Meldonium - instructions for use, dose, side effects, contraindications

Structural analogues of gamma-butyrobetaine, inhibits gamma butirobetaingidroksinazu, reduces the synthesis of carnitine and transportation of long chain fatty acids across cell membranes and prevents the accumulation of cells in the activated forms of unoxidized fatty acids - acylcarnitine derivatives and atsilkoenzima A. ischemia restores equilibrium processes oxygen delivery and consumption in cells, prevents disruption of transport of adenosine triphosphate (ATP); simultaneously, it activates glycolysis, which proceeds without additional consumption of oxygen. As a result of a decrease in the concentration of carnitine, gamma-butyrobetaine, which has vasodilating properties, is synthesized intensively.The mechanism of action determines the variety of its pharmacological effects: an increase working capacity, reducing the symptoms of mental and physical overstrain, the activation of tissue and humoral immunity, cardioprotective action. In the case of acute ischemic injury, the myocardium slows down the formation of necrotic zone, shortens the rehabilitation period, With cardiac insufficiency increases myocardial contractility, increases exercise tolerance, reduces the incidence of angina attacks. In acute and chronic ischemic disorders of cerebral circulation improves blood circulation in the ischemic focus, promotes redistribution of blood flow in favor of the ischemic site. Effective in the case of vascular and dystrophic pathology of the fundus. Characteristic is also a tonic effect on the central nervous system (CNS). Eliminates functional disorders of somatic and autonomic nervous systems in patients with chronic alcoholism during the period of withdrawal.

Pharmacokinetics:

With intravenous administration, the bioavailability of meldonia is 100%. Maximum concentration of the drug in plasma (C_m_Oh) is achieved immediately after administration.Metabolized with the formation of two major metabolites, which are excreted by the kidneys. The half-life period depends on the dose, is 3-6 hours.

Indications:

- As a part of complex therapy for ischemic heart disease (CHD) (angina pectoris, myocardial infarction), chronic heart failure (CHF), cardiomyopathy against a background of dyshormonal disorders.

- In the complex therapy of acute and chronic disorders of cerebral circulation (stroke, cerebrovascular insufficiency).

- As part of complex therapy for hemophthalmia and hemorrhage into the retina of various etiologies, thrombosis of the central vein of the retina and its branches, retinopathy of various etiologies (including diabetic and hypertensive).

- The syndrome of withdrawal from chronic alcoholism (in combination with a specific therapy of chronic alcoholism).

- Reduced performance, mental and physical overexertion (including athletes).

The drug may give a positive result in the doping control (see section "Special instructions").

Contraindications:

Hypersensitivity to the drug, increased intracranial pressure (with violation of venous outflow and intracranial tumors), pregnancy,period breastfeeding, age under 18 years (due to lack of data on efficiency and safety).

Carefully:

Chronic liver and / or kidney disease.

Pregnancy and lactation:

The safety of use in pregnant women has not been studied, therefore, to avoid possible adverse effects on the fetus, its use is contraindicated. The penetration of meldonia into milk and its effect on the health of the newborn have not been studied, therefore, if necessary, use should stop breastfeeding.

Dosing and Administration:

Intravenously (intravenously), intramuscularly (in / m), parabulbar.

In view of the possible development of an exciting effect, it is recommended to apply the drug in the morning. The method of administration, dose and duration of the course of treatment are set by the doctor individually, depending on the indications, the severity of the condition,

Cardiovascular disease

As part of complex therapy:

- ischemic heart disease (myocardial infarction) in / in jet 0.5 to 1.0 g per day (5-10 ml of the preparation Meldoney), applying the whole dose at once or dividing it into 2 injections;

- ischemic heart disease (stable angina); chronic heart failure and cardiomyopathy against a background of dyshormonal disorders in / in a jet 0.5 to 1.0 g per day (5-10 ml of the preparation Meldoney), applying the entire dose at once or dividing it into 2 injections, the course of treatment 10-14 days, with the subsequent transition to dosage forms for oral administration. The general course of treatment is 4-6 weeks.

Disorders of cerebral circulation

In the complex therapy in the acute phase of 0.5 g (5 ml of the drug Meldoney) 1 time per day iv in the course of 10 days, then switching to oral dosage forms. The general course of treatment is 4-6 weeks.

