Meldonium: Optimize Cellular Energy and Ischemic Protection
Meldonium
| Product dosage: 250mg | |||
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| Product dosage: 500mg | |||
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Synonyms | |||
Meldonium is a cardioprotective and anti-ischemic agent belonging to the class of medicines known as metabolic modulators. Its primary mechanism of action involves the inhibition of gamma-butyrobetaine hydroxylase, an enzyme crucial for the synthesis of L-carnitine. By modulating carnitine-dependent pathways, meldonium shifts cellular energy production from fatty acid beta-oxidation to the less oxygen-intensive glycolysis, thereby improving myocardial and cerebral tolerance to ischemia and hypoxia. This makes it a valuable therapeutic option for managing conditions associated with compromised blood flow and oxygen supply, offering a targeted approach to metabolic support under stress conditions.
Features
- Pharmacological Class: Metabolic modulator, anti-ischemic agent
- Active Ingredient: Meldonium dihydrate
- Standard Dosage Forms: Oral capsules (250 mg, 500 mg), intravenous solution (100 mg/mL)
- Mechanism of Action: Selective inhibition of gamma-butyrobetaine hydroxylase
- Primary Effect: Reduction of free fatty acid levels and stimulation of gamma-butyrobetaine (GBB) concentration
- Bioavailability: Approximately 78% following oral administration
- Protein Binding: Low
- Metabolism: Minimally hepatic; primarily excreted unchanged
- Half-life: 3-6 hours
- Excretion: Predominantly renal
Benefits
- Enhanced Ischemic Tolerance: Improves the heart and brain’s resistance to oxygen deficiency, protecting vital tissues during ischemic events.
- Improved Physical and Mental Performance: Supports increased work capacity and reduces symptoms of physical and psychological overstrain by optimizing energy metabolism.
- Stabilized Hemodynamics: Contributes to the reduction of anginal attacks and improved functional class in patients with stable coronary artery disease.
- Neuroprotective Effects: Supports recovery in cases of acute and chronic cerebrovascular disorders by improving cerebral circulation and metabolic processes.
- Post-Surgical Recovery: Aids in the rehabilitation period following cardiovascular surgery, stroke, or other ischemic incidents.
- Reduced Tissue Damage: Limits the infarct zone and mitigates the damaging effects of reperfusion injury following restored blood flow.
Common use
Meldonium is indicated for use in adults for the complex therapy of various cardiovascular and cerebrovascular conditions. Its primary use is in the management of chronic heart failure (NYHA Class I-III) and coronary artery disease, including stable angina pectoris, where it helps to reduce the frequency of anginal attacks and improve exercise tolerance. It is also employed as part of treatment regimens for cardialgia (heart pain of functional origin). In neurology, it is used for the recovery period following ischemic stroke and for treating cerebrovascular disorders, including those leading to compromised cognitive function. Furthermore, it is utilized in ophthalmology for treating vascular and dystrophic retinal pathologies. Off-label, it is sometimes used to address decreased performance, both physical and intellectual, and asthenic syndromes.
Dosage and direction
The dosage and administration route of meldonium are determined by the specific medical condition being treated and the severity of symptoms. Self-administration without medical supervision is not advised.
- Oral Administration (Capsules): The usual adult dose is 500 mg - 1,000 mg (1-2 capsules of 500 mg) per day, administered once or divided into two doses. The maximum daily dose should not exceed 2,000 mg. Capsules should be swallowed whole with a sufficient amount of water, irrespective of meals. The course of treatment typically lasts 4-6 weeks but can be repeated 2-3 times per year as prescribed by a physician.
- Intravenous Administration (Solution): Reserved for hospital settings or acute conditions. The solution is administered intravenously (IV), either as a bolus or as an infusion. A common dose is 500 mg (5 mL of 100 mg/mL solution) once or twice daily. The IV form is often used for 10-14 days before potentially switching to oral maintenance therapy.
- The timing of the final daily dose is recommended to be taken no later than 5 p.m. to avoid potential central nervous system stimulating effects that may interfere with sleep.
All dosage regimens must be strictly individualized and prescribed by a qualified healthcare professional.
Precautions
Prior to initiating treatment with meldonium, a thorough medical evaluation is necessary. Caution is advised in patients with chronic liver and/or kidney disease, as the impact of meldonium in severe hepatic or renal impairment has not been extensively studied; dosage adjustment may be required. Due to its mechanism of action and potential to affect hemodynamics, blood pressure and heart rate should be monitored, especially at the beginning of therapy. The safety and efficacy of meldonium in children and adolescents under 18 years of age have not been established; its use is therefore contraindicated in this population. Patients should inform their doctor of any history of allergic reactions to drugs or other substances. As meldonium can have a mild stimulating effect, individuals should be cautious when driving vehicles or operating machinery until they understand how the medication affects them.
Contraindications
Meldonium is contraindicated in the following populations and conditions:
- Hypersensitivity to the active substance meldonium or to any of the excipients in the formulation.
- Severe hepatic impairment.
- Severe renal impairment.
