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16 Cards in this Set

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Selective Estrogen Receptor Modulators (SERM)
1. clomiphene
2. tamoxifen
3. raloxifen
clomiphene
Tx: amenorrheic/anovulatory women who want to get pregnant

MOA: blocks est receptors in hypo & pit so that no neg feedback from estrogen on GnRH and LH
==>incr FSH/LH secretion
==>gametogenesis & estrogen
==>ovulation

PE: 80% ovulate,
30-40% get pregnant

S/E: X-ind in women with hypercoagulation b/c clomiphene acts as gonist in liver
==>incr clotting factor synthesis
tamoxiphen
Tx:
*breast cancer
*prophylatic Tx in women with high risk of breast cancer

MOA:
*est antagonist at breast
*est agonist at
--uterus
==>endometrial hyperplasia
--liver
==>incr clotting factor synthesis
--bone (good)

S/E:
*Endometrial hyperplasia
--minimized by coadministration of PROGESTIN like:
-progesterone
-medroxy-progesterone
-norethindrone
-norgestimate
-norelgestromin
-levanorgestrel
raloxiphen
Tx: breast cancer that is estrogen-sensitive

MOA:
*est antagonist at breast & uterus
*est agonist at
--liver
--bone

S/E:
alenDRONATE, ibanDRONATE
(bisphosphanates)

Tx: post-menopausal women who do not want anything to touch their estrogen receptors but want to maintain bone density

MOA:
*drug incorporated into bone
*inhibits osteoclastic resorption of bone

PE: incr bone density

S/E: esophagitis

*take with only 6-8 oz water and remain standing for 30 minutes after (these are corrosive compounds and can aggravata LES if water level is too high in stomach and drug approach LES)
after using tamoxifen for 5 years, how Tx pt?
-switch to aromatase inhibitor:
*LETrozole
*ANAstrozole
S/E of endometrial hyperplasia
tamoxifen
S/E esophagitis
___dronate (bisphosphanate)
(corrosive compounds that can irritate LES)

prevent by stand up for 30 minute after take and take iwth only 6-8 oz water)
what drug take with only 6-8 oz water and remain standing for 30 min
__dronates (bisphosphanates)
aromatase inhibitors
LETrozole
ANAstrozole
letrozole
Tx:
1. women who have been on tamoxifen for 5 yrs
2. women who are not responsive to tamoxifen
3. women with estrogen-sensitive breast cancer
4. women with advanced metastatic breast cancer

PE: no estrogens at all!

MOA:
*pre-menopausal woman:
block conversion of
test==>estradiol in granulosa cell
*post-menopausal:
block conversion of
DHEA==>estrone in fat cells
anastrozole
Tx:
1. women who have been on tamoxifen for 5 yrs
2. women who are not responsive to tamoxifen
3. women with estrogen-sensitive breast cancer
4. women with advanced metastatic breast cancer

PE: no estrogens at all!

MOA:
*pre-menopausal woman:
block conversion of
test==>estradiol in granulosa cell
*post-menopausal:
block conversion of
DHEA==>estrone in fat cells
Tx women with est+ breas tcancer
letrozole
anastrozole
(aromatase - )
Tx women with advanced/metastastic breast cancer
letrozole
anastrozole
(aromatase - )
Tx women on tamoxifen for 5 yrs
letrozole
anastrozole
(aromatase - )
Tx women not responsive to tamoxifen
letrozole
anastrozole
(aromatase - )