What happens if I overdose Fosaprepitant?
Contact 1-800-222-1222 (the American Association of Poison Control Centers), your local, or emergency room immediately. Symptoms may include drowsiness; headache.
Proper storage of Fosaprepitant:
Fosaprepitant is usually handled and stored by a health care provider. Keep Fosaprepitant out of the reach of children and away from pets.
Overdose of Fosaprepitant in details
There is no specific information on the treatment of overdosage with Fosaprepitant or aprepitant.
In the event of overdose, Fosaprepitant for Injection should be discontinued and general supportive treatment and monitoring should be provided. Because of the antiemetic activity of Fosaprepitant for Injection, drug-induced emesis may not be effective in cases of Fosaprepitant for Injection overdosage.
Aprepitant is not removed by hemodialysis.
What should I avoid while taking Fosaprepitant?
Follow your doctor's instructions about any restrictions on food, beverages, or activity.
Fosaprepitant warnings
Clinically Significant CYP3A4 Drug Interactions
Fosaprepitant, a prodrug of aprepitant, is a weak inhibitor of CYP3A4, and aprepitant is a substrate, inhibitor, and inducer of CYP3A4.
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- Use of Fosaprepitant for Injection with other drugs that are CYP3A4 substrates, may result in increased plasma concentration of the concomitant drug.
- o
- Use of pimozide with Fosaprepitant for Injection is contraindicated due to the risk of significantly increased plasma concentrations of pimozide, potentially resulting in prolongation of the QT interval, a known adverse reaction of pimozide.
- •
- Use of Fosaprepitant for Injection with strong or moderate CYP3A4 inhibitors (e.g., ketoconazole, diltiazem) may increase plasma concentrations of aprepitant and result in an increased risk of adverse reactions related to Fosaprepitant for Injection.
Use of Fosaprepitant for Injection with strong CYP3A4 inducers (e.g., rifampin) may result in a reduction in aprepitant plasma concentrations and decreased efficacy of Fosaprepitant for Injection.
Hypersensitivity Reactions
Serious hypersensitivity reactions, including anaphylaxis and anaphylactic shock, during or soon after infusion of Fosaprepitant have occurred. Symptoms including flushing, erythema, dyspnea, hypotension and syncope have been reported.
Monitor patients during and after infusion. If hypersensitivity reactions occur, discontinue the infusion and administer appropriate medical therapy. Do not reinitiate Fosaprepitant for Injection in patients who experience these symptoms with previous use.
Infusion Site Reactions
Infusion site reactions (ISRs) have been reported with the use of Fosaprepitant for Injection. The majority of severe ISRs, including thrombophlebitis and vasculitis, were reported with concomitant vesicant (anthracycline-based) chemotherapy administration, particularly when associated with extravasation. Necrosis was also reported in some patients with concomitant vesicant chemotherapy. Most ISRs occurred with the first, second or third exposure to single doses of Fosaprepitant for Injection and in some cases, reactions persisted for two weeks or longer. Treatment of severe ISRs consisted of medical, and in some cases surgical, intervention.
Avoid infusion of Fosaprepitant for Injection into small veins or through a butterfly catheter. If a severe ISR develops during infusion, discontinue the infusion and administer appropriate medical treatment.
Decrease in INR with Concomitant Warfarin
Coadministration of Fosaprepitant for Injection with warfarin, a CYP2C9 substrate, may result in a clinically significant decrease in the International Normalized Ratio (INR) of prothrombin time. Monitor the INR in patients on chronic warfarin therapy in the 2-week period, particularly at 7 to 10 days, following initiation of Fosaprepitant for Injection with each chemotherapy cycle.
Risk of Reduced Efficacy of Hormonal Contraceptives
Upon coadministration with Fosaprepitant for Injection, the efficacy of hormonal contraceptives may be reduced during administration of and for 28 days following the last dose of Fosaprepitant for Injection. Advise patients to use effective alternative or back-up methods of contraception during treatment with Fosaprepitant for Injection and for 1 month following administration of Fosaprepitant for Injection.
What should I discuss with my healthcare provider before taking Fosaprepitant?
You should not use this medication if you are allergic to Fosaprepitant, aprepitant (oral Emend), or polysorbate 80, or if you also take pimozide.
Using Fosaprepitant while you are also taking pimozide can cause unwanted or dangerous effects.
To make sure Fosaprepitant is safe for you, tell your doctor if you have liver disease.
