Comparative Pharmacology
Head-to-head clinical analysis: FOSAPREPITANT DIMEGLUMINE versus ZUPLENZ.
Peer-Reviewed Evidence
Head-to-head clinical analysis: FOSAPREPITANT DIMEGLUMINE versus ZUPLENZ.
FOSAPREPITANT DIMEGLUMINE vs ZUPLENZ
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Fosaprepitant dimeglumine is a prodrug of aprepitant, a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. It inhibits emesis by blocking NK1 receptors in the central nervous system, particularly in the area postrema and the nucleus tractus solitarius.
Competitive serotonin 5-HT3 receptor antagonist; acts centrally on the chemoreceptor trigger zone and peripherally on GI vagal nerve terminals to inhibit emesis.
150 mg intravenous over 30 minutes on day 1, combined with dexamethasone and a 5-HT3 antagonist; alternatively, 115 mg IV on day 1 followed by 80 mg IV on day 2 and 80 mg IV on day 3, or 150 mg oral (as fosaprepitant dimeglumine or aprepitant) on day 1 and 80 mg oral on days 2 and 3.
8 mg administered intraorally as a single dose 1 hour before chemotherapy; may repeat once if vomiting occurs within 30 minutes after initial dose.
None Documented
None Documented
Terminal elimination half-life of aprepitant is approximately 9 to 13 hours; clinical significance includes once-daily dosing for prevention of chemotherapy-induced nausea and vomiting.
Terminal elimination half-life 3.5 hours; in hepatic impairment increases to 7-9 hours
Fosaprepitant is rapidly converted to aprepitant. Aprepitant is eliminated primarily by metabolism; <5% of the dose is excreted unchanged in urine. Fecal excretion accounts for approximately 58% of the dose, and urinary excretion accounts for 43% (mostly as metabolites).
Renal 70% unchanged, fecal 20% (including biliary metabolites), 10% metabolized
Category C
Category C
Antiemetic
Antiemetic