Meldonium

When ATH:
C01EB

The pharmacological action of mel′doniâ

Means, improve metabolism, analog of gamma-butyrobetaine. Suppresses gamma butirobetaingidroksinazu, inhibits the synthesis of carnitine and transport of long-chain fatty acids through cell membranes, препятствует накоплению в клетках активированных форм неокисленных жирных кислот – производных ацилкарнитина и ацилкоэнзима А.

The ischemia restores equilibrium processes oxygen delivery and consumption in cells, to prevent violations of transport ATP; simultaneously activates glycolysis, which proceeds without additional consumption of oxygen. As a result of reducing the concentration of carnitine is synthesized hard gamma-butyrobetaine, vasodilating properties. The mechanism of action determines the diversity of its pharmacological effects: increase efficiency, reducing the symptoms of the mental and physical stress, activation of tissue and humoral immunity, cardioprotective effect.

In the case of acute ischemic myocardial damage slows the formation of necrotic zone, shortens the rehabilitation period. In heart failure, increases myocardial contractility, increases exercise tolerance, reduces the frequency of angina attacks. In acute and chronic ischemic cerebrovascular disorders improves blood circulation in the ischemic focus, It promotes redistribution of blood to the ischemic area. Effective with vascular and dystrophic pathology of the fundus. It has a tonic effect on the CNS, eliminates functional disorders of the nervous system in patients with chronic alcoholism during abstinence syndrome.

Pharmacokinetics mel′doniâ

After intake of rapidly absorbed from the gastrointestinal tract. Bioavailability is about 78%. Cmax in plasma achieved through 1-2 h after administration. Biotransformed in the body to form two major metabolites, that the kidneys. T1 / 2 is 3-6 hours and was dose-dependent.

Indications for use mel′doniâ

For intake or / in the introduction: in the complex treatment of coronary artery disease (angina, myocardial infarction), chronic heart failure, dyshormonal cardiomyopathy; in the complex therapy of acute and chronic disorders of cerebral circulation (strokes and cerebrovascular insufficiency); reduced working capacity, physical strain (incl. athletes), postoperative period to accelerate the rehabilitation; abstinence syndrome in chronic alcoholism (in combination with a specific treatment of alcoholism).

For parabulbarnom: acute circulatory disorder in the retina, hemophthalmus and retinal hemorrhages of different etiologies, thrombosis of the central retinal vein and its branches, retinopathy of different etiology (incl. Diabetic and hypertensive) – только для парабульбарного введения.

Dosage mel′doniâ

In connection with the possibility of exciting effect it is recommended to use in the first half of the day. The dose is determined individually depending on indications and route of administration.

If ingestion of a single dose 0.25-1 g, dosing frequency and duration of treatment depend on the evidence.

The on / in a dose of 0.5-1 g 1 time /, treatment duration depends on indication.

Parabulbarno administered by 0.5 ml injection solution with a concentration of 500 mg / 5 ml for 10 days.

Side effects of mel′doniâ

Cardio-vascular system: rarely - tachycardia, changes in blood pressure.

CNS: редко – психомоторное возбуждение.

From the digestive system: редко – диспептические симптомы.

Allergic reactions: редко – кожный зуд, redness, rash, edema.

Contraindications mel′doniâ

Increased intracranial pressure (incl. in violation of the venous outflow, intracranial tumors), pregnancy, lactation (breast-feeding), Hypersensitivity to meldonium.

Pregnancy and lactation and reception mel′doniâ

During pregnancy and lactation (breast-feeding) use of the drug is contraindicated.

Special instructions when taking mel′doniâ

Be wary of in diseases of the liver and / or kidney, especially for a long time.

Many years of experience in the treatment of acute myocardial infarction and unstable angina in the cardiology departments shows, meldonium that is not a first-line agent for acute coronary syndrome.

Use of mel′doniâ in Pediatrics

In children and adolescents under the age of 18 s effectiveness and safety has not been established meldonium.

Meldonium in capsule form is contraindicated for use in children and adolescents under the age of 18 years; в форме сиропа – у детей в возрасте до 12 years.

Prescribed drug interaction mel′doniâ

In a joint application meldonium enhances the action of antianginal drugs, Some antihypertensive drugs, cardiac glycosides.

In an application with nitroglycerin meldonium, nifedipine, Alpha-blockers, antihypertensive agents and peripheral vasodilators may develop mild tachycardia, hypotension (when these combinations require careful).