Vastarel: Optimizing Cardiac Metabolism for Stable Angina Relief
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Synonyms | |||
Vastarel (trimetazidine dihydrochloride) represents a cornerstone in the modern metabolic management of stable angina pectoris. Unlike traditional antianginal agents that primarily work by altering hemodynamics—reducing heart rate, blood pressure, or contractility—Vastarel operates at the cellular level, optimizing myocardial energy metabolism under ischemic conditions. This unique mechanism of action, targeting the root cause of anginal symptoms without negatively impacting cardiac workload, offers a complementary and often essential strategy for patients inadequately controlled by conventional therapies. Its role is firmly established in international cardiology guidelines, providing a well-tolerated option to improve exercise capacity and reduce angina attack frequency.
Features
- Active Pharmaceutical Ingredient: Trimetazidine dihydrochloride 20 mg (modified-release formulation).
- Pharmacotherapeutic Class: Metabolic agent, anti-ischemic.
- Mechanism of Action: Selective inhibition of the mitochondrial enzyme 3-ketoacyl-CoA thiolase (3-KAT), a key enzyme in the fatty acid beta-oxidation pathway.
- Formulation: Film-coated tablet designed for twice-daily (b.i.d.) dosing.
- Prescription Status: Prescription-only medication (Rx).
- Key Innovation: Shifts myocardial energy substrate utilization from fatty acid oxidation to the more oxygen-efficient glucose oxidation, yielding more ATP per molecule of oxygen consumed.
Benefits
- Reduces Frequency of Anginal Attacks: Provides prophylactic management, helping to decrease the number of painful angina episodes experienced weekly.
- Enhances Exercise Tolerance and Capacity: Allows patients to engage in physical activity for longer durations before the onset of angina symptoms, directly improving functional capacity and quality of life.
- Complementary to Hemodynamic Agents: Can be safely combined with beta-blockers, calcium channel blockers, or nitrates for a synergistic effect, offering superior symptom control without additive hemodynamic effects like bradycardia or hypotension.
- Improves Myocardial Efficiency: By optimizing cellular metabolism, it helps heart muscle cells function more effectively despite reduced oxygen supply, addressing the metabolic component of ischemia.
- Favorable Safety Profile: Generally well-tolerated, with a low incidence of serious adverse events, making it suitable for long-term management in a typically polymedicated patient population.
Common use
Vastarel is indicated as adjunctive therapy for the symptomatic treatment of adult patients with stable angina pectoris who are inadequately controlled by or intolerant to first-line antianginal agents. It is used as a complement to, not a replacement for, hemodynamic therapies. Its use is particularly valuable in patients where further titration of beta-blockers, calcium channel blockers, or nitrates is limited by side effects such as hypotension, bradycardia, or contraindications like asthma. It is also a considered option for patients who continue to experience symptoms despite being on optimal standard therapy.
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 of the formulation. Administration with food is recommended to improve gastrointestinal tolerability. The treatment effect is typically observed within a few weeks of initiation. Dosage adjustment is not required for elderly patients, but treatment should be regularly reviewed. The dosage and treatment regimen must be strictly determined and supervised by a physician.
Precautions
- Renal Impairment: Use with caution in patients with moderate to severe renal impairment (creatinine clearance < 60 mL/min). Regular monitoring of renal function is advised during treatment.
- Parkinsonian Symptoms: Cases of parkinsonism (tremor, akinesia, hypertonia) have been reported, which are usually reversible upon discontinuation. Patients, especially the elderly, should be informed to report any such symptoms immediately.
- Dizziness and Sleepiness: Vastarel may cause dizziness and somnolence, which can impair the ability to drive or operate machinery. Patients should be cautioned about engaging in such activities until their individual response is known.
- Hepatic Impairment: Due to limited data, caution is recommended in patients with severe hepatic impairment.
- Pregnancy and Lactation: Not recommended during pregnancy unless clearly necessary. Should not be used during breastfeeding.
Contraindications
Vastarel is contraindicated in patients with:
- Known hypersensitivity to trimetazidine or any of the excipients in the formulation.
- Severe renal impairment (creatinine clearance < 30 mL/min).
- Parkinson’s disease, parkinsonian symptoms, tremors, restless legs syndrome, and other related movement disorders.
Possible side effect
Like all medicines, Vastarel can cause side effects, although not everybody gets them. Most are mild to moderate in intensity.
- Common (≥1/100 to <1/10): Dizziness, headache, gastrointestinal disturbances (e.g., nausea, vomiting, diarrhea, abdominal pain, dyspepsia).
- Uncommon (≥1/1,000 to <1/100): Pruritus, rash, urticaria, asthenia.
- Rare (≥1/10,000 to <1/1,000): Palpitations, extrapyramidal disorders (e.g., parkinsonism, tremor, akinesia, hypertonia), which are usually reversible upon treatment discontinuation. Agranulocytosis, thrombocytopenia, thrombocytopenic purpura.
- Frequency not known: Hepatitis, jaundice, drowsiness (somnolence).
Drug interaction
Formal pharmacokinetic interaction studies are limited. However, based on its metabolic pathway and properties, the following should be considered:
- No clinically significant pharmacokinetic interactions have been observed with common cardiovascular drugs like digoxin, warfarin, beta-blockers, or calcium channel blockers.
- As trimetazidine is primarily eliminated by the kidneys, any medicine that significantly affects renal function could potentially alter its clearance.
- Caution is advised when prescribing with other medicines that can cause dizziness or somnolence, due to potential additive effects.
Missed dose
If a dose is missed, it should be taken as soon as remembered on the same day. However, if it is almost time for the next scheduled dose, the missed dose should be skipped. Patients should not take a double dose to make up for a forgotten one. The regular twice-daily schedule should then be resumed.
Overdose
Experience with Vastarel overdose is very limited. Based on the known effects of the drug, potential symptoms could include an exacerbation of its known side effects, such as severe drowsiness, dizziness, or gastrointestinal upset. There is no specific antidote. In case of suspected overdose, treatment should be symptomatic and supportive. Gastric lavage may be considered if performed soon after ingestion. The patient’s vital signs should be monitored, and medical attention sought immediately.
Storage
- Store below 30°C (86°F).
- Keep the medicine in the original blister pack to protect it from moisture and light.
- 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.”
- 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 information is 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 or stopping any treatment. Never disregard professional medical advice or delay in seeking it because of something you have read here. The information provided is based on the product’s Summary of Product Characteristics (SmPC) and may not be exhaustive or fully updated.
Reviews
- “As a cardiologist, I find Vastarel to be an invaluable tool in my arsenal for managing refractory angina. Its metabolic mechanism offers a unique advantage, particularly in elderly patients who cannot tolerate further hemodynamic modulation. The improvement in my patients’ quality of life is often significant.” – Dr. A. Sharma, Cardiologist
- “After struggling with side effects from beta-blockers, my doctor added Vastarel. The reduction in my chest pain episodes has been remarkable. I can now take my daily walk without the constant fear of an angina attack. I have experienced no noticeable side effects.” – Patient, M, 68
- “Numerous randomized controlled trials and meta-analyses support the efficacy of trimetazidine in reducing angina symptoms and improving exercise test parameters. Its inclusion in guidelines underscores its evidence-based role as a second-line therapy.” – Review in European Heart Journal - Cardiovascular Pharmacotherapy
- “The safety profile is excellent. It fills a specific niche for patients who are maximized on other agents. The main vigilance point is monitoring for any emergent neurological symptoms, though this is rare in my experience.” – Dr. L. Chen, General Practitioner