Emend 80mg Capsules Bi-Fold Card
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
Sep 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 a natural substance in your body that causes these symptoms.
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. When taking the medication, swallow the tablet whole - do not chew, open, or crush it.
To store this medication properly, keep it at room temperature in a dry location, avoiding storage in a 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 storage in a 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 your chemotherapy treatment.
- Can be taken with or without food.
- Do not stop taking it early, even if you feel well, as it is designed to prevent delayed nausea and vomiting.
- If you are taking warfarin, your doctor will need to monitor your blood clotting (INR) more closely.
- If you are using birth control pills, use an additional non-hormonal method of contraception (like condoms) during treatment and for 28 days after your last dose, as aprepitant can make birth control pills less effective.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
For Chemotherapy-Induced Nausea and Vomiting (CINV): 125 mg orally on Day 1, followed by 80 mg orally once daily on Days 2 and 3. Administered 1 hour before chemotherapy on Day 1.
Dose Range:
80 - 125 mg
Condition-Specific Dosing:
Highly Emetogenic Chemotherapy (HEC):
125 mg on Day 1, then 80 mg on Days 2 and 3, as part of a multi-drug regimen (e.g., with a corticosteroid and a 5-HT3 antagonist).
Moderately Emetogenic Chemotherapy (MEC):
125 mg on Day 1, then 80 mg on Days 2 and 3, as part of a multi-drug regimen (e.g., with a corticosteroid and a 5-HT3 antagonist).
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
For CINV (ages 6 months to <12 years): 3 mg/kg (max 125 mg) on Day 1, then 2 mg/kg (max 80 mg) on Days 2 and 3. (Note: Oral suspension or IV formulation typically used for younger children).
Adolescent:
For CINV (ages 12 to 17 years): Same as adult dosing (125 mg on Day 1, then 80 mg on Days 2 and 3).
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:
Approximately 4 hours
FoodEffect:
No clinically significant effect on bioavailability when administered with food.
Distribution:
Vd:
Approximately 70 L
ProteinBinding:
Greater than 95%
CnssPenetration:
Yes (crosses blood-brain barrier)
Elimination:
HalfLife:
Approximately 9-13 hours
Clearance:
Approximately 6.7 L/hr (oral)
ExcretionRoute:
Primarily fecal (86%), minor renal (5%)
Unchanged:
Less than 1% (renal)
Pharmacodynamics
OnsetOfAction:
Rapid (within 1 hour for oral absorption)
PeakEffect:
Correlates with Tmax (approx. 4 hours)
DurationOfAction:
Sustained antiemetic effect for at least 24 hours due to long half-life and high receptor affinity.
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 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 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 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 or persistent hiccups
- Unusual fatigue or weakness
- Signs of an allergic reaction (rash, itching, swelling of face/tongue/throat, severe dizziness, trouble breathing)
- Signs of liver problems (yellowing of skin/eyes, dark urine, severe stomach pain)
- Any new or worsening symptoms that concern you.
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, that may interact with this medication. Certain medications used to treat conditions like HIV, infections, and seizures should not be taken with this drug.
* Please note that this is not an exhaustive list of all potential drug interactions or health problems that may affect the use of this medication.
To ensure your safety, it is crucial 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 to take this medication in combination with your other medications and health conditions. Never start, stop, or change 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, that may interact with this medication. Certain medications used to treat conditions like HIV, infections, and seizures should not be taken with this drug.
* Please note that this is not an exhaustive list of all potential drug interactions or health problems that may affect the use of this medication.
To ensure your safety, it is crucial 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 to take this medication in combination with your other medications and health conditions. Never start, stop, or change 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, 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. 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, 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:
- Limited experience with overdose. Symptoms may include drowsiness, headache, or other exaggerated side effects.
What to Do:
No specific antidote. Treatment should be symptomatic and supportive. Aprepitant is not removed by hemodialysis. Contact a poison control center or seek immediate medical attention. Call 1-800-222-1222.
