Meldonium is a cardioprotective and anti-ischemic pharmaceutical agent classified as a modulator of cellular energy metabolism. Its primary mechanism of action involves the inhibition of gamma-butyrobetaine hydroxylase, an enzyme crucial for the final synthesis of L-carnitine. By reducing L-carnitine availability, meldonium limits the transport of long-chain fatty acids into the mitochondria, shifting the cell’s energy production preference from fatty acid beta-oxidation to the more oxygen-efficient glycolysis. This metabolic adaptation is particularly beneficial under conditions of ischemia, hypoxia, or intense metabolic stress, where it helps preserve ATP levels, reduce lactate accumulation, and protect cellular structures from damage. It is a prescription medication indicated for specific medical conditions and should only be used under strict medical supervision.

Features

• Pharmacological Class: Cardiovascular agent, metabolic modulator
• Active Ingredient: Meldonium dihydrate
• Standard Dosage Forms: Oral capsules (250mg, 500mg), intravenous solution for injection (100 mg/mL)
• Mechanism of Action: Selective inhibitor of gamma-butyrobetaine hydroxylase
• Bioavailability: Approximately 78% following oral administration
• Plasma Protein Binding: Found to be relatively low
• Elimination Half-Life: Ranges from 3 to 6 hours
• Primary Route of Elimination: Renal excretion

Benefits

• Enhances myocardial tolerance to ischemia by optimizing oxygen utilization and preserving cellular energy (ATP) levels during hypoxic stress.
• Supports recovery of function in tissues following periods of ischemia or inadequate blood flow, aiding in post-event rehabilitation.
• Improves physical capacity and reduces symptoms of fatigue in patients with chronic cardiovascular conditions like stable angina pectoris and chronic heart failure.
• Provides neuroprotective effects by stabilizing neuronal metabolism and protecting brain tissue during and after ischemic events, such as strokes.
• Assists in normalizing metabolic processes compromised by various disease states, contributing to overall cellular stability and function.
• May enhance work capacity and exercise tolerance in healthy individuals under extreme physical and psychological strain, though this is an off-label use and subject to regulatory restrictions in athletics.

Common use

Meldonium is clinically approved for use in the management and treatment of various cardiovascular and cerebrovascular conditions. Its primary on-label indications include the treatment of stable angina pectoris (chest pain due to heart disease) and chronic heart failure (NYHA Class I-III), where it is used as part of a comprehensive therapeutic regimen to improve patient functional capacity and reduce symptoms. It is also indicated for the complex therapy of cerebrovascular disorders, including post-stroke recovery and chronic insufficient blood supply to the brain (dyscirculatory encephalopathy), to aid in the recovery of neurological function. Furthermore, it is used as adjunctive therapy during the recovery period following myocardial infarction and cardiosurgery. Its off-label application to improve physical performance and recovery in athletes has led to its prohibition by the World Anti-Doping Agency (WADA).

Dosage and direction

Dosage is highly individualized and must be determined by a qualified healthcare professional based on the specific indication, patient status, and formulation.

Oral Administration (Capsules):

• Adults: The typical recommended dose is 500 mg - 1000 mg (1-2 capsules of 500mg), administered once or twice daily.
• The total daily dosage should not exceed 2000 mg.
• The course of treatment usually lasts from 4 to 6 weeks. Therapy may be repeated 2-3 times per year.
• Capsules should be swallowed whole with a sufficient amount of water, independent of meals.

Intravenous Administration (Solution):

• Adults: 500 mg - 1000 mg (5-10 mL of the 100 mg/mL solution) administered once daily via intravenous drip or slow intravenous injection.
• As the patient’s condition improves, a transition to oral therapy is standard.
• IV administration should only be performed by healthcare personnel.

The duration of treatment and any necessary dosage adjustments are at the discretion of the prescribing physician.

