Mildronate (meldonium) in sports: facts, mechanism of action, how to take it and is it worth it?

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Mildronate is known not only to those who “pump iron”. It is used in almost all sports, since it is universal in its action. However, since 01/01/2016, mildronate has been included in the list of prohibited drugs of the World Anti-Doping Agency (WADA). Now this drug is officially considered a doping.

The active ingredient of mildronate is meldonium (trimethylhydrazinium propionate). It was synthesized in the 70s of the last century. And immediately it became widespread both among medical practice and among athletes.

Why is Mildronate needed in sports?

The drug has many effects that can be useful in sports. For athletes, Mildronate is, first of all, a medicine that affects cell metabolism.

• It inhibits the production of carnitine, a substance that inhibits the breakdown of fatty acids and thus helps reduce the amount of fat in the body.
• Increases the amount of oxygen in cells by reducing vascular spasm, which helps nourish all organs and tissues.
• Successfully reduces the amount of free radicals accumulated by cells over time.
• By successfully delivering oxygen to the heart muscle and improving its nutrition, Mildronate helps the heart get more workload. As a result, it helps you withstand more frequent and intense workouts.

All this has made Mildronate an extremely popular drug in sports pharmacology courses among athletes in a variety of sports.

Benefit for ordinary people

Despite the high prevalence of the drug among athletes, it is also popular among those who hardly engage in sports and reviews about it are mostly positive. And all thanks to a large set of properties:

• assistance in supplying blood filled with oxygen to the tissues and cells of the body, where its concentration is below normal;
• normalization of metabolism throughout the body;
• increasing a person’s endurance to both physical and mental stress;
• increased performance;
• voltage reduction;
• assistance in rehabilitation after surgery;
• improved concentration and memory;
• assistance in the treatment of cardiovascular diseases, bronchitis, asthma, alcoholism;
• improving the transport of glucose to cells;
• accelerating the removal of decomposition products;
• maintaining cardiac tone;
• rapid restoration of energy resources;
• improving the condition of people prone to suffocation, fatigue and weakness from exertion;
• help in losing weight.

For those who do not exercise, mildronate is used for illnesses, to restore the body, to increase mental abilities and to reduce physical, mental and mental stress. The list of main indications for use is in the instructions for use.

Why Mildronate is considered a doping

Everyone knows the loud scandal that erupted around the Olympic champions who used Mildronate. According to the sports website, the development of events with the doping scandal around Mildronate occurred quite quickly.

In October 2015, the International Anti-Doping Commission included Mildronate in the list of substances prohibited for use by athletes. This decision came into force at the beginning of the following year - in January. The content of Mildronate in the body is maintained for about 120 days, so literally in March a doping scandal broke out, in which Russian athletes became the central figures.

The fact is that meldonium is one of the most popular substances used as additional maintenance therapy during heavy sports training. After the commission declared that Mildronate is a doping, athletes, even after stopping taking it, would not be able to completely remove it from the body. As a result of the scandal, many Russian athletes were suspended from competitions. However, a statement was later issued that more carefully regulated the dose that could be detected in the blood of athletes, which had a positive impact on their return to world competitions.

After the doping scandal surrounding Mildronate broke out all over the world, the demand for it among people outside of sports has increased markedly. Most consumers believed that the hype around this drug indirectly confirms the effectiveness of the drug. Thanks to him, sales of Mildronate increased sharply, despite the fact that there was no additional advertising for the drug.

How long does it take for meldonium to be eliminated from the body?

There is no clear answer to the question about the time of removal of meldonium from the body, since it has not been studied by scientists.

Some sources report an average elimination time of 24 hours with a single dose; if it is taken regularly, detection in the blood is possible even several months after stopping use.

Some experts say that complete elimination of mildronate from the body occurs after 100-120 days .

The complete elimination time of meldonium from the body can reach 3-4 months with regular use

Directions for use and doses

You can read about how to dose and drink Mildronate for diseases, including the heart, directly in the package insert in the drug packaging. But it doesn’t say how athletes should take Midronat. Therefore, we will try to provide information on how Mildronate is taken in bodybuilding and during particularly intense exercise in other sports.

The drug is dosed depending on the weight of the athlete; when taken orally, there is no difference whether it is taken in tablets or capsules. The dosage in both of these forms is the same.

Important!

Per kilogram of weight, from 15 to 20 mg of the drug is used, taken once a day. Most often, it is recommended to take the medicine half an hour before the start of a workout, since during this time it will have time to successfully enter the bloodstream and activate its properties.

The duration of the course can vary greatly depending on the needs of a particular person, but it is recommended to take it for at least 3 weeks, and the maximum duration threshold is 3 months. After completing the course, it is necessary to take a break, also for at least a month, since Mildronate can cause a decrease in effectiveness if taken for an excessively long time.

It is important to take breaks from using the drug

The drug is available in several dosage forms:

• pills;
• capsules;
• ampoules for injection.

If, as mentioned above, there is no significant difference between tablets and capsules when taking them, apart from convenience, then there is a slight difference between ampoules. It lies, first of all, in the speed of entry into the blood, since injection allows the substance to begin to act not after half an hour, but almost immediately. Therefore, if an athlete chooses this method of administration, then he needs to keep this in mind in order to calculate the exact time of application.

It should also be remembered that the drug in the form of a solution quickly collapses upon contact with air, so after opening the ampoule it must be administered immediately.

Indications for use

Mildronate is indicated in the following cases:

1. Heart problems, including heart failure and cardiomyopathy caused by hormonal imbalance, as well as myocardial infarction and angina.
2. Decreased performance.
3. Overexertion in bodybuilders.
4. Bronchial asthma of infectious-allergic origin.
5. Chronic bronchitis of a non-obstructive nature (in such cases it is prescribed as an immunomodulator as part of complex treatment).
6. Chronic withdrawal caused by alcoholism.
7. Retinal blood supply disorders (central vein thrombosis).
8. Strokes.

