Aprepitant

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Aprepitant

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Medically reviewed

Laura Arias

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 Aprepitant

Quick Facts

Property Description
Active ingredient Aprepitant (C23H21F7N4O3)
Form Oral capsule, Oral suspension, Intravenous prodrug (Fosaprepitant)
Pharmacological class Neurokinin-1 (NK1) Receptor Antagonist
General purpose Prevention of severe nausea and vomiting
Origin Synthetic compound

What Type of Medicine is Aprepitant?

Aprepitant is a potent, synthetic compound classified as an antiemetic, a type of medicine specifically used to prevent and control the sensation of severe sickness. Taxonomically, this prescription-only medication belongs to the highly specialized pharmacological class of Neurokinin-1 (NK1) receptor antagonists. This classification means the medicine is designed to target a specific brain pathway that triggers the vomiting reflex, a mechanism that is clinically recognized for its role in antiemetic regimens. The active substance, Aprepitant, is a single-active ingredient product, which simplifies the understanding of its direct action within the central nervous system (CNS).

Aprepitant’s Function and Available Forms

The general function of Aprepitant is to deliver a robust central antiemetic effect by acting as a selective antagonist against the NK1 receptor. This action prevents the body's powerful signaling chemical, Substance P, from initiating the sickness reflex, thereby aiding in the effective prevention of pronounced sickness sensations. The drug is primarily administered via the oral route as an oral capsule or an oral suspension. For patients unable to tolerate oral intake, the compound fosaprepitant is available as an intravenous prodrug, which is quickly converted into the active Aprepitant substance in the body to ensure consistent antiemetic coverage, offering a differentiating factor in clinical administration compared to solely oral agents.

Regulatory References

  1. Aprepitant - StatPearls - NCBI Bookshelf

What side effects are possible with Aprepitant?

Possible Side Effects and Safety Information

Aprepitant's safety profile is defined by officially documented adverse reactions and crucial drug interaction warnings found in government regulatory documents.

Frequency-Classified Adverse Reactions

The most commonly documented side effects are categorized by frequency:

  • Very Common (Affecting 1 in 10 people or more): Diarrhea (in certain adult populations) and neutropenia (a reduction in a type of white blood cell, primarily noted in some pediatric uses).
  • Common (Affecting between 1 in 100 and 1 in 10 people): Fatigue, headache, hiccups, constipation, decreased appetite, and increased levels of liver enzymes (ALT).

Serious Adverse Reactions and Safety Restrictions

Although rare, serious adverse reactions have been documented, including severe hypersensitivity reactions such as anaphylaxis (a life-threatening allergic reaction) and severe skin reactions like Stevens-Johnson syndrome and Toxic Epidermal Necrolysis.

Contraindications (situations where the drug must not be used) are in place due to the risk of serious or life-threatening reactions resulting from drug interactions. These include co-administration with certain medications, such as pimozide, terfenadine, astemizole, or cisapride.

Population-Specific and Interaction Safety Notes

The drug is a modulator of the CYP3A4 enzyme system, which leads to several key safety notes:

  • Hormonal Contraceptives: Aprepitant may reduce the effectiveness of hormonal contraceptives (including oral pills, patches, or rings) during treatment and for up to 28 days after the last dose, requiring alternative non-hormonal birth control methods.
  • Other Medications: Doses of co-administered oral corticosteroids, like dexamethasone or methylprednisolone, may require reduction due to an interaction. Monitoring of the International Normalised Ratio (INR) is necessary for patients receiving chronic warfarin therapy.
  • Hepatic Impairment: Caution is advised in patients with moderate or severe liver problems due to limited safety data.

Overdose and Emergency Response

Overdose and When to Seek Help

Official regulatory information regarding Aprepitant overdose focuses on documented symptoms and necessary management steps, as detailed in government-authorized prescribing documents.

Documented Overdose Presentations

Clinical experience with acute overdose is limited. The single case of a subject who received a high single dose (1440 mg) of Aprepitant reported two specific symptoms:

  • Drowsiness
  • Headache

When to Seek Urgent Medical Help

In the event of a suspected overdose, the medicinal product should be immediately discontinued. Because the potential for serious effects cannot be ruled out, individuals experiencing symptoms after taking an excessive amount of Aprepitant must seek urgent medical attention. General supportive treatment and monitoring should be initiated promptly by healthcare professionals.

