Estrogen & Progestin Drugs Flashcards
17-beta-estradiol (E2)
oral, transdermal, vaginal estrogen
Esters of 17-beta-estradiol (EE)
longer half life/more soluble estrogen
oral/IM
Estrone Sulfate
Oral synthetic estrogen
Premarin
conjugated equine estrogen
Ethinyl estradiol
oral birth control pill estrogen
Ethyl at postition 17 decreases hepatic degradation
Estrogen Side Effects
Oral increases hepatic production TBG, CBG, SHBG, TGs, HDL, cholesterol, & clotting factors
Tamoifen
SERM
Breast cancer
Endometrial cancer risk
Raloxifen
SERM
Osteoporosis
Toremiphene
SERM
Breast cancer
Endometrial cancer risk
Clomiphene
SERM
Infertility
Fulvestrant
Anti-estrogen
Full antagonist
Monthly IM
Breast Cancer
Aromatase Inhibitor
Anti-estrogen
Prevents androgen -> estrogen
Breast cancer (postmenopausal)
SE: joint probs, osteoporosis, hypercholesterolemia
Progesterone
oral, oil, vaginal, IUD
Provera/Depo-provera
Progesterone Esters
Longer
Oral vs IM
19-norestosterone derivatives
Primary component in OCs
Oral, subdermal, ethinyl estradiol, vaginal ring, transdermal
Progestin SE
Weight gain, depression, acne, thromboembolic, weak androgenic, breast discomfort, break through bleeding
Mefipristone
Anti-progestin at uterus to terminate pregnancy
Given w/PGEs
Can also be postcoital contraceptive
SE: bleeding, N/V, diarrhea
Estrogen Receptor A
Endometrium, breast cancer cells, & ovarian stroma
ERb
Granulosa cells & nonclassic tissues (lung, kidney, bone, etc)
Estrogen-like compounds
Phytoestrogens:
Isofalvones - soybeans, chickpeas, lentils
Coumestans - split peas, lima & pinto beans
Lignans - flaxseed, lentils, grains, F/V
Bisphenol A: synthetic in plastics
