Emend 125mg For Oral Suspension
It is used to prevent upset stomach and throwing up.
Drug Class
Antiemetic
Pharmacologic Class
Neurokinin-1 (NK1) Receptor Antagonist
Pregnancy Category
Not available
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 these symptoms.
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. The medication will be prepared by a healthcare professional, such as a doctor or pharmacist. When you're ready to take it, place the pre-filled device against the inside of your cheek and slowly release the medication into your mouth.
To store this medication, keep it in the refrigerator at all times. Do not allow it to freeze. If you miss a dose, contact your doctor immediately to determine the best course of action.
To store this medication, keep it in the refrigerator at all times. Do not allow it to freeze. If you miss a dose, contact your doctor immediately to determine the best course of action.
Lifestyle & Tips
- Take exactly as prescribed by your doctor.
- Do not take more or less than directed.
- This medication is usually given with other anti-nausea medicines (like corticosteroids and 5-HT3 blockers) for best effect.
- For oral suspension, ensure proper mixing and administration. Follow instructions carefully for measuring the dose.
- Report any unusual or severe side effects to your doctor immediately.
Available Forms & Alternatives
Dosing & Administration
Adult Dosing
Standard Dose:
For CINV (HEC): 125 mg on Day 1, then 80 mg on Days 2 and 3 (capsules). For CINV (MEC): 125 mg on Day 1. For PONV: 125 mg as a single dose within 3 hours prior to induction of anesthesia.
Dose Range:
40 - 125 mg
Condition-Specific Dosing:
Chemotherapy-Induced Nausea and Vomiting (CINV) - Highly Emetogenic Chemotherapy (HEC):
125 mg oral suspension on Day 1, followed by 80 mg oral capsules on Days 2 and 3 (as part of a multi-day regimen).
Chemotherapy-Induced Nausea and Vomiting (CINV) - Moderately Emetogenic Chemotherapy (MEC):
125 mg oral suspension as a single dose on Day 1.
Postoperative Nausea and Vomiting (PONV):
125 mg oral suspension as a single dose within 3 hours prior to induction of anesthesia.
Pediatric Dosing
Neonatal:
Not established
Infant:
For CINV (6 months to <12 years or <30 kg): 3 mg/kg (max 125 mg) on Day 1, then 2 mg/kg (max 80 mg) on Days 2 and 3. Administer 30 minutes prior to chemotherapy.
Child:
For CINV (6 months to <12 years or <30 kg): 3 mg/kg (max 125 mg) on Day 1, then 2 mg/kg (max 80 mg) on Days 2 and 3. Administer 30 minutes prior to chemotherapy.
Adolescent:
For CINV (12 years and older or >=30 kg): Same as adult dosing (125 mg on Day 1, then 80 mg on Days 2 and 3 for HEC; 125 mg single dose for MEC). Administer 30 minutes prior to chemotherapy.
Dose Adjustments
Renal Impairment:
Mild:
No dosage adjustment necessary.
Moderate:
No dosage adjustment necessary.
Severe:
No dosage adjustment necessary.
Dialysis:
No dosage adjustment necessary. Aprepitant is 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:
No clinical experience; use with caution (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. It also inhibits nausea and vomiting associated with surgery.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 59-69% (oral capsule), oral suspension bioavailability is comparable.
Tmax:
Approximately 4 hours.
FoodEffect:
Food has no clinically meaningful effect on the bioavailability of aprepitant.
Distribution:
Vd:
Approximately 70 L (steady state).
ProteinBinding:
>95% (primarily to albumin and alpha1-acid glycoprotein).
CnssPenetration:
Limited (crosses blood-brain barrier but saturates NK1 receptors in the brain).
Elimination:
HalfLife:
Approximately 9-13 hours (terminal half-life).
Clearance:
Approximately 62 to 84 mL/min (plasma clearance).
ExcretionRoute:
Primarily fecal (approximately 57%), renal (approximately 5%).
Unchanged:
Less than 1% of the dose is excreted unchanged in urine.
Pharmacodynamics
OnsetOfAction:
Within 1 hour (for antiemetic effect, typically given prior to emetogenic stimuli).
PeakEffect:
Not directly applicable as an acute effect, but plasma concentrations peak around 4 hours.
DurationOfAction:
Antiemetic effect lasts for approximately 24 hours or longer due to slow dissociation from NK1 receptors and long half-life.
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 symptoms that concern you or do not go away, contact your doctor or seek medical help:
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 symptoms that concern you or do not go away, contact your doctor or seek medical help:
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 lightheadedness
- Unusual bleeding or bruising (especially if on warfarin)
- Signs of infection (fever, chills, sore throat)
- Severe skin reactions (rash, itching, hives, swelling of face/lips/tongue)
- Difficulty breathing or swallowing
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 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
* Any health problems you are experiencing
Before starting, stopping, or changing the dose of any medication, including this one, consult with your doctor to confirm that it is safe to do so in conjunction with your other medications and health conditions.
