Aprepitant 125mg Capsules
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
Mar 2003
DEA Schedule
Not Controlled
Overview
What is this medicine?
Aprepitant is a medicine used to prevent nausea and vomiting that can happen after chemotherapy. It works by blocking certain natural substances in your body 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 medication with or without food, but be sure to follow your doctor's specific guidance on this. Swallow the medication whole, without chewing, opening, or crushing 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, usually for 3 days around your chemotherapy treatment.
- Can be taken with or without food.
- Do not open, crush, or chew the capsule; swallow it whole.
- If you are taking warfarin, your doctor will need to check your blood clotting time (INR) more often.
- If you are using hormonal birth control (pills, patch, ring), use an alternative or back-up method of birth control during treatment and for 28 days after your last dose, as aprepitant can make hormonal birth control less effective.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
For highly emetogenic chemotherapy (HEC) or moderately emetogenic chemotherapy (MEC): 125 mg orally 1 hour before chemotherapy on Day 1, followed by 80 mg orally once daily in the morning on Days 2 and 3.
Dose Range:
80 - 125 mg
Condition-Specific Dosing:
HEC:
125 mg on Day 1, 80 mg on Days 2 and 3, in combination with a corticosteroid and a 5-HT3 antagonist.
MEC:
125 mg on Day 1, 80 mg on Days 2 and 3, in combination with a corticosteroid and a 5-HT3 antagonist.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Oral capsules not typically used; IV formulation (fosaprepitant) approved for children âĨ6 months for CINV. Oral aprepitant for children âĨ12 years for CINV: 125 mg on Day 1, 80 mg on Days 2 and 3.
Adolescent:
For CINV (âĨ12 years): 125 mg orally 1 hour before chemotherapy on Day 1, followed by 80 mg orally once daily in the morning on Days 2 and 3.
Dose Adjustments
Renal Impairment:
Mild:
No dosage adjustment necessary.
Moderate:
No dosage adjustment necessary.
Severe:
No dosage adjustment necessary (including end-stage renal disease requiring hemodialysis).
Dialysis:
No dosage adjustment necessary. Aprepitant is highly protein bound and not removed by hemodialysis.
Hepatic Impairment:
Mild:
No dosage adjustment necessary (Child-Pugh score 5-6).
Moderate:
No dosage adjustment necessary (Child-Pugh score 7-9).
Severe:
Use with caution; no clinical data available (Child-Pugh score >9).
Confidence:
Medium
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:
Food has no clinically meaningful effect on the bioavailability of aprepitant.
Distribution:
Vd:
Approximately 70 L
ProteinBinding:
>95%
CnssPenetration:
Limited (crosses blood-brain barrier but primarily acts peripherally for antiemetic effect)
Elimination:
HalfLife:
Approximately 9-13 hours
Clearance:
Not available (primarily metabolized)
ExcretionRoute:
Primarily fecal (86%), minor renal (5%)
Unchanged:
<1% in urine, <5% in feces
Pharmacodynamics
OnsetOfAction:
Within 1 hour (oral absorption)
PeakEffect:
Approximately 4 hours (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
+ 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 experience no side effects or only mild ones. If you experience any of the following side effects, or if they bother you or do not go away, contact your doctor:
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, 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
+ 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 experience no side effects or only mild ones. If you experience any of the following side effects, or if they bother you or do not go away, contact your doctor:
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, 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:
- Signs of an allergic reaction: rash, hives, itching, swelling of your face, lips, tongue, or throat, trouble breathing or swallowing.
- Severe dizziness or fainting.
- Unusual bleeding or bruising (if on warfarin).
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 symptoms you experienced.
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 issues that may interact with this drug.
To ensure your safety, it is vital to discuss all of your medications (prescription and OTC), natural products, vitamins, and health problems with your doctor and pharmacist. This will help determine whether it is safe for you to take this medication in conjunction with your other medications and health conditions. Never start, stop, or adjust the dosage 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 symptoms you experienced.
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 issues that may interact with this drug.
