Comparative Pharmacology
Head-to-head clinical analysis: EMEND versus MAREZINE.
Head-to-head clinical analysis: EMEND versus MAREZINE.
EMEND vs MAREZINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Selective substance P/neurokinin 1 (NK1) receptor antagonist, which inhibits the binding of substance P in the emetic pathway.
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.
125 mg orally once 1 hour before chemotherapy; then 80 mg orally once daily 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
9–13 hours (terminal) in healthy adults; clinically, this supports once-daily dosing. In patients with severe renal impairment (CrCl <30 mL/min), half-life is prolonged to ~16 hours.
Terminal elimination half-life is 4-6 hours in adults; prolonged to 8-12 hours in elderly or hepatic impairment
Primarily metabolized; ~5% unchanged in urine, ~57% in feces as metabolites, ~32% in urine as metabolites. Renal elimination of parent drug is minimal.
Renal: 70-80% as unchanged drug and metabolites; fecal: ~20%; biliary: minor
Category C
Category C
Antiemetic
Antiemetic