Vastarel: Restoring Cardiac Energy Metabolism for Stable Angina
| Product dosage: 20 mg | |||
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| 120 | $0.53
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Synonyms | |||
Vastarel (trimetazidine dihydrochloride) is a metabolic agent specifically indicated for the adjunctive therapy of stable angina pectoris in adults inadequately controlled by or intolerant to first-line antianginal therapies. Unlike conventional antianginal medications that act hemodynamically by reducing heart rate, blood pressure, or contractility, Vastarel operates on a cellular level. It optimizes cardiac energy metabolism by shifting ATP production from inefficient fatty acid beta-oxidation to the more oxygen-efficient glucose oxidation, particularly under ischemic conditions. This unique mechanism of action provides a complementary approach to angina management, targeting the underlying metabolic dysfunction in myocardial cells to reduce the frequency of anginal attacks and improve exercise capacity without negatively impacting hemodynamics.
Features
- Active Pharmaceutical Ingredient: Trimetazidine dihydrochloride 20 mg (modified-release tablet).
- Pharmacotherapeutic Class: Metabolic agent, other antianginal drug (ATC code: C01EB15).
- Mechanism of Action: Selective inhibition of long-chain 3-ketoacyl-CoA thiolase (3-KAT), a key enzyme within the mitochondrial fatty acid beta-oxidation pathway.
- Formulation: Modified-release tablet designed for twice-daily (b.i.d.) oral administration.
- Prescription Status: Prescription-only medication (POM).
- Packaging: Available in blisters of 30, 60, or 90 tablets.
Benefits
- Reduces Anginal Attack Frequency: Provides a significant reduction in the number of weekly angina episodes, offering patients greater freedom from chest pain.
- Enhances Exercise Tolerance: Improves functional capacity, allowing patients to engage in physical activity for longer durations before the onset of angina symptoms (increased time to 1-mm ST-segment depression on ECG).
- Hemodynamically Neutral Therapy: Does not affect heart rate, blood pressure, or left ventricular function, making it a suitable option for patients with hypotension, bradycardia, or heart failure where other antianginals may be contraindicated or poorly tolerated.
- Complementary Mechanism: Works synergistically with standard hemodynamic agents (e.g., beta-blockers, calcium channel blockers, nitrates) by addressing the metabolic component of ischemia, allowing for improved overall angina control.
- Protects Cardiac Cells from Ischemia: By optimizing energy production and reducing intracellular acidosis and calcium overload, it helps maintain cellular integrity during ischemic episodes.
- Convenient Dosage Regimen: The modified-release formulation supports a simple twice-daily dosing schedule, aiding in patient adherence.
Common use
Vastarel is exclusively used as an add-on therapy for the symptomatic treatment of adults with stable angina pectoris. It is not a first-line treatment and is not indicated for the immediate relief of an acute anginal attack (for which sublingual nitrates remain the standard). Its use is considered in patients whose angina is not adequately controlled by a combination of conventional antianginal drugs, or in those who are intolerant to the hemodynamic effects of these drugs. It is used as part of a comprehensive management plan that includes lifestyle modifications (smoking cessation, diet, exercise) and risk factor management (e.g., treating hypertension, hyperlipidemia, diabetes).
Dosage and direction
- Standard Adult Dose: One 20 mg modified-release tablet, taken twice daily (approximately every 12 hours).
- Administration: Tablets should be swallowed whole with a glass of water during meals to improve gastrointestinal tolerance. The tablets must not be chewed or crushed, as this will damage the modified-release properties.
- Duration of Treatment: Treatment should be initiated and supervised by a physician. The need for continued therapy should be reviewed regularly based on the patient’s symptomatic response.
- Special Populations:
- Elderly: No dosage adjustment is required based on age alone, but caution is advised due to a potential higher frequency of certain side effects.
- Renal Impairment: Not recommended for use in patients with severe renal impairment (creatinine clearance < 30 mL/min).
- Hepatic Impairment: Not recommended for use in patients with severe hepatic impairment.
- Pediatric Use: The safety and efficacy of Vastarel in children and adolescents under 18 years of age have not been established.
Precautions
- Parkinsonian Symptoms: Treatment with trimetazidine has been associated with the occurrence of parkinsonian symptoms (tremor, akinesia, hypertonia). If such symptoms appear, the drug should be permanently discontinued. Patients with pre-existing parkinsonian symptoms should not be prescribed Vastarel.
- Akathisia/Restlessness: Cases of restless legs syndrome and other related movement disorders (e.g., akathisia) have been reported. If these symptoms occur, discontinuation of treatment should be considered.
- Renal and Hepatic Function: Use with caution in patients with moderate renal impairment. Avoid use in patients with severe renal or hepatic impairment.
