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Questions and Answers
Which adverse effect is more commonly associated with GnRH antagonists compared to GnRH agonists?
Which adverse effect is more commonly associated with GnRH antagonists compared to GnRH agonists?
- Hot flashes
- Gynecomastia
- Reduced libido
- Injection site reactions (correct)
Which of these drugs is considered the most potent androgen receptor antagonist?
Which of these drugs is considered the most potent androgen receptor antagonist?
- Flutamide
- Enzalutamide (correct)
- Bicalutamide
- Nilutamide
Which 5-alpha reductase inhibitor is prescribed to treat both benign prostatic hyperplasia (BPH) and male pattern baldness?
Which 5-alpha reductase inhibitor is prescribed to treat both benign prostatic hyperplasia (BPH) and male pattern baldness?
- Finasteride (correct)
- Ketoconazole
- Flutamide
- Dutasteride
What is a therapeutic application of GnRH agonists in children?
What is a therapeutic application of GnRH agonists in children?
What is the direct effect of GnRH antagonists on gonadotropin secretion?
What is the direct effect of GnRH antagonists on gonadotropin secretion?
What is the primary mechanism by which GnRH antagonists like degarelix induce 'chemical castration'?
What is the primary mechanism by which GnRH antagonists like degarelix induce 'chemical castration'?
Which condition is commonly treated with degarelix?
Which condition is commonly treated with degarelix?
What is a unique initial adverse effect observed with GnRH agonists, such as leuprolide, in men with prostate cancer before receptor downregulation occurs?
What is a unique initial adverse effect observed with GnRH agonists, such as leuprolide, in men with prostate cancer before receptor downregulation occurs?
How does the continuous administration of leuprolide impact the GnRH receptors and gonadotropin secretion?
How does the continuous administration of leuprolide impact the GnRH receptors and gonadotropin secretion?
Which drug serves as a GnRH antagonist utilized for achieving 'chemical castration' by rapidly reducing testosterone levels?
Which drug serves as a GnRH antagonist utilized for achieving 'chemical castration' by rapidly reducing testosterone levels?
What is a characteristic initial side effect of GnRH agonists in men with advanced prostate cancer?
What is a characteristic initial side effect of GnRH agonists in men with advanced prostate cancer?
What is a primary therapeutic use of androgen receptor antagonists like enzalutamide?
What is a primary therapeutic use of androgen receptor antagonists like enzalutamide?
What is the primary action of flutamide at the cellular level?
What is the primary action of flutamide at the cellular level?
Which antiandrogen requires careful monitoring of liver function due to potential adverse effects?
Which antiandrogen requires careful monitoring of liver function due to potential adverse effects?
How does ketoconazole work to reduce androgen levels in the treatment of prostate cancer?
How does ketoconazole work to reduce androgen levels in the treatment of prostate cancer?
What is an important difference between the mechanisms of action between a GnRH agonist and a GnRH antagonist?
What is an important difference between the mechanisms of action between a GnRH agonist and a GnRH antagonist?
Which of the following is a distinguishing side effect of degarelix compared to GnRH agonists?
Which of the following is a distinguishing side effect of degarelix compared to GnRH agonists?
Which androgen receptor antagonist demonstrates the highest potency when treating prostate cancer?
Which androgen receptor antagonist demonstrates the highest potency when treating prostate cancer?
What is the typical method of administration for bicalutamide and what is a common co-administration strategy?
What is the typical method of administration for bicalutamide and what is a common co-administration strategy?
What is the primary mechanism of action of GnRH agonists in the treatment of prostate cancer?
What is the primary mechanism of action of GnRH agonists in the treatment of prostate cancer?
Which shared adverse effect is a significant concern when using both ketoconazole and androgen receptor antagonists?
Which shared adverse effect is a significant concern when using both ketoconazole and androgen receptor antagonists?
How do GnRH antagonists like cetrorelix function in ovarian stimulation protocols?
How do GnRH antagonists like cetrorelix function in ovarian stimulation protocols?
What is a long-term risk associated with the use of GnRH agonists in males?
What is a long-term risk associated with the use of GnRH agonists in males?
What key factor limits the use of ketoconazole in the treatment of prostate cancer?
What key factor limits the use of ketoconazole in the treatment of prostate cancer?
What is the initiating factor contributing to the 'tumor flare' phenomenon observed with GnRH agonists?
What is the initiating factor contributing to the 'tumor flare' phenomenon observed with GnRH agonists?
