Fosaprepitan 150mg Soln Inj, 1 Vial
It is used to prevent upset stomach and throwing up from chemo.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Antiemetic
Pharmacologic Class
Neurokinin-1 (NK1) Receptor Antagonist
Pregnancy Category
Category B
FDA Approved
Jan 2008
DEA Schedule
Not Controlled
Overview
What is this medicine?
Fosaprepitant is a medicine given by injection to help prevent nausea and vomiting, especially after chemotherapy or surgery. It works by blocking a natural substance in your body that causes these symptoms.
How to Use This Medicine
To use this medication correctly, follow your doctor's instructions and carefully read all accompanying information. Take this medication exactly as directed, and adhere to all guidelines provided. This drug is administered via infusion into a vein over a specified period of time.
For storage and disposal, consult with your doctor, nurse, or pharmacist to determine the best approach if you need to keep this medication at home.
If you miss a dose, contact your doctor immediately to receive guidance on the appropriate course of action.
For storage and disposal, consult with your doctor, nurse, or pharmacist to determine the best approach if you need to keep this medication at home.
If you miss a dose, contact your doctor immediately to receive guidance on the appropriate course of action.
Lifestyle & Tips
- Report any unusual bleeding or bruising, especially if taking warfarin.
- If using hormonal birth control, use an alternative or back-up method for at least 28 days after receiving this injection, as its effectiveness may be reduced.
- Stay hydrated as advised by your healthcare provider.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
150 mg IV as a single dose
Dose Range:
150 - 150 mg
Condition-Specific Dosing:
chemotherapyInducedNauseaAndVomiting(CINV):
150 mg IV infused over 20-30 minutes on Day 1, approximately 30 minutes prior to chemotherapy. Used in combination with a corticosteroid (e.g., dexamethasone) and a 5-HT3 antagonist.
postoperativeNauseaAndVomiting(PONV):
150 mg IV infused over 20-30 minutes within 30 minutes before induction of anesthesia.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established for infants <6 months of age. For CINV in infants 6 months to <2 years: 5 mg/kg IV (max 150 mg) on Day 1.
Child:
For CINV in children 2 to <12 years: 5 mg/kg IV (max 150 mg) on Day 1. For CINV in children 12 to <18 years: 150 mg IV on Day 1.
Adolescent:
For CINV in adolescents 12 to <18 years: 150 mg IV on Day 1.
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. Fosaprepitant 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:
Use with caution; no clinical data available (Child-Pugh score >9).
Confidence:
Medium
Pharmacology
Mechanism of Action
Fosaprepitant is a prodrug of aprepitant. It is rapidly converted to aprepitant in vivo. 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:
Not applicable (IV administration); aprepitant oral bioavailability is ~60-65%.
Tmax:
Aprepitant Tmax is approximately 3 hours after the start of a 30-minute IV infusion of fosaprepitant.
FoodEffect:
Not applicable (IV administration).
Distribution:
Vd:
Aprepitant: Approximately 70 L at steady state.
ProteinBinding:
Aprepitant: >95% bound to plasma proteins.
CnssPenetration:
Limited (aprepitant crosses the blood-brain barrier but does not occupy a significant number of brain NK1 receptors).
Elimination:
HalfLife:
Aprepitant: Approximately 9-13 hours.
Clearance:
Aprepitant: Approximately 67 to 84 mL/min.
ExcretionRoute:
Aprepitant: Primarily fecal (approximately 57%), with a minor amount excreted in urine (approximately 5%).
Unchanged:
Less than 1% of aprepitant is excreted unchanged in urine.
Pharmacodynamics
OnsetOfAction:
Rapid conversion to aprepitant, antiemetic effect begins shortly after administration.
PeakEffect:
Peak plasma concentration of aprepitant reached approximately 3 hours post-infusion.
DurationOfAction:
Antiemetic effect lasts for at least 24 hours, covering both acute and delayed phases of emesis.
