Pharmacology of GnRH Agonists and Antagonists
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Questions and Answers

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?

  • Flutamide
  • Enzalutamide (correct)
  • Bicalutamide
  • Nilutamide

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?

<p>Central precocious puberty (D)</p> Signup and view all the answers

What is the direct effect of GnRH antagonists on gonadotropin secretion?

<p>Competitive inhibition, leading to decreased LH and FSH release. (B)</p> Signup and view all the answers

What is the primary mechanism by which GnRH antagonists like degarelix induce 'chemical castration'?

<p>Suppression of LH secretion and testosterone production (A)</p> Signup and view all the answers

Which condition is commonly treated with degarelix?

<p>Advanced or metastatic prostate cancer. (A)</p> Signup and view all the answers

What is a unique initial adverse effect observed with GnRH agonists, such as leuprolide, in men with prostate cancer before receptor downregulation occurs?

<p>Initial tumor flare (C)</p> Signup and view all the answers

How does the continuous administration of leuprolide impact the GnRH receptors and gonadotropin secretion?

<p>It leads to receptor downregulation, suppressing LH and testosterone production. (D)</p> Signup and view all the answers

Which drug serves as a GnRH antagonist utilized for achieving 'chemical castration' by rapidly reducing testosterone levels?

<p>Degarelix (C)</p> Signup and view all the answers

What is a characteristic initial side effect of GnRH agonists in men with advanced prostate cancer?

<p>An initial 'tumor flare' due to increased gonadotropin and testosterone levels. (D)</p> Signup and view all the answers

What is a primary therapeutic use of androgen receptor antagonists like enzalutamide?

<p>Treat metastatic prostate cancer (D)</p> Signup and view all the answers

What is the primary action of flutamide at the cellular level?

<p>Prevention of androgens from binding to their receptors. (C)</p> Signup and view all the answers

Which antiandrogen requires careful monitoring of liver function due to potential adverse effects?

<p>Flutamide (B)</p> Signup and view all the answers

How does ketoconazole work to reduce androgen levels in the treatment of prostate cancer?

<p>By inhibiting steroidogenesis, reducing the synthesis of androgens. (B)</p> Signup and view all the answers

What is an important difference between the mechanisms of action between a GnRH agonist and a GnRH antagonist?

<p>Both lower testosterone but through different mechanisms. Agonists desensitize receptors and antagonists block them. (B)</p> Signup and view all the answers

Which of the following is a distinguishing side effect of degarelix compared to GnRH agonists?

<p>Significant injection site reactions (B)</p> Signup and view all the answers

Which androgen receptor antagonist demonstrates the highest potency when treating prostate cancer?

<p>Enzalutamide (D)</p> Signup and view all the answers

What is the typical method of administration for bicalutamide and what is a common co-administration strategy?

<p>Oral administration, with GnRH agonists (C)</p> Signup and view all the answers

What is the primary mechanism of action of GnRH agonists in the treatment of prostate cancer?

<p>Inducing a 'chemical castration' by lowering testosterone levels (B)</p> Signup and view all the answers

Which shared adverse effect is a significant concern when using both ketoconazole and androgen receptor antagonists?

<p>Hepatotoxicity (C)</p> Signup and view all the answers

How do GnRH antagonists like cetrorelix function in ovarian stimulation protocols?

<p>Prevent premature LH surges (A)</p> Signup and view all the answers

What is a long-term risk associated with the use of GnRH agonists in males?

<p>The development of osteoporosis (B)</p> Signup and view all the answers

What key factor limits the use of ketoconazole in the treatment of prostate cancer?

<p>Its involvement in numerous CYP450-mediated drug interactions (B)</p> Signup and view all the answers

What is the initiating factor contributing to the 'tumor flare' phenomenon observed with GnRH agonists?

<p>Initial surge in LH and subsequent rise in testosterone (C)</p> Signup and view all the answers

Which of the following best describes the primary mechanism of action for GnRH antagonists, like degarelix, in treating prostate cancer?