FDA pregnancy category B. Fosaprepitant is not expected to harm an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment.
Fosaprepitant can make birth control pills less effective. This effect can last for up to 28 days after your last dose of Fosaprepitant. Ask your doctor about using non-hormonal birth control (condom, diaphragm with spermicide) to prevent pregnancy while you are receiving Fosaprepitant, and for at least 1 month after your treatment ends.
It is not known whether Fosaprepitant passes into breast milk or if it could harm a nursing baby. You should not breast-feed while using this medicine.
Fosaprepitant precautions
Clinically Significant CYP3A4 Drug Interactions
Fosaprepitant, a prodrug of aprepitant, is a weak inhibitor of CYP3A4, and aprepitant is a substrate, inhibitor, and inducer of CYP3A4.
- •
- Use of Fosaprepitant for Injection with other drugs that are CYP3A4 substrates, may result in increased plasma concentration of the concomitant drug.
- o
- Use of pimozide with Fosaprepitant for Injection is contraindicated due to the risk of significantly increased plasma concentrations of pimozide, potentially resulting in prolongation of the QT interval, a known adverse reaction of pimozide.
- •
- Use of Fosaprepitant for Injection with strong or moderate CYP3A4 inhibitors (e.g., ketoconazole, diltiazem) may increase plasma concentrations of aprepitant and result in an increased risk of adverse reactions related to Fosaprepitant for Injection.
Use of Fosaprepitant for Injection with strong CYP3A4 inducers (e.g., rifampin) may result in a reduction in aprepitant plasma concentrations and decreased efficacy of Fosaprepitant for Injection.
Hypersensitivity Reactions
Serious hypersensitivity reactions, including anaphylaxis and anaphylactic shock, during or soon after infusion of Fosaprepitant have occurred. Symptoms including flushing, erythema, dyspnea, hypotension and syncope have been reported.
Monitor patients during and after infusion. If hypersensitivity reactions occur, discontinue the infusion and administer appropriate medical therapy. Do not reinitiate Fosaprepitant for Injection in patients who experience these symptoms with previous use.
Infusion Site Reactions
Infusion site reactions (ISRs) have been reported with the use of Fosaprepitant for Injection. The majority of severe ISRs, including thrombophlebitis and vasculitis, were reported with concomitant vesicant (anthracycline-based) chemotherapy administration, particularly when associated with extravasation. Necrosis was also reported in some patients with concomitant vesicant chemotherapy. Most ISRs occurred with the first, second or third exposure to single doses of Fosaprepitant for Injection and in some cases, reactions persisted for two weeks or longer. Treatment of severe ISRs consisted of medical, and in some cases surgical, intervention.
Avoid infusion of Fosaprepitant for Injection into small veins or through a butterfly catheter. If a severe ISR develops during infusion, discontinue the infusion and administer appropriate medical treatment.
Decrease in INR with Concomitant Warfarin
Coadministration of Fosaprepitant for Injection with warfarin, a CYP2C9 substrate, may result in a clinically significant decrease in the International Normalized Ratio (INR) of prothrombin time. Monitor the INR in patients on chronic warfarin therapy in the 2-week period, particularly at 7 to 10 days, following initiation of Fosaprepitant for Injection with each chemotherapy cycle.
Risk of Reduced Efficacy of Hormonal Contraceptives
Upon coadministration with Fosaprepitant for Injection, the efficacy of hormonal contraceptives may be reduced during administration of and for 28 days following the last dose of Fosaprepitant for Injection. Advise patients to use effective alternative or back-up methods of contraception during treatment with Fosaprepitant for Injection and for 1 month following administration of Fosaprepitant for Injection.
What happens if I miss a dose of Fosaprepitant?
Since Fosaprepitant injection is given only once on the first day of your chemotherapy treatment, you are not likely to be on a dosing schedule.
References
- DailyMed. "FOSAPREPITANT DIMEGLUMINE: DailyMed provides trustworthy information about marketed drugs in the United States. DailyMed is the official provider of FDA label information (package inserts).". https://dailymed.nlm.nih.gov/dailyme... (accessed September 17, 2018).
- DrugBank. "Fosaprepitant". http://www.drugbank.ca/drugs/DB06717 (accessed September 17, 2018).
- MeSH. "Neurokinin-1 Receptor Antagonists". https://www.ncbi.nlm.nih.gov/mesh/68... (accessed September 17, 2018).
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Information checked by Dr. Sachin Kumar, MD Pharmacology