Safety & Warnings
Side Effects
Serious 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 medical attention immediately:
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 urinary tract infection (UTI), including:
+ Blood in the urine
+ Burning or pain when passing urine
+ Frequent or urgent need to urinate
+ Fever
+ Lower stomach pain
+ Pelvic pain
Flushing
Dizziness or fainting
Fast or abnormal heartbeat
Burning, numbness, or tingling sensations that are not normal
If the medication leaks from the vein, it can cause tissue damage. Inform your nurse immediately if you experience:
+ Redness
+ Burning
+ Pain
+ Swelling
+ Blisters
+ Skin sores
+ Leaking of fluid at the injection site
Low blood cell counts can occur with this medication, which may lead to:
+ Bleeding problems
+ Infections
+ Anemia
+ If you experience signs of infection, such as fever, chills, or sore throat, or notice any unexplained bruising or bleeding, or feel extremely tired or weak, contact your doctor right away
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people may not experience any side effects or only have mild ones. If you are bothered by any of the following side effects or if they do not go away, contact your doctor or seek medical attention:
Feeling tired or weak
Stomach pain or diarrhea
Heartburn
Pain in arms or legs
Reporting Side Effects
This is not an exhaustive list of all 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 medical attention immediately:
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 urinary tract infection (UTI), including:
+ Blood in the urine
+ Burning or pain when passing urine
+ Frequent or urgent need to urinate
+ Fever
+ Lower stomach pain
+ Pelvic pain
Flushing
Dizziness or fainting
Fast or abnormal heartbeat
Burning, numbness, or tingling sensations that are not normal
If the medication leaks from the vein, it can cause tissue damage. Inform your nurse immediately if you experience:
+ Redness
+ Burning
+ Pain
+ Swelling
+ Blisters
+ Skin sores
+ Leaking of fluid at the injection site
Low blood cell counts can occur with this medication, which may lead to:
+ Bleeding problems
+ Infections
+ Anemia
+ If you experience signs of infection, such as fever, chills, or sore throat, or notice any unexplained bruising or bleeding, or feel extremely tired or weak, contact your doctor right away
Other Possible Side Effects
Like all medications, this drug can cause side effects. Many people may not experience any side effects or only have mild ones. If you are bothered by any of the following side effects or if they do not go away, contact your doctor or seek medical attention:
Feeling tired or weak
Stomach pain or diarrhea
Heartburn
Pain in arms or legs
Reporting Side Effects
This is not an exhaustive list of all 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 injection site reactions (pain, redness, swelling, blistering)
- Signs of allergic reaction (rash, itching, swelling of face/tongue/throat, severe dizziness, trouble breathing)
- Unusual bleeding or bruising (if on warfarin)
- Persistent or worsening nausea/vomiting despite treatment
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.
All 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 potential drug interactions or health problems that may affect the safety of this medication.
To ensure your safety, it is vital to discuss all of your medications and health conditions 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 modify 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 allergic reaction you experienced, including any symptoms that occurred.
All 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 potential drug interactions or health problems that may affect the safety of this medication.
To ensure your safety, it is vital to discuss all of your medications and health conditions 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 modify 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, or fatigue.
What to Do:
No specific antidote. Treatment should be symptomatic and supportive. Discontinue the drug and monitor the patient. Due to high protein binding, dialysis is unlikely to be an effective treatment for overdose. Call 1-800-222-1222 (Poison Control).
Drug Interactions
Contraindicated Interactions
- Pimozide
- Terfenadine
- Astemizole
- Cisapride
Major Interactions
- Warfarin (increased INR, monitor closely)
- Oral contraceptives (reduced efficacy, use alternative contraception)
- Corticosteroids (e.g., Dexamethasone, Methylprednisolone - dose reduction required)
- CYP3A4 substrates with narrow therapeutic index (e.g., Alfentanil, Cyclosporine, Everolimus, Fentanyl, Sirolimus, Tacrolimus, Quinidine, Ergot alkaloids)
Moderate Interactions
- CYP3A4 inducers (e.g., Rifampin, Phenytoin, Carbamazepine, Phenobarbital - may decrease aprepitant levels)
- CYP3A4 inhibitors (e.g., Ketoconazole, Itraconazole, Clarithromycin, Ritonavir, Nefazodone - may increase aprepitant levels)
- Diltiazem (increased aprepitant levels)
- Midazolam (increased midazolam levels)
Minor Interactions
- Tolbutamide (weak induction of CYP2C9)
Monitoring
Routine Monitoring
INR (International Normalized Ratio)
Frequency: Monitor for several weeks after administration
Target: Therapeutic range for patient's indication
Action Threshold: Significant increase above target range; adjust warfarin dose as needed.
