Meldonium is a cardioprotective and anti-ischemic agent indicated for the improvement of energy metabolism in cells subjected to ischemia or hypoxia. Its primary mechanism of action involves the modulation of carnitine biosynthesis, shifting cellular energy production from fatty acid oxidation to the more oxygen-efficient glycolysis. This pharmacological profile makes it a valuable therapeutic option in a range of cardiovascular and neurological conditions where compromised blood flow leads to cellular energy deficits. It is a prescription medication that requires careful patient assessment and monitoring under expert medical supervision.

Features

• Active Pharmaceutical Ingredient: Meldonium dihydrate
• Pharmacotherapeutic Group: Other cardiac preparations, ATC code: C01EB22
• Standard Tablet Strength: 500 mg
• Primary Mechanism: Inhibition of gamma-butyrobetaine hydroxylase, reducing L-carnitine synthesis
• Bioavailability: Approximately 78% following oral administration
• Elimination Half-Life: Approximately 3-6 hours
• Protein Binding: Low
• Primary Excretion Route: Renal

Benefits

• Enhances myocardial tolerance to ischemia by reducing the heart’s reliance on oxygen-intensive fatty acid oxidation.
• Improves physical capacity and functional status in patients with chronic heart failure and stable angina pectoris.
• Supports neurological recovery and reduces the area of ischemic damage following acute cerebrovascular incidents.
• Promotes efficient glucose utilization under hypoxic conditions, providing a protective metabolic shift for vulnerable tissues.
• Contributes to the normalization of microcirculation and hemodynamics in affected vascular beds.
• Aids in the reduction of symptoms associated with compromised blood flow, such as exercise intolerance and fatigue.

Common use

Meldonium is clinically prescribed for the treatment and management of conditions characterized by insufficient blood supply (ischemia) to vital organs. Its most common application is within the field of cardiology. It is indicated for patients with chronic heart failure (NYHA Class II-III), stable angina pectoris, and myocardial infarction in complex therapy. In neurology, it is used during the recovery phase following ischemic strokes and transient ischemic attacks (TIAs) to support neurological function. It is also utilized in ophthalmology for treating retinal vascular occlusions and dystrophies, and in cases of reduced work capacity, physical overstrain, and post-surgical recovery to improve patient resilience and convalescence.

Dosage and direction

The dosage of meldonium must be individualized based on the patient’s clinical condition, severity of disease, and therapeutic response. Treatment is typically initiated and supervised by a physician.

• Standard Adult Dosage: The usual oral dose is 500 mg - 1,000 mg (one to two 500 mg tablets) taken once or twice daily.
• Course of Treatment: The duration of therapy typically ranges from 4 to 6 weeks. Treatment courses may be repeated 2-3 times per year, as determined by a healthcare provider.
• Administration: Tablets should be swallowed whole with a sufficient amount of water. They can be taken with or without food, though consistency in administration relative to meals is advised.
• Timing: Due to its potential central nervous system effects, it is not recommended to take the medication later than 5 PM to avoid possible interference with sleep.
• Intravenous Use: In hospital settings for acute conditions, an intravenous formulation may be used initially, followed by a transition to oral maintenance therapy.

Always follow the specific dosage and administration instructions provided by the prescribing physician.

Precautions

• Renal Impairment: Use with caution in patients with renal dysfunction. Dose adjustment may be necessary due to the primary renal route of excretion.
• Hepatic Impairment: Although not extensively studied, caution is advised in patients with severe liver disease.
• Elderly Patients: Older patients may be more sensitive to the effects of the drug. A lower dose may be indicated, especially in the presence of age-related renal decline.
• Pregnancy and Lactation: The safety of meldonium during pregnancy and breastfeeding has not been established. Use is only permissible if the potential benefit justifies the potential risk to the fetus or infant, as decided by a physician.
• Driving and Operating Machinery: Patients should exercise caution, as the drug may occasionally cause dizziness or a transient drop in blood pressure, which could affect the ability to perform hazardous activities.

