Fosaprepitan 150mg Soln Inj, 1vial

Fosaprepitant is a prodrug of aprepitant. 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.

Serious Side Effects: Seek Medical Help Right Away

Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience 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
Tissue damage at the injection site, characterized by:
+ Redness
+ Burning
+ Pain
+ Swelling
+ Blisters
+ Skin sores
+ Leaking of fluid
Low blood cell counts, which can increase the risk of:
+ Infections (fever, chills, sore throat)
+ Bleeding problems (unexplained bruising or bleeding)
+ Anemia (feeling very tired or weak)

Other Possible Side Effects

Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms, 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 list is not exhaustive, and you may experience other 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.

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.
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.

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.

• Pimozide (due to potential for increased plasma concentrations of pimozide, leading to QT prolongation and serious adverse reactions)

• Warfarin (monitor INR closely, especially in the first 2 weeks after fosaprepitant administration, as aprepitant can decrease INR)
• Oral Contraceptives (reduced efficacy; advise alternative or backup contraception for 28 days after fosaprepitant administration)
• Corticosteroids (e.g., Dexamethasone, Methylprednisolone - aprepitant increases their plasma concentrations; reduce corticosteroid dose)
• CYP3A4 Substrates with narrow therapeutic index (e.g., Alfentanil, Fentanyl, Quinidine, Ergot Alkaloids like Ergotamine, Dihydroergotamine - monitor for increased toxicity)

• CYP3A4 Inducers (e.g., Rifampin, Phenytoin, Carbamazepine, Phenobarbital - may decrease aprepitant plasma concentrations)
• CYP3A4 Inhibitors (e.g., Ketoconazole, Itraconazole, Clarithromycin, Ritonavir, Diltiazem - may increase aprepitant plasma concentrations)
• Benzodiazepines (e.g., Midazolam, Alprazolam, Triazolam - monitor for increased sedation)
• Immunosuppressants (e.g., Cyclosporine, Tacrolimus, Sirolimus, Everolimus - monitor drug levels and for increased toxicity)

• Not specifically categorized as minor for fosaprepitant, but general caution with other drugs metabolized by CYP3A4.

• Nausea
• Vomiting
• Hiccups
• Fatigue
• Headache
• Constipation
• Dyspepsia
• Dizziness
• Injection site reactions

Limited data on fosaprepitant use in pregnant women are insufficient to inform a drug-associated risk of adverse developmental outcomes. Use only if the potential benefit justifies the potential risk to the fetus.

Aprepitant (the active moiety) is present in human milk. There are no data on the effects of aprepitant on the breastfed infant or on milk production. Advise women not to breastfeed during treatment and for 28 days after the last dose.

The 150 mg single dose of fosaprepitant is not indicated for pediatric patients. Fosaprepitant (Emend IV) is approved for pediatric patients 6 months and older for CINV, but dosing is weight-based (e.g., 3 mg/kg up to 150 mg).

No dose adjustment is necessary for elderly patients. However, elderly patients may be more susceptible to some adverse reactions. Monitor for age-related comorbidities and polypharmacy, especially regarding drug interactions.

• Fosaprepitant 150 mg is a convenient single-dose IV formulation for CINV prevention, eliminating the need for multi-day oral aprepitant.
• It is a prodrug that rapidly converts to aprepitant, the active NK1 receptor antagonist.
• Significant drug interactions occur due to aprepitant's effects on CYP3A4 (moderate inhibitor, weak inducer), requiring careful monitoring and potential dose adjustments for co-administered medications, especially warfarin, corticosteroids, and oral contraceptives.
• Administer as an IV infusion over 20-30 minutes; do not administer as a bolus.
• Always use in combination with a 5-HT3 antagonist and a corticosteroid for optimal CINV prevention.

• 5-HT3 receptor antagonists (e.g., Ondansetron, Palonosetron, Granisetron, Dolasetron)
• Corticosteroids (e.g., Dexamethasone)
• Olanzapine (for CINV)
• Dopamine receptor antagonists (e.g., Prochlorperazine, Metoclopramide - less common for CINV prophylaxis)

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; do not flush them down the toilet or pour them down the drain unless instructed to do so by a healthcare professional. 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 emergency medical attention. Be prepared to provide information about the medication taken, the quantity, and the time of ingestion.