Fitzakerly: Antineoplastics IV

Question 1

what are 2 GnRH analogs? what are their 2 therapeutic uses?

Answer 1

Goserelin and Leuprolide!

Prostate and breast cancer!

Question 2

what side effects (2) are associated with GnRH analogs? Why?

Answer 2

(1) flare response at injection site (2) pain at injection site. Since they are ANALOGUES they will initially stimulate the system, takes about 7-10 days to REDUCE levels at a CONTINUOUS administration

Question 3

what is used in conjunction with Goserelin/Leuoprolide, in PROSTATE CANCER, to decrease the initial ‘flare response’? what are their mechanisms of action?

Answer 3

Anti-androgen (decrease ligand binding therefore inhibiting translocation of receptor -> increased FSH/LH levels -> testosterone HOWEVER the receptors are blocked so it doesnt matter that there are increased gonadotropin levels). “-UTAMIDE”. Bicalutamide, flutamide, nilutamide.

Question 4

Name that drug! GnRH competitive ANTAGONIST

Answer 4

DEGARELIX

Question 5

T or F: GnRH antagonists, such as Degarelix, also have a flare like GnRH analogues (Goserelin, leuprolide)

Answer 5

FALSE. they are ANTAGONISTS and have NO FLARE.

Question 6

What side effects are associated with GnRH antagonists?

Answer 6

generally WELL TOLERATED, injection site rxn possiblitity

Question 7

Does Degarelix, a GnRH competitive antagonist, work on: (A) only breast cancer (b) only prostate cancer (c) both breast and prostate cancer (d) breast and ovarian cancer

Answer 7

B. PROSTATE ONLY!

Question 8

What are 2 ANDROGEN BIOSYNTHESIS INHIBITORS? And what specific ENZYME do they inhibit?

Answer 8

Dutasteride and FINASTERIDE (“-steride”). 5 alpha reductase inhibitor, therefore blocking the testosterone conversion to DHT!

Question 9

What drugs do we use for BPH, male pattern baldness, AND prostate cancer prevention (pt w/increase PSA)?

Answer 9

Finasteride, dutasteride

Question 10

What is an ANDROGEN BIOSYNTHESIS INHIBITOR, other than finasteride and dutasteride? what specifically does it inhibit?

Answer 10

ABRATERONE ACETATE. CYP 17 inhibitor!

Question 11

What drug is used for metastatic prostate cancer that is resistant to other androgen blocking regimens?

Answer 11

ABRATERONE ACETATE

Question 12

What is a REVERSIBLE aromatase inhibitor? Is it steroidal or non-steroidal?

Answer 12

AMINOGLUTETHIMIDE. NONsteroidal

Question 13

what is a (3rd line) drug to use for breast cancer in POST-MENOPAUSAL women?

Answer 13

AMINOGLUTETHIMIDE

Question 14

AMINOGLUTETHIMIDE can be used in:
(A) pre-menopausal women with breast cancer and prostate cancer
B) post-menopausal women with breast cancer and prostate cancer
C) all women with breast cancer and prostate cancer

Answer 14

B. DONT USE AROMATASE INHIBITORS on premenopausal women!

Question 15

What is the toxicity associated with AMINOGLUTETHIMIDE?

Answer 15

fever, nausea, rash, HA. ADRENAL INSUFFICIENCY (Tx: hydrocortisone) but increases ACTH -> increase cortisol -> Bone marrow suppression = BAD BAD BAD

Question 16

what are the two 1st line NON-steroidal REVERSIBLE aromatase inhibitors?

Answer 16

ANASTROZOLE, LETROZOLE

Question 17

what type of REVERSIBLE aromatase inhibitors are used for only BREAST CANCER? hint: nonsteroidal

Answer 17

ANASTROZOLE, LETROZOLE

Question 18

What type of drug is EXEMESTANE?

Answer 18

an IREVERSIBLE AROMATASE INHIBITOR. aka steroid analogue (‘suicide inhibitors’)

Question 19

what is the therapeutic use for an irreversible aromatase inhibitor?

Answer 19

BREAST CANCER

Question 20

what side effect is associated with Exemastane?

Answer 20

Polyarthralgias

Question 21

which breast cancer drug specifically increases appetite ?

Answer 21

Exemastane

Question 22

what is BICALUTAMIDE, FLUTAMIDE, NILUTAMIDE used for? is it given for a short or long period of time?

