21883373
Description
Flashcards by Sam Adeyiga, updated more than 1 year ago
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Created by Sam Adeyiga
over 4 years ago
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| Question | Answer |
| 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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