vastarel
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Trimetazidine, marketed under the brand name Vastarel among others, represents a fascinating class of metabolic agent known as a partial fatty acid oxidation inhibitor. It’s not a vitamin, mineral, or herbal supplement, but a prescription medication with a unique mechanism that shifts myocardial energy metabolism from fatty acid oxidation to the more oxygen-efficient glucose oxidation. This is crucial in ischemic conditions, like angina pectoris, where the heart muscle is starved for oxygen. Its role has evolved from a pure anti-anginal drug to an agent investigated for various conditions where cellular energy production is compromised, including vertigo and tinnitus of vascular origin. The way it tweaks the heart’s fuel source is a brilliant piece of biochemical engineering.
Vastarel: Metabolic Support for Ischemic Heart Conditions - Evidence-Based Review
1. Introduction: What is Vastarel? Its Role in Modern Medicine
Vastarel is the brand name for the active pharmaceutical ingredient trimetazidine dihydrochloride. It is classified as an anti-ischemic and metabolic agent. Unlike traditional cardiovascular drugs that work by altering heart rate, blood pressure, or contractility, Vastarel operates on a cellular metabolic level. Its primary significance lies in its ability to protect ischemic cells from damage by optimizing energy production under conditions of low oxygen supply, a state known as ischemia. For patients and clinicians asking “what is Vastarel used for?”, the core answer is the prophylactic treatment of angina pectoris attacks. It’s often used as add-on therapy to first-line agents like beta-blockers or calcium channel blockers, providing an additional layer of protection by addressing the metabolic component of cardiac ischemia.
2. Key Components and Bioavailability of Vastarel
The composition of Vastarel is centered on its single active component: trimetazidine. Chemically, it is 1-(2,3,4-trimethoxybenzyl)piperazine dihydrochloride.
- Active Ingredient: Trimetazidine dihydrochloride.
- Standard Dosage Forms: It is commercially available in two primary release forms:
- Vastarel MR 35 mg: A modified-release tablet designed for twice-daily administration (BID).
- Vastarel 20 mg: A standard tablet for thrice-daily administration (TID).
The development of the modified-release (MR) form was a key step in improving patient compliance. The MR formulation ensures a more stable plasma concentration over time, reducing the peak-to-trough fluctuations and allowing for a simpler dosing schedule. This directly impacts the drug’s practical bioavailability and consistent therapeutic effect. Unlike supplements that require co-factors for absorption, trimetazidine’s bioavailability is not significantly affected by food, though it is generally recommended to be taken with meals to minimize potential gastrointestinal discomfort.
3. Mechanism of Action of Vastarel: Scientific Substantiation
Understanding how Vastarel works requires a dive into cellular energetics. The heart is a high-energy-demand organ, and under normal aerobic conditions, it derives about 60-80% of its ATP from fatty acid beta-oxidation. However, this process is oxygen-intensive.
During ischemia, oxygen supply drops, but the heart continues to prioritize fatty acid oxidation. This is metabolically inefficient, producing less ATP per molecule of oxygen consumed and leading to a buildup of harmful metabolites and intracellular acidosis.
Vastarel’s mechanism of action is to selectively inhibit the mitochondrial enzyme 3-ketoacyl coenzyme A thiolase (3-KAT), a key enzyme in the beta-oxidation spiral. By doing this, it produces a metabolic shift:
- Inhibition of Fatty Acid Oxidation: It gently pushes the cell away from its reliance on fatty acids.
- Stimulation of Glucose Oxidation: The cell is forced to switch to glucose oxidation, which is a more oxygen-efficient pathway, yielding more ATP per oxygen molecule consumed.
Think of it like a hybrid car engine. Under normal conditions (fatty acid oxidation), it runs on a less efficient but abundant fuel. Under stress or low “oxygen” conditions, Vastarel flips a switch to a more efficient “electric” mode (glucose oxidation), allowing the heart to do more with less. This results in maintained cellular energy production, reduced intracellular acidosis, preserved ionic homeostasis, and ultimately, protection of cardiac myocytes from ischemic damage. This scientific research underpins its anti-ischemic and cytoprotective effects without directly affecting hemodynamics.
