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HRM Exam 3 > Fitzakerly: Antineoplastics IV > Flashcards

Fitzakerly: Antineoplastics IV Flashcards

1
Q

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

A

Goserelin and Leuprolide!

Prostate and breast cancer!

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2
Q

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

A

(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

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3
Q

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

A

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.

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4
Q

Name that drug! GnRH competitive ANTAGONIST

A

DEGARELIX

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5
Q

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

A

FALSE. they are ANTAGONISTS and have NO FLARE.

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6
Q

What side effects are associated with GnRH antagonists?

A

generally WELL TOLERATED, injection site rxn possiblitity

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7
Q

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

A

B. PROSTATE ONLY!

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8
Q

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

A

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

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9
Q

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

A

Finasteride, dutasteride

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10
Q

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

A

ABRATERONE ACETATE. CYP 17 inhibitor!

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11
Q

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

A

ABRATERONE ACETATE

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12
Q

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

A

AMINOGLUTETHIMIDE. NONsteroidal

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13
Q

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

A

AMINOGLUTETHIMIDE

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14
Q

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

A

B. DONT USE AROMATASE INHIBITORS on premenopausal women!

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15
Q

What is the toxicity associated with AMINOGLUTETHIMIDE?

A

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

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16
Q

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

A

ANASTROZOLE, LETROZOLE

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17
Q

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

A

ANASTROZOLE, LETROZOLE

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18
Q

What type of drug is EXEMESTANE?

A

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

19
Q

what is the therapeutic use for an irreversible aromatase inhibitor?

A

BREAST CANCER

20
Q

what side effect is associated with Exemastane?

A

Polyarthralgias

21
Q

which breast cancer drug specifically increases appetite ?

A

Exemastane

22
Q

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

A

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

23
Q

what toxicities are associated with bicalutamide, flutamide and nilutamide?

A

HEPATOTOXICITY. RARE: methenoglobinemia

24
Q

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

A

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

25
Q

Where is TAMOXIFEN an agonist?

A

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

26
Q

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

A

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

27
Q

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

A

RALOXIFENE, TOREMIPHENE and i guess Tamoxifen as well.

28
Q

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?

A

FULVESTRANT. drug interactions with CYP3A4!

29
Q

how is FULVESTRANT administered?

A

intramuscular in 1 month intervals

30
Q

what drug is associated with IMPOTENCE and is a TERATOGEN?

A

Finasteride!

31
Q

what is a 17-alpha Hydroxylase inhibitor?

A

ABIRATERONE ACETATE. APPARENTLY CYP17 inhibitor is the same!

32
Q

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

A

Tamoxifen (SERM) and Raloxifene (SERM)

33
Q

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

A

Fulvestrant.

34
Q

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

A

Fulvestrant!

35
Q

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

A

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

36
Q

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

A

Trastuzumab

37
Q

Name that drug! GnRH competitive ANTAGONIST

A

DEGARELIX.

38
Q

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

A

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)

39
Q

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

A

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

40
Q

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

A

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

41
Q

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

A

B. PROSTATE ONLY!

42
Q

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

A

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)

43
Q

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

A

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

HRM Exam 3 (16 decks)

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