estrogen and antiestrogen

Question 1

physiological function of estrogen

Answer 1

1) breast prolif.
2) bone integrity.
3) follice maturation
4) uterine growth
5) HDL increased, LDL decrease and TAG increase
6) anabolic effect: weight gain.
7) pro-coagulation.
8) increased stress and sympathetic activity.
9) secondary and primary growth.

Question 2

natural estrogen

Answer 2

1) estradiol, estrone and estriol.
2) phytoestrogen
3) equine estrogen

Question 3

synthetic estrogen, steroid-

Answer 3

ethinylestradiol, mestranol, quinestrol

Question 4

synthetic estrogen, non-steroid

Answer 4

benzestrol, methestrol, hexestrol, dienestrol .diethylstilbestrol and more.

Question 5

indications

Answer 5

1) hormone replacement therapy:
A) primary hypogonadism
B) post menopause- hot flashes and vaginal atrophy.
2)estrogen progestins:
Dysmenorrhea, amenorrhea and hirsutism, contraceptives,
Osteoporosis.

Question 6

kinetics:

Answer 6

natural steroid- high first pass metabolism- given transdermal, intravaginal (Cream tablet, ring), injection.
synthetic- good oral bioavailability.
hormones bind to albumin.
metabolized and exreted in urine

Question 7

adverse-

Answer 7

1) weight gain and acne and hyperpigmentation
2) increased thromboembolic risk
3) cancer- breast and endometrial
4) postmenopausal bleeding
5) headache, breast-tender.
6) GI- cholestasis, gallbladder disease and hepatic adenoma.

Question 8

diethylstilbestrol (DES)

Answer 8

vaginal carcinoma, taken off.

Question 9

contra

Answer 9

1. pregnancy.
2. estrogen dependent cancer.
3. liver disease.
4. thromboembolic past events.
5. undiagonsed genital bleed.

Question 10

SERMS-

Answer 10

Tamoxifen-breast cancer,
raloxifen- breast cancer and osteoporsis (agonist effect in bone), also no risk for endometrial cancer.
toremifene- breast cancer
clomiphene- fertility pill- partial estrogen agonist in the hypothalamus-> gnrh release-> ovulation.

Question 11

ospemifene

Answer 11

used for painful intercourse

Question 12

kinetics of SERMS

Answer 12

oral and then bile excretion

Question 13

adverse of SERMS

Answer 13

1) increased risk for PE and DVT.
2) hot flashes, nausea.
3) increased risk for cancer- endometrial (raloxifene does not cause it but tamoxifene and toremifene do).

Question 14

antiestrogens

Answer 14

fulvestrant- indicated for cancer resistant tamoxifene, given IV– estrogen receptor antagonist.

armomatase inhibitors- exemestane and formestane-
like fulvestrant