aprepitant and dexamethasone-21-phosphate

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.

Topics: Antiemetics; Aprepitant; Dexamethasone; Drug Combinations; Drug Incompatibility; Drug Stability; Drug Storage; Glucocorticoids; Glucose; Infusions, Intravenous; Methylprednisolone Hemisuccinate; Morpholines; Serotonin 5-HT3 Receptor Antagonists; Sodium Chloride

One of the most common and distressing side effects for cancer patients is chemotherapy-induced nausea and vomiting (CINV). New antiemetics, such as the NK-1 receptor inhibitor aprepitant, have been reported to improve control of this side effect in adults. However, little is known about its effect in the pediatric oncology population, with only a few reported cases in the literature.. This was a retrospective chart review on the use of aprepitant in the pediatric oncology population in our institution.. Thirty-two charts and a total of 146 cycles of chemotherapy were reviewed. Mean age was 10 years. Highly emetogenic chemotherapy was used in 23/32 patients and moderately emetogenic chemotherapy in 9/32. Antiemetic regimens consisted of aprepitant+5-HT3 RA+dexamethasone (Regimen 1, 20/32 patients) or aprepitant +5-HT3 RA (Regimen 2, in 12/32). Eight out of thirty-two patients were chemotherapy-naïve and received aprepitant on their first cycle. In 24/32 patients, aprepitant was added later in their treatment, with 12/24 reporting resolution of CINV after its addition.. Aprepitant when combined with standard antiemetics, was well tolerated in the pediatric oncology population studied. However, there is still a need to conduct prospective studies to determine the optimal efficacy of aprepitant in the pediatric oncology population.

Topics: Adolescent; Antiemetics; Antineoplastic Combined Chemotherapy Protocols; Aprepitant; Child; Child, Preschool; Dexamethasone; Drug Therapy, Combination; Female; Glucocorticoids; Humans; Male; Morpholines; Nausea; Neoplasms; Retrospective Studies; Serotonin 5-HT3 Receptor Antagonists; Treatment Outcome; Vomiting