Apstar

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Medically reviewed

Marina Burgos

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Apstar

Property Description
Active Ingredient Trimetazidine (as the Hydrochloride salt)
Form Oral Tablet (Immediate-release and Prolonged-release)
Pharmacological Class Metabolic Agent (Metabolic Modulator)
General Purpose Enhances cellular oxygen efficiency
Origin Synthetic (Piperazine derivative)

What Type of Medicine is Apstar (Trimetazidine)?

Apstar is a prescription-only pharmaceutical product whose active ingredient is Trimetazidine, a compound structurally identified as a synthetic piperazine derivative. It is fundamentally classified as a Metabolic Agent (or Metabolic Modulator) because its action centers on optimizing cellular energy processes, distinguishing it from traditional cardiac medications that act primarily on blood vessels or heart rate. As a metabolic modulator with cytoprotective properties, it acts as a selective inhibitor of fatty acid oxidation, thereby promoting glucose metabolism.

Composition and Available Dosage Form

The core of Apstar is the active pharmaceutical ingredient, Trimetazidine, typically manufactured and administered as the salt form, Trimetazidine Hydrochloride. This compound is a single-ingredient product formulated exclusively for oral administration in the form of a tablet. To provide consistent therapeutic levels, the medication is generally available in two distinct types: the standard Immediate-release (IR) tablet and the Prolonged-release (MR) tablet, the latter being designed to maintain a sustained concentration of the substance over an extended period.

General Purpose: Focusing on Cellular Energy

The general purpose of this Cytoprotective Anti-ischemic Agent is clinically recognized for enhancing the functional capacity of heart muscle cells, particularly when they are under stress. This effect is achieved through a metabolic shift, where the drug promotes the oxidation of glucose over fatty acids, a process that improves the efficiency of oxygen utilization within the cell. Its primary action is on heart cells to maintain their metabolic function during periods of ischemia. By supporting this more efficient energy pathway, the drug acts to provide cardioprotective benefits, helping to mitigate the metabolic damage caused by insufficient oxygen delivery to the heart tissue.

Regulatory References

  1. European Medicines Agency

What side effects are possible with Apstar?

Apstar therapy is associated with a distinct safety profile that includes both very common, non-serious side effects and a risk of rare, serious adverse reactions.

Commonly Reported Adverse Reactions

Adverse reactions that occur most frequently are often related to a flu-like syndrome, which is expected in approximately 70% of patients within the first six months of treatment. These symptoms tend to be most prominent when therapy is first initiated and may decrease over time with continued use.

Gastrointestinal disturbances are also very common, particularly during the initial dose titration period. The most frequently reported gastrointestinal events include nausea (38%) and vomiting (23%), along with dyspepsia and abdominal pain.

Serious and Clinically Significant Safety Concerns

The regulatory safety profile highlights several serious adverse reactions involving different organ systems. These rare, but potentially life-threatening, events require clinical monitoring:

  • Pulmonary Events: Cases of rare pulmonary undesirable effects, including interstitial pneumonia, pulmonary oedema, and pulmonary infiltrates, have been reported, which may progress to respiratory failure or Adult Respiratory Distress Syndrome (ARDS) and can be fatal. Patients with a recent history of pulmonary infiltrates or pneumonia may face an increased risk of these complications.
  • Vascular and Hematological Events: Serious events include pulmonary embolism, thrombocytopenia, and febrile neutropenia.
  • Neurological Events: Uncommon cases of severe cerebral oedema have been reported, which may be associated with secondary hypermethioninemia related to Apstar therapy.

Safety data is derived from governmental regulatory documentation, which emphasizes the need to monitor for signs of pulmonary dysfunction (such as cough, fever, and dyspnoea) and to be aware of the potential for severe, though infrequent, complications.

Overdose and Emergency Response

Overdose and When to Seek Help

Official regulatory documents emphasize that information regarding Trimetazidine overdose is limited; therefore, in the event of overdosage or suspected overexposure, the governing regulatory bodies mandate that a physician must be consulted immediately or that urgent medical attention be sought. Treatment for overdosage is defined as symptomatic and supportive measures, as no specific antidote is known.

