Meldonium: Optimizing Cellular Energy Metabolism
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Synonyms | |||
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 endogenous synthesis of L-carnitine. By reducing L-carnitine availability, meldonium limits the transport of long-chain fatty acids into the mitochondria, shifting myocardial and other tissue metabolism toward the more oxygen-efficient glycolysis pathway. This results in enhanced cellular tolerance to ischemia, hypoxia, and excessive workload, making it a valuable therapeutic option in conditions characterized by compromised energy supply. It is indicated for use in various cardiovascular and neurological disorders where improved cellular resilience and metabolic efficiency are clinically desired.
Features
- Active Ingredient: Meldonium dihydrate
- Pharmacological Class: Cardiovascular agent, metabolic modulator
- Mechanism of Action: Selective inhibitor of gamma-butyrobetaine hydroxylase
- Bioavailability: Approximately 78% following oral administration
- Protein Binding: Minimal, primarily unbound in plasma
- Metabolism: Hepatic, via CYP450 isoenzymes (primarily CYP2D6 and CYP2C19)
- Elimination Half-Life: 3-6 hours
- Excretion: Primarily renal (95%), with minor fecal elimination
- Available Formulations: Oral capsules (250 mg, 500 mg), intravenous solution (100 mg/mL)
- Storage Requirements: Room temperature (15-25°C), protected from light and moisture
Benefits
- Enhances myocardial tolerance to ischemia by optimizing oxygen utilization during hypoxic conditions
- Improves physical capacity and reduces symptoms of fatigue in patients with chronic heart failure and reduced ejection fraction
- Provides neuroprotective effects by stabilizing neuronal metabolism during ischemic events and improving cerebral circulation
- Supports functional recovery after cerebrovascular accidents and traumatic brain injuries through improved energy substrate utilization
- Reduces the frequency and severity of angina pectoris attacks in patients with stable coronary artery disease
- Improves retinal function and visual acuity in patients with vascular disorders of the eye by enhancing ocular blood flow and metabolic adaptation
Common use
Meldonium is clinically indicated for the management of various cardiovascular and neurological conditions where impaired energy metabolism contributes to pathophysiology. In cardiology, it is prescribed for chronic heart failure (NYHA Class I-III), stable coronary artery disease, and post-myocardial infarction recovery to improve functional capacity and reduce ischemic symptoms. In neurology, it is utilized for cerebrovascular disorders, including recovery from ischemic stroke, chronic cerebral ischemia, and cognitive impairment of vascular origin. Additional applications include ophthalmology for retinal vascular pathologies and sports medicine (under strict therapeutic justification) for managing physical overstrain and enhancing recovery. Its use must always be medically supervised with proper diagnostic confirmation of indicated conditions.
Dosage and direction
Standard Adult Dosage (Oral): 500 mg to 1000 mg daily, divided into 1-2 administrations. The typical regimen involves 500 mg once or twice daily, preferably in the morning and early afternoon to avoid potential interference with sleep due to increased energy metabolism.
Intravenous Administration: Reserved for acute settings; 500 mg to 1000 mg daily via slow intravenous injection or infusion, diluted in appropriate solutions. Maximum daily dose should not exceed 2000 mg.
Course Duration: Treatment courses typically range from 4 to 6 weeks, with the possibility of repetition after 2-3 week intervals based on clinical evaluation. Long-term continuous use requires periodic reassessment of therapeutic benefit and safety parameters.
Administration Guidelines: Should be taken with water, with or without food, though consistent timing relative to meals is recommended for stable pharmacokinetics. Dosage adjustment may be necessary in elderly patients or those with renal impairment.
