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Flashcards in Female Pharmacology Deck (19):
1

list the 3 major estrogens in order of highest to lowest potency

estradiol > estrone > estriol

2

aromatase converts androstenedione to ______ and testosterone to ______

estrone; estradiol

3

compare the effects of estrogens and progestins on endometrium, cervical mucus, and uterine contractions

endometrium: estrogens cause proliferation, progestins decrease proliferation and leads to development of a secretory endometrium
cervical mucus: estrogens decrease viscosity and increase the amount, progestins increase viscosity and decrease the amount (scant viscid material)
uterine contractions: estrogens favor rhythmic contractions and progestins decrease contractions

4

most potent estrogen available

ethinyl estradiol

5

mestranol: mechanism of action

converted to ethinyl estradiol

6

effect of progesterone on GnRH

decreases frequency of GnRH pulses --> suppresses gonadotropin release (therefore used as hormonal contraceptive)

7

therapeutic uses of estrogens

combination oral contraceptives, postmenopausal hormone replacement therapy, ovarian failure

8

toxicities and contraindications of estrogens

toxicity: increased risk of endometrial cancer and thrombi
contraindications: pregnancy, estrogen-dependent cancer (ER+ breast cancer), history of DVTs

9

first-line therapy for infertility caused by anovulation

clomiphene (antagonist at estrogen receptors in hypothalamus)

10

clomiphene: mechanism of action, side effects

antagonist at estrogen receptors in hypothalamus; prevents normal feedback inhibition and inceases release of FSH and LH from pituitary, which stimulates ovulation
side effects: hot flashes, ovarian enlargement, multiple simultaneous pregnancies, visual disturbances

11

therapy for ER/PR+ breast cancer

tamoxifen

12

tamoxifen: mechanism of action, side effects, use

ER antagonist at breast; agonist at bone, uterus
side effects: hot flashes, increased risk of thromboembolic events and endometrial cancer
use: treat and prevent recurrence of ER/PR+ breast cancer

13

treatment for osteoporosis in postmenopausal women

raloxifene

14

raloxifene: mechanism of action, side effects, use

antagonist at breast, uterus, agonist at bone
side effects: increased risk of thromboembolic events but no increased risk of endometrial cancer (vs. tamoxifen), hot lashes
use: osteoporosis

15

aromatase inhibitors: name 3, use, side effect

letrozole, anastrozole, exemestane
use: treat ER+ breast cancer
side effect: hot flashes

16

drug used to terminate pregnancy

mifepristone

17

mifepristone: mechanism of action, use, side effects

competitive inhibitor of progestins and progesterone receptors
use: administered with misoprostol (PGE1) to terminate pregnancy
side effect: heavy bleeding, GI effects, abdominal pain

18

medication used as emergency contraception

ulipristal

19

ulipristal: mechanism of action, use

partial agonist of progesterone receptors, blocks ovulation
use: postcoital emergency contraception