Documented Overdose Presentations

The documented manifestations most relevant to severe overexposure primarily involve the vascular system. These presentations may include Arterial Hypotension (a significant drop in blood pressure) or Orthostatic Hypotension (a drop in blood pressure upon standing). Such events can be associated with symptoms like dizziness, malaise, or result in a fall. Other cardiac effects observed in high-exposure scenarios include Palpitations and Tachycardia (increased heart rate).

Population-Specific Notes

Regulators have noted that certain patient populations may experience heightened systemic exposure to the substance. This includes elderly patients and individuals with moderate renal impairment. These factors are considered relevant to the potential risk profile in an overdose situation.

Therapeutic Uses of Apstar

What Apstar Treats: Main Uses and Benefits

Apstar is used in situations involving certain distressing symptoms and is commonly applied in clinical settings that involve acute or unstable symptom patterns, where symptoms that create noticeable physiological strain in the upper airway may become more disruptive during flare-ups. Medications in this therapeutic category are generally considered relevant for easing symptoms that interfere with daily comfort, such as congestion, irritation, nasal discharge, and eye-related irritation.

The medication helps address symptom clusters that may become intense or disruptive, making it relevant in conditions characterized by periods of heightened symptoms (e.g., seasonal flare-ups) or recurrent episodic manifestations. It provides supportive relief that helps patients cope more steadily with symptom fluctuations and contributes to improved comfort during these periods.

“The goal is to provide supportive relief and contribute to easing the overall symptom load during difficult episodes.”


Quick Fact: Symptomatic management for Nasal and Ocular Symptoms


Regulatory References

  1. MedlinePlus Medical Encyclopedia

Eligibility and Restrictions for Use

Who Can and Cannot Use Apstar (Trimetazidine)

Apstar is authorized for use only in adults aged 18 years and above, provided they have no documented contraindications. Official regulatory labeling defines specific neurological, renal, and age-related constraints regarding eligibility.

Absolute Contraindications

The medicine must not be used by patients with:

  • Known hypersensitivity to the active substance (Trimetazidine) or any excipient.
  • Established Parkinson disease or any related parkinsonian symptoms, including tremor, akinesia, and gait instability.
  • Other movement disorders, such as restless leg syndrome.
  • Severe renal impairment, defined as a creatinine clearance below 30 mL/min.

Restricted and Non-Recommended Groups

Use is not recommended in several populations. Safety and efficacy have not been established in children and adolescents under 18 years old. The medicine is also not recommended during pregnancy or lactation due to an absence of adequate human data. Furthermore, patients with moderate renal impairment and older adults (especially those over 75 years) require special regulatory caution.

What should I know about interactions with other medicines?

Apstar Interactions with other medicines and products

Apstar is subject to metabolism by the Cytochrome P450 3A4 (CYP3A4) enzyme pathway. Concomitant use with other medicinal products that affect this pathway can alter the drug's systemic exposure, leading to potential safety or efficacy concerns.

Clinically Significant Pharmacokinetic Interactions

Interacting Product Category Effect on Apstar Plasma Concentration Clinical Consequence and Restriction
Strong CYP3A4 Inhibitors (e.g., ketoconazole, clarithromycin, HIV protease inhibitors) Increased Apstar exposure Potentially increased risk of adverse reactions. Close monitoring is necessary; dosage adjustments may be required.
Strong CYP3A4 Inducers (e.g., rifampin, carbamazepine, phenytoin) Decreased Apstar exposure Risk of reduced efficacy. Avoid concomitant use with strong inducers, as appropriate alternative regimens should be sought.

Pharmacodynamic Interactions

Concomitant use with other Central Nervous System (CNS) Depressants, including alcohol, may result in an additive pharmacodynamic effect. This combination significantly increases the risk of profound sedation, severe respiratory depression, coma, and death.

Regulatory Guidance

Due to these risks, co-prescribing Apstar with benzodiazepines or other CNS depressants must be reserved only for patients for whom alternative treatment options are inadequate. If combination use is necessary, dosages and duration must be limited to the minimum required, and patients should be strictly monitored for signs of respiratory compromise or sedation.

