Hormones and their Antagonists

Question 1

Glucocorticoids

Answer 1

inhibit mitosis in lymphocytes

DO NOT induce myelosuppression

Question 2

Prednisone USES & MOA

Answer 2

type of glucocorticoid

1) ALL
2) MOPP/CHOP regimen, multiple myeloma, CLL

Question 3

Dexamethasone MOA & USE

Answer 3

type of glucocorticoid

1) use w/ radiation to reduce edema in brain/spinal tumors

Question 4

Tamoxifen MOA

Answer 4

SERM = selective estrogen receptor modulator
competes with estradiol for binding to the ER = makes nonfxnal ER-hormone complex
stabilizes or even increases ER expression

Question 5

Tamoxifen USES

Answer 5

ER + metastatic breast cancer
adjuvent therapy for excision
prevention for high risk people
BEST For post-menopausal women because lower affinity for receptor than estradiol

Question 6

Tamoxifen Toxicity

Answer 6

1) hot flashes, hair loss
2) increased risk of endometrial cancer
3) increased risk for thromboembolic events

Question 7

Fulvestrant MOA

Answer 7

selective estrogen-receptor downregulators (SERDs)
pure ANTI-estrogen
1) binds to ER with much higher affinity than tamoxifen
2) inhibits dimerization of ER, increases degradation
3) reduces number of ER molecules in cells

Question 8

Fulvestrant USES

Answer 8

postmenopausal women with ER + metastatic breast cancer

Question 9

Aromatase Inhibitors (AIs) Name & MOA, use

Answer 9

Anastrozole
selective inhibitor of aromatase = profound estrogen deprivation
ER + breast cancer postmenopausal women

Question 10

Leuprolide (Lupron) & Goserelin (Zoladex)

Answer 10

GnRH analogs
bind to GnRH receptor
Inhibit release of FSH & LH
Reduced testicular production of testosterone

Question 11

Flutamide & Bicalutamide

Answer 11

nonsteroidal androgen-receptor blockers

prevents translocation of AR to nucleus