Emend 80mg/125mg Caps Tri-Pack
It is used to prevent upset stomach and throwing up.
Drug Class
Antiemetic
Pharmacologic Class
Neurokinin-1 (NK1) Receptor Antagonist
Pregnancy Category
Category B
FDA Approved
Aug 2003
DEA Schedule
Not Controlled
Overview
What is this medicine?
Aprepitant is a medication used to prevent nausea and vomiting, especially after chemotherapy or surgery. It works by blocking certain natural substances in the brain that cause nausea and vomiting.
How to Use This Medicine
To take this medication correctly, follow your doctor's instructions and read all the information provided. You can take this drug with or without food, but be sure to follow your doctor's specific guidance on this. Swallow the medication whole - do not chew, open, or crush it.
To store this medication properly, keep it at room temperature in a dry location, avoiding the bathroom. If you miss a dose, contact your doctor for advice on what to do next.
To store this medication properly, keep it at room temperature in a dry location, avoiding the bathroom. If you miss a dose, contact your doctor for advice on what to do next.
Lifestyle & Tips
- Take exactly as prescribed by your doctor, usually before chemotherapy or surgery.
- Can be taken with or without food.
- Do not crush, chew, or open the capsules.
- If you miss a dose, take it as soon as you remember, but do not take a double dose. Contact your doctor for advice.
- Inform your doctor about all other medications, supplements, and herbal products you are taking, as aprepitant can interact with many drugs, including birth control pills and blood thinners.
- Use an alternative method of birth control during treatment with aprepitant and for at least 28 days after the last dose, as it can make oral contraceptives less effective.
- Avoid grapefruit and grapefruit juice while taking this medication.
Available Forms & Alternatives
Available Strengths:
Generic Alternatives:
Dosing & Administration
Adult Dosing
Standard Dose:
Highly Emetogenic Chemotherapy (HEC): Day 1: 125 mg orally 1 hour before chemotherapy. Days 2 and 3: 80 mg orally once daily in the morning. Moderately Emetogenic Chemotherapy (MEC): Day 1: 125 mg orally 1 hour before chemotherapy. Postoperative Nausea and Vomiting (PONV): 40 mg orally within 3 hours prior to induction of anesthesia.
Dose Range:
40 - 125 mg
Condition-Specific Dosing:
Chemotherapy-Induced Nausea and Vomiting (CINV) - HEC:
Day 1: 125 mg, Days 2 & 3: 80 mg
Chemotherapy-Induced Nausea and Vomiting (CINV) - MEC:
Day 1: 125 mg
Postoperative Nausea and Vomiting (PONV):
40 mg
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
For CINV in patients 6 months to <12 years: Oral suspension based on body surface area (BSA). For CINV in patients 12 to 17 years: Day 1: 125 mg, Days 2 & 3: 80 mg (capsules).
Adolescent:
For CINV in patients 12 to 17 years: Day 1: 125 mg, Days 2 & 3: 80 mg (capsules).
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment needed.
Moderate:
No dose adjustment needed.
Severe:
No dose adjustment needed (including end-stage renal disease on hemodialysis).
Dialysis:
No dose adjustment needed for patients on hemodialysis.
Hepatic Impairment:
Mild:
No dose adjustment needed (Child-Pugh score 5-6).
Moderate:
No dose adjustment needed (Child-Pugh score 7-9).
Severe:
Not recommended due to lack of clinical data (Child-Pugh score >9).
Pharmacology
Mechanism of Action
Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. It augments the antiemetic activity of 5-HT3 receptor antagonists and corticosteroids and inhibits both the acute and delayed phases of chemotherapy-induced emesis.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 59-69% (oral capsule)
Tmax:
Approximately 4 hours
FoodEffect:
Food has no clinically significant effect on the bioavailability of aprepitant.
