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 typical vasodilator or anti-anginal, but rather works by shifting myocardial energy metabolism during ischemia. You’ll find it prescribed primarily for stable angina pectoris when first-line therapies like beta-blockers or calcium channel blockers aren’t sufficient or tolerated. The mechanism is quite elegant - during oxygen deprivation, it inhibits the mitochondrial enzyme 3-ketoacyl coenzyme A thiolase, which forces the heart muscle to switch from fatty acid oxidation to the more oxygen-efficient glucose oxidation. This metabolic modulation can relieve anginal symptoms and improve exercise capacity without significantly affecting hemodynamics. The standard formulation is Vastarel 20 mg (trimetazidine dihydrochloride), typically administered as a modified-release tablet to maintain stable plasma concentrations.
1. Introduction: What is Vastarel? Its Role in Modern Medicine
What is Vastarel used for? In clinical practice, we’re talking about a second-line anti-ischemic agent that’s been around since the late 1970s but has gained renewed interest with better understanding of cardiac metabolism. The benefits of Vastarel extend beyond just symptom relief - we’re looking at cellular protection during ischemic episodes. The medical applications have expanded from initial angina treatment to investigating potential benefits in heart failure, diabetic cardiomyopathy, and even some neurological conditions due to its cytoprotective effects. Unlike many cardiovascular drugs that work on receptors or ion channels, Vastarel operates at the metabolic level, making it particularly useful in patients who can’t tolerate hemodynamic changes.
2. Key Components and Bioavailability Vastarel
The composition of Vastarel centers around trimetazidine dihydrochloride as the active pharmaceutical ingredient. The standard release form is the modified-release tablet designed for twice-daily dosing, though immediate-release formulations exist in some markets. The bioavailability of Vastarel is approximately 90% after oral administration, with peak plasma concentrations reached within 5 hours for the modified-release form. Food doesn’t significantly affect absorption, which is convenient for patient compliance.
The molecular structure features a piperazine derivative that’s crucial for its metabolic activity. What’s interesting is that despite being a small molecule, it has specific mitochondrial targeting properties. The modified-release formulation uses a hydrophilic matrix system that controls drug release through hydration and gel formation - this maintains relatively stable plasma levels between doses, which is important for continuous metabolic modulation.
3. Mechanism of Action Vastarel: Scientific Substantiation
How Vastarel works is fundamentally different from most cardiovascular drugs. While beta-blockers reduce heart rate and contractility, and calcium channel blockers affect vascular tone, Vastarel works at the cellular energy production level. The mechanism of action involves selective inhibition of long-chain 3-ketoacyl-CoA thiolase in the mitochondrial matrix. This enzyme is crucial for the final step of fatty acid beta-oxidation.
During ischemia, fatty acid metabolism becomes particularly inefficient - it consumes more oxygen per ATP molecule produced compared to glucose oxidation. By partially blocking fatty acid oxidation, Vastarel essentially forces the cardiac myocyte to switch to glucose oxidation, which generates more ATP per oxygen molecule consumed. Think of it like optimizing fuel efficiency in a car engine when fuel is scarce.
The effects on the body are primarily metabolic rather than hemodynamic. You don’t see significant changes in heart rate, blood pressure, or contractility, which makes it particularly valuable in patients who are hemodynamically compromised. The scientific research shows it reduces intracellular acidosis, calcium overload, and free radical damage during ischemia - all while maintaining mechanical function with less oxygen consumption.
4. Indications for Use: What is Vastarel Effective For?
Vastarel for Angina Pectoris
This remains the primary approved indication. Multiple randomized trials have shown that adding Vastarel to conventional anti-anginal therapy can further reduce angina attacks and improve exercise tolerance. The European Society of Cardiology guidelines mention it as a second-line option when first-line therapies are insufficient.
Vastarel for Heart Failure
Emerging evidence suggests potential benefits in heart failure patients, particularly those with ischemic cardiomyopathy. The metabolic approach may improve myocardial efficiency in failing hearts, though this remains off-label in most jurisdictions.
Vastarel for Vertigo and Tinnitus
Interestingly, the cytoprotective effects extend to the inner ear, and Vastarel has approval in some countries for vestibular disorders. The mechanism likely involves protection of hair cells and vestibular neurons from ischemic damage.
Vastarel for Visual Disorders
Some ophthalmological applications exist for vascular-related visual disturbances, again leveraging its cytoprotective properties in ischemic retinal conditions.
5. Instructions for Use: Dosage and Course of Administration
The standard dosage for most indications is 20 mg three times daily with meals for immediate-release formulations, or 35 mg twice daily for the modified-release version. The course of administration is typically long-term for chronic conditions like angina.
| Indication | Dosage | Frequency | Duration |
|---|---|---|---|
| Stable angina | 20 mg | 3 times daily with food | Long-term |
| Prophylaxis | 35 mg MR | 2 times daily | Continuous |
| Vertigo treatment | 20 mg | 3 times daily | 3-6 months |
How to take Vastarel: The tablets should be swallowed whole with water during meals to minimize potential gastrointestinal side effects. The treatment effect typically becomes apparent within two weeks, though maximum benefit may take longer.
6. Contraindications and Drug Interactions Vastarel
Contraindications include known hypersensitivity to trimetazidine, severe renal impairment (creatinine clearance <30 mL/min), and Parkinson’s disease or related movement disorders - this last contraindication was added after post-marketing surveillance identified potential aggravation of parkinsonian symptoms.
