Androgen Questions - Pharm 2 PDF

1. What is the mechanism of action of GnRH antagonists such as degarelix? A. Inhibition of testosterone synthesis in the adrenal glands​ B. Competitive inhibition of GnRH receptors, suppressing gonadotropin secretion​ C. Pulsatile stimulation of GnRH receptors to increase gonadotropin release​ D. I...

1. What is the mechanism of action of GnRH antagonists such as degarelix? A. Inhibition of testosterone synthesis in the adrenal glands​ B. Competitive inhibition of GnRH receptors, suppressing gonadotropin secretion​ C. Pulsatile stimulation of GnRH receptors to increase gonadotropin release​ D. Inhibition of dihydrotestosterone synthesis Answer: B​ Explanation: GnRH antagonists directly block GnRH receptors, leading to a rapid decrease in LH and testosterone production. 2. Which of the following is a therapeutic use for degarelix? A. Treatment of male pattern baldness​ B. Prevention of premature LH surges in controlled ovarian stimulation​ C. Metastatic prostate cancer​ D. Endometriosis Answer: C​ Explanation: Degarelix is used for metastatic prostate cancer to reduce testosterone production ("chemical castration"). 3. How does continuous administration of a GnRH agonist, such as leuprolide, affect gonadotropin secretion? A. It stimulates gonadotropin release continuously.​ B. It causes receptor desensitization, suppressing gonadotropin secretion.​ C. It increases testosterone production through adrenal stimulation.​ D. It enhances DHT production. Answer: B​ Explanation: Continuous administration of GnRH agonists downregulates receptors, leading to decreased LH and testosterone production. 4. What is a unique adverse effect of GnRH agonists like leuprolide in men? A. Priapism​ B. Tumor flare in metastatic prostate cancer​ C. Increased libido​ D. Weight loss Answer: B​ Explanation: GnRH agonists initially increase gonadotropin secretion, causing a transient "tumor flare" in men with prostate cancer. 5. What is the mechanism of action of androgen receptor antagonists like flutamide? A. Block the synthesis of testosterone in the testis​ B. Inhibit DHT binding to androgen receptors​ C. Competitive inhibition of androgen receptors​ D. Suppress gonadotropin secretion Answer: C​ Explanation: Androgen receptor antagonists, such as flutamide, competitively block androgen receptors, preventing androgen activity. 6. Which androgen receptor antagonist is known for hepatotoxicity as a potential adverse effect? A. Flutamide​ B. Bicalutamide​ C. Nilutamide​ D. Enzalutamide Answer: A​ Explanation: Flutamide is associated with hepatotoxicity, requiring close monitoring of liver function. 7. What is the primary mechanism of action of ketoconazole in advanced prostate cancer? A. Inhibition of GnRH receptors​ B. Blockage of androgen receptor binding​ C. Inhibition of adrenal and gonadal steroid synthesis via CYP450 enzymes​ D. Downregulation of 5-alpha reductase Answer: C​ Explanation: Ketoconazole inhibits cytochrome P450 enzymes, disrupting adrenal and gonadal steroidogenesis. 8. Which of the following is a common side effect of androgen receptor antagonists like bicalutamide? A. Osteoporosis​ B. Gynecomastia​ C. Priapism​ D. Myalgia Answer: B​ Explanation: Androgen receptor antagonists can cause gynecomastia due to altered hormone levels. 9. Which GnRH agonist is administered as a depot formulation for slow release? A. Ganirelix​ B. Leuprolide​ C. Ketoconazole​ D. Flutamide Answer: B​ Explanation: Leuprolide can be administered as a depot formulation for long-acting suppression of gonadotropins. 10. What adverse effect is shared by both GnRH agonists and antagonists in men? A. Increased libido​ B. Reduced bone density​ C. Alopecia​ D. Hypertension Answer: B​ Explanation: Both drug classes can cause reduced bone density due to suppression of testosterone. 