Comparative Pharmacology
Head-to-head clinical analysis: EMEND versus ZUPLENZ.
Head-to-head clinical analysis: EMEND versus ZUPLENZ.
EMEND vs ZUPLENZ
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.
Competitive serotonin 5-HT3 receptor antagonist; acts centrally on the chemoreceptor trigger zone and peripherally on GI vagal nerve terminals to inhibit emesis.
125 mg orally once 1 hour before chemotherapy; then 80 mg orally once daily on Days 2 and 3.
8 mg administered intraorally as a single dose 1 hour before chemotherapy; may repeat once if vomiting occurs within 30 minutes after initial dose.
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 3.5 hours; in hepatic impairment increases to 7-9 hours
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% unchanged, fecal 20% (including biliary metabolites), 10% metabolized
Category C
Category C
Antiemetic
Antiemetic