) is an anabolic steroid
originally developed by John Ziegler
and released in the US
in 1958 by Ciba
. It was used as an aid to muscle growth by bodybuilders
until its ban by the FDA
under the Controlled Substances Act
. Despite this, methandrostenolone continues to be produced in countries such as Mexico
under the trade name Reforvit-b
, and is being manufactured in Russia
, as well as Thailand
, and subsequently is still seen on the United States black market
. Production in most of Western Europe
and the United States
Methandrostenolone does not react strongly with the androgen receptor
but still exerts its effects through the androgen receptor in vivo
. These include dramatic increases in protein synthesis
, and muscle strength over a short space of time. However, due to its mode of action, it decreases the rate of cell respiration
and decreases production of red blood cells
. In high doses (30 mg
or more per day), side effects such as gynecomastia
, high blood pressure
and male pattern baldness
may begin to occur. The drug causes severe masculinising effects in women even at low doses. In addition, it is metabolized into methylestradiol
. This means that without the administration of aromatase inhibitors such as Anastrozole
effects will appear over time in men. Many users will combat the estrogenic
side effects with Nolvadex
. In addition, as with other 17α-alkylated steroids, the use of methandrostenolone over extended periods of time can result in liver damage
without appropriate care.
The 17α-methylation of the steroid does allow it to pass through the liver without being broken down (hence causing the aforementioned damage to the liver) allowing it to be taken orally. It also has the effect of decreasing the steroid's affinity for sex hormone binding globulin, a protein that de-activates steroid molecules and prevents them from further reactions with the body. As a result, methandrostenolone is significantly more active than an equivalent quantity of testosterone, resulting in rapid growth of muscle tissue. However, the concomitant elevation in estrogen levels - a result of the aromatization of methandrostenolone - results in significant water retention. This gives the appearance of great gains in mass and strength, which prove to be temporary once the steroid is discontinued and water weight drops. Because of this, it is often used by bodybuilders only at the start of a "steroid cycle", to facilitate rapid strength increases and the appearance of great size, while compounds such as testosterone or nandrolone with long acting esters build up in the body to an appreciable amount capable of supporting anabolic function on their own.
In the early 1960s, doctors commonly prescribed a tablet per day for women as a tonic
. This use was quickly discontinued upon discovery of the heavily masculinising effects of methandrostenolone.
However, despite the lack of any known therapeutic applications, the drug remained legal until the early 1990s. The ban by the FDA was not completely successful in eliminating its use by bodybuilders, and methandrostenolone continues to be used illegally to this day, typically being combined (stacked) with drugs that react strongly with the androgen receptor, such as Oxandrolone
, in order to increase the overall effectiveness of steroid use.
Several successful athletes and professional bodybuilders have come forward and admitted long-term methandrostenolone use before the drug was banned, including Arnold Schwarzenegger and Sergio Oliva.
For a period of time Dr. Ziegler
worked at the Ciba Pharmaceutical
company, who supplied testosterone for experimental purposes. In the early 1950s his patients included people suffering from burns, as well as the seriously injured or handicapped. In 1954 he administered testosterone, for a period of less than 6 weeks, to several high-level competitive bodybuilders on an experimental basis, but had disappointing results. Dissatisfied and possibly overburdened with patients, he distanced himself from research into performance-enhancing drugs
until May 1960, or possibly as early as 1959 (conflicting testimonials).
By the time of the 1960 European Championships in Milan he was understandably suspicious of the Russians - "the Russians are giving their athletes something." Therefore, he asked John Grimek to propose to his chief, Bob Hoffman that steroids be administered to members of the American Olympic team. Mr. Hoffman, however, was cautious and later remarked it was "too close to give to the men who will represent the USA". According to Grimek, "Apparently, he doesn’t think it will do that much good, and may even have detrimental effects , . . .He appears doubtful." Instead, Dianabol was given to two lower level lifters to investigate its effectiveness and safety. After that, Hoffmann retracted his decision and Dianabol was administered to certain Weightlifters on the team.