11. Which androgen receptor antagonist is often used in combination with GnRH agonists? A. Ketoconazole​ B. Bicalutamide​ C. Finasteride​ D. Tadalafil Answer: B​ Explanation: Bicalutamide is commonly combined with GnRH agonists to prevent the initial tumor flare and provide additional androgen blockade. 12. Which of the following drugs inhibits 5-alpha reductase and is used for BPH? A. Flutamide​ B. Finasteride​ C. Ketoconazole​ D. Leuprolide Answer: B​ Explanation: Finasteride inhibits 5-alpha reductase, reducing DHT synthesis and prostate size. 13. Which GnRH antagonist is also used to prevent premature LH surges during ovarian stimulation? A. Leuprolide​ B. Degarelix​ C. Ganirelix​ D. Flutamide Answer: C​ Explanation: Ganirelix is used in fertility treatments to prevent premature LH surges during ovarian stimulation. 14. What is a significant adverse effect of ketoconazole in advanced prostate cancer? A. Hyperkalemia​ B. Hepatotoxicity​ C. Osteoporosis​ D. Alopecia Answer: B​ Explanation: Ketoconazole can cause hepatotoxicity due to its effect on CYP450 enzymes. 15. What therapeutic use is shared by GnRH agonists and antagonists? A. Treatment of alopecia​ B. Management of metastatic prostate cancer​ C. Treatment of erectile dysfunction​ D. Management of osteoporosis Answer: B​ Explanation: Both classes are used to suppress testosterone production in metastatic prostate cancer. 16. What adverse effect is unique to GnRH antagonists compared to agonists? A. Tumor flare​ B. Injection site reactions​ C. Reduced libido​ D. Hot flashes Answer: B​ Explanation: Injection site reactions are more common with GnRH antagonists compared to agonists. 17. Which androgen receptor antagonist is the most potent? A. Flutamide​ B. Bicalutamide​ C. Nilutamide​ D. Enzalutamide Answer: D​ Explanation: Enzalutamide is a potent androgen receptor antagonist with fewer side effects compared to earlier drugs like flutamide. 18. Which 5-alpha reductase inhibitor is also approved for treating male pattern baldness? A. Finasteride​ B. Dutasteride​ C. Flutamide​ D. Ketoconazole Answer: A​ Explanation: Finasteride is FDA-approved for both BPH and male pattern baldness. 19. What is a therapeutic use of GnRH agonists in children? A. Central precocious puberty​ B. Growth hormone deficiency​ C. Hypogonadism​ D. Cryptorchidism Answer: A​ Explanation: GnRH agonists like leuprolide are used to manage central precocious puberty by suppressing premature gonadotropin release. 20. What is the mechanism of "chemical castration" achieved by GnRH antagonists like degarelix? A. Suppression of LH secretion and testosterone production​ B. Inhibition of DHT synthesis​ C. Competitive blockade of androgen receptors​ D. Increased metabolism of testosterone Answer: A​ Explanation: GnRH antagonists suppress LH secretion, which decreases testosterone production, leading to "chemical castration." 1. Which of the following is a unique adverse effect associated with GnRH agonists, such as leuprolide, in men with prostate cancer? A. Hot flashes​ B. Initial tumor flare​ C. Gynecomastia​ D. Injection site reactions Answer: B​ Explanation: GnRH agonists initially increase gonadotropin and testosterone secretion, causing a tumor flare before receptor desensitization reduces hormone levels. 2. Which drug is a GnRH antagonist used for "chemical castration"? A. Leuprolide​ B. Degarelix​ C. Ketoconazole​ D. Flutamide Answer: B​ Explanation: Degarelix is a GnRH antagonist that rapidly reduces testosterone levels without causing an initial tumor flare. 