Comparative Pharmacology
Head-to-head clinical analysis: DEMULEN 1 50 21 versus LO OVRAL.
Peer-Reviewed Evidence
Head-to-head clinical analysis: DEMULEN 1 50 21 versus LO OVRAL.
DEMULEN 1/50-21 vs LO/OVRAL
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
DEMULEN 1/50-21 is a combined oral contraceptive containing ethinyl estradiol and ethynodiol diacetate. Ethinyl estradiol and progestins inhibit gonadotropin release (FSH and LH) from the pituitary, suppressing ovulation. Progestins also increase cervical mucus viscosity and alter endometrial receptivity, impeding sperm penetration and implantation.
Combination estrogen-progestin oral contraceptive; suppresses gonadotropin release, primarily FSH and LH, inhibiting ovulation; increases viscosity of cervical mucus, impeding sperm penetration; alters endometrial receptivity.
1 tablet (ethinyl estradiol 50 mcg, norethindrone 1 mg) orally once daily for 21 days, followed by 7 days off.
One tablet (30 mcg ethinyl estradiol, 0.3 mg norgestrel) orally once daily for 28-day cycle (21 active, 7 placebo).
None Documented
None Documented
Ethinylestradiol: 13 ± 3 h (biphasic; terminal phase used for dosing interval). Clinical context: steady-state achieved after ~3 days; missed dose may reduce contraceptive efficacy if >36 h.
Norgestrel (levonorgestrel): 11-45 hours (mean ~24 hours); ethinyl estradiol: 7-21 hours (mean ~14 hours). Half-life increases slightly with repeated dosing due to saturable metabolism.
Renal (approx. 50% as metabolites, <1% unchanged), fecal (approx. 40%, largely as ethinylestradiol conjugates), biliary (minor, enterohepatic recirculation of ethinylestradiol)
Urine (50-60% as conjugated metabolites), feces (30-40% as metabolites), enterohepatic recirculation present.
Category C
Category C
Combination Oral Contraceptive
Combination Oral Contraceptive