Aprepitant 80mg/125mg Caps Tri-Pack
It is used to prevent upset stomach and throwing up.
Drug Class
Antiemetic
Pharmacologic Class
Substance P/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 medicine used to prevent nausea and vomiting, especially after chemotherapy. It works by blocking certain signals in your brain that cause you to feel sick.
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, 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, 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.
- Do not take more or less than directed.
- Can be taken with or without food.
- If you are taking birth control pills, use an alternative or backup method of contraception (like condoms) during treatment with aprepitant and for 28 days after your last dose, as aprepitant can make birth control less effective.
- If you are taking warfarin (a blood thinner), your doctor will need to monitor your blood clotting time more closely.
- Inform your doctor about all other medications, supplements, and herbal products you are taking.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
For prevention of CINV: Day 1: 125 mg orally 1 hour before chemotherapy. Day 2 & 3: 80 mg orally once daily in the morning.
Dose Range:
80 - 125 mg
Condition-Specific Dosing:
highlyEmetogenicChemotherapy:
Day 1: 125 mg orally 1 hour before chemotherapy. Day 2 & 3: 80 mg orally once daily in the morning.
moderatelyEmetogenicChemotherapy:
Day 1: 125 mg orally 1 hour before chemotherapy. Day 2 & 3: 80 mg orally once daily in the morning.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
For CINV (âĨ6 months to <12 years or <30 kg): Day 1: 3 mg/kg (max 125 mg) IV or 2 mg/kg (max 125 mg) oral suspension. Day 2 & 3: 2 mg/kg (max 80 mg) oral suspension. (Note: Oral capsules not typically used for this age group due to fixed doses)
Adolescent:
For CINV (âĨ12 years): Day 1: 125 mg orally 1 hour before chemotherapy. Day 2 & 3: 80 mg orally once daily in the morning.
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment needed.
Moderate:
No dose adjustment needed.
Severe:
No dose adjustment needed.
Dialysis:
No dose adjustment needed. Aprepitant is not removed by hemodialysis.
Hepatic Impairment:
Mild:
No dose adjustment needed (Child-Pugh A).
Moderate:
No dose adjustment needed (Child-Pugh B).
Severe:
Not studied. Use with caution (Child-Pugh C).
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:
60-65%
Tmax:
4 hours (oral capsule)
FoodEffect:
No clinically meaningful effect on bioavailability when administered with food.
Distribution:
Vd:
70 L
ProteinBinding:
Approximately 97-98%
CnssPenetration:
Yes (crosses blood-brain barrier)
Elimination:
HalfLife:
9-13 hours
Clearance:
Not available (primarily hepatic metabolism)
ExcretionRoute:
Primarily fecal (86%), minor renal (5%)
Unchanged:
<1% in urine, <5% in feces
Pharmacodynamics
OnsetOfAction:
Within 1 hour (oral absorption)
PeakEffect:
4 hours (Tmax)
DurationOfAction:
Up to 72 hours (due to long half-life and 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 immediately or seek emergency 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
+ Trouble 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
+ Fast heartbeat
+ Dizziness
+ Fast 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 may not experience any side effects or may only have mild ones. If you notice any of the following side effects or any other unusual symptoms, contact your doctor for advice:
Feeling dizzy, tired, or weak
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, consult 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 immediately or seek emergency 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
+ Trouble 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
+ Fast heartbeat
+ Dizziness
+ Fast 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 may not experience any side effects or may only have mild ones. If you notice any of the following side effects or any other unusual symptoms, contact your doctor for advice:
Feeling dizzy, tired, or weak
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, consult 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 allergic reactions (rash, itching, swelling of face/tongue/throat, severe dizziness, trouble breathing)
- Signs of infection (fever, chills, sore throat, unusual weakness) - especially if you are receiving chemotherapy
- Unusual bleeding or bruising (if on warfarin)
- Persistent hiccups
- Severe constipation or diarrhea
- Severe abdominal pain
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
* Health problems
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 in conjunction with your other medications and health conditions.
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
* Health problems
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 in conjunction with your other medications and health conditions.
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. As a precaution, use an additional form of birth control, such as a condom, during treatment and for 1 month after your last dose.
If you are pregnant, planning to become pregnant, or are breast-feeding, consult your doctor 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. As a precaution, use an additional form of birth control, such as a condom, during treatment and for 1 month after your last dose.
If you are pregnant, planning to become pregnant, or are breast-feeding, consult your doctor to discuss the potential benefits and risks of this medication to both you and your baby.
Overdose Information
Overdose Symptoms:
- Drowsiness
- Headache
- Constipation
- No specific antidote is available.
What to Do:
Call 1-800-222-1222 (Poison Control Center) or seek immediate medical attention. Supportive care and symptomatic treatment are recommended.
Drug Interactions
Contraindicated Interactions
- Pimozide
- Terfenadine
- Astemizole
- Cisapride
Major Interactions
- Warfarin (INR monitoring required)
- Oral contraceptives (reduced efficacy, use alternative contraception)
- Corticosteroids (e.g., Dexamethasone, Methylprednisolone - dose reduction needed)
- Midazolam (or other CYP3A4 substrates with narrow therapeutic index)
- Fentanyl (increased exposure)
- Alfentanil (increased exposure)
- Ergot alkaloids (e.g., Ergotamine, Dihydroergotamine - increased exposure)
- Immunosuppressants (e.g., Cyclosporine, Tacrolimus, Sirolimus, Everolimus - increased exposure, monitor levels)
Moderate Interactions
- Phenytoin
- Carbamazepine
- Rifampin
- Phenobarbital
- Ketoconazole
- Itraconazole
- Clarithromycin
- Nefazodone
- Ritonavir
- Nelfinavir
- Paroxetine
- Tolbutamide
- Theophylline
Minor Interactions
- Not specifically listed as minor, but general caution with other CYP3A4 substrates/inducers.
Monitoring
Baseline Monitoring
Baseline INR (if on Warfarin)
Rationale: Aprepitant can decrease INR due to CYP2C9 induction, potentially reducing warfarin efficacy.
Timing: Before starting aprepitant
Concomitant medications review
Rationale: Identify potential drug interactions, especially with CYP3A4 substrates (e.g., corticosteroids, oral contraceptives, immunosuppressants).
Timing: Before starting aprepitant
Routine Monitoring
INR (if on Warfarin)
Frequency: Closely monitor for 2 weeks after starting and for 2 weeks after completing aprepitant.
Target: Individualized therapeutic range
Action Threshold: Adjust warfarin dose as needed to maintain target INR.
Efficacy of oral contraceptives
Frequency: Throughout aprepitant treatment and for 28 days after the last dose.
Target: Not applicable
Action Threshold: Advise use of alternative or backup contraception.
Signs/symptoms of adverse reactions
Frequency: Daily during treatment course.
Target: Not applicable
Action Threshold: Manage symptoms, consider dose adjustment or discontinuation if severe.
Symptom Monitoring
- Nausea
- Vomiting
- Fatigue
- Hiccups
- Constipation
- Diarrhea
- Headache
- Dizziness
- Dyspepsia
- Abdominal pain
- Anorexia
- Neutropenia
- Anemia
- Febrile neutropenia (in CINV patients)
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
L3 (Moderately safe). Aprepitant is excreted in rat milk. It is unknown if it is excreted in human milk. Caution should be exercised when aprepitant is administered to a nursing woman. Consider the benefits of breastfeeding versus the potential risks to the infant.
Infant Risk:
Potential for infant exposure and adverse effects (e.g., drowsiness, gastrointestinal upset). Monitor infant for adverse effects.
Pediatric Use
Approved for CINV in children âĨ6 months of age. Dosing varies by age and weight, and oral suspension/IV formulations are often used for younger children. Capsules are typically for adolescents (âĨ12 years) due to fixed doses.
Geriatric Use
No dose adjustment is necessary based on age. Efficacy and safety profiles are similar to younger adults. However, elderly patients may be more sensitive to drug effects or have more comorbidities/concomitant medications, requiring careful monitoring for adverse effects and drug 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) for CINV.
- The tri-pack formulation simplifies dosing for the 3-day CINV regimen.
- Crucial to counsel patients on potential drug interactions, especially with oral contraceptives and warfarin, due to CYP3A4 inhibition and CYP2C9 induction.
- Hiccups are a relatively common side effect, often self-limiting.
- Ensure patients understand the importance of taking the medication on Day 2 and 3, even if they feel well, to prevent delayed CINV.
Alternative Therapies
- Other NK1 receptor antagonists (e.g., Rolapitant, Netupitant)
- 5-HT3 receptor antagonists (e.g., Ondansetron, Granisetron, Palonosetron)
- Corticosteroids (e.g., Dexamethasone)
- Dopamine receptor antagonists (e.g., Prochlorperazine, Metoclopramide)
- Olanzapine (off-label for CINV)
Cost & Coverage
Average Cost:
Varies widely, typically $150-$300+ per Tri-Pack (1x125mg, 2x80mg)
Generic Available:
Yes
Insurance Coverage:
Tier 2 or Tier 3 (often requires prior authorization for brand, generic may be preferred)
General Drug Facts
If your symptoms or health issues persist or worsen, it's 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 be sure to check with your pharmacist for more information. If you have any questions or concerns about your 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 medical attention. When seeking help, be prepared to provide details about the medication, including the amount taken and the time it happened, to facilitate prompt and effective treatment.