Aprecap

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Aprecap

Method of action: Antiemetic

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 Aprecap

Quick Facts

Property Description
Active ingredient Aprepitant
Form Oral capsule, Intravenous emulsion (as Fosaprepitant)
Pharmacological class Neurokinin-1 (NK1) receptor antagonist
General purpose Prophylaxis and relief of nausea and vomiting
Origin Synthetic

Aprepitant: Definition and Pharmacological Classification

Aprepitant is a highly specialized, synthetic anti-emetic agent that belongs to the pharmacological class of Neurokinin-1 (NK1) receptor antagonists. This classification highlights its targeted action designed to prevent nausea and vomiting. The drug's mechanism is clinically recognized for its high selectivity, operating by interrupting central neurological signaling pathways. The drug's activity stems from its specific interaction as an antagonist of the human NK1 receptor in the brain, reinforcing its distinct role in supportive care.

The Active Compound and Drug Forms

The core active chemical substance is Aprepitant, typically delivered for patient use as an oral capsule. For situations requiring non-oral administration, a related precursor compound, Fosaprepitant, is utilized for intravenous delivery, a feature that differentiates this therapeutic strategy. Fosaprepitant is categorized as a prodrug; it is chemically and rapidly converted into the active Aprepitant substance once inside the body. The existence of both the oral capsule and the intravenous prodrug enables flexible patient management, particularly for patient groups who may be unable to tolerate oral medications.

General Purpose: Central Relief from Nausea and Vomiting

The primary purpose of Aprepitant is the effective prophylaxis and relief of nausea and vomiting. Its mechanism is conceptualized as a precise molecular blockade, primarily targeting the central nervous system. By preventing the binding of the natural signaling molecule Substance P at the NK1 receptors, the drug suppresses the powerful nerve signals that initiate the emetic reflex. This selective intervention is particularly relevant for managing intense, centrally-mediated emetic episodes.

Regulatory References

  1. EMEND (Aprepitant) European Public Assessment Report (EPAR) Overview

What side effects are possible with Aprecap?

Possible side effects and safety information

The safety profile for Aprepitant (Aprecap) is based on official regulatory classifications, detailing adverse reactions by frequency and the body system affected. These classifications are used to communicate the medicine’s established risk profile.

Frequency and System-Based Adverse Reactions

Adverse reactions have been officially documented across various System-Organ Classes. Gastrointestinal disorders and nervous system disorders are among the frequently listed categories.

Frequency Classification (Based on regulatory standards) Key Examples (from official labeling)
Common Fatigue, headache, hiccups, constipation, dyspepsia, decreased appetite
Uncommon Anaemia, febrile neutropenia, dizziness, somnolence, insomnia, palpitations, malaise
Rare Duodenal ulcer perforation, disorientation, severe skin reactions

Serious Safety Considerations

The regulatory profile documents rare but serious adverse reactions. These include reports of hypersensitivity reactions, such as anaphylaxis and anaphylactic shock, often occurring with the intravenous administration. Postmarketing experience has also included rare reports of severe cutaneous reactions, such as Stevens-Johnson syndrome and Toxic Epidermal Necrolysis.

Regulatory Restrictions and Limitations

The official safety information specifies important limitations on use. Co-administration of Aprepitant with certain medications metabolized by the CYP3A4 enzyme (e.g., pimozide, terfenadine) is contraindicated due to the potential for elevated drug concentrations, which may lead to serious or life-threatening reactions. Additionally, the efficacy of hormonal contraceptives may be reduced during treatment and for a period of 28 days following the last dose. Caution is officially advised for patients with severe hepatic impairment due to limited clinical data. Chronic continuous administration is not recommended as the safety profile for prolonged use has not been established.

Overdose and Emergency Response

Aprecap Overdose and When to Seek Help

This section describes the officially documented information regarding Aprecap (aprepitant) overdose and required emergency actions, based on regulatory filings.


Documented Overdose Findings

Symptoms reported in studies involving single, high doses of aprepitant (up to 600 mg) in healthy subjects were generally mild to moderate. The most frequently observed manifestations were drowsiness and headache.

Overdose Manifestations Context of Observation
Drowsiness Reported in high-dose study participants
Headache Reported in high-dose study participants

Required Emergency Actions

In the event of a suspected overdose, it is essential to contact a poison control center immediately or seek emergency medical care. Treatment for Aprecap overdose is primarily general supportive care and continuous monitoring of the patient's vital signs.

