Cardionate (Meldonium)

The capsules of 250 mg or 500 mg of meldonium dihydrate (trimethylhydrasine propionate dihydrate); Excipients: potato starch, colloidal silicon dioxide (Aerosil), calcium stearate.

Injection solution 100 mg in 1 ml, in 5 ml ampoules.

Pharmacological Effects are cardioprotective and metabolic.

Pharmacodynamics

The synthetic analogue of gamma-butyrobetaine, inhibits gamma-butyrobetaine hydroxylase, reduces the synthesis of carnitine and transport of long-chain fatty acids across cell membranes, prevents the accumulation in the cells of the activated forms of unoxidized fatty acids - derivatives of acylcarnitine and atsilkofermenta A.

Cardioprotective agent normalizing myocardial metabolism. In conditions of ischemia restores the balance of oxygen delivery process and its consumption in the cells, to prevent violations of transport ATP; simultaneously activates glycolysis, which proceeds without the use of supplemental oxygen. As a result of reducing the concentration of carnitine is synthesized hard gamma-butyrobetaine, which has vasodilating properties. The mechanism of action determines the diversity of its pharmacological effects: increasing efficiency, reducing the symptoms of mental and physical stress, tissue and activation of humoral immunity, cardioprotective effects. In the case of acute ischemic myocardial damage slows the formation of necrotic areas, reduces 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, promotes redistribution of blood to the ischemic area. It is effective in the case of vascular and dystrophic pathology of the ocular fundus. It is also characteristic tonic effect on CSN.

Pharmacokinetics

After intake of rapidly absorbed, bioavailability - 78%, in the blood plasma is reached within 1-2 hours after ingestion. It is metabolized in the body into two major metabolites which the kidneys. Tt 2 when administered depends on the dose, it is 6-8 hours.

Indications:

• Meldonium decreased performance, physical stress (including the athletes), post-operative period to accelerate rehabilitation.
• Meldonium for cardialgia on background dyshormonal myocardial dystrophy, as part of combination therapy of coronary heart disease (angina), congestive heart failure.
• Meldonium for violations of cerebral circulation (stroke, cerebrovascular insufficiency). Additionally for solution for injection.
• Acute circulatory disorder in the retina, hemophthalmus and retinal hemorrhages of different etiologies, thrombosis of the central retinal vein and its branches.

Dosage:

Capsules: inside, swallowing whole with water.

In view of the possible development of stimulating effect it is recommended to use in the morning.

By reducing the health and physical overexertion (including the athletes).

Athletes - 0.5-1 g, 2 times daily before training. The duration of the preparatory period - 14-21 days, during the competition -10-14 days.

Adults - 0.5-1 g 1-2 reception. The course -10-14 days. If you want to receive repeated after 2-3 weeks.

Stable Angina - 0.5-1 g per day in one or two divided doses for the first 3-4 days, then - 2 times a week. The course - 4-6 weeks.

Cardialgia amid dyshormonal myocardial dystrophy - 500 mg per day. The course of treatment - 12 days.

Chronic disorders of cerebral circulation - 0.5 grams per day. The course of treatment - 2-3 weeks.

Injection: intravenous, intramuscular, and retrobulbarno subkonyunktivalno.

Increased physical and mental load: intravenously, 1 ml of 10 times a day. The course - 10-14 days. If necessary, repeat the course in 2-3 weeks.

In cardiovascular diseases (in the complex therapy): iv, 5-10 ml solution for injection (500 mg / 5 ml); a course of treatment - 10-14 days.

Drug interactions

It increases the vasodilatig funds, some antihypertensive drugs, cardiac glycosides.

It can be combined with antianginal drugs, anticoagulants, antiplatelet agents, antiarrhythmics, diuretics, bronchodilators ITIC.

In view of the possible development of mild tachycardia and hypotension should be careful in combination with nitroglycerin, nifedipine, alpha-blockers, antihypertensive agents and peripheral vasodilators.