Overdose Management Considerations

Official regulatory profiles provide specific context for medical management, noting that typical procedures may be ineffective:

  • Antiemetic Effect Constraint: Due to the drug's anti-emetic properties, vomiting induced by other medicinal products is unlikely to be an effective treatment measure for decontamination.
  • Ineffectiveness of Dialysis: Aprepitant is highly protein bound (greater than 95%), which means that elimination by hemodialysis is unlikely to be an effective method for removing the drug from the body during an overdose situation.

Therapeutic Uses of Aprepitant

Aprepitant is used in situations involving certain distressing symptoms, primarily applied across domains where additional symptomatic support is needed. The medicine is commonly used to help with two major symptomatic areas.

The therapeutic scope of Aprepitant is relevant across conditions presenting with acute or disruptive episodes, where it assists in managing groups of symptoms that may become intense or disruptive caused by chemotherapy or experienced in the postoperative period. This approach helps address symptom clusters that may become intense, and is applied in addressing both immediate acute sickness and the persistent delayed sickness. The medication is applied across domains where additional symptomatic support is needed, such as supportive oncology care, and is also indicated for the prevention of postoperative sickness in high-risk adult patients. This prophylactic use is relevant when supportive symptom management is appropriate, providing support that helps ease the overall symptom burden and contributes to improved comfort during periods of heightened symptoms.


Quick Fact: Support for Intense Symptomatic Manifestations Aprepitant is commonly used to help with symptoms that create noticeable physiological strain and may become temporarily overwhelming, especially in situations where symptoms have been refractory (unresponsive) to other symptomatic management.

Eligibility and Restrictions for Use

Official Eligibility Profile

Aprepitant's eligibility is strictly defined by regulatory documents, excluding specific patient groups and requiring caution in others.

Classification Who Must NOT Use Aprepitant (Contraindications)
Absolute Contraindication Patients with known hypersensitivity to aprepitant or any component of the formulation.
Co-Medication Exclusion Patients taking pimozide, or other specific CYP3A4-metabolized medicines such as terfenadine or astemizole, due to the risk of dangerously increased drug levels.

Age and Physiological Status:

  • Pediatrics: The medicine is generally approved for use in adults and pediatric patients starting from 6 months of age. Use is not recommended in infants under 6 months due to insufficient data.
  • Pregnancy & Lactation: Use during pregnancy is generally not recommended unless clearly necessary, as clinical data are limited. For lactation, the potential benefits must be weighed against risks due to limited human data.
  • Contraception: The drug may reduce the effectiveness of hormonal contraceptives (e.g., birth control pills or patches); patients must use alternative or back-up contraception during and for a specified time (e.g., 28 days) following treatment.

Condition-Based Caution:

  • Hepatic Impairment: While no dose adjustment is required for mild-to-moderate liver impairment, caution is advised when using the medicine in patients with severe hepatic impairment (Child-Pugh score >9), as clinical data are absent for this population.
  • Renal Impairment: No dose adjustment is necessary for patients with renal impairment or those with end-stage renal disease (ESRD) undergoing hemodialysis.

What should I know about interactions with other medicines?

Aprepitant Interactions with other medicines and products

Documented Metabolic Interactions

Aprepitant is documented as a complex modulator of the Cytochrome P450 enzyme system, acting as a moderate inhibitor and a transient inducer of CYP3A4, and an inducer of CYP2C9. These roles define the official interaction profile and impact the plasma concentration of many co-administered substances.

Formal Restrictions and Contraindications

Co-administration is contraindicated with certain drugs that are highly dependent on CYP3A4 for clearance, including Pimozide, Terfenadine, Astemizole, and Cisapride. This restriction is due to the potential for Aprepitant to significantly increase the exposure of these medicines.

