Comparative Pharmacology
Head-to-head clinical analysis: LESSINA 28 versus NORTREL 0 5 35 21.
Head-to-head clinical analysis: LESSINA 28 versus NORTREL 0 5 35 21.
LESSINA-28 vs NORTREL 0.5/35-21
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Combination of a progestin (levonorgestrel) and an estrogen (ethinyl estradiol). Inhibits ovulation by suppressing gonadotropin release; increases cervical mucus viscosity to impede sperm penetration, and induces endometrial changes that reduce implantation likelihood.
Combination hormonal contraceptive containing norethindrone (a progestin) and ethinyl estradiol (an estrogen). Norethindrone inhibits ovulation by suppressing gonadotropin release (LH and FSH) and alters cervical mucus and endometrial receptivity. Ethinyl estradiol provides negative feedback on the hypothalamic-pituitary-ovarian axis, further suppressing ovulation.
One tablet (0.1 mg levonorgestrel and 0.02 mg ethinyl estradiol) orally once daily for 28 days, starting on the first day of menstrual cycle.
1 tablet orally once daily for 21 days, followed by 7 days off. Each tablet contains 0.5 mg norethindrone and 35 mcg ethinyl estradiol.
None Documented
None Documented
Terminal elimination half-life: 18-22 hours; clinically relevant for once-daily dosing.
Norethindrone: terminal half-life approximately 7-8 hours. Ethinyl estradiol: terminal half-life approximately 13-27 hours, mean about 17 hours. Ethinyl estradiol exhibits a longer half-life due to enterohepatic recirculation and extensive tissue distribution.
Renal: 30% as unchanged drug and metabolites; biliary/fecal: 70% as metabolites.
Norethindrone is primarily excreted renally (approximately 60-80% as metabolites) and approximately 20-40% fecally. Ethinyl estradiol is excreted renally (about 40%) and fecally (about 60%) as glucuronide and sulfate conjugates.
Category C
Category C
Oral Contraceptive
Oral Contraceptive