Comparative Pharmacology
Head-to-head clinical analysis: APREPITANT versus PROMETHAZINE HYDROCHLORIDE AND DEXTROMETHORPHAN HYDROBROMIDE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: APREPITANT versus PROMETHAZINE HYDROCHLORIDE AND DEXTROMETHORPHAN HYDROBROMIDE.
APREPITANT vs PROMETHAZINE HYDROCHLORIDE AND DEXTROMETHORPHAN HYDROBROMIDE
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, and sedative. Dextromethorphan is a cough suppressant that acts as an NMDA receptor antagonist and sigma-1 receptor agonist.
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.
For cough and upper respiratory symptoms: 5 mL (containing promethazine hydrochloride 6.25 mg and dextromethorphan hydrobromide 15 mg) orally every 4 to 6 hours, not to exceed 30 mL in 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).
Promethazine: 10-19 hours (mean 12 hours). Dextromethorphan: extensive metabolizers (CYP2D6) 3-5 hours; poor metabolizers 20-30 hours. Clinical context: accumulation with repeated dosing, especially in poor metabolizers.
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.
Promethazine: primarily hepatic metabolism, renal excretion of metabolites (~70%, <1% unchanged); fecal excretion (20-30%). Dextromethorphan: hepatic metabolism, renal excretion of metabolites and <1% unchanged drug.
Category C
Category A/B
Antiemetic
Antihistamine / Antiemetic
"The metabolism of Zaltoprofen can be increased when combined with Aprepitant."