Comparative Pharmacology
Head-to-head clinical analysis: DROSPIRENONE versus MEGESTROL ACETATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: DROSPIRENONE versus MEGESTROL ACETATE.
DROSPIRENONE vs MEGESTROL ACETATE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Spironolactone analog that antagonizes aldosterone at the mineralocorticoid receptor, leading to increased sodium and water excretion and potassium retention. Also has antiandrogenic activity by blocking androgen receptors and decreasing ovarian androgen production via inhibition of gonadotropin release.
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.
3 mg orally 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: ~30-35 hours (range 25-40 h); significant clinical accumulation occurs after repeated dosing, requiring 10-14 days to reach steady state.
Terminal half-life: 13-105 hours (mean ~34 hours) in adults; prolonged in hepatic impairment.
Renal: ~50% (as metabolites; <10% unchanged); Fecal: ~40-50% (as metabolites; bile-mediated); Urinary and fecal elimination account for >95% of an oral dose.
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."