Hormonal Cancer Management Flashcards
Selective Estrogen Receptor modulator Drugs
Tamoxifen
Raloxifene
Tamoxifen Mechanism
Block Estrogen-R
antagonist to estradiol
partial agonist in uterus
Tamoxifen Use
ER positive tumors
prevent breast cancer
Tamoxifen Side Effects
Risk of endometrial cancer
hot flashes
thromboembolic events (DVT)
Raloxifene Mechanism
Block Estrogen-R
antagonist to estradiol
partial agonist in bone
Raloxifene Use
prevent breast cancer
Raloxifene Side Effects
Increase Thromboembolic events (DVT)
Fulvestrant mechanism
Selective Estrogen Receptor Downregulator (SERD)
binds Estrogen-R with high affinity to decrease receptor numbers
Fulvestrant Use
ER positive breast cancer
follows tamoxifen when it is no longer effective
Fulvestrant Side Effects
N/V
Hot Flashes
GI symptoms
Aromatase Inhibitor Drugs
Anastrozole
Letrozole(non-steroidal)
Exemestane(steroid: non-reversible)
Anastrozole Mechanism
Convert Androstenedion and testosterone into estrone and estradiol
Anastrozole Use
First line in menopausal women with ER positive breast cancer who cannot tolerate Tamoxifen
5 years of Tamoxifen followed by 2.5 years of aromatase inhibitor
Anastrozole Side Effects
N/V
hot flashes, fatigue
risk bone loss and fracture
Less than thrombosis than Tamoxifen
Letrozole Mechanism
Non-steroidal
Convert Androstenedion and testosterone into estrone and estradiol