral AAS that is responsible for much of the hepatotoxicity associated with AAS use. Thus, Dianabol is a form of testosterone that is protected by two modifications from being deactivated prior to reaching muscle, making it an orally active androgen. Testosterone is not active when taken orally without these modifications.
Yet, Dianabol is not just oral testosterone. In comparing the two, supplying testosterone by injection or as methyltestosterone, Dianabol was shown to be twice as anabolic (muscle growth) relative to the amount of androgenic stimulation (prostate growth) it induced. There is still a high propensity for androgenic side effects, particularly for women. In fact, very few steroid “gurus” recommend Dianabol to women unless masculine side effects are not considered.13 Men may see prostate symptoms, accelerated hair loss, fertility problems and aggression/mood disorders.14-16 Similar to testosterone, Dianabol can be converted to a potent estrogen, giving rise to water and fat retention, possibly gynecomastia as well in some individuals.13 The “look” on Dianabol is very similar to that of testosterone esters, being size with some degree of bloat.13 Acne appears to be more common with Dianabol, but that is based upon observation and has not been empirically evaluated. Evidence of liver strain or damage (being the organ that receives the highest concentration of the drug) is frequently reported.17 Even modest users may experience elevation of liver enzymes on blood tests, a non-specific sign that the liver cell is being exposed to a toxic substance or condition.13 Notably, liver enzymes also rise with intense exercise, leading many experts to believe that the prevalence of liver toxicity has been over-reported.18 Changes in cholesterol levels and serious cardiovascular consequences have also been noted in the clinical literature.19-21 As can be seen, there are serious health considerations when contemplating Dianabol use. Readers wishing to learn more of the pharmacology of Dianabol may benefit from reading the relevant section in Anabolics 2007, written by William Llewelln
Dianabol: Will The King Be Dethroned?
Having acknowledged the convenience of an oral AAS and briefly touching on the chemistry of the drug, many people may still wonder why Dianabol continues to hold such a commanding presence in the field of AAS. Frankly speaking, it works very well. This statement is not an endorsement to use the drug, licitly or illicitly, as the risk-to-benefit ratio of any oral AAS exceeds my professional parameters. However, it is folly to deny the potency of Dianabol, a scheme government and industry groups attempted during the 1970s and 1980s, fueling the distrust most athletes have towards health professionals. Recreational users, who often abandon disciplined training and diet regimens in a matter of weeks, may see 10 percent to 50 percent increases in their strength, combined with a gain of 10-30 pounds in two months. More dedicated athletes and bodybuilders will not see such dramatic gains, beginning from a higher baseline due to their lifestyle and training practices. However, relatively modest Dianabol intake (10-30 mg/day) can increase strength significantly; higher doses will result in greater gains as all AAS generate dose-related responses, but the risks of adverse effects increases as well.13,22 Even the lowest doses hold the potential of causing health problems, so it is important to that individuals be aware of the consequences of this or any AAS use. Of course, the legal consequences arise with a single tablet, even before it is consumed.
To avoid the adverse effects of higher doses, yet still experience greater gains, many users stack Dianabol with one or more other AAS. The most popular stack for decades was Deca (nandrolone decanoate) and Dbol, as this combination provided appreciable gains at low cost. The Deca and Dbol look really defined the bodybuilding culture throughout the 1980s, a time many see as the Pinnacle of the sport. Certainly, this was not a pre-competition stack, but most users were not, and are not, competitive bodybuilders.
Later generations of bodybuilders have left the mundane avenues of Deca and Dbol, developing exaggerated physiques through the use of insulin, growth hormone, IGF-1 and prostaglandins. The future has already arrived in some, with reports of myostatin inhibitors and other research-grade biologicals being whispered among well-connected trainers, coaches and athletes. Though no evidence of such has surfaced yet, the International Olympic Committee has already begun discussing gene doping.23 Yet, even as sports doping enters into the era of gene alteration, demand on the street remains high for Dianabol. The majority of AAS users are not competitive athletes, nor do they wish to face the uncertainties and expense of exotic hormones. The purpose for most is to look and feel better, which implicitly carries with it the desire not to detract from their current or future health.24 Dianabol is generally felt to offer results in a convenient and relatively safe manner, without the need for injections (a selling point for those who are averse to needles). Dianabol will not be an option from a physician, as the risks are unnecessary and avoidable. Testosterone esters can provide similar benefits without risking liver damage, changes to blood lipids and cholesterol, and wild fluctuations in androgen concentration. Yet, one can be sure that nearly every black-market dealer can access the drug in some form. Unfortunately, the allure of Dianabol is sure to attract newcomers, some of whom may be harmed as they naively accept counterfeit or adulterated drugs from unscrupulous dealers.25
Dianabol remains the king of oral AAS. Were it not for drug testing, it likely would continue to be use widely by professional athletes. Yet, even as it stands above its chemical peers, the future is dimming for Dianabol. Interest in bodybuilding is waning, anti-doping efforts are making headway against the use of AAS by competitive athletes and teens, the economy is dropping gym membership and the advent of other AAS (topical gels, non-alkylated oral testosterone, etc.), which may be available to middle-aged or older men, will all erode the demand for the drug. If AAS had a Hall of Fame, Dianabol would certainly be inducted. But like all Hall-of-Famers, the recognition comes as it retires its crown.
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