Vastarel: Restoring Cellular Energy for Optimal Cardiac Function
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Synonyms | |||
Vastarel (trimetazidine dihydrochloride) is a metabolic agent specifically designed to optimize cellular energy metabolism in ischemic conditions. It represents a cornerstone in the management of stable angina pectoris, offering a unique mechanism of action that complements traditional antianginal therapies. By shifting cardiac metabolism to a more efficient pathway, Vastarel helps protect myocardial cells from the damaging effects of ischemia, thereby reducing angina symptoms and improving functional capacity. This targeted approach makes it a valuable option for patients requiring additional symptomatic control.
Features
- Active Pharmaceutical Ingredient: Trimetazidine dihydrochloride 20 mg (modified-release tablet).
- Pharmacotherapeutic Class: Other cardiac preparations, metabolic agent.
- Mechanism of Action: Selective inhibition of the mitochondrial long-chain 3-ketoacyl coenzyme A thiolase (3-KAT) enzyme, a key enzyme in the fatty acid beta-oxidation pathway.
- Pharmaceutical Form: Film-coated, modified-release tablet for twice-daily administration.
- Prescription Status: Prescription-only medication (POM).
Benefits
- Reduces the frequency of angina attacks by improving myocardial tolerance to ischemia.
- Decreases the need for short-acting nitrate (e.g., glyceryl trinitrate) use for acute symptom relief.
- Improves exercise capacity and reduces exercise-induced ST segment depression, allowing for greater physical activity with less discomfort.
- Provides cytoprotective effects by preventing a decrease in intracellular ATP levels and reducing intracellular acidosis and calcium overload during ischemic episodes.
- Offers a complementary mechanism of action to hemodynamic agents (e.g., beta-blockers, calcium channel blockers), allowing for effective combination therapy.
- Contributes to the maintenance of cardiac function and cellular homeostasis under stressful conditions.
Common use
Vastarel is primarily indicated as adjunctive therapy for the symptomatic treatment of patients with stable angina pectoris who are inadequately controlled by or intolerant to first-line antianginal agents. It is used as a complement to hemodynamic treatments to provide a more comprehensive management strategy. Its use is centered on improving metabolic efficiency in cardiac cells that are oxygen-deprived due to coronary artery disease.
Dosage and direction
The recommended adult dosage is one 20 mg modified-release tablet twice daily, taken with meals (e.g., breakfast and dinner). The tablets must be swallowed whole with a glass of water and should not be chewed, crushed, or divided, as this would compromise the modified-release properties. The treatment should be initiated under the supervision of a physician experienced in the management of chronic stable angina. Dosage adjustment is not typically required for elderly patients, but treatment should be regularly reviewed. The duration of treatment is determined by the treating physician based on the patient’s clinical response.
Precautions
Vastarel should be used with caution in patients with moderate to severe renal impairment. Although the active substance is mainly eliminated by the kidneys, specific dosage recommendations for this population are not established, and a benefit-risk assessment is necessary. Caution is also advised in patients with Parkinson’s disease, parkinsonian symptoms, tremors, restless legs syndrome, or other related movement disorders, as trimetazidine may induce or aggravate these symptoms. Regular monitoring for such neurological symptoms is recommended, especially in the elderly. Patients should be advised that Vastarel is not indicated for the acute relief of an angina attack and does not replace preventative or acute therapies like nitrates.
Contraindications
Vastarel is contraindicated in patients with known hypersensitivity to trimetazidine or any of the excipients in the formulation. Its use is also contraindicated in patients with severe renal impairment (creatinine clearance < 30 mL/min). Due to the potential for exacerbating symptoms, it must not be used in patients with Parkinson’s disease, other parkinsonian symptoms, tremors, restless legs syndrome, or other severe movement disorders.
Possible side effect
The most commonly reported adverse reactions are related to the gastrointestinal system and nervous system. As with all medications, side effects can vary in incidence and severity.
- Common (≥1/100 to <1/10): Dizziness, headache, nausea, vomiting, diarrhea, dyspepsia, abdominal pain.
- Uncommon (≥1/1,000 to <1/100): Pruritus, rash, urticaria, palpitations, orthostatic hypotension (which may be associated with dizziness), asthenia.
- Rare (≥1/10,000 to <1/1,000): Agranulocytosis, thrombocytopenia, thrombocytopenic purpura.
- Frequency not known: Extrapyramidal disorders (e.g., parkinsonism: tremor, akinesia, hypertonia), gait instability, restless legs syndrome, sleep disorders such as insomnia, and acute hepatitis. Patients should be monitored for the emergence of movement disorders.
Drug interaction
Formal interaction studies have not been performed. However, due to its metabolic pathway, the potential for pharmacokinetic interactions is considered low. Trimetazidine is primarily eliminated renally, with minimal metabolism by the cytochrome P450 system. Nevertheless, caution is advised when co-administering with other drugs that have the potential to cause or worsen extrapyramidal symptoms or QT interval prolongation. The additive effects on metabolic processes should be considered when used with other cardiac medications, though this is typically synergistic rather than antagonistic.
Missed dose
If a dose is missed, the patient should take it 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. Patients should be instructed not to take a double dose to make up for a forgotten one, as this increases the risk of adverse effects.
Overdose
Cases of overdose have been reported very rarely. Based on the known pharmacological profile, potential symptoms of a significant overdose could include an exacerbation of the known adverse effects, particularly severe gastrointestinal discomfort, nausea, vomiting, drowsiness, and hypotension. There is no known specific antidote for trimetazidine overdose. Management should be symptomatic and supportive, including gastric lavage if ingestion was recent and monitoring of vital signs. In case of suspected overdose, immediate medical attention should be sought.
Storage
Store in the original package below 25°C to protect the tablets from moisture and light. Keep the medication out of the sight and reach of children. Do not use Vastarel after the expiry date printed on the carton and blister. The expiry date refers to the last day of that month. Do not dispose of medication via wastewater or household waste; return any unused product to a pharmacy for proper disposal.
Disclaimer
This information is intended for healthcare professionals and is a summary of the product characteristics. It does not constitute exhaustive medical advice. The prescribing physician remains responsible for determining the appropriate treatment for an individual patient, considering their complete medical history, concomitant conditions, and other medications. The information provided here is not a substitute for professional medical advice, diagnosis, or treatment. Patients must always consult their doctor or a qualified healthcare provider with any questions regarding a medical condition or treatment.
Reviews
(Clinical perspective summary) Vastarel is well-established in international cardiology guidelines as an effective second-line antianginal therapy. Clinical trials and meta-analyses have consistently demonstrated its efficacy in reducing angina attack frequency and nitrate consumption while improving exercise test parameters. Its unique metabolic mode of action is valued for providing benefits without negatively affecting heart rate or blood pressure, making it suitable for a wide range of patients, including those who cannot tolerate hemodynamic agents. Expert consensus views it as a useful tool in the comprehensive management of chronic stable angina, particularly for symptom persistence despite first-line treatment.