Efficacy of oral contraceptives
Frequency: Throughout treatment cycle
Target: Not applicable
Action Threshold: Consider alternative or back-up contraception for 28 days after fosaprepitant administration.
Adverse effects (e.g., fatigue, hiccups, dyspepsia, constipation, injection site reactions)
Frequency: Regularly during and after administration
Target: Not applicable
Action Threshold: Manage symptoms as appropriate; consider discontinuation if severe.
Symptom Monitoring
- Nausea
- Vomiting
- Fatigue
- Hiccups
- Dyspepsia
- Constipation
- Headache
- Dizziness
- Injection site reactions (pain, erythema, swelling)
Special Patient Groups
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 and potential benefits outweigh potential risks.
Trimester-Specific Risks:
First Trimester:
No specific increased risk identified in animal studies.
Second Trimester:
No specific increased risk identified in animal studies.
Third Trimester:
No specific increased risk identified in animal studies.
Lactation
Aprepitant (the active metabolite) is excreted in breast milk. Caution should be exercised when fosaprepitant is administered to a nursing woman. Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for fosaprepitant and any potential adverse effects on the breastfed infant from fosaprepitant or from the underlying maternal condition.
Infant Risk:
L3 (Moderately safe - limited data, potential for mild non-serious adverse effects).
Pediatric Use
Approved for CINV in children 6 months and older. Dosing is weight-based. Safety and effectiveness for PONV in pediatric patients have not been established.
Geriatric Use
No dose adjustment is necessary based on age. Clinical studies did not show differences in efficacy or safety between elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out. Monitor for adverse effects.
Clinical Information
Clinical Pearls
- Fosaprepitant is a prodrug of aprepitant, offering an IV option for NK1 receptor antagonism.
- Must be administered as an intravenous infusion over 20-30 minutes, not as a bolus.
- Always check compatibility with other IV fluids and medications before mixing or co-administering.
- Crucial for preventing delayed CINV, often used in combination with a 5-HT3 antagonist and a corticosteroid.
- Patients on warfarin require close INR monitoring for several weeks due to potential interaction.
- Advise patients using hormonal contraceptives to use an alternative method for 28 days after administration.
Alternative Therapies
- Ondansetron (5-HT3 receptor antagonist)
- Palonosetron (5-HT3 receptor antagonist)
- Granisetron (5-HT3 receptor antagonist)
- Dexamethasone (corticosteroid)
- Olanzapine (atypical antipsychotic with antiemetic properties)
- Aprepitant (oral NK1 receptor antagonist)
Cost & Coverage
Average Cost:
Varies, typically $400-$600 per 150mg vial
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (Specialty/Non-preferred Brand, but often covered for CINV/PONV)
General Drug Facts
If your symptoms or health problems persist or worsen, it is essential to contact your doctor promptly. To ensure safe use, never share your medication with others, and do not take medication prescribed for someone else. Store all medications in a secure location, out of reach of children and pets, to prevent accidental ingestion. Dispose of unused or expired medications properly. Unless instructed to do so by a healthcare professional, do not flush medications down the toilet or drain. If you are unsure about the proper disposal method, consult your pharmacist, who can also inform you about potential drug take-back programs in your area. Some medications may come with an additional patient information leaflet, which your pharmacist can provide. If you have any questions or concerns about your medication, discuss them with your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately contact your local poison control center or seek medical attention. Be prepared to provide information about the medication taken, the quantity, and the time of the incident.