Meldonium

Dosage form Meldonium:

hard gelatin capsules No. 00. Body and cap are white, opaque.
Capsule contents: white or almost white powder or mixture of powder and crystals, with a weak characteristic odor, hygroscopic. Compaction of the contents of the capsule into lumps is allowed.

Composition Meldonium

Each capsule contains:

Active ingredient:
Meldonium dihydrate - 500 mg.
Excipients: potato starch - 16 mg
microcrystalline cellulose - 28 mg
colloidal silicon dioxide - 9.6 mg
magnesium stearate- 5.6 mg

The composition of the capsule body: titanium dioxide - 2.0%; gelatin - up to 100%.
The composition of the capsule cap: titanium dioxide - 2.0%; gelatin - up to 100%.

Special conditions Meldonium:

Patients with chronic liver and kidney diseases should be careful with prolonged use of the drug. If you need a long (more than a month) use of the drug, you should consult a specialist. There is insufficient data on the use of the drug in children under 18 years of age. The drug can give a positive result during doping control.
Influence on the ability to drive vehicles, mechanisms
There is no evidence of an adverse effect on the ability to drive a vehicle and the performance of potentially hazardous activities requiring increased concentration of attention and speed of psychomotor reactions. However, given the spectrum of adverse reactions, in some cases caution should be exercised when driving and performing potentially hazardous activities.

Drug interactions Meldonium:

Strengthens the effect of coronary dilatants
some antihypertensive drugs
cardiac glycosides.
Can be combined with prolonged forms of nitrates 
other antianginal drugs
anticoagulants 
antiplatelet agents 
antiarrhythmics 
diuretics,
bronchodilators.
In view of the possible development of tachycardia and arterial hypotension, caution should be exercised when combined with nitroglycerin (for sublingual use) and antihypertensive drugs (especially alpha-blockers and short-acting forms of nifedipine). The simultaneous use of the drug with other drugs containing Meldonium is not allowed, since the risk of adverse reactions may increase.

Pharmacodynamics Meldonium:
Meldonium is a structural analogue of the carnitine precursor gamma-butyrobetaine, a substance found in every cell of the human body. Inhibits gamma butyrobetaine hydroxinase, reduces carnitine synthesis and transport of long-chain
fatty acids through the cell membranes, preventing the accumulation in the cell of activated forms of unoxidized fatty acids, derivatives of acylcarnitine and acyl coenzyme A.
The mechanism of action determines the variety of its pharmacological effects: increased efficiency, reduced symptoms of mental and physical stress, activation of tissue and humoral immunity, cardioprotective effect.

Under conditions of ischemia, Meldonium restores balance between the processes of oxygen delivery and its consumption in cells, prevents disruption of the transport of adenosine triphosphate (ATP), and simultaneously activates glycolysis, which proceeds without additional oxygen consumption. Under conditions of increased load, Meldonium restores the balance between the delivery and demand of cells for oxygen, eliminates the accumulation of toxic metabolic products in cells, protecting them from damage; also has a tonic effect.

As a result of its use, the body acquires the ability to withstand stress and quickly restore energy reserves. Due to these properties, Meldonium is used to treat various disorders of the cardiovascular system, blood supply to the brain, as well as to improve physical and mental performance. Effective in the case of vascular and dystrophic pathology of the vessels of the fundus. In the case of acute ischemic damage to the myocardium, Meldonium slows down the formation of a necrotic zone, shortens the rehabilitation period. Cardioprotective agent, improves metabolism in the myocardium. In case of heart failure, it increases myocardial contractility, increases exercise tolerance, and reduces the frequency of angina attacks. In acute and chronic ischemic disorders of cerebral circulation, meldonium improves blood circulation in the ischemic focus, promotes blood redistribution in favor of the ischemic area. The drug eliminates functional disorders of the nervous system in patients with chronic alcoholism with withdrawal symptoms. The drug Meldonium has a stimulating effect on the central nervous system, increasing motor activity and physical endurance. Due to these properties, Meldonium is used, among other things, to increase physical and mental performance.

Pharmokinetics Meldonium:
After oral administration, meldonium is rapidly absorbed from the gastrointestinal tract. Bioavailability - 78%. The time to reach the maximum concentration in blood plasma is achieved within 1-2 hours after oral administration. It is metabolized mainly in the liver with the formation of two main metabolites, which are excreted by the kidneys. The half-life (T1 / 2) when taken orally depends on the dose, is 3-6 hours. Trace concentrations of the drug remain in the body for a long time.

Indications Meldonium:

In the complex therapy of ischemic heart disease (angina pectoris, myocardial infarction), chronic heart failure and dyshormonal cardiomyopathy;
In the complex therapy of subacute and chronic disorders of the blood supply to the brain (the consequences of stroke, cerebrovascular insufficiency);
Reduced working capacity; mental and physical overload (including among athletes);
Withdrawal syndrome in chronic alcoholism (in combination with specific therapy).

Contraindications Meldonium:

Hypersensitivity to the active substance and other components of the drug, increased intracranial pressure (in case of impaired venous outflow, intracranial tumors), age up to 18 years (efficacy and safety have not been established), pregnancy, breastfeeding period.
Carefully
Caution should be exercised when prescribing Meldonium to patients with liver and / or kidney disease.

Application during pregnancy and during breastfeeding
The safety of using the drug in pregnant women has not been studied, therefore, in order to avoid possible adverse effects on the fetus, the use of the drug in pregnant women is contraindicated.

No data on excretion in breast milk, impact on health

Side effects Meldonium:

According to the World Health Organization (WHO), adverse effects
classified according to their frequency of development as follows: often (> 1/100, <1/10), infrequently (> 1/1000, <1/100), rarely (> 1/10000. <1/1000) and very rarely (<1/10000), including isolated messages: frequency unknown - from the available data, it was not possible to establish the frequency of occurrence.
On the part of the blood and lymphatic system: the frequency is unknown - eosinophilia.
From the immune system: rarely - allergic reactions (skin redness, skin rash, urticaria, itching, swelling, angioedema).
From the side of the heart: very rarely - tachycardia.
From the side of the vessels: rarely - a decrease or increase in blood pressure.
From the gastrointestinal tract: often - dyspeptic symptoms.
From the nervous system: often - headaches, the frequency is unknown - excitement.
General disorders: frequency unknown - general weakness.

Overdose Meldonium:

Cases of overdose of Meldonium have not been reported. Meldonium has low toxicity and does not cause severe adverse reactions.
Symptoms: a decrease in blood pressure, accompanied by headache, tachycardia, dizziness and general weakness.
Treated: symptomatic.
In case of severe overdose, it is necessary to monitor the function of the liver and kidneys.