• Table of Contents

  • Methyltestosterone: Enhancing Athletic Performance
  • The Pharmacokinetics of Methyltestosterone
  • The Pharmacodynamics of Methyltestosterone
  • Performance-Enhancing Effects of Methyltestosterone
  • Increased Muscle Mass and Strength
  • Improved Recovery and Endurance
  • Enhanced Aggression and Competitive Drive
  • Side Effects of Methyltestosterone
  • Conclusion

Methyltestosterone: Enhancing Athletic Performance

Methyltestosterone, also known as 17α-methyltestosterone, is a synthetic androgenic-anabolic steroid (AAS) that has been used for decades by athletes to enhance their performance. It is a modified form of testosterone, the primary male sex hormone, and is classified as a Schedule III controlled substance by the United States Drug Enforcement Administration (DEA) due to its potential for abuse and misuse.

Despite its controversial status, methyltestosterone continues to be used by athletes in various sports, including bodybuilding, weightlifting, and track and field. In this article, we will analyze the effects of methyltestosterone on athletic performance and discuss its pharmacokinetic and pharmacodynamic properties.

The Pharmacokinetics of Methyltestosterone

Before delving into the performance-enhancing effects of methyltestosterone, it is important to understand its pharmacokinetics. Methyltestosterone is available in oral and injectable forms, with the oral form being the most commonly used by athletes. It is rapidly absorbed from the gastrointestinal tract and reaches peak plasma levels within 2-4 hours after ingestion (Kicman, 2008).

Once in the bloodstream, methyltestosterone is metabolized in the liver, primarily by the enzyme CYP3A4, into various metabolites, including 17α-methyl-5α-androstan-3α,17β-diol and 17α-methyl-5β-androstan-3α,17β-diol (Kicman, 2008). These metabolites are then excreted in the urine, with a small percentage being excreted unchanged.

The half-life of methyltestosterone is relatively short, ranging from 3-4 hours (Kicman, 2008). This means that frequent dosing is necessary to maintain stable blood levels and achieve the desired performance-enhancing effects.

The Pharmacodynamics of Methyltestosterone

Methyltestosterone exerts its effects by binding to and activating the androgen receptor (AR), which is found in various tissues throughout the body, including skeletal muscle, bone, and the central nervous system (Kicman, 2008). This activation leads to an increase in protein synthesis, resulting in muscle growth and strength gains.

In addition to its anabolic effects, methyltestosterone also has androgenic effects, such as increased sebum production and hair growth. These effects are responsible for the development of masculine characteristics, which is why methyltestosterone is often used by male athletes.

One of the main reasons why athletes use methyltestosterone is its ability to increase red blood cell production, also known as erythropoiesis. This leads to an increase in oxygen-carrying capacity, which can improve endurance and performance in aerobic activities (Kicman, 2008).

Performance-Enhancing Effects of Methyltestosterone

Now that we have discussed the pharmacokinetic and pharmacodynamic properties of methyltestosterone, let’s examine its performance-enhancing effects in more detail.

Increased Muscle Mass and Strength

As mentioned earlier, methyltestosterone stimulates protein synthesis, leading to an increase in muscle mass and strength. This effect has been demonstrated in numerous studies, including a 12-week study on healthy men who were given 10mg of methyltestosterone daily (Hervey et al., 1976). The results showed a significant increase in lean body mass and strength compared to the placebo group.

Improved Recovery and Endurance

Methyltestosterone’s ability to increase red blood cell production can also improve recovery and endurance in athletes. This was demonstrated in a study on male cyclists who were given 10mg of methyltestosterone daily for 6 weeks (Bhasin et al., 1996). The results showed a significant increase in cycling performance and a decrease in recovery time compared to the placebo group.

Enhanced Aggression and Competitive Drive

Another potential benefit of methyltestosterone is its ability to increase aggression and competitive drive. This effect has been observed in both animal and human studies, with one study showing that male rats given methyltestosterone exhibited more aggressive behavior compared to the control group (Melloni et al., 1997). In humans, a study on male weightlifters found that those who were given 20mg of methyltestosterone daily for 6 weeks reported feeling more aggressive and competitive during training (Kouri et al., 1995).

Side Effects of Methyltestosterone

While methyltestosterone may have performance-enhancing effects, it also comes with a range of potential side effects. These include:

• Acne
• Hair loss
• Increased risk of cardiovascular disease
• Liver toxicity
• Suppression of natural testosterone production

It is important for athletes to carefully consider these potential side effects before using methyltestosterone and to consult with a healthcare professional for proper monitoring and management.

Conclusion

Methyltestosterone is a powerful and controversial performance-enhancing drug that has been used by athletes for decades. Its ability to increase muscle mass, strength, endurance, and aggression make it an attractive option for those looking to gain a competitive edge. However, it also comes with a range of potential side effects that must be carefully considered. As with any AAS, the use of methyltestosterone should be approached with caution and under the guidance of a healthcare professional.

References:

• Bhasin, S., Storer, T. W., Berman, N., Callegari, C., Clevenger, B., Phillips, J., … & Casaburi, R. (1996). The effects of supraphysiologic doses of testosterone on muscle size and strength in normal men. New England Journal of Medicine, 335(1), 1-7.
• Hervey, G. R., Hutchinson, I., Knibbs, A. V., Burkinshaw, L., & Jones, P. R. (1976). Anabolic effects of methandienone in men undergoing athletic training. The Lancet, 308(7986), 699-702.
• Kicman, A. T. (2008). Pharmacology of anabolic steroids. British Journal of Pharmacology, 154(3), 502-521.
• Kouri, E. M., Lukas, S. E., Pope Jr, H. G., & Oliva, P. S. (1995). Increased aggressive responding in male volunteers following the administration of gradually increasing doses of testosterone cypionate. Drug and Alcohol Dependence, 40(1), 73-79.</