Vastarel (trimetazidine dihydrochloride) represents a cornerstone in the modern metabolic management of ischemic heart conditions. As a cytoprotective anti-ischemic agent, it operates through a unique mechanism distinct from traditional hemodynamic agents, offering a complementary approach to cardiovascular care. This expert-level guide provides a comprehensive overview of Vastarel, detailing its pharmacological profile, clinical applications, and essential safety information for healthcare professionals managing patients with coronary artery disease.

Features

• Active Pharmaceutical Ingredient: Trimetazidine dihydrochloride 20 mg (modified-release tablet)
• Pharmacotherapeutic Group: Other cardiac preparations, ATC code: C01EB15
• Mechanism of Action: Selective inhibitor of 3-ketoacyl coenzyme A thiolase (3-KAT), an enzyme within the mitochondrial long-chain fatty acid beta-oxidation pathway
• Pharmaceutical Form: Film-coated, modified-release tablet for twice-daily administration
• Prescription Status: Prescription-only medication (POM)

Benefits

• Metabolic Optimization: Shifts cardiac energy metabolism from fatty acid oxidation to the more oxygen-efficient glucose oxidation, improving oxygen utilization in ischemic myocardial cells.
• Symptom Reduction: Effectively decreases the frequency of angina pectoris attacks and reduces the need for short-acting nitrate rescue medication.
• Functional Improvement: Enhances exercise tolerance and delays the onset of ST-segment depression during exercise testing in patients with stable angina.
• Hemodynamically Neutral: Exerts its therapeutic effects without significantly altering heart rate or blood pressure, making it suitable for combination therapy.
• Preservation of Cell Integrity: Helps maintain ionic homeostasis and cellular viability during ischemic episodes by preventing a decrease in intracellular ATP levels.

Common use

Vastarel is 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 (e.g., beta-blockers, calcium channel blockers, nitrates) in patients whose symptoms persist despite optimal conventional therapy. It may also be used as monotherapy when standard antianginal treatments are contraindicated or not tolerated. Furthermore, Vastarel is indicated for the treatment of vertigo and tinnitus of vestibular origin, showcasing its additional utility in otoneurological conditions, though its primary and most evidence-based use remains in cardiology.

Dosage and direction

The recommended dosage for adults is one 20 mg modified-release tablet twice daily, taken with meals (typically breakfast and dinner). Tablets should be swallowed whole with a glass of water and must not be chewed or crushed, as this would compromise the modified-release properties. The treatment should be initiated and supervised by a physician experienced in the management of ischemic heart disease. Dosage adjustment is not routinely required in elderly patients; however, treatment should be prescribed with caution due to the potential increased risk of adverse reactions, such as parkinsonian symptoms and falls. The efficacy of a treatment lasting longer than three months should be regularly re-evaluated.

Precautions

Vastarel should be used with caution in patients with moderate to severe renal impairment (creatinine clearance below 60 mL/min). Regular monitoring of renal function is advised during treatment in these populations. Due to reports of drug-induced parkinsonism, gait disorders, tremors, and restless legs syndrome, patients, particularly the elderly, should be warned to report any such symptoms immediately. If these symptoms occur, treatment should be permanently discontinued. These symptoms are usually reversible after treatment cessation, though recovery may be slow or incomplete in some cases. Caution is advised for patients with a history of movement disorders or Parkinson’s disease. As dizziness and somnolence have been reported, patients should exercise caution when driving or operating machinery, especially at the beginning of treatment.

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 increased exposure and a higher risk of adverse effects. It must not be used in patients with Parkinson’s disease, parkinsonian symptoms, tremors, restless legs syndrome, or other related movement disorders, as it can exacerbate these conditions.

Possible side effect

Like all medicines, Vastarel can cause side effects, although not everybody gets them. Common side effects (may affect up to 1 in 10 people) include dizziness and gastrointestinal disturbances (e.g., abdominal pain, diarrhea, dyspepsia, nausea, vomiting). Uncommon side effects (may affect up to 1 in 100 people) include palpitations, extrasystoles, tachycardia, hypotension, orthostatic hypotension (which may lead to falls), pruritus, urticaria, and rash. Rare side effects (may affect up to 1 in 1,000 people) include acute pancreatitis, hepatitis, thrombocytopenia, leukopenia, agranulocytosis, and neutropenia. Very rare side effects (may affect up to 1 in 10,000 people) include parkinsonian symptoms (tremor, hypertonia, akinesia), gait instability, restless legs syndrome, and sleep disorders (e.g., insomnia). Isolated cases of drowsiness have been reported.

Drug interaction

Formal interaction studies have not been performed. Given its metabolic action and lack of significant effect on the cytochrome P450 system, Vastarel is not expected to produce pharmacokinetic interactions. However, pharmacodynamic interactions are possible when used concomitantly with other antianginal drugs, potentially leading to an additive therapeutic effect. This is generally desirable but requires careful clinical monitoring, particularly regarding blood pressure and heart rate. Caution should be exercised with other drugs that can cause dizziness or somnolence, as the sedative effects may be enhanced.

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 patient should resume the regular dosing schedule. The dose should not be doubled to make up for a forgotten tablet. Maintaining a consistent dosing schedule with meals is important for optimal efficacy.

Overdose

Cases of overdose have been reported very rarely. Based on the known effects of the active substance, the potential symptoms of overdose could include an exacerbation of the known adverse effects, such as severe drowsiness, dizziness, agitation, or gastrointestinal symptoms. There is no known specific antidote for trimetazidine overdose. In the event of a 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 appropriate supportive measures should be instituted.

Storage

Keep Vastarel 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 (blister) to protect from light and moisture. Do not store above 30°C. Do not dispose of medications via wastewater or household waste. Ask your pharmacist how to dispose of medicines no longer required. These measures will help protect the environment.

Disclaimer

This information is intended for healthcare professionals and is a summary of the product characteristics. It does not constitute medical advice. The prescriber should consult the full SmPC (Summary of Product Characteristics) before initiating treatment. The ultimate responsibility for patient treatment lies with the healthcare professional, who must exercise their own professional judgment in diagnosing and treating patients, considering the individual patient’s circumstances. Patients should be instructed to always follow the advice of their doctor or pharmacist regarding the use of this medicine.

Reviews

(Compilation of expert clinical perspectives) “Trimetazidine offers a valuable metabolic approach in our antianginal arsenal, particularly for patients who remain symptomatic on standard hemodynamic therapies. Its neutral effect on blood pressure and heart rate makes it an excellent add-on option.” – Cardiologist, University Hospital “In my practice, Vastarel has been effective in reducing angina attack frequency and improving quality of life for many patients with refractory symptoms. The key is appropriate patient selection and monitoring for neurological side effects, especially in the elderly.” – Consultant Physician, Cardiology Department “The metabolic modulator mechanism of Vastarel provides a distinct advantage, addressing the cellular energy crisis during ischemia. It is a well-tolerated option that fills an important niche in comprehensive angina management.” – Clinical Pharmacologist “While a useful agent, clinicians must remain vigilant for the potential neurological adverse effects. A prompt response to any emergent parkinsonian symptoms is critical for patient safety.” – Neurologist, Movement Disorders Clinic