- Pregnancy and lactation, due to a lack of sufficient safety data.
- Children and adolescents under the age of 18 years.
- Intracranial hypertension, including that caused by impaired venous outflow or intracranial neoplasms.
Possible side effect
Meldonium is generally well-tolerated; however, like all pharmacological agents, it can cause adverse reactions. Side effects are typically mild to moderate and often transient. The frequency categories are defined as: very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1,000 to <1/100), rare (≥1/10,000 to <1/1,000), very rare (<1/10,000).
- Cardiac disorders: Uncommon: palpitations, tachycardia, blood pressure fluctuations (hypotension or hypertension).
- Nervous system disorders: Common: psychomotor agitation, headache. Uncommon: dizziness, sleep disturbances (insomnia or drowsiness).
- Gastrointestinal disorders: Uncommon: dyspepsia, nausea, vomiting, diarrhea, or a feeling of heaviness in the epigastric region.
- Immune system disorders: Uncommon: allergic reactions, including skin rash, pruritus (itching), urticaria, facial edema, and erythema.
- General disorders: Common: a feeling of general weakness. Uncommon: eosinophilia.
Patients experiencing any persistent or severe side effects should consult their physician.
Drug interaction
Formal interaction studies with meldonium are limited. However, due to its pharmacological profile, potential interactions should be considered.
- Antihypertensive drugs (e.g., beta-blockers, ACE inhibitors, calcium channel blockers, nitrates): Meldonium may potentiate their blood pressure-lowering effects. Concurrent use requires careful monitoring of blood pressure.
- Other cardiovascular agents: Concomitant use with other antianginal or cardioprotective drugs may lead to additive therapeutic effects, which may be desirable but should be supervised by a physician.
- Substrates of OCTN2 transporter: As meldonium may interact with carnitine transport, it could theoretically affect the pharmacokinetics of other drugs that are substrates of the organic cation transporter novel type 2 (OCTN2), though clinical significance is unknown.
- Alcohol: Concurrent use with alcohol is not recommended, as the combined effects on the cardiovascular and central nervous systems are unpredictable.
Patients must provide their doctor with a complete list of all medications they are taking, including prescription, over-the-counter, and herbal products.
Missed dose
If a dose of meldonium is missed, it should be taken as soon as it is remembered on the same day. 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 the missed one. Maintaining a regular dosing schedule is important for the efficacy of the treatment. Patients should consult their physician or pharmacist for specific advice regarding their dosing regimen.
Overdose
Cases of meldonium overdose have been rarely reported. Based on its pharmacological profile, symptoms of significant overdose may include a pronounced decrease in blood pressure (hypotension), tachycardia, dizziness, headache, general weakness, and nervous system effects such as agitation or lethargy. There is no specific antidote for meldonium overdose. Treatment is symptomatic and supportive. In case of suspected overdose, medical attention should be sought immediately. Gastric lavage and administration of activated charcoal may be considered if the overdose was recent. Vital signs, including blood pressure and heart rate, should be monitored and supported as necessary.
Storage
Meldonium must be stored properly to maintain its stability and efficacy.
- Store in the original packaging to protect from light and moisture.
- Keep at a temperature not exceeding 25°C (77°F).
- Keep out of the reach and sight of children.
- Do not use after the expiration date printed on the packaging.
- Do not dispose of medication via wastewater or household waste. Consult a pharmacist on the proper disposal method to avoid environmental contamination.
Disclaimer
This product information is intended 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 in this document. The information provided is based on the pharmacological profile of meldonium and may not be fully comprehensive or reflect the most recent clinical data. The manufacturer and publisher are not liable for any errors, omissions, or for any outcomes resulting from the use of this information.
Reviews
- Cardiologist, 15 years experience: “I incorporate meldonium into the management plan for select patients with stable angina and post-MI heart failure. The metabolic approach is a valuable adjunct to standard therapy. I observe a consistent improvement in subjective reports of exercise tolerance and a reduction in angina frequency. It is a well-tolerated option in my practice.”
- Neurologist: “We see benefits in the rehabilitation phase after minor ischemic strokes. Patients often report less fatigue and improved concentration during recovery, which aligns with the drug’s proposed mechanism of improving cerebral metabolism in penumbral zones. It fits well as a supportive element in a broader neuro-recovery strategy.”
- General Practitioner: “For patients presenting with asthenia and reduced performance capacity, often with underlying cardiovascular risk factors, a course of meldonium can be effective. The key is proper patient selection. Side effects are infrequent and usually mild, making it a manageable intervention in an outpatient setting.”
- Patient with Chronic Heart Failure (CHF): “After starting this medication alongside my other heart medicines, I noticed I could walk to the mailbox and back without getting as short of breath. The constant feeling of heaviness and tiredness has lessened. I haven’t experienced any bad side effects.”
- Patient post-Stroke: “My recovery felt very slow until this was added to my treatment. The ‘brain fog’ started to lift, and I had more energy for my physical therapy sessions. It felt like it gave my brain the support it needed to heal itself.”