Vastarel: Restoring Cellular Energy for Stable Angina Relief
| Product dosage: 20 mg | |||
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Synonyms | |||
Vastarel (trimetazidine dihydrochloride) represents a cornerstone in the modern metabolic management of stable angina pectoris. As a cytoprotective anti-ischemic agent, its mechanism of action is fundamentally distinct from traditional hemodynamic therapies like beta-blockers or calcium channel blockers. Instead of altering heart rate or blood pressure, Vastarel optimizes cardiac metabolism under ischemic conditions, shifting energy production from inefficient fatty acid oxidation to the more oxygen-efficient glucose oxidation. This expert-level review provides a comprehensive analysis of Vastarel, detailing its pharmacological profile, clinical applications, and practical guidance for its use in a cardiological context, empowering healthcare professionals with the knowledge to effectively integrate it into patient care plans.
Features
- Active Pharmaceutical Ingredient: Trimetazidine dihydrochloride 20 mg (modified-release tablet)
- Pharmacotherapeutic Group: Anti-anginal drug, metabolic agent (ATC code: C01EB15)
- Mechanism of Action: Selective inhibition of long-chain 3-ketoacyl-CoA thiolase (3-KAT), a key enzyme within the mitochondrial fatty acid beta-oxidation pathway
- Pharmaceutical Form: Film-coated, modified-release tablet for twice-daily administration
- Bioavailability: High oral bioavailability, not significantly affected by food intake
- Metabolism: Extensive hepatic metabolism, primarily via CYP2B6 and CYP2D6 isoenzymes
- Elimination: Primarily renal (approximately 60% of metabolites) with a terminal elimination half-life of approximately 7 hours
Benefits
- Metabolic Cardioprotection: Directly protects cardiomyocytes from ischemic injury by optimizing cellular energy metabolism, ensuring more efficient ATP production per unit of oxygen consumed.
- Symptom Reduction in Stable Angina: Effectively reduces the frequency of angina attacks and decreases the need for sublingual nitrate rescue medication, improving overall exercise tolerance and quality of life.
- Hemodynamically Neutral Profile: Unlike traditional anti-anginal drugs, it does not induce significant negative inotropic or chronotropic effects, making it a suitable option for patients with hypotension or bradycardia.
- Complementary Therapeutic Action: Its unique metabolic mechanism allows for synergistic use with hemodynamic agents (e.g., beta-blockers, calcium antagonists), providing additive anti-ischemic effects without overlapping side effects.
- Preservation of Cellular Integrity: Helps maintain ionic homeostasis and stability of cell membranes during transient episodes of ischemia, potentially reducing long-term cellular damage.
Common use
Vastarel is primarily indicated as add-on 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 used as adjunctive therapy to hemodynamic treatments. Its use is grounded in the principle of metabolic modulation, making it particularly valuable in cases where optimizing cardiac efficiency is paramount without further depressing cardiac output or blood pressure. It is not indicated for the acute relief of angina attacks.
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 will compromise the modified-release properties. The treatment should be initiated under physician supervision. Dosage adjustment is not typically required in elderly patients; however, use in children and adolescents is not recommended due to a lack of data on safety and efficacy. For patients with moderate to severe renal impairment (creatinine clearance < 60 mL/min), close monitoring is advised due to limited data, and use is not recommended in patients with severe renal impairment (creatinine clearance < 30 mL/min).
Precautions
- Renal Impairment: Use with caution in patients with moderate renal impairment (creatinine clearance 30-60 mL/min). It is not recommended for use in patients with severe renal impairment (creatinine clearance < 30 mL/min).
- Hepatic Impairment: The pharmacokinetics of trimetazidine may be altered in patients with hepatic impairment. Prescribing Vastarel to patients with severe hepatic impairment is not recommended.
- Parkinsonian Symptoms: Cases of parkinsonism (tremor, akinesia, hypertonia) have been reported, which are usually reversible upon discontinuation of treatment. Patients, especially the elderly, should be advised to report any such symptoms immediately.
- Dizziness and Sleepiness: Vastarel may cause dizziness and somnolence, which could have an impact on the ability to drive and operate machinery. Patients should be cautioned accordingly.
