Fosaprepitant Dimeglumine (3 brand names, 3 dosage forms, 2 routes)
Available dosage forms: POWDER, UNKNOWN, SOLUTION.
Routes of administration: INTRAVENOUS, UNKNOWN.
Brand Names
- EMEND
- FOCINVEZ
- FOSAPREPITANT DIMEGLUMINE
Indications and Usage
Fosaprepitant for Injection, in combination with other antiemetic agents, is indicated in adults and pediatric patients 6 months of age and older for the prevention of: •acute and delayed nausea and vomiting associated with initial and repeat courses of highly emetogenic cancer chemotherapy (HEC) including high-dose cisplatin. •delayed nausea and vomiting associated with initial and repeat courses of moderately emetogenic cancer chemotherapy (MEC). Limitations of Use •Fosaprepitant for Injection has not been studied for the treatment of established nausea and vomiting.
Contraindications
Fosaprepitant for Injection is contraindicated in patients: •who are hypersensitive to any component of the product. Hypersensitivity reactions including anaphylactic reactions, flushing, erythema, and dyspnea have been reported [see Warnings and Precautions (5.2), Adverse Reactions (6.2)]. •taking pimozide. Inhibition of CYP3A4 by aprepitant, the active moiety, could result in elevated plasma concentrations of this drug, which is a CYP3A4 substrate, potentially causing serious or life-threatening reactions, such as QT prolongation, a known adverse reaction of pimozide [see Warnings and Precautions (5.1)].
Adverse Reactions
The following clinically significant adverse reactions are described elsewhere in the labeling: •Hypersensitivity Reactions [see Warnings and Precautions (5.2)] •Infusion Site Reactions [see Warnings and Precautions (5.3)]
Mechanism of Action
Fosaprepitant is a prodrug of aprepitant and accordingly, its antiemetic effects are attributable to aprepitant.Aprepitant is a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. Aprepitant has little or no affinity for serotonin (5-HT3), dopamine, and corticosteroid receptors, the targets of existing therapies for chemotherapy-induced nausea and vomiting (CINV). Aprepitant has been shown in animal models to inhibit emesis induced by cytotoxic chemotherapeutic agents, such as cisplatin, via central actions. Animal and human Positron Emission Tomography (PET) studies with aprepitant have shown that it crosses the blood brain barrier and occupies brain NK1 receptors. Animal and human studies have shown that aprepitant augments the antiemetic activity of the 5-HT3-receptor antagonist ondansetron and the corticosteroid dexamethasone and inhibits both the acute and delayed phases of cisplatin-induced emesis.
Overdosage
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.