Methandrostenolone
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Methandrostenolone
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| Systematic (IUPAC) name | |
| (8S,9S,10S,13S,14S,17S)-17-hydroxy-10, 13,17-trimethyl-7,8,9,11,12,14,15,16- octahydro-6H-cyclopenta[a]phenanthren-3-one |
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| Identifiers | |
| CAS number | |
| ATC code | A14 |
| PubChem | |
| Chemical data | |
| Formula | C20H28O2 |
| Mol. mass | 300.441 g/mol |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | Hepatic |
| Half life | 4.5-6 hours |
| Excretion | Renal |
| Therapeutic considerations | |
| Pregnancy cat. |
X(US) |
| Legal status | |
| Routes | Oral |
Methandrostenolone (Dianabol, DBOL) is an anabolic steroid originally developed by John Ziegler and released in the US in 1958 by Ciba.[1][2] 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 has ceased.
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. [3] [4] Despite its illegality many athletes continue to use the drug for the muscle mass gains it can cause.
Methandrostenolone does not react strongly with the androgen receptor[5], instead relying on activity not mediated by the receptor for its effects. These include dramatic increases in protein synthesis, glycogenolysis, 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, acne 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 estradiol by aromatase. This means that without the administration of aromatase inhibitors such as Anastrozole or Aminoglutethimide, estrogenic effects will appear over time in men. Many users will combat the estrogenic side effects with Nolvadex or Clomid. 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.
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 stacked (combined) with drugs that react strongly with the androgen receptor, such as Oxandrolone, in order to increase the overall effectiveness of steroid use.
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.
[edit] Dr. Ziegler
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 1952 he worked with a number of trainees but had mixed results using testosterone. Dissatisfied and possibly overburdened with patients, he distanced himself from research into performance-enhancing drugs until 1959, a year or so before the 1960 Olympics.
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." However, Hoffmann later retracted on his decision and administered drugs to the certain American weightlifters on the team.
John Ziegler retired from medical practice in 1963. About this time, he reportedly told Hoffman "It is very, very possible, that special training techniques and other devices along with greater physiological knowledge may enable man to achieve physical performances now considered SUPERHUMAN!".
[edit] References
- Death due to Liver Failure Following the Use of Methandrostenolone Edmund M. Wilder, Can Med Assoc J. 1962 October 6; 87(14): 768–769.
- Some Experiences with a New Anabolic Steroid (Methandrostenolone) George L. Foss, Br Med J. 1960 April 30; 1(5182): 1300–1305.
- The Effect of Methandrostenolone on Nitrogen Excretion Following Open-Heart Surgery Walter Zingg, Can Med Assoc J, Oct.9, 1965, vol 93
- ^ NIDA Research Monograph 1990, Number 102, p97 [1]
- ^ Journal of Sport History, 1993, Vol.20 p2 [2]
- ^ Steve Theunissen: Arnold & Steroids: Truth Revealed 2002
- ^ Interview with Sergio Oliva
- ^ The effect of anabolic-androgenic steroids on aromatase activity and androgen receptor binding in the rat preoptic area. Brain Research 1998 May 11;792(2):271-6.
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