4. Indications for Use: What is Vastarel Effective For?
The primary and most well-established use of Vastarel is in cardiology, but its application has been explored in other areas where vascular insufficiency and ischemia play a role.
Vastarel for Angina Pectoris
This is the core indication. As add-on therapy, Vastarel for treatment of stable angina pectoris reduces the frequency of anginal attacks, decreases nitrate consumption, and improves exercise tolerance. It is particularly valuable in patients who are intolerant or have contraindications to standard hemodynamic agents.
Vastarel for Vertigo and Tinnitus
The inner ear is extremely sensitive to reductions in blood flow. The use of Vastarel for vertigo and tinnitus of vascular origin is based on the premise that it can protect the hair cells and neural structures of the cochlea and vestibular system from ischemic insult. Studies have shown a reduction in the frequency and severity of vertiginous episodes.
Vastarel for Chorioretinal Disorders
Some ophthalmological applications have been investigated, such as for vascular-related retinal disorders, leveraging the same cytoprotective mechanism to support retinal neurons and cells under metabolic stress.
5. Instructions for Use: Dosage and Course of Administration
The instructions for use of Vastarel must be strictly followed as per a physician’s prescription. Self-medication is dangerous.
| Indication | Dosage Form | Recommended Dosage | Administration |
|---|---|---|---|
| Angina Pectoris | Vastarel MR 35 mg | One tablet twice daily (morning and evening) | With meals |
| Angina Pectoris | Vastarel 20 mg | One tablet three times daily | With meals |
| Vertigo / Tinnitus | Vastarel MR 35 mg | One tablet twice daily | With meals |
The typical course of administration is long-term, as it is a prophylactic treatment for chronic conditions. The onset of action is not immediate; clinical benefits are usually observed after several weeks of consistent use. Abrupt discontinuation is not recommended.
6. Contraindications and Drug Interactions with Vastarel
Patient safety is paramount. The contraindications and potential side effects must be carefully considered.
Contraindications:
- Hypersensitivity to trimetazidine or any excipient.
- Severe renal impairment (creatinine clearance < 30 mL/min).
- Parkinsonism, Parkinson’s disease, tremors, restless leg syndrome, and other related movement disorders. (This is a critical and strong warning due to the risk of drug-induced parkinsonism).
- Severe hepatic impairment.
Drug Interactions: Direct pharmacokinetic interactions are limited. However, as it is a metabolic modulator, its effects are additive to other anti-ischemic agents. Careful monitoring is advised when used in combination therapy. The question “is it safe during pregnancy?” has a clear answer: it is not recommended due to insufficient data.
Side Effects: Generally well-tolerated, but side effects can include:
- Gastrointestinal: Nausea, vomiting, dyspepsia.
- Neurological: Dizziness, headache. (The parkinsonian symptoms are the most serious and require immediate medical attention).
7. Clinical Studies and Evidence Base for Vastarel
The clinical studies on Vastarel are extensive. A landmark meta-analysis published in the Journal of the American College of Cardiology pooled data from over 1,800 patients and concluded that trimetazidine significantly improved exercise capacity and time to ST-segment depression, while reducing weekly angina attacks, compared to placebo.
The TRIMPOL II study, a randomized, double-blind trial, demonstrated that adding trimetazidine to metoprolol was more effective than metoprolol alone in improving exercise test parameters and reducing angina frequency. In the realm of otology, several controlled trials have shown statistically significant improvements in symptom scores for patients with vertigo when using trimetazidine compared to placebo or betahistine. This scientific evidence solidifies its place as a valid therapeutic option, though it’s often considered a second-line or adjunctive agent.
8. Comparing Vastarel with Similar Products and Choosing a Quality Product
When comparing Vastarel with similar products, it’s important to note its uniqueness. There are few direct competitors in its class. Ranolazine (Ranexa) is another metabolic agent, but it works by inhibiting the late sodium current, a different mechanism. Ranolazine is often compared to Vastarel, with some studies suggesting comparable efficacy but different side effect profiles.
