Comparative Pharmacology
Head-to-head clinical analysis: MEGACE versus MEGESTROL ACETATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: MEGACE versus MEGESTROL ACETATE.
MEGACE vs MEGESTROL ACETATE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Megestrol acetate is a synthetic progestin that inhibits pituitary gonadotropin secretion, leading to suppression of ovarian function and reduction of sex hormone levels. It also has antineoplastic effects through interference with estrogen receptor binding and may stimulate appetite via effects on neuropeptide Y and cytokines.
Synthetic progestin with antineoplastic activity; suppresses pituitary gonadotropin secretion and exerts direct cytotoxic effects on endometrial cancer cells via binding to progesterone receptors. Also stimulates appetite through unclear mechanisms, possibly involving neuropeptide Y and inhibition of proinflammatory cytokines.
Oral: 625 mg (suspension) or 400–800 mg (tablets) once daily.
400 mg orally once daily or 800 mg orally once daily (suspension) for appetite stimulation; 40-320 mg orally daily in divided doses for endometrial cancer.
None Documented
None Documented
Clinical Note
moderateMegestrol acetate + Digoxin
"Megestrol acetate may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateMegestrol acetate + Digitoxin
"Megestrol acetate may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateMegestrol acetate + Deslanoside
"Megestrol acetate may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateMegestrol acetate + Acetyldigitoxin
Terminal elimination half-life: 70-95 hours (mean 85 hours) in chronic dosing; shorter in initial doses; clinical context: requires 3-4 weeks to reach steady state.
Terminal half-life: 13-105 hours (mean ~34 hours) in adults; prolonged in hepatic impairment.
Primarily renal: ~75% as glucuronide conjugates and unchanged drug; biliary/fecal: ~25% as metabolites.
Renal: 50-79% as glucuronide conjugates; fecal: 8-30%; biliary: minor.
Category C
Category D/X
Progestin
Progestin
"Megestrol acetate may decrease the cardiotoxic activities of Acetyldigitoxin."