Aprepitant 80mg Capsules
It is used to prevent upset stomach and throwing up.
Drug Class
Antiemetic
Pharmacologic Class
Neurokinin-1 (NK1) Receptor Antagonist
Pregnancy 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 or surgery. It works by blocking certain natural substances in your body that cause nausea and vomiting.
How to Use This Medicine
To use this medication correctly, follow your doctor's instructions and read all the information provided. You can take this medication with or without food, but be sure to follow your doctor's specific guidance on this.
When taking this medication, swallow the tablet 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.
When taking this medication, swallow the tablet 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.
Lifestyle & Tips
- Take exactly as prescribed by your doctor.
- Do not stop taking it without consulting your doctor, even if you feel better.
- If you are taking warfarin, your doctor will need to monitor your blood clotting time more closely.
- If you are using hormonal birth control (pills, patch, ring), aprepitant can make it less effective. Use an additional non-hormonal birth control method (like condoms) during treatment and for 28 days after your last dose.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
For highly emetogenic chemotherapy (HEC) or moderately emetogenic chemotherapy (MEC): 125 mg orally on Day 1, followed by 80 mg orally once daily on Days 2 and 3. (Aprepitant 80mg capsule is used for Day 2 and 3 dosing).
Dose Range:
80 - 125 mg
Condition-Specific Dosing:
chemotherapy_induced_nausea_vomiting_HEC:
125 mg on Day 1, then 80 mg on Day 2 and Day 3
chemotherapy_induced_nausea_vomiting_MEC:
125 mg on Day 1, then 80 mg on Day 2 and Day 3
postoperative_nausea_vomiting_prevention:
40 mg orally within 3 hours prior to induction of anesthesia (single dose, not typically 80mg capsule)
Pediatric Dosing
Neonatal:
Not established
Infant:
For CINV (6 months to <2 years): 3 mg/kg (max 125 mg) on Day 1, then 2 mg/kg (max 80 mg) on Days 2 and 3 (oral suspension).
Child:
For CINV (2 to <12 years): 3 mg/kg (max 125 mg) on Day 1, then 2 mg/kg (max 80 mg) on Days 2 and 3 (oral suspension).
Adolescent:
For CINV (>=12 years): 125 mg orally on Day 1, then 80 mg orally once daily on Days 2 and 3 (capsules).
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
Moderate:
No dose adjustment needed
Severe:
Use with caution; no clinical data available for patients with severe hepatic impairment (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:
60-65%
Tmax:
Approximately 4 hours
FoodEffect:
No clinically significant effect on AUC when taken with food.
Distribution:
Vd:
Approximately 70 L
ProteinBinding:
>95%
CnssPenetration:
Yes
Elimination:
HalfLife:
Approximately 9-13 hours
Clearance:
Not available
ExcretionRoute:
Primarily fecal (approximately 57%), minor renal (approximately 5%)
Unchanged:
Not available
Pharmacodynamics
OnsetOfAction:
Within hours (due to oral absorption and receptor binding)
PeakEffect:
Not precisely defined for antiemetic effect, but plasma concentrations peak around 4 hours.
DurationOfAction:
Up to 24 hours or longer due to prolonged receptor occupancy and long half-life, allowing for once-daily dosing.
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
+ 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. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms, contact your doctor for guidance:
Feeling dizzy, tired, or weak
Diarrhea or constipation
Decreased appetite
Stomach pain or heartburn
Hiccups
Headache
* Burping
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, don't hesitate to reach out to 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
+ 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. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms, contact your doctor for guidance:
Feeling dizzy, tired, or weak
Diarrhea or constipation
Decreased appetite
Stomach pain or heartburn
Hiccups
Headache
* Burping
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, don't hesitate to reach out to 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 (e.g., rash, hives, itching, difficulty breathing or swallowing, swelling of the face, throat, tongue, lips, or eyes)
- Dizziness
- Fatigue
- Headache
- Hiccups
- Constipation
- Diarrhea
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, should not be taken with this drug. There are many medications that interact with this drug, and this list is not exhaustive.
* All your health problems, as they may affect the safety of taking this medication.
To ensure your safety, it is critical to discuss all your medications and health problems with your doctor and pharmacist. They will help you determine whether it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting 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, should not be taken with this drug. There are many medications that interact with this drug, and this list is not exhaustive.
