Comparative Pharmacology
Head-to-head clinical analysis: APREPITANT versus PROMETHAZINE DM.
Peer-Reviewed Evidence
Head-to-head clinical analysis: APREPITANT versus PROMETHAZINE DM.
APREPITANT vs PROMETHAZINE DM
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Selective high-affinity antagonist of the human substance P/neurokinin 1 (NK1) receptor, inhibiting emesis by blocking the binding of substance P in the central nervous system.
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 on day 1, then 80 mg orally once on days 2 and 3 of a 3-day chemotherapy regimen, given 1 hour before chemotherapy. Alternatively, a single 165 mg oral dose for prevention of postoperative nausea and vomiting.
2 teaspoonfuls (10 mL) orally every 4-6 hours, not to exceed 8 teaspoonfuls (40 mL) per 24 hours.
None Documented
None Documented
Clinical Note
moderateAprepitant + Torasemide
"The metabolism of Torasemide can be increased when combined with Aprepitant."
Clinical Note
moderateAprepitant + Lornoxicam
"The metabolism of Lornoxicam can be increased when combined with Aprepitant."
Clinical Note
moderateAprepitant + Aceclofenac
"The metabolism of Aceclofenac can be increased when combined with Aprepitant."
Clinical Note
moderateAprepitant + Zaltoprofen
Terminal elimination half-life is approximately 9 to 13 hours in adults, allowing once-daily dosing. In pediatric patients, half-life may be shorter (about 5-6 hours).
16-19 hours (terminal); note: effect may last longer due to active metabolites and tissue binding
Aprepitant is eliminated primarily by metabolism; less than 5% is excreted unchanged in urine or feces. Approximately 50% of a dose is recovered in feces (mostly metabolites) and 10% in urine.
Renal (70-80% as metabolites, <1% unchanged); biliary/fecal (20-30%)
Category C
Category A/B
Antiemetic
Antihistamine / Antiemetic
"The metabolism of Zaltoprofen can be increased when combined with Aprepitant."