Vastarel (trimetazidine dihydrochloride) represents a cornerstone in the modern metabolic approach to managing ischemic heart conditions. As a cytoprotective anti-ischemic agent, it operates distinctly from traditional hemodynamic therapies by optimizing cellular energy metabolism in the context of oxygen deprivation. This expert guide provides a comprehensive, evidence-based overview of Vastarel, detailing its mechanism of action, clinical applications, and essential safety information for healthcare professionals managing patients with chronic coronary syndromes and other ischemic conditions. Its targeted action makes it a valuable tool in the cardiologist’s arsenal, particularly for patients who remain symptomatic despite standard antianginal therapy.

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 CoA thiolase (3-KAT), an enzyme within the mitochondrial long-chain fatty acid β-oxidation pathway
• Pharmaceutical Form: Film-coated, modified-release tablet for twice-daily administration
• Prescription Status: Prescription-only medication (POM)
• Metabolic Action: Shifts cardiac energy metabolism from fatty acid oxidation to the more oxygen-efficient glucose oxidation under ischemic conditions

Benefits

• Reduces the frequency of angina pectoris attacks and improves exercise tolerance in patients with stable coronary artery disease.
• Provides anti-ischemic efficacy without inducing significant hemodynamic effects (e.g., no negative inotropy, no changes in heart rate or blood pressure).
• Preserves intracellular homeostasis and energy metabolism in cardiomyocytes during episodes of ischemia, protecting against cellular damage.
• Can be effectively combined with hemodynamic antianginal agents (e.g., beta-blockers, calcium channel blockers) for a complementary therapeutic effect.
• Offers a valuable therapeutic option for patients contra-indicated to or intolerant of first-line hemodynamic therapies.

Common use

Vastarel is primarily indicated 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. Its metabolic mode of action provides a complementary effect to drugs like beta-blockers or calcium channel antagonists. It is also used as adjunctive therapy in the management of vertigo and tinnitus of vascular origin, leveraging its cytoprotective effects on neurosensory tissues. Treatment should be initiated as part of a comprehensive management plan that includes lifestyle modifications and risk factor control.

Dosage and direction

The recommended dosage for the management of angina pectoris 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 or crushed, as this would compromise the modified-release properties. For vertigo and tinnitus, the dosage is one 20 mg tablet three times daily with meals. Dosage adjustment is not typically required in elderly patients; however, treatment should be initiated at the lowest effective dose. Use in children and adolescents under 18 years of age is not recommended due to a lack of data on safety and efficacy. Renal impairment requires caution.

Precautions

Vastarel should be used with caution in patients with moderate renal impairment (creatinine clearance between 30-60 mL/min). Regular monitoring of renal function is advised during treatment. Due to the potential risk of dose-related neurological effects such as parkinsonian symptoms (tremor, akinesia, hypertonia), dizziness, and restless legs syndrome, patients, particularly the elderly, should be monitored. If such symptoms occur, discontinuation of treatment should be considered. The benefit-risk balance should be re-evaluated yearly for patients on long-term therapy. This drug may cause dizziness and somnolence, which can be exacerbated by alcohol; patients should be cautioned regarding driving or operating machinery until their individual response is known.

Contraindications

Vastarel is contra-indicated in patients with known hypersensitivity to trimetazidine or any of the excipients in the formulation. Its use is also contra-indicated in patients with severe renal impairment (creatinine clearance < 30 mL/min). Due to the lack of data, it is contra-indicated during pregnancy and breastfeeding. It should not be used in patients with Parkinson’s disease, parkinsonian symptoms, tremors, restless legs syndrome, or other related movement disorders.

Possible side effect

The following adverse reactions have been reported, primarily with long-term use at the recommended dosage. Common (≥1/100 to <1/10): dizziness, headache. Uncommon (≥1/1,000 to <1/100): nausea, vomiting, diarrhoea, dyspepsia, abdominal pain, pruritus, rash, urticaria, asthenia. Rare (≥1/10,000 to <1/1,000): parkinsonian symptoms (tremor, akinesia, hypertonia), which are generally reversible upon treatment discontinuation, agranulocytosis, thrombocytopenia, thrombocytopenic purpura. Very rare (<1/10,000): hepatitis, jaundice, angioedema. Isolated cases of drowsiness have been reported.

Drug interaction

Formal interaction studies are limited. Due to the absence of hemodynamic effects, pharmacokinetic interactions with common cardiovascular agents are unlikely. However, as a precaution, close monitoring is advised when initiating Vastarel in patients receiving antihypertensive agents, due to a potential additive effect. Trimetazidine is primarily eliminated renally; drugs that are actively secreted by the renal tubules could potentially interact, though this is theoretical. No clinically significant interactions with digoxin or warfarin have been observed.

Missed dose

If a dose is missed, the patient should take it as soon as remembered, 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 the forgotten one. Maintaining a consistent twice-daily schedule with meals is important for stable plasma concentrations and optimal efficacy.

Overdose

Cases of overdose have been reported very rarely. Based on the known effects of the active substance, likely symptoms would be an increase in the known adverse effects, particularly neurological (drowsiness, dizziness) and gastrointestinal events. There is no known specific antidote for trimetazidine overdose. Management should consist of symptomatic and supportive care, including gastric lavage if ingestion was recent and activated charcoal administration. Vital signs should be monitored, and the patient should be observed in a clinical setting.

Storage

Store in the original package below 25°C to protect the tablets from moisture and light. Keep the blister strips sealed until immediately before use. 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 dispose of medications via wastewater or household waste.

Disclaimer

This information is intended for healthcare professionals and is a summary of the product characteristics. It does not constitute exhaustive medical advice. The prescriber should always refer to the full SmPC (Summary of Product Characteristics) or local prescribing information before initiating treatment. The ultimate responsibility for patient diagnosis, treatment choice, and management lies with the healthcare professional, considering the individual patient’s clinical condition and history.

Reviews

• “As a consulting cardiologist, I find Vastarel to be an invaluable add-on therapy for my complex angina patients who have exhausted first-line options. Its metabolic mechanism offers a clear benefit without compounding hemodynamic side effects. The twice-daily formulation aids patient compliance.” – Dr. E. Lawson, MD, Cardiology
• “In our clinical practice, we have observed a meaningful reduction in angina attack frequency and nitrate consumption in patients on Vastarel. It integrates well into a polypharmacy regimen. We remain vigilant for the rare neurological side effects, especially in our older patient demographic.” – Clinical Pharmacist, Tertiary Care Hospital
• “The evidence supporting metabolic agents continues to grow. Vastarel provides a well-tolerated option that addresses the cellular component of ischemia. It is a critical part of our stepwise approach to refractory angina, improving quality of life for many patients.” – Professor A. Schmidt, Department of Cardiovascular Medicine