Comparative Pharmacology
Head-to-head clinical analysis: APREPITANT versus COMPAZINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: APREPITANT versus COMPAZINE.
APREPITANT vs COMPAZINE
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.
Dopamine D2 receptor antagonist in the chemoreceptor trigger zone; also blocks alpha-1 adrenergic, histamine H1, and muscarinic M1 receptors.
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.
5-10 mg IM/IV every 3-4 hours as needed; or 25 mg PO/PR twice daily for severe nausea/vomiting.
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 is approximately 23 hours (range 15-30 hours) after oral or intramuscular administration. Clinical context: requires multiple daily dosing for steady state.
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.
Renal (approximately 70% as metabolites, <1% unchanged), biliary/fecal (approximately 30%).
Category C
Category C
Antiemetic
Antipsychotic (Phenothiazine) / Antiemetic
"The metabolism of Zaltoprofen can be increased when combined with Aprepitant."