<p>Reducing testosterone levels (B)</p> Signup and view all the answers

Which of these adverse effects is most characteristically associated with the use of the androgen receptor antagonist nilutamide?

<p>Visual disturbances (A)</p> Signup and view all the answers

Which androgen receptor antagonist exhibits a more favorable safety profile regarding liver toxicity when compared to flutamide?

<p>Bicalutamide (A)</p> Signup and view all the answers

In the context of central precocious puberty, what is the primary therapeutic role of GnRH agonists?

<p>Inhibiting premature release of gonadotropins (C)</p> Signup and view all the answers

Which drug impacts steroidogenesis by inhibiting cytochrome P450 enzymes?

<p>Ketoconazole (A)</p> Signup and view all the answers

What is a significant long-term adverse effect that may occur due to chronic use of GnRH agonists in women?

<p>Osteoporosis (D)</p> Signup and view all the answers

What is the primary mechanism by which androgen receptor antagonists, such as enzalutamide, acts in the treatment of prostate cancer?

<p>Preventing androgen receptor binding activity (B)</p> Signup and view all the answers

What is the primary effect of androgen receptor antagonists?

<p>Block androgen receptor activation (B)</p> Signup and view all the answers

Which of the following is commonly administered as a depot formulation?

<p>Leuprolide (D)</p> Signup and view all the answers

Which adverse effect is most associated with ketoconazole usage in advanced prostate cancer treatment?

<p>Hepatotoxicity (A)</p> Signup and view all the answers

What is the mechanism of action of 5-alpha reductase inhibitors?

<p>Inhibit the conversion of testosterone to DHT (C)</p> Signup and view all the answers

Which adverse effect is more common with androgen receptor antagonists than GnRH agonists?

<p>Hepatotoxicity (A)</p> Signup and view all the answers

Which GnRH antagonist is used to prevent premature LH surges in fertility treatment?

<p>Ganirelix (B)</p> Signup and view all the answers

How does 'chemical castration' occur via GnRH antagonists like degarelix?

<p>Suppression of LH secretion (A)</p> Signup and view all the answers

Which drug class can cause an initial tumor flare in metastatic prostate cancer?

<p>GnRH agonists (B)</p> Signup and view all the answers

What is the primary therapeutic use of ketoconazole in prostate cancer treatment?

<p>Advanced prostate cancer resistant to other therapies (B)</p> Signup and view all the answers

Which androgen receptor antagonist is known to delay dark adaptation as a side effect?

<p>Nilutamide (A)</p> Signup and view all the answers

What is the standard method of administration for GnRH antagonists such as degarelix?

<p>Subcutaneous injection (C)</p> Signup and view all the answers

Which of the following is a long-term adverse effect of androgen suppression in men?

<p>Gynecomastia (D)</p> Signup and view all the answers

Which GnRH agonist is specifically indicated for treating endometriosis?

<p>Leuprolide (B)</p> Signup and view all the answers

What mechanism do GnRH agonists like leuprolide use to reduce testosterone production?

<p>Continuous administration leading to receptor desensitization (A)</p> Signup and view all the answers

Finasteride is primarily used for which conditions?

<p>Benign prostatic hyperplasia (BPH) and male pattern baldness (D)</p> Signup and view all the answers

Which effect is commonly associated with the use of GnRH agonists in men?

<p>Immediate testosterone surge and tumor flare (B)</p> Signup and view all the answers

Flashcards

GnRH Antagonists

Drugs that competitively inhibit GnRH receptors, suppressing gonadotropin secretion.

Degarelix Usage

Used therapeutically for metastatic prostate cancer to reduce testosterone production.

GnRH Agonists

Continuous administration causes receptor desensitization, suppressing gonadotropin secretion.

Tumor Flare

A transient increase in tumor size due to initial increase in gonadotropins from GnRH agonists.

