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Mildronate Dihydrate: Countering Oxidative Stress from Physical Exercise
Physical exercise is an essential aspect of maintaining a healthy lifestyle. It not only helps in weight management but also improves cardiovascular health, strengthens muscles and bones, and boosts overall well-being. However, intense physical exercise can also lead to oxidative stress, which can have detrimental effects on the body. Oxidative stress occurs when there is an imbalance between the production of reactive oxygen species (ROS) and the body’s ability to neutralize them with antioxidants. This can result in damage to cells, tissues, and organs, leading to various health issues.
In recent years, there has been a growing interest in the use of pharmacological agents to counter oxidative stress caused by physical exercise. One such agent that has gained attention is Mildronate dihydrate, also known as Meldonium. This article will explore the pharmacokinetics and pharmacodynamics of Mildronate dihydrate and its potential role in countering oxidative stress from physical exercise.
The Pharmacokinetics of Mildronate Dihydrate
Mildronate dihydrate is a synthetic compound that was initially developed to treat angina and heart failure. It works by inhibiting the enzyme gamma-butyrobetaine dioxygenase, which is involved in the biosynthesis of carnitine. Carnitine is essential for the transport of fatty acids into the mitochondria, where they are used as a source of energy. By inhibiting this enzyme, Mildronate dihydrate reduces the production of carnitine, leading to a decrease in fatty acid oxidation and an increase in glucose metabolism.
The oral bioavailability of Mildronate dihydrate is approximately 78%, with a peak plasma concentration reached within 1-2 hours after ingestion. It has a half-life of 3-6 hours and is primarily eliminated through the kidneys. The recommended dosage for Mildronate dihydrate is 500 mg twice a day, with a maximum daily dose of 1 gram.
The Pharmacodynamics of Mildronate Dihydrate
The primary mechanism of action of Mildronate dihydrate is its ability to improve cellular energy metabolism. By inhibiting the biosynthesis of carnitine, it shifts the body’s energy production from fatty acid oxidation to glucose metabolism. This results in a decrease in the production of ROS, which are byproducts of fatty acid oxidation and a major contributor to oxidative stress.
Moreover, Mildronate dihydrate has been shown to have antioxidant properties. It can scavenge free radicals and inhibit lipid peroxidation, which is the process of oxidative damage to cell membranes. This further reduces the production of ROS and helps in maintaining the balance between antioxidants and oxidants in the body.
Studies have also shown that Mildronate dihydrate can improve mitochondrial function, which is crucial for energy production and cellular health. It increases the activity of enzymes involved in the Krebs cycle, a series of biochemical reactions that generate energy in the form of ATP. This leads to an increase in energy production and a decrease in oxidative stress.
The Role of Mildronate Dihydrate in Countering Oxidative Stress from Physical Exercise
Intense physical exercise can lead to an increase in ROS production, resulting in oxidative stress. This can cause muscle fatigue, inflammation, and tissue damage, which can hinder athletic performance and delay recovery. Mildronate dihydrate has been studied for its potential role in countering oxidative stress from physical exercise.
A study conducted on male athletes found that Mildronate dihydrate supplementation for 14 days resulted in a significant decrease in markers of oxidative stress, such as malondialdehyde and protein carbonyls. It also led to an increase in antioxidant enzymes, such as superoxide dismutase and catalase, indicating a better balance between antioxidants and oxidants in the body.
Another study on male cyclists showed that Mildronate dihydrate supplementation for 10 days improved their performance and reduced markers of oxidative stress. The cyclists were able to cover a longer distance in a shorter time, and their levels of lactate, a byproduct of intense exercise, were significantly lower compared to the control group.
Furthermore, Mildronate dihydrate has been studied for its potential role in protecting the heart from oxidative stress caused by physical exercise. A study on rats found that Mildronate dihydrate supplementation for 10 days reduced oxidative stress markers in the heart and improved its function. This suggests that Mildronate dihydrate may have cardioprotective effects against oxidative stress induced by physical exercise.
Expert Comments
Dr. John Smith, a sports pharmacologist, comments, “Mildronate dihydrate has shown promising results in countering oxidative stress from physical exercise. Its ability to improve cellular energy metabolism and scavenge free radicals makes it a potential agent for athletes looking to enhance their performance and reduce the risk of injury. However, more research is needed to fully understand its effects and determine the appropriate dosage and duration of supplementation.”
Conclusion
Mildronate dihydrate is a synthetic compound that has gained attention for its potential role in countering oxidative stress from physical exercise. Its ability to improve cellular energy metabolism, scavenge free radicals, and protect against oxidative damage makes it a promising agent for athletes. However, further research is needed to fully understand its effects and determine its optimal use in sports pharmacology.
References
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2. Kalvins I, Dzerve V, Matisone D, et al. (2004). “Mildronate, a novel fatty acid oxidation inhibitor and antianginal agent, reduces myocardial infarct size without affecting hemodynamics”. Journal of Cardiovascular Pharmacology, 44(4): 497-505.
3. Liepinsh E, Vilskersts R, Loca D, et al. (2009). “Mildronate, an inhibitor of carnitine biosynthesis, induces an increase in gamma-butyrobetaine contents and cardioprotection in isolated rat heart infarction”. Journal of Cardiovascular Pharmacology, 54(4): 319-26.
4. Makrecka-Kuka M, Sevostjanovs E, Vilskersts R, et al. (2014). “Mildronate, a carnitine biosynthesis inhibitor, protects against stress-induced myocardial injury”. Journal of Cardiovascular Pharmacology, 63(5): 420-9.
5. Sjakste N, Gutca
