Comparative Pharmacology
Head-to-head clinical analysis: EMEND versus PROCHLORPERAZINE MALEATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: EMEND versus PROCHLORPERAZINE MALEATE.
EMEND vs PROCHLORPERAZINE MALEATE
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.
Prochlorperazine is a phenothiazine antipsychotic that primarily antagonizes dopamine D2 receptors in the chemoreceptor trigger zone (CTZ) and central nervous system. It also has anticholinergic and antiemetic effects through blockade of histamine H1 and muscarinic M1 receptors.
125 mg orally once 1 hour before chemotherapy; then 80 mg orally once daily on Days 2 and 3.
5-10 mg orally 3-4 times daily; or 25 mg rectally twice daily; or 5-10 mg intramuscularly every 3-4 hours up to 40 mg/day; or 2.5-10 mg intravenously slowly at 2.5 mg/min, maximum 20 mg/day.
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 is approximately 6-8 hours in adults, but may extend up to 12-15 hours after chronic dosing or in hepatic impairment.
Primarily metabolized; ~5% unchanged in urine, ~57% in feces as metabolites, ~32% in urine as metabolites. Renal elimination of parent drug is minimal.
Primarily renal (70-80% as metabolites, <1% unchanged); fecal/biliary excretion accounts for 20-30% via enterohepatic circulation.
Category C
Category A/B
Antiemetic
Typical Antipsychotic / Antiemetic