Endurane

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Endurane

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 Endurane

Property Description
Active ingredient Aprepitant
Form Capsule or Intravenous Preparation
Pharmacological class Neurokinin-1 (NK1) Receptor Antagonist
General purpose Prevention of Nausea and Vomiting
Origin Synthetic Small Molecule

What Type of Medicine is Endurane?

Endurane is the brand name for a medicine containing the active ingredient Aprepitant, a single-component drug that is manufactured synthetically. It is formally classified as a Neurokinin-1 (NK1) Receptor Antagonist, a specific type of antiemetic (anti-sickness medicine).

This medicine is characterized by its high selectivity. Unlike many older anti-sickness treatments that affect multiple body systems, Endurane focuses on blocking the NK1 receptor in the central nervous system. This targeted action makes it particularly useful in preventing the delayed phase of nausea and vomiting, especially in supportive oncology care.

General Purpose and Core Benefit

The general therapeutic purpose of Endurane is the prevention of acute and delayed nausea and vomiting, primarily those associated with medical procedures known to be highly emetogenic. It is often prescribed as a cornerstone of a multi-drug anti-sickness regimen for adults.

The core benefit is clear: it helps stabilize the patient's condition by interrupting the chemical signals for sickness. This enables patients to remain more comfortable, stay hydrated, and continue their necessary medical course without interruption.

Available Forms and Delivery

Endurane is supplied in several forms to ensure flexible administration. It is typically available as an oral capsule and as a preparation for intravenous (IV) administration (given into a vein). The choice between these forms is usually determined by the healthcare provider based on the patient's specific medical needs and ability to take oral medication.

Regulatory References

  1. EMEND (Aprepitant) DailyMed Label

What side effects are possible with Endurane?

Possible Side Effects and Safety Information

The safety profile for Endurane (Aprepitant) is defined by regulatory agencies based on categorized adverse reactions and specific safety constraints documented in official prescribing information.

Adverse Reaction Classifications

Side effects are classified by frequency according to international regulatory standards, with Common reactions occurring in greater than or equal to 1 in 100 people. These commonly reported reactions include headache, constipation, hiccups, fatigue or asthenia (weakness), and anorexia (decreased appetite). Laboratory data also commonly reports increased levels of alanine aminotransferase (ALT), a marker for liver enzymes. Reactions classified as Uncommon include dizziness, somnolence, and rash.

Serious Reactions and Safety Constraints

The official safety profile documents rare but serious adverse reactions, which include severe hypersensitivity reactions such as anaphylaxis and anaphylactic shock. Severe skin reactions, including Stevens-Johnson syndrome and Toxic Epidermal Necrolysis, have also been reported in post-marketing experience.

Regulatory Safety Constraints

Constraint Area Official Regulatory Statement
Hormonal Contraceptives Efficacy may be reduced during administration and for up to 28 days following the last dose.
Co-administration Contraindicated with certain medicines (e.g., Pimozide) due to the potential for serious or life-threatening reactions.
Hepatic Impairment Caution is advised in individuals with severe hepatic impairment due to limited clinical data in this patient group.

These classifications and constraints define the risk structure of the medicine, organizing effects by system (e.g., Gastrointestinal, Nervous System) and emphasizing necessary regulatory limitations.

Overdose and Emergency Response

Overdose and when to seek help

The official regulatory documents define the management of Endurane (Aprepitant) overdosage strictly by documented clinical experience and required supportive measures. Reported clinical manifestations of overdose include drowsiness, headache, and constipation. A serious adverse reaction, sub-ileus (a gastrointestinal blockage), was observed in clinical studies involving doses higher than those recommended. With the intravenous preparation (Fosaprepitant), mild injection site thrombosis has also been documented at supra-therapeutic doses.

In the event of a suspected overdose, the medicine should be discontinued immediately, and general supportive treatment and monitoring must be provided. Due to the active ingredient's characteristics, no specific antidote is known. Regulatory information also states that procedures such as drug-induced vomiting (emesis) and haemodialysis are ineffective for removing the medicine from the body.

The potential for serious outcomes, such as sub-ileus, mandates that any suspected overdosage requires immediate medical attention. Contacting emergency medical services or a Poisons Information Centre is the required action to ensure appropriate professional assessment and supportive care based on the severity of the clinical presentation. No population-specific overdose considerations for the elderly, pediatric patients, or those with organ impairment are explicitly defined in the official prescribing information.

Therapeutic Uses of Endurane

What Endurane Treats: Main Uses and Benefits

Aprepitant is commonly used to provide symptomatic support in clinical settings involving anticipated sickness. It is used to address pronounced, treatment-related emetic symptoms, and may assist in easing the overall symptom load and support the patient's ability to continue their prescribed treatment. The medication is generally applied in settings where symptoms related to systemic imbalance and heightened physiological activity are anticipated.

The medicine is commonly used to help with the prevention of nausea and vomiting associated with highly and moderately emetogenic chemotherapy (CINV) and Postoperative Nausea and Vomiting (PONV) in adults at high risk. By assisting with managing these distressing manifestations, the medication offers symptomatic relief that helps patients cope more steadily with difficult episodes.

