Comparative Pharmacology
Head-to-head clinical analysis: EMEND versus TRANSDERM SCOP.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EMEND versus TRANSDERM SCOP.
EMEND vs TRANSDERM SCOP
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 antagonist at muscarinic acetylcholine receptors (M1, M2, M3 subtypes) in the vestibular system, gastrointestinal tract, and central nervous system, inhibiting vagal nerve activity and preventing motion-induced nausea and vomiting.
125 mg orally once 1 hour before chemotherapy; then 80 mg orally once daily on Days 2 and 3.
One transdermal patch (1 mg/72 hours) applied to the hairless area behind the ear at least 4 hours before anticipated exposure; replace every 72 hours as needed.
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.
The terminal elimination half-life of scopolamine is approximately 9.5 hours (range 6-12 hours) following transdermal administration. In elderly patients, half-life may be prolonged to up to 20 hours.
Primarily metabolized; ~5% unchanged in urine, ~57% in feces as metabolites, ~32% in urine as metabolites. Renal elimination of parent drug is minimal.
Scopolamine is extensively metabolized; about 50% of a dose is excreted renally as metabolites and unchanged drug, with less than 10% excreted unchanged in urine. Biliary/fecal excretion accounts for approximately 30-40% of the dose.
Category C
Category C
Antiemetic
Antiemetic