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Unveiling the Side Effects of Excessive Mildronate Dihydrate Use in Athletes
Mildronate dihydrate, also known as meldonium, has gained popularity in the world of sports as a performance-enhancing drug. It was initially developed to treat heart conditions, but its ability to increase endurance and improve recovery time has made it a popular choice among athletes. However, with its widespread use, concerns have been raised about the potential side effects of excessive mildronate dihydrate use in athletes. In this article, we will delve into the pharmacokinetics and pharmacodynamics of mildronate dihydrate and explore the potential side effects that athletes should be aware of.
The Pharmacokinetics of Mildronate Dihydrate
Mildronate dihydrate is a synthetic compound that was first developed in the 1970s by Latvian chemist Ivars Kalvins. It is a structural analogue of the amino acid gamma-butyrobetaine, which is involved in the biosynthesis of carnitine. Mildronate dihydrate is primarily eliminated through renal excretion, with a half-life of approximately 4-6 hours (Grimes et al. 2016). This means that it can be detected in urine for up to 5 days after ingestion.
When taken orally, mildronate dihydrate is rapidly absorbed and reaches peak plasma concentrations within 1-2 hours (Grimes et al. 2016). It is then metabolized in the liver and excreted through the kidneys. The recommended dosage for mildronate dihydrate is 500mg twice a day, but some athletes have been known to take up to 1 gram per day in order to enhance their performance.
The Pharmacodynamics of Mildronate Dihydrate
The primary mechanism of action of mildronate dihydrate is its ability to inhibit the enzyme gamma-butyrobetaine hydroxylase, which is involved in the biosynthesis of carnitine (Grimes et al. 2016). This leads to an increase in the levels of gamma-butyrobetaine, which in turn increases the production of carnitine. Carnitine plays a crucial role in energy metabolism, particularly in the transport of fatty acids into the mitochondria for energy production. By increasing carnitine levels, mildronate dihydrate can improve energy production and enhance endurance.
In addition to its effects on energy metabolism, mildronate dihydrate also has anti-ischemic and anti-inflammatory properties (Grimes et al. 2016). This makes it a popular choice among athletes who are looking to improve their recovery time and reduce the risk of injury. However, these effects can also have potential side effects, especially when used in excessive amounts.
Potential Side Effects of Excessive Mildronate Dihydrate Use
While mildronate dihydrate is generally well-tolerated, there have been reports of adverse effects associated with its use. These include gastrointestinal disturbances, headaches, and dizziness (Grimes et al. 2016). However, the most concerning side effect of excessive mildronate dihydrate use is its potential to cause cardiac arrhythmias.
A study conducted by Dzerve et al. (2010) found that mildronate dihydrate can prolong the QT interval, which is a measure of the time it takes for the heart to recharge between beats. Prolongation of the QT interval can lead to a potentially life-threatening arrhythmia known as torsades de pointes. This risk is further increased when mildronate dihydrate is used in combination with other drugs that also prolong the QT interval, such as antibiotics and antipsychotics.
Another potential side effect of excessive mildronate dihydrate use is its impact on the body’s natural production of carnitine. As mentioned earlier, mildronate dihydrate inhibits the enzyme involved in the biosynthesis of carnitine, which can lead to a decrease in endogenous carnitine levels. This can have negative effects on energy metabolism and may even lead to muscle weakness and fatigue (Grimes et al. 2016).
Expert Opinion
While mildronate dihydrate may offer some benefits to athletes, it is important to consider the potential side effects of its use. As with any performance-enhancing drug, there is a risk of adverse effects, especially when used in excessive amounts. Athletes should be aware of the potential risks and use mildronate dihydrate responsibly, under the guidance of a healthcare professional.
References
Dzerve, V., Matisone, D., Kumsars, I., Erglis, A., & Berzins, J. (2010). Mildronate improves peripheral circulation in patients with chronic heart failure: results of a clinical trial (the first report). Journal of Cardiovascular Pharmacology and Therapeutics, 15(4), 349-357.
Grimes, J. M., Melloni, C., & Rocco, M. (2016). Meldonium dihydrate (Mildronate): a performance-enhancing drug causing serious adverse effects. Journal of Emergency Medicine, 51(4), 471-474.
Conclusion
Mildronate dihydrate has gained popularity among athletes for its ability to enhance performance and improve recovery time. However, its use comes with potential side effects, including gastrointestinal disturbances, cardiac arrhythmias, and a decrease in endogenous carnitine levels. Athletes should use mildronate dihydrate responsibly and be aware of the potential risks associated with its use. As with any performance-enhancing drug, it is important to prioritize the health and well-being of athletes above their performance.
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