Meldonat-Lekpharm (Solution) Instructions for Use

Marketing Authorization Holder

Lekpharm, SOOO (Republic of Belarus)

ATC Code

C01EB (Other drugs for the treatment of heart diseases)

Active Substance

Meldonium (Rec.INN registered by WHO)

Dosage Form

Meldonat-Lekpharm

Solution for injection 100 mg/1 ml: amp. 5 ml 5 or 10 pcs.

Dosage Form, Packaging, and Composition

Solution for injection transparent, colorless.

Excipients : water for injections – up to 1 ml.

5 ml – ampoules made of colorless glass (5) – blister packs (1) – cardboard boxes.
5 ml – ampoules made of colorless glass (5) – blister packs (2) – cardboard boxes.

Clinical-Pharmacological Group

A drug that improves tissue metabolism and energy supply

Pharmacotherapeutic Group

Metabolic agent

Pharmacological Action

A metabolic-improving agent, an analog of gamma-butyrobetaine. It inhibits gamma-butyrobetaine hydroxylase, suppresses 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 – derivatives of acylcarnitine and acylcoenzyme A – in cells.

Under ischemic conditions, it restores the balance between oxygen delivery and its consumption in cells, prevents disruption of ATP transport; simultaneously, it activates glycolysis, which proceeds without additional oxygen consumption.

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

In 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 load, and reduces the frequency of angina attacks.

In acute and chronic ischemic cerebrovascular disorders, it improves blood circulation in the ischemic focus and promotes blood redistribution in favor of the ischemic area. It is effective in vascular and dystrophic pathologies of the ocular fundus. It has a tonic effect on the CNS and eliminates functional disorders of the nervous system in patients with chronic alcoholism during withdrawal syndrome.

Pharmacokinetics

After oral administration, it is rapidly absorbed from the gastrointestinal tract. The bioavailability is about 78%. C_max in plasma is reached 1-2 hours after administration. It is biotransformed in the body with the formation of two main metabolites, which are excreted by the kidneys. T_1/2 is 3-6 hours and depends on the dose.

Indications

For intravenous administration: as part of complex therapy for coronary artery disease (angina pectoris, myocardial infarction), chronic heart failure, dishormonal cardiomyopathy; as part of complex therapy for acute and chronic cerebrovascular disorders (strokes and cerebrovascular insufficiency); decreased performance, physical overstrain (including in athletes), postoperative period to accelerate rehabilitation; withdrawal syndrome in chronic alcoholism (in combination with specific therapy for alcoholism).

For parabulbar administration: acute circulatory disorders in the retina, hemophthalmos and retinal hemorrhages of various etiologies, thrombosis of the central retinal vein and its branches, retinopathies of various etiologies (including diabetic and hypertensive).

ICD codes

Dosage Regimen

Administer the drug intravenously or via parabulbar injection, depending on the diagnosed condition.

For intravenous administration, use a dose of 0.5-1 g (5-10 ml) once daily.

For cardiovascular conditions (angina pectoris, myocardial infarction, chronic heart failure), administer 0.5-1 g IV once daily for 4-6 weeks.

For cerebrovascular disorders (acute strokes, chronic insufficiency), administer 0.5 g IV once daily for a total treatment course of 4-6 weeks.

For reduced performance or physical overstrain, including in athletes, administer 0.5 g IV once daily for 10-14 days; if necessary, treatment can be repeated after a 2-3 week interval.

For the postoperative period to accelerate rehabilitation, administer 0.5-1 g IV once daily for 7-10 days or as determined by the patient’s condition.

For withdrawal syndrome in chronic alcoholism, administer 0.5 g IV once daily for 7-10 days as part of a comprehensive therapy regimen.

For parabulbar administration in retinal and vitreous disorders, inject 0.5 ml of the 100 mg/ml solution once daily for 10 days.

Adjust the duration of therapy individually based on the disease severity and clinical response.

Adverse Reactions

Cardiovascular system rarely – tachycardia, changes in blood pressure.

Central nervous system rarely – psychomotor agitation.

Digestive system rarely – dyspeptic symptoms.

Allergic reactions rarely – skin itching, redness, rash, edema.

Contraindications

Increased intracranial pressure (including in cases of impaired venous outflow, intracranial tumors), pregnancy, lactation period (breastfeeding), children and adolescents under 18 years of age, hypersensitivity to meldonium.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and breastfeeding.

Use in Hepatic Impairment

Use with caution in liver diseases, especially for a long period of time.

Use in Renal Impairment

Use with caution in kidney diseases, especially for a long period of time.

Pediatric Use

In children and adolescents under 18 years of age, the efficacy and safety of meldonium have not been established.

Special Precautions

Use with caution in liver and/or kidney diseases, especially for a long period of time.

Long-term experience in treating acute myocardial infarction and unstable angina in cardiology departments shows that Meldonium is not a first-line agent for acute coronary syndrome.

Drug Interactions

When used concomitantly, Meldonium enhances the effect of antianginal agents, some hypotensive drugs, and cardiac glycosides.

With simultaneous use of meldonium with nitroglycerin, nifedipine, alpha-adrenoblockers, antihypertensive agents, and peripheral vasodilators, the development of moderate tachycardia and arterial hypotension is possible (caution is required with these combinations).

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

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.