Meldonium

Meldonium is a cardioprotective and anti-ischemic agent belonging to the class of fatty acid oxidation inhibitors. Its primary mechanism of action involves the modulation of carnitine biosynthesis, shifting cellular energy production from fatty acid β-oxidation to the more oxygen-efficient glycolysis. This results in enhanced protection of cells under ischemic conditions, improved metabolic efficiency, and support for physical and mental performance during periods of elevated stress or hypoxia. It is a well-researched pharmaceutical compound with a defined clinical profile, primarily indicated for conditions related to compromised blood flow and energy metabolism.

Features

• Active Pharmaceutical Ingredient: Meldonium dihydrate
• Pharmacotherapeutic group: Other cardiac preparations, ATC code: C01EB22
• Mechanism: Inhibitor of gamma-butyrobetaine hydroxylase, reducing L-carnitine synthesis
• Standard formulations: 250 mg and 500 mg capsules; 500 mg/5 mL syrup
• Bioavailability: Approximately 78% following oral administration
• Half-life: 3-6 hours in healthy individuals
• Metabolism: Minimally hepatic, primarily excreted renally unchanged

Benefits

• Enhances myocardial tolerance to ischemia by optimizing oxygen utilization in cardiac tissue
• Improves physical capacity and reduces symptoms of fatigue in patients with chronic heart failure and stable angina pectoris
• Supports recovery of central nervous system functions following cerebrovascular incidents
• Provides metabolic support during periods of high physical and psychological stress
• May improve exercise tolerance in athletes under hypoxic conditions (note: WADA prohibited substance in competition)
• Contributes to stabilization of endothelial function and microcirculation

Common use

Meldonium is clinically indicated for the complex therapy of cardiovascular diseases, including chronic heart failure (NYHA Class I-III), stable angina pectoris, and myocardial infarction during the rehabilitation phase. It is also utilized in neurology for the recovery period following ischemic cerebrovascular accidents and for treating reduced performance, physical and psychoemotional overstrain. Its application extends to ophthalmology for vascular disorders of the retina and choroid. Off-label use has been documented in sports medicine, though this remains controversial and is prohibited by most athletic governing bodies during competition periods.

Dosage and direction

The standard adult dosage is 500 mg - 1000 mg per day, divided into 1-2 administrations. For cardiovascular indications, the typical regimen is 250 mg capsules taken three times daily or 500 mg capsules taken twice daily. The maximum daily dose should not exceed 2000 mg. Treatment duration varies from 4-6 weeks for performance recovery to several months for chronic cardiac conditions. Administration should occur with meals to improve gastrointestinal tolerance. Dosage adjustment is recommended for patients with renal impairment (creatinine clearance <60 mL/min). Treatment should be initiated under medical supervision with periodic evaluation of therapeutic response.

Precautions

Exercise caution in patients with hepatic or renal impairment, requiring appropriate dose adjustments and monitoring of renal function. Use with care in elderly patients due to potential age-related decreases in renal function. Meldonium may affect the ability to drive or operate machinery, particularly during the initial treatment phase, until individual response is established. Regular monitoring of blood pressure and heart rate is advised during therapy. Patients should be advised to avoid concomitant consumption of alcohol due to potential additive effects on the central nervous system. The safety profile during pregnancy and lactation has not been established—use only if potential benefits outweigh risks.

Contraindications

Hypersensitivity to meldonium or any excipients in the formulation; severe hepatic impairment (Child-Pugh Class C); end-stage renal disease (creatinine clearance <30 mL/min); intracranial hypertension due to impaired venous outflow; acute myocardial infarction with hemodynamic instability; pregnancy and breastfeeding unless explicitly indicated by a healthcare professional after careful risk-benefit assessment. Concomitant use with other medications that significantly affect carnitine metabolism is not recommended.

Possible side effect

The most commonly reported adverse reactions (≥1/100 to <1/10) include: tachycardia, blood pressure fluctuations (both hypertension and hypotension), headache, dizziness, nervous excitation, dyspepsia, allergic skin reactions (rash, pruritus, erythema). Less frequent side effects (<1/100) may comprise: eosinophilia, agitation, general weakness, heaviness in the head. In rare instances (<1/1000), cases of angioedema and urticaria have been reported. Most adverse effects are mild to moderate in intensity and typically diminish with continued treatment or dose reduction.

Drug interaction

Meldonium may potentiate the effects of antianginal drugs, antihypertensives, cardiac glycosides, and other cardioprotective agents. Concurrent administration with drugs that affect carnitine metabolism (such as valproic acid) may require dosage adjustments. Caution is advised when co-administering with central nervous system depressants due to potential additive sedative effects. Meldonium may enhance the vasodilatory effects of nitrates and calcium channel blockers. No significant interactions with cytochrome P450 enzymes have been documented, but monitoring is recommended when used with narrow therapeutic index drugs.

Missed dose

If a dose is missed, it should be taken as soon as remembered unless it is nearly time for the next scheduled dose. In that case, skip the missed dose and resume the regular dosing schedule. Do not double the dose to make up for a missed administration. Maintaining consistent plasma concentrations is important for optimal therapeutic effect, so patients should strive for regular dosing intervals. If multiple doses are missed, consult a healthcare provider for guidance on resuming therapy.

Overdose

Cases of overdose are rare. Symptoms may include pronounced hypotension, tachycardia, headache, dizziness, general weakness, and nervous excitation. In severe cases, cardiac arrhythmias may occur. There is no specific antidote. Treatment should be symptomatic and supportive, including gastric lavage if ingestion occurred recently, activated charcoal administration, and monitoring of vital signs. Hemodialysis may be considered in severe cases due to the drug’s renal excretion profile. Cardiovascular parameters should be closely monitored until stabilization is achieved.

Storage

Store in original packaging at temperatures not exceeding 25°C (77°F). Protect from light and moisture. Keep out of reach of children. Do not use after the expiration date printed on the packaging. Once the bottle is opened, use within the period specified by the manufacturer (typically 30-60 days for capsules, 14 days for syrup after opening). Do not freeze the liquid formulation. Proper storage conditions are essential for maintaining pharmaceutical stability and efficacy.

Disclaimer

This information is provided for educational purposes only and does not constitute medical advice. Meldonium is a prescription medication that should only be used under the supervision of a qualified healthcare professional. The prescribing physician should be consulted for diagnosis, dosage recommendations, and treatment decisions. Individual response to therapy may vary. Patients should not discontinue or modify treatment without medical consultation. Regulatory status may vary by country—users are responsible for complying with local regulations regarding possession and use.

Reviews

Clinical studies demonstrate meldonium’s efficacy in improving exercise tolerance in patients with chronic heart failure (average improvement of 25-30% in treadmill test duration) and reducing angina attacks frequency by approximately 50% in stable angina patients. Neurological applications show improved cognitive recovery in post-stroke patients, with significant improvements in MMSE scores observed after 4-6 weeks of therapy. Patient-reported outcomes indicate reduced fatigue and improved quality of life measures in cardiovascular populations. However, systematic reviews note the need for larger, multicenter trials to further establish long-term benefits and optimal treatment durations across different patient populations.