Methyltestosterone: is it so bad?

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Author: Vasily Roldugin

- coach and master of sports in powerlifting. Date: 2014-04-12

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Important! We do not encourage the use of steroids and other strong drugs. All information is given so that those who decide to take them do so with minimal risk to health.

This drug has earned a lot of negative words spoken and written on the pages of various publications and on the Internet. At the same time, the authors of the negative, except for the meager data from the instructions for use and their own conclusions based on these data, do not offer any compelling arguments in support of their position. As a result, all the information about methyltestosterone fits on a page with one single conclusion: never take it under any circumstances! Is this conclusion true? Let's try to figure it out.

Pharmacodynamics and pharmacokinetics

Pharmacodynamics

It has androgenic activity and is an artificial analogue of testosterone . Has a stimulating effect on the development of male secondary and primary sexual characteristics, stimulates libido and potency , demonstrates an anabolic effect; in a woman’s body it acts as an antagonist to estrogen .

Pharmacokinetics

Absorbed from the digestive tract and from the oral mucosa. Has a longer elimination period than testosterone .

Distinctive features of methyltestosterone

Methyltestosterone is the world's first oral form of testosterone. It has a pronounced androgenic and slight anabolic effect on the user’s body.

The main effects of taking methyltestosterone are an increase in mass and strength, increased strength endurance, and improved recovery abilities of the body.

Training using methyltestosterone as one of the components of an athlete's rehabilitation therapy is more effective.

The scope of application of methyltestosterone is powerlifting, weightlifting, American football, where the drug is used primarily to increase aggressiveness before the start and to increase strength and mass during preparation for competitions. In bodybuilding, methyltestosterone is practically not used due to significant water retention in the body.

Side effects

  • Hormonal disorders: masculinization in women, early puberty in male children, gynecomastia .
  • Digestive disorders: cholestasis , nausea , cholestatic hepatitis .
  • Other disorders: acne , edema , dizziness , thrombophlebitis .

Methyltestosterone, instructions for use (Method and dosage)

The largest daily dose for adults is 0.1 grams, a single dose is 0.05 grams.

In the treatment of primary eunuchoidism (incomplete development of secondary sexual characteristics) and hypogenitalism (insufficient development of the external genitalia) due to congenital underdevelopment of the male gonads or due to their removal, half a tablet of the drug is prescribed per day. For moderate hypogenitalism, 0.02-0.025 grams of medication once a day or every other day is sufficient. Therapy is carried out for a long time based on the severity of the disease and the effectiveness of treatment.

For the treatment of impotence due to insufficient functioning of the gonads, nervous exhaustion or fatigue, it is recommended to take 0.01-0.02 grams of the drug per day.

When treating menopausal syndrome , take 0.005-0.015 grams of the drug orally for up to 2 months; for prostate adenoma in the initial stage, approximately half a tablet per day is recommended for 1-2 months; The course of therapy is repeated, monitoring the progress of the process.

When treating infantilism (a painful condition characterized by delayed psycho-physical development in adolescents), delayed sexual development and slow growth in children and adolescents, it is recommended to take 0.005-0.01 grams of Methyltestosterone per day. The duration of treatment depends on the therapeutic effect.

In some cases, Methyltestosterone is prescribed to be taken (0.005-0.015 grams daily) as a tonic for those recovering from severe injuries, infections, surgical interventions, as well as for premature aging. However, for this purpose it is better to use anabolic steroids .

When treating dysfunctional bleeding from the uterus in the paramenopausal and menopausal periods, it is recommended to take 0.01-0.02 grams of the drug per day for up to 4 weeks. In especially severe cases, the dosage is increased.

In the treatment of menopausal nervous and vascular disorders in women, the medicine is prescribed only in cases where there are contraindications to taking estrogen drugs, at a dose of 0.005 grams up to 3 times a day until the disorders are relieved; if necessary, the course is repeated at the same dose.

When treating dysmenorrhea and algodysmenorrhea in elderly women, 0.01-0.02 grams per day is prescribed for 6 days before the onset of menstruation.

When treating ovarian and breast , take 1-2 tablets of the drug per day.

Methyltestosterone

Stylab / Catalog / Hormones and stimulants / Androgens / Methyltestosterone

STYLAB offers test systems for analyzing the content of methyltestosterone in meat, liver, fish and urine using the ELISA method, as well as standard solutions of methyltestosterone.

Enzyme-linked immunosorbent assay (ELISA), strip plate
R3611 RIDASCREEN® Methyltestosterone
Biosystem for androgen analysisAR CALUX®
Standard solutionsR3699 RIDA® Methyltestosterone Spiking Solution
Standards and mixtures of anabolic steroids and stilbenes for their analysis according to GOST 33482-2015

Methyltestosterone (17α-methyltestosterone) is a synthetic anabolic steroid, similar in action to testosterone . It was first synthesized in 1935. The structural features of the molecules of this substance determine both its better digestibility when taken orally compared to testosterone, and more pronounced estrogenic properties. Drugs containing methyltestosterone are used in medicine to treat infertility, some hormonal abnormalities associated with a lack of endogenous testosterone and prostate adenoma in men, as well as some breast or ovarian tumors in women.

