Cardionate^® (Capsules, Solution) Instructions for Use

ATC Code

C01EB22 (Meldonium)

Active Substance

Meldonium (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Metabolic drug

Pharmacotherapeutic Group

Metabolic agent

Pharmacological Action

A drug that improves metabolism and energy supply to tissues, a synthetic analogue of gamma-butyrobetaine. It inhibits gamma-butyrobetaine hydroxylase, reduces the synthesis of carnitine and the transport of long-chain fatty acids across cell membranes, and prevents the accumulation of activated forms of non-oxidized fatty acids – acyl carnitine and acyl coenzyme A derivatives – in cells.

A cardioprotective agent that normalizes myocardial metabolism. Under ischemic conditions, it restores the balance between oxygen delivery and its consumption in cells and prevents disruption of ATP transport; at the same time, it activates glycolysis, which proceeds without additional oxygen consumption.

As a result of the decrease in carnitine concentration, gamma-butyrobetaine, which has vasodilating properties, is synthesized more intensively. The mechanism of action determines the variety of its pharmacological effects: increased performance, reduction of symptoms of mental and physical overstrain, activation of tissue and humoral immunity, cardioprotective action.

In the case of acute ischemic myocardial damage, it slows down the formation of the necrotic zone and shortens the rehabilitation period. In heart failure, it increases myocardial contractility, increases tolerance to physical activity, and reduces the frequency of angina attacks.

In acute and chronic cerebral circulation disorders, it improves blood circulation in the ischemic focus and promotes blood redistribution in favor of the ischemic area. It is effective in cases of vascular and dystrophic pathology of the fundus. A tonic effect on the central nervous system is also characteristic, as well as the elimination of functional disorders of the somatic and autonomic nervous systems in patients with chronic alcoholism during withdrawal syndrome.

Pharmacokinetics

Absorption

After oral administration, it is rapidly absorbed from the gastrointestinal tract. C_max in blood plasma is reached in 1-2 hours. Bioavailability is 78%.

Metabolism and Excretion

It is metabolized in the body to form two main metabolites, which are excreted by the kidneys. T_1/2 after oral administration is dose-dependent and is 3-6 hours.

Indications

• Reduced performance;
• Physical overstrain (including in athletes);
• Postoperative period to accelerate rehabilitation;
• As part of combination therapy for coronary artery disease (angina pectoris), chronic heart failure, cardialgia against the background of dishormonal myocardial dystrophy;
• Alcohol withdrawal syndrome (in combination with specific therapy);
• Cerebrovascular circulation disorders (stroke, cerebrovascular insufficiency).

ICD codes

Dosage Regimen

Capsules

Due to the possible development of a stimulating effect, it is recommended to use it in the first half of the day.

For reduced performance and physical overstrain (including in athletes), it is prescribed orally at 250 mg 4 times/day. The course of treatment is 10-14 days. If necessary, the treatment is repeated after 2-3 weeks.

Athletes are prescribed orally 0.5-1 g 2 times/day before training. The duration of the course in the preparatory period is 14-21 days, during the competition period – 10-14 days.

For stable angina pectoris, 250 mg is prescribed 3 times/day for the first 3-4 days, then 250 mg 3 times/day 2 times/week.

For cardialgia against the background of dishormonal myocardial dystrophy – 250 mg 2 times/day (morning and evening). The course of treatment is 12 days.

For chronic alcoholism – 500 mg 4 times/day. The course of treatment is 7-10 days.

For chronic cerebrovascular circulation disorders – 0.5-1 g/day, preferably in the first half of the day. The course of treatment is 2-3 weeks.

The capsules are swallowed whole with water.

Solution

Increased mental and physical stress: IV 1 g (10 ml) 1 time/day. The course of treatment is 10-14 days. If necessary, the course is repeated after 2-3 weeks.

For cardiovascular diseases (as part of complex therapy): IV 0.5-1 g (5-10 ml); the course of treatment is 10-14 days.

Cerebrovascular circulation disorder: acute phase – IV 500 mg (5 ml) 1 time/day for 7-10 days, then switch to oral administration.

Chronic cerebrovascular insufficiency: IM 500 mg (5 ml) 1 time/day. The course of treatment is 10-14 days, then switch to oral administration.

Chronic alcoholism: IV – 500 mg (5 ml) 2 times/day. The course of treatment is 7-10 days.

Vascular pathology of the fundus and retinal dystrophy: retrobulbar and subconjunctival administration of 50 mg (0.5 ml of injection solution) for 10 days.

Adverse Reactions

From the cardiovascular system rarely – tachycardia, decreased blood pressure.

Allergic reactions rarely – redness, rash, itching, swelling.

Other rarely – dyspepsia, agitation.

Contraindications

• Increased intracranial pressure (in case of impaired venous outflow, intracranial tumors);
• Age under 18 years (efficacy and safety have not been established);
• Hypersensitivity to the components of the drug.

With caution, the drug should be used for liver and/or kidney diseases.

Use in Pregnancy and Lactation

The safety of the drug during pregnancy has not been proven. To avoid possible adverse effects on the fetus, Cardionate^® should not be prescribed during pregnancy.

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

Use in Hepatic Impairment

With caution, the drug should be used for liver diseases.

Use in Renal Impairment

Use the drug with caution for a long time in patients with chronic kidney diseases.

Pediatric Use

Contraindication: age under 18 years (efficacy and safety have not been established).

Special Precautions

Use the drug with caution for a long time in patients with chronic liver and kidney diseases.

Use in pediatrics

There is insufficient data on the use of Cardionate^® in children.

Effect on the ability to drive vehicles and machinery

There are no data on the adverse effect of the drug on the speed of psychomotor reactions.

Overdose

Cases of Cardionate^® overdose are unknown. The drug is low-toxic and does not cause side effects dangerous to the health of patients.

Drug Interactions

It enhances the effect of coronary vasodilators, some antihypertensive agents, and cardiac glycosides.

It can be combined with antianginal agents, anticoagulants and antiplatelet agents, antiarrhythmic agents, diuretics, and bronchodilators.

Due to the possible development of moderate tachycardia and arterial hypotension, caution should be exercised when combining with nitroglycerin, nifedipine, alpha-blockers, antihypertensive agents, and peripheral vasodilators.

Storage Conditions

List B. The drug should be stored out of the reach of children, in a dry place at a temperature not exceeding 25°C (77°F).

Shelf Life

Shelf life – 3 years.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.