Comparative Pharmacology
Head-to-head clinical analysis: LEVONORGESTREL versus PROVERA.
Head-to-head clinical analysis: LEVONORGESTREL versus PROVERA.
LEVONORGESTREL vs PROVERA
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Synthetic progestin that suppresses gonadotropin release (GnRH, LH, FSH) via negative feedback on the hypothalamic-pituitary-ovarian axis; inhibits ovulation, thickens cervical mucus, and alters endometrial lining.
Provera (medroxyprogesterone acetate) is a progestin that binds to progesterone receptors, suppressing gonadotropin secretion, inhibiting endometrial growth, and inducing secretory changes in the endometrium. It also has antigonadotropic effects by reducing LH and FSH release from the pituitary.
For emergency contraception: 1.5 mg orally as a single dose or 0.75 mg orally 12 hours apart. For hormonal contraception: 0.03 mg to 0.05 mg orally once daily in combined oral contraceptives; for progestin-only oral contraceptive (mini-pill): 0.03 mg orally once daily. For intrauterine system (IUD): 52 mg intrauterine device inserted for up to 5 years.
Oral: 5-10 mg daily for 5-10 days for secondary amenorrhea; 5-10 mg daily for 12-14 days per cycle in combination with estrogen for endometrial hyperplasia; 400-1000 mg/day IM monthly for endometriosis.
None Documented
None Documented
Clinical Note
moderateLevonorgestrel + Sulfisoxazole
"The metabolism of Sulfisoxazole can be decreased when combined with Levonorgestrel."
Clinical Note
moderateLevonorgestrel + Erythromycin
"The metabolism of Erythromycin can be decreased when combined with Levonorgestrel."
Clinical Note
moderateLevonorgestrel + Cyclosporine
"The metabolism of Cyclosporine can be decreased when combined with Levonorgestrel."
Clinical Note
moderateLevonorgestrel + Fluconazole
Terminal half-life: 24-30 hours (range 11-45 hours). This prolonged half-life supports once-daily or extended-cycle dosing in contraceptive formulations.
Terminal elimination half-life is approximately 12-17 hours for medroxyprogesterone acetate (oral). With depot intramuscular injection, the half-life is extended to approximately 50 days due to slow absorption from the injection site.
Renal: 45-60% (metabolites), Fecal: 32-45% (unchanged and metabolites). Biliary excretion contributes to fecal elimination.
Renal (50-60% as metabolites), biliary/fecal (30-40%). Less than 1% excreted unchanged.
Category C
Category C
Progestin
Progestin
"The metabolism of Fluconazole can be decreased when combined with Levonorgestrel."