3. What is the primary therapeutic use of androgen receptor antagonists such as enzalutamide? A. Treat male pattern baldness​ B. Treat metastatic prostate cancer​ C. Treat central precocious puberty​ D. Treat erectile dysfunction Answer: B​ Explanation: Androgen receptor antagonists like enzalutamide are used as adjuvant therapies for metastatic prostate cancer. 4. Which androgen receptor antagonist is associated with gynecomastia and hepatotoxicity? A. Flutamide​ B. Bicalutamide​ C. Nilutamide​ D. Enzalutamide Answer: A​ Explanation: Flutamide can cause gynecomastia and hepatotoxicity due to its effect on androgen signaling and liver metabolism. 5. What is the mechanism of action of 5-alpha reductase inhibitors like finasteride? A. Inhibit DHT synthesis from testosterone​ B. Block androgen receptors​ C. Suppress gonadotropin secretion​ D. Increase aromatization of testosterone Answer: A​ Explanation: 5-alpha reductase inhibitors block the conversion of testosterone to DHT, reducing prostate growth and treating conditions like BPH and male pattern baldness. 6. Which drug is a non-steroidal androgen receptor antagonist? A. Finasteride​ B. Flutamide​ C. Ketoconazole​ D. Goserelin Answer: B​ Explanation: Flutamide is a non-steroidal androgen receptor antagonist used in combination with GnRH agonists for prostate cancer. 7. Which adverse effect is specific to androgen receptor antagonists like bicalutamide? A. Tumor flare​ B. Hepatotoxicity​ C. Osteoporosis​ D. Alopecia Answer: B​ Explanation: Hepatotoxicity is a common adverse effect of androgen receptor antagonists, particularly flutamide and bicalutamide. 8. What is the primary action of ketoconazole in advanced prostate cancer? A. Direct inhibition of DHT​ B. Inhibition of adrenal and gonadal steroid synthesis via CYP450​ C. Competitive blockade of androgen receptors​ D. Suppression of gonadotropin secretion Answer: B​ Explanation: Ketoconazole inhibits cytochrome P450 enzymes responsible for steroid synthesis, suppressing adrenal and gonadal hormone production. 9. What is a common adverse effect of GnRH agonists in women? A. Priapism​ B. Menopause-like symptoms (hot flashes, headaches)​ C. Hepatotoxicity​ D. Hyperkalemia Answer: B​ Explanation: GnRH agonists cause menopausal symptoms in women due to suppression of ovarian hormones. 10. Which 5-alpha reductase inhibitor is FDA-approved for male pattern baldness? A. Dutasteride​ B. Finasteride​ C. Flutamide​ D. Ketoconazole Answer: B​ Explanation: Finasteride is approved for male pattern baldness due to its ability to inhibit DHT, which contributes to hair follicle miniaturization. 11. What is the therapeutic use of GnRH agonists in children? A. Central precocious puberty​ B. Cryptorchidism​ C. Growth hormone deficiency​ D. Male hypogonadism Answer: A​ Explanation: GnRH agonists, such as leuprolide, are used to suppress gonadotropins in children with central precocious puberty. 12. What is a potential adverse effect of degarelix that is less common with GnRH agonists? A. Bone loss​ B. Injection site reactions​ C. Gynecomastia​ D. Tumor flare Answer: B​ Explanation: Degarelix, a GnRH antagonist, often causes injection site reactions but avoids the tumor flare seen with GnRH agonists. 13. Which androgen receptor antagonist has the highest potency? A. Flutamide​ B. Bicalutamide​ C. Nilutamide​ D. Enzalutamide Answer: D​ Explanation: Enzalutamide is the most potent androgen receptor antagonist and has improved efficacy in advanced prostate cancer. 14. Which androgen receptor antagonist is administered orally and used with GnRH agonists? A. Finasteride​ B. Bicalutamide​ C. Ketoconazole​ D. Degarelix Answer: B​ Explanation: Bicalutamide is given orally and is often combined with GnRH agonists to reduce tumor flare and enhance androgen blockade. 