Gonadal Hormones and Inhibitors

Question 1

Clinical applications of ethinyl estradiol

Answer 1

Hypogonadism in girls, women
OCP, parenteral contraceptive (combined with a progestin)
Intractable dysmenorrhea or uterine bleeding

Question 2

Moderate toxicities of ethinyl estradiol

Answer 2

Breakthrough bleeding, nausea, breast tenderness

Question 3

Serious toxicities of ethinyl estradiol

Answer 3

Thromboembolism, gallbladder disease, hypertriglyceridemia, migraine headache, HTN, depression
In postmenopausal women: breast cancer, endometrial hyperplasia

Question 4

Mestranol

Answer 4

A prodrug that is converted to ethinyl estradiol, contained in some contraceptives

Question 5

Long-acting estrogens administered IM and used for hypogonadism in young females

Answer 5

Estrogen esters (eg, estradiol cypionate)

Question 6

What type of hormonal receptors does norgestrel activate?

Answer 6

Progesterone

Question 7

Clinical uses of norgestrel

Answer 7

Contraception: oral in combination with estrogen, as an IUD, or as a postcoital contraceptive

Question 8

Adverse effects of norgestrel

Answer 8

weight gain, reversible decrease in bone mineral density (high doses)

Question 9

MOA of Tamoxifen

Answer 9

Estrogen antagonist in breast tissue and CNS

Estrogen agonist effects in endometrium, liver, and bone

Question 10

Clinical use of tamoxifen

Answer 10

prevention and adjuvant treatment of hormone-responsive breast cancer

Question 11

Adverse effects of tamoxifen

Answer 11

Hot flushes, thromboembolism, endometrial hyperplasia

Question 12

SERM approved for osteoporosis and prevention of breast cancer in selected patients

Answer 12

Raloxifene

Question 13

MOA of raloxifene

Answer 13

Antagonist effects in breast, CNS, and endometrium;

agonist effects in the liver

Question 14

SERM used for ovulation induction

Answer 14

Clomiphene

Question 15

MOA of clomiphene

Answer 15

Estrogen antagonist in pituitary –> increases LH, FSH secretion

Question 16

MOA of fulvestrant

Answer 16

Estrogen receptor antagonist in all tissues. IM admin.

Question 17

What is fulvestrant used for?

Answer 17

Adjuvant treatment of hormone-responsive breast cancer that is resistant to first-line anti estrogen therapy

Question 18

Aromatase inhibitors used in adjuvant treatment of hormone-responsive breast cancers

Answer 18

Anastrozole, Letrozole, and exemastane (irreversible)

Question 19

Adverse effects of aromatase inhibitors

Answer 19

Hot flushes, musculoskeletal disorders, reduced bone mineral density
Joint symptoms (arthralgia, arthritis, arthritis, cervical spondylosis, osteoarthritis, and disk herniation)

Question 20

GnRH agonist; used in controlled ovarian hyperstimulation and also for the treatment of precocious puberty in children and short-term (

Answer 20

Leuprolide

Question 21

GnRH antagonists used for controlled ovarian hyperstimulation

Answer 21

Ganirelix, cetrorelix

Question 22

Weak cytochrome P450 inhibitor and partial agonist of progestin and androgen receptors

Answer 22

Danazol

Question 23

What is danazol used for?

Answer 23

Endometriosis, fibrocystic breast disease

Question 24

Adverse effects of danazol

Answer 24

Acne, hirsutism, weight gain, menstrual disturbances, hepatic dysfunction

Question 25

MOA of finasteride, dutasteride

Answer 25

5alpha-reductase inhibitors

Question 26

What is finasteride used for?

Answer 26

BPH, male-pattern hair loss

Question 27

Possible side effects of finasteride

Answer 27

Rarely, impotence, gynecomastia

Question 28

Competitive inhibitors of androgen receptors

Answer 28

flutamide, bicalutamide, nilutamide (bicalutamide and nilutamide have lower risk of hepatotoxicity)

Question 29

Adverse effects of flutamide?

Answer 29

Gynecomastia, hot flushes, impotence, hepatotoxicity

Question 30

What type of cancer can ketoconazole be used to to treat?

Answer 30

Advanced prostate cancer that is resistant to first-line anti androgen drugs