Mildronate in sport

Mildronate (meldonium) — the drug improving a metabolism and power supply of tissues is released according to the prescription. Drug was framed in the seventies the 20th century at Institute of organic synthesis of the Latvian SSR, professor Ivar Kalvinsh was engaged in development. Initially bond was patented as an agent for control of body height of plants and stimulation of body height of animals and poultry.

WADA considers mildronate as the metabolism modulator similar to insulin. The research published in December, 2015 in the Drug Testing and Analysis magazine claims that meldonium increases results of athletes, endurance, improves restoration after the performance, protects from a stress and increases functional activity of the central nervous system. At the same time the listed effects were confirmed, mainly, only by the Latvian scientists.

Since January 1, 2016 meldonium is added to the class S4 (Hormones and modulators of a metabolism) of the Forbidden list and forbidden to use during the competitive and out of competition period.

Scandal will lock mildronate and dope

Mildronate was one of the main components of pharmacological support of domestic athletes. According to the French specialists mildronat has property to accumulate and remain in an organism up to 120 days.

In October, 2015 at the international level it was accepted the anti-doping commission it is decided to include medicine mildronate-meldonium in the list of monitoring. The decision on a prohibition came into force on January 1, 2016 whereas doping scandal ran high in March. 

In news information extends that mildronate got under a prohibition at the initiative of the Anti-doping agency of the USA (USADA). According to a source, the Anti-doping agency of the USA the beginning of a research of meldonium in 2014. And in the fall of the same year data on doping tests of athletes from the former USSR in which meldonium was found were at the disposal of USADA. From 8300 researched samples 182 contained traces of use of medicine. As a result, based on these researches, medicine officially was included in the list prohibited since January 1, 2016.

"Doping scandal" with mildronat caused sharp increase in interest in it from buyers: in the last three days meldonium medicines Mildronate and Kardionat - leaders of information demand among drugs. So, for example, according to service of the order of the drugs Apteka.ru, medicine sales Mildronate for March 7-8 grew approximately at 15-20 times. At the same time no special advertizing actions concerning this product were taken. You can try Meldonium.

Positive test dope at athletes

For application of a mildronate from competitions detached already several Russian athletes. Positive doping tests on mildronate were handed over by the leader of Russian men's national team in short track, the Olympic champion of 2014 in relay, the world champion of 2015 at a distance of 1500 m and the all-around champion of Europe of 2016 Semyon Elistratov, the Olympic champion of 2014 in figure skating Ekaterina Bobrova, the winner of five tournaments of the Grand Slam, the prize-winner of the Olympic Games-2012 on tennis Maria Sharapova, the five-time world champion in speed skating Pavel Kulizhnikov and the volleyball player of Moscow "Dynamo" and Russian national team Alexander Markin.

In April there was a statement that the decision on temporary disqualification of the athletes convicted of meldonium use remains behind federation if concentration of substance in dope to the sample taken till March 1, 2016 makes from 1 to 15 mkg or if in the doping test taken after March 1, its concentration makes less than 1 mkg. Thus, actually all Russian athletes in whose organism meldonium was found will be acquitted.

Indications to use

• Indications to meldonium use:
• the lowered working capacity;
• physical overstrain, including at athletes;
• coronary heart disease (stenocardia, a myocardial infarction, a chronic heart failure and a cardialgia against the background of a disgormrnalny dystrophia of a myocardium);
• infectious and allergic bronchial asthma and chronic not obstructive bronchitis (as an immunomodulator in a combination therapy);
• abstinence syndrome at an alcoholism (in a combination with specific therapy of an alcoholism);
• acute disorders of a circulation in a retina; acute and chronic disorders of blood supply of a brain (cerebral strokes and chronic failure of a cerebral circulation).

Contraindications to use:

• With care to use drug to people with chronic diseases of a liver and kidneys for a long time.

Effects of a mildronat in bodybuilding

• Interferes with accumulating in cages of the activated forms of unoxidized fatty acids.
• In the conditions of ischemia recovers balance of processes of delivery of oxygen and its consumption in cages, prevents violation of transport of ATP.
• Activates glycolysis which proceeds without additional consumption of oxygen.
• Improves food of muscles.
• Increases efficiency of trainings.
• Reduces exhaustion.
• Protects heart and raises a myocardium sokratimost.