Drug Interactions
Major Interactions
- Pimozide (increased QTc prolongation risk)
- Terfenadine (increased QTc prolongation risk)
- Astemizole (increased QTc prolongation risk)
- Cisapride (increased QTc prolongation risk)
Moderate Interactions
- Warfarin (decreased INR, especially in first 2 weeks after aprepitant initiation)
- Oral Contraceptives (reduced efficacy, use alternative contraception)
- Corticosteroids (e.g., Dexamethasone, Methylprednisolone - dose reduction may be needed)
- CYP3A4 substrates with narrow therapeutic index (e.g., Cyclosporine, Tacrolimus, Sirolimus, Everolimus, Alfentanil, Fentanyl, Quinidine, Ergot alkaloids)
- CYP3A4 inhibitors (e.g., Ketoconazole, Itraconazole, Clarithromycin, Ritonavir - may increase aprepitant levels)
- CYP3A4 inducers (e.g., Rifampin, Phenytoin, Carbamazepine, Phenobarbital - may decrease aprepitant levels)
Minor Interactions
- Diltiazem (increased aprepitant levels)
- Paroxetine (decreased aprepitant levels)
Monitoring
Baseline Monitoring
Concomitant Medications
Rationale: To identify potential drug-drug interactions, especially with CYP3A4 substrates, inhibitors, or inducers.
Timing: Prior to initiation of aprepitant.
Routine Monitoring
INR (International Normalized Ratio)
Frequency: Monitor closely for 2 weeks after initiation of aprepitant, especially if patient is on chronic warfarin therapy.
Target: Individualized based on warfarin indication.
Action Threshold: Significant deviation from target INR; adjust warfarin dose as needed.
Efficacy of Oral Contraceptives
Frequency: Ongoing
Target: Not applicable
Action Threshold: Advise patients to use alternative or backup contraception during and for 28 days after aprepitant treatment.
Adverse Reactions
Frequency: Daily during treatment course
Target: Not applicable
Action Threshold: Report any unusual or severe side effects (e.g., fatigue, hiccups, dyspepsia, constipation, headache).
Symptom Monitoring
- Nausea and vomiting control
- Fatigue
- Hiccups
- Dyspepsia
- Constipation
- Headache
- Dizziness
- Hypotension (rare)
- Hypersensitivity reactions (rash, pruritus, urticaria, angioedema - rare)
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 unknown if aprepitant is excreted in human milk. Caution should be exercised when aprepitant is administered to a nursing woman. The developmental and health benefits of breastfeeding should be considered along with the mother’s clinical need for aprepitant and any potential adverse effects on the breastfed infant from aprepitant or from the underlying maternal condition.
Infant Risk:
L3 (Moderately Safe - no human data, but low molecular weight and long half-life suggest potential for accumulation; however, high protein binding may limit transfer. Monitor infant for sedation or GI upset.)
Pediatric Use
Approved for CINV in children 6 months and older. Dosing is weight-based for younger children. Safety and efficacy in children younger than 6 months have not been established.
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 and potential interactions.
Clinical Information
Clinical Pearls
- Aprepitant is most effective when used as part of a multi-drug antiemetic regimen (e.g., with a 5-HT3 antagonist and a corticosteroid).
- It is particularly useful for preventing delayed CINV, which often occurs 24 hours or more after chemotherapy.
- Ensure patients understand the importance of using alternative contraception if on oral contraceptives due to potential interaction.
- Remind patients to complete the full 3-day course, even if they feel well after the first dose, to maximize protection against delayed emesis.
- Be vigilant for drug interactions, especially with warfarin and other CYP3A4 substrates with narrow therapeutic indices.
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)
- Cannabinoids (e.g., Dronabinol, Nabilone)
Cost & Coverage
Average Cost:
Varies widely, typically $100-$300 per 3-day course (1x125mg, 2x80mg)
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 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. If you have any questions or concerns about this medication, don't hesitate to discuss them with 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 information about what was taken, the amount, and the time it occurred.