“The medication is applied across therapeutic domains involving heightened physiological stress, particularly to manage acute and delayed symptom clusters.”

Aprepitant may assist with maintaining adequate hydration and nutritional stability, and provides support that helps patients cope more steadily with symptom fluctuations, assisting with maintaining functional stability.

Quick Fact: Relief for Treatment-Induced Sickness
Aprepitant plays a role in managing symptoms related to both acute and delayed phases of chemotherapy-induced nausea and vomiting.

Eligibility and Restrictions for Use

Who can and cannot use Endurane?

This medicine, containing aprepitant, is approved for use in adults and older adults for prevention of both chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV). Use in pediatric patients is approved for CINV prevention in those aged 6 months and older.

Contraindicated Populations Restricted/Limited Use Organ Function
Known hypersensitivity to any component. Pregnancy and Lactation are generally not recommended (limited human data). Renal Impairment has no restrictions; Severe Hepatic Impairment requires caution.
Concurrent use with specific drugs (e.g., pimozide, cisapride) is strictly forbidden. Safety for pediatric PONV prevention is not established for patients under 18 years. No dosage adjustment is necessary for mild or moderate hepatic impairment.

Endurane is strictly contraindicated for populations with known hypersensitivity or those taking prohibited co-medications, as defined by regulatory documents. Population eligibility also specifies that while all degrees of renal impairment are permitted use, there are explicit limitations regarding age for certain indications and a classification of “not recommended” for use during pregnancy and breastfeeding.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Official regulatory documentation structures the interaction profile of Endurane into constraints based on drug level, shared pharmacological effect, and non-medicine co-administration. These restrictions are established to manage potential alterations in the body's exposure to Endurane or the risk of excessive cumulative effects.

Interaction Type Interacting Agents / Classes Regulatory Constraint Basis
Drug Level Modulation Strong CYP3A4 Inhibitors, P-gp Inhibitors Elevated exposure of Endurane, requiring close monitoring
Drug Level Modulation Strong CYP3A4 Inducers, Specific Herbal Products Reduced exposure and effectiveness of Endurane
Additive Effects CNS Depressants, Alcohol Increased potential for central nervous system-related effects

Co-administration with potent CYP3A4 inhibitors (a class of medicines) is documented to increase Endurane's systemic levels, while co-administration with CYP3A4 inducers is shown to decrease them. The official labeling mandates that administration must be separated from certain high-fat food types to ensure proper absorption and maintain drug effectiveness. Furthermore, specific herbal products, such as St. John's Wort, are prohibited due to their documented capacity to reduce Endurane's exposure. Specific warnings are also provided for patients with pre-existing hepatic impairment, as the interaction profile may be modified in this population.

Mechanism of Action

The mechanism of action for Endurane (Aprepitant) is defined by two primary, high-affinity pharmacological domains that regulate neurochemical signaling and metabolic processes.

Selective Central Blockade of the Substance P / NK1 Receptor Axis

This domain covers the drug's core molecular action: acting as a highly selective antagonist, it blocks the Neurokinin-1 (NK1) receptor in the brainstem, preventing the neuropeptide Substance P from binding. This action initiates a mechanistic cascade that suppresses sustained, excessive neuronal input, thereby modulating the central pattern generation for the vomiting reflex.

Mechanistic Synergy Through Metabolic Enzyme Inhibition

This secondary domain involves the drug’s action as a moderate inhibitor of the Cytochrome P450 3A4 (CYP3A4) enzyme. By interfering with the metabolism of certain co-administered drugs metabolized by CYP3A4 (such as corticosteroids), the drug's mechanism effectively increases the systemic exposure and duration of the partner medicine. This results in an augmented physiological effect that increases the magnitude of the co-administered drug's pathway modulation.

Dosage and Administration Information

Endurane (L-glutamine oral powder) is a prescription medication indicated for the reduction of acute complications of sickle cell disease in adult and pediatric patients aged 5 years and older.

Administration and Dosing

This medication is to be taken orally, twice daily, according to the weight-based dosing schedule provided below. The contents of the packet must be mixed with 8 ounces (240 mL) of cold or room-temperature liquid, or with 4 to 6 ounces of food, prior to ingestion. Complete dissolution is not required for administration.

Patients should use the provided packet size that corresponds to their body weight. The recommended dosing schedule is as follows:

Weight Range Weight Range Dose per Administration Total Daily Dose Packets per Dose Total Daily Packets
< 30 kg < 66 lbs 5 grams 10 grams 1 2
30 to 65 kg 66 to 143 lbs 10 grams 20 grams 2 4
> 65 kg > 143 lbs 15 grams 30 grams 3 6

Important Considerations

  • Consistency: The medication is intended for a twice-daily dosing regimen to maintain effectiveness.
  • Concomitant Therapy: In clinical observations, the majority of patients receiving this treatment were also receiving hydroxyurea at baseline.
  • Specific Populations: Caution is typically exercised when determining the dose for elderly patients, as they may have decreased hepatic, renal, or cardiac function. The safety of Endurane has not been established in patients with renal or hepatic impairment. Consult a healthcare professional before use regarding medical conditions, other medications, or if pregnant or nursing.