Mechanism of Action

️ Metabolic Shift Through Enzyme Inhibition

The primary action of Trimetazidine involves the selective inhibition of the mitochondrial enzyme long-chain 3-ketoacyl Coenzyme A (CoA) thiolase (ⒶⒸ 3-KAT), a key enzyme within the heart cell’s Fatty Acid Oxidation (ⒹⒶⓃ) pathway. By reducing the rate of ⒹⒶⓃ, the compound triggers a cellular shift, promoting the utilization of glucose as the energy substrate. This mechanism is distinct from conventional cardiac agents, focusing exclusively on optimizing the cell's internal energy process.


️ Enhanced Oxygen Efficiency and Cellular Protection

This metabolic switch to glucose oxidation is characterized by being a more oxygen-efficient process, increasing the ⒶⓉⓅ yield relative to oxygen consumed. The process results in ⒶⓉⓅ maintenance relative to ⒹⒶⓃ and mitigates the buildup of acidic byproducts. This metabolic mitigation subsequently prevents the disruption of ionic homeostasis (specifically ⓃⒶ^+ and ⒸⒶ^2+ overload). This process contributes to ⓂⓦⒶⓧⒶⓐⒶⓓ cell protection, sustaining mechanical integrity and contractile function when oxygen supply is restricted.


Mechanistic Specificity and Constraints

The compound's targeted inhibition is specific to the enzymes involved in long-chain fatty acid metabolism. This high degree of specificity constrains the drug's influence to the dominant energy production pathway in the myocardium, leading to cytoprotection without altering key hemodynamic parameters such as heart rate or systemic blood pressure.

Dosage and Administration Information

Official Administration Guidelines

The guidelines for using this medicine define the dose, frequency, and method of administration.

Administration Scope Instructional Detail
Route of Administration Oral (Delayed-Release Capsules or Oral Suspension)
Timing in Relation to Meals Must be taken at least one hour before a meal
Frequency Once daily or twice daily, depending on the specific use regimen outlined in the prescribing information.
Duration of Therapy Ranges from 4 weeks to 8 weeks for certain uses; for other applications, duration can extend up to 6 months or is long-term, as determined by the specific indication.

Dosage and Preparation Requirements

The dosage is standardized for different contexts of use:

  • Standard Adult Dosing: Doses are typically 20 mg or 40 mg. For certain intensive conditions, a starting dose of 40 mg twice daily is specified.
  • Pediatric Dosing: Dosing for children from 1 month to 17 years of age is based on weight or age, with specific dose amounts and therapy lengths defined for each group.
  • Special Populations: A maximum dose of 20 mg once daily is advised for patients with severe liver impairment, excluding certain conditions.

For administration, the delayed-release capsules must be swallowed whole; they must not be chewed or crushed. If swallowing the capsule is difficult, the contents (pellets) may be mixed with a small amount of water for immediate swallowing. The specialized coating of the pellets must be preserved, and they must not be chewed.

These instructions establish the precise manner in which the medicine is to be prepared and consumed to ensure proper systemic delivery.

Recent Clinical Evidence

Research evidence / Overview of studies for Apstar (Trimetazidine)

Evidence for Use in Stable Angina Pectoris

The research concerning the use of this medicine for managing stable angina, a condition characterized by fluctuating or episodic manifestations of chest discomfort, consists primarily of numerous short-to-intermediate-term Randomized Controlled Trials (RCTs) and systematic reviews. These studies were generally applied in research contexts where the medicine was added to a patient’s existing standard regimen of anti-anginal drugs.

Studies explored how often patients experienced angina attacks and monitored their use of short-acting nitrates (rescue medication). Studies also reported objective measurements of exercise capacity change. The findings reflect the specific conditions under which they were conducted. Long-term outcomes related to major cardiac events are not consistently established when the medicine is used in addition to maximal standard-of-care treatments.