15. What is the main use of GnRH agonists in prostate cancer? A. Reduce prostate size​ B. "Chemical castration" by reducing testosterone levels​ C. Enhance androgen receptor sensitivity​ D. Inhibit 5-alpha reductase Answer: B​ Explanation: GnRH agonists desensitize receptors with continuous use, leading to suppression of gonadotropins and testosterone production ("chemical castration"). 16. What is the shared adverse effect of both ketoconazole and androgen receptor antagonists? A. Hepatotoxicity​ B. Osteoporosis​ C. Hot flashes​ D. Tumor flare Answer: A​ Explanation: Both ketoconazole and androgen receptor antagonists like flutamide are associated with hepatotoxicity. 17. How do GnRH antagonists like cetrorelix work in ovarian stimulation protocols? A. Stimulate LH secretion​ B. Prevent premature LH surges​ C. Suppress estrogen production​ D. Enhance follicular development Answer: B​ Explanation: GnRH antagonists prevent premature LH surges during controlled ovarian stimulation. 18. What class of drugs can cause osteoporosis with long-term use in men? A. 5-alpha reductase inhibitors​ B. GnRH agonists​ C. Ketoconazole​ D. Androgen receptor antagonists Answer: B​ Explanation: Long-term use of GnRH agonists suppresses testosterone, increasing the risk of bone density loss and osteoporosis. 19. What is a major limitation of ketoconazole for prostate cancer treatment? A. Poor oral bioavailability​ B. Numerous CYP450-mediated drug interactions​ C. Lack of androgen suppression​ D. High risk of gynecomastia Answer: B​ Explanation: Ketoconazole inhibits CYP450 enzymes, leading to numerous drug interactions that limit its clinical use. 20. Which of the following describes the mechanism of "tumor flare" in GnRH agonists? A. Initial increase in LH and testosterone levels​ B. Direct stimulation of androgen receptors​ C. Inhibition of androgen metabolism​ D. Increase in DHT synthesis Answer: A​ Explanation: GnRH agonists cause an initial surge in gonadotropins and testosterone before receptor desensitization occurs, leading to a tumor flare. 1. What is the primary therapeutic use of GnRH antagonists such as degarelix? A. Treat male pattern baldness​ B. Treat metastatic prostate cancer​ C. Treat erectile dysfunction​ D. Treat central precocious puberty Answer: B​ Explanation: GnRH antagonists are used to treat metastatic prostate cancer by reducing testosterone levels. 2. Which adverse effect is commonly associated with androgen receptor antagonists like nilutamide? A. Hypotension​ B. Visual disturbances​ C. Hyperkalemia​ D. Myalgia Answer: B​ Explanation: Nilutamide can cause visual disturbances, including delayed adaptation to darkness. 3. Which androgen receptor antagonist is associated with fewer hepatotoxic effects? A. Flutamide​ B. Bicalutamide​ C. Ketoconazole​ D. Nilutamide Answer: B​ Explanation: Bicalutamide has a better safety profile regarding hepatotoxicity compared to flutamide. 4. What is the role of GnRH agonists in managing central precocious puberty? A. Increase testosterone production​ B. Suppress premature gonadotropin release​ C. Block androgen receptor activity​ D. Inhibit 5-alpha reductase Answer: B​ Explanation: GnRH agonists suppress premature gonadotropin release, delaying puberty in affected children. 5. Which drug inhibits steroidogenesis by targeting cytochrome P450 enzymes? A. Ketoconazole​ B. Finasteride​ C. Bicalutamide​ D. Enzalutamide Answer: A​ Explanation: Ketoconazole inhibits CYP450 enzymes, disrupting steroid synthesis in both adrenal and gonadal tissues. 6. What is a common adverse effect of long-term GnRH agonist use in women? A. Osteoporosis​ B. Hypertension​ C. Hypercalcemia​ D. Alopecia Answer: A​ Explanation: GnRH agonists suppress estrogen production, leading to bone density loss and osteoporosis with long-term use. 7. What is the primary action of androgen receptor antagonists like enzalutamide in prostate cancer treatment? A. Block androgen receptor activation​ B. Inhibit DHT synthesis​ C. Suppress gonadotropin release​ D. Reduce estrogen levels Answer: A​ Explanation: Androgen receptor antagonists block androgen receptor activation, reducing the effect of testosterone and DHT in prostate cancer. 