With chronic insufficiency of cerebral circulation of 0.5 g (5 ml of the drug Meldoney) iv once a day for 10 days, with the subsequent transition to oral dosage forms.

The general course of treatment is 4-6 weeks.

Repeated courses (usually 2-3 times a year) are possible according to the doctor's prescription.

AT ophthalmology (hemophthalmia and hemorrhages in the retina of various etiologies, thrombosis of the central vein of the retina and its branches, retinopathy of various etiologies (diabetic, hypertonic)).

To 0.05 g (0.5 ml of the preparation Meldoney) parabulbar, including in the combination therapy, within 10 days.

Mental and physical overloads

0.5 g (5 ml of the preparation Meldoney) in / m or iv once a day. The course of treatment is 10-14 days. If necessary, the treatment is repeated after 2-3 weeks.

Chronic alcoholism

0.5 g (5 ml of the preparation Meldoney) in / m or iv twice a day. The course of treatment is 7-10 days.

Side effects:

The frequency of adverse reactions is determined by the following categories:

Often (≥ 1/10), often (≥ 1/100, < 1/10), infrequently (≥ 1/1000, <1/100), rarely (≥1 / 10000, < 1/1000), rarely (< 1/10 000).

From the cardiovascular system: rarely - tachycardia, decrease or increase in blood pressure.

From the nervous system: rarely - psychomotor agitation.

From the gastrointestinal tract: rarely - dyspeptic disorders.

From the immune system: allergic reactions - rarely - skin itching, redness of skin, skin rash, angioedema; rarely - eosinophilia.

Common violations: very rarely - general weakness.

Overdose:

Symptoms: decrease in blood pressure, headache, tachycardia, dizziness, general weakness.

Treatment: symptomatic.

Interaction:

You can combine with antianginal drugs, anticoagulants, antiaggregants, antiarrhythmic drugs, diuretics, bronchodilators. Strengthens the coronarodilating and some hypotensive drugs (LS), cardiac glycosides. In view of the possible development of moderate tachycardia and arterial hypotension, caution should be exercised when combined with nitroglycerin, nifedipine, alpha-adrenoblockers, other antihypertensive drugs and peripheral vasodilators.

Special instructions:

Many years of experience in the treatment of acute myocardial infarction and unstable angina in cardiac units shows that Meldoney is not a drug of the 1st row in acute coronary syndrome and its use is not strictly necessary.

From 01/01/2016. meldoon is included in the list of banned substances of the World Anti-Doping Agency.

Effect on the ability to drive transp. cf. and fur:

There is no evidence of adverse effects of the drug Meldoney on the ability to drive vehicles and engage in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Form release / dosage:

Solution for injection 100 mg / ml.

Packaging:

5 ml per ampoule of colorless neutral glass type 1 with a colored break ring or with a colored dot and a notch or without a kink ring, a colored dot and a notch. One, two or three color rings and / or a two-dimensional bar code, and / or alphanumeric coding or without additional color rings, a two-dimensional bar code, and alphanumeric coding can additionally be applied to the ampoules.

By 5, 10 ampoules per contour cell packaging made of polyvinylchloride film and foil of aluminum lacquered or polymer film or without foil and without film. Or 5, 10 ampoules are placed in a preformed form (tray) made of cardboard with cells for laying ampoules.

1 or 2 contour cellular packs or cardboard trays, together with the instruction for use and the ampoule ampoule or ampoule scarifier, or without the ampoule ampoule ampoule scraper and ampoule ampoule are placed in cardboard packing (bundle).

Storage conditions:

In the dark place at a temperature of no higher than 25⁰C. Do not freeze.

Keep out of the reach of children.

Shelf life:

3 years. Do not use the drug after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:LP-004141

Date of registration:13.02.2017

Expiration Date:13.02.2022

The owner of the registration certificate:ATOLL, LLC ATOLL, LLC Russia

Manufacturer: & nbsp

OZONE, LLC Russia

Information update date: & nbsp24.03.2017

Illustrated instructions

Instructions

Meldoney (Meldonium)