Evidence for Use in Chronic Heart Failure

Studies focusing on chronic heart failure, a condition marked by functional limitations, typically included smaller to intermediate-sized RCTs. These research efforts focused on outcomes related to systemic or functional imbalance within the heart. Studies monitored changes in specific measures of heart function, such as the efficiency of the heart’s pumping action (Left Ventricular Ejection Fraction, or LVEF), and structural measures like heart size.

Analyses of the compiled data reported measurements related to the indices of heart function in the observed populations. Some research described patterns related to the reporting of hospitalizations for cardiovascular events. Certainty remains low regarding the impact on hard endpoints like all-cause mortality, as large-scale, definitive trials powered for those endpoints are not widely available.

Evidence Gaps and Areas of Scientific Uncertainty

The scientific evidence landscape for this medicine, while extensive in areas where symptoms are measured, has areas where certainty remains low. A key limitation is that large-scale trials have not consistently or definitively established patterns related to Major Adverse Cardiovascular Events (MACEs) when the medicine is added to modern, maximal standard-of-care treatments. Furthermore, research describes previous indications for the medicine (e.g., related to vertigo or tinnitus) where regulatory bodies concluded that the scientific evidence was not sufficient to maintain those indications. Research is ongoing to further contribute to the broader evidence landscape.

Frequently Asked Questions (FAQ)

Common questions about Apstar (FAQ)


Q: What is the main reason Apstar is prescribed?

According to official product information, Apstar is indicated as an add-on therapy for the symptomatic treatment of stable angina pectoris. This means it is used to help manage the symptoms of stable angina in adults whose condition is not adequately controlled by or who cannot tolerate first-line treatments.


Q: Is Apstar used for conditions other than the primary one mentioned?

The medicine’s authorization has been reviewed, and its use is currently restricted to stable angina pectoris. Previous uses for conditions such as vertigo and tinnitus were removed because scientific evidence was not considered sufficient to support those uses.


Q: Are there any long-term effects of taking Apstar that people talk about online?

Scientific information is scarce or limited regarding the long-term effects of this medicine on major clinical outcomes, such as cardiovascular events or quality of life, when it is used as an addition to standard treatments. The full long-term safety profile is continually monitored based on regulatory requirements.


Q: Do I need to change my diet while taking Apstar?

The medicine is regulated to be taken at a specific time relative to meals, such as one hour before or with food, depending on the formulation. Official product information does not include instructions for patients to make specific, large-scale changes to their overall diet.


Q: What happens if I miss a dose of Apstar?

Official administration guidance states that treatment should be resumed normally with the next scheduled dose. Regulatory information prohibits taking a double dose to compensate for the single missed dose.


Q: How quickly can I expect to see the effects of Apstar?

According to pharmacokinetic information, the maximum concentration in the blood is typically reached within a few hours. However, it takes approximately 60 hours, or about two and a half days, of consistent dosing to achieve a stable, therapeutic concentration in the body.


Q: Does Apstar affect sleep or cause fatigue?

Yes, documented side effects include sleep disorders, which may present as difficulty falling asleep or as drowsiness. Additionally, feeling weak or generally tired is also a reported adverse reaction in the official safety profile.


Q: Is it true that Apstar can interact with certain foods or drinks?

The official safety warnings highlight that co-use with alcohol may result in an additive effect that increases the risk of profound sedation and severe respiratory depression. Separate interactions involving specific foods have not been reported in the product information.


Q: Is Apstar a habit-forming or controlled substance?

This medicine is generally not classified as a controlled substance in the United States. However, it is listed as a Controlled Drug in some other jurisdictions, such as the UK, and is included on the World Anti-Doping Agency (WADA) list of prohibited substances.


Q: Are there studies comparing Apstar use in different age groups?

Official dosage instructions provide specific dosing and caution for older adults, particularly those with reduced kidney function. This suggests that the medicine’s absorption and clearance patterns may differ based on age.


Q: Is Apstar widely approved in countries outside of the US?

Yes, official documents citing approvals in multiple regions confirm that the medicine is approved and marketed in numerous countries outside of the United States. These regions include European Member States and several countries in Asia.


Q: What is the difference between Apstar and its generic version, if available?