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 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
* Any health problems you are experiencing
Before starting, stopping, or changing the dose of any medication, including this one, 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
- Fatigue
What to Do:
There is no specific antidote for aprepitant overdose. In case of overdose, discontinue Emend and provide general supportive care and monitoring. Due to high protein binding, hemodialysis is unlikely to be an effective method for removal. Call 1-800-222-1222 (Poison Control).
Drug Interactions
Contraindicated Interactions
- Pimozide
- Terfenadine
- Astemizole
- Cisapride
Major Interactions
- Warfarin (monitor INR)
- Oral Contraceptives (reduced efficacy)
- Corticosteroids (e.g., Dexamethasone, Methylprednisolone - dose reduction may be needed)
- Benzodiazepines (e.g., Midazolam, Alprazolam - dose reduction may be needed)
- Immunosuppressants (e.g., Cyclosporine, Tacrolimus, Sirolimus, Everolimus - monitor levels)
- CYP3A4 substrates with narrow therapeutic index (e.g., Fentanyl, Alfentanil, Quinidine, Ergot alkaloids)
Moderate Interactions
- Calcium Channel Blockers (e.g., Diltiazem, Verapamil)
- Statins (e.g., Simvastatin, Lovastatin)
- Antifungals (e.g., Ketoconazole, Itraconazole - strong CYP3A4 inhibitors increase aprepitant levels)
- Macrolide Antibiotics (e.g., Clarithromycin, Erythromycin - strong CYP3A4 inhibitors increase aprepitant levels)
- HIV Protease Inhibitors (e.g., Ritonavir, Indinavir - strong CYP3A4 inhibitors increase aprepitant levels)
- Phenytoin, Carbamazepine, Rifampin (CYP3A4 inducers decrease aprepitant levels)
Minor Interactions
- Paroxetine (weak CYP2D6 inhibition by aprepitant)
Monitoring
Baseline Monitoring
Baseline INR (for patients on warfarin)
Rationale: Aprepitant can significantly decrease INR in patients on chronic warfarin therapy.
Timing: Prior to initiation of aprepitant.
Routine Monitoring
INR (International Normalized Ratio)
Frequency: Closely monitor for 2 weeks following each 3-day regimen of aprepitant, particularly on Days 7 to 10.
Target: Therapeutic range for warfarin.
Action Threshold: Adjust warfarin dose as needed to maintain target INR.
Efficacy (nausea and vomiting control)
Frequency: Daily during chemotherapy cycles and post-operative period.
Target: Absence or significant reduction of nausea and vomiting.
Action Threshold: Consider alternative or additional antiemetics if control is inadequate.
Adverse effects (e.g., fatigue, hiccups, constipation, headache)
Frequency: Regularly during treatment.
Target: Not applicable.
Action Threshold: Manage symptoms, consider dose adjustment or discontinuation if severe.
Symptom Monitoring
- Nausea
- Vomiting
- Hiccups
- Fatigue
- Constipation
- Headache
- Dizziness
- Dyspepsia
- Abdominal pain
- Changes in bowel habits
- Signs of infection (e.g., fever, chills) due to potential neutropenia
Special Patient Groups
Pregnancy
Limited data on aprepitant use in pregnant women are insufficient to inform a drug-associated risk for major birth defects and miscarriage. Use only if the potential benefit justifies the potential risk to the fetus.
Trimester-Specific Risks:
First Trimester:
Limited human data, animal studies show no direct harm but some developmental effects at high doses.
Second Trimester:
Limited human data.
Third Trimester:
Limited human data.
Lactation
Aprepitant is excreted in human 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 (Moderate risk - possible hazard to infant; weigh risk vs. benefit).
Pediatric Use
Approved for CINV in pediatric patients 6 months of age and older. Dosing is weight-based for younger children. Safety and effectiveness for PONV in pediatric patients have not been established.
Geriatric Use
No dosage 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, typically with a 5-HT3 antagonist and a corticosteroid.
- The oral suspension formulation is particularly useful for pediatric patients or adults who have difficulty swallowing capsules.
- Careful monitoring of INR is crucial for patients on warfarin due to significant drug interaction.
- Advise patients using hormonal contraceptives to use an alternative or backup method of contraception during and for 28 days after the last dose of aprepitant.
- Aprepitant can cause hiccups, which are generally mild to moderate and self-limiting.
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:
Varies widely, typically high per 125mg oral suspension
Generic Available:
Yes
Insurance Coverage:
Tier 3 or Specialty Tier (requires prior authorization)
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 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 details about the medication taken, the amount, and the time it occurred.