Fitzaekerly: Antineoplatic Hormonal Drugs

Question 1

cancers depend on this for growth

Answer 1

steroids

Question 2

benefit of steroid dependent cancer

Answer 2

predict whether cancer will respond to tx (take biopsy and see if receptors are present)

Question 3

Drugs that inhibit LH and FSH secretion

Answer 3

GnRH analogues

GnRH antagonist

Question 4

Goserelin

leuprolide

Answer 4

GnRH analogues

Question 5

how do GnRH analogues cause a flare response

Answer 5

mimic release of GnRH>
increase in FSH/LH>
increase in testosterone/estrogen>
FLARE (increase in cancer growth/bone pain)

Question 6

long term continuous administration of GnRH analogue

Answer 6

increase in steady state concentrations>
decrease receptor expression in pituitary>
decrease in FSH/LH>
decrease in estrogen/testosterone>
decrease in GnRH expression

Question 7

how are GnRH analogues administered

Answer 7

depot form

Question 8

TU of Goserelin and Leuprolide

Answer 8

advanced prostate cancer

PRE-MW w/ ER + breast cancer

Question 9

acute toxicity of GnRH analogues

Answer 9

flare response> bone pain
pain at injection site

*can lead to decreased hormone levels long term

Question 10

Degarelix

Answer 10

GnRH antagonist

Question 11

Why may Degarelix be preferred over a GnRH analogue?

Answer 11

NO flare response
FASTER decrease in testosterone levels

injection site rxn is only toxcitiy

EXPENSIVE

Question 12

Dutasteride

Finasteride

Answer 12

5 alpha reductase inhibitors

Question 13

MOA of Finasteride

Answer 13

inhibits converstion of testosterone to DHT> decreased cell growth

Question 14

used to tx:
BPH
Male pattern baldness
prevention in prostate cancer pts w/ high PSA

Answer 14

Finasteride

Question 15

TERATOGENCITIY

impotence

Answer 15

Finasteride

*may lessen decrease in bone density/muscle wasting!!

Question 16

abiraterone acetate

Answer 16

17 alpha hydroxylase

Question 17

blocks early stages of androgen syntehsis but DOES NOT INTERFERE w/ conversion of pregnenolone

Answer 17

17 alpha hydroylase

Question 18

used to tx:

metastatic prostate cancer that is resistant to other androgen blocking regimens

Answer 18

abiraterone acetate

Question 19

Irreversibly binds and inhibits aromatase

Answer 19

exemastane

Question 20

first line non steroidal aromatase inhibitors

Answer 20

anastrozole

letrozole

Question 21

3rd line non steroidal aromatase inhibiotr

Answer 21

aminoglutethimide

Question 22

why is aminoglutethimide a third line tx?

Answer 22

decreases concentrations of adrenal glucocorticoids, mineralcorticoids, sex hormones

Question 23

blocks the conversion of testosterone/adrostenedione to estradiol and estrone

Answer 23

aromatase inhibitors

Question 24

which aromatase inhibotrs REVERSIBLY block the enzyme

Answer 24

non steroidals

Question 25

1st line tx for ER+ breast cancer in POST MW

Answer 25

Aromatase inhibitors

Question 26

ADRENAL INSUFFICIENCY toxicity | F, Nausea, rash, HA

Answer 26

aminoglutethamide > ultimately leads to increase in ACTH> increase in cortisol and bone marrow suppression

Question 27

``` POLYARTHRALGIA decreased bone density increased hot flashes Nausea HA ```

Answer 27

Anastrazole letrozole exemestane

Question 28

Bicalutamide flutamide nilutamide

Answer 28

anti androgens

Question 29

decrease binding of Test to receptor> increase in LH/FSH> increased production of testosterone

Answer 29

Bicalutamide flutamide nilutamide

Question 30

not given ALONG or for very long because of SE and are often used w/ GnRH analogue (goserelin/leuprolide) to prevent FLARE response

Answer 30

Anti-androgens

Question 31

androgen deprivation therapy

Answer 31

main stay of prostate cancer tx

Question 32

NSSA + GnRH agonist

Answer 32

complete androgen blockade

Question 33

newer anti-androgens that have decreased toxicity

Answer 33

bicalutamide | nilutamide

Question 34

DECREASE IN SEXUAL FXN HOT FLASHES DECREASE IN LVIER FXN METHENOGLOBINEAMIA

Answer 34

anti-androgens

Question 35

MOA of anti-estrogens

Answer 35

compete w/ estrogen for binding to estrogen receptor

Question 36

raloxifene tamoxifen toremifene

Answer 36

SERMS | partial agonists

Question 37

Fulverstrant

Answer 37

SERD | full antagonist

Question 38

these drugs will give you NO benefit after 5 yrs are taken orally and take 4-6 weeks to reach a steady state

Answer 38

SERM

Question 39

given IM at 1 month internvals | and take only 7 mos to reach a steady state

Answer 39

SERD

Question 40

which anti-estrogen is metabolized in the liver by CYP3A?

Answer 40

SERD

Question 41

mainstay tx for ER+ cancers in POST MW

Answer 41

Anti-estrogens

Question 42

what drugs are NOT used in PRE-MW b/c of feedback loop?

Answer 42

anti-estrogens

Question 43

Tamoxifen is most effective in what cancers

Answer 43

ER+ PR+

Question 44

affect of estrogen on tissues

Answer 44

poliferative in breast and uterus | prevents bone resorption

Question 45

decrease in estrogen can lead to hot flashes, N and V

Answer 45

anti-estrogens

Question 46

agonist in the uterus that can lead to an increase in endometrial cancer

Answer 46

tamoxifen

Question 47

anti-androgen that can cause GI problems, HA, back pain and injection site rxns

Answer 47

fulverstrant

Question 48

which mechanism of antineoplastic drugs is NOT used in bresat cancer therapy

Answer 48

differntiating agents

Question 49

Cytotoxic Drug regimens for BC

Answer 49

FAC: Fu, Doxo, cyclophosphamide (used until reach max dose of doxo b/c of cardiotoxicity) CMF: cyclo, MTX, 5-FU

Question 50

target ER + BC

Answer 50

tamoxifen, tormifene, fulverstrant | anastrazole, letrozole, exemestane

Question 51

used to tx her2NEU cancers

Answer 51

trastuzumab