Comparative Pharmacology
Head-to-head clinical analysis: BARHEMSYS versus FOSAPREPITANT DIMEGLUMINE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: BARHEMSYS versus FOSAPREPITANT DIMEGLUMINE.
BARHEMSYS vs FOSAPREPITANT DIMEGLUMINE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
BARHEMSYS (amisulpride) is a selective dopamine D2/D3 receptor antagonist. It also has weak affinity for serotonin 5-HT2A and 5-HT2B receptors, with no significant activity at other dopamine or serotonin receptor subtypes. Its antiemetic effect is primarily mediated through blockade of D2 receptors in the chemoreceptor trigger zone (CTZ).
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.
BARHEMSYS (amisulpride) 10 mg intravenously over 2 minutes, once daily for prevention of postoperative nausea and vomiting.
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.
None Documented
None Documented
Terminal elimination half-life is approximately 24 hours, supporting once-daily dosing in most patients.
Terminal 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.
Renal excretion accounts for approximately 50% of the dose as unchanged drug; fecal elimination (including biliary) accounts for approximately 30-40%.
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).
Category C
Category C
Antiemetic
Antiemetic