Comparative Pharmacology
Head-to-head clinical analysis: ETHINYL ESTRADIOL AND NORELGESTROMIN versus STILBESTROL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ETHINYL ESTRADIOL AND NORELGESTROMIN versus STILBESTROL.
ETHINYL ESTRADIOL AND NORELGESTROMIN vs STILBESTROL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Combination contraceptive: estrogen (ethinyl estradiol) suppresses gonadotropin release via negative feedback on pituitary; progestin (norelgestromin) thickens cervical mucus and inhibits ovulation.
Synthetic nonsteroidal estrogen that acts by binding to estrogen receptors (ERα and ERβ), leading to translocation to the nucleus, modulation of gene transcription, and promotion of estrogenic effects in target tissues.
One transdermal patch (releasing 0.035 mg ethinyl estradiol and 0.150 mg norelgestromin per 24 hours) applied once weekly for 3 weeks, followed by 1 week patch-free.
0.5 to 2 mg orally once daily; or 25 mg intramuscularly once daily for 5 days; for prostate cancer: 1 to 3 mg orally once daily.
None Documented
None Documented
Clinical Note
moderateDiethylstilbestrol + Digoxin
"Diethylstilbestrol may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateDiethylstilbestrol + Digitoxin
"Diethylstilbestrol may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateDiethylstilbestrol + Deslanoside
"Diethylstilbestrol may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateDiethylstilbestrol + Acetyldigitoxin
Ethinyl estradiol has a terminal elimination half-life of approximately 13-27 hours (mean ~17 hours). Norelgestromin has a terminal half-life of about 28 hours. These half-lives support once-weekly dosing of the transdermal system, achieving steady-state by the second application.
Terminal elimination half-life is approximately 24-48 hours, with a prolonged phase due to enterohepatic recirculation; requires dosing adjustment in hepatic impairment.
Ethinyl estradiol and norelgestromin are excreted primarily via urine and feces. Ethinyl estradiol undergoes extensive metabolism; about 40% is excreted in urine and 60% in feces as glucuronide and sulfate conjugates. Norelgestromin is metabolized to norgestrel and other metabolites; approximately 45% is excreted in urine and 35% in feces.
Renal excretion of glucuronide and sulfate conjugates accounts for approximately 60-80% of an administered dose; biliary/fecal excretion accounts for 15-30%; less than 5% is excreted unchanged in urine.
Category D/X
Category C
Estrogen
Estrogen
"Diethylstilbestrol may decrease the cardiotoxic activities of Acetyldigitoxin."