Skip to main content
Erschienen in: Cancer Chemotherapy and Pharmacology 3/2013

01.09.2013 | Original Article

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

verfasst von: Susan Sun, Joseph Schaller, Jiri Placek, Brett Duersch

Erschienen in: Cancer Chemotherapy and Pharmacology | Ausgabe 3/2013

Einloggen, um Zugang zu erhalten

Abstract

Purpose

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.

Methods

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.

Results

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.

Conclusions

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.
Literatur
1.
2.
Zurück zum Zitat Aapro MS, Walko CM (2010) Aprepitant: drug–drug interactions in perspective. Ann Oncol 12:2316–2323CrossRef Aapro MS, Walko CM (2010) Aprepitant: drug–drug interactions in perspective. Ann Oncol 12:2316–2323CrossRef
3.
Zurück zum Zitat Emend (aprepitant) capsules [package insert]. Whitehouse Station, NJ: Merck & Co., Inc., 2003 Emend (aprepitant) capsules [package insert]. Whitehouse Station, NJ: Merck & Co., Inc., 2003
4.
Zurück zum Zitat Emend (fosaprepitant dimeglumine for injection) [package insert]. Whitehouse Station, NJ: Merck & Co., Inc., 2008 Emend (fosaprepitant dimeglumine for injection) [package insert]. Whitehouse Station, NJ: Merck & Co., Inc., 2008
5.
Zurück zum Zitat Hesketh PJ, Grunberg SM, Gralla RJ et al (2003) The oral neurokinin-1 antagonist aprepitant for the prevention of chemotherapy-induced nausea and vomiting: a multinational, randomized, double-blind, placebo-controlled trial in patients receiving high-dose cisplatin—the Aprepitant Protocol 052 Study Group. J Clin Oncol 21:4112–4119PubMedCrossRef Hesketh PJ, Grunberg SM, Gralla RJ et al (2003) The oral neurokinin-1 antagonist aprepitant for the prevention of chemotherapy-induced nausea and vomiting: a multinational, randomized, double-blind, placebo-controlled trial in patients receiving high-dose cisplatin—the Aprepitant Protocol 052 Study Group. J Clin Oncol 21:4112–4119PubMedCrossRef
6.
Zurück zum Zitat Poli-Bigelli S, Rodrigues-Pereira J, Carides AD et al (2003) Addition of the neurokinin 1 receptor antagonist aprepitant to standard antiemetic therapy improves control of chemotherapy-induced nausea and vomiting. Results from a randomized, double-blind, placebo-controlled trial in Latin America. Cancer 97:3090–3098PubMedCrossRef Poli-Bigelli S, Rodrigues-Pereira J, Carides AD et al (2003) Addition of the neurokinin 1 receptor antagonist aprepitant to standard antiemetic therapy improves control of chemotherapy-induced nausea and vomiting. Results from a randomized, double-blind, placebo-controlled trial in Latin America. Cancer 97:3090–3098PubMedCrossRef
7.
Zurück zum Zitat Warr DG, Hesketh PJ, Gralla RJ et al (2005) Efficacy and tolerability of aprepitant for the prevention of chemotherapy-induced nausea and vomiting in patients with breast cancer after moderately emetogenic chemotherapy. J Clin Oncol 23:2822–2830PubMedCrossRef Warr DG, Hesketh PJ, Gralla RJ et al (2005) Efficacy and tolerability of aprepitant for the prevention of chemotherapy-induced nausea and vomiting in patients with breast cancer after moderately emetogenic chemotherapy. J Clin Oncol 23:2822–2830PubMedCrossRef
8.
Zurück zum Zitat Rapoport BL, Jordan K, Boice JA et al (2010) Aprepitant for the prevention of chemotherapy-induced nausea and vomiting associated with a broad range of moderately emetogenic chemotherapies and tumor types: a randomized, double-blind study. Support Care Cancer 18:423–431PubMedCrossRef Rapoport BL, Jordan K, Boice JA et al (2010) Aprepitant for the prevention of chemotherapy-induced nausea and vomiting associated with a broad range of moderately emetogenic chemotherapies and tumor types: a randomized, double-blind study. Support Care Cancer 18:423–431PubMedCrossRef
9.
Zurück zum Zitat Schmoll HJ, Aapro MS, Poli-Bigelli S et al (2006) Comparison of an aprepitant regimen with a multiple-day ondansetron regimen, both with dexamethasone, for antiemetic efficacy in high-dose cisplatin treatment. Ann Oncol 17:1000–1006PubMedCrossRef Schmoll HJ, Aapro MS, Poli-Bigelli S et al (2006) Comparison of an aprepitant regimen with a multiple-day ondansetron regimen, both with dexamethasone, for antiemetic efficacy in high-dose cisplatin treatment. Ann Oncol 17:1000–1006PubMedCrossRef