Route of administration and doses

"Attention" Mental and physical overworks, including in bodybuilding and powerlifting.

The adult from 15 to 20 mg on weight kg once a day, are desirable in 30 minutes prior to a training. The recommended courses of use are from 6 weeks to 3 months. Then it is desirable to take a break for a month that efficiency of impact of a mildronat on an organism didn't decrease.

Heart diseases

Stable angina of exertion. On 0,25 g in three times a day within 3-4 days, further two times a week on 0,25 g in three times a day. A course of treatment — 1-1,5 months. At prolonged treatment drug is combined with Sodium nitritums of long action.

Unstable stenocardia and myocardial infarction. For 0,5 - 1,0 intravenously struyno once a day then to the patient prescribe drug inside on 0,25 g twice a day in the first 3-4 days, further — two times a week on 0,25 g three times a day.

At an acute failure of a coronary circulation in the necrotic period of a myocardial infarction inside on 0,25 g twice a day in the first 3-4 days. In addition prescribe the patient with an acute heart failure high-speed cardiac glycosides (a strophanthin, Korglykonum, Celanidum) and diuretic agents.

Cardialgia against the background of a dishormonal dystrophia of a myocardium. On 0,25 g in twice a day morning and in the evening. A course of treatment — 12 days.

Infectious and allergic bronchial asthma.

Inside on 0,25 g every day within 3 weeks. Treatment is combined with broncholitic drugs.

Alcoholism

Inside on 0,5 g four times a day; intravenously and intramusculary on 0,5 g twice a day. A course of treatment — 7-10 days. Vascular pathology of an eyeground and dystrophia of a retina. Retrobulbarno and subkonjyunktivalno on 0,5 ml of 10% solution of a mildronate within 10 days. At an eye inflammation treatment is combined with parenteral or local administration of corticosteroids, at vascular and dystrophic diseases — with the drugs improving microcirculation.

Disturbance of a circulation of a brain

Acute phase of cerebrovascular pathology. On 5 ml of 10% solution once a day intravenously within 10 days then drug is prescribed to the patient inside on 0,5 g a day. A course of treatment — 2-3 weeks.

Chronic disturbances of blood supply of a brain. Enter 5 ml of 10% solution intramusculary once a day or on 0,25 g in 1-3 times a day, it is preferable in the first half of day. A course of treatment — 2-3 weeks.

Contraindications:

• Organic injury of the central nervous system.
• Diseases of a liver and kidneys.

Precautionary measures

As drug can cause moderate tachycardia and a lowering of arterial pressure, it is necessary to be careful at a combination of a mildronate with Nitroglycerinum, nifedipine, alpha adrenoblockers, antihypertensives and peripheric vazodilatator.

Side effects

In rare instances dermal itch, dyspeptic phenomena, tachycardia, exaltation, different changes of arterial pressure.

Storage

Ampoules and capsules — in the dry place at a temperature not above 25 °C. Not to freeze an ampoule.

Additional information

Mildronat (mildronate) renders cardioprotective, anti-anginal, anti-hypoxemic, angioprotektivny action. Is a structural synthetic analog at - a butyrobetaine — the precursor of a carnitine. Enzyme inhibits an at-butyrobetaine-hydroxylase, the dlinnotsepochechnykh of fatty acids through cellular membranes reduces synthesis of a carnitine and transport, interferes with accumulation in cells of the activated forms of unoxidized fatty acids (including the acylcarnitine blocking delivery of ATP to cell organellas). Improves metabolic processes. At an ischemia prevents disturbance of transport of ATP and activates a glycolysis. As a result of depression of synthesis of a carnitine in a cell contents at - the butyrobetaine having effect increases. Against the background of a heart failure improves contractility of a myocardium, enlarges tolerance to an exercise stress. Increases cellular and humoral immunity. Increases working capacity, reduces symptoms of a mental and physical overstrain, promotes endurance rising. At intake it is well soaked up from digestive tract. Bioavailability — about 78%. The maximum concentration in a blood plasma is reached in 1-2 h. An elimination half-life — 3-6 h. Side effects — a dyspepsia, exaltation, tachycardia, hypotension, a dermal itch. Average doses for adults at intake — 250 mg 2-4 times a day.