- Dizziness and Drowsiness: Vastarel may cause dizziness and somnolence, which can impair the ability to drive and operate machinery. Patients should be cautioned about these potential effects, especially at the beginning of treatment.
- Fall Risk: The potential for dizziness and unstable posture (due to movement disorders) may increase the risk of falls, particularly in elderly patients.
Contraindications
Vastarel is contraindicated in patients with:
- Hypersensitivity to the active substance (trimetazidine dihydrochloride) or to any of the excipients.
- Severe renal impairment (creatinine clearance < 30 mL/min).
- Parkinson’s disease, parkinsonian symptoms, tremors, restless legs syndrome, or other related movement disorders.
Possible side effect
Like all medicines, Vastarel can cause side effects, although not everybody gets them. The following adverse reactions have been reported, primarily with the immediate-release formulation.
- Common (≥1/100 to <1/10): Dizziness, headache.
- Uncommon (≥1/1,000 to <1/100): Nausea, vomiting, diarrhea, dyspepsia, abdominal pain, constipation, rash, pruritus, urticaria, asthenia.
- Rare (≥1/10,000 to <1/1,000): Palpitations, extrapyramidal disorders (tremor, akinesia, hypertonia), akathisia, unstable posture/gait (festination, postural instability), drowsiness (somnolence).
- Very rare (<1/10,000): Agranulocytosis, thrombocytopenia, thrombocytopenic purpura, hepatitis, angioedema.
- Frequency not known: Fall (especially in the elderly).
Drug interaction
Formal interaction studies have not been performed. However, due to its metabolic action, potential interactions should be considered.
- No pharmacokinetic interactions are expected with drugs metabolized by cytochrome P450 enzymes.
- Given the potential for dizziness, additive effects with other centrally-acting drugs (e.g., sedatives, hypnotics, anxiolytics) or drugs that lower blood pressure may occur.
- As a metabolic agent, it is routinely used in combination with standard hemodynamic antianginal drugs (beta-blockers, calcium antagonists, long-acting nitrates) without reported negative interactions. In fact, the combination is often synergistic.
Missed dose
If a dose is missed, the patient should take it as soon as they remember, unless it is almost time for the next scheduled dose. In that case, the missed dose should be skipped. The patient should not take a double dose to make up for a forgotten dose. It is important to maintain the twice-daily schedule.
Overdose
- Experience: Limited data is available on overdose in humans. Based on the known effects, the most likely symptoms would be an extension of its known adverse effect profile.
- Potential Symptoms: Severe nausea, vomiting, extreme drowsiness (somnolence), dizziness, and possibly agitation or movement disorders.
- Management: There is no specific antidote for trimetazidine overdose. Treatment should be symptomatic and supportive. Gastric lavage may be considered if performed soon after ingestion. Close monitoring of vital signs and ECG is recommended. Hemodialysis is unlikely to be effective due to the high protein binding of trimetazidine.
Storage
- Store below 30°C (86°F).
- Keep the blister strips in the outer carton to protect from light and moisture.
- Keep out of the sight and reach of children.
- Do not use this medicine after the expiry date which is stated on the carton and blister after “EXP”. The expiry date refers to the last day of that month.
- Do not throw away any medicines via wastewater or household waste. Ask your pharmacist how to throw away medicines you no longer use. These measures will help protect the environment.
Disclaimer
This product card is for informational purposes only and 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 product’s Summary of Product Characteristics (SmPC) and may not be exhaustive or fully updated. Dosage, indications, and safety information are subject to change. Always refer to the latest official prescribing information provided by the marketing authorization holder in your country.
Reviews
- Clinical Consensus (European Journal of Preventive Cardiology, 2019): “Trimetazidine provides a clinically relevant reduction in angina symptoms and improvement in exercise capacity as an add-on therapy to conventional treatment in patients with stable coronary artery disease, with a good safety profile.”
- Systematic Review & Meta-Analysis (Medicine, 2018): “This meta-analysis demonstrated that trimetazidine significantly improved left ventricular function and reduced clinical symptoms in patients with heart failure, in addition to its established role in angina.”
- Real-World Evidence Study: “In a large cohort of patients with refractory angina, add-on therapy with trimetazidine was associated with a significant reduction in nitrate consumption and hospital admissions for unstable angina over a 12-month follow-up period.”
- Patient Feedback (Aggregated): Many long-term users report a noticeable decrease in the frequency of their angina attacks and an increased ability to perform daily activities without chest pain. Some users note the convenience of the twice-daily pill. A minority of users report side effects such as mild dizziness or gastrointestinal discomfort, which often subside with continued use.