Contraindications

Meldonium is one of the safest drugs and the list of contraindications for its use is insignificant. This is also an argument in favor of using the product during training. The main conditions that require stopping the use of the drug are as follows:

• Allergic reactions and individual intolerance. Mildronate cannot be called a drug that often causes such reactions, but if this occurs, it would be better to choose another medication for maintenance therapy.
• Pregnancy and breastfeeding. This contraindication has been added to avoid any potential harm to the baby or mother. The exact effect of the medication on a woman and child during this period has not been studied, and therefore the instructions for use urge you not to take Mildronate during pregnancy or lactation.
• Children's age up to 12 years. The effects on children of this age have also not been studied, and therefore the medication is contraindicated for them for the same reason as for pregnant women: reducing the potential harm to the body when taken.
• Liver disorders. The liver is the main site of meldonium deactivation, and therefore excessive stress on it can cause a negative reaction in the body.
• It is not advisable for people with tumors to take the drug, since any maintenance therapy can provoke their growth.

You should also take meldonium strictly in the first half of the day (the best time is morning), as it can cause insomnia and overexcitability if taken in the evening.

Precautionary measures

In some cases, the drug may interact with drugs that mainly act on the cardiovascular system. This happens because due to its action it can cause a slight tachycardia and a drop in blood pressure. Therefore, when taken together with nitroglycerin and drugs from the antihypertensive group, you need to be careful and try not to combine them in one course.

How to use

General rules

As follows from the explanations of experts, Mildronate has some application features:

1. The effect of meldonium is more effective if you take the drug half an hour before meals. In this case, it is advisable to have something to eat so as not to irritate the gastric mucosa.
2. For intramuscular and intravenous infusions, the meal schedule does not matter.
3. Since meldonium has a strong tonic effect on the body, it is advisable to drink or inject it before lunch. Otherwise, your sleep schedule may be disrupted.
4. Mildronate is excellent for complex treatment. It goes well with anticoagulants, antirhythmic and diuretic drugs, as well as bronchodilators, glycosides and a number of other drugs. If you are taking other medications, meldonium should be taken only half an hour after eating.

In medicine

Capsules are taken orally, injections intravenously. Capsules are prescribed in 0.5 - 1 mg doses, evenly distributed throughout the day in 2-4 doses. Each time the drug should be taken with a glass of water.

Intravenously – 5-10 ml in 1-2 doses. The duration of treatment, dosage of the drug and method of administration are determined by the nature of the disease. As part of complex therapy, capsules are taken once a day.

Reception scheme in sports

For prevention, Mildronate for athletes is prescribed during training; how to take it is reflected in special diagrams. Capsules are taken twice a day for two to three weeks before competition, half an hour before training. During competitions, the period of use of the drug for an athlete is 10–14 days.

Is the drug harmful to health?

Despite the almost complete absence of contraindications for use, Mildronate was and remains a drug that can be harmful if taken incorrectly. This is especially true for people who take it uncontrollably and do not consult with specialist doctors on how exactly to do it.

As a rule, the main harm that occurs when taking the drug is associated with the lack of a pause between doses. Failure to take a break can lead to the fact that, having felt a decrease in effectiveness, a person begins to use the drug in increasingly larger dosages, and after this the risk of side effects increases. As a result, tachycardia, skin rashes, drop in blood pressure and stomach problems occur.

Therefore, before starting a course of even such an almost harmless drug, it is necessary to clarify the rules of administration with a doctor and make sure that the course is prescribed in accordance with your needs.

Afterword

Mildronate is a product of the domestic doping industry, which athletes from all over the world want to try (thanks to Maria Sharapova for this).

Widespread distribution and use by Russian athletes indicates its likely effectiveness. A few scientific studies confirm the benefits of meldonium in aerobic sports (running, skiing, cycling) and indirect in strength sports (bodybuilding, powerlifting).

Mildronate is excreted from the body over several months and has no serious side effects.

Reviews from doctors and athletes

• Doctor. Most of my athlete patients already know about the drug, the dosage of use and why it is needed. Unfortunately, the main reason for treatment is complaints about side effects from the drug, which are caused by uncontrolled use. The body quickly gets used to any dose of the medicine. And the lack of pauses in reception aggravates the situation. Most often, before a competition, the course of use is delayed for 5-6 months with a systematic increase in dosage. This negatively affects the cardiovascular system, leads to disorders of the nervous system, as well as disorders of the gastrointestinal tract.
• Gleb, 32 years old. I've been doing bodybuilding for a long time. Before the doping story, I was not at all interested in meldonium; there was something like doubt that it worked. Now I’m taking it for the second month, I’m thinking about taking a break and then coming back again. Surprisingly, it really works, there are no side effects. My muscle endurance has increased, I can increase the number of workouts and my working weights.
• Lena, 24 years old. I lost 15 kg. I have taken Mildronate in courses of 3 months already 2 times. Recommended by the trainer. The doses were prescribed to be the minimum acceptable for me. When there was a pause in taking it for 1 month, it was noticeably felt on endurance and physical capabilities. Now I don’t plan to return to the drug, because I heard that it can negatively affect the reproductive system of women.

Description of the drug

The active substance of meldonium is trimethylhydrazinium propionate. Mildronate is a non-steroidal drug used in the treatment of many diseases (ophthalmology, neurology, cardiology, etc.). In case of hypoxia or ischemia, it is able to restore cell metabolism. The product is also indispensable in bodybuilding, it gives stamina and restores strength. The medicine is made in tablet form, capsule form, syrup form, as well as a solution of 5 percent, 10 percent.