Comparative Pharmacology
Head-to-head clinical analysis: MEGESTROL ACETATE versus NORLUTATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: MEGESTROL ACETATE versus NORLUTATE.
MEGESTROL ACETATE vs NORLUTATE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
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.
Progestin that suppresses gonadotropin secretion, inhibits ovulation, and induces endometrial transformation.
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.
5 mg orally once daily for 5 days, starting on day 1 of menstrual cycle; for menorrhagia, 5 mg orally three times daily from day 19 to day 26 of cycle.
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 half-life: 13-105 hours (mean ~34 hours) in adults; prolonged in hepatic impairment.
Terminal elimination half-life is approximately 5-6 hours. Clinical context: supports twice-daily dosing; steady state reached within 2 days.
Renal: 50-79% as glucuronide conjugates; fecal: 8-30%; biliary: minor.
Primarily renal (approximately 60% of metabolites, mostly glucuronides), with about 40% fecal/biliary elimination. Less than 1% excreted unchanged.
Category D/X
Category C
Progestin
Progestin
"Megestrol acetate may decrease the cardiotoxic activities of Acetyldigitoxin."