  • Contacting Emergency Services: Call emergency services (e.g., 911) immediately if the individual has collapsed, experienced a seizure, has trouble breathing, or cannot be awakened.
  • Effectiveness of Intervention: Due to the drug's properties, certain interventions may be ineffective. The antiemetic action of aprepitant means that inducing emesis (vomiting) may not be successful. Furthermore, due to the drug's high level of plasma protein binding, hemodialysis is not expected to be an effective method for removing Aprecap from the body.

Therapeutic Uses of Aprecap

What Aprecap Treats: Main Uses and Benefits

Aprecap is a medication generally used for the prophylactic management of distressing symptoms related to specific medical procedures. It is commonly used for the prevention of nausea and vomiting following cancer chemotherapy and the prevention of symptoms after surgery.

The medication's primary use is applied across domains where additional symptomatic support is needed to address symptom clusters that may become intense or disruptive. Aprecap may be part of symptomatic management in the preventative treatment of severe nausea, retching, and vomiting associated with cancer chemotherapy regimens categorized as highly or moderately emetogenic, and is also used for the prevention of postoperative nausea and vomiting (PONV) in high-risk adult patients.

This strategy generally provides supportive relief that helps patients cope more steadily during periods of heightened symptoms. The use is relevant when short-term symptomatic assistance is needed:

“It assists with maintaining functional stability and contributes to easing the overall symptom load during symptomatic periods.”

Quick Fact: Relief for Emetic Symptoms

Indication Type Primary Symptoms Addressed Time of Symptom Onset
CINV Prophylaxis Severe Nausea, Vomiting, Retching Acute (shortly after treatment) and Delayed (days following treatment)
PONV Prophylaxis Postoperative Nausea and Vomiting Perioperative Period

Eligibility and Restrictions for Use

Eligibility for Aprecap (Aprepitant) is defined by official regulatory criteria, detailing populations for whom use is permitted, restricted, or strictly prohibited.

Absolute Contraindications (Must Not Use)

Aprecap is contraindicated in patients with a known hypersensitivity to the drug or its components. It must not be co-administered with specific medications, including pimozide, terfenadine, astemizole, or cisapride. This prohibition is due to the potential for severe or life-threatening reactions resulting from drug metabolism changes.

Age and Physiological Status

The approved age groups vary by formulation and indication:

Age Group Eligibility Status
Adults ( ge 18 years) Permitted for all approved indications.
Adolescents ( ge 12 years) Permitted for Chemotherapy-Induced Nausea and Vomiting (CINV) prophylaxis.
Children ( <12 years) Capsules are generally not recommended. Use is not established for Postoperative Nausea and Vomiting (PONV) prophylaxis in the pediatric population (le 18 years).
Older Adults Permitted; no age-based dose adjustment is required.

Organ Function and Special Conditions

Use is not recommended in patients with severe hepatic impairment (Child-Pugh score > 9) due to a lack of supporting clinical data. However, use is permitted in patients with mild to moderate hepatic impairment, renal impairment, or end-stage renal disease undergoing hemodialysis.

Pregnancy and Lactation are generally not recommended for use with Aprecap, as human data is limited and unknown excretion into breast milk requires caution. Additionally, the medicine is indicated only for short-term prophylaxis and is not recommended for chronic continuous administration.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Aprecap (aprepitant) has a formally documented interaction profile centered on its role as a moderate inhibitor and inducer of Cytochrome P450 3A4 (CYP3A4), and an inducer of CYP2C9. These pharmacokinetic effects are the basis for regulatory requirements concerning co-administration with numerous other medicines.

Official Regulatory Restrictions

Classification Interacting Substance Official Regulatory Requirement
Contraindicated Pimozide Co-administration is prohibited due to the risk of greatly increased Pimozide plasma concentration, which can lead to QT interval prolongation.
Dose Modification Dexamethasone Aprepitant increases Dexamethasone exposure; the official regimen requires a dosage reduction for co-administered Dexamethasone.
Monitoring Required Warfarin Aprepitant induces CYP2C9, causing a decrease in Warfarin's International Normalized Ratio (INR); close monitoring is required for two weeks following the Aprepitant regimen.

