Comparative Pharmacology
Head-to-head clinical analysis: MEGACE ES versus NORETHINDRONE ACETATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: MEGACE ES versus NORETHINDRONE ACETATE.
MEGACE ES vs NORETHINDRONE 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.
Progestin that suppresses gonadotropin secretion, inhibits ovulation, and induces endometrial thinning. Also binds to progesterone receptors, exerting antiestrogenic effects.
625 mg orally once daily (MEGACE ES suspension contains 625 mg/5 mL; shake well before use). For appetite stimulation in cachexia.
Oral, 5 mg once daily for 14 days per cycle, beginning on day 1 of menstrual cycle; for endometriosis, 5 mg daily for 14 days then 10 mg daily for 14 days, then 15 mg daily, or as tolerated up to 15 mg daily continuous.
None Documented
None Documented
Approximately 34 hours in plasma; steady-state achieved after 2-3 weeks of daily dosing.
Terminal elimination half-life is approximately 5-8 hours (mean 7.5 hours). Clinically, steady-state is achieved within 2-3 days of daily dosing.
Primarily renal (≤1% unchanged) and biliary; extensive metabolism to inactive glucuronide conjugates excreted in feces.
Renal (39-61% as metabolites), biliary/fecal (35-49% as metabolites). Less than 1% excreted unchanged.
Category C
Category D/X
Progestin
Progestin