Exposure-Modifying Combinations

  • Corticosteroids: The official prescribing information mandates specific dose reductions for co-administered Dexamethasone and Methylprednisolone to mitigate the increased exposure resulting from CYP3A4 inhibition.
  • Anticoagulants: Due to CYP2C9 induction, co-administration with Warfarin requires close INR monitoring in the two weeks following the start of Aprepitant therapy.
  • Hormonal Contraceptives: Aprepitant may reduce the efficacy of low-dose oral contraceptives and other hormonal methods, requiring the use of alternative barrier methods during treatment and for 28 days following the last dose.
  • Strong CYP Modulators: Co-administration with strong CYP3A4 inhibitors (e.g., Ketoconazole) or strong CYP3A4 inducers (e.g., Rifampin, St. John's Wort) may significantly alter the plasma concentration of Aprepitant itself.

Mechanism of Action

Selective Blockade of the NK1 Receptor

Aprepitant functions as a selective antagonist by binding with high affinity to the Neurokinin-1 ( NK1) receptor. This receptor is the primary target for the neuropeptide Substance P ( SP). The competitive blockade prevents SP from activating the receptor site, thereby suppressing the SP-mediated communication cascade essential for the initiation of the emetic reflex.


Interrupting the Central Emetic Pathway

The central action of aprepitant disrupts the neural pathways in the brainstem that govern emetic signaling. The drug's high lipid solubility ensures it crosses the blood-brain barrier to effectively occupy NK1 receptors in the Area Postrema and Vomiting Center. This action dampens neural activity, effectively modulating the neural threshold for emetic signal propagation.


Mechanistic Complementarity and Duration

The NK1 receptor blockade targets a pathway that is separate from those addressed by 5- HT3 receptor antagonists. This mechanistic complementarity results in a non-overlapping suppression of emetic signaling. Furthermore, the drug achieves sustained receptor occupancy, meaning its antagonistic effect is prolonged, thereby modulating sustained physiological signaling within the targeted pathways.

Dosage and Administration Information

Official Administration and Dosing Guidelines

Aprepitant and its prodrug, Fosaprepitant, are used in fixed, short-term courses and must be administered strictly according to established schedules. The routes of administration are oral (capsule or suspension) or intravenous (IV) via the prodrug Fosaprepitant.

Standard Adult Dosing Regimens

Indication Route / Form Regimen Timing Constraint
CINV (3-Day Oral) Oral Capsule (125 mg, 80 mg) 125 mg on Day 1, then 80 mg on Days 2 & 3. Day 1 dose is 1 hour prior to chemotherapy.
CINV (Single-Dose IV) Intravenous (Fosaprepitant 150 mg) 150 mg on Day 1 only. Infusion completed ~30 minutes prior to chemotherapy.
PONV (Single Oral Dose) Oral Capsule (40 mg) 40 mg single dose. Administer within 3 hours prior to anesthesia induction.

Administration Instructions and Conditions

  • Food Status: Oral capsules and the oral suspension may be taken with or without food. Capsules must be swallowed whole and should not be opened or crushed.
  • Co-Administration Requirement: Aprepitant must be used as a component of a combination antiemetic regimen that includes a 5-HT3 antagonist and a corticosteroid (e.g., Dexamethasone).
  • Co-Therapy Dosing Constraint: The dose of co-administered oral Dexamethasone must be reduced by approximately 50% when used with the Aprepitant regimen.
  • Pediatric Dosing: For pediatric patients aged 6 months and older, dosing for CINV is weight-based, utilizing the oral suspension or IV formulation, with specific timing and dose requirements defined by age and weight.
  • Special Populations: No dosage adjustment is necessary for older adults, or for patients with renal impairment or mild-to-moderate hepatic impairment.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Aprepitant

Evidence for use in Chemotherapy-Induced Nausea and Vomiting (CINV)

Research has primarily focused on Aprepitant's role in regimens used for prophylaxis against Chemotherapy-Induced Nausea and Vomiting (CINV). The evidence is drawn from numerous large-scale, methodologically rigorous Randomized Controlled Trials (RCTs). These studies compared Aprepitant alongside standard antiemetics against the standard regimen combined with a placebo. Research examined outcomes related to acute symptom patterns (the first 24 hours after chemotherapy) and delayed symptom patterns (25 to 120 hours post-chemotherapy).

