Vastarel

Vastarel (trimetazidine dihydrochloride) is a metabolic agent specifically designed for the adjunctive treatment of stable angina pectoris. Unlike traditional anti-anginal medications that primarily work by altering hemodynamics—reducing heart rate, blood pressure, or vascular resistance—Vastarel operates at the cellular level. It optimizes cardiac energy metabolism under ischemic conditions, shifting ATP production from inefficient fatty acid beta-oxidation to the more oxygen-efficient glucose oxidation. This unique mechanism of action provides a cardioprotective effect, reducing the frequency of angina attacks and improving exercise tolerance without negatively impacting hemodynamic parameters. It represents a cornerstone in metabolic management for patients where conventional therapies are insufficient, contraindicated, or poorly tolerated.

Features

• Active ingredient: Trimetazidine dihydrochloride 35 mg modified-release tablet
• Pharmacotherapeutic classification: Metabolic agent, ATC code C01EB15
• Mechanism: Selective inhibition of long-chain 3-ketoacyl-CoA thiolase, a key enzyme in fatty acid beta-oxidation
• Formulation: Modified-release tablet for twice-daily dosing
• Prescription status: Pharmacy-only medicinal product
• Packaging: Blister packs of 30, 60, or 90 tablets

Benefits

• Reduces the frequency of angina attacks by improving myocardial energy efficiency
• Increases exercise tolerance and delays the onset of ischemia during physical exertion
• Provides anti-ischemic effects without negative hemodynamic consequences (no effect on heart rate or blood pressure)
• Serves as an adjunctive therapy when beta-blockers, calcium channel blockers, or nitrates are insufficient or contraindicated
• Offers a favorable safety profile with minimal risk of pharmacokinetic interactions
• Improves patient quality of life by enabling greater physical activity with reduced anginal symptoms

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 anti-anginal agents. It is particularly valuable in patients where hemodynamic modifications are undesirable, such as those with hypotension, bradycardia, or heart failure. The metabolic approach makes it suitable for elderly patients and those with comorbidities where traditional anti-anginal drugs might pose risks. It is used in combination with other anti-ischemic treatments or as monotherapy when standard options are not feasible.

Dosage and direction

The recommended adult dosage is one 35 mg modified-release tablet twice daily, taken with meals. Tablets should be swallowed whole with water and not chewed, crushed, or divided, as this would compromise the modified-release properties. Treatment should be initiated and supervised by a physician experienced in cardiology. The therapeutic effect typically becomes apparent within two to three weeks of initiation. Dosage adjustment is not required in elderly patients or those with renal impairment (creatinine clearance >30 mL/min). In cases of severe renal impairment (creatinine clearance <30 mL/min), use is not recommended due to limited data.

Precautions

Vastarel should be used with caution in patients with moderate renal impairment (creatinine clearance 30-60 mL/min). Regular monitoring of renal function is advised during long-term treatment. Although the drug has no direct hemodynamic effects, patients should be monitored for symptoms of Parkinsonism (tremor, rigidity, akinesia) and other movement disorders, as these have been reported during treatment. If such symptoms occur, discontinuation should be considered. Patients should be advised that Vastarel does not provide immediate relief of anginal attacks and should not be used as rescue medication. It is not recommended during pregnancy unless clearly necessary, and should be avoided during breastfeeding.

Contraindications

Hypersensitivity to trimetazidine or any excipients in the formulation. Severe renal impairment (creatinine clearance <30 mL/min). Parkinson’s disease, parkinsonian symptoms, tremors, restless legs syndrome, or other related movement disorders. Severe hepatic impairment. Use in children and adolescents under 18 years of age due to insufficient safety and efficacy data.

Possible side effects

Common (≥1/100 to <1/10): Dizziness, headache, gastrointestinal disturbances (nausea, vomiting, diarrhea, abdominal pain). Uncommon (≥1/1,000 to <1/100): Palpitations, extrasystoles, tachycardia, hypotension, pruritus, rash, urticaria, asthenia. Rare (≥1/10,000 to <1/1,000): Agranulocytosis, thrombocytopenia, thrombocytopenic purpura, hepatitis, acute pancreatitis, parkinsonian symptoms (tremor, rigidity, akinesia), gait instability, restless legs syndrome, other movement disorders. Very rare (<1/10,000): Angioedema, decreased vigilance, confusion, hallucinations. Isolated cases of drowsiness and insomnia have been reported.

Drug interaction

Vastarel has low potential for pharmacokinetic interactions as it is not metabolized by cytochrome P450 enzymes. However, pharmacodynamic interactions may occur with other anti-anginal drugs, potentially enhancing the therapeutic effect. No clinically significant interactions have been observed with beta-blockers, calcium channel blockers, nitrates, antiplatelet agents, statins, or oral hypoglycemics. Caution is advised when co-administering with drugs that may cause movement disorders (e.g., neuroleptics, metoclopramide) due to potential additive effects.

Missed dose

If a dose is missed, it should be taken as soon as remembered 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. Double doses should not be taken to make up for a missed dose. Patients should be educated on maintaining regular dosing intervals to ensure stable plasma concentrations.

Overdose

Cases of overdose are rare. Reported symptoms include flushing, hypotension, tachycardia, drowsiness, and gastrointestinal discomfort. There is no specific antidote. Treatment should be symptomatic and supportive, including gastric lavage if ingestion was recent and activated charcoal administration. Vital signs should be monitored, and appropriate supportive measures instituted based on clinical presentation. Hemodialysis is not effective due to high protein binding.

Storage

Store below 30°C in the original packaging to protect from light and moisture. Keep out of sight and reach of children. Do not use after the expiration date printed on the packaging. Proper disposal should be in accordance with local regulations, not via wastewater or household waste.

Disclaimer

This information is provided for educational purposes only and does not constitute medical advice. Vastarel is a prescription medication that should only be used under the supervision of a qualified healthcare professional. The prescribing physician should be consulted for complete information regarding indications, contraindications, warnings, precautions, and adverse reactions. Individual patient response may vary, and treatment decisions should be based on professional medical judgment considering the patient’s complete medical history and current condition.

Reviews

Clinical studies demonstrate that Vastarel significantly reduces weekly angina attack frequency by approximately 40-50% and decreases nitrate consumption by a similar margin. Exercise tolerance tests show consistent improvement in time to onset of ischemia (1 mm ST-segment depression) and total exercise duration. In a meta-analysis of randomized controlled trials, trimetazidine showed significant improvement in left ventricular ejection fraction in heart failure patients with ischemic etiology. Long-term observational studies indicate maintained efficacy over 12 months with good tolerability. Specialist consensus guidelines recognize metabolic agents like trimetazidine as valuable options in management strategies for stable coronary artery disease, particularly in patients with persistent symptoms despite conventional therapy.