8. Which GnRH agonist is commonly used as a depot formulation for long-term treatment of hormone-responsive tumors? A. Cetorelix​ B. Leuprolide​ C. Flutamide​ D. Ketoconazole Answer: B​ Explanation: Leuprolide is administered as a depot formulation for long-term suppression of gonadotropin secretion. 9. What is a significant adverse effect of ketoconazole when used for advanced prostate cancer? A. Hepatotoxicity​ B. Osteoporosis​ C. Hypertension​ D. Hyperkalemia Answer: A​ Explanation: Ketoconazole inhibits CYP450 enzymes, which can lead to hepatotoxicity. 10. What is the mechanism of action of 5-alpha reductase inhibitors like dutasteride? A. Block androgen receptor activation​ B. Inhibit the conversion of testosterone to DHT​ C. Suppress gonadotropin secretion​ D. Enhance testosterone metabolism Answer: B​ Explanation: 5-alpha reductase inhibitors block the enzyme that converts testosterone to DHT, reducing androgenic stimulation of the prostate and hair follicles. 11. Which adverse effect is unique to androgen receptor antagonists compared to GnRH agonists? A. Hot flashes​ B. Tumor flare​ C. Hepatotoxicity​ D. Injection site reactions Answer: C​ Explanation: Hepatotoxicity is more commonly associated with androgen receptor antagonists like flutamide. 12. Which GnRH antagonist is used to prevent premature LH surges during fertility treatments? A. Degarelix​ B. Ganirelix​ C. Leuprolide​ D. Ketoconazole Answer: B​ Explanation: Ganirelix is used in fertility protocols to prevent premature LH surges. 13. What is the mechanism of "chemical castration" achieved by GnRH antagonists like degarelix? A. Inhibition of androgen receptors​ B. Suppression of LH secretion​ C. Inhibition of DHT synthesis​ D. Downregulation of testosterone metabolism Answer: B​ Explanation: GnRH antagonists suppress LH secretion, leading to a rapid decline in testosterone levels and "chemical castration." 14. Which drug class can cause an initial tumor flare in metastatic prostate cancer? A. GnRH agonists​ B. GnRH antagonists​ C. 5-alpha reductase inhibitors​ D. Androgen receptor antagonists Answer: A​ Explanation: GnRH agonists can cause an initial tumor flare due to transient increases in testosterone levels. 15. What is the primary indication for ketoconazole in prostate cancer? A. Treatment of hormone-resistant prostate cancer​ B. Primary therapy for early-stage prostate cancer​ C. Adjuvant therapy for metastatic disease​ D. Suppression of DHT synthesis Answer: A​ Explanation: Ketoconazole is used for advanced prostate cancer that is resistant to other antiandrogen therapies. 16. Which androgen receptor antagonist is associated with delayed dark adaptation as a side effect? A. Flutamide​ B. Bicalutamide​ C. Nilutamide​ D. Enzalutamide Answer: C​ Explanation: Nilutamide is known for causing visual disturbances, particularly delayed adaptation to darkness. 17. What is the normal administration route for GnRH antagonists like degarelix? A. Oral​ B. Subcutaneous injection​ C. Intranasal spray​ D. Intravenous infusion Answer: B​ Explanation: GnRH antagonists like degarelix are administered via subcutaneous injection. 18. Which 5-alpha reductase inhibitor is commonly used to treat BPH and male pattern baldness? A. Ketoconazole​ B. Finasteride​ C. Flutamide​ D. Leuprolide Answer: B​ Explanation: Finasteride is FDA-approved for both BPH and male pattern baldness. 