Comparative Pharmacology
Head-to-head clinical analysis: MEGESTROL ACETATE versus NORGESTIMATE ETHINYL ESTRADIOL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: MEGESTROL ACETATE versus NORGESTIMATE ETHINYL ESTRADIOL.
MEGESTROL ACETATE vs NORGESTIMATE; ETHINYL ESTRADIOL
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.
Combination oral contraceptive containing norgestimate (a progestin) and ethinyl estradiol (an estrogen). The primary mechanism is suppression of gonadotropins (FSH and LH) via negative feedback on the hypothalamic-pituitary-ovarian axis, preventing ovulation. Additional effects include thickening cervical mucus (inhibiting sperm penetration) and altering endometrial receptivity.
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.
Oral, one tablet daily at the same time for 21 days, followed by 7 placebo tablets.
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.
Norgestimate: terminal half-life of norelgestromin (active metabolite) is 27.6 ± 7.8 hours; ethinyl estradiol: terminal half-life is 17.5 ± 6.3 hours. Steady state achieved within 14 days.
Renal: 50-79% as glucuronide conjugates; fecal: 8-30%; biliary: minor.
Norgestimate metabolites are primarily excreted via urine (60-80%) and feces (35-49%) as glucuronide and sulfate conjugates; ethinyl estradiol is excreted in urine (40%) and feces (60%) as conjugates.
Category D/X
Category D/X
Progestin
Progestin + Estrogen
"Megestrol acetate may decrease the cardiotoxic activities of Acetyldigitoxin."