The trials monitored outcomes related to physical discomfort, such as the absence of vomiting and retching, and the rate of rescue anti-sickness medicine use, which is referred to as achieving a "Complete Response." Studies conducted during periods of increased symptom activity described patterns where the Complete Response rate in regimens that included Aprepitant was observed to differ from those that did not, particularly during the delayed phase. Findings describe patterns observed in these studies where the inclusion of Aprepitant in the regimen was associated with differing measured outcomes compared to the standard antiemetic regimen alone.

Evidence for use in Postoperative Nausea and Vomiting (PONV)

The research supporting Aprepitant for preventing sickness after surgery primarily involves short-term, double-blind RCTs. Research examined the medicine's use in adult patients identified as being at high risk for PONV. The studies monitored outcomes capturing phases of heightened symptom activity, such as the incidence of vomiting and nausea during the initial 24 to 48 hours after the procedure.

What is Still Uncertain About Aprepitant's Research

A key limitation is that for CINV, the trials examined Aprepitant as part of a combination regimen that also included other anti-sickness medicines. The results apply only to the studied combination, meaning the research did not evaluate the effects of the medicine when used alone. Furthermore, long-term effects are not fully established, as the evidence primarily focuses on the acute and delayed phases of symptoms.

Key Studies & References

  1. Label: APREPITANT capsule APREPITANT - aprepitant kit - Full Prescribing Information
  2. Comparison of oral aprepitant and intravenous fosaprepitant for prevention of chemotherapy-induced nausea and vomiting in pediatric oncology patients: a randomized phase III trial
  3. Aprepitant for postoperative nausea and vomiting: A systematic review and meta-analysis
  4. Aprepitant and fosaprepitant as a prophylactic antiemetic for preventing postoperative nausea and vomiting after general anaesthesia: a systematic review and meta-analysis

Frequently Asked Questions (FAQ)

Common questions about Aprepitant (FAQ)

Q: Is Aprepitant the same as other anti-sickness medicines?

A: Aprepitant is classified as a Neurokinin-1 ( NK1) receptor antagonist, which is a different class of medicine than other common anti-sickness treatments like 5- HT3 antagonists. This classification describes how it functions to block the action of a specific chemical called Substance P, which plays a key role in triggering the vomiting reflex.


Q: When can I expect Aprepitant to start working?

A: Official product information indicates the drug is quickly absorbed after it is taken. It typically reaches its highest concentration in the blood about four hours after you take a dose. It is generally administered prior to the triggering event to ensure the antiemetic action is established.


Q: If I only take a single dose of Aprepitant, how long does the effect last?

A: Studies indicate that the drug has a relatively long elimination half-life of approximately 9 to 13 hours. This prolonged presence in the body facilitates sustained receptor blockade, as described in the official mechanism of action.


Q: Are there any major food or drink interactions with Aprepitant?

A: According to the official instructions, you can take oral Aprepitant capsules with or without food. Regulatory documents do not contain specific warnings about interactions with non-alcoholic drinks.


Q: Why do doctors prescribe Aprepitant in a multi-day regimen?

A: The use of Aprepitant in a multi-day regimen is designed to prevent both the nausea and vomiting that occurs immediately (acute) and the symptoms that can arise later (delayed) after chemotherapy. This sustained regimen is indicated to help prevent symptoms that may occur up to 120 hours after treatment.


Q: Is it normal to still feel a little nauseous even after taking Aprepitant?

A: Clinical trials measure the drug's success by whether patients achieve a 'Complete Response,' meaning no vomiting and no need for additional medication. While studies show efficacy, the official results describe achieving a response, but they do not suggest the complete absence of all nausea sensations for every patient.


Q: Does Aprepitant commonly cause skin rashes?

A: Regulatory labeling includes reports of severe, life-threatening skin reactions, such as Stevens-Johnson syndrome, that were observed during post-marketing experience. Common, mild skin rashes are not listed among the most frequent adverse reactions.


Q: Why is the official guidance so specific about drug interactions with Aprepitant?

