Female Pharmacology

Question 1

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

Answer 1

estradiol > estrone > estriol

Question 2

aromatase converts androstenedione to ______ and testosterone to ______

Answer 2

estrone; estradiol

Question 3

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

Answer 3

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

Question 4

most potent estrogen available

Answer 4

ethinyl estradiol

Question 5

mestranol: mechanism of action

Answer 5

converted to ethinyl estradiol

Question 6

effect of progesterone on GnRH

Answer 6

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

Question 7

therapeutic uses of estrogens

Answer 7

combination oral contraceptives, postmenopausal hormone replacement therapy, ovarian failure

Question 8

toxicities and contraindications of estrogens

Answer 8

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

Question 9

first-line therapy for infertility caused by anovulation

Answer 9

clomiphene (antagonist at estrogen receptors in hypothalamus)

Question 10

clomiphene: mechanism of action, side effects

Answer 10

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

Question 11

therapy for ER/PR+ breast cancer

Answer 11

tamoxifen

Question 12

tamoxifen: mechanism of action, side effects, use

Answer 12

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

Question 13

treatment for osteoporosis in postmenopausal women

Answer 13

raloxifene

Question 14

raloxifene: mechanism of action, side effects, use

Answer 14

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

Question 15

aromatase inhibitors: name 3, use, side effect

Answer 15

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

Question 16

drug used to terminate pregnancy

Answer 16

mifepristone

Question 17

mifepristone: mechanism of action, use, side effects

Answer 17

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

Question 18

medication used as emergency contraception

Answer 18

ulipristal

Question 19

ulipristal: mechanism of action, use

Answer 19

partial agonist of progesterone receptors, blocks ovulation

use: postcoital emergency contraception