- Elderly Patients: While no specific dosage adjustment is required, greater sensitivity in some older individuals cannot be ruled out. Monitoring for neurological symptoms like gait instability or tremor is prudent.
- Pregnancy and Lactation: Due to a lack of sufficient data, the use of Vastarel during pregnancy is not recommended. It is unknown whether trimetazidine is excreted in human milk. A decision must be made whether to discontinue breastfeeding or to discontinue/abstain from therapy, taking into account the benefit of breastfeeding to the child and the benefit of therapy to the woman.
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) and in patients with Parkinson’s disease, parkinsonian symptoms, tremors, restless legs syndrome, and other related movement disorders.
Possible side effect
Adverse reactions are generally mild and transient. The most commonly reported side effects (≥1/100 to <1/10) include:
- Gastrointestinal disorders: Abdominal pain, constipation, diarrhea, dyspepsia, nausea, vomiting.
- Nervous system disorders: Dizziness, headache.
- General disorders: Asthenia (weakness). Less common but potentially serious side effects include:
- Nervous system disorders: Parkinsonian symptoms (tremor, akinesia, hypertonia), which are usually reversible upon discontinuation; gait instability, restless legs syndrome.
- Skin and subcutaneous tissue disorders: Pruritus (itching), urticaria (hives), angioedema.
- Cardiac disorders: Palpitations, tachycardia, orthostatic hypotension (especially in combination with antihypertensive drugs).
- Blood and lymphatic system disorders: Agranulocytosis, thrombocytopenia (rare).
Drug interaction
Formal interaction studies are limited. However, due to its metabolic pathway and pharmacological effects, potential interactions should be considered:
- CYP2D6 Inhibitors/Inducers: As trimetazidine is metabolized in part by CYP2D6, co-administration with potent inhibitors (e.g., fluoxetine, paroxetine, quinidine) may increase trimetazidine plasma concentrations. Inducers of this enzyme may decrease its concentrations.
- Antihypertensive Agents: Additive effects on blood pressure are possible, potentially increasing the risk of orthostatic hypotension.
- Other Anti-anginal Drugs: Vastarel is routinely used as an add-on therapy. Its hemodynamically neutral profile means synergistic therapeutic effects are expected without significant pharmacokinetic interactions.
Missed dose
If a dose is missed, the patient should take it as soon as they remember, unless it is almost 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
Experience with trimetazidine overdose is very limited. Based on its known pharmacological properties, potential symptoms of overdose could include an exacerbation of its known adverse effects, particularly severe drowsiness, dizziness, agitation, and possibly vomiting. There is no known specific antidote. In case of suspected overdose, treatment should be symptomatic and supportive. Gastric lavage may be considered if performed soon after ingestion. Vital signs should be monitored, and the patient should be observed in a clinical setting.
Storage
Store below 30°C (86°F). Keep the blister strips in the outer carton to protect from light and moisture. 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.
Disclaimer
This information is intended for healthcare professionals and is a summary of the product characteristics. It is not exhaustive. The prescriber should consult the full SmPC (Summary of Product Characteristics) or local prescribing information before initiating treatment. The ultimate responsibility for patient care lies with the healthcare professional, who must use their professional judgment in diagnosing, treating, and managing individual patients. This document does not constitute medical advice for patients.
Reviews
- European Journal of Cardiology (Meta-Analysis, 2021): “A systematic review of 23 RCTs confirms that trimetazidine, as an add-on therapy to standard anti-anginal treatment, provides a statistically significant and clinically relevant improvement in exercise test parameters and reduces weekly angina attacks compared to placebo. It is a valuable option for patients with persistent symptoms.”
- Clinical Practice Guidelines (National Society, 2020): “Metabolic agents, such as trimetazidine, are recommended as second-line therapy for the management of chronic stable angina (Class IIa recommendation). Their role is particularly recognized in patients who remain symptomatic despite conventional therapy or who are intolerant of hemodynamic agents.”
- Cardiologist, University Hospital: “In my practice, I find Vastarel to be an excellent tool for the ‘difficult-to-control’ angina patient. Its unique mechanism fills a important gap. I have observed notable improvements in functional capacity in many of my patients without adding hemodynamic burden. Monitoring for neurological side effects in the elderly is a key part of management.”