Contraindications

Meldonium is contraindicated in patients with known hypersensitivity to the active substance or any of the excipients in the formulation. Its use is also contraindicated in:

• Severe hepatic impairment.
• Severe renal impairment.
• Conditions associated with increased intracranial pressure (e.g., intracranial tumors, disturbances of venous outflow).
• Pediatric Population: Safety and efficacy in children and adolescents under 18 years of age have not been established.

Possible side effect

Meldonium is generally well-tolerated. Adverse reactions are usually mild and transient. The frequency categories are defined as: very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1,000 to <1/100), rare (≥1/10,000 to <1/1,000).

• Immune System Disorders: Uncommon: allergic reactions (skin rash, pruritus, erythema, edema).
• Nervous System Disorders: Common: psychomotor agitation; Uncommon: headache, dizziness, sleep disturbances (insomnia or drowsiness), tremor, paresthesia.
• Cardiac Disorders: Uncommon: palpitations, tachycardia, blood pressure fluctuations (most commonly a decrease).
• Gastrointestinal Disorders: Common: dyspepsia; Uncommon: nausea, vomiting, diarrhea, abdominal pain.
• General Disorders: Common: asthenia (weakness); Uncommon: feeling of heat.

Drug interaction

Formal interaction studies are limited. However, interactions are theoretically possible based on its pharmacological action.

• Other Cardiovascular Agents: Meldonium may potentiate the effects of antianginal drugs (e.g., nitrates, beta-blockers, calcium channel blockers), antihypertensives, and other peripheral vasodilators. This can lead to additive hypotensive and bradycardic effects, requiring careful monitoring of heart rate and blood pressure.
• Substrates of OCTN2 Transporter: As meldonium may influence carnitine-dependent processes, it could potentially interact with other drugs that are substrates of the organic cation transporter novel type 2 (OCTN2).
• Alcohol: Concomitant use with alcohol is not recommended due to a potential increase in the risk of adverse cardiovascular and central nervous system effects.

Patients must inform their doctor of all medications they are taking, including prescription, over-the-counter, and herbal products.

Missed dose

If a dose is missed, it should be taken as soon as remembered. However, if it is almost time for the next scheduled dose, the missed dose should be skipped. A double dose should not be taken to make up for the missed one. Patients should not alter the dosage regimen without consulting their physician.

Overdose

Cases of overdose with meldonium have been rarely reported. Based on its pharmacological profile, symptoms of significant overdose may include a pronounced decrease in blood pressure (hypotension), tachycardia, dizziness, headache, general weakness, and asthenia. There is no specific antidote. Treatment should be symptomatic and supportive, including monitoring of vital signs and ECG. Gastric lavage may be considered if ingestion was recent.

Storage

• Store in the original package to protect from light and moisture.
• Keep at a temperature not exceeding 25°C (77°F).
• Keep out of the sight and reach of children.
• Do not use the medicine after the expiration date printed on the packaging.

Disclaimer

This information is provided for educational and informational purposes only and does not constitute medical advice. It is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or before starting any new treatment. Never disregard professional medical advice or delay in seeking it because of something you have read here. The efficacy and safety profile described are based on general product characteristics and may not apply to every individual.

Reviews

• “As a cardiologist, I have incorporated meldonium into the management plan for select patients with stable angina and Class II heart failure. The most notable outcome is the reported improvement in exercise tolerance and reduction in angina episodes. It serves as a useful adjunct therapy, particularly for patients who remain symptomatic on standard regimens.” – Cardiologist, 15 years of experience
• “We utilize meldonium in our neurology department during the subacute phase of ischemic stroke recovery. While not a first-line thrombolytic, its metabolic action appears to support rehabilitation efforts. Patients often show a more favorable trajectory in regaining motor and cognitive functions compared to historical controls, though more robust data is always welcome.” – Neurologist
• “Patient feedback often highlights a noticeable decrease in fatigue and shortness of breath during daily activities. It’s important to manage expectations and emphasize that this is part of a comprehensive lifestyle and pharmacological management plan.” – Clinical Nurse Specialist, Heart Failure Clinic
• “From a clinical pharmacology perspective, the drug’s mechanism is intellectually compelling—forcing a metabolic shift to spare oxygen. Its tolerability profile is favorable, which is crucial for long-term management of chronic conditions. However, its placement in treatment guidelines varies significantly between regions.” – Clinical Pharmacologist