Comparative Pharmacology
Head-to-head clinical analysis: FOSAPREPITANT DIMEGLUMINE versus PROCHLORPERAZINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: FOSAPREPITANT DIMEGLUMINE versus PROCHLORPERAZINE.
FOSAPREPITANT DIMEGLUMINE vs PROCHLORPERAZINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Fosaprepitant dimeglumine is a prodrug of aprepitant, a selective high-affinity antagonist of human substance P/neurokinin 1 (NK1) receptors. It inhibits emesis by blocking NK1 receptors in the central nervous system, particularly in the area postrema and the nucleus tractus solitarius.
Prochlorperazine is a phenothiazine antipsychotic that acts as a dopamine D2 receptor antagonist in the chemoreceptor trigger zone (CTZ) and at high doses in the mesolimbic system. It also has anticholinergic and antiemetic effects.
150 mg intravenous over 30 minutes on day 1, combined with dexamethasone and a 5-HT3 antagonist; alternatively, 115 mg IV on day 1 followed by 80 mg IV on day 2 and 80 mg IV on day 3, or 150 mg oral (as fosaprepitant dimeglumine or aprepitant) on day 1 and 80 mg oral on days 2 and 3.
5-10 mg IM/IV every 3-4 hours as needed; or 5-10 mg PO 3-4 times daily; or 25 mg PR twice daily. Maximum IM/IV: 40 mg/day; PO: 40 mg/day.
None Documented
None Documented
Clinical Note
moderateProchlorperazine + Fluticasone propionate
"The risk or severity of adverse effects can be increased when Prochlorperazine is combined with Fluticasone propionate."
Clinical Note
moderateProchlorperazine + Haloperidol
"The metabolism of Haloperidol can be decreased when combined with Prochlorperazine."
Clinical Note
moderateProchlorperazine + Methylphenidate
"The risk or severity of adverse effects can be increased when Prochlorperazine is combined with Methylphenidate."
Clinical Note
moderateTerminal elimination half-life of aprepitant is approximately 9 to 13 hours; clinical significance includes once-daily dosing for prevention of chemotherapy-induced nausea and vomiting.
Terminal elimination half-life: 23-25 hours, with prolonged elimination in hepatic impairment.
Fosaprepitant is rapidly converted to aprepitant. Aprepitant is eliminated primarily by metabolism; <5% of the dose is excreted unchanged in urine. Fecal excretion accounts for approximately 58% of the dose, and urinary excretion accounts for 43% (mostly as metabolites).
Renal: 70-80% (as metabolites), Fecal: 20-30% (unchanged and metabolites), Biliary: 10-15% of dose excreted in bile.
Category C
Category A/B
Antiemetic
Typical Antipsychotic / Antiemetic
Prochlorperazine + Quinagolide
"The therapeutic efficacy of Quinagolide can be decreased when used in combination with Prochlorperazine."