estrogen and antiestrogen Flashcards Preview

pharmacology second semsester > estrogen and antiestrogen > Flashcards

Flashcards in estrogen and antiestrogen Deck (14):
1

physiological function of estrogen

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.

2

natural estrogen

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

3

synthetic estrogen, steroid-

ethinylestradiol, mestranol, quinestrol

4

synthetic estrogen, non-steroid

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

5

indications

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

6

kinetics:

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

7

adverse-

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.

8

diethylstilbestrol (DES)

vaginal carcinoma, taken off.

9

contra

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

10

SERMS-

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.

11

ospemifene

used for painful intercourse

12

kinetics of SERMS

oral and then bile excretion

13

adverse of SERMS

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).

14

antiestrogens

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

armomatase inhibitors- exemestane and formestane-
like fulvestrant