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Compatibility of intravenous fosaprepitant with intravenous 5-HT3 antagonists and corticosteroids.

Cancer chemotherapy and pharmacology (2013-07-19)
Susan Sun, Joseph Schaller, Jiri Placek, Brett Duersch
ABSTRACT

Fosaprepitant dimeglumine for injection is the water-soluble phosphorylated prodrug of the neurokinin-1 receptor antagonist aprepitant. Both agents are approved (in combination with a 5-HT3 antagonist and a corticosteroid) for prevention of chemotherapy-induced nausea and vomiting. Because fosaprepitant is likely to be combined and stored in the same intravenous (IV) bag with 5-HT3 antagonists and corticosteroids, the in vitro compatibility of fosaprepitant with these agents and other IV diluents was assessed. Fosaprepitant (1 mg/mL in 0.9 % sodium chloride injection solution) was combined in binary or tertiary fashion with therapeutic-dose preparations of a 5-HT3 antagonist (ondansetron, granisetron, palonosetron, or tropisetron) and/or a corticosteroid (dexamethasone sodium phosphate or methylprednisolone sodium succinate). For diluent compatibility assessment, fosaprepitant was also prepared 1 mg/mL in 0.9 % sodium chloride injection solution, water for injection, or 5 % dextrose injection solution. After 24-h storage under ambient conditions, samples were assayed for degradation. Fosaprepitant demonstrated compatibility when combined in the same IV infusion bag with common 5-HT3 antagonists and corticosteroids for storage and IV coadministration, with the exception of palonosetron (incompatible under all experimental conditions) and tropisetron (incompatible unless combined with a corticosteroid). No incompatibility was observed between fosaprepitant and any of the 3 diluents tested. Use of fosaprepitant in combination with other antiemetics may provide a flexible option for administration of antiemetics to patients receiving moderately or highly emetogenic chemotherapy.

MATERIALS
Product Number
Brand
Product Description

Dexamethasone sodium phosphate, European Pharmacopoeia (EP) Reference Standard
Methylprednisolone hydrogen succinate, European Pharmacopoeia (EP) Reference Standard
Methylprednisolone hydrogen succinate for performance test, European Pharmacopoeia (EP) Reference Standard
USP
Methylprednisolone hemisuccinate, United States Pharmacopeia (USP) Reference Standard
Sigma-Aldrich
Dexamethasone 21-phosphate disodium salt, ≥98%