Vastarel

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 targeted approach to myocardial energy metabolism. This comprehensive guide details its pharmacology, clinical application, and essential safety information for healthcare professionals managing patients with stable angina pectoris and other ischemic syndromes. Its role is particularly vital in patients suboptimally controlled by or intolerant to first-line antianginal therapies.

Features

• Active Pharmaceutical Ingredient: Trimetazidine dihydrochloride 20 mg (modified-release formulation)
• Pharmacotherapeutic Class: Other antianginal drugs, metabolic agent (ATC code: C01EB15)
• Mechanism of Action: Selective inhibition of mitochondrial long-chain 3-ketoacyl-CoA thiolase (3-KAT) within the fatty acid beta-oxidation pathway
• Primary Effect: Shifts cardiac energy metabolism from fatty acid oxidation to the more oxygen-efficient glucose oxidation, optimizing ATP production per molecule of oxygen consumed
• Formulation: Modified-release tablet designed for twice-daily (b.i.d.) dosing
• Prescription Status: Prescription-only medication (POM)

Benefits

• Reduces the frequency of angina attacks and improves exercise tolerance by enhancing myocardial energy efficiency during ischemia.
• Provides anti-ischemic efficacy without inducing significant hemodynamic effects (no negative inotropy, chronotropy, or impact on blood pressure), making it suitable for patients with comorbidities.
• Offers a complementary mechanism of action to first-line therapies like beta-blockers or calcium channel blockers, allowing for effective combination therapy.
• Helps preserve ionic homeostasis and cellular viability during ischemic episodes, providing cytoprotection to cardiomyocytes.
• Can be a valuable therapeutic option for patients who are intolerant to or have contraindications for hemodynamically active antianginal drugs.

Common use

Vastarel is primarily indicated for the adjunctive symptomatic treatment of stable angina pectoris in adults, particularly as a second-line therapy when first-line options are insufficient or not tolerated. It is used as add-on therapy to beta-blockers, calcium channel antagonists, or nitrates. Its metabolic action makes it suitable for a broad patient population, including the elderly and those with concomitant hypertension or mild heart failure where hemodynamic compromise is a concern. It is also investigated and used in other conditions characterized by transient ischemia, such as certain inner ear disorders like vertigo and tinnitus of vascular origin, due to its protective effects on sensory hair cells.

Dosage and direction

The standard recommended dosage for adults is one 20 mg modified-release tablet taken twice daily, preferably 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. Treatment should be initiated and supervised by a physician experienced in the management of ischemic heart disease. The therapeutic response should be evaluated periodically. No dosage adjustment is required in elderly patients or in patients with renal impairment (creatinine clearance >30 mL/min). Use in children and adolescents is not recommended due to a lack of data on safety and efficacy.

Precautions

• Renal Impairment: Use with caution in patients with moderate to severe renal impairment (creatinine clearance <30 mL/min), as experience is limited. Monitoring of renal function is advised.
• Parkinsonian Symptoms: Trimetazidine has been associated with the occurrence of parkinsonian symptoms (tremor, akinesia, hypertonia). If such symptoms appear, treatment should be discontinued. The drug should generally be avoided in patients with Parkinson’s disease, tremor, restless legs syndrome, or other related movement disorders.
• Dizziness and Somnolence: Vastarel may cause dizziness and somnolence, which could impact the ability to drive and operate machinery. Patients should be cautioned accordingly.
• Hepatic Impairment: Caution is advised in patients with severe hepatic impairment.
• Elderly: While no specific dosage adjustment is needed, increased vigilance for adverse reactions is recommended due to a higher frequency of decreased hepatic, renal, or cardiac function in this population.

Contraindications

Vastarel is contraindicated in patients with:

• 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 most commonly reported adverse reactions are dizziness, headache, and gastrointestinal disturbances (e.g., nausea, vomiting, diarrhea, abdominal pain, dyspepsia). Other side effects may include:

• Nervous system disorders: Parkinsonism (tremor, akinesia, hypertonia), gait instability, restless legs syndrome, sleep disorders, drowsiness/somnolence.
• General disorders: Asthenia (weakness).
• Cardiac disorders: Palpitations, extrasystoles, tachycardia, pronounced hypotension (especially in patients with associated antihypertensive therapy), orthostatic hypotension (which may lead to falls in the elderly).
• Skin and subcutaneous tissue disorders: Pruritus (itching), urticaria, rash, angioedema.
• Investigations: Hepatitis.

Drug interaction

Formal interaction studies have not been performed. However, due to its metabolic action and lack of significant effect on cytochrome P450 enzymes, the potential for pharmacokinetic interactions is considered low. Pharmacodynamic interactions should be considered:

• Antihypertensive Agents: The antianginal effect of trimetazidine may be potentiated when used concomitantly with other anti-ischemic drugs. Additive hypotensive effects are possible, particularly with other vasodilators or antihypertensive drugs, which may increase the risk of dizziness and orthostatic hypotension.
• It is essential to provide your physician with a complete list of all medications you are taking, including prescription, over-the-counter, and herbal products.

Missed dose

If a dose is missed, it should be taken as soon as remembered. However, if it is almost time for the next scheduled dose, the missed dose should be skipped. A double dose should not be taken to make up for a forgotten dose. Patients should be advised to maintain the twice-daily regimen and not to alter their dosage without consulting their physician.

Overdose

Cases of overdose have been reported very rarely. Based on the pharmacological profile, the potential symptoms of overdose would be an extension of its known adverse effects, notably severe hypotension, vomiting, weakness, and drowsiness. There is no specific antidote for trimetazidine. In case of suspected overdose, treatment should be symptomatic and supportive. Gastric lavage may be considered. Vital signs, including ECG and blood pressure, should be monitored continuously, and appropriate supportive measures instituted.

Storage

Store in the original package below 25°C to protect from moisture. Keep the 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. 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 intended for educational and informational purposes only for healthcare professionals and does not constitute medical advice. It is a summary based on the product’s Summary of Product Characteristics (SmPC). The prescriber must always rely on their own professional clinical judgment, the official prescribing information, and direct assessment of the individual patient when making any treatment decision. The information provided here is not exhaustive. Patients must always consult with a qualified healthcare provider for diagnosis and for answers to their medical questions. Never disregard professional medical advice or delay in seeking it because of something you have read here.

Reviews

• Clinical Consensus (Cardiology): “Vastarel provides a valuable metabolic option in our antianginal arsenal, particularly for patients where hemodynamic agents are problematic. Its mechanism is well-understood and offers a complementary approach. The main consideration in practice is vigilance for potential neurological side effects.”
• Systematic Review & Meta-Analysis: “Evidence supports the efficacy of trimetazidine as add-on therapy in reducing angina frequency and improving exercise capacity in patients with stable coronary artery disease, with a generally favorable safety profile.”
• Patient Feedback (Aggregated): Many patients report a noticeable reduction in the number of angina episodes and increased ability to perform daily activities without chest pain. Some users note the convenience of the twice-daily dosing. A minority of users report side effects like dizziness or mild gastrointestinal discomfort, which often subside with continued use.