Buy Mildronate Grindex (Meldonium dihydricum) 60x500mg

Mildronate Grindex (Meldonium dihydricum) 60x500mg
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Mildronate Grindex (Meldonium dihydricum) 60x500mg

Best known as the drug that was responsible for getting Maria Sharapovato  banned from professional tennis tournaments.

 

Meldonium (INN; trade name Mildronate, among others) is a limited-market pharmaceutical, developed in 1970 by Ivars Kalviņš at the USSR Latvia Institute of Organic Synthesis, and now manufactured by the Latvian pharmaceutical company Grindeks and several generic manufacturers. It is primarily distributed in Eastern European countries as an anti-ischemia medication.

 

Since 1 January 2016, it has been on the World Anti-Doping Agency (WADA) list of substances banned from use by athletes. However, there are debates over its use as an athletic performance enhancer. Some athletes are known to have been using it before it was banned. It is currently unscheduled in the US.

 

Medical use

Meldonium may be used to treat coronary artery disease. These heart problems may sometimes lead to ischemia, a condition where too little blood flows to the organs in the body, especially the heart. Because this drug is thought to expand the arteries, it helps to increase the blood flow as well as increase the flow of oxygen throughout the body. Meldonium has also been found to induce anticonvulsant and antihypnotic effects involving alpha 2-adrenergic receptors as well as nitric oxide-dependent mechanisms. This, in summary, shows that meldonium given in acute doses could be beneficial for the treatment of seizures and alcohol intoxication. It is also used in cases of cerebral ischemia, ocular ischemic syndrome and other ocular disease caused by disturbed arterial circulation and may also have some effect on decreasing the severity of withdrawal symptoms caused by the cessation of chronic alcohol use.

 

Pharmacology

Meldonium and its various forms of packaging showing 250 mg capsules and the injection 10% 5 ml

Although initial reports suggested meldonium is a non-competitive and non-hydroxylatable analogue of gamma-butyrobetaine; further studies have identified that meldonium is a substrate for gamma-butyrobetaine dioxygenase. X-ray crystallographic and in vitro biochemical studies suggest that meldonium binds to the substrate pocket of γ-butyrobetaine hydroxylase and acts as an alternative substrate, and therefore a competitive inhibitor. Normally, this enzyme's action on its substrates γ-butyrobetaine and 2-oxoglutarate gives, in the presence of the further substrate oxygen, the products L-carnitine, succinate, and carbon dioxide; in the presence of this alternate substrate, the reaction yields malonic acid semialdehyde, formaldehyde (akin to the action of histone demethylases), dimethylamine, and (1-methylimidazolidin-4-yl)acetic acid, "an unexpected product with an additional carbon-carbon bond resulting from N-demethylation coupled to oxidative rearrangement, likely via an unusual radical mechanism." The unusual mechanism is thought likely to involve a Steven's type rearrangement.

Meldonium's inhibition of γ-butyrobetaine hydroxylase gives a half maximal inhibitory concentration (IC50) value of 62 micromolar, which other study authors have described as "potent." Meldonium is an example of an inhibitor that acts as a non-peptidyl substrate mimic.

 

Structure of meldonium

The chemical name of meldonium is 3-(2,2,2-trimethylhydraziniumyl) propionate. It is a structural analogue of γ-butyrobetaine, with an amino group replacing the C-4 methylene of γ-butyrobetaine. γ-Butyrobetaine is a precursor in the biosynthesis of carnitine.

Meldonium is a white crystalline powder, with a melting point of 87 °C (189 °F)

 

Doping

Meldonium was added to the World Anti-Doping Agency (WADA) list of banned substances effective 1 January 2016 because of evidence of its use by athletes with the intention of enhancing performance. It was on the 2015 WADA's list of drugs to be monitored. An alarmingly high prevalence of meldonium use by athletes in sport was demonstrated by the laboratory findings at the Baku 2015 European Games. 13 medallists or competition winners were taking meldonium at the time of the Baku Games. Meldonium use was detected in athletes competing in 15 of the 21 sports during the Games. Most of the athletes taking meldonium withheld the information of their use from anti-doping authorities by not declaring it on their doping control forms as they should have. Only 23 of the 662 (3.5%) athletes tested declared the personal use of meldonium. However, 66 of the total 762 (8.7%) of athlete urine samples analysed during the Games and during pre-competition tested positive for meldonium.

 

WADA classes the drug as a metabolic modulator, just as it does insulin. Metabolic modulators are classified as S4 substances according to the WADA banned substances list. These substances have the ability to modify how some hormones accelerate or slow down different enzymatic reactions in the body. In this way, these modulators can block the body's conversion of testosterone into oestrogen, which is necessary for females. Based on the overall effects these drugs have, they have been banned since 2001 from men's competitions and 2005 for women's.[31] On April 13, 2016 it was reported that WADA had issued updated guidelines allowing less than 1 microgram per milliliter of meldonium for tests done before March 1, 2016.[32] The agency cited that "preliminary tests showed that it could take weeks or months for the drug to leave the body".

Affected athletes

On March 7, 2016, former world number one tennis player Maria Sharapova announced that she had failed a drug test in Australia due to the detection of meldonium. She said that she had been taking the drug for ten years for various health issues, and had not noticed that it had been banned. On June 8, 2016, she was suspended from playing tennis for two years by the International Tennis Federation (ITF). Earlier the same year (March 7), Russian ice dancer Ekaterina Bobrova announced that she had also tested positive for meldonium at the 2016 European Figure Skating Championships. Bobrova said she was shocked about the test result, because she had been made aware of meldonium's addition to the banned list, and had been careful to avoid products containing banned substances. In May 2016, Russian professional boxer Alexander Povetkin—a former two-time World Boxing Association (WBA) Heavyweight Champion—tested positive for meldonium. This was discovered just a week prior to his mandatory title match against World Boxing Council (WBC) Heavyweight Champion, Deontay Wilder. As a result, the match—scheduled to take place in Povetkin's native Russia—was postponed indefinitely by the WBC.

 

Other athletes who are provisionally banned for using meldonium include Ethiopian-Swedish middle-distance runner Abeba Aregawi,[40] Ethiopian long-distance runner Endeshaw Negesse, Russian cyclist Eduard Vorganov, and Ukrainian biathletes Olga Abramova and Artem Tyshchenko.

The Ice Hockey Federation of Russia replaced the Russia men's national under-18 ice hockey team with an under-17 team for the 2016 IIHF World U18 Championships after players on the original roster tested positive for meldonium.

 

More than 170 failed tests by athletes were identified in a relatively brief period after the ban on meldonium was imposed on January 1, 2016, almost all of which were from Eastern European countries, with much smaller numbers since. Many of the early cases were dropped when athletes claimed that they had ceased use in 2015, with the claim often consistent with the low concentrations of the drug in their samples.

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