Which of the following best describes the primary mechanism of action for GnRH antagonists, like degarelix, in treating prostate cancer?
Which of the following best describes the primary mechanism of action for GnRH antagonists, like degarelix, in treating prostate cancer?
Which of these adverse effects is most characteristically associated with the use of the androgen receptor antagonist nilutamide?
Which of these adverse effects is most characteristically associated with the use of the androgen receptor antagonist nilutamide?
Which androgen receptor antagonist exhibits a more favorable safety profile regarding liver toxicity when compared to flutamide?
Which androgen receptor antagonist exhibits a more favorable safety profile regarding liver toxicity when compared to flutamide?
In the context of central precocious puberty, what is the primary therapeutic role of GnRH agonists?
In the context of central precocious puberty, what is the primary therapeutic role of GnRH agonists?
Which drug impacts steroidogenesis by inhibiting cytochrome P450 enzymes?
Which drug impacts steroidogenesis by inhibiting cytochrome P450 enzymes?
What is a significant long-term adverse effect that may occur due to chronic use of GnRH agonists in women?
What is a significant long-term adverse effect that may occur due to chronic use of GnRH agonists in women?
What is the primary mechanism by which androgen receptor antagonists, such as enzalutamide, acts in the treatment of prostate cancer?
What is the primary mechanism by which androgen receptor antagonists, such as enzalutamide, acts in the treatment of prostate cancer?
What is the primary effect of androgen receptor antagonists?
What is the primary effect of androgen receptor antagonists?
Which of the following is commonly administered as a depot formulation?
Which of the following is commonly administered as a depot formulation?
Which adverse effect is most associated with ketoconazole usage in advanced prostate cancer treatment?
Which adverse effect is most associated with ketoconazole usage in advanced prostate cancer treatment?
What is the mechanism of action of 5-alpha reductase inhibitors?
What is the mechanism of action of 5-alpha reductase inhibitors?
Which adverse effect is more common with androgen receptor antagonists than GnRH agonists?
Which adverse effect is more common with androgen receptor antagonists than GnRH agonists?
Which GnRH antagonist is used to prevent premature LH surges in fertility treatment?
Which GnRH antagonist is used to prevent premature LH surges in fertility treatment?
How does 'chemical castration' occur via GnRH antagonists like degarelix?
How does 'chemical castration' occur via GnRH antagonists like degarelix?
Which drug class can cause an initial tumor flare in metastatic prostate cancer?
Which drug class can cause an initial tumor flare in metastatic prostate cancer?
What is the primary therapeutic use of ketoconazole in prostate cancer treatment?
What is the primary therapeutic use of ketoconazole in prostate cancer treatment?
Which androgen receptor antagonist is known to delay dark adaptation as a side effect?
Which androgen receptor antagonist is known to delay dark adaptation as a side effect?
What is the standard method of administration for GnRH antagonists such as degarelix?
What is the standard method of administration for GnRH antagonists such as degarelix?
Which of the following is a long-term adverse effect of androgen suppression in men?
Which of the following is a long-term adverse effect of androgen suppression in men?
Which GnRH agonist is specifically indicated for treating endometriosis?
Which GnRH agonist is specifically indicated for treating endometriosis?
What mechanism do GnRH agonists like leuprolide use to reduce testosterone production?
What mechanism do GnRH agonists like leuprolide use to reduce testosterone production?
Finasteride is primarily used for which conditions?
Finasteride is primarily used for which conditions?
Which effect is commonly associated with the use of GnRH agonists in men?
Which effect is commonly associated with the use of GnRH agonists in men?
Flashcards
GnRH Antagonists
GnRH Antagonists
Drugs that competitively inhibit GnRH receptors, suppressing gonadotropin secretion.
Degarelix Usage
Degarelix Usage
Used therapeutically for metastatic prostate cancer to reduce testosterone production.
GnRH Agonists
GnRH Agonists
Continuous administration causes receptor desensitization, suppressing gonadotropin secretion.
