Meldonium: Optimize Cellular Energy and Ischemic Protection
Meldonium
| Product dosage: 250mg | |||
|---|---|---|---|
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| 270 | 0.88 $ | 789.75 $ 237.51 $ (70%) | 🛒 Add to cart |
| 360 | 0.70 $
Best per pill | 1053.00 $ 252.72 $ (76%) | 🛒 Add to cart |
| Product dosage: 500mg | |||
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Synonyms | |||
Meldonium is a cardioprotective and anti-ischemic agent indicated for the improvement of physical capacity and functional state in patients with compromised energy metabolism. Its primary mechanism of action involves the modulation of carnitine biosynthesis, shifting energy production towards the more efficient oxygen utilization pathway and protecting cells from ischemic damage. This makes it a valuable therapeutic option in a range of cardiovascular and neurological conditions where tissue hypoxia is a concern.
Features
- Active Pharmaceutical Ingredient: Meldonium dihydrate
- Pharmacotherapeutic Group: Other cardiac preparations, ATC code: C01EB22
- Mechanism of Action: Competitive inhibitor of gamma-butyrobetaine hydroxylase, an enzyme in the carnitine biosynthesis pathway
- Primary Effect: Reduction of elevated levels of long-chain acylcarntine, shifting metabolism from fatty acid oxidation to glycolysis
- Bioavailability: Approximately 78% following oral administration
- Protein Binding: Low, facilitating wide tissue distribution
- Metabolism: Minimally metabolized; primarily excreted unchanged by the kidneys
- Elimination Half-Life: Approximately 3-6 hours
Benefits
- Enhances physical and mental performance under conditions of reduced oxygen supply
- Provides cytoprotection for myocardial and neural tissues during ischemic episodes
- Improves microcirculation and reduces the area of tissue damage post-ischemia
- Supports recovery of functional capacity after periods of excessive exertion or stress
- Contributes to the normalization of cellular energy metabolism in compromised states
- Exhibits a favorable safety and tolerability profile in the indicated patient populations
Common use
Meldonium is clinically indicated for the treatment and management of various conditions characterized by compromised energy metabolism and tissue ischemia. Its primary use is within the field of cardiology for patients with chronic heart failure (NYHA Class I-III), stable angina pectoris, and myocardial infarction, where it aids in improving exercise tolerance and reducing angina attacks. In neurology, it is employed as part of a comprehensive treatment plan for patients recovering from acute cerebrovascular accidents, such as ischemic strokes, and for managing chronic insufficient blood supply to the brain. Furthermore, it is utilized in ophthalmology for cases of retinal vascular pathology and hemodynamic lesions of the optic nerve. Off-label, it has been used by athletes to enhance performance under hypoxic conditions, though this use is restricted by anti-doping agencies.
Dosage and direction
The dosage of meldonium must be individualized based on the specific medical condition, its severity, and patient response. For cardiovascular conditions like chronic heart failure and stable angina, the typical adult oral dosage is 500 mg to 1000 mg per day, usually administered as one or two divided doses. The course of treatment generally spans 4 to 6 weeks, which may be repeated 2-3 times per year as clinically warranted. In cases of acute myocardial infarction, an initial parenteral administration may be used (500 mg to 1000 mg intravenously once daily) for up to 10 days, followed by an oral maintenance regimen. For cerebrovascular disorders, the standard oral dose is 500 mg once or twice daily for 4 to 6 weeks. The medication is recommended to be taken before noon to avoid potential effects on sleep architecture due to its activating properties. It can be taken with or without food.
Precautions
Patients should be advised that meldonium may influence blood pressure and heart rate; regular monitoring is advised, particularly in hypertensive individuals. Caution is recommended when operating machinery or driving, as the drug can cause dizziness or other central nervous system effects in some patients. The safety and efficacy of meldonium in pediatric populations have not been established; therefore, its use in children and adolescents is not recommended. In elderly patients, especially those with renal impairment, dosage adjustment may be necessary. Patients should inform their healthcare provider of all other medications they are taking due to potential interactions. Use during strenuous physical activity should be medically supervised.
