Reproductive Pharmacology (590-592)

Question 1

what is leuprolide

Answer 1

GnRH analog that acts as an agonist when pulsatile and an antagonist when continuous

Question 2

what is leuprolide used to treat

Answer 2

infertility (given pulsatile);
prostate cancer (continuous infusion with flutamide);
uterine fibroids (continuous);
precocious puberty (continuous)

Question 3

what are the toxicities of leuprolide

Answer 3

antiandrogenic, nausea, vomiting

Question 4

what are estrogens (ethinyl estradiol, diesthylstilbestrol and mestranol) used to treat

Answer 4

hypogonadism or ovarian failure, menstrual abnormalities, hormone replacement therapy in postmenopausal women, androgen-dependent prostate cancer

Question 5

what are the toxicities of exogenous estrogens

Answer 5

increased risk of endometrial cancer, bleeding in postmenopausal women, DES in utero exposure causes vaginal clear cell adenocarcinoma, increased risk of thrombi, contraindicated in women with ER pos. breast cancer

Question 6

name three selective estrogen receptor modulators (SERMs) and where they each work

Answer 6

clomiphene, tamoxifen and raloxifene

Question 7

how/where does clomiphene work

Answer 7

estrogen receptor antagonist in hypothalamus; prevents feedback inhibition ==> increased LH and FSH

Question 8

what is clomiphene used to treat

Answer 8

infertility due to anovulation (e.g. PCOS)

Question 9

toxicities of clomiphene

Answer 9

hot flashes, multiple simultaneous pregnancies, ovarian enlargement, visual disturbances

Question 10

how/where does tamoxifen work

Answer 10

estrogen receptor antagonist in breast tissues; estrogen receptor agonist in bone and uterus

Question 11

what are the toxicities of tamoxifen

Answer 11

endometrial cancer, thromboemolism

Question 12

what is tamoxifen used to treat

Answer 12

ER positive breast cancer

Question 13

how/where does raloxifene work

Answer 13

estrogen receptor agonist in bone; estrogen receptor antagonist in uterus

Question 14

what does raloxifene treat

Answer 14

treats osteoporosis by decreasing bone resorption

Question 15

what is the toxicity associated with raloxifene

Answer 15

increased risk of thromboembolism

Question 16

why is progesterone added to estrogen in hormone replacement therapy

Answer 16

unopposed estrogen causes

Question 17

what are anastrozole and exemestane used for and what do they do

Answer 17

aromatase inhibitors used to treat postmenopausal women with breast cancer

Question 18

how do progestins work

Answer 18

they bind progesterone receptors to decrease endometrial growth (by opposing estrogen) and increase vascularization of the endometrium

Question 19

what are progestins used to treat

Answer 19

used in OCP’s, to treat endometrial cancer and to treat abnormal uterine bleeding

Question 20

how does mifepristone (RU-486) work

Answer 20

competitive inhibitor of progestins and progesterone receptor

Question 21

what is mifepristone used for

Answer 21

administered with misoprostol to terminate pregnancies

Question 22

toxicities of mifepristone

Answer 22

heavy bleeding, nausea vomiting, anorexia, abdominal pain

Question 23

how do oral contraceptives prevent ovulation

Answer 23

progestins and estrogens feedback negatively to decrease LH and FSH, preventing LH surge and thereby preventing ovulation

Question 24

contraindications of oral contraceptives

Answer 24

smokers over the age of 35, history of thromboembolic disease or stroke, history of estrogen-dependent tumor

Question 25

what is terbutaline and what does it do

Answer 25

beta-2 agonist that decreases frequency of uterine contractions during labor

Question 26

what is danazol

Answer 26

synthetic androgen that acts as a partial agonist of androgen receptors (causes negative feedback on gonadotropins)

Question 27

what is danazol used to treat

Answer 27

endometriosis and hereditary angioedema

Question 28

what are the side effects of danazol

Answer 28

danazol has been largely replaced by leuprolide as a treatment for endometriosis because of side effects of weight gain, edema, acne, hirsutism, hepatotoxicity, decreased HDL, masculinization

Question 29

what are testosterone and methyltestosterone used to treat

Answer 29

to treat secondary hypogonadism, stimulation of anabolism to promote recovery after burn or injury