Methandrostenolone
Encyclopedia
Methandrostenolone is an orally-effective anabolic steroid
originally developed by John Ziegler
and released in the US
in the early 1960s by Ciba
. It was used as an aid to muscle growth by bodybuilders
until its ban by Congress under the Controlled Substances Act
. However, methandrostenolone is readily available without a prescription in countries such as Mexico
under the trade name Reforvit-b and is being manufactured in Asia and many East European countries, and consequently is still seen on the United States
black market.
but still exerts its effects through the androgen receptor in vivo. These include dramatic increases in protein synthesis
, glycogenolysis
, and muscle strength over a short space of time. 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 methylestradiol by aromatase
. This means that without the administration of aromatase inhibitors such as anastrozole
or aminoglutethimide
, estrogen
ic effects will appear over time in men. Many users will combat the estrogen
ic side effects with Arimidex, 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.
The 17α-methylation of the steroid does allow it to pass through the liver with only a small portion of it broken down (hence causing the aforementioned damage to the liver) allowing it to be effective when 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.
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
. Other steroids stacked with methandrostenolone are primarily, if not always, injectable compounds such as testosterone
, trenbolone
and nandrolone
.
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.
Anabolic steroid
Anabolic steroids, technically known as anabolic-androgen steroids or colloquially simply as "steroids", are drugs that mimic the effects of testosterone and dihydrotestosterone in the body. They increase protein synthesis within cells, which results in the buildup of cellular tissue ,...
originally developed by John Ziegler
John Bosley Ziegler
John Bosley Ziegler, John Ziegler, Montana Jack, was an American physician who originally developed the anabolic steroid Methandrostenolone which was released in the USA in 1958 by Ciba. He pioneered its athletic use as an aid to muscle growth by bodybuilders, administering it to U.S...
and released in the US
United States
The United States of America is a federal constitutional republic comprising fifty states and a federal district...
in the early 1960s by Ciba
Ciba Specialty Chemicals
Ciba was a chemical company based in and near Basel, Switzerland. "Ciba" stood for "Chemische Industrie Basel" . It was formed as the non-pharmaceuticals elements of Novartis were spun out in 1997, following the merger in the previous year of Ciba-Geigy and Sandoz that created Novartis.In 2008,...
. It was used as an aid to muscle growth by bodybuilders
Bodybuilding
Bodybuilding is a form of body modification involving intensive muscle hypertrophy. An individual who engages in this activity is referred to as a bodybuilder. In competitive and professional bodybuilding, bodybuilders display their physiques to a panel of judges, who assign points based on their...
until its ban by Congress under the Controlled Substances Act
Controlled Substances Act
The Controlled Substances Act was enacted into law by the Congress of the United States as Title II of the Comprehensive Drug Abuse Prevention and Control Act of 1970. The CSA is the federal U.S. drug policy under which the manufacture, importation, possession, use and distribution of certain...
. However, methandrostenolone is readily available without a prescription in countries such as Mexico
Mexico
The United Mexican States , commonly known as Mexico , is a federal constitutional republic in North America. It is bordered on the north by the United States; on the south and west by the Pacific Ocean; on the southeast by Guatemala, Belize, and the Caribbean Sea; and on the east by the Gulf of...
under the trade name Reforvit-b and is being manufactured in Asia and many East European countries, and consequently is still seen on the United States
United States
The United States of America is a federal constitutional republic comprising fifty states and a federal district...
black market.
Biophysiology
Methandrostenolone doesn't react strongly with the androgen receptorAndrogen receptor
The androgen receptor , also known as NR3C4 , is a type of nuclear receptor that is activated by binding of either of the androgenic hormones testosterone or dihydrotestosterone in the cytoplasm and then translocating into the nucleus...
but still exerts its effects through the androgen receptor in vivo. These include dramatic increases in protein synthesis
Protein biosynthesis
Protein biosynthesis is the process in which cells build or manufacture proteins. The term is sometimes used to refer only to protein translation but more often it refers to a multi-step process, beginning with amino acid synthesis and transcription of nuclear DNA into messenger RNA, which is then...
, glycogenolysis
Glycogenolysis
Glycogenolysis is the conversion of glycogen polymers to glucose monomers. Glycogen is catabolized by removal of a glucose monomer through cleavage with inorganic phosphate to produce glucose-1-phosphate...
