Prostate Cancer (PC) [2] Drugs

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Final Exam review
Sam Adeyiga
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Sam Adeyiga
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Hormonal Therapy (Antiandrogens) "tamides" 1. Bicalutamide (Casodex®) 2. Flutamide 3. Nilutamide (Nilandron®) 4. Enzalutamide (Xtandi®) capsules 5. Apalutamide (Erleada®)
Hormonal Therapy Androgen Biosynthesis Inhibitors 1. Abiraterone acetate (Zytiga®) 2. Ketoconazole
Hormonal Therapy GNRH/LHRH Agonists [Pulsatile and non-pulsatile admin] 1. Goserelin acetate (Zoladex®) SubQ implant 2. Histrelin acetate (Vantas®) SubQ implant 3. Leuprolide acetate (Eligard®, Lupron®, 4. Lupron Depot®) IV, SubQ implant, and IM depot 5. Triptorelin (Trelstar Depot®, Trelstar LA®, Trelstar Mixject®) IM depot
Hormonal Therapy GNRH/LHRH Antagonists Degarelix acetate (Firmagon®) SubQ injection
How does LHRH works 1. It causes release of LH and FSH from the anterior pituitary gland
What is the effect of administering LHRH agonist in a pulsatile manner (i.e., similar to intermittent dosing)? 1. they promote the release of LH and FSH, which in turn promotes the synthesis of testosterone. 2. Graphically, it shows LH AND FSH in a wave like curve 3. The result is INCREASED LH & FSH and androgens (testosterone and Estrogen) 4. It takes about 2 wks to see a decrease in androgens.
What is the effect of administering LHRH agonist in a non-pulsatile manner? 1. drug exposure remains constant in the body, with time they suppress the release of LH and FSH via receptor desensitization. 2. Graphically, it shows LH & FSH rising curve and eventually flat out (steady) 3. during the first 2 wks, initial "flare-up" of snxs related to LHRH activity may occur. 4. The result is DECREASE in LH & FSH and androgens (testosterone and Estrogen)
For ADT (androgen deprivation therapy), what is the appropriate medication 1. Both LHRH agonists and LHRH antagonists.
Among the LHRH agonist therapy, wh/ one is considered medical castration? a. Pulsatile b. Non-pulsatile b. Non-pulsatile
There 2 methods for ADT wh/ are 1. Surgical castration = implantation = Histrelin acetate, Goserelin acetate and Leuprolide acetate 2. Medical Castration = injection = Leuprolide acetate and Triptorelin
What is the best indication of GNRH/LHRH antagonist - Degarelix acetate (Firmagon®)? is reserve for a symptomatic and high risk PC.
What are the differences btw Eligard and Lupron formulation? 1. Eligard requires refrigeration and causes more pain. 2. Lupron requires room temperature and causes less pain.
LHRH agonists AEs include 1. "flare-up" [only during non-pulsatile admin] 2. hot flashes 3. ED and impotence 3. decreased libido and depression 4. injection-site reactions 5. osteoporosis
Which of the ff is a steroidal antiandrogen and does not bind to AR? a. Flutamide b. nilutamide c. bicalutamide d. enzalutamide e. Abiraterone acetate e. Abiraterone acetate
Which of the ff is a nonsteroidal antiandrogen? a. Flutamide b. nilutamide c. bicalutamide d. enzalutamide e. Abiraterone acetate a. Flutamide b. nilutamide c. bicalutamide d. enzalutamide
The androgen receptor (AR) is located in ------ and upon binding, it translocate into ------ and affects --------- 1. cytoplasm 2. nucleus 3. gene expression
------ and ------ binds to AR in the cytoplasm and affects ---------- in the nucleus. 1. Testosterone 2. DHT 3. gene expression
What is/are indications for antiandrogen drugs? 1. adjunct to medical/surgical castration 2. Androgen use alone does not result in decrease of androgens.
Which of the ff is a pure antiandrogen and has been linked to seizure activity in clinical trial? a. Flutamide b. nilutamide c. bicalutamide d. Enzalutamide e. Abiraterone acetate d. Enzalutamide
-------------- does not act as an androgen receptor antagonist, but as a selective and irreversible inhibitor of CYP17 (17 alpha-hydroxylase/ C17,20-lyase), an enzyme required for androgen biosynthesis which is expressed in testicular, adrenal, and prostatic tumor tissues. Abiraterone acetate
------------- inhibits the formation of the testosterone precursors dehydroepiandrosterone (DHEA) and androstenedione Abiraterone acetate
How is Abiraterone acetate administered? Abiraterone acetate should be administered on an EMPTY stomach, at least ONE hour B4 or TWO hours AFTER a meal.
Antiandrogen therapy AEs 1. gynecomastia, 2. hot flashes, 3. breast tenderness, **** 4. diarrhea or constipation, (depending on the drug) 5. liver function (LFT) abnormalities.
Flutamide carries a black-box warning for ------------ hepatic injury
Nilutamide has a black-box warning for ------------ 1. interstitial pneumonitis (iP) 2. can lead to pulmonary fibrosis resulting in hospitalization and death. 3. Symptoms include cough, dyspnea upon exertion, chest pain, and fever
Abiraterone acetate specific SEs include---------? 1. decrease in cortisol synthesis = adrenal insufficiency 2. increase in mineralocorticoid.
Which of the ff has has the lowest rates of diarrhea and hematuria often preferred by patients a. Flutamide b. nilutamide c. bicalutamide d. Enzalutamide e. Abiraterone acetate bicalutamide
Which of the ff can cause a decrease in cortisol synthesis which results in adrenal insufficiency and you must add prednisone. a. Flutamide b. nilutamide c. bicalutamide d. Enzalutamide e. Abiraterone acetate Abiraterone acetate
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