Fitzakerly: Antineoplastics IV Flashcards
what are 2 GnRH analogs? what are their 2 therapeutic uses?
Goserelin and Leuprolide!
Prostate and breast cancer!
what side effects (2) are associated with GnRH analogs? Why?
(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
what is used in conjunction with Goserelin/Leuoprolide, in PROSTATE CANCER, to decrease the initial ‘flare response’? what are their mechanisms of action?
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.
Name that drug! GnRH competitive ANTAGONIST
DEGARELIX
T or F: GnRH antagonists, such as Degarelix, also have a flare like GnRH analogues (Goserelin, leuprolide)
FALSE. they are ANTAGONISTS and have NO FLARE.
What side effects are associated with GnRH antagonists?
generally WELL TOLERATED, injection site rxn possiblitity
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
B. PROSTATE ONLY!
What are 2 ANDROGEN BIOSYNTHESIS INHIBITORS? And what specific ENZYME do they inhibit?
Dutasteride and FINASTERIDE (“-steride”). 5 alpha reductase inhibitor, therefore blocking the testosterone conversion to DHT!
What drugs do we use for BPH, male pattern baldness, AND prostate cancer prevention (pt w/increase PSA)?
Finasteride, dutasteride
What is an ANDROGEN BIOSYNTHESIS INHIBITOR, other than finasteride and dutasteride? what specifically does it inhibit?
ABRATERONE ACETATE. CYP 17 inhibitor!
What drug is used for metastatic prostate cancer that is resistant to other androgen blocking regimens?
ABRATERONE ACETATE
What is a REVERSIBLE aromatase inhibitor? Is it steroidal or non-steroidal?
AMINOGLUTETHIMIDE. NONsteroidal
what is a (3rd line) drug to use for breast cancer in POST-MENOPAUSAL women?
AMINOGLUTETHIMIDE
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
B. DONT USE AROMATASE INHIBITORS on premenopausal women!
What is the toxicity associated with AMINOGLUTETHIMIDE?
fever, nausea, rash, HA. ADRENAL INSUFFICIENCY (Tx: hydrocortisone) but increases ACTH -> increase cortisol -> Bone marrow suppression = BAD BAD BAD
what are the two 1st line NON-steroidal REVERSIBLE aromatase inhibitors?
ANASTROZOLE, LETROZOLE
what type of REVERSIBLE aromatase inhibitors are used for only BREAST CANCER? hint: nonsteroidal
ANASTROZOLE, LETROZOLE
What type of drug is EXEMESTANE?
an IREVERSIBLE AROMATASE INHIBITOR. aka steroid analogue (‘suicide inhibitors’)
what is the therapeutic use for an irreversible aromatase inhibitor?
BREAST CANCER
what side effect is associated with Exemastane?
Polyarthralgias
which breast cancer drug specifically increases appetite ?
Exemastane
what is BICALUTAMIDE, FLUTAMIDE, NILUTAMIDE used for? is it given for a short or long period of time?
these are anti-androgens and are given for the ‘flare rxn’ with GnRH analogues.
what toxicities are associated with bicalutamide, flutamide and nilutamide?
HEPATOTOXICITY. RARE: methenoglobinemia
What is TAMOXIFEN’s MOA? what is its clinical use then?
SERMs (ER ANTAGONIST). BREAST CANCER IN POST-MENOPAUSAL WOMEN.
Where is TAMOXIFEN an agonist?
endometrium! THEREFORE a catch, antagonist in BREAST tissue but AGONIST in endometrial tissue.
How is TAMOXIFEN administered? how long does it take to reach steady state?
ORALLY, 4-6wks and NO additional benefit after 5 yrs
what is a PARTIAL AGONIST and under the sublcass of a SERM in the treatment of breast cancer?
RALOXIFENE, TOREMIPHENE and i guess Tamoxifen as well.
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?
FULVESTRANT. drug interactions with CYP3A4!
how is FULVESTRANT administered?
intramuscular in 1 month intervals
what drug is associated with IMPOTENCE and is a TERATOGEN?
Finasteride!
what is a 17-alpha Hydroxylase inhibitor?
ABIRATERONE ACETATE. APPARENTLY CYP17 inhibitor is the same!
which of the following Anti-Estrogens are AGONISTS in the bone???
Tamoxifen, Toremifene, Raloxifene, Fulvestrant
Tamoxifen (SERM) and Raloxifene (SERM)
What Anti-estrogen is an antagonist in the bone, breast and uterus??
Fulvestrant.
What drug has side effects of: GI upset, headache, back pain and injection site reaction?
Fulvestrant!
Why is their a life-time dose limitation with DOXORUBICIN?
CARDIOTOXICITY. when you hit that upper limit, you cant take it anymore.
what drug is used for Her-2-neu + breast cancer?
Trastuzumab
Name that drug! GnRH competitive ANTAGONIST
DEGARELIX.
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
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)
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
B. PROSTATE ONLY! (this is a little vulgar, but D (degarelix) for dick- since it only treats males)
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
B. PROSTATE ONLY! (kinda vulgar but D (degarelix) for dick since it only treats males)
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
B. PROSTATE ONLY!
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
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)
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
B. PROSTATE ONLY! (kinda vulgar but D (degarelix) for dick since it only treats males)
