Comparative Pharmacology
Head-to-head clinical analysis: FOSAPREPITANT DIMEGLUMINE versus MEZOFY.
Peer-Reviewed Evidence
Head-to-head clinical analysis: FOSAPREPITANT DIMEGLUMINE versus MEZOFY.
FOSAPREPITANT DIMEGLUMINE vs MEZOFY
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.
MEZOFY is a selective serotonin reuptake inhibitor (SSRI) that potentiates serotonergic activity in the CNS by inhibiting the reuptake of serotonin at the presynaptic neuronal membrane.
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.
MEZOFY (mexiletine) 200 mg orally every 8 hours; may increase to 300 mg every 8 hours if needed.
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.
Terminal half-life: 8-12 hours (mean 10 h); prolonged in renal impairment (up to 24 h in CrCl <30 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: 60% unchanged; biliary/fecal: 25% as metabolites; 15% other
Category C
Category C
Antiemetic
Antiemetic/Antivertigo