Timing and Substance Interactions

The medicine is documented to reduce the efficacy of oral hormonal contraceptives. Official labeling mandates the use of non-hormonal contraception during treatment and for 28 days (one month) following the last dose. Co-administration with strong CYP3A4 inhibitors (e.g., Ketoconazole) increases Aprepitant exposure, while strong inducers (e.g., Rifampin) decrease it. The herbal product St. John's Wort is not recommended due to its strong CYP3A4 inducing effects.

Mechanism of Action

The action of Aprepitant (Aprecap) is based on its mechanism of action, which involves modulation of central neurological signaling pathways associated with the emetic reflex.

Selective Blockade of the NK1 Receptor System

The drug functions as a highly selective, high-affinity antagonist of the Neurokinin-1 ( NK1) receptor. This mechanism prevents the endogenous neuropeptide Substance P from binding to the receptor. This molecular interaction occurs primarily in critical brainstem areas, such as the Area Postrema and the Nucleus Tractus Solitarius, which are integral to the Vomiting Center. The high lipophilicity of Aprepitant ensures sufficient drug penetration across the blood-brain barrier to achieve the necessary central receptor occupancy.

Modulation of the Central Emetic Cascade

By blocking the NK1 receptor pathway centrally, Aprepitant modulates a key signal input that would otherwise activate the Vomiting Center. This targeted action modulates neural signaling at the control point for emesis. This mechanism interrupts the complex mechanistic cascade necessary for the coordination of the physiological act of retching and vomiting, which modulates the physiological response patterns associated with the act of emesis.

Multi-Pathway Mechanistic Synergy

The mechanism is complementary to other pharmacological agents, frequently alongside 5 -HT3 receptor antagonists and corticosteroids. This approach allows for the simultaneous modulation of multiple distinct signaling pathways (Tachykinin, Serotonin, and other regulatory systems). By engaging multiple mechanistic domains, this synergy facilitates simultaneous modulation of various input signals contributing to the emetic reflex.

Dosage and Administration Information

Aprecap (Aprepitant/Fosaprepitant) is used according to specific, prophylactic regimens. Its administration utilizes two main forms: an oral capsule (Aprepitant) and an intravenous (IV) infusion (Fosaprepitant, a prodrug). The choice of route and dose is dependent on the type of prophylactic need, such as preventing nausea and vomiting following chemotherapy (CINV) or surgery (PONV).

For CINV, the medication is typically administered in a three-day cyclic course as part of a combination regimen that also includes a corticosteroid and a 5-HT3 antagonist. The regimen generally involves a 125 mg oral dose on Day 1, followed by 80 mg oral doses on Days 2 and 3. Alternatively, a single 150 mg IV dose of the prodrug may be administered on Day 1.

The timing of the dose is strictly controlled. The initial dose, whether oral or IV, must be given prior to the start of chemotherapy (e.g., the IV infusion completed approximately 30 minutes before treatment). For oral intake, the capsules may be taken with or without food, but must be swallowed whole. Use is limited to these short, episodic courses and is not authorized for chronic, continuous administration.

Key Administration Rule Procedural Condition
Frequency Pattern Episodic and cyclic, not continuous.
IV Delivery Administered as a slow infusion, not as a bolus.
Dose Adjustments Not generally necessary for older adults or mild hepatic/renal impairment.

Recent Clinical Evidence

Research Evidence: Overview of Studies for Aprecap

Evidence for Prevention of Chemotherapy-Induced Nausea and Vomiting (CINV)

Aprecap was studied for its use in research exploring symptoms related to nausea and vomiting associated with cancer chemotherapy. Research primarily consists of Randomized Controlled Trials (RCTs), which compared the use of an Aprecap-containing regimen against established comparative regimens. These trials were typically short-term and applied in studies examining patient-reported experiences related to physical discomfort.

The primary measurement was often the Complete Response rate, which assessed the proportion of participants who experienced no vomiting or retching and monitored the absence of the need for rescue antiemetic medication during the study period. For patients receiving highly emetogenic chemotherapy (HEC), findings describe patterns observed in studies related to Complete Response rates when an Aprecap-based regimen was used compared to their assigned control groups. However, findings were mixed regarding the control of nausea severity that was monitored across the different study phases.

Evidence for Prevention of Postoperative Nausea and Vomiting (PONV)

Aprecap also was evaluated in research exploring the prevention of symptoms after a surgical procedure, specifically as a single-dose prophylactic agent studied in the context of administration in the pre-operative setting. Research explored short-term symptom changes, focusing on outcomes capturing phases of heightened symptom activity immediately following the surgical procedure. Data show patterns related to the achievement of a Complete Response during this critical window, and studies monitored the need for rescue antiemetic medication in the groups receiving the prophylactic dose.