19. What is a common adverse effect of long-term androgen suppression in men? A. Increased libido​ B. Gynecomastia​ C. Hypertension​ D. Hypercalcemia Answer: B​ Explanation: Long-term androgen suppression can lead to gynecomastia due to altered hormone balance. 20. Which GnRH agonist is indicated for the treatment of endometriosis? A. Degarelix​ B. Leuprolide​ C. Finasteride​ D. Ketoconazole Answer: B​ Explanation: Leuprolide is used to suppress ovarian hormone production, making it effective in managing endometriosis.. GnRH Agonists vs. Antagonists ​ GnRH Agonists: ○​ Examples: Leuprolide, Goserelin, Histrelin. ○​ Mechanism: Continuous administration causes receptor desensitization, suppressing gonadotropin release (LH and FSH) → reduced testosterone production. ○​ Uses: ​ Metastatic prostate cancer (hormone-responsive tumors). ​ Central precocious puberty. ​ Endometriosis. ​ Transgender hormone therapy. ○​ Adverse Effects: ​ Men: Tumor flare (initial testosterone surge), gynecomastia, hot flashes, reduced libido, bone loss (osteoporosis). ​ Women: Menopause-like symptoms (hot flashes, headaches), long-term bone loss. ​ GnRH Antagonists: ○​ Examples: Degarelix, Ganirelix, Cetrorelix. ○​ Mechanism: Directly block GnRH receptors, rapidly suppressing LH and testosterone without causing a tumor flare. ○​ Uses: ​ Degarelix: Metastatic prostate cancer ("chemical castration"). ​ Ganirelix/Cetrorelix: Prevent premature LH surges during controlled ovarian stimulation. ○​ Adverse Effects: Injection site reactions, hot flashes, weight gain. 2. Androgen Receptor Antagonists ​ Examples: Flutamide, Bicalutamide, Nilutamide, Enzalutamide. ​ Mechanism: Competitive inhibition of androgen receptors, blocking testosterone and DHT action. ​ Uses: ○​ Adjuvant therapy with GnRH agonists for metastatic prostate cancer to prevent tumor flare. ​ Adverse Effects: ○​ Gynecomastia. ○​ Hot flashes. ○​ Hepatotoxicity (notably with flutamide). ○​ Nilutamide: Visual disturbances (e.g., delayed dark adaptation). 3. 5-Alpha Reductase Inhibitors ​ Examples: Finasteride, Dutasteride. ​ Mechanism: Inhibit conversion of testosterone to DHT, reducing androgenic stimulation of the prostate and hair follicles. ​ Uses: ○​ BPH (especially for larger prostates >40 mL). ○​ Male pattern baldness (finasteride). ​ Adverse Effects: ○​ Decreased libido. ○​ Erectile dysfunction. 4. Ketoconazole ​ Mechanism: Inhibits adrenal and gonadal steroid synthesis by blocking CYP450 enzymes. ​ Uses: ○​ Advanced, hormone-resistant prostate cancer (off-label). ○​ Antifungal (systemic and topical). ​ Adverse Effects: ○​ Hepatotoxicity. ○​ Drug interactions due to CYP450 inhibition. 5. Shared Adverse Effects Across Therapies ​ GnRH Agonists/Antagonists: ○​ Bone loss (osteoporosis) with long-term use. ○​ Hot flashes, reduced libido. ​ Androgen Receptor Antagonists: ○​ Hepatotoxicity (flutamide, nilutamide). ○​ Gynecomastia. ​ 5-Alpha Reductase Inhibitors: ○​ Sexual dysfunction (decreased libido, erectile dysfunction). 6. Clinical Applications to Prostate Cancer ​ GnRH Agonists: ○​ "Chemical castration" via long-term suppression of testosterone. ○​ Tumor flare with initial use (prevented by androgen receptor antagonists). ​ GnRH Antagonists: ○​ Rapid suppression of testosterone without tumor flare (e.g., degarelix). ​ Androgen Receptor Antagonists: ○​ Combined with GnRH agonists to enhance androgen blockade.  ​ Ketoconazole: ○​ Hormone-resistant metastatic prostate cancer. 7. Fertility Treatments ​ GnRH Antagonists (Ganirelix, Cetrorelix): ○​ Prevent premature LH surges during controlled ovarian stimulation. 8. Unique Adverse Effects ​ Tumor Flare: GnRH agonists (e.g., leuprolide). ​ Hepatotoxicity: Flutamide > Bicalutamide. ​ Visual Disturbances: Nilutamide (delayed dark adaptation). ​ Injection Site Reactions: GnRH antagonists (e.g., degarelix).