Vastarel: Restoring Cellular Energy for Stable Angina Relief

Vastarel

Product dosage: 20 mg
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Synonyms Trimetazidine

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Vastarel (trimetazidine dihydrochloride) is a metabolic agent specifically indicated for the adjunctive therapy of stable angina pectoris in adults. It represents a unique therapeutic approach, functioning not as a traditional hemodynamic agent like beta-blockers or calcium channel blockers, but by optimizing cellular energy metabolism within the ischemic heart. This mechanism directly targets the underlying metabolic dysfunction that occurs during myocardial ischemia, offering a complementary strategy to manage symptoms and improve functional capacity when other antianginal therapies are insufficient or not tolerated. By shifting cardiac metabolism to a more efficient pathway, Vastarel helps protect myocardial cells from the damaging effects of oxygen supply-demand mismatch.

Features

• Active Pharmaceutical Ingredient: Trimetazidine dihydrochloride 20 mg (modified-release tablet).
• 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.
• Pharmaceutical Form: Modified-release, film-coated tablet for twice-daily administration.
• Prescription Status: Prescription-only medication (POM).

Benefits

• Reduces the frequency of angina attacks by improving the heart’s metabolic efficiency during periods of ischemia.
• Decreases the patient’s reliance on short-acting nitrate (e.g., GTN spray) use for acute angina relief.
• Improves exercise tolerance and delays the onset of exercise-induced angina, enhancing overall quality of life and functional capacity.
• Provides complementary efficacy when added to standard hemodynamic antianginal therapies (e.g., beta-blockers, calcium antagonists).
• Offers a well-tolerated therapeutic option with a mechanism of action distinct from other antianginal classes, making it suitable for patients who cannot tolerate hemodynamic effects like bradycardia or hypotension.

Common use

Vastarel is used as add-on therapy for the symptomatic treatment of adult patients with stable angina pectoris who are inadequately controlled by or intolerant to first-line antianginal therapies. It is not intended for the management of acute anginal attacks, for which sublingual nitrates remain the standard of care. Its use is predicated on a confirmed diagnosis of stable coronary artery disease, and it should be part of a comprehensive management plan that includes lifestyle modifications (smoking cessation, diet, exercise) and management of cardiovascular risk factors (hypertension, hyperlipidemia, diabetes).

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 efficacy of treatment should be evaluated after three months of therapy. If no clinical benefit is observed, the treatment should be reconsidered and potentially discontinued. Dosage adjustment is not required for elderly patients but is contraindicated in patients with severe renal impairment.

Precautions

• Renal Impairment: Use is contraindicated in patients with severe renal impairment (creatinine clearance < 30 mL/min). Use with caution in patients with moderate renal impairment.
• Parkinsonian Symptoms: Trimetazidine has been associated with the occurrence of parkinsonian symptoms (tremor, akinesia, hypertonia). Treatment should be discontinued if such symptoms appear.
• Movement Disorders: Cases of gait instability or restless legs syndrome have been reported. Elderly patients may be at higher risk.
• Hepatic Impairment: As the pharmacokinetics may be altered, Vastarel should be used with caution in patients with moderate hepatic impairment and is not recommended in severe hepatic impairment.
• Driving and Operating Machinery: Patients experiencing dizziness or episodes of sudden onset of drowsiness should refrain from driving or engaging in activities where impaired alertness may pose a risk to themselves or others.

Contraindications

• 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, tremor, restless legs syndrome, and 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 long-term use of the immediate-release formulation.

• Common (may affect up to 1 in 10 people): Dizziness, headache.
• Uncommon (may affect up to 1 in 100 people): Palpitations, extrasystoles, tachycardia, hypotension, orthostatic hypotension (which may lead to falls in elderly patients), nausea, vomiting, diarrhea, dyspepsia, abdominal pain, constipation, rash, pruritus, urticaria, asthenia.
• Rare (may affect up to 1 in 1,000 people): Agranulocytosis, thrombocytopenia, thrombocytopenic purpura, drowsiness, somnolence, insomnia, gait instability (mostly in elderly patients).
• Parkinsonian symptoms (tremor, akinesia, hypertonia) have been reported, typically reversible upon discontinuation of treatment.

Drug interaction

Formal interaction studies have not been performed. However, due to its metabolic pathway and properties, the following should be considered:

• Given the potential for dizziness and drowsiness, a pharmacodynamic interaction leading to an additive effect is possible when administered with other centrally sedating drugs (e.g., benzodiazepines, barbiturates, opiate derivatives).
• As an antianginal agent used in combination therapy, its effects are complementary to those of hemodynamic agents. No negative interactions with standard antianginal drugs (beta-blockers, calcium antagonists, long-acting nitrates) have been reported.
• Caution is advised when prescribing with drugs that may cause or exacerbate parkinsonian symptoms.

Missed dose

If a dose is missed, the patient should take it as soon as they remember, 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. The patient should not take a double dose to make up for a forgotten one.

Overdose

Cases of overdose have been reported very rarely. Based on the known pharmacological profile, potential symptoms of significant overdose could include severe drowsiness, sedation, and hypotension. There is no specific antidote for trimetazidine overdose. Treatment should be symptomatic and supportive, including monitoring of vital signs and ECG. Gastric lavage may be considered if performed soon after ingestion.

Storage

• Keep this medicine 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.
• Store in the original package to protect from moisture.
• 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 purposes 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 product information provided here may not be exhaustive or fully up-to-date. Always refer to the latest local prescribing information approved by your national health authority.

Reviews

• “As a cardiologist, I find Vastarel a valuable tool in my arsenal for managing refractory angina. Its metabolic mechanism offers a different angle of attack, particularly in patients who are maxed out on or cannot tolerate standard therapies. I’ve observed a meaningful reduction in angina frequency in a significant subset of my patients.” – Dr. A. Sharma, Cardiologist
• “After adding Vastarel to my existing beta-blocker, the constant background fear of an angina attack has significantly reduced. I still carry my GTN spray, but I use it far less frequently. I’ve been able to walk further without chest pain.” – Patient, 68
• “The evidence from clinical trials supports its role as add-on therapy. It shows a consistent, albeit modest, benefit in reducing angina attacks and improving exercise capacity. Its safety profile is generally favorable, though the risk of movement disorders requires vigilance, especially in the elderly population.” – Clinical Pharmacologist Review
• “It took about six weeks to notice a definite improvement, but the change was clear. The side effects were minimal for me—a little dizziness at the very start that went away. It has given me a piece of my life back.” – Patient, 71