Aprepitant 40mg 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
B
FDA Approved
Aug 2003
DEA Schedule
Not Controlled
Overview
What is this medicine?
Aprepitant is a medication used to prevent nausea and vomiting after surgery. It works by blocking certain natural substances in your body 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 place, 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 place, avoiding the bathroom. If you miss a dose, contact your doctor for advice on what to do next.
Lifestyle & Tips
- Take the capsule whole with or without food, as directed by your doctor, usually within 3 hours before your surgery.
- Do not crush, chew, or open the capsule.
- Report any persistent nausea, vomiting, or unusual side effects to your healthcare provider.
- If you are taking warfarin, you will need extra blood tests (INR) to monitor your blood clotting.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
40 mg orally as a single dose within 3 hours prior to induction of anesthesia
Dose Range:
40 - 40 mg
Condition-Specific Dosing:
Prevention of Postoperative Nausea and Vomiting (PONV):
40 mg orally as a single dose within 3 hours prior to induction of anesthesia.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established for PONV. For CINV, specific formulations and dosing exist for children âĨ6 months.
Adolescent:
Not established for PONV. For CINV, specific formulations and dosing exist for adolescents.
Dose Adjustments
Renal Impairment:
Mild:
No dose adjustment necessary.
Moderate:
No dose adjustment necessary.
Severe:
No dose adjustment necessary (including end-stage renal disease requiring hemodialysis).
Dialysis:
No dose adjustment necessary for patients on hemodialysis. Aprepitant is not removed by hemodialysis.
Hepatic Impairment:
Mild:
No dose adjustment necessary (Child-Pugh score 5-6).
Moderate:
No dose adjustment necessary (Child-Pugh score 7-9).
Severe:
Not studied. Avoid use in 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 emesis induced by chemotherapy or surgery.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 60-65% (for 80mg/125mg doses, similar for 40mg)
Tmax:
Approximately 4 hours
FoodEffect:
No clinically significant effect on AUC when administered with a standard breakfast.
Distribution:
Vd:
Approximately 70 L
ProteinBinding:
>95%
CnssPenetration:
Yes (crosses blood-brain barrier)
Elimination:
HalfLife:
Approximately 9-13 hours
Clearance:
Approximately 67-84 mL/min
ExcretionRoute:
Primarily fecal (approximately 86%), renally (approximately 14%)
Unchanged:
<1% in urine
Pharmacodynamics
OnsetOfAction:
Within 1 hour (based on receptor occupancy)
PeakEffect:
Approximately 4 hours (Tmax)
DurationOfAction:
Up to 24 hours (single dose for PONV)
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), including:
+ 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, including:
+ 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 any other unusual symptoms, contact your doctor or seek medical help if they bother you or do not go away:
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), including:
+ 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, including:
+ 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 any other unusual symptoms, contact your doctor or seek medical help if they bother you or do not go away:
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:
- Severe dizziness or fainting
- Unusual bleeding or bruising (if on warfarin)
- Signs of an allergic reaction (e.g., rash, itching, swelling, severe dizziness, trouble breathing)
- Persistent or worsening nausea/vomiting despite medication
Before Using This Medicine
Before taking this medication, it is essential to inform your doctor about the following:
Any allergies you have, including allergies to this drug, any of its components, or other substances, such as foods or medications. Be sure to describe the symptoms you experienced as a result of the allergy.
Any medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins, as some of these may interact with this medication. Specifically, certain medications used to treat HIV, infections, seizures, and other conditions should not be taken with this drug.
* It is crucial to note that this is not an exhaustive list of all potential drug interactions or health problems that may affect the safety of taking this medication.
To ensure your safety, it is vital to provide your doctor and pharmacist with a comprehensive list of all your medications (prescription and OTC), natural products, vitamins, and health problems. This will enable them to assess 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.
Any allergies you have, including allergies to this drug, any of its components, or other substances, such as foods or medications. Be sure to describe the symptoms you experienced as a result of the allergy.
Any medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins, as some of these may interact with this medication. Specifically, certain medications used to treat HIV, infections, seizures, and other conditions should not be taken with this drug.
* It is crucial to note that this is not an exhaustive list of all potential drug interactions or health problems that may affect the safety of taking this medication.