Answer 22

these are anti-androgens and are given for the ‘flare rxn’ with GnRH analogues.

Question 23

what toxicities are associated with bicalutamide, flutamide and nilutamide?

Answer 23

HEPATOTOXICITY. RARE: methenoglobinemia

Question 24

What is TAMOXIFEN’s MOA? what is its clinical use then?

Answer 24

SERMs (ER ANTAGONIST). BREAST CANCER IN POST-MENOPAUSAL WOMEN.

Question 25

Where is TAMOXIFEN an agonist?

Answer 25

endometrium! THEREFORE a catch, antagonist in BREAST tissue but AGONIST in endometrial tissue.

Question 26

How is TAMOXIFEN administered? how long does it take to reach steady state?

Answer 26

ORALLY, 4-6wks and NO additional benefit after 5 yrs

Question 27

what is a PARTIAL AGONIST and under the sublcass of a SERM in the treatment of breast cancer?

Answer 27

RALOXIFENE, TOREMIPHENE and i guess Tamoxifen as well.

Question 28

A SERD used in the treatment of POSTmenopausal women for breast cancer, takes 7 days to take effect, and is metabolized in the liver. NAME that DRUG! what do you have to watch out for?

Answer 28

FULVESTRANT. drug interactions with CYP3A4!

Question 29

how is FULVESTRANT administered?

Answer 29

intramuscular in 1 month intervals

Question 30

what drug is associated with IMPOTENCE and is a TERATOGEN?

Answer 30

Finasteride!

Question 31

what is a 17-alpha Hydroxylase inhibitor?

Answer 31

ABIRATERONE ACETATE. APPARENTLY CYP17 inhibitor is the same!

Question 32

which of the following Anti-Estrogens are AGONISTS in the bone??? Tamoxifen, Toremifene, Raloxifene, Fulvestrant

Answer 32

Tamoxifen (SERM) and Raloxifene (SERM)

Question 33

What Anti-estrogen is an antagonist in the bone, breast and uterus??

Answer 33

Fulvestrant.

Question 34

What drug has side effects of: GI upset, headache, back pain and injection site reaction?

Answer 34

Fulvestrant!

Question 35

Why is their a life-time dose limitation with DOXORUBICIN?

Answer 35

CARDIOTOXICITY. when you hit that upper limit, you cant take it anymore.

Question 36

what drug is used for Her-2-neu + breast cancer?

Answer 36

Trastuzumab

Question 37

Name that drug! GnRH competitive ANTAGONIST

Answer 37

DEGARELIX.

Question 38

Does Degarelix, a GnRH competitive antagonist, work on: (A) only breast cancer (b) only prostate cancer (c) both breast and prostate cancer (d) breast and ovarian cancer

Answer 38

B. PROSTATE ONLY! (this is a little vulgar, but D (degarelix) for dick- since it only treats male prostate cancer and not women's breast cancer)

Question 39

Does Degarelix, a GnRH competitive antagonist, work on: (A) only breast cancer (b) only prostate cancer (c) both breast and prostate cancer (d) breast and ovarian cancer

Answer 39

B. PROSTATE ONLY! (this is a little vulgar, but D (degarelix) for dick- since it only treats males)

Question 40

Does Degarelix, a GnRH competitive antagonist, work on: (A) only breast cancer (b) only prostate cancer (c) both breast and prostate cancer (d) breast and ovarian cancer

Answer 40

B. PROSTATE ONLY! (kinda vulgar but D (degarelix) for dick since it only treats males)

Question 41

Does Degarelix, a GnRH competitive antagonist, work on: (A) only breast cancer (b) only prostate cancer (c) both breast and prostate cancer (d) breast and ovarian cancer

Answer 41

B. PROSTATE ONLY!

Question 42

Does Degarelix, a GnRH competitive antagonist, work on: (A) only breast cancer (b) only prostate cancer (c) both breast and prostate cancer (d) breast and ovarian cancer

Answer 42

B. PROSTATE ONLY! (this is a little vulgar, but D (degarelix) for dick- since it only treats male prostate cancer and not women's breast cancer)

Question 43

Does Degarelix, a GnRH competitive antagonist, work on: (A) only breast cancer (b) only prostate cancer (c) both breast and prostate cancer (d) breast and ovarian cancer

Answer 43

B. PROSTATE ONLY! (kinda vulgar but D (degarelix) for dick since it only treats males)