Description

Dianabol is the most recognized trade name for the drug methandrostenolone, also referred to as methandienone in many countries. Methandrostenolone is a derivative of testosterone, modified so that the hormone’s androgenic (masculinizing) properties are reduced and it's anabolic (tissue-building) properties preserved. Having a lower level of relative androgenicity than testosterone, methandrostenolone is classified as an “anabolic” steroid, although quite a distinct androgenic side is still present. This drug was designed and is principally sold, as an oral medication, although it can also be found in a number of injectable veterinary solutions. Dianabol is today and has historically been, the most commonly used oral anabolic/androgenic steroid for physique and performance-enhancing purposes.

History

Methandrostenolone was first described in 1955. It was released to the U.S. prescription drug market in 1958, under the brand name Dianabol by Ciba Pharmaceuticals. Ciba developed methandrostenolone into medicine with the help of Dr. John Ziegler, who was the team physician for a number of U.S. Olympic teams, including weightlifting. Ziegler makes a note in Bob Goldman’s Death in the Locker Room that he was first exposed to steroids at the 1956 World Games, seeing that the Russians were heavily abusing testosterone on their strength athletes. According to Ziegler, the hormone was having noticeable side effects, and one athlete had such profound prostate enlargement that he was forced to urinate with the aid of a catheter. While working with Ciba, the company tested a steroid (synthesized earlier) that had reduced androgenic compared to testosterone, but with retained tissue-building (anabolic) properties. This had been accomplished by altering the basic chemical structure of testosterone in a way that altered its metabolism and disposition in the body. With the help of Dr. Ziegler, Ciba brought to market one of the most effective oral “anabolic” steroid medicines ever known, methandrostenolone. The success of the drug was rapid and far-reaching.

Dr. Ziegler’s athletes were quickly making great advancements in their competitive careers with the help of the drug. According to reports, Ziegler too seemed to be very impressed, at least for a while. But by the early 1960s, it was starting to look like Dianabol had sparked a great wave of steroid abuse in competitive sports. Dr. Ziegler’s early recommendations, which depending on the source called for as little as 5 mg per day or as much as 15 mg per day, were being largely ignored, as athletes developed their own more aggressive (and potentially dangerous) dosing strategies. Dr. Ziegler soon became disgusted with the misuse of the drug, and would eventually become a voice of opposition to sports doping. By 1967, approximately 10 years after first introducing Dianabol to his athletes, he had categorically condemned the use of anabolic steroids in sports.

As early as 1965, Dianabol was already starting to fall under the scrutiny of the U.S. Food and Drug Administration. That year the FDA requested Ciba to clarify Dianabol’s medical uses, which were then stated to include helping patients in debilitated states and those with weakened bones. In 1970, the FDA accepted that Dianabol was “Probably Effective” in treating postmenopausal osteoporosis and pituitary-deficient dwarfism. These changes were reflected in the drug’s prescribing recommendations during the 1970s, and Ciba was allowed to continue selling and studying the agent. Ciba eventually lost patent protection, however, and companies like Parr, Barr, Bolar, and Rugby were soon cutting deeply into their market with their own generic version of the drug.

By the early-80’s the FDA had withdrawn its “Probably Effective” position on the pituitary-deficient dwarfism and continued to press Ciba for more data. Sufficient clarification never came, and in 1983 Ciba officially withdrew Dianabol from the U.S. market. Perhaps financial disinterest had a hand in their abandoned push to keep the drug approved. The FDA pulled all generic forms of methandrostenolone from the U.S. market in 1985, a time when most Western nations were also eliminating the drug, finding its existence to be justified mainly by sports doping. Methandrostenolone is still produced today, but typically in nations with loose prescription drug regulations, and by companies that still prefer to cater to an underground athletic market.

How Supplied

Methandrostenolone is widely available in both human and veterinary drug markets. Composition and dosage may vary by country and manufacturer. Methandrostenolone was designed as an oral anabolic steroid containing 2.5 mg or 5 mg of steroid per tablet (Dianabol). Modern brands usually contain 5 mg or 10 mg per tablet. Methandrostenolone can also be found in injectable veterinary preparations. These are typically oil-based solutions that carry 25 mg/ml of steroid.

