Methasterone gained popularity as a "supplement" with very fast effects, but it became one of the most prominent examples of an unregistered steroid entering the medical journals due to complications. The editors have collected all the main risks of the drug in one place, grouped them by organ, and indicated whether each statement is based on clinical cases or knowledge of the 17-alpha-alkylated androgen class.
Why the evidence base is limited
Methasterone has never undergone clinical trials. There is no randomized trial evaluating its safety at different doses and duration of administration. All that is known comes from three sources: clinical case reports, general knowledge about 17-alpha-alkylated androgens, and user surveys.
Clinical cases are good at capturing severe, visible complications, such as jaundice. Instead, "silent" risks — changes in lipids, pressure, heart structure — rarely come to the attention of doctors immediately and are almost never associated with a specific drug.
Surveys and forums are prone to bias: people are more likely to report expected effects and less likely to attribute subsequent problems to the steroid. In addition, the real composition of products is often unknown.
Therefore, the editors consider the risks of methasterone as a minimum estimate: what is documented is there, but the absence of data on other complications does not mean their absence.
Liver: major documented risk
The best described side effect of methasterone is cholestatic liver damage. A series of five cases published by Shah et al in 2008 showed a typical presentation: jaundice, pruritus, markedly elevated bilirubin, and cholestasis on biopsy without significant inflammation.
Nasr and Ahmad (2009) described a patient with severe cholestasis and renal failure after taking Superdrol. Kidney damage with very high bilirubin is a known complication that has been seen with other anabolic steroids.
Analysis of the Spanish registry of drug-induced liver damage (Robles-Diaz et al., 2015) found that cholestatic damage from illegal steroids is characterized by a long course: normalization of indicators can take months.
The mechanism is attributed to the 17-alpha-methyl group, which provides oral activity. This same modification is associated with rare but serious complications — liver peliosis and adenomas with long-term use of androgens of this class.
Cardiovascular system and blood
17-alpha-alkylated androgens are characterized by a significant decrease in the level of HDL ("good" cholesterol) and an increase in LDL. A review by Achar et al (2010) systematized data on the effects of anabolic steroids on lipids, blood pressure, and heart structure and found that oral drugs particularly adversely affect the lipid profile.
Long-term use of anabolic steroids is associated with hypertrophy and decreased contractile function of the myocardium, as well as with accelerated development of atherosclerosis of coronary arteries. This is evidenced by the research of Baggish et al. (2017), who compared long-term steroid users with those who did not use them.
Androgens stimulate erythropoiesis, which can increase hematocrit and blood viscosity. There are no separate data for methasterone, but this effect is common to the class.
The editors discuss the cardiovascular risks of methasterone in detail in a separate article on lipids, blood pressure, and hematocrit.
Hormones, skin and psyche
Hormonal axis. Like any androgen, methasterone suppresses the production of luteinizing and follicle-stimulating hormones through a negative feedback loop. The result is a decrease in own testosterone, a decrease in the volume of the testes and inhibition of spermatogenesis. Recovery from androgen withdrawal can take months (Rahnema et al., 2014).
Skin and hair. As a derivative of DHT, methasterone has a pronounced androgenic effect on the skin and hair follicles. Possible acne, increased oiliness of the skin and acceleration of androgenetic alopecia in genetically predisposed people.
Psyche. For anabolic steroids, irritability, aggressiveness, mood swings, sleep disturbances, and after withdrawal — depressive symptoms during hormonal deficiency are generally described. The Endocrine Society in a scientific statement (Pope et al., 2014) singles out the risk of anabolic steroid addiction.
Women. For women, methasterone carries a high risk of virilization: hoarseness of the voice, male-type hair growth, clitoral enlargement, menstrual cycle disorders. Voice changes are often irreversible.
| System | Possible consequences | What clinicians monitor |
|---|---|---|
| Liver | Cholestasis, jaundice, kidney damage | Bilirubin, ALT, AST, GGT, alkaline phosphatase, creatinine |
| Lipids and the heart | Decreased HDL, hypertension, myocardial hypertrophy | Lipid panel, blood pressure, ECG, echocardiography |
| Blood | Hematocrit increase | Complete blood count |
| Endocrine system | LH/FSH suppression, infertility | LH, FSH, testosterone, semen analysis |
| Skin | Acne, baldness | Examination by a dermatologist |
| Mental health | Irritability, post-withdrawal depression, addiction | Consultation of a psychiatrist or psychologist |
Hidden risk: product composition
Methasterone is not an approved human medicine. It entered the market in the form of "supplements", and after the ban - through illegal channels.
Analyzes of products marketed as sports supplements have repeatedly detected undeclared anabolic steroids. Therefore, a person can take methasterone without knowing about it, or vice versa - buy "methasterone" that contains a different substance or a different amount.
For athletes, this also means the risk of a positive doping test: methasterone is included in section S1 of the WADA Prohibited List, and the athlete is responsible for the content of the product.
Even when a product does contain methasterone, the amount can vary significantly from batch to batch. Therefore, any "typical" sensations or side effects reported by users do not actually describe a single substance, but rather an undefined mixture of products.
- Unknown concentration of the active substance.
- It is possible to replace with another, in particular, an even more hepatotoxic steroid.
- Lack of control of impurities.
- The risk of a positive doping test even with "accidental" intake.
Editorial conclusions
The best documented risk of methasterone is severe cholestatic liver injury, sometimes with renal failure. This complication became the cause of regulatory measures.
Cardiovascular, hormonal, skin, and mental risks are known from studies of the anabolic steroid class and there is no reason to consider methasterone an exception.
The lack of clinical trials and quality control makes the drug's risk profile even less predictable.
We also advise you to read our articles on the oral bioavailability of methasterone, on its effects on the cardiovascular system and on suppression of own testosterone.
References
- Shah NL, Zacharias I, Khettry U, Afdhal N, Gordon FD. Methasteron-associated cholestatic liver injury: clinicopathologic findings in 5 cases. Clin Gastroenterol Hepatol. 2008;6(2):255–258.
- Nasr J, Ahmad J. Severe cholestasis and renal failure associated with the use of the designer steroid Superdrol (methasteron): a case report and literature review. Dig Dis Sci. 2009;54(5):1144–1146.
- Robles-Diaz M, Gonzalez-Jimenez A, Medina-Caliz I, et al. Distinct phenotype of hepatotoxicity associated with illicit use of anabolic androgenic steroids. Aliment Pharmacol Ther. 2015;41(1):116–125.
- Achar S, Rostamian A, Narayan SM. Cardiac and metabolic effects of anabolic-androgenic steroid abuse on lipids, blood pressure, left ventricular dimensions, and rhythm. Am J Cardiol. 2010;106(6):893–901.
- Baggish AL, Weiner RB, Kanayama G, et al. Cardiovascular toxicity of illicit anabolic-androgenic steroid use. Circulation. 2017;135(21):1991–2002.
- Pope HG Jr, Wood RI, Rogol A, et al. Adverse health consequences of performance-enhancing drugs: an Endocrine Society scientific statement. Endocr Rev. 2014;35(3):341–375.
- Rahnema CD, Lipshultz LI, Crosnoe LE, et al. Anabolic steroid-induced hypogonadism: diagnosis and treatment. Fertil Steril. 2014;101(5):1271–1279.
