A.9- Estrogens and antiestrogens

Question 1

function of estrogens (ovarian hormones)

Answer 1

1. female reproductive development
2. metabolic effects- TG ↑ HDL ↑ LDL ↓
3. blood coagulability ↑
4. bone resorption ↓

Question 2

list estrogen drugs

Answer 2

Premarin (conjugated estrogen)
Ethinyl-estradiol
Mestranol

Question 3

how is Premarin given?

Answer 3

oral, parenteral, transdermal patch

Question 4

indications for estrogen drugs

Answer 4

hypogonadism in girls
hormone replacement therapy
prevent bone loss and osteoporosis
oral hormone contraceptives (Ethinyl-estradiol, mestranol)

Question 5

SE of estrogens

Answer 5

moderate: bleedings, nausea, breast tenderness
severe: thromboembolism, gallbladder disease, hypertriglyceridemia, migraine, depression, hypertension

Question 6

estrogen given to postmenopausal women can increase risk for

Answer 6

breast cancer
endometrial hyperplasia and cancer
cardiovascular events

Question 7

types of anti-estrogens

Answer 7

1. SERM- selective estrogen receptor modulators
2. estrogen receptor antagonists
3. synthesis inhibitors
4. GnRH analogs and antagonists

Question 8

list SERM

Answer 8

Tamoxifen
Raloxifene
Clomifene

Question 9

how are SERM given?

Answer 9

oral

Question 10

indication for tamoxifen

Answer 10

hormone-responsive breast cancer

Question 11

SE for tamoxifen

Answer 11

hot flushes, thromboembolism, endometrial hyperplasia

Question 12

indication for Raloxifene

Answer 12

treatment of postmenopausal osteoporosis

Question 13

indication for clomifene

Answer 13

ovulation induction

Question 14

what is fulvestrant?

Answer 14

estrogen receptor antagonist

Question 15

how do we give fulvestrant?

Answer 15

intramuscular injection

Question 16

when is fulvestrant given?

Answer 16

breast cancer ( resistant to tamoxifen-1st line therapy)

Question 17

what are: Letrozole, exemestrane, anastrazole ?

Answer 17

aromatase inhibitors

Question 18

when do we give aromatase inhibitors?

Answer 18

adjuvant treatment of hormone-responsive breast cancer

Question 19

SE of Aromatase inhibitors (e.g anastrozole)

Answer 19

hot flushes, musculoskeletal disorders, ↓ bone mineral density

Question 20

what is Danazol?

Answer 20

estrogen synthesis inhibitor

Question 21

SE of Danazol

Answer 21

“Dana is fat, hairy, with pimples ..”

acne, hirsutism, weight gain, menstrual disturbances

Question 22

GnRH analogues

Answer 22

Leuprolide, Goserelin

Question 23

GnRH antagonists

Answer 23

Ganirelix, Degarelix