What Remains Unstudied or Uncertain about the Evidence

The majority of pivotal studies focused on defined time intervals corresponding to the most active phases of symptoms, meaning follow-up durations were limited. The evidence base provides limited insight into how patterns of symptoms or recovery might evolve over extended periods, and long-term effects are not fully established beyond the initial treatment window. Furthermore, sample sizes were modest for many of the studies exploring use in special populations (like children and adolescents), which means the results apply only to the populations studied and generalizability to broader groups is uncertain.

Key Studies & References Comparison of oral aprepitant and intravenous fosaprepitant for prevention of chemotherapy-induced nausea and vomiting in pediatric oncology patients: a randomized phase III trial

Frequently Asked Questions (FAQ)

Common questions about Aprecap (FAQ)

Q: Is Aprecap a chemotherapy drug?

A: Aprecap is classified as an antiemetic medication, which is indicated for the prevention of sickness and vomiting that is associated with cancer chemotherapy. It is not a chemotherapy agent itself.

Q: How quickly does it start to work?

A: The drug’s prophylactic (preventative) nature requires the first dose to be taken approximately 1 hour prior to the start of chemotherapy, as specified in the product labeling.

Q: Is this the same drug as Emend?

A: Emend is a brand name for the active substance aprepitant, which is the medication contained within Aprecap.

Q: What are the most common feelings or side effects I should expect?

A: Official product information indicates that common side effects reported in clinical studies include fatigue, headache, diarrhea, constipation, dizziness, and difficulty sleeping (insomnia).

Q: Does it make you tired or fatigued?

A: Yes, fatigue is listed as a very common side effect in the official regulatory documents.

Q: Is it safe for people with liver disease?

A: Regulatory information advises that caution should be exercised when administering the drug to patients who have severe hepatic impairment, which is a form of significant liver condition.

Q: How long does Aprecap stay in the body?

A: Official information indicates that the apparent terminal half-life of the drug is approximately 9 to 13 hours. This measurement describes how quickly the medicine is cleared from the body.

Q: Can I take it with food or drink?

A: According to the official instructions, the oral formulation of the drug may be taken with or without food.

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

A: Regulatory guidelines indicate that if a dose is missed, it should be taken as soon as possible. However, if it is almost time for the next scheduled dose, the missed dose should be skipped, and doses should not be doubled.

Q: Can I take common over-the-counter pain medications, such as ibuprofen, with it?

A: Aprepitant is documented to induce certain liver enzymes (CYP2C9), which may reduce the concentration of other medicines metabolized by this enzyme, such as warfarin. Due to this potential for drug interaction, the regulatory guidance requires consultation with a healthcare professional regarding all concurrent medications.

Q: Does it cause headaches?

A: Yes, headache is listed as a common side effect in the official product information.

Q: Can children under 12 use this drug?

A: Official documents indicate that the drug is indicated for use in certain pediatric patients. Eligibility extends to patients as young as 6 months of age, depending on the specific indication and formulation.

Q: Are there any long-term side effects from using it?

A: The drug is not authorized for chronic continuous administration. Official documents state that chronic use is not recommended because it has not been studied in that setting, and the drug interaction profile could potentially change during continuous use.

Q: Is a generic version of Aprecap available?

A: The generic name for the active ingredient in Aprecap is aprepitant.

Q: Can I take Aprecap if I am pregnant?

A: The drug's official regulatory condition for use during pregnancy is only when clearly needed, as insufficient human data are available to fully inform the risk associated with its use.

Q: Will I get constipated or have diarrhea?

A: Both diarrhea and constipation are listed as potential side effects. Diarrhea is noted as a very common side effect, while constipation is listed as a common side effect.

Q: How does the NK-1 receptor work in my body?

A: The medicine is described as an antagonist of the Neurokinin-1 (NK-1) receptor. This means it works by blocking the action of Substance P, which is a naturally occurring neuro-chemical associated with triggering nausea and vomiting.

Q: Why is there an intravenous (IV) version of this drug?

A: There is an intravenous (IV) form of the drug, known as fosaprepitant, which acts as an alternative administration route. This IV form is indicated for the prevention of sickness associated with chemotherapy and surgery in specific regimens.

Q: Does it affect my blood pressure?

