Comparative Pharmacology
Head-to-head clinical analysis: FOSAPREPITANT DIMEGLUMINE versus VONTROL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: FOSAPREPITANT DIMEGLUMINE versus VONTROL.
FOSAPREPITANT DIMEGLUMINE vs VONTROL
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.
VONTROL (trimethobenzamide) acts centrally to inhibit the chemoreceptor trigger zone (CTZ) in the medulla oblongata, thereby suppressing nausea and vomiting. Its exact mechanism is not fully understood but may involve antagonism of dopamine D2 receptors and serotonin 5-HT3 receptors.
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 twice daily; maximum 20 mg/day.
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.
12 hours; prolonged in renal impairment (up to 24 hours in ESRD)
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: 60% unchanged; fecal: 30% (biliary); hepatic metabolism: 10%
Category C
Category C
Antiemetic
Antiemetic