Contraindications
Meldonium is contraindicated in patients with a known hypersensitivity to meldonium or any of the excipients in the formulation. It must not be used in individuals with severely elevated intracranial pressure, including cases due to intracranial tumors, acute intracranial hemorrhage, or disturbed venous outflow. Its use is contraindicated in patients with severe hepatic impairment (Child-Pugh Class C) or severe renal impairment (eGFR <30 mL/min/1.73m²) due to the lack of sufficient safety data in these populations. It is also contraindicated during pregnancy and lactation due to the absence of adequate human data regarding potential risks to the fetus or infant.
Possible side effect
The majority of adverse reactions associated with meldonium are mild to moderate in intensity and often transient. The most commonly reported side effects are related to the cardiovascular and central nervous systems. These may include tachycardia, palpitations, fluctuations in blood pressure (both hypertension and hypotension), and a feeling of heart rhythm disturbances. CNS-related effects can manifest as psychomotor agitation, emotional lability, sleep disturbances (including insomnia), and headache. Allergic reactions, though rare, may present as skin rash, pruritus, erythema, or angioedema. Gastrointestinal disturbances such as dyspepsia, nausea, or a feeling of heaviness in the epigastric region have been reported infrequently. Eosinophilia has been observed in some laboratory reports.
Drug interaction
Meldonium may potentiate the effects of other antianginal and antihypertensive drugs, such as nitrates, beta-blockers, calcium channel blockers, and other vasodilators, necessitating careful monitoring of blood pressure and possible adjustment of concomitant therapy. Concurrent use with other centrally acting stimulants or drugs that increase heart rate (e.g., theophylline, other xanthines) may lead to additive effects on heart rate and CNS excitation. It may enhance the effects of anticoagulants and antiplatelet agents, though clinical data is limited. Caution is advised when co-administering with drugs that are substrates of OCT2 or MATE transporters, as meldonium may inhibit their renal secretion. Always inform the prescribing physician of all concomitant medications, including over-the-counter drugs and supplements.
Missed dose
If a dose of meldonium is missed, it should be taken as soon as remembered on the same day. However, if it is close to the time for the next scheduled dose, the missed dose should be skipped, and the regular dosing schedule resumed. Patients should not take a double dose to make up for a missed one. Maintaining a consistent daily schedule is recommended for optimal therapeutic effect, but occasional missed doses are not expected to significantly impact the overall course of treatment.
Overdose
Cases of meldonium overdose are rare. Based on its pharmacological profile, symptoms of significant overdose may include a pronounced decrease in blood pressure, tachycardia, headache, dizziness, general weakness, and asthenia. In cases of severe overdose, more marked CNS effects such as agitation or anxiety might occur. There is no specific antidote for meldonium overdose. Management should consist of symptomatic and supportive care, including monitoring of vital signs and ECG. Gastric lavage may be considered if ingestion was recent. Hemodialysis is unlikely to be effective due to the drug’s volume of distribution and protein binding characteristics.
Storage
Meldonium should be stored in its original packaging at a temperature not exceeding 25°C (77°F). The medication must be kept in a dry place, protected from light and moisture. It should be stored out of reach and sight of children and pets. Do not use the medicine after the expiration date printed on the packaging. Do not dispose of unused medication via wastewater or household waste; consult a pharmacist for proper disposal methods in accordance with local regulations.
Disclaimer
This information is intended for medical professionals and provides a summary of the product characteristics. It is not exhaustive and does not replace the full prescribing information or professional medical advice. The prescribing physician should be consulted for diagnosis, treatment decisions, and complete information regarding indications, contraindications, warnings, precautions, and adverse reactions. The use of meldonium should be based on the approved product information within the specific country of use.
Reviews
Clinical studies and post-marketing surveillance indicate that meldonium is generally well-tolerated and effective for its approved indications. In cardiological practice, many specialists report observable improvements in exercise tolerance and a reduction in angina symptoms in compliant patients. Neurologists note its utility as an adjunct therapy in post-stroke recovery, particularly for improving cognitive function and reducing asthenic syndrome. The most frequently cited advantages in expert reviews are its targeted mechanism of action on cellular energy metabolism and its favorable safety profile compared to some other cardioprotective agents. Some reviews note the need for more large-scale, long-term outcome studies to further solidify its position in treatment guidelines. A consistent point in user-reported outcomes is the perceived increase in energy levels and reduction in fatigue associated with chronic conditions.