, and muscle strength over a short space of time. In high doses (30 mg or more per day) , side effects such as gynecomastia
Gynecomastia
Gynecomastia or Gynaecomastia, , is the abnormal development of large mammary glands in males resulting in breast enlargement. The term comes from the Greek γυνή gyné meaning "woman" and μαστός mastós meaning "breast"...
, high blood pressure
Blood pressure
Blood pressure is the pressure exerted by circulating blood upon the walls of blood vessels, and is one of the principal vital signs. When used without further specification, "blood pressure" usually refers to the arterial pressure of the systemic circulation. During each heartbeat, BP varies...
, acne
Acne vulgaris
Acne vulgaris is a common human skin disease, characterized by areas of skin with seborrhea , comedones , papules , pustules , Nodules and possibly scarring...
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 by aromatase
Aromatase
Aromatase is an enzyme responsible for a key step in the biosynthesis of estrogens. It is a member of the cytochrome P450 superfamily , which are monooxygenases that catalyze many reactions involved in steroidogenesis. In particular, aromatase is responsible for the aromatization of androgens into...
. This means that without the administration of aromatase inhibitors such as anastrozole
Anastrozole
Anastrozole is an aromatase-inhibiting drug approved for treatment of breast cancer after surgery, as well as for metastasis in both pre and post-menopausal women. The severity of breast cancer is increased by estrogen, as sex hormones cause hyperplasia, and differentiation at estrogen receptor...
or aminoglutethimide
Aminoglutethimide
Aminoglutethimide is an anti-steroid drug marketed under the tradename Cytadren by Novartis around the world. It blocks the production of steroids derived from cholesterol and is clinically used in the treatment of Cushing's syndrome and metastatic breast cancer...
, estrogen
Estrogen
Estrogens , oestrogens , or œstrogens, are a group of compounds named for their importance in the estrous cycle of humans and other animals. They are the primary female sex hormones. Natural estrogens are steroid hormones, while some synthetic ones are non-steroidal...
ic effects will appear over time in men. Many users will combat the estrogen
Estrogen
Estrogens , oestrogens , or œstrogens, are a group of compounds named for their importance in the estrous cycle of humans and other animals. They are the primary female sex hormones. Natural estrogens are steroid hormones, while some synthetic ones are non-steroidal...
ic side effects with Arimidex, 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
Cirrhosis
Cirrhosis is a consequence of chronic liver disease characterized by replacement of liver tissue by fibrosis, scar tissue and regenerative nodules , leading to loss of liver function...
without appropriate care.
The 17α-methylation of the steroid does allow it to pass through the liver with only a small portion of it broken down (hence causing the aforementioned damage to the liver) allowing it to be effective when taken orally. It also has the effect of decreasing the steroid's affinity for sex hormone binding globulin
Sex hormone binding globulin
Sex hormone-binding globulin or sex steroid-binding globulin is a glycoprotein that binds to sex hormones, to be specific, testosterone and estradiol...
, 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
Testosterone
Testosterone is a steroid hormone from the androgen group and is found in mammals, reptiles, birds, and other vertebrates. In mammals, testosterone is primarily secreted in the testes of males and the ovaries of females, although small amounts are also secreted by the adrenal glands...
, resulting in rapid growth of muscle tissue. However, the concomitant elevation in estrogen
Estrogen
Estrogens , oestrogens , or œstrogens, are a group of compounds named for their importance in the estrous cycle of humans and other animals. They are the primary female sex hormones. Natural estrogens are steroid hormones, while some synthetic ones are non-steroidal...
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
Testosterone
Testosterone is a steroid hormone from the androgen group and is found in mammals, reptiles, birds, and other vertebrates. In mammals, testosterone is primarily secreted in the testes of males and the ovaries of females, although small amounts are also secreted by the adrenal glands...
or nandrolone
Nandrolone
Nandrolone is an anabolic steroid that may be present naturally in the human body, albeit in minute quantities of less than 0.4 ng/ml. Nandrolone is most commonly sold commercially as its decanoate ester and less commonly as a phenylpropionate ester...
with long acting esters build up in the body to an appreciable amount capable of supporting anabolic function on their own.