Distribution:
Vd:
Approximately 70 L
ProteinBinding:
Greater than 99.5%
CnssPenetration:
Yes (crosses blood-brain barrier)
Elimination:
HalfLife:
Approximately 9-13 hours (dose-dependent)
Clearance:
Approximately 67-84 mL/min
ExcretionRoute:
Primarily fecal (86%), minor renal (5%)
Unchanged:
Less than 1% (urine), approximately 24% (feces)
Pharmacodynamics
OnsetOfAction:
Within 1 hour (oral administration)
PeakEffect:
Approximately 4 hours (corresponds to Tmax)
DurationOfAction:
Up to 72 hours (due to long half-life and sustained NK1 receptor occupancy)
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing
+ Tightness in the chest or throat
+ Difficulty breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of a severe skin reaction (Stevens-Johnson syndrome/toxic epidermal necrolysis), such as:
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Red or irritated eyes
+ Sores in the mouth, throat, nose, or eyes
Signs of dehydration, such as:
+ Dry skin, mouth, or eyes
+ Thirst
+ Rapid heartbeat
+ Dizziness
+ Rapid breathing
+ Confusion
Signs of infection, such as:
+ Fever
+ Chills
+ Severe sore throat
+ Ear or sinus pain
+ Cough
+ Increased or changed sputum production
+ Pain while urinating
+ Mouth sores
+ Wounds that will not heal
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people experience no side effects or only mild ones. If you notice any of the following side effects, or if they bother you or do not go away, contact your doctor or seek medical help:
Dizziness, tiredness, or weakness
Diarrhea or constipation
Decreased appetite
Stomach pain or heartburn
Hiccups
Headache
* Burping
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek immediate medical attention:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing
+ Tightness in the chest or throat
+ Difficulty breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of a severe skin reaction (Stevens-Johnson syndrome/toxic epidermal necrolysis), such as:
+ Red, swollen, blistered, or peeling skin (with or without fever)
+ Red or irritated eyes
+ Sores in the mouth, throat, nose, or eyes
Signs of dehydration, such as:
+ Dry skin, mouth, or eyes
+ Thirst
+ Rapid heartbeat
+ Dizziness
+ Rapid breathing
+ Confusion
Signs of infection, such as:
+ Fever
+ Chills
+ Severe sore throat
+ Ear or sinus pain
+ Cough
+ Increased or changed sputum production
+ Pain while urinating
+ Mouth sores
+ Wounds that will not heal
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people experience no side effects or only mild ones. If you notice any of the following side effects, or if they bother you or do not go away, contact your doctor or seek medical help:
Dizziness, tiredness, or weakness
Diarrhea or constipation
Decreased appetite
Stomach pain or heartburn
Hiccups
Headache
* Burping
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe dizziness or fainting
- Rash, itching, or hives
- Swelling of the face, lips, tongue, or throat
- Difficulty breathing or swallowing
- Unusual bleeding or bruising (if on warfarin)
- Signs of infection (fever, chills, persistent sore throat)
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
Any medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This is crucial because certain medications, such as those used to treat HIV, infections, seizures, and other conditions, may interact with this drug and should not be taken concurrently.
Please note that this is not an exhaustive list of all medications or health conditions that may interact with this drug.
To ensure your safety, it is vital to discuss all of your medications and health conditions with your doctor and pharmacist. This includes:
All prescription and OTC medications
Natural products
Vitamins
* Any health problems you are experiencing
Before starting, stopping, or changing the dose of any medication, including this one, you must consult with your doctor to confirm that it is safe to do so. This will help prevent any potential interactions or adverse effects.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction you experienced, including any symptoms that occurred.
Any medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. This is crucial because certain medications, such as those used to treat HIV, infections, seizures, and other conditions, may interact with this drug and should not be taken concurrently.
Please note that this is not an exhaustive list of all medications or health conditions that may interact with this drug.
To ensure your safety, it is vital to discuss all of your medications and health conditions with your doctor and pharmacist. This includes:
All prescription and OTC medications
Natural products
Vitamins
* Any health problems you are experiencing
Before starting, stopping, or changing the dose of any medication, including this one, you must consult with your doctor to confirm that it is safe to do so. This will help prevent any potential interactions or adverse effects.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.
To avoid potential interactions, do not consume grapefruit or grapefruit juice while taking this drug.
If you are using birth control pills or other hormone-based birth control methods, be aware that this medication may reduce their effectiveness in preventing pregnancy. Therefore, it is recommended to use an additional form of birth control, such as a condom, during treatment and for 1 month after the last dose.
If you are pregnant, planning to become pregnant, or are breast-feeding, notify your doctor. You and your doctor will need to discuss the potential benefits and risks of this medication to both you and your baby.
To avoid potential interactions, do not consume grapefruit or grapefruit juice while taking this drug.
If you are using birth control pills or other hormone-based birth control methods, be aware that this medication may reduce their effectiveness in preventing pregnancy. Therefore, it is recommended to use an additional form of birth control, such as a condom, during treatment and for 1 month after the last dose.
If you are pregnant, planning to become pregnant, or are breast-feeding, notify your doctor. You and your doctor will need to discuss the potential benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- Drowsiness
- Headache
- Constipation
What to Do:
There is no specific antidote for aprepitant overdose. Treatment should be symptomatic and supportive. Call 911 or your local poison control center (e.g., 1-800-222-1222 in the US) immediately.
