-
Table of Contents
Methyltestosterone: Implications for Athletes’ Health
Methyltestosterone, also known as 17α-methyltestosterone, is a synthetic androgenic-anabolic steroid (AAS) that has been used for decades in the world of sports. It was first developed in the 1930s and has since been used by athletes to enhance their performance and physical appearance. However, the use of methyltestosterone has been surrounded by controversy due to its potential health implications. In this article, we will explore the pharmacokinetics and pharmacodynamics of methyltestosterone and its impact on athletes’ health.
Pharmacokinetics of Methyltestosterone
The pharmacokinetics of methyltestosterone refers to how the drug is absorbed, distributed, metabolized, and eliminated from the body. Methyltestosterone is available in oral, injectable, and transdermal forms. When taken orally, it is rapidly absorbed from the gastrointestinal tract and reaches peak plasma levels within 1-2 hours. However, its bioavailability is low due to extensive first-pass metabolism in the liver (Kicman, 2008).
Once in the bloodstream, methyltestosterone is bound to sex hormone-binding globulin (SHBG) and albumin. Only a small percentage of the drug remains unbound and is considered the active form. Methyltestosterone is metabolized in the liver by the enzyme 17β-hydroxysteroid dehydrogenase (17β-HSD) into its active metabolite, 17α-methyl-5α-androstan-3α,17β-diol (Kicman, 2008). This metabolite has a longer half-life than methyltestosterone and is responsible for its androgenic and anabolic effects.
The elimination half-life of methyltestosterone is approximately 4 hours, but its metabolite has a half-life of 10-20 hours (Kicman, 2008). This means that the effects of methyltestosterone can last for several hours after administration, making it a popular choice among athletes who need a quick boost in performance.
Pharmacodynamics of Methyltestosterone
The pharmacodynamics of methyltestosterone refers to how the drug affects the body. Methyltestosterone is a synthetic derivative of testosterone, the primary male sex hormone. It exerts its effects by binding to androgen receptors in various tissues, including muscle, bone, and the central nervous system (Kicman, 2008). This results in an increase in protein synthesis, leading to muscle growth and strength gains.
Methyltestosterone also has androgenic effects, meaning it can cause masculinizing effects such as increased body hair, deepening of the voice, and clitoral enlargement in women (Kicman, 2008). These effects are due to the conversion of methyltestosterone into dihydrotestosterone (DHT) by the enzyme 5α-reductase. DHT is a more potent androgen than testosterone and is responsible for the development of male characteristics.
Aside from its anabolic and androgenic effects, methyltestosterone also has a negative impact on the body. It can increase blood pressure, cholesterol levels, and liver enzymes, which can lead to cardiovascular and liver problems (Kicman, 2008). It can also suppress the body’s natural production of testosterone, leading to hormonal imbalances and potential infertility.
Implications for Athletes’ Health
The use of methyltestosterone by athletes has been linked to numerous health implications. In a study by Hartgens and Kuipers (2004), it was found that AAS use, including methyltestosterone, can lead to cardiovascular diseases such as hypertension, left ventricular hypertrophy, and myocardial infarction. These effects are due to the increase in blood pressure and cholesterol levels caused by AAS use.
Methyltestosterone has also been associated with liver damage, particularly cholestasis, a condition where the flow of bile from the liver is impaired (Kicman, 2008). This can lead to jaundice, liver failure, and even death. In addition, the suppression of natural testosterone production can result in hormonal imbalances, which can have long-term effects on an athlete’s health, including decreased bone density and fertility issues (Hartgens & Kuipers, 2004).
Moreover, the use of methyltestosterone and other AAS has been linked to psychological effects such as aggression, mood swings, and dependence (Hartgens & Kuipers, 2004). These effects can have a significant impact on an athlete’s mental health and overall well-being.
Real-World Examples
The use of methyltestosterone and other AAS has been prevalent in the world of sports for decades. In 2013, Major League Baseball player Ryan Braun was suspended for 65 games after testing positive for elevated levels of testosterone, which he claimed was due to a medication he was taking for a medical condition (Associated Press, 2013). However, it was later revealed that the medication contained synthetic testosterone, likely methyltestosterone, and Braun was suspended for violating the league’s drug policy.
In 2016, Russian tennis player Maria Sharapova tested positive for meldonium, a drug that was recently banned by the World Anti-Doping Agency (WADA). However, it was also discovered that she had been using meldonium to mask the use of milder AAS, including methyltestosterone, for over a decade (Associated Press, 2016). This revelation led to a 15-month suspension for Sharapova and a tarnished reputation in the world of sports.
Expert Opinion
As an experienced researcher in the field of sports pharmacology, I have seen the detrimental effects of AAS use, including methyltestosterone, on athletes’ health. While these drugs may provide short-term performance benefits, the long-term consequences can be severe and irreversible. It is crucial for athletes to understand the potential risks and consequences of using these substances and to prioritize their health and well-being above temporary gains.
References
Associated Press. (2013). Ryan Braun suspended for rest of season. ESPN. Retrieved from https://www.espn.com/mlb/story/_/id/9512025/ryan-braun-milwaukee-brewers-suspended-rest-season
Associated Press. (2016). Maria Sharapova banned for 2 years for doping. The New York Times. Retrieved from https://www.nytimes.com/2016/06/09/sports/tennis/maria-sharapova-doping.html
Hartgens, F., & Kuipers, H. (2004). Effects of androgenic-anabolic steroids in athletes. Sports Medicine, 34(8), 513-554. https://doi.org/10.2165/00007256-200434080-00003
Kicman
Leave a Reply