Comparative Pharmacology
Head-to-head clinical analysis: EMEND versus EMETE CON.
Head-to-head clinical analysis: EMEND versus EMETE CON.
EMEND vs EMETE-CON
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.
Antiemetic; dopaminergic antagonist at D2 receptors in the chemoreceptor trigger zone; also exhibits anticholinergic and antihistaminic properties.
125 mg orally once 1 hour before chemotherapy; then 80 mg orally once daily on Days 2 and 3.
12.5 mg intravenously over 30 seconds as a single dose; may repeat once after 1 hour if necessary.
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 8-12 hours in adults with normal renal and hepatic function; may extend to 15-20 hours in elderly or patients with 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.
Primarily hepatic metabolism (CYP2D6, CYP3A4) with <5% excreted unchanged in urine. Biliary/fecal excretion accounts for approximately 60-70% of metabolites, with renal elimination of metabolites constituting 25-35%.
Category C
Category C
Antiemetic
Antiemetic