Tumor Flare
Tumor Flare
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Androgen Receptor Antagonists
Androgen Receptor Antagonists
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Flutamide
Flutamide
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Ketoconazole Action
Ketoconazole Action
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GnRH Receptor Mechanism
GnRH Receptor Mechanism
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Injection site reactions
Injection site reactions
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Enzalutamide
Enzalutamide
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Finasteride
Finasteride
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Chemical castration
Chemical castration
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Degarelix
Degarelix
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Degarelix adverse effect
Degarelix adverse effect
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Most potent androgen antagonist
Most potent androgen antagonist
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Oral androgen antagonist
Oral androgen antagonist
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GnRH agonists use
GnRH agonists use
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Shared adverse effect of ketoconazole
Shared adverse effect of ketoconazole
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GnRH antagonists in ovarian stimulation
GnRH antagonists in ovarian stimulation
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Osteoporosis risk with drugs
Osteoporosis risk with drugs
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Limitations of ketoconazole
Limitations of ketoconazole
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Estrogen Reduction
Estrogen Reduction
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Leuprolide
Leuprolide
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Ketoconazole Adverse Effect
Ketoconazole Adverse Effect
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5-alpha Reductase Inhibitors
5-alpha Reductase Inhibitors
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Ganirelix Usage
Ganirelix Usage
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Tumor Flare Effect
Tumor Flare Effect
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GnRH Antagonists Administration
GnRH Antagonists Administration
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Adverse Effects of Androgen Suppression
Adverse Effects of Androgen Suppression
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Tumor Flare in GnRH Agonists
Tumor Flare in GnRH Agonists
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Mechanism of GnRH Agonists
Mechanism of GnRH Agonists
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Visual Disturbances with Nilutamide
Visual Disturbances with Nilutamide
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Tumor flare mechanism
Tumor flare mechanism
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GnRH antagonists use
GnRH antagonists use
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Nilutamide side effects
Nilutamide side effects
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Bicalutamide safety
Bicalutamide safety
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GnRH agonists in precocious puberty
GnRH agonists in precocious puberty
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GnRH agonists adverse effect
GnRH agonists adverse effect
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Enzalutamide function
Enzalutamide function
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Study Notes
GnRH Agonists and Antagonists
- GnRH agonists initially increase gonadotropin and testosterone secretion, causing a transient "tumor flare". This effect is unique to agonists.
- GnRH antagonists directly block GnRH receptors, leading to a rapid decrease in LH and testosterone production; they do not cause a tumor flare.
- Continuous use of GnRH agonists causes receptor desensitization, suppressing gonadotropin secretion.
- Degarelix is a GnRH antagonist used for metastatic prostate cancer to reduce testosterone production.
Therapeutic Uses
- Degarelix is used for metastatic prostate cancer.
- GnRH agonists are used to manage central precocious puberty in children.
- GnRH agonists and antagonists are used to treat metastatic prostate cancer.
- GnRH agonists are often used in combinations with androgen receptor antagonists to block androgen receptors.
- GnRH agonists are used for long-term suppression of gonadotropins in hormone-responsive tumors.
Adverse Effects
- GnRH agonists can cause a "tumor flare" in men and menopause-like symptoms in women.
- Injection site reactions are more common with GnRH antagonists than agonists.
- Hepatotoxicity is a potential adverse effect, mainly with flutamide.
- Visual disturbances (delayed adaptation to darkness) are associated with nilutamide.
- Bone loss (osteoporosis) is a potential adverse effect with long-term use.
- Gynecomastia and decreased libido can be side effects of GnRH agonists and antagonists.
5-alpha Reductase Inhibitors
- Finasteride inhibits 5-alpha reductase, reducing DHT synthesis and prostate size.
- Finasteride is FDA-approved for treating male pattern baldness.
Ketoconazole
- Ketoconazole inhibits adrenal and gonadal steroid synthesis, suppressing adrenal and gonadal hormone production.
- Ketoconazole is used for hormone-resistant prostate cancer.
- Hepatotoxicity is a significant adverse effect of ketoconazole.
Androgen Receptor Antagonists
- Androgen receptor antagonists competitively block androgen receptors, preventing androgen activity.
- Enzalutamide is a potent androgen receptor antagonist, with improved efficacy in advanced prostate cancer.
- Flutamide is associated with hepatotoxicity and requires close monitoring of liver function.
Fertility Treatments
- GnRH antagonists like ganirelix are used to prevent premature LH surges during ovarian stimulation.
Other Notes
- GnRH antagonists are used for "chemical castration".
- Bicalutamide is a non-steroidal androgen antagonist often used in combination with GnRH agonists.
- Flutamide is associated with gynecomastia and hepatotoxicity.
- GnRH agonists and antagonists suppress testosterone production, reducing prostate growth.
- Long-term use of GnRH agonists can cause osteoporosis in men and women.
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