Precautions

• Meldonium should be used with caution in patients with hepatic or renal impairment, as these conditions may alter its metabolism and excretion, potentially necessitating dosage adjustment.
• Due to its pharmacological effects, caution is advised in patients with severely low blood pressure ( hypotension).
• The safety and efficacy of meldonium in children and adolescents under the age of 18 have not been established; therefore, its use in this population is not recommended.
• Use during pregnancy is not recommended unless the potential benefit to the mother clearly outweighs the potential risk to the fetus, as there is insufficient data on its use in pregnant women.
• It is not known whether meldonium is excreted in human breast milk. A decision should be made whether to discontinue breastfeeding or to discontinue the drug, taking into account the importance of the drug to the mother.
• Patients should exercise caution when driving or operating machinery until they know how meldonium affects them, as individual responses regarding alertness may vary.

Contraindications

• Hypersensitivity to the active substance meldonium or to any of the excipients listed in the formulation.
• Severe hepatic impairment.
• Severe renal impairment.
• Elevated intracranial pressure, including due to intracranial tumors, impaired venous outflow, or acute cerebrovascular accidents with swelling and increased pressure in the brain.

Possible side effect

Meldonium is generally well-tolerated; however, like all pharmacological agents, it may cause adverse reactions in some individuals. Side effects are typically mild to moderate and transient.

• Cardiac disorders: Tachycardia (fast heart rate), blood pressure fluctuations (hypotension or hypertension).
• Nervous system disorders: Headache, agitation, emotional lability, dizziness, sleep disturbances (insomnia or drowsiness).
• Gastrointestinal disorders: Dyspepsia (indigestion), nausea, vomiting, diarrhea, abdominal pain.
• Immune system disorders: Allergic reactions, including skin rash, pruritus (itching), urticaria (hives), angioedema, and erythema.
• General disorders: Asthenia (weakness), a feeling of pressure in the chest, a feeling of heat.

Drug interaction

Formal interaction studies have not been extensively conducted. Based on its mechanism of action and pharmacokinetic profile, potential interactions may include:

• Other cardiovascular agents: Meldonium may potentiate the effects of antianginal drugs (e.g., nitrates, beta-blockers, calcium channel blockers), cardiac glycosides (e.g., digoxin), and other antihypertensive drugs, requiring careful monitoring of heart rate and blood pressure.
• Substrates of OCTN2 transporter: As a substrate of the organic cation transporter novel type 2 (OCTN2), meldonium may potentially compete for transport with other substrates (e.g., L-carnitine, certain beta-lactam antibiotics), though the clinical significance is unknown.
• Alcohol: Concomitant use with alcohol is not recommended due to a potential additive effect on vasodilation and hypotension.

It is crucial to inform your physician of all medications you 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 a missed one. Patients should not alter the dosage or frequency without consulting their doctor.

Overdose

Cases of overdose with meldonium have been reported very rarely. 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. In case of suspected overdose, medical attention should be sought immediately. Treatment is symptomatic and supportive; there is no known specific antidote. Hemodialysis may be considered due to the drug’s relatively low molecular weight and protein binding.

Storage

• Store in the original package at a temperature not exceeding 25°C (77°F).
• Protect from light and moisture.
• 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 use of meldonium for performance enhancement in sports is banned by the World Anti-Doping Agency (WADA).

Reviews

• “As a cardiologist, I have prescribed meldonium as part of a comprehensive regimen for patients with stable angina and Class II heart failure. The most consistent feedback is an improvement in exercise tolerance and a reduction in angina episodes. It’s a valuable tool in our arsenal for metabolic support.” – Medical Professional, Latvia
• “Following a minor ischemic stroke, my neurologist added meldonium to my recovery plan. I noticed a significant difference in my energy levels and cognitive fog within a few weeks. The rehabilitation process felt more manageable.” – Patient, Lithuania
• “The metabolic rationale behind meldonium is scientifically sound. Its role in shifting energy substrate utilization during stress is well-documented in preclinical models. However, its clinical application requires careful patient selection and more large-scale, robust trials to further define its place in therapy.” – Clinical Pharmacologist, Research Institution
• “I was prescribed this medication for chronic fatigue associated with a diagnosed cardiovascular condition. The effect was subtle but noticeable; I felt less exhausted after minor physical tasks. I experienced no side effects during the 4-week course.” – Patient, Russia