Structural Characteristics

Methandrostenolone is a modified form of testosterone. It differs by 1) the addition of a methyl group at carbon 17- alpha to protect the hormone during oral administration and 2) the introduction of a double bond between carbons 1 and 2, which reduces its relative androgenicity. The resulting steroid also has a much weaker relative binding affinity for the androgen receptor than testosterone, but at the same time displays a much longer half-life and lower affinity for serum-binding proteins in comparison. These features (among others) allow methandrostenolone to be a very potent anabolic steroid in spite of a weaker affinity for receptor binding. Recent studies have additionally confirmed that its primary mode of action involves interaction with the cellular androgen receptor.¹

Side Effects (Estrogenic)

Methandrostenolone is aromatized by the body and is a moderately estrogenic steroid. Gynecomastia is often a concern during treatment and may present itself quite early into a cycle (particularly when higher doses are used). At the same time, water retention can become a problem, causing a notable loss of muscle definition as both subcutaneous water retention and fat levels to build. Sensitive individuals may, therefore, want to keep the estrogen under control with the addition of an anti-estrogen such as Nolvadex® and/or Proviron®. One may alternately use an aromatase inhibitor like Arimidex® (anastrozole), which is a more effective remedy for estrogen control. Aromatase inhibitors, however, can be quite expensive in comparison to standard estrogen maintenance therapies, and may also have negative effects on blood lipids.

It is interesting to note that methandrostenolone is structurally identical to boldenone, except that it contains the added c17-alpha-methyl group. This fact makes clear the impact of altering a steroid in such a way, as these two compounds appear to act very differently in the body. A key dissimilarity seems to lie in the tendency for estrogenic side effects. Equipoise® (boldenone undecylenate) is known to be quite mild in this regard, and users commonly take this drug without the need to add an anti-estrogen. Methandrostenolone is much more estrogenic, often necessitating anti-estrogen use. But this difference is not caused by methandrostenolone being more easily aromatized. In fact, the 17-alpha methyl group and c1-2 double bond both slow the process of aromatization considerably. The issue actually is caused by methandrostenolone converting to 17alpha-methyl estradiol, a more biologically active form of estrogen than estradiol.

Side Effects (Androgenic)

Although classified as an anabolic steroid, androgenic side effects are still common with this substance. This may include bouts of oily skin, acne, and body/facial hair growth. Anabolic/androgenic steroids may also aggravate male pattern hair loss. Individuals sensitive to the androgenic effects of methandrostenolone may find a milder anabolic such as Deca-Durabolin® to be more comfortable. Women are additionally warned of the potential virilizing effects of anabolic/androgenic steroids. These may include a deepening of the voice, menstrual irregularities, changes in skin texture, facial hair growth, and clitoral enlargement.

While methandrostenolone does convert to a more potent steroid via interaction with the 5-alpha reductase enzyme (the same enzyme responsible for converting testosterone to dihydrotestosterone), it has an extremely low affinity to do so.² The androgenic metabolite 5-alpha dihydromethandrostenolone is produced only in trace amounts, so the relative androgenicity of methandrostenolone is not significantly affected by finasteride or dutasteride.

Side Effects (Hepatotoxicity)

Methandrostenolone is a c17-alpha alkylated compound. This alteration protects the drug from deactivation by the liver, allowing a very high percentage of the drug entry into the bloodstream following oral administration. C17-alpha-alkylated anabolic/androgenic steroids can be hepatotoxic. Prolonged or high exposure may result in liver damage. In rare instances, life-threatening dysfunction may develop. It is advisable to visit a physician periodically during each cycle to monitor liver function and overall health. Intake of c17-alpha-alkylated steroids is commonly limited to 6-8 weeks, in an effort to avoid escalating liver strain.

Studies have shown that several weeks of methandrostenolone administration offers minimal hepatic stress so long as it is given at a dosage of 10 mg per day or below. At a dose of 15 mg per day, a majority of patients will begin to demonstrate disturbed liver function as measured by clinically elevated bromosulphalein retention (a marker of hepatic stress). Even at 2.5 and 5 mg per day, elevations in BSP retention have been reported in patients. Severe liver complications are rare given the periodic nature in which most people use oral anabolic/androgenic steroids, although cannot be excluded from methandrostenolone, especially with high doses and/or prolonged administration periods.

Side Effects (Cardiovascular)

Anabolic/androgenic steroids can have deleterious effects on serum cholesterol. This includes a tendency to reduce HDL (good) cholesterol values and increase LDL (bad) cholesterol values, which may shift the HDL to LDL balance in a direction that favors greater risk of arteriosclerosis. The relative impact of an anabolic/androgenic steroid on serum lipids is dependant on the dose, route of administration (oral vs. injectable), type of steroid (aromatizable or non-aromatizable), and level of resistance to hepatic metabolism. Methandrostenolone has a strong effect on the hepatic management of cholesterol due to its structural resistance to liver breakdown and route of administration. Anabolic/androgenic steroids may also adversely affect blood pressure and triglycerides, reduce endothelial relaxation, and support left ventricular hypertrophy, all potentially increasing the risk of cardiovascular disease and myocardial infarction.