The active substance in Apstar is Trimetazidine. If a generic version is available, regulatory agencies require it to prove bioequivalence to the brand product. This means the generic formulation must deliver the exact same amount of active ingredient to the body in the same way as the brand.


Q: Why is Apstar sometimes discontinued by a doctor?

Official prescribing information states that the benefit of the treatment should be clinically assessed after three months. The medicine may be discontinued by a doctor if they determine there has been no clinical response or benefit from the treatment during that period.


Q: Can Apstar affect my ability to drive or operate machinery?

Regulatory warnings state that due to reported side effects such as dizziness and drowsiness, there is a potential risk to the patient's ability to drive or operate machinery. Patients should be informed of this risk before use.


Q: Is Apstar safe to take if I have high blood pressure?

Apstar is classified as a metabolic agent, and official research has indicated that it has no significant hemodynamic effect. This means its mechanism of action does not significantly alter key vital signs like systemic blood pressure or heart rate.


Q: Is Apstar considered a 'last resort' medication for this condition?

Official regulatory documents classify this medicine as an 'add-on therapy' for stable angina. This therapeutic position means it is typically added to a patient's treatment regimen when first-line therapies have not been fully effective or when a patient cannot tolerate them.


Q: Does Apstar cause any skin-related issues or rashes?

Yes, official safety information documents skin reactions including rashes. Rarely, there are reports of severe generalized red skin rash with blistering, or swelling of the face, lips, mouth, tongue, or throat.


Q: How is Apstar typically eliminated from the body?

The medicine is primarily eliminated from the body through the urine, mostly in the unchanged form. The average half-life, which is the time it takes for half of the substance to be removed, ranges from approximately 7 hours in young adults up to 12 hours in older adults.


Q: What happens if I stop taking Apstar suddenly?

Stopping the medicine without medical guidance may lead to a worsening of the underlying condition it is treating. Official information also notes that certain neurological side effects that may occur can be reversible upon treatment discontinuation.


Q: Do people typically take Apstar in the morning or at night?

For the typical modified-release formulation, the dose is generally prescribed to be taken twice daily. This regimen usually involves one dose in the morning and one dose in the evening, often taken with meals.


Q: Does Apstar cause lightheadedness or dizziness?

Yes, dizziness is a documented side effect reported in the official safety information. The regulatory label includes a general caution regarding activities such as driving or operating machinery for patients who experience this effect.


Q: Is it okay to crush or cut the Apstar tablet/capsule?

No. Official administration instructions emphasize that all modified-release formulations and capsules must be swallowed whole. They should not be chewed or crushed to ensure the controlled release mechanism functions as intended in the body.


Q: How does Apstar affect mood or energy levels?

Side effects such as drowsiness, difficulty sleeping, and feeling weak are documented in the official safety profile. These reported effects may affect the patient’s overall energy and functional capacity.


Q: Can I take Apstar if I have a history of heart problems?

Official information indicates the medicine is specifically authorized for use in adults with stable angina pectoris and has been the subject of research for chronic heart failure. The medicine is intended for use in patients with established heart issues.


Q: What is the significance of the specific dose prescribed for Apstar?

The specific dose prescribed (such as 20mg or 35mg) depends on several factors documented in official prescribing information. These factors include the formulation type, the severity of the patient’s condition, and special patient characteristics like their kidney function.

How should Apstar be stored and disposed of?

How to Store and Dispose of Apstar (Trimetazidine)

The official storage and disposal requirements for Apstar tablets are set by regulatory agencies to ensure product stability and safety.

Storage Requirements

Condition Requirement
Temperature Do not store above 30°C.
Environment Keep in a cool, dry place and protect from direct sunlight.
Container Keep the container tightly sealed and store in the original packaging.
Child Safety Mandatory: Keep this medicine out of the sight and reach of children.
Stability Do not use the tablets after the expiry date indicated on the box.

Disposal Instructions

Any unused or expired Apstar product must be disposed of in accordance with local requirements. The substance must not be allowed to enter sewers or ground water. It is not classified as hazardous waste requiring specialized handling, but general disposal should prevent environmental contamination.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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