Drug Interactions
Contraindicated Interactions
- Pimozide
- Terfenadine
- Astemizole
- Cisapride
Major Interactions
- Warfarin (INR monitoring required)
- Oral contraceptives (alternative contraception recommended)
- Corticosteroids (e.g., Dexamethasone, Methylprednisolone - dose reduction needed)
- Immunosuppressants (e.g., Cyclosporine, Tacrolimus, Sirolimus, Everolimus - monitor levels)
- Benzodiazepines (e.g., Midazolam, Alprazolam, Triazolam - monitor for increased sedation)
- Chemotherapeutic agents metabolized by CYP3A4 (e.g., Docetaxel, Paclitaxel, Etoposide, Irinotecan, Vinblastine, Vincristine, Ifosfamide - monitor for toxicity)
- Strong CYP3A4 inducers (e.g., Rifampin, Phenytoin, Carbamazepine, Phenobarbital - may reduce aprepitant efficacy)
- Strong CYP3A4 inhibitors (e.g., Ketoconazole, Itraconazole, Clarithromycin, Ritonavir, Nelfinavir - may increase aprepitant levels)
Moderate Interactions
- Calcium channel blockers (e.g., Diltiazem, Verapamil)
- Erythromycin
- Grapefruit juice
Minor Interactions
- Not specifically listed as minor, but general caution with other CYP3A4 substrates/inhibitors/inducers.
Monitoring
Baseline Monitoring
Baseline liver function tests (LFTs)
Rationale: Aprepitant is extensively metabolized by the liver; caution in severe hepatic impairment.
Timing: Prior to initiation, especially in patients with known hepatic dysfunction.
Routine Monitoring
INR (International Normalized Ratio)
Frequency: Regularly, especially during the 2-week period following the start of aprepitant, and for several days after the last dose.
Target: Therapeutic range for warfarin
Action Threshold: Adjust warfarin dose as needed based on INR.
Signs and symptoms of adverse reactions
Frequency: Daily during treatment and for several days after.
Target: N/A
Action Threshold: Manage symptoms, consider dose adjustment or discontinuation if severe.
Efficacy of antiemetic regimen
Frequency: Daily during chemotherapy cycles.
Target: Absence or minimal nausea and vomiting
Action Threshold: Adjust concomitant antiemetics if inadequate control.
Symptom Monitoring
- Nausea
- Vomiting
- Fatigue
- Hiccups
- Constipation
- Diarrhea
- Headache
- Dizziness
- Signs of hypersensitivity reaction (rash, itching, swelling, severe dizziness, trouble breathing)
- Signs of infection (fever, chills, sore throat) due to potential neutropenia (rare)
Special Patient Groups
Pregnancy
Category B. Animal studies have not shown harm to the fetus, but there are no adequate and well-controlled studies in pregnant women. Use only if clearly needed.
Trimester-Specific Risks:
First Trimester:
Low risk based on animal data, but human data limited.
Second Trimester:
Low risk based on animal data, but human data limited.
Third Trimester:
Low risk based on animal data, but human data limited.
Lactation
Aprepitant is excreted in the milk of lactating rats. It is not known whether aprepitant is excreted in human milk. Caution should be exercised when aprepitant is administered to a nursing woman. The decision to discontinue nursing or discontinue the drug should take into account the importance of the drug to the mother.
Infant Risk:
L3 - Moderate risk; potential for adverse effects on the infant. Monitor infant for drowsiness, constipation, or other adverse effects.
Pediatric Use
Approved for CINV in pediatric patients 6 months and older. Dosing varies by age and body surface area for younger children. Safety and efficacy for PONV not established in pediatric patients.
Geriatric Use
No dosage adjustment is necessary for elderly patients. Efficacy and safety profiles are similar to those in younger adults. However, elderly patients may be more sensitive to drug effects and potential interactions.
Clinical Information
Clinical Pearls
- Aprepitant is highly effective when used as part of a multi-drug antiemetic regimen (e.g., with a 5-HT3 antagonist and a corticosteroid).
- The tri-pack formulation (125mg Day 1, 80mg Day 2, 80mg Day 3) is specifically designed for highly emetogenic chemotherapy.
- Due to its CYP3A4 interactions, careful review of concomitant medications is crucial, especially for warfarin (INR monitoring) and oral contraceptives (alternative contraception).
- The long half-life of aprepitant contributes to its efficacy in preventing delayed CINV.
- Oral suspension formulation is available for pediatric patients who cannot swallow capsules.
Alternative Therapies
- 5-HT3 receptor antagonists (e.g., Ondansetron, Granisetron, Palonosetron)
- Corticosteroids (e.g., Dexamethasone)
- Dopamine receptor antagonists (e.g., Prochlorperazine, Metoclopramide)
- Olanzapine (atypical antipsychotic with antiemetic properties)
Cost & Coverage
Average Cost:
Varies widely, typically $100-$300+ per Tri-Pack (1x125mg, 2x80mg)
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (Brand), Tier 1 (Generic) - often covered for CINV/PONV with prior authorization or step therapy requirements.
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so it's a good idea to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it happened.