10.
Zurück zum Zitat Jordan K, Sippel C, Schmoll HJ (2007) Guidelines for antiemetic treatment of chemotherapy-induced nausea and vomiting: past, present, and future recommendations. Oncologist 12:1143–1150PubMedCrossRef Jordan K, Sippel C, Schmoll HJ (2007) Guidelines for antiemetic treatment of chemotherapy-induced nausea and vomiting: past, present, and future recommendations. Oncologist 12:1143–1150PubMedCrossRef
11.
Zurück zum Zitat Herrstedt J (2008) Antiemetics: an update and the MASCC guidelines applied in clinical practice. Nat Clin Pract Oncol 5:32–43PubMedCrossRef Herrstedt J (2008) Antiemetics: an update and the MASCC guidelines applied in clinical practice. Nat Clin Pract Oncol 5:32–43PubMedCrossRef
12.
Zurück zum Zitat Herrstedt J, Roila F (2008) Chemotherapy-induced nausea and vomiting: ESMO clinical recommendations for prophylaxis. Ann Oncol 19 (Suppl 2):ii110–ii112 Herrstedt J, Roila F (2008) Chemotherapy-induced nausea and vomiting: ESMO clinical recommendations for prophylaxis. Ann Oncol 19 (Suppl 2):ii110–ii112
13.
Zurück zum Zitat Kris MG, Hesketh PJ, Somerfield MR et al (2006) American society of clinical oncology guideline for antiemetics in oncology: update. J Clin Oncol 24:2932–2947PubMedCrossRef Kris MG, Hesketh PJ, Somerfield MR et al (2006) American society of clinical oncology guideline for antiemetics in oncology: update. J Clin Oncol 24:2932–2947PubMedCrossRef
14.
Zurück zum Zitat Blum RA, Majumdar A, McCrea J et al (2003) Effects of aprepitant on the pharmacokinetics of ondansetron and granisetron in healthy subjects. Clin Ther 25:1407–1419PubMedCrossRef Blum RA, Majumdar A, McCrea J et al (2003) Effects of aprepitant on the pharmacokinetics of ondansetron and granisetron in healthy subjects. Clin Ther 25:1407–1419PubMedCrossRef
15.
Zurück zum Zitat Shah AK, Hunt TL, Gallagher SC, Cullen MT Jr (2005) Pharmacokinetics of palonosetron in combination with aprepitant in healthy volunteers. Curr Med Res Opin 21:595–601PubMedCrossRef Shah AK, Hunt TL, Gallagher SC, Cullen MT Jr (2005) Pharmacokinetics of palonosetron in combination with aprepitant in healthy volunteers. Curr Med Res Opin 21:595–601PubMedCrossRef
16.
Zurück zum Zitat McCrea JB, Majumdar AK, Goldberg MR et al (2003) Effects of the neurokinin1 receptor antagonist aprepitant on the pharmacokinetics of dexamethasone and methylprednisolone. Clin Pharmacol Ther 74:17–24PubMedCrossRef McCrea JB, Majumdar AK, Goldberg MR et al (2003) Effects of the neurokinin1 receptor antagonist aprepitant on the pharmacokinetics of dexamethasone and methylprednisolone. Clin Pharmacol Ther 74:17–24PubMedCrossRef
17.
Zurück zum Zitat Convention United States Pharmacopeial (2009) Particulate matter in injections. USP NF 2010. U.S. Pharmacopeia, Rockville Convention United States Pharmacopeial (2009) Particulate matter in injections. USP NF 2010. U.S. Pharmacopeia, Rockville
18.
Zurück zum Zitat Eisenberg S (1997) Intravenous drug compatibility: a challenge for the oncology nurse. Oncol Nurs Forum 24:859–869PubMed Eisenberg S (1997) Intravenous drug compatibility: a challenge for the oncology nurse. Oncol Nurs Forum 24:859–869PubMed
19.
Zurück zum Zitat Longfield V (2003) Compatibility and stability of 5-HT3 receptor antagonists: a pharmacology review. Oncol Nurs Forum 29:1469–1482CrossRef Longfield V (2003) Compatibility and stability of 5-HT3 receptor antagonists: a pharmacology review. Oncol Nurs Forum 29:1469–1482CrossRef
20.
Zurück zum Zitat Aloxi (palonosetron HCl) [package insert]. Helsinn Healthcare: SA Switzerland, 2009 Aloxi (palonosetron HCl) [package insert]. Helsinn Healthcare: SA Switzerland, 2009
Metadaten
Titel
Compatibility of intravenous fosaprepitant with intravenous 5-HT3 antagonists and corticosteroids
verfasst von
Susan Sun
Joseph Schaller
Jiri Placek
Brett Duersch
Publikationsdatum
01.09.2013
Verlag
Springer Berlin Heidelberg
Erschienen in
Cancer Chemotherapy and Pharmacology / Ausgabe 3/2013
Print ISSN: 0344-5704
Elektronische ISSN: 1432-0843
DOI
https://doi.org/10.1007/s00280-013-2201-2

