Comparative Pharmacology
Head-to-head clinical analysis: FOSAPREPITANT DIMEGLUMINE versus MAREZINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: FOSAPREPITANT DIMEGLUMINE versus MAREZINE.
FOSAPREPITANT DIMEGLUMINE vs MAREZINE
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.
Marezine (cyclizine) is a piperazine-derivative histamine H1-receptor antagonist with central anticholinergic and antiemetic activity. It competitively blocks H1 receptors in the vestibular apparatus and the chemoreceptor trigger zone (CTZ), suppressing nausea and vomiting. It also has antimuscarinic effects on the vomiting center.
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.
50 mg intramuscularly or intravenously every 4 to 6 hours as needed for motion sickness; 50 mg orally 30 to 60 minutes before travel, then every 4 to 6 hours up to 150 mg/24h.
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 is 4-6 hours in adults; prolonged to 8-12 hours in elderly or hepatic impairment
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: 70-80% as unchanged drug and metabolites; fecal: ~20%; biliary: minor
Category C
Category C
Antiemetic
Antiemetic