A: The official guidance is specific because Aprepitant acts as a modulator of important liver enzymes, mainly CYP3A4 and CYP2C9. Because these enzymes are responsible for breaking down many other medicines, Aprepitant has the potential to alter the blood levels of those co-administered medicines.


Q: If I take a supplement, could it interact with Aprepitant?

A: The regulatory label specifically warns that the herbal supplement St. John’s Wort should not be taken with Aprepitant. This is due to the potential for it to alter the body's processing of Aprepitant.


Q: Is there a maximum number of days Aprepitant can be used in a row?

A: Continuous daily administration of Aprepitant is not recommended. According to official documents, the drug's approved use is limited to short-term, fixed regimens (like the three-day course) because the effects of chronic use have not been studied.


Q: How long does Aprepitant stay in your system?

A: Pharmacokinetic data indicate the drug has an apparent terminal half-life of 9 to 13 hours.


Q: I'm worried about dizziness; is that a known side effect of Aprepitant?

A: Dizziness is listed as a common adverse reaction in the clinical trials for both chemotherapy-induced and postoperative nausea and vomiting.


Q: Can Aprepitant affect my blood pressure?

A: Hypotension (low blood pressure) is listed as an adverse reaction that was observed in clinical trials for the prevention of postoperative nausea and vomiting.


Q: Are there any warnings about driving or operating machinery after taking Aprepitant?

A: The patient information leaflet advises caution with driving or operating machinery until an individual knows how the medicine affects them. This warning is based on the potential for side effects such as dizziness and fatigue.


Q: Is Aprepitant available as a generic medicine?

A: Yes. Aprepitant is the non-proprietary, or generic, name for the active drug ingredient. It is available under generic and various brand formulations.


Q: How is the safety of Aprepitant monitored by health authorities?

A: Health authorities monitor the drug's safety by requiring mandatory reporting of serious adverse events and collecting reports from healthcare professionals and the public through post-marketing surveillance programs. This allows them to update the official safety profile over time.


Q: Does Aprepitant cause any changes to my sense of taste?

A: A change in the sense of taste, clinically called dysgeusia, is listed as an uncommon adverse reaction in the clinical studies.


Q: Is Aprepitant a narcotic or addictive substance?

A: Official documents state that Aprepitant is classified as a Neurokinin-1 ( NK1) Receptor Antagonist. It is not classified as a controlled substance or narcotic.


Q: Can Aprepitant be used for morning sickness?

A: Aprepitant is indicated only for the prevention of nausea and vomiting caused by chemotherapy or surgery. It is not approved or indicated for morning sickness (nausea and vomiting associated with pregnancy).


Q: Are there different brand names for the drug Aprepitant?

A: Yes. The active ingredient Aprepitant is sold under various brand names, most commonly EMEND. Its intravenous formulation is sold under the name IVEMEND.


Q: Does the effectiveness of Aprepitant change over time with repeated use?

A: Clinical trial data describes that the efficacy of the Aprepitant-containing regimen was generally maintained across multiple cycles of chemotherapy.


Q: What is the difference between Aprepitant and its active metabolite?

A: Aprepitant is the primary active compound that works to block the NK1 receptor. Although the drug is broken down into various metabolites in the liver, these resulting compounds are considered to be only weakly active.

How should Aprepitant be stored and disposed of?

How to Store and Dispose of Aprepitant

Storage requirements for Aprepitant formulations are strictly defined to maintain product stability and must be followed as described in official labeling.


Storage Conditions

  • Aprepitant Capsules: Must be stored at 20 C to 25 C (68 F to 77 F) (Controlled Room Temperature). They must be kept out of the reach of children.
  • Injectable Solution (Unopened Vial): Requires refrigeration at 2 C to 8 C (36 F to 46 F) and must not be frozen.

Stability and Handling

Stability limits apply once the injectable product is prepared (diluted). The diluted solution must be inspected for particulate matter or discoloration and discarded if either is present. Any unused portion of the prepared injectable solution must also be discarded.

Disposal

Unused or expired Aprepitant must be disposed of according to local regulations to prevent environmental contamination.

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

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