Meldonium is a cardioprotective and anti-ischemic agent indicated for the improvement of metabolic processes and energy supply in tissues under conditions of ischemia. 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 conditions characterized by compromised oxygen delivery and energy deficit. It is a prescription medication that requires careful patient evaluation and monitoring under the supervision of a qualified healthcare professional.

Features

• Active Ingredient: Meldonium dihydrate
• Pharmacological Class: Metabolic modulator, cardioprotective agent
• Mechanism of Action: Competitive inhibitor of gamma-butyrobetaine hydroxylase, reducing L-carnitine synthesis and shifting energy metabolism towards glycolysis
• Bioavailability: Approximately 78% following oral administration
• Half-life: 3-6 hours
• Protein Binding: Minimal
• Metabolism: Hepatic, via CYP450 enzymes (primarily CYP2D6 and CYP2C19)
• Excretion: Primarily renal (95%), with minor fecal elimination
• Available Formulations: Oral capsules (250mg, 500mg), intravenous solution (100mg/mL)

Benefits

• Enhances myocardial tolerance to ischemia by optimizing cellular energy utilization
• Improves physical capacity and reduces symptoms in patients with chronic heart failure and stable angina
• Supports functional recovery in post-stroke and post-infarction rehabilitation
• Reduces neurological deficit in cerebrovascular disorders
• Improves retinal function in vascular ophthalmopathies
• May enhance exercise tolerance in certain cardiovascular conditions

Common use

Meldonium is primarily indicated for the treatment of various cardiovascular and cerebrovascular conditions where tissue ischemia is a contributing factor. Its most common therapeutic applications include stable angina pectoris, chronic heart failure (NYHA Class I-III), and post-myocardial infarction management. In neurological practice, it is used for the recovery period following ischemic stroke, transient ischemic attacks, and cerebrovascular insufficiency. Additionally, it finds application in ophthalmology for retinal vascular disorders, including retinopathies and hemorrhages. Some sports medicine specialists have utilized it off-label for improving exercise tolerance, though this application remains controversial and is subject to anti-doping regulations in competitive athletics.

Dosage and direction

Oral Administration: The typical adult dosage is 500mg-1000mg daily, divided into 1-2 doses. The maximum daily dose should not exceed 2000mg. Treatment duration typically ranges from 4-6 weeks, with possible repetition after consultation with a healthcare provider.

Intravenous Administration: For acute conditions, 500mg-1000mg may be administered intravenously once daily for 10-14 days, followed by oral maintenance therapy.

The medication is preferably taken in the morning or early afternoon due to potential mild CNS stimulation. Capsules should be swallowed whole with water, with or without food, though consistent administration relative to meals is recommended. Dosage adjustments may be necessary for elderly patients or those with renal impairment. Treatment should always be initiated and monitored under medical supervision.

Precautions

Patients should be carefully monitored during treatment, particularly those with pre-existing hepatic or renal impairment. Regular assessment of renal function is recommended during prolonged therapy. Caution is advised when operating machinery or driving, as meldonium may cause dizziness in some patients. The safety and efficacy in pediatric patients have not been established. Use during pregnancy should only be considered if the potential benefit justifies the potential risk to the fetus. Breastfeeding should be discontinued during treatment. Patients should inform their healthcare provider of all medications they are taking, including over-the-counter drugs and supplements. Regular cardiovascular monitoring is recommended throughout treatment.

Contraindications

Meldonium is contraindicated in patients with known hypersensitivity to the active substance or any excipients in the formulation. It should not be used in patients with severe hepatic impairment (Child-Pugh Class C) or severe renal impairment (eGFR <30 mL/min/1.73m²). Contraindications include intracranial hypertension, regardless of etiology, and conditions associated with increased cerebrospinal fluid pressure. The medication is not recommended during pregnancy and lactation unless clearly necessary. Concomitant use with other metabolic modulators or drugs affecting carnitine metabolism should be avoided unless specifically indicated and monitored.

Possible side effect

The most commonly reported adverse reactions are generally mild and transient. Cardiovascular effects may include tachycardia, blood pressure fluctuations, and palpitations. Nervous system reactions can include headache, dizziness, emotional lability, and sleep disturbances. Gastrointestinal complaints such as dyspepsia, nausea, and abdominal discomfort have been reported. Dermatological reactions including rash and pruritus may occur in sensitive individuals. Allergic reactions, though rare, can manifest as urticaria or angioedema. Laboratory abnormalities may include transient elevations in liver enzymes or eosinophilia. Most side effects are dose-dependent and often resolve with continued therapy or dose reduction.

Drug interaction

Meldonium may interact with several medication classes. Concomitant use with antihypertensive agents may potentiate their effects, requiring blood pressure monitoring. Interactions with antiplatelet agents and anticoagulants may increase bleeding risk. Co-administration with other metabolic agents or drugs affecting mitochondrial function should be carefully considered. CYP2D6 and CYP2C19 inhibitors may increase meldonium plasma concentrations. The medication may enhance the effects of nitrates and other antianginal drugs. Concomitant use with alcohol is not recommended due to potential additive CNS effects. Healthcare providers should conduct thorough medication reviews before initiating therapy.

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, the missed dose should be skipped, and the regular dosing schedule resumed. Doubling the dose to make up for a missed dose is not recommended. Patients should maintain a consistent dosing schedule to ensure stable plasma concentrations. If multiple doses are missed, consultation with a healthcare provider is advised before resuming treatment. A medication diary or reminder system may help maintain adherence to the prescribed regimen.

Overdose

Cases of overdose are rare due to the medication’s favorable safety profile. Symptoms of overdose may include pronounced hypotension, tachycardia, headache, dizziness, and general weakness. Gastrointestinal distress including nausea and vomiting may occur. In case of suspected overdose, immediate medical attention should be sought. Treatment is primarily supportive and symptomatic. Gastric lavage may be considered if ingestion occurred within 1-2 hours. Hemodialysis may be effective due to the drug’s renal excretion. Cardiac monitoring and symptomatic treatment of cardiovascular effects should be instituted as necessary.

Storage

Store at room temperature (15-25°C/59-77°F) in the original container, protected from light and moisture. Keep the medication out of reach of children and pets. Do not use after the expiration date printed on the packaging. Avoid storing in bathrooms or other areas with high humidity. For intravenous formulations, follow specific storage instructions provided with the product. Do not freeze the medication. Proper storage conditions are essential for maintaining stability and efficacy throughout the shelf life.

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 information presented here may not be exhaustive or current. Always consult with a healthcare provider for personalized medical advice, diagnosis, and treatment. Do not disregard professional medical advice or delay seeking it because of something you have read in this product description. Actual product labeling and prescribing information may vary by jurisdiction and should be consulted before use.

Reviews

Clinical studies have demonstrated meldonium’s efficacy in improving exercise tolerance and reducing angina symptoms in patients with chronic heart failure. A 12-week randomized controlled trial involving 512 patients with stable angina showed significant improvement in exercise duration and time to ST-segment depression compared to placebo. Another study in patients with chronic heart failure demonstrated improved functional capacity and quality of life scores. Neurological applications have shown promise in post-stroke rehabilitation, with studies indicating improved cognitive recovery and reduced neurological deficit scores. However, more large-scale, randomized controlled trials are needed to further establish its efficacy across various indications. Patient-reported outcomes generally indicate good tolerability, with most adverse effects being mild and transient.