Pharmacology: 17a-Ethinylestradiol Metabolism

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Questions and Answers

Which statement accurately describes Tamoxifen's mechanism of action?

  • Tamoxifen is a pure estrogen antagonist.
  • Tamoxifen competes with estradiol for ER binding. (correct)
  • Tamoxifen is an agonist of ER.
  • Tamoxifen binds, blocks, and degrades ER.

What distinguishes Fulvestrant in terms of its mechanism of action?

  • Fulvestrant acts as an agonist on ER.
  • Fulvestrant is a competitive antagonist that interferes with ER dimerization. (correct)
  • Fulvestrant is a nonsteroidal anti-aromatase.
  • Fulvestrant enhances estrogen signaling.

Why is Fulvestrant considered a potent anti-estrogen?

  • Fulvestrant degrades ER and does not allow estrogen signaling. (correct)
  • Fulvestrant is a non-aromatic estradiol derivative.
  • Fulvestrant is an estradiol derivative with no modifications.
  • Fulvestrant does not compete with estradiol for ER binding.

Which of the following correctly describes Fulvestrant's structure?

<p>Fulvestrant is a non-aromatic estradiol-derivative. (B)</p> Signup and view all the answers

What role does Fulvestrant play in estrogen receptor-positive metastatic breast cancer treatment?

<p>Fulvestrant degrades estrogen receptors and blocks estrogen signaling. (C)</p> Signup and view all the answers

Which characteristic makes Fulvestrant different from Tamoxifen?

<p>Fulvestrant binds to ER competitively with estradiol, while Tamoxifen degrades ER. (B)</p> Signup and view all the answers

What distinguishes Fulvestrant from being an agonist on estrogen receptors?

<p>Fulvestrant does not induce estrogen receptor degradation. (C)</p> Signup and view all the answers

Why is Fulvestrant considered a potent pure estrogen antagonist?

<p>Fulvestrant blocks and degrades estrogen receptors effectively. (C)</p> Signup and view all the answers

Which component of representative oral contraceptives is known for potentially interfering with enterohepatic cycling of EE, reducing its efficacy?

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

What role does the ethinyl group play in 17a-ethinylestradiol (EE)?

<p>Blocks oxidative metabolism at the D-ring (C)</p> Signup and view all the answers

Which type of estradiol derivative shows prolonged activity due to deposition in adipose tissue, where it is slowly released and converted to EE?

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

Which type of estrogens contain one or two additional double bonds in the steroidal B ring, leading to potentiation of estrogenic activity?

<p>Conjugated Equine Estrogens (A)</p> Signup and view all the answers

What is the primary reason for the metabolic stability of 17a-ethinylestradiol (EE)?

<p>Ethinyl substituent's effect on oxidative metabolism (D)</p> Signup and view all the answers

Which metabolites of 17a-ethinylestradiol undergo enterohepatic recycling?

<p>3-O-glucoronide and 3-O-sulfate (A)</p> Signup and view all the answers

How do antibacterial agents affect the enterohepatic cycling of EE when used as a major oral contraceptive?

<p>Reduce contraceptive efficacy of EE (C)</p> Signup and view all the answers

'Metabolic O-demethylation' is primarily associated with the estrogenicity of which EE-ether derivative?

<p>[EE]-ether derivatives (mestranol, quinestrol) (A)</p> Signup and view all the answers

'Chemically inert ethinyl-C17 substituent blocks oxidative metabolism at the D-ring' refers to which synthetic steroidal estrogen?

<p>[EE] Synthetic steroidal estrogens with prolonged activity (B)</p> Signup and view all the answers

Which of the following is the most water-soluble estrogen receptor ligand?

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

Which medication is approved by the FDA for preventing breast cancer in women at high risk?

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

Which compound is a prodrug metabolized in the liver by the cytochrome P450 isoform CYP2D6?

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

Which medication is a third-generation aromatase inhibitor?

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

Which medication is a pure anti-oestrogen?

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

Which medication is used for the treatment of early and advanced estrogen receptor positive breast cancer?

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

Which medication is used to prevent osteoporosis with breast and endometrial safety?

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

Which medication is a Selective Estrogen Receptor Modulator (SERM)?

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

Which of the following estrogenic agents can undergo enterohepatic recycling?

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

What is the primary route of administration for hormonal replacement therapy (HRT) for the treatment of menopausal symptoms?

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

Which of the following is an example of an estrogen-only HRT?

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

Which of the following medications is used to treat symptoms of menopause using a transdermal patch?

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

What is the purpose of adding a progestin to estrogen in HRT for the treatment of menopausal symptoms?

<p>To reduce the risk of endometrial cancer associated with estrogen therapy (D)</p> Signup and view all the answers

Which of the following is NOT a common side effect of estrogen therapy