Comparative Pharmacology
Head-to-head clinical analysis: EMEND versus PROMETHAZINE DM.
Head-to-head clinical analysis: EMEND versus PROMETHAZINE DM.
EMEND vs PROMETHAZINE DM
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.
Promethazine is a phenothiazine derivative that acts as a histamine H1 receptor antagonist, antiemetic via blockade of dopamine D2 receptors in the chemoreceptor trigger zone, and sedative via central anticholinergic effects. Dextromethorphan is an NMDA receptor antagonist and sigma-1 receptor agonist, suppressing cough by central action on the cough center.
125 mg orally once 1 hour before chemotherapy; then 80 mg orally once daily on Days 2 and 3.
2 teaspoonfuls (10 mL) orally every 4-6 hours, not to exceed 8 teaspoonfuls (40 mL) per 24 hours.
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.
16-19 hours (terminal); note: effect may last longer due to active metabolites and tissue binding
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 metabolites, <1% unchanged); biliary/fecal (20-30%)
Category C
Category A/B
Antiemetic
Antihistamine / Antiemetic