A - 9. Estrogens and antiestrogens

Question 1

Estrogen receptor locations

Answer 1

Alpha

• vagina
• ovaries
• breasts
• hypothalamus
• blood vessels

Beta

• prostate
• ovaries

Question 2

Estrogen function/role

Answer 2

• Contraction of myometrium and fallopian tubes
• Eases sperm travel, thins out vaginal secretion
• Promotes breast tissue proliferation
• Osteoclastic activity decrease
• HDL up, LDL down
• Salt and water retention (edema)
• Coagulability increase
• Induction of progresterone synthesis

Question 3

Coagulability and estrogen; why?

Answer 3

Increased factor II, VII, IX and X production

Decreased antithrombin III production

Question 4

Natural estrogen

Answer 4

ESTRADIOL estrone -> estriol

not effective orally - high first pass metabolism

Question 5

Synthetic estrogen

Answer 5

Ethinylestradiol

Question 6

Estrogen treatment indication

Answer 6

1. HRT in post menopausal women
2. Osteoporosis
3. Senile vaginitis
4. Dysmenorrhea
5. Delayed female puberty
6. Prostate cancer - improve quality of life

Question 7

SE of estrogen treatment

Answer 7

Nausea, vomiting, tenderness, thromboembolism

Question 8

Competative estrogen receptor blockers

Answer 8

Clomifen

Indication: infertility, assisted reproduction
SE:
- ovarian hyperstimulation -> cysts and cancer
- hair loss
- hot flashes
- weight gain
- multiple pregnancies

Question 9

Aromatase inhibitors

Answer 9

Anastrozolone

Blocks testosterone -> estradiol conversion
Used in breast cancer
SE: hot flashes, probably more

Question 10

Partial agonists/selective action drugs; names

Answer 10

Tamoxifen
Raloxifen

Only active in absence of androgens (will be antagonistic in presence of ligand)

Indications

• osteoporosis (agonistic)
• breast cancer (antagonistic)
• endometrial cancer (antagonistic)

Question 11

Other antiandrogens mentioned in earlier topics

Answer 11

goserelin

degarelix