Comparative Pharmacology
Head-to-head clinical analysis: APREPITANT versus FOSAPREPITANT DIMEGLUMINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: APREPITANT versus FOSAPREPITANT DIMEGLUMINE.
APREPITANT vs FOSAPREPITANT DIMEGLUMINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Selective high-affinity antagonist of the human substance P/neurokinin 1 (NK1) receptor, inhibiting emesis by blocking the binding of substance P in the central nervous system.
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.
125 mg orally once on day 1, then 80 mg orally once on days 2 and 3 of a 3-day chemotherapy regimen, given 1 hour before chemotherapy. Alternatively, a single 165 mg oral dose for prevention of postoperative nausea and vomiting.
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.
None Documented
None Documented
Clinical Note
moderateAprepitant + Torasemide
"The metabolism of Torasemide can be increased when combined with Aprepitant."
Clinical Note
moderateAprepitant + Lornoxicam
"The metabolism of Lornoxicam can be increased when combined with Aprepitant."
Clinical Note
moderateAprepitant + Aceclofenac
"The metabolism of Aceclofenac can be increased when combined with Aprepitant."
Clinical Note
moderateAprepitant + Zaltoprofen
Terminal elimination half-life is approximately 9 to 13 hours in adults, allowing once-daily dosing. In pediatric patients, half-life may be shorter (about 5-6 hours).
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.
Aprepitant is eliminated primarily by metabolism; less than 5% is excreted unchanged in urine or feces. Approximately 50% of a dose is recovered in feces (mostly metabolites) and 10% in urine.
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).
Category C
Category C
Antiemetic
Antiemetic
"The metabolism of Zaltoprofen can be increased when combined with Aprepitant."