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

Analogue of gamma-butyrobetaine, suppresses gamma-butyrobetaine hydroxynase, reduces synthesis of carnitine and transport of long chain fatty acids through cell membranes, prevents the accumulation of activated forms of unoxidized fatty acids - acylcarnitine and acylcoenzyme A in cells. Under conditions of ischemia, the equilibrium of oxygen delivery and consumption in cells, prevents disruption of the transport of adenosine triphosphate (ATP); simultaneously, it activates glycolysis, which proceeds without additional consumption of oxygen. AT 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: increasing efficiency, reducing the symptoms of mental and physical overstrain, the activation of tissue and humoral immunity, cardioprotective action. In the case of acute ischemic damage, the myocardium slows the formation of the necrotic zone, shortens the rehabilitation period. With heart failure (CH) increases myocardial contractility, increases exercise tolerance, reduces the frequency of angina attacks. In acute and chronic ischemic disorders of cerebral circulation improves blood circulation in the ischemic focus, promotes redistribution of blood 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), the elimination of functional disorders of the somatic and autonomic nervous systems in alcoholics during the period of abstinence.

Pharmacokinetics:

The maximum concentration of the drug in plasma (CmAch) is achieved in 1 to 2 hours. It is metabolized in the body with the formation of 2 main metabolites, which are excreted by the kidneys. The half-life of the preparation (T1 / 2) is 3-6 hours.

Indications:

Reduced performance, physical overexertion (including athletes).

As part of complex therapy:

- ischemic heart disease (CHD) (angina pectoris, myocardial infarction), chronic heart failure (CHF), cardialgia against the background of dyshormonal myocardial dystrophy.

- disorders of the blood supply to the brain (stroke, cerebrovascular insufficiency).

- 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).

Abstinence alcohol syndrome (in combination with specific therapy).

Contraindications:

Hypersensitivity, increased intracranial pressure (with violation of venous outflow and intracranial tumors), pregnancy, lactation. Not applicable in children under 18 due to lack of data.

Carefully:

Chronic liver and kidney disease.

Pregnancy and lactation:

Safety of use in pregnancy is not proven.To avoid possible adverse effects on the fetus, the drug should not be administered during pregnancy.

It is not known whether the drug is excreted in breast milk. If it is necessary to apply meldonia during lactation, breastfeeding should be discontinued.

Dosing and Administration:

Intravenous, intramuscular, parabulbar.

The drug should be used in the morning due to the possible exciting effect.

Mental and physical overloads (including athletes): intravenously, 500 mg once a day. The course of treatment is 10-14 days. If necessary, repeat the treatment after 2-3 weeks.

Unstable angina and myocardial infarction: intravenously sprayed, 0.5-1 g per day. A daily dose can be administered in 1 or 2 doses. The course of treatment is 10-14 days.

Chronic heart failure: intravenously struyno 0.5-1 g once a day or intramuscularly 500 mg 1-2 times a day, the course of treatment 10-14 days, then switch to oral intake.

Cardialgia against the background of dyshormonal myocardial dystrophy: intravenously strontium 0.5-1 g once a day or intramuscularly 500 mg 1 -2 times a day, the course of treatment 10-14 days, then switch to oral administration.An abstinent alcoholic syndrome: 500 mg intravenously twice a day. The course of treatment is 7-10 days.

Violation of cerebral circulation:

- acute phase of cerebrovascular pathology: intravenously, 500 mg once a day for 10 days, then switch to oral administration.

- chronic disorders of cerebral circulation: intramuscularly 500 mg once a day, preferably in the morning.

The course of treatment - 10 days, then switch to oral intake.

Vascular pathology of the fundus and dystrophy of the retina (hemophthalmia and hemorrhage into the retina of various etiologies, thrombosis of the central vein of the retina and its branches): 50 mg (0.5 ml) of the drug solution are parabulbarically injected for 10 days.

Side effects:

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

Very often (≥ 1/10), often (≥ 1/100, <1/10), infrequently (≥ 1/1000, <1/100), rarely (≥ 1/10 000, <1/1000), very rarely (<1/10 000).

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

From the side of the central nervous system: rarely - psychomotor agitation.

From the digestive system: rarely - dyspeptic disorders.

Allergic reactions: rarely - itching, redness, skin rash, swelling; very rarely - eosinophilia.

Other: very rarely - general weakness.

Overdose:

Symptoms: lowering blood pressure, headache, tachycardia, dizziness, general weakness.

Treatment: symptomatic.

Interaction:

Strengthens the coronarodilating and some hypotensive drugs (LS), cardiac glycosides. You can combine with antianginal drugs, anticoagulants, antiaggregants, antiarrhythmic drugs, diuretics, bronchodilators. In view of the possible development of moderate tachycardia and arterial hypotension, caution should be exercised when combined with nitroglycerin, nifedipine, alpha-adrenoblockers, 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 trimethylhydrazinium propionate dihydrate is not the first-line preparation in acute coronary syndrome and its use is not an urgent need.

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

There is no evidence of adverse effects of the drug Meldoney on the reaction rate.

Form release / dosage:

Solution for injection 100 mg / ml.

Packaging:

5 ml into ampoules of colorless neutral glass.

5 ampoules are placed in a contour cell pack. 1 or 2 contour squares are placed in a pack of cardboard.

5, 10 ampoules are placed in a pack of cardboard with baffles or lattices, or a separator made of cardboard or sack paper.

10 ampoules are placed in a box of cardboard.

In each pack or box, put the instructions for use and the ampoule scaler. When using ampoules with an incision, a ring of fracture or a break point, the ampoule scaper is not inserted.

Storage conditions:

In the dark place at a temperature of no higher than 25 ° C. Do not freeze. Keep out of the reach of children.

Shelf life:

4 years.

Do not use after the expiry date shown on the package.

Terms of leave from pharmacies:On prescription

Registration number:LP-002595

Date of registration:21.08.2014 / 12.09.2017

Expiration Date:21.08.2019

The owner of the registration certificate:BIOCHEMIST, OJSC BIOCHEMIST, OJSC Russia

Manufacturer: & nbsp

BIOCHEMIST, OJSC Russia

Information update date: & nbsp23.04.2018

Illustrated instructions

Instructions

Meldoney (Meldonium)