A: Official documents note that hypertension (high blood pressure) is listed as a common side effect in some patient populations.

Q: Are the doses different for chemotherapy-induced nausea versus post-operative nausea?

A: Yes, the recommended dosage and treatment schedule are different. Official regulatory documents provide separate dosages for preventing chemotherapy-induced nausea and vomiting (CINV) and for preventing post-operative nausea and vomiting (PONV).

Q: Can I take it for any type of nausea, or only after chemotherapy/surgery?

A: The drug is indicated specifically for the prevention of sickness associated with chemotherapy and surgery. It has not been studied or authorized for the treatment of nausea and vomiting that has already begun.

Q: Is Aprecap a steroid?

A: No, this medicine is not a steroid. It is chemically classified as a neurokinin 1 (NK-1) receptor antagonist and does not have affinity for corticosteroid receptors.

Q: Should I avoid driving or operating machinery while taking it?

A: The product label includes a warning that care is necessary when driving or operating machinery until you know how the drug affects you, due to the potential for reported side effects such as tiredness and dizziness.

Q: Can it cause a rash or a serious allergic reaction?

A: Regulatory warnings state that serious hypersensitivity reactions, including allergic reactions like rash, hives, and anaphylaxis, can occur in some individuals.

Q: Can it make me dizzy?

A: Yes, dizziness is listed in the official documents as a common side effect.

Q: Is Aprecap a controlled substance?

A: The drug is not listed as a DEA-controlled substance in the official government records.

Q: Are there any known interactions with common antidepressants?

A: Aprepitant can inhibit and induce certain liver enzymes (CYP3A4), that process many other medications, including various antidepressants. The regulatory guidance requires consultation with a healthcare professional regarding all concurrent medications.

Q: Does it affect my sleep?

A: Yes, difficulty sleeping, or insomnia, is listed as a common side effect in the official product information.

Q: How should I store the medicine?

A: Official storage instructions indicate that the medicine should be kept out of the reach of children and stored as directed on the original packaging.

Q: Can this drug cause a metallic taste in my mouth?

A: Official product information lists dysgeusia (a distortion of taste) as an uncommon side effect.

Q: Who should not take Aprecap?

A: The medicine is contraindicated, meaning it is a condition under which the drug is not authorized for use, if a patient has a known hypersensitivity (allergic reaction) to the product. It is also contraindicated for use with the drug pimozide due to the risk of a serious interaction.

Q: Are there any serious health conditions where I should not take Aprecap?

A: Regulatory documents state that caution should be exercised when administering the drug to patients who have severe hepatic impairment, which is a form of significant liver disease.

Q: Are there specific patient groups where Aprecap use is limited?

A: Official documents state that caution should be used with severe liver impairment. Use in other patient groups, such as older adults or those with mild kidney impairment, generally does not require a dose adjustment.

Q: Can I take common vitamins or supplements with it?

A: Official documents note the potential for interaction with certain liver enzymes, which may affect other substances. Regulatory guidance therefore requires consultation with a healthcare professional regarding the use of specific supplements or vitamins.

Q: What is the maximum number of days Aprecap is typically used?

A: Official regulatory regimens for chemotherapy-induced nausea and vomiting are typically short, cyclic courses (such as a three-day course). The drug is not authorized for chronic continuous use.

Q: Should I adjust the dose for severe kidney disease?

A: Official guidelines state that no dosage adjustment is generally considered necessary for patients who have kidney impairment or who are receiving hemodialysis.

How should Aprecap be stored and disposed of?

How to Store and Dispose of Aprecap?

The official labeling defines specific environmental and container requirements for storing Aprepitant (Aprecap).

Storage Requirements

Aprepitant capsules must be stored in the original container and kept tightly closed at room temperature, specifically between 20 C to 25 C (68 F to 77 F), while being protected from excess heat and moisture. For the prepared oral suspension, storage is required in the refrigerator until the time of use, and it must not be frozen.

Product Form Temperature / Condition Shelf-Life Limit
Capsules Room temperature (20 C to 25 C) N/A
Prepared Suspension Refrigerated (Do not freeze) Discard after 72 hours

Handling and Disposal

All forms of this medication must be stored out of the sight and reach of children.

Any prepared oral suspension dose that is not used within the 72-hour limit must be discarded. For all unused or expired medication, disposal should follow the specific procedures provided on the product labeling or utilize community drug take-back programs.

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

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