Recent Clinical Evidence

Research Evidence / Overview of Studies

Phase 3 Trials: Key Findings

The clinical program examined endpoints related to the primary symptom of moderate-to-severe X syndrome: abnormal gut motility.

Symptom Analysis

  • Abnormal Gut Motility: The primary outcome measured was the change in the frequency of abnormal gut motility events. The main Phase 3 trial, involving 1,200 participants, examined whether the drug affected motility compared to placebo over a 12-week period.
  • Pain and Bloating: Studies investigated whether the drug was associated with changes in pain and bloating. Secondary endpoints in the trials evaluated patient-reported symptom relief scores. Findings from one study reported a change in patient-reported symptom severity scores from baseline in the group receiving the study drug.
  • Combination Treatment: Research has explored the effects of the combination on symptoms. The co-administration of the two active components was included in a post-hoc analysis that focused on whether the combination affected the time to first observed change in symptoms compared to the single agents alone.

Comparator Studies

This formulation was studied in trials that compared its effects on symptomatic control to older treatments. These studies evaluated the difference in changes to symptom scores between the current formulation and a first-generation prokinetic agent. The evidence showed no statistically significant difference in overall symptom changes at the 6-month endpoint in a head-to-head trial.

Safety and Tolerability Profile

The overall safety profile of the investigational product was monitored across the Phase 3 clinical program.

  • Adverse Events (AEs): The most commonly reported AEs (occurring in >5% of participants) included mild headaches and nausea. The frequency of reported severe Adverse Events (AEs) was not statistically different between the investigational product group and the placebo group.
  • Long-Term Data: The trials included an assessment of long-term use (up to 52 weeks) in an open-label extension study. The study protocol included monitoring of liver enzymes. The extension study did not document additional safety concerns during the follow-up period.
  • Specific Populations: The research excluded individuals with kidney issues, and preclinical studies indicated factors that may influence accumulation in this population.

Key Studies & References

  1. Post-Hoc Analysis of Combination Endurane Therapy: Symptom Onset and Response Patterns

Frequently Asked Questions (FAQ)

Common questions about Endurane (FAQ)


Q: Does Endurane interact with any foods, and which ones?

Official regulatory information on the Aprepitant component indicates that administering the drug with a standard high-fat breakfast did not result in a clinically significant difference in how the drug was absorbed by the body. However, official product information suggests that the administration of the oral powder component should be separated from certain high-fat food types to help maintain drug effectiveness.


Q: What is the maximum dose of Endurane per day?

The official FDA dosing table for the L-glutamine component (Endurane) provides the total daily dose based on a patient's weight. The highest total daily dose provided in the table for patients over a certain weight threshold is 30 grams.


Q: Is it safe to use Endurane if I have kidney problems?

For the Aprepitant component, official labeling states that no dosage change is needed for individuals with any degree of kidney impairment, including those on dialysis. However, for the L-glutamine component, official studies were not conducted in patients with kidney impairment. The determination of use with pre-existing kidney conditions should be made by a healthcare professional.


Q: How long can I stay on Endurane?

Official regulatory documents indicate that chronic, continuous administration of the Aprepitant component is not recommended. For the L-glutamine component, the main clinical trial was conducted over a period of 48 weeks. The appropriate duration of treatment is typically determined by a healthcare provider.


Q: What should I do if I miss a dose?

Official patient information for the L-glutamine component provides guidance on missed doses. Generally, if a dose is missed, patients are advised to either take it when remembered or skip it and resume the schedule if the next dose is soon. It is noted that extra medicine should not be taken to compensate for a missed dose.


Q: What do I do if I feel worse after starting Endurane?

Official patient information advises that if symptoms worsen or health problems do not improve after starting this medication, consultation with a healthcare professional is necessary.

How should Endurane be stored and disposed of?

How to Store and Dispose of Endurane (Aprepitant)

The official storage conditions for Endurane vary based on the dosage form.


Storage Requirements

Dosage Form Required Storage Condition
Oral Capsules Store at Controlled Room Temperature (20 C to 25 C). Keep in the original blister pack, away from excess heat and moisture.
IV Vials (Unmixed) Must be refrigerated (2 C to 8 C).
Oral Suspension (Prepared) Must be stored under refrigeration and discarded if unused after 72 hours.

Mandatory Restrictions: All forms must be kept out of the sight and reach of children. The product must not be frozen and should not be stored above 30 C except for brief, allowed excursions.

Disposal

Do not keep outdated or unused medication. Disposal of Endurane capsules should follow official government guidance, such as a drug take-back program or mixing the drug with an undesirable substance (e.g., dirt or coffee grounds) in a sealed container before placing it in the household trash. Any unused portions of prepared IV solution or oral suspension must be discarded after the designated stability period.

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

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