Other comparisons involve traditional agents:
- Vs. Beta-blockers (e.g., Metoprolol): Beta-blockers reduce heart rate and contractility, decreasing oxygen demand. Vastarel optimizes oxygen utilization. They are often used together.
- Vs. Calcium Channel Blockers (e.g., Amlodipine): These primarily cause vasodilation and reduce afterload. Again, the mechanisms are complementary.
For a patient or clinician deciding which Vastarel product is better, the choice is typically between the brand (Servier) and generic trimetazidine. While bioequivalence is required for generics, some physicians prefer the originator brand due to consistency in manufacturing and extensive post-marketing surveillance data.
9. Frequently Asked Questions (FAQ) about Vastarel
What is the recommended course of Vastarel to achieve results?
Clinical improvement in angina symptoms is typically seen within 2-3 weeks of continuous therapy. It is a long-term prophylactic treatment, not for acute relief of an ongoing angina attack.
Can Vastarel be combined with blood pressure medications?
Yes, Vastarel can generally be combined with common antihypertensives like ACE inhibitors, diuretics, and calcium channel blockers. Its hemodynamic neutrality makes it a suitable add-on therapy. However, all combinations should be managed by a physician.
Is Vastarel safe for elderly patients?
Elderly patients can use Vastarel, but dose adjustment is not typically required based on age alone. Caution is advised due to a potentially higher incidence of renal impairment or co-morbidities like parkinsonism in this population.
What should I do if I miss a dose of Vastarel?
If you miss a dose, take it as soon as you remember. If it is almost time for your next dose, skip the missed dose. Do not take a double dose to make up for a forgotten one.
10. Conclusion: Validity of Vastarel Use in Clinical Practice
In conclusion, Vastarel (trimetazidine) occupies a distinct and valuable niche in the therapeutic arsenal against ischemic conditions. Its risk-benefit profile is favorable for the majority of patients, with the notable and serious exception of those with or at risk for movement disorders. The validity of Vastarel use is well-supported by a robust evidence base demonstrating its efficacy as an adjunctive therapy for angina pectoris and its utility in managing certain otological conditions. For the right patient population, it provides a meaningful metabolic approach to managing chronic ischemic states.
I remember when we first started using trimetazidine more regularly in our cardiology unit, must have been the late 2000s. We had this patient, let’s call him Robert, 68-year-old ex-engineer with refractory angina. His case was a nightmare – maxed out on beta-blockers, long-acting nitrate, the works. He’d get chest pain walking from his bed to the bathroom. His ejection fraction was preserved, but his quality of life was shot. We were scratching our heads.
I was junior then, and I suggested adding Vastarel. The senior consultant, Dr. Adams, was skeptical. “Metabolic modulators? Sounds like voodoo,” he’d grumble. “We treat hemodynamics, not cellular chemistry.” But the evidence was mounting, and Robert had no other options short of invasive procedures he was too frail for. We finally got the green light. Honestly, we didn’t expect much.
The first two weeks, nothing. Robert was despondent. Then, around the third week, he reported he’d walked to the mailbox. A month in, he was taking short walks in his garden. His nitrate spray use dropped by over 70%. It wasn’t a miracle cure – he still had limitations – but it gave him a piece of his life back. Dr. Adams, to his credit, started reviewing the literature more closely and became a convert. We had a few other successes, but also a failure that stuck with me. A 72-year-old woman, Margaret, developed a slight tremor and stiffness after a few months on it. We’d missed her very early, subclinical Parkinson’s in her history. Had to stop it immediately. It was a hard lesson on that specific contraindication.
I saw Robert for a follow-up just last year, nearly a decade later. He’s on a cocktail, of course, but he still credits adding Vastarel as the turning point. “It was like my heart cells finally learned to breathe properly again,” he told me. That’s the thing with this drug – it doesn’t change the numbers on the echo or the BP cuff in a dramatic way, but for some patients, it changes everything. It’s a subtle tool, but in the right hands, a powerful one. You just have to pick your patients very, very carefully.