To help reduce cardiovascular strain it is advised to maintain an active cardiovascular exercise program and minimize the intake of saturated fats, cholesterol, and simple carbohydrates at all times during active AAS administration. Supplementing with fish oils (4 grams per day) and a natural cholesterol/antioxidant formula such as Lipid Stabil or a product with comparable ingredients is also recommended.

Side Effects (Testosterone Suppression)

All anabolic/androgenic steroids, when taken in doses sufficient to promote muscle gain, are expected to suppress endogenous testosterone production. Methandrostenolone is no exception and is noted for its strong influence on the hypothalamic-pituitary-testicular axis. Clinical studies giving 15 mg per day to resistance-training males for 8 weeks caused the mean plasma testosterone level to fall by 69%.Without the intervention of testosterone-stimulating substances, testosterone levels should return to normal within 1-4 months of drug secession. Note that prolonged hypogonadotrophic hypogonadism can develop secondary to steroid abuse, necessitating medical intervention.

Administration (General)

Studies have shown that taking an oral anabolic steroid with food may decrease its bioavailability.This is caused by the fat-soluble nature of steroid hormones, which can allow some of the drug to dissolve with undigested dietary fat, reducing its absorption from the gastrointestinal tract. For maximum utilization, this steroid should be taken on an empty stomach.

Administration (Men)

The original prescribing guidelines for Dianabol called for a daily dosage of 5 mg. This was to be administered on an intermittent basis, with the drug taken for no more than 6 consecutive weeks. Thereafter, a break of 2 to 4 weeks was advised before therapy was resumed. For physique- or performance-enhancing purposes, the drug is also used intermittently, with cycles usually lasting between 6 and 8 weeks in length followed by 6-8 weeks off. Although a low dose of 5 mg daily may be effective for improving performance, athletes typically take much higher amounts. A daily dosage of three to six 5 mg tablets (15-30 mg) is most common and typically produces very dramatic results. Some venture even higher in dosage, but this practice usually leads to a more profound incidence of side effects, and is generally discouraged.

Dianabol stacks well with a variety of other steroids. It is noted to mix particularly well with the mild anabolic Deca-Durabolin®, for example. Together one can expect an exceptional muscle and strength gains, with side effects not much worse than one would expect from Dianabol alone. For sheer mass, a long-acting testosterone ester like enanthate or cypionate can be used. With the high estrogenic/androgenic properties of this androgen, however, side effects should be more pronounced. Gains would be pronounced as well, which usually makes such an endeavor worthwhile to the user. As discussed earlier, ancillary drugs can be added to reduce the side effects associated with this kind of cycle.

The half-life of Dianabol is only about 3 to 5 hours. A single daily dosage schedule will produce a varying blood level, with ups and downs throughout the day. The user, likewise, has a choice, to either split up the tablets during the day or to take them all at one time. The usual recommendation has been to divide them and try to regulate the concentration in your blood. This, however, will produce a lower peak blood level than if the tablets were taken all at once, so there may be a trade-off with this option. Both options work fine, but anecdotal evidence seems to support single daily doses as being better for overall results. With such a schedule, it seems logical that taking the pills earlier in the day would be optimal. This would allow a considerable number of daytime hours for an androgen-rich metabolism to heighten the uptake of nutrients, especially the critical hours following training.

Administration (Women)

Being moderately androgenic, Dianabol is really only a popular steroid with men. When used by women, strong virilization symptoms are possible. Some do experiment with it, however, and often find low doses (2.5-5 mg) of this steroid quite effective for new muscle growth. Studies have demonstrated that a majority of women will notice acne, which is indicative of androgenicity, at a dosage of only 10 mg per day. Children are likely to notice virilizing effects with as little as 2.5 mg per day.

References

1. Anabolic-androgenic steroid interaction with rat androgen receptor in vivo and in vitro: a comparative study. Feldkoren BI, Andersson S. J Steroid Biochem Mol Biol. 2005 Apr;94(5):481-7. Epub 2005 Mar 17.
2. Relative imporance of 5alpha reduction for the androgenic and LH-inhibiting activities of delta-4-3-ketosteroids. Steroids 29 (1997):331-48.