Comparative Pharmacology
Head-to-head clinical analysis: MEGACE ES versus MEGESTROL ACETATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: MEGACE ES versus MEGESTROL ACETATE.
MEGACE ES 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 and testicular hormone production. It also has antineoplastic effects possibly through local action on hormone-sensitive tissues and stimulates appetite via modulation of neuropeptide Y and other appetite-regulating factors.
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.
625 mg orally once daily (MEGACE ES suspension contains 625 mg/5 mL; shake well before use). For appetite stimulation in cachexia.
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
Approximately 34 hours in plasma; steady-state achieved after 2-3 weeks of daily dosing.
Terminal half-life: 13-105 hours (mean ~34 hours) in adults; prolonged in hepatic impairment.
Primarily renal (≤1% unchanged) and biliary; extensive metabolism to inactive glucuronide conjugates excreted in feces.
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."