To ensure your safety, it is vital to discuss all of your medications (prescription and OTC), natural products, vitamins, and health problems with your doctor and pharmacist. This will help determine whether it is safe for you to take this medication in conjunction with your other medications and health conditions. Never start, stop, or adjust the dosage 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 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
- Hiccups
What to Do:
There is no specific antidote for aprepitant overdose. In case of overdose, discontinue aprepitant and provide general supportive care. Due to high protein binding, hemodialysis is unlikely to be an effective method for removal. Contact a poison control center immediately (e.g., 1-800-222-1222).
Drug Interactions
Contraindicated Interactions
- Pimozide
- Terfenadine
- Astemizole
- Cisapride
Major Interactions
- Warfarin (INR monitoring required)
- Oral contraceptives (reduced efficacy)
- Corticosteroids (e.g., dexamethasone, methylprednisolone - dose reduction needed)
- CYP3A4 substrates with narrow therapeutic index (e.g., cyclosporine, tacrolimus, sirolimus, everolimus, alfentanil, fentanyl, quinidine, irinotecan, ergot alkaloids)
- CYP3A4 inducers (e.g., rifampin, phenytoin, carbamazepine, phenobarbital - may reduce aprepitant efficacy)
- CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, nelfinavir - may increase aprepitant levels)
Moderate Interactions
- Benzodiazepines (e.g., midazolam, alprazolam - increased levels)
- Diltiazem
- Verapamil
- Paroxetine
- Tolbutamide
- Theophylline
Minor Interactions
- Not specifically identified as minor, but general caution with other CYP3A4 substrates/inhibitors/inducers.
Monitoring
Baseline Monitoring
Baseline INR (if on warfarin)
Rationale: Aprepitant can decrease INR in patients on chronic warfarin therapy.
Timing: Before initiation of aprepitant.
Routine Monitoring
INR (International Normalized Ratio)
Frequency: Monitor closely for 2 weeks after each 3-day aprepitant regimen, particularly at 7 to 10 days post-initiation.
Target: Individualized based on warfarin indication.
Action Threshold: Adjust warfarin dose as needed to maintain target INR.
Efficacy of oral contraceptives
Frequency: Throughout aprepitant therapy and for 28 days after the last dose.
Target: Not applicable
Action Threshold: Advise use of alternative or back-up birth control methods.
Signs and symptoms 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 and vomiting (for efficacy)
- Skin rash, itching, swelling of face/lips/tongue, difficulty breathing (signs of hypersensitivity)
- Dizziness, fatigue, headache, hiccups, constipation, diarrhea, dyspepsia, abdominal pain
Special Patient Groups
Pregnancy
Aprepitant is 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:
No increased risk of major birth defects observed in animal studies.
Second Trimester:
No increased risk of major birth defects observed in animal studies.
Third Trimester:
No increased risk of major birth defects observed in animal studies.
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. Consider the benefits of breastfeeding and the potential risks to the infant.
Infant Risk:
L3 (Moderate risk - limited human data, potential for adverse effects, but not severe; weigh benefits vs. risks).
Pediatric Use
Oral aprepitant capsules (125mg) are approved for adolescents âĨ12 years of age for CINV. For children 6 months to <12 years, the IV formulation (fosaprepitant) is approved for CINV. Safety and effectiveness in pediatric patients <6 months of age have not been established.
Geriatric Use
No dosage adjustment is necessary for elderly patients. However, elderly patients may be more susceptible to some adverse reactions. Monitor for adverse effects.
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 125mg capsule is specifically for CINV; a 40mg capsule or IV formulation is used for PONV.
- Be vigilant for drug interactions, especially with warfarin (monitor INR) and oral contraceptives (advise alternative contraception).
- Aprepitant's long half-life allows for once-daily dosing on Days 2 and 3, providing sustained NK1 receptor blockade.
Alternative Therapies
- 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:
$150 - $300 per 3-day regimen (1x125mg, 2x80mg)
Generic Available:
Yes
Insurance Coverage:
Tier 2 or Tier 3 (Specialty/Non-Preferred Brand, or Preferred Generic)
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 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 overdose, including the medication taken, the amount, and the time it occurred.