Weitere Artikel der Ausgabe 3/2013

Cancer Chemotherapy and Pharmacology 3/2013 Zur Ausgabe

CUP-Syndrom: Künstliche Intelligenz kann Primärtumor finden

30.04.2024 Künstliche Intelligenz Nachrichten

Krebserkrankungen unbekannten Ursprungs (CUP) sind eine diagnostische Herausforderung. KI-Systeme können Pathologen dabei unterstützen, zytologische Bilder zu interpretieren, um den Primärtumor zu lokalisieren.

Sind Frauen die fähigeren Ärzte?

30.04.2024 Gendermedizin Nachrichten

Patienten, die von Ärztinnen behandelt werden, dürfen offenbar auf bessere Therapieergebnisse hoffen als Patienten von Ärzten. Besonders gilt das offenbar für weibliche Kranke, wie eine Studie zeigt.

Adjuvante Immuntherapie verlängert Leben bei RCC

25.04.2024 Nierenkarzinom Nachrichten

Nun gibt es auch Resultate zum Gesamtüberleben: Eine adjuvante Pembrolizumab-Therapie konnte in einer Phase-3-Studie das Leben von Menschen mit Nierenzellkarzinom deutlich verlängern. Die Sterberate war im Vergleich zu Placebo um 38% geringer.

Alectinib verbessert krankheitsfreies Überleben bei ALK-positivem NSCLC

25.04.2024 NSCLC Nachrichten

Das Risiko für Rezidiv oder Tod von Patienten und Patientinnen mit reseziertem ALK-positivem NSCLC ist unter einer adjuvanten Therapie mit dem Tyrosinkinase-Inhibitor Alectinib signifikant geringer als unter platinbasierter Chemotherapie.

Update Onkologie

Bestellen Sie unseren Fach-Newsletter und bleiben Sie gut informiert.