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Androgen Receptor Antagonists

Drugs that competitively inhibit androgen receptors to prevent androgen activity.

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Flutamide

An androgen receptor antagonist known for its potential hepatotoxicity.

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Ketoconazole Action

Inhibits androgen synthesis, used for treating advanced prostate cancer.

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GnRH Receptor Mechanism

GnRH antagonists block receptors leading to decreased LH and testosterone.

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Injection site reactions

Adverse effects that occur at the site of injection, commonly with GnRH antagonists.

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Enzalutamide

A potent androgen receptor antagonist used to treat metastatic prostate cancer.

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Finasteride

A 5-alpha reductase inhibitor approved for BPH and male pattern baldness.

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Chemical castration

Achieved by GnRH antagonists that suppress LH and testosterone production.

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Degarelix

A GnRH antagonist that provides chemical castration without an initial tumor flare.

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Degarelix adverse effect

Degarelix causes injection site reactions, unlike GnRH agonists that may cause tumor flare.

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Most potent androgen antagonist

Enzalutamide is the most potent androgen receptor antagonist for advanced prostate cancer.

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Oral androgen antagonist

Bicalutamide is given orally and combined with GnRH agonists to reduce tumor flare.

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GnRH agonists use

GnRH agonists are primarily used for 'chemical castration' by reducing testosterone levels.

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Shared adverse effect of ketoconazole

Both ketoconazole and androgen receptor antagonists are associated with hepatotoxicity.

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GnRH antagonists in ovarian stimulation

GnRH antagonists prevent premature LH surges in controlled ovarian stimulation protocols.

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Osteoporosis risk with drugs

Long-term GnRH agonist use can increase osteoporosis risk in men due to testosterone suppression.

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Limitations of ketoconazole

Ketoconazole has numerous CYP450-mediated drug interactions, limiting its use in treatment.

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Estrogen Reduction

Lowering estrogen levels to manage conditions like prostate cancer.

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Leuprolide

A GnRH agonist used for long-term treatment of hormone-responsive tumors.

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Ketoconazole Adverse Effect

Significant risk of hepatotoxicity when used for prostate cancer treatment.

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5-alpha Reductase Inhibitors

Drugs like dutasteride that block conversion of testosterone to DHT.

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Ganirelix Usage

GnRH antagonist used to prevent premature LH surges in fertility treatments.

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Tumor Flare Effect

Initial increase in tumor size due to GnRH agonists raising testosterone levels.

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GnRH Antagonists Administration

GnRH antagonists like degarelix are administered via subcutaneous injection.

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Adverse Effects of Androgen Suppression

Long-term androgen suppression can lead to gynecomastia in men.

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Tumor Flare in GnRH Agonists

A transient increase in tumor size due to an initial testosterone surge.

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Mechanism of GnRH Agonists

They cause receptor desensitization, reducing LH and testosterone production.

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Visual Disturbances with Nilutamide

Nilutamide is known for causing delayed dark adaptation as a side effect.

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Tumor flare mechanism

An initial increase in LH and testosterone levels due to GnRH agonists.

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GnRH antagonists use

Primarily used to treat metastatic prostate cancer by reducing testosterone.

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Nilutamide side effects

Commonly associated with visual disturbances.

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Bicalutamide safety

Associated with fewer hepatotoxic effects compared to flutamide.

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GnRH agonists in precocious puberty

Suppress premature gonadotropin release to delay puberty.

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GnRH agonists adverse effect

Long-term use can lead to osteoporosis due to estrogen suppression.

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Enzalutamide function

Blocks androgen receptor activation in prostate cancer treatment.

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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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Description

This quiz covers essential topics related to GnRH agonists and antagonists, including their therapeutic applications, mechanisms of action, and associated adverse effects. Test your knowledge of the pharmacological treatments for conditions like prostate cancer and benign prostatic hyperplasia.

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