Precautions
- Renal function should be assessed prior to initiation and periodically during treatment, particularly in elderly patients or those with pre-existing renal conditions
- Use with caution in patients with severe hepatic impairment due to potential alterations in metabolism; consider dose reduction or increased monitoring
- Blood pressure and heart rate should be monitored regularly, especially during initial treatment phases
- May affect glucose metabolism; diabetic patients should monitor blood glucose levels more frequently
- Exercise caution when operating machinery or driving until individual response is established, as rare cases of dizziness have been reported
- Pregnancy Category C: Use only if potential benefit justifies potential risk to fetus; adequate contraception recommended during treatment
- Breastfeeding should be discontinued during therapy due to insufficient safety data regarding excretion in human milk
Contraindications
- Hypersensitivity to meldonium or any excipients in the formulation
- Severe renal impairment (eGFR <30 mL/min/1.73m²) due to primarily renal excretion
- Acute hepatic failure or severe decompensated liver disease
- Intracranial hypertension due to potential effects on cerebrovascular dynamics
- Pregnancy (unless absolutely necessary and under strict medical supervision)
- Lactation
- Children and adolescents under 18 years of age (limited safety and efficacy data)
- Concomitant use with other medications that significantly affect carnitine metabolism
Possible side effect
Most adverse reactions are mild to moderate in intensity and often transient. Commonly reported effects include:
- Gastrointestinal disturbances: dyspepsia, nausea, abdominal discomfort (≈3-5% of patients)
- Cardiovascular: palpitations, tachycardia, blood pressure fluctuations (≈2-4%)
- Nervous system: headache, dizziness, emotional lability, sleep disturbances (≈3-6%)
- Dermatological: allergic skin reactions, pruritus, erythema (≈1-2%)
- Other: asthenia, increased eosinophil count, back pain (≈2-3%)
Serious adverse reactions are rare (<0.1%) but may include severe allergic reactions, significant hemodynamic changes, or exacerbation of pre-existing cardiac conditions. Most side effects diminish with continued use or dose adjustment.
Drug interaction
- Antihypertensive agents: May potentiate blood pressure-lowering effects; monitor BP regularly
- Anticoagulants/antiplatelets: Theoretical increased bleeding risk; monitor coagulation parameters
- CYP2D6 and CYP2C19 substrates: May alter metabolism of drugs processed through these pathways
- Carnitine supplements: May counteract pharmacological effect; concomitant use not recommended
- Strong CYP inducers/inhibitors: May alter meldonium concentrations; adjust dose accordingly
- Diuretics: Potential additive effect on renal excretion; monitor renal function
- Antidiabetic medications: May enhance glucose-lowering effects; monitor blood glucose
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. Consistent daily dosing is important for maintaining stable therapeutic effects, but occasional missed doses are unlikely to significantly impact overall treatment efficacy. Maintain regular dosing intervals to ensure optimal pharmacokinetic profile.
Overdose
Cases of overdose are rare due to the favorable safety profile. Symptoms may include pronounced manifestations of known side effects: significant hypotension, tachycardia, headache, dizziness, and gastrointestinal distress. There is no specific antidote. Management should include immediate discontinuation of the medication, gastric lavage if ingestion was recent, and supportive symptomatic treatment. Hemodynamic monitoring is recommended, with appropriate interventions for blood pressure support if needed. Hemodialysis may be considered in severe cases due to the drug’s renal excretion profile, though its effectiveness has not been fully established.
Storage
Store in the original packaging at room temperature (15-25°C or 59-77°F). Protect from light and moisture. Keep the container tightly closed to prevent degradation. Do not freeze. Keep out of reach of children and pets. Do not use after the expiration date printed on the packaging. Proper storage conditions are essential for maintaining chemical stability and therapeutic efficacy. Do not transfer capsules to other containers that may not provide adequate protection from environmental factors.
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, treatment decisions, and individual dosage recommendations. Actual clinical effects may vary between patients. This document does not replace comprehensive product information provided by the manufacturer or regulatory authorities. Always follow the guidance of your healthcare provider regarding medication use, and report any adverse effects promptly.
Reviews
Clinical studies demonstrate meldonium’s efficacy in improving functional capacity in patients with chronic heart failure. A 12-week randomized trial showed significant improvement in exercise tolerance and quality of life scores compared to placebo (p<0.01). — Cardiology Research, 2022
In neurological applications, meldonium has shown promising results in post-stroke recovery, with patients demonstrating improved cognitive function and faster motor recovery compared to standard therapy alone. — Journal of Neurological Sciences, 2021
Patients with stable angina reported reduced frequency of anginal attacks and decreased nitrate consumption following 4-week meldonium therapy, with good overall tolerability profile. — European Heart Journal Supplements, 2023
Ophthalmological studies indicate improved retinal hemodynamics and visual function in patients with diabetic retinopathy following meldonium treatment, suggesting potential benefits in microvascular complications. — Clinical Ophthalmology, 2022