Pharm: estrogen (ethinyl estradiol, DES, mestranol)

Question 1

MOA

Answer 1

Bind estrogen receptor

Question 2

Use

Answer 2

Hypogonadism or ovarian vailure
Menstrual abnormalities
HRT in postmenopausal
Use in men with androgen dependent prostate cancer

Question 3

Toxicity

Answer 3

Increased risk of endometrial cancer
Bleeding in postmenopausal women
Clear cell adnocarcinoma of vagina (DES in utero)
Increased risk of thrombi

Contraindicated in ER positive breast cancer, hx of DVT

Question 4

SERMS:

Answer 4

1) clomiphene
2) tamoxifen
3) raloxifen

Question 5

SERM: clomiphene

Answer 5

Partial agonist in hypothalamus, which prevent normal feedback inhibition and increase release of LH and FSH from pituitary=> ovulation

Used to treat infertility and PCOS

May cause hot flashes, ovarian enlargement, multiple pregnancies, visual disturbances

Question 6

SERM: tamoxifen

Answer 6

Antagonist in breast tissue;

used to treat and prevent recurrence of ER positive breast cancer

Question 7

SERM: raloxifen

Answer 7

Agonist on bone;
reduce resorption of bone
used to treat osteoporosis

Question 8

Hormone replacement therapy: use

Answer 8

For relief or prevention of menopausal symptoms;
(hot flashes, vaginal atrophy) and osteoporosis
(high estrogen reduces osteoclast activity)

Question 9

Hormone replacement therapy: risk

Answer 9

Unopposed estrogen replacement therapy
increases risk of endometrial cancer so progesterone is added

Possible increased CV risk