Estrogens / Progestins Flashcards
Conjugated equine estrogens
Natural water soluble estrogen
high dose b/c readily metabolized (0.624 mg)
ethinyl estradiol
synthetic steroid estrogen
mestranol
synthetic steroid estrogen
diethylstilbestrol (DES)
first synthetic nonsteroidal estrogen
not used much today
Pharmacological uses of estrogen
Hypogonadism (promote development of female sex organs)
HRT (maintain bone density / suppress hot flashes / suppress urogenital atrophy)
Contraception (negative feedback on HPG axis -> inhibit ovulation)
Acne Tx (suppress steroidogenesis / ↑ SHBG)
Estrogen Side-Effects
Breast tenderness (proliferation effect)
Endometrial hyperplasia (use progestin to challenge this)
↑ coagulation (↓ antithrombin)
cholestatis (cholesterol secretion changes)
nausea / migraine / cancer / bloating
Estrogen and Cancer
HRT (monotherapy): endometrial CA
Contraception: ↓ ovarian, ↓ endometrial, ↑ breast cancer
due to trophic effecs of hormones + ROS of metabolism
medroxyprogesterone (MPA)
Depo-Provera
progestin
Rx: HRT (w/ estrogen) / long acting contraceptive
norethindrone
progestin
Rx: contraception
norgestrel
progestin
Rx: contraception
Pharmacological Use of Progestins
Contraception (negative feedback to HPG axis –> prevent ovulation + ↑ cervical mucus viscosity)
HRT (prevent endometrial hyperplasia)
Dysmenorrhea (decrease SM contractions, prostaglandin production)
Endometriosis (↓ enometrial proliferation)
Progestin Side Effects
Break-through bleeding
Impaired glucose tolerance
Lipid metabolism changes
19-nor: acne / hirsutism
Injectable Birth Control
“Depo-provera”
(Progesterone)
Estrogen + Progestin
Implant Birth Control
Progestin
IUD Birth Control
Progestin