The mechanism of action of methyltestosterone is a direct effect on gene expression in muscle cells, promoting the release of other hormones with anabolic effects and increasing food digestibility and conversion. Nowadays it is rarely used as a doping due to the serious consequences of using this substance. Methyltestosterone is on the WADA Prohibited List.

Side effects of methyltestosterone include liver problems, increased blood pressure, swelling and acne. In addition, women under the influence of this substance may develop male-type hair growth and masculinization of the body, including changes in voice timbre and body features. In men, methyltestosterone often causes gynecomastia - enlargement of the mammary gland due to fatty or glandular tissue, as well as oligospermia. Large doses of methyltestosterone cause testicular atrophy and infertility. In addition, experiments in mice suggest that this and other synthetic androgenic anabolics cause damage to nerve cells.

The anabolic effect of methyltestosterone is manifested not only in mammals, but also in fish. Therefore, some manufacturers add methyltestosterone to animal feed, from where it is well absorbed. However, such use of methyltestosterone is prohibited by law in the Russian Federation, the European Union and China. This is due to both the danger to the health of consumers and the fact that part of the methyltestosterone is released into the environment and affects other animals.

To determine the content of methyltestosterone, it is convenient to use test systems based on the enzyme-linked immunosorbent assay (ELISA) method. They enable fast and accurate testing of large numbers of samples and are validated for a variety of matrices.

Literature

  1. Schänzer W. Metabolism of anabolic androgenic steroids. Clin Chem. 1996 Jul;42(7):1001-20.
  2. KP Lone, AJ Matty. The effect of feeding androgenic hormones on the proteolytic activity of the alimentary canal of carp Cyprinus carpio. L J Fish Biol 1981,18(3):353–358
  3. Uzunov R, Hajrulai-Musliu Z, Stojanovska-Dimzoska B, Dimitrieska-Stojkovic E, Todorovic A, Stojkovski V. Validation of Screening Method for Determination of Methyltestosterone in Fish. Mac Vet Rev 2013; 36(1):19–23
  4. Namjoshi DR, Cheng WH, Carr M, Martens KM, Zareyan S, Wilkinson A, McInnes KA, Cripton PA, Wellington CL. Chronic Exposure to Androgenic-Anabolic Steroids Exacerbates Axonal Injury and Microgliosis in the CHIMERA Mouse Model of Repetitive Concussion. PLoS One. 2021 Jan 19;11(1):e0146540.

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Methyltestosterone analogues

Level 4 ATC code matches:
Sustanon 250

Androgel

Nebido

Andriol

Testosterone Isocaproate

Testosterone Decanoate

Testosterone Phenylpropionate

Testosterone Cypionate

Testosterone Undecanoate

Testosterone Enanthate

Omnadren 250

Methandren, Testoral, Androral, Gormal, Glosso-Sterandril, Madiol, Malogen, Oraviron, Stenendiol, Oreton M, Virormoneoral.

Dosages and regimens

First of all, attention is drawn to the recommendations that methyltestosterone can be used as a replacement for methandrostenolone. Even the indication that methyltestosterone has a short half-life, resulting in its level in the body having to be maintained by repeated use throughout the day, is very similar to the description of methane. It is also similar that the use of methyltestosterone is recommended to be limited to a period of 6-8 weeks.

But as for dosages, there are some interesting points here. For example, it is suggested that dosages of 50-60 mg per day be considered optimal if methyltestosterone is used “solo”. And 25-30 mg - if the drug is combined with other AAS. It is also recommended to take the entire daily dose at once (!!!) early in the morning to reduce the load on the liver.

As a result, we see a contradiction. If a drug has so many side effects, how can its optimal daily dose be higher than the dose of “less toxic” methane? If the concentration of the drug in the blood must be constantly maintained, then what will a single dose give in this regard?

In addition, methyltestosterone is available in the form of 5 mg tablets. This means that upon getting out of bed in the morning, the user will have to swallow 10-12 tablets at once. The stomach, apparently, will say “thank you” for such a thing.

There is an option to use methyltestosterone sublingually (dissolve under the tongue until completely dissolved), as recommended in some sources. Supposedly for faster absorption into the blood. Moreover, in the instructions for use the drug is presented as oral, not sublingual. This means that there is no point in all these manipulations with resorption.

As for combinations of methyltestosterone with other AAS, in my opinion, it is very reasonable to recommend combining it with non-aromatizing or slightly aromatizing drugs. Such as nandrolone, trenbolone, stanozolol or turinabol.

Taking into account all the available information on methyltestosterone, as well as all the inconsistencies and discrepancies, I bring to your attention a regimen for taking this drug as part of a comprehensive course of AAS.

Regimen for taking methyltestosterone (M) in combination with stanozolol (S) and turinabol (T)

The scheme presented in the table was tested in practice in the pre-competition cycle of powerlifting athletes. The result was a significant increase in strength indicators with an increase in relatively high-quality muscle mass. There were also no extreme side effects observed. Slight acne, increased activity of the sebaceous glands, and a slight increase in aggressiveness were noted. After completing the course, a significant part of the gains, especially in terms of strength indicators, were retained. After the course, appropriate rehabilitation measures were carried out.

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