Comparative Pharmacology
Head-to-head clinical analysis: FOSAPREPITANT DIMEGLUMINE versus MAXOLON.
Peer-Reviewed Evidence
Head-to-head clinical analysis: FOSAPREPITANT DIMEGLUMINE versus MAXOLON.
FOSAPREPITANT DIMEGLUMINE vs MAXOLON
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.
Metoclopramide, the active ingredient in MAXOLON, is a dopamine D2 receptor antagonist and also enhances the response to acetylcholine at muscarinic receptors in the gastrointestinal tract, leading to increased gastric motility and accelerated gastric emptying. It also has antiemetic effects by blocking dopamine receptors in the chemoreceptor trigger zone (CTZ).
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.
10 mg orally, intramuscularly, or intravenously three to four times daily. Maximum daily dose: 30 mg or 0.5 mg/kg.
None Documented
None Documented
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.
5-6 hours in adults with normal renal function; prolonged to 15-20 hours in severe renal impairment (CrCl <10 mL/min).
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: 85-95% as unchanged drug and metabolites; biliary/fecal: <5%.
Category C
Category C
Antiemetic
Antiemetic