Comparative Pharmacology
Head-to-head clinical analysis: COMPAZINE versus FOSAPREPITANT DIMEGLUMINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: COMPAZINE versus FOSAPREPITANT DIMEGLUMINE.
COMPAZINE vs FOSAPREPITANT DIMEGLUMINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Dopamine D2 receptor antagonist in the chemoreceptor trigger zone; also blocks alpha-1 adrenergic, histamine H1, and muscarinic M1 receptors.
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.
5-10 mg IM/IV every 3-4 hours as needed; or 25 mg PO/PR twice daily for severe nausea/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
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.
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.
Renal (approximately 70% as metabolites, <1% unchanged), biliary/fecal (approximately 30%).
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
Antipsychotic (Phenothiazine) / Antiemetic
Antiemetic