To ensure your safety, it is vital to provide your doctor and pharmacist with a comprehensive list of all your medications (prescription and OTC), natural products, vitamins, and health problems. This will enable them to assess 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 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. Symptoms may include drowsiness, headache, and fatigue.
What to Do:
There is no specific antidote for aprepitant overdose. In case of suspected overdose, discontinue the drug and provide supportive care. Due to high protein binding, hemodialysis is unlikely to be effective. Call 1-800-222-1222 (Poison Control Center) for further guidance.
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)
- Midazolam (oral)
- Fentanyl
- Alfentanil
- Ergot alkaloids (e.g., Ergotamine, Dihydroergotamine)
- Immunosuppressants (e.g., Cyclosporine, Tacrolimus, Sirolimus, Everolimus)
- CYP3A4 substrates with narrow therapeutic index (e.g., Quinidine, Irinotecan, Vinca alkaloids)
Moderate Interactions
- Calcium channel blockers (e.g., Diltiazem, Verapamil)
- Statins (e.g., Simvastatin, Lovastatin)
- Phenytoin
- Carbamazepine
- Rifampin
- Phenobarbital
- St. John's Wort
- Paroxetine
Minor Interactions
- Not specifically identified as minor, but caution with any CYP3A4 substrate/inducer.
Monitoring
Baseline Monitoring
Patient history for drug interactions
Rationale: Aprepitant is a CYP3A4 modulator, requiring careful review of concomitant medications.
Timing: Prior to administration
Routine Monitoring
Efficacy (absence of nausea/vomiting)
Frequency: Post-operatively, as needed
Target: No nausea or vomiting
Action Threshold: Persistent nausea/vomiting may require additional antiemetic therapy.
Adverse effects (e.g., fatigue, dizziness, constipation, headache)
Frequency: Post-operatively, as needed
Target: Absence or mild, tolerable symptoms
Action Threshold: Severe or persistent adverse effects may require symptomatic treatment or re-evaluation.
INR (for patients on warfarin)
Frequency: Closely monitor for 2 weeks after each single dose or 7 days after the last dose of a multi-day regimen.
Target: Individualized therapeutic range
Action Threshold: Significant deviation from target INR may require warfarin dose adjustment.
Symptom Monitoring
- Nausea
- Vomiting
- Headache
- Fatigue
- Dizziness
- Constipation
- Diarrhea
- Dyspepsia
- Hiccups
- Hypotension
- Bradycardia
- Rash
- Pruritus
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 into breast milk in rats. It is unknown if it is excreted in human milk. The decision to discontinue breastfeeding or discontinue the drug should consider the importance of the drug to the mother and the potential risks to the infant. Lactation risk is L3 (Moderately Safe).
Infant Risk:
Potential for adverse effects on the breastfed infant is unknown. Monitor for drowsiness, poor feeding, or other adverse effects.
Pediatric Use
Safety and effectiveness of Aprepitant 40mg for PONV have not been established in pediatric patients under 18 years of age. For CINV, specific formulations and dosing are approved for children âĨ6 months.
Geriatric Use
No dose adjustment is necessary based on age. Efficacy and safety profiles are generally similar to younger adults, but elderly patients may be more sensitive to drug effects and potential interactions.
Clinical Information
Clinical Pearls
- Aprepitant 40mg is a single-dose regimen specifically for the prevention of PONV, administered pre-operatively.
- It is a moderate inhibitor of CYP3A4 and a mild inducer of CYP3A4, CYP2C9, and P-glycoprotein, leading to significant drug interactions.
- Crucial to review all concomitant medications, especially warfarin, oral contraceptives, and corticosteroids, due to potential for altered efficacy or toxicity.
- For patients on warfarin, close INR monitoring is essential for up to 2 weeks after aprepitant administration.
- Aprepitant does not treat existing nausea/vomiting; it is for prevention.
Alternative Therapies
- 5-HT3 receptor antagonists (e.g., Ondansetron, Granisetron, Palonosetron)
- Corticosteroids (e.g., Dexamethasone)
- Dopamine receptor antagonists (e.g., Prochlorperazine, Metoclopramide)
- Antihistamines (e.g., Promethazine)
- Anticholinergics (e.g., Scopolamine patch)
Cost & Coverage
Average Cost:
Varies widely, typically $50-$150 per 40mg capsule (single dose)
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (often covered for approved indications)
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.