As tonic
Bodybuilding
However, despite the lack of any known therapeutic applications, the drug remained legal until the early 1990s. The United States Congress added steroids to the Controlled Substances Act as an amendment known as the Anabolic Steroid Control Act of 1990. This act placed steroids in the same category as amphetamines as a "Schedule III" drug and possession of these drugs results in a felony. Contrary to popular belief, steroids were banned by Congress without the support of the FDA, the American Medical Association, the DEA or the National Institute on Drug Abuse. Its used by bodybuilders, and methandrostenolone continues to be used illegally to this day, typically being combined (stacked) with injectable compounds, such as testosterone propionate, enanthate, cypionate as well as other injectables like trenbolone acetate.Several successful athletes and professional bodybuilders have come forward and admitted long-term methandrostenolone use before the drug was banned, including Arnold Schwarzenegger
Arnold Schwarzenegger
Arnold Alois Schwarzenegger is an Austrian-American former professional bodybuilder, actor, businessman, investor, and politician. Schwarzenegger served as the 38th Governor of California from 2003 until 2011....
and Sergio Oliva
Sergio Oliva
Sergio Oliva is a bodybuilder known as "The Myth". This sobriquet was given to him by bodybuilder/writer Rick Wayne. Wayne had begun calling Oliva "The Myth" ""....
. Other steroids stacked with methandrostenolone are primarily, if not always, injectable compounds such as testosterone
Testosterone
Testosterone is a steroid hormone from the androgen group and is found in mammals, reptiles, birds, and other vertebrates. In mammals, testosterone is primarily secreted in the testes of males and the ovaries of females, although small amounts are also secreted by the adrenal glands...
, trenbolone
Trenbolone
Trenbolone is a steroid used by veterinarians on livestock to increase muscle growth and appetite. To increase its effective half-life, trenbolone is not used in an unrefined form, but is rather administered as ester derivatives such as trenbolone acetate, trenbolone enanthate or trenbolone...
and nandrolone
Nandrolone
Nandrolone is an anabolic steroid that may be present naturally in the human body, albeit in minute quantities of less than 0.4 ng/ml. Nandrolone is most commonly sold commercially as its decanoate ester and less commonly as a phenylpropionate ester...
.
Detection of use
Methandrostenolone is subject to extensive hepatic biotransformation by a variety of enzymatic pathways. The primary urinary metabolites are detectable for up to 4 days, and a recently discovered hydroxymethyl metabolite is found in urine for up to 19 days after a single 5 mg oral dose. Several of the metabolites are unique to methandrostenolone. Methods for detection in urine specimens usually involve gas chromatography-mass spectrometry.Dr. Ziegler
For a period of time Dr. ZieglerJohn Bosley Ziegler
John Bosley Ziegler, John Ziegler, Montana Jack, was an American physician who originally developed the anabolic steroid Methandrostenolone which was released in the USA in 1958 by Ciba. He pioneered its athletic use as an aid to muscle growth by bodybuilders, administering it to U.S...
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
Performance-enhancing drugs
Performance-enhancing drugs are substances used by athletes to improve their performances in the sports in which they engage.- Types of performance-enhancing drugs :...
until May 1960, or possibly as early as 1959 (conflicting testimonials).
By the time of the 1960 European Championships in Milan
Milan
Milan is the second-largest city in Italy and the capital city of the region of Lombardy and of the province of Milan. The city proper has a population of about 1.3 million, while its urban area, roughly coinciding with its administrative province and the bordering Province of Monza and Brianza ,...
he was understandably suspicious of the Russians - "the Russians are giving their athletes something." Therefore, he asked John Grimek
John Grimek
John Carroll Grimek is recognized as one of the world's greatest bodybuilders and weight lifters of the 1930s and 1940s.Grimek was born on June 17, 1910 in Perth Amboy, New Jersey, son of Slovak immigrants George and Maria Grimek.Besides his bodybuilding exploits, in which he was never defeated,...
to propose to his chief, Bob Hoffman
Bob Hoffman
Wayne Robert Hoffman was a U.S. American football running back in the NFL for the Washington Redskins and Los Angeles Rams. He also played in the All-America Football Conference for the Los Angeles Dons and in the Pacific Coast Professional Football League for the Hollywood Bears...
that steroids be administered to members of the American
United States
The United States of America is a federal constitutional republic comprising fifty states and a federal district...
Olympic
Olympic Games
The Olympic Games is a major international event featuring summer and winter sports, in which thousands of athletes participate in a variety of competitions. The Olympic Games have come to be regarded as the world’s foremost sports competition where more than 200 nations participate...
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.