* All your health problems, as they may affect the safety of taking this medication.
To ensure your safety, it is critical to discuss all your medications and health problems with your doctor and pharmacist. They will help you determine whether it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor.
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 the 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 the 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:
- Limited experience with overdose. Single doses up to 2000 mg were well tolerated. Drowsiness and headache have been reported.
What to Do:
There is no specific antidote for aprepitant overdose. In case of overdose, the drug should be discontinued and general supportive treatment and monitoring should be employed. Aprepitant is not removed by hemodialysis. Call 1-800-222-1222 (Poison Control).
Drug Interactions
Contraindicated Interactions
- Pimozide
- Astemizole
- Terfenadine
Major Interactions
- Warfarin (monitor INR)
- Oral contraceptives (reduced efficacy)
- Corticosteroids (e.g., Dexamethasone - reduce dose)
- Benzodiazepines (e.g., Midazolam - reduce dose)
- Chemotherapy agents metabolized by CYP3A4 (e.g., Docetaxel, Paclitaxel, Etoposide, Irinotecan, Vinblastine, Vincristine, Ifosfamide)
Moderate Interactions
- CYP3A4 substrates with narrow therapeutic index (e.g., Cyclosporine, Tacrolimus, Sirolimus, Everolimus - monitor levels)
- Phenytoin
- Carbamazepine
- Rifampin
- Ketoconazole
- Paroxetine
Minor Interactions
- Not available
Monitoring
Baseline Monitoring
Baseline INR (if co-administering warfarin)
Rationale: Aprepitant can cause a decrease in INR when co-administered with warfarin.
Timing: Before starting aprepitant
Routine Monitoring
INR (if co-administering warfarin)
Frequency: Monitor closely for 2 weeks after each cycle of aprepitant, and for 2 weeks after the last dose of aprepitant.
Target: Individualized therapeutic range for warfarin
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 back-up birth control methods.
Signs of hypersensitivity reactions
Frequency: During and after administration
Target: Not applicable
Action Threshold: Discontinue aprepitant and administer appropriate medical therapy if symptoms occur.
Symptom Monitoring
- Nausea
- Vomiting
- Signs of hypersensitivity (e.g., rash, pruritus, dyspnea, anaphylaxis)
- Signs of infection (due to potential interaction with chemotherapy)
Special Patient Groups
Pregnancy
Pregnancy Category B. Limited human data suggest no increased risk of major birth defects. Use during pregnancy only if clearly needed.
Trimester-Specific Risks:
First Trimester:
No increased risk observed in animal studies; human data limited.
Second Trimester:
No specific data suggesting increased risk.
Third Trimester:
No specific data suggesting increased risk.
Lactation
It is unknown if aprepitant is excreted in human milk. Aprepitant is excreted in rat milk. Due to the potential for serious adverse reactions in breastfed infants, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Infant Risk:
L3 (Moderately Safe - limited data, potential for minor adverse effects; caution advised).
Pediatric Use
Approved for CINV in children 6 months and older. Dosing is weight-based for younger children (oral suspension) and capsule for adolescents (>=12 years). Safety and effectiveness for PONV in pediatric patients have not been established.
Geriatric Use
No dose adjustment is necessary for elderly patients. Efficacy and safety profiles are similar to those in younger adults.
Clinical Information
Clinical Pearls
- Aprepitant is typically used as part of a multi-drug antiemetic regimen (e.g., with a 5-HT3 antagonist and a corticosteroid) for optimal control of chemotherapy-induced nausea and vomiting.
- The 80mg capsule is specifically for the Day 2 and Day 3 dosing in multi-day CINV regimens, following a 125mg dose on Day 1.
- Counsel patients thoroughly on the potential for drug interactions, especially with warfarin (INR monitoring) and hormonal contraceptives (need for backup birth control).
- Administer aprepitant orally without regard to food.
Alternative Therapies
- 5-HT3 receptor antagonists (e.g., Ondansetron, Granisetron, Palonosetron)
- Corticosteroids (e.g., Dexamethasone)
- Dopamine receptor antagonists (e.g., Prochlorperazine, Metoclopramide)
- Olanzapine (for refractory CINV)
Cost & Coverage
Average Cost:
$100 - $200 per 80mg capsule (estimated)
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 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 taken, the amount, and the time it happened.