Methandrostenolone first appeared in literature in 1955 and was released to the U.S. prescription market in 1958 by Ciba Pharmaceuticals under the name Dianabol.
This drug is a testosterone derivative, designed to reduce androgenic properties while preserving its anabolic action.
While Dianabol was primarily used for physique enhancement, it also has deep roots in medical prescription.
Dr. John Ziegler, the physician for the U.S. Olympic team, developed Methandrostenolone to level the playing field against Russian athletes.
Dbol, with its low androgenicity but retained anabolic action, quickly brought significant changes to the world of sports.
However, within five years, steroid abuse became widespread as many athletes ignored the initial prescribing guidelines of 5-15mg.
In 1970, the FDA demanded a clear explanation from Ciba regarding its approved uses, judging it “probably effective” for treating osteoporosis and pituitary-deficient dwarfism while continuing research.
Additionally, cases of its use in pediatric dystrophy have been reported.
In 1983, Ciba withdrew Dianabol from the U.S. market, and in 1985, the FDA pulled generic versions of Methandrostenolone.
In 1990, its non-medical use was banned under the Anabolic Steroid Control Act.
Metabolism of Methandrostenolone
Methandrostenolone is primarily metabolized in the liver through reactions such as 6β-hydroxylation, 3α- and 3β-oxidation, 5β-reduction, 17-epimerization, and conjugation, and is excreted in the urine.
The human mitochondrial steroid hydroxylase enzymes CYP11B1 and CYP11B2 (of non-hepatic origin) can also form 11β-hydroxy and 18-hydroxy metabolites.
Unconjugated, beta-glucuronidated, and sulfated metabolites are also found in the urine.
With long-term use at high doses, unmetabolized drug may appear in the urine.
Side Effects of Dbol (Methandrostenolone)
Although Methandrostenolone is an anabolic steroid, it can cause androgenic side effects.
Women should be cautious of virilizing effects such as deepening of the voice, menstrual irregularities, facial hair growth, and clitoral enlargement.
Clinical reports show that prepubertal girls treated with Dianabol cream experienced accelerated growth and bone maturation, clitoral hypertrophy, and voice changes, with some symptoms reversing.
The potential for conversion to 5-alpha-dihydromethandrostenolone by 5-alpha reductase exists, but the rate is slow.
Thyroid-binding globulin (TBG) levels can be affected even at low doses, leading to an increase in free thyroxine and triiodothyronine.
Methandrostenolone is highly estrogenic and converts to 17α-methylestradiol.
This triggers negative feedback on the HPTA, lowering testosterone levels; a 15mg dose can reduce testosterone levels by 69%.
HPTA function typically recovers after discontinuing use.
It also reduces sex hormone-binding globulin (SHBG), thereby increasing free testosterone.
Sperm density and the percentage of motile cells also decrease, with some cases of azoospermia, though this is reversible.
Its C17-alpha alkylated structure is associated with hepatotoxicity, with reports of jaundice, hepatitis, and, in severe cases, liver cancer.
Medical monitoring is necessary if liver values become elevated.
Cardiovascular side effects include an increase in LDL and a decrease in HDL, mediated by hepatic triglyceride lipase.
The impact on HDL is greater with oral administration.
While not directly nephrotoxic, it can raise blood pressure by enhancing the RAAS, which may be associated with acute kidney injury.
Past literature attempted to link anabolic steroid use with violent crime, but the evidence is inconclusive, and the neurochemical effects of Methandrostenolone are not clear.
Cardiovascular (Cholesterol/Lipids)
Reported Clinical Uses
Early clinical use of Methandrostenolone focused on treating pediatric muscular dystrophy and growth issues.
Later clinical use shifted to increasing nitrogen retention, which reduces nitrogen excretion by about 30%, and increasing serum protein levels to promote recovery after surgery, burns, fractures, and skin grafts, shortening healing time.
It has also been reported to be effective in senile states, recovery after chronic infections, increasing calcium retention in osteoporosis patients, and boosting red blood cell count in anemic patients.
Methandrostenolone interacts not only with androgen receptors but also with glucocorticoid receptors, exhibiting anti-inflammatory effects and lowering cortisol levels by suppressing corticotropin production.
Its association with increased insulin resistance and visceral fat is an area requiring further research.
Athletes and Strength Training
The first report of Dianabol being used for physique enhancement showed a 2.48 kg (5.45 lbs) increase in lean muscle tissue after taking 5mg for three weeks, and it was proven to aid in strength maintenance and recovery after 12 weeks without training.
Anti-Doping / Counterfeit Supplements
Since the late 2000s, dietary supplements have been closely scrutinized for the possible illegal inclusion of AAS, especially prohormones.
A study of 103 supplements found undisclosed Methandrostenolone in three of them.
From an anti-doping perspective, consumers must be aware of the ingredients in the products they purchase, and new methods for detecting AAS are continuously being developed and improved.
Reported Deaths
Most deaths associated with Methandrostenolone use reported in the literature are related to myocardial infarction or the progression of cardiovascular disease.
However, most cases are reported as reactions to polydrug use, not a specific substance.
Recommended Health Supplements with Dianabol Use
Methandrostenolone is a C17-alpha alkylated compound, making it crucial to prevent hepatotoxicity and manage bile metabolism.
To support bile flow, it is recommended to take bile acids like Tauroursodeoxycholic acid (TUDCA) and Ox-Bile, as well as lipotropic compounds like choline and inositol.
A Liver Stack consists of 1000mg Ox Bile, 800mg TUDCA, 800mg Choline, and 800mg Inositol.
Caution is needed as using Methandrostenolone with TUDCA may increase hepatocellular uptake, potentially increasing hepatotoxicity.
Dianabol Dosage
Originally, a dose of 0.1-0.3 mg/kg was prescribed for children to treat muscular dystrophy.
For men, the initial prescribing guideline was 5mg daily, not to exceed 6 weeks.
While effective at the time, doses of 30-50mg are reported today to produce faster and more noticeable results for physique and performance enhancement.
A 1981 paper noted that a 100mg dose for 6 weeks was well-tolerated.
Another report mentions a dose of 0.6mg/kg.
For women, 2.5mg was prescribed for osteoporosis, with caution advised for virilizing side effects.
Availability of Dianabol
Dbol (Methandrostenolone) is a controlled substance in many countries, but it remains popular among bodybuilders who source it from underground labs (UGLs).
However, Methandrostenolone is readily available without a prescription in certain countries and is manufactured by underground pharmaceutical facilities like Alpha-Pharma (India) and GlobalAnabolic in Asia and many Eastern European countries.
| Chemical Name | 17a-methyl-17b-hydroxy-1,4-androstadien-3-one |
| Half-Life | 3 – 6 hours |
| Anabolic: Androgenic Ratio |
1:1-1:8 (Testosterone is the standard at 1:1 in rats) |