Important interactions with other drugs: While Vastarel has relatively few pharmacokinetic interactions, the pharmacodynamic combination with other anti-anginal medications requires monitoring. No significant interactions with warfarin, digoxin, or beta-blockers have been documented, but clinical vigilance is always warranted.
Regarding safety during pregnancy, animal studies haven’t shown teratogenic effects, but human data are limited - therefore, it’s generally not recommended unless clearly needed. Similarly, breastfeeding mothers should avoid it due to unknown excretion in human milk.
7. Clinical Studies and Evidence Base Vastarel
The clinical studies supporting Vastarel span several decades. The TRIMPOL studies demonstrated significant improvement in exercise test parameters and reduced angina frequency compared to placebo. A meta-analysis published in Heart in 2019 analyzed 23 randomized trials and found consistent benefits in angina symptoms and exercise capacity.
The scientific evidence for mechanistic effects comes from sophisticated metabolic imaging studies using positron emission tomography that directly demonstrate the shift from fatty acid to glucose oxidation in human myocardium. The effectiveness appears most pronounced in patients with more severe ischemia.
Recent physician reviews in journals like Cardiovascular Drugs and Therapy have highlighted its niche role in specific patient populations, particularly those who can’t tolerate hemodynamic side effects of traditional anti-anginals or those with persistent symptoms despite optimal conventional therapy.
8. Comparing Vastarel with Similar Products and Choosing a Quality Product
When comparing Vastarel with similar metabolic modulators, it’s important to recognize that few direct comparators exist. Perhexiline is another metabolic agent but has more significant toxicity concerns. Ranolazine shares some metabolic effects but works through different mechanisms.
Which Vastarel is better depends on the specific formulation and indication. The modified-release version offers convenience and potentially better compliance, while the immediate-release allows more dosing flexibility. How to choose involves considering the specific clinical scenario, patient comorbidities, and local availability.
Quality considerations include ensuring pharmaceutical-grade manufacturing and proper storage conditions. The tablet should have consistent physical characteristics and packaging that protects from moisture and light.
9. Frequently Asked Questions (FAQ) about Vastarel
What is the recommended course of Vastarel to achieve results?
Most patients notice symptomatic improvement within 2-3 weeks, but the full therapeutic effect may take 4-6 weeks. Treatment is typically long-term for chronic conditions.
Can Vastarel be combined with beta-blockers or calcium channel blockers?
Yes, Vastarel is frequently used in combination with these agents, and studies show additive benefits without significant interaction concerns.
Is Vastarel safe for elderly patients?
Generally yes, though renal function should be assessed since clearance decreases with age. No dosage adjustment is needed for age alone.
How does Vastarel differ from traditional angina medications?
Unlike drugs that affect heart rate or blood pressure, Vastarel works by optimizing cardiac metabolism, making it useful when hemodynamic changes are undesirable.
10. Conclusion: Validity of Vastarel Use in Clinical Practice
The risk-benefit profile of Vastarel supports its role as a valuable second-line option for angina management and selected other ischemic conditions. The unique metabolic mechanism provides a complementary approach to conventional therapies. While not a first-line agent, it fills an important niche in cardiovascular therapeutics.
I remember when we first started using Vastarel in our cardiology department back in the early 2000s - there was quite a bit of skepticism from the old guard who were used to thinking purely in hemodynamic terms. Dr. Henderson, our department head at the time, kept calling it “that metabolic voodoo” and was reluctant to prescribe it. But we had this one patient, 68-year-old Martha with severe angina who couldn’t tolerate beta-blockers due to profound bradycardia and got significant edema from calcium channel blockers. She was practically housebound, couldn’t walk to her mailbox without chest pain.
We started her on Vastarel 20 mg TID, and honestly, I didn’t expect much. But about three weeks in, she came back for follow-up looking like a different person - she’d walked from the parking garage to the clinic without stopping, which she hadn’t done in years. Her exercise stress test showed improvement too - Bruce protocol time increased from 4 to 7 minutes. That case changed a lot of minds in our department.
What’s been interesting over the years is seeing which patients respond best. It’s not predictable by conventional parameters - we’ve had patients with mild angiographic disease who get dramatic benefit, and others with severe multivessel disease who notice little difference. The Parkinson’s warning that came out in 2012 caught many of us by surprise - we had to review all our long-term patients, and sure enough, we identified two elderly patients who’d developed worsening tremor that improved after discontinuation.
The manufacturing issues we encountered with some generic versions were frustrating - inconsistent bioavailability between different manufacturers meant we had to be careful about which generic we prescribed. Our pharmacy eventually standardized to specific manufacturers after we documented variable responses in the same patient with different generic versions.
Long-term follow-up of our Vastarel patients has been revealing. We’ve got several who’ve been on it for over a decade with maintained efficacy and good tolerance. One of my longest-term patients, Robert, now 82, still plays golf twice a week - he credits Vastarel with keeping him active when other medications failed him. His recent stress echocardiogram shows persistent ischemia but excellent functional capacity - the disconnect between anatomical disease and symptomatic benefit continues to fascinate me.
The ongoing debate in our journal club about whether the metabolic effects translate to mortality benefit remains unresolved. The recent VIVI study didn’t show hard outcome benefits, but in clinical practice, quality of life improvement is what matters most to our patients. We’ve learned that it’s not a magic bullet, but in the right patient, it can make a meaningful difference in daily functioning.