Winstrol: Bad News and More Bad News PDF Print E-mail
Written by Dan Gwartney, MD
Wednesday, 06 January 2010
winstrol1.jpgIn 1988, the sporting world was rocked by the announcement proclaiming that Ben Johnson, a Canadian sprinter who’d just shamed Carl Lewis in the Olympic 100-meter race, tested positive for anabolic steroid use. Johnson, who tested positive for stanozolol, was banned for several years from competition, losing his gold medal and an estimated $8.2 million in endorsements.1 Then, the Steroid Control Act of 1990 was passed and steroids became classified as a controlled substance.
Little Potency, Lots of Danger
Stanozolol, known classically by the trade name Winstrol, is a relatively mild steroid in terms of mass or strength gains, yet is extremely popular, particularly with bodybuilders and performance athletes.2 Winstrol (now sold under a variety of brand names and varying tablet strengths and concentrations) was originally available either as a low-strength tablet of two milligrams or as an aqueous suspension containing 50 milligrams per milliliter (mg/ml). Its use was commonly reserved for pre-competition phases for bodybuilders, as it aided in imparting a hardened appearance. In an audiotape series released in 1995 by the magazine Muscle Media 2000, one speaker suggested that a number of runners, particularly endurance runners, used a comparatively low dose of Winstrol to prevent muscle loss secondary to the catabolism experienced during long-distance training and competitions.
Stanozolol is the generic name for the chemical 17-Methyl-5alpha-androstano(3,2-c)pyrazol-17beta-ol, identified as CAS registry number 302-96-5.3 Considered to be a highly anabolic steroid due to its impressive anabolic/androgenic ratio, it’s in fact a very mild steroid in terms of muscle or strength gains. The surprising lack of potency is explained by the fact that stanozolol is a very weak androgen and as an anabolic agent, is less effective than a comparable dose of testosterone.4
Despite its relatively low potency, stanozolol is still commonly abused, in part due to its reputation for being a “safe” steroid. While stanozolol does not have the more dramatic or obvious side effects seen with many of the highly androgenic steroids, it’s by no means safe. In fact, the published record of medical reports suggests stanozolol may be one of the most dangerous forms of steroids to use.
State of Confusion
The confusion surrounding stanozolol is understandable as its actions are complex and poorly understood. Stanozolol, based upon the highly androgenic, reduced form of testosterone, DHT, would seemingly be a potent androgen, responsible for increased aggression, hair loss and acne. In fact, stanozolol is a very weak androgen4 and rather than promoting aggression, it’s been found to suppress aggression in animals such that they will not even respond to physical provocation or the presence of a male intruder.5,6 Further, the male sex glands, specifically the seminal vesicles, do not respond to stanozolol as a testosterone substitute and rats maintained on stanozolol lose the ability to ejaculate,6,7 eventually eliminating all sexual behavior.8 A similar response is seen in female rats failing to become sexually receptive under the influence of estrogen.9 Thus, in terms of behavior, stanozolol appears to act more as an anti-androgen, rather than an androgen. If these results are applicable to humans, it would make an athlete less competitive and interfere with normal sexual relations.
Complicating the social and psychological effects of stanozolol are the numerous reports demonstrating that stanozolol actively blocks normal brain function in a variety of receptor systems, and may interfere with anti-depressants and anxiety medications.10-12 Many steroid users describe a period of “depression” after completing a cycle of steroids and the findings from these studies suggest stanozolol may be exceptionally problematic for those who are subject to the psychological effects of steroid withdrawal. While stanozolol may be a less likely candidate to cause events described as “roid rage,” it may be a dangerous drug for anyone predisposed to suicide or other psychological trauma.
Examined by Science
Referring back to its chemical structure, as a DHT derivative, stanozolol is a reduced steroid, meaning it’s not a substrate for the enzyme aromatase, which is the enzyme responsible for converting most androgens into estrogens (female hormones). Indeed, few bodybuilders report estrogen-related side effects during or following a stanozolol-only cycle. However, the safety of stanozolol in this regard appears to be overstated; drawing upon an animal study, stanozolol was found to accelerate sexual maturation in female, pre-pubescent mice.13 This effect was prevented when an estrogen blocker was given to the mice prior to the stanozolol treatment. Interestingly, though stanozolol caused early changes in the vaginas of these mice, it was not strong enough at the dose studied to cause complete sexual maturation.
While this study is inconclusive, it might suggest that stanozolol may be capable of acting as a partial-agonist for the estrogen receptor, similar to the more familiar Nolvadex (Tamoxifen). Though it may not be a substrate for aromatase, meaning it is resistant to being converted into an estrogenic (female) hormone, stanozolol can modestly stimulate aromatase activity, possibly adding to the potential for other androgens to be converted to estrogens.14
Another study, examining the effects of stanozolol on skin cells in a lab, discovered that some of the results produced by stanozolol were unique, not explained by its chemical relationship to testosterone.15 Stanozolol has been shown to increase collagen production,16 as well as certain prostaglandins and enzymes within the skin. Investigating this phenomenon, researchers discovered that in the skin fibroblast (an early, undeveloped skin cell), stanozolol could not be displaced (removed) by nortestosterone (an androgen), dexamethasone (a cortisol derivative) or estradiol (an estrogen). Rather, it was partially displaced by progesterone, another female hormone.15 Again, it was interesting to note that though progesterone could displace stanozolol from receptors in the skin cells, progesterone failed to cause the same response. The actions of stanozolol are unclear from this study. It may be possible that stanozolol is capable of interacting with many different receptors, either interfering with other hormones or acting as a weak substitute.
None of these studies directly implicate stanozolol as an estrogenic or feminizing compound, and most users’ experiences with stanozolol would confirm that it is non-estrogenic, leading to a hardened appearance with minimal water retention and few reports of gynecomastia. However, the effect of stanozolol, when combined with other agents, may not be as worry free.
Stanozolol is provided in both oral and injectable forms. The chemical is identical in both preparations, the practical difference being that the injectable suspension allows for a higher concentration, usually at a lower cost.2 Stanozolol may be taken orally due to the presence of a methyl group (a small side chain) added to the steroid structure. This addition of the methyl group makes stanozolol one of the 17-alkylated steroids, which are commonly known for being more toxic to the liver than the injectable steroid esters.
The liver toxicity of stanozolol is often understated, with most users believing stanozolol is among the least toxic of steroids. In fact, the exact opposite may be closer to the truth. Oral stanozolol has been used for many years in the treatment of a variety of medical conditions, and new uses are being investigated.17-28 Even under conditions in which the drug is prescribed by a physician, dispensed from a legitimate pharmacy, and taken as directed, serious liver damage can occur. In some of the long-term studies reported, half or more of the subjects needed to have the dose lowered or even discontinue treatment due to elevations of the liver enzymes, a sign of cellular damage.22,26 However, most studies concluded that in nearly all cases, the signs and symptoms of liver damage went away with proper intervention and that stanozolol was felt to be a safe treatment alternative for certain conditions.18-20,22,25,27,28
The damaging effect of stanozolol upon the liver appears to be very common, and is of greater severity at higher doses. A binding protein has been discovered in rat and human liver specific for stanozolol and danazol, another steroid.29 Studies have proven stanozolol to be hepatotoxic (damaging to the liver).30-32 The effect of an extremely high level of stanozolol (400 times the recommended dose) upon liver cells failed to show any evidence of stanozolol causing or promoting cancer in those cells, even when exposed to other known carcinogens.33 This does not mean, however, that stanozolol is protective against cancer or risk-free, as these results would have to be confirmed and other chemicals may interact with stanozolol in a way that was not evaluated.
A case report has been published detailing severe liver damage and acute renal failure in a bodybuilder following the use of stanozolol (i.m. 50 mg every other day) stacked with metandienone (10-50 mg/day) for 80 days.34 This 28-year-old man showed up jaundiced (yellow skin and eyes) three weeks after completing his cycle, and deteriorated for seven weeks until time and treatment allowed him to recover (at significant expense).
More Bad News
This is not the only reported case of serious health consequences associated with stanozolol. A brief literature search revealed two deaths due to heart attacks,35 two heart attack survivors,36,37 one dangerous cardiac rhythm38 and a life-threatening blood loss,39 all in young men. Few steroids are so commonly associated with serious events such as these, which suggests stanozolol is not yet fully understood.
There are a number of other side effects and consequences associated with stanozolol use, but these are well known and generally accepted by the professional and athletic community. Briefly, stanozolol negatively affects the risk of heart attack or stroke by lowering the “good cholesterol” and raising the “bad cholesterol.”25,40,41 Women may experience masculinizing effects even at very low doses (2 mg/day).2,22,26,28 Stanozolol also increases the risk of serious bleeding, from the annoyance of nosebleeds to the life-threatening condition known as esophageal varices;23-25,31,39 may make tendons more prone to injury;42,43 is easily detected in hair and urine and remains detectable for several months following discontinuation;44-48 suppresses natural testosterone production;49,50 and dramatically lowers the carrier protein for androgens in the blood, called sex-hormone binding protein (SHBG).51,52
SHBG, which protects androgens from being metabolized and cleared from the body, is decreased by 50 percent with three days’ use of a low dose of stanozolol.51,52 At first glance, this may appear to be a positive effect, making what androgens are injected or swallowed less likely to be “bound” (prevented from stimulating muscle growth), instead allowing the steroid to float in the bloodstream as a “free” steroid, whereby it can interact with the muscle cell and cause hypertrophy. This is not such a benefit in the body, as SHBG protects androgens from rapid degradation and allows for the effect of testosterone or other androgens to persist for a longer period. SHBG lowers as a defense mechanism, allowing the body to shed excess androgens more quickly.
In conclusion, stanozolol, generally known as Winstrol, is a commonly abused steroid that’s felt by many users to be a very mild and safe anabolic. Though stanozolol doesn’t carry the risk of the more obvious and dramatic androgenic or estrogenic side effects of other drugs, it may be all the more dangerous for its subtle nature. Stanozolol appears to act upon many different systems in the body and brain, affecting many functions beyond androgen-stimulated hypertrophy of the muscle.
It’d been shown to mimic the effects of estrogen and shares a binding site with progesterone (female hormones); decreases sexual drive, sexual function and aggression; may cause or interfere with the treatment of psychological disorders; is highly likely to cause liver damage (fortunately this appears to be reversible in most cases); and may be involved with the development of life-threatening or fatal events, including heart attacks and bleeding. It may cause the body to more rapidly clear androgens and is easily detectable for long periods in both hair and urine.
Bodybuilders report using doses of 50-100 mg/day,2 yet doses as low as six to 10 mg/day have been shown to increase nitrogen retention greater than 200-300 milligrams of testosterone enanthate/week.53 This low dose has been used safely in studies monitored by physicians, though more than half of users, even at this low dose, need to have the dose lowered or discontinued due to liver damage or other side effects. Given that there are other steroids with fewer known risks, and that stanozolol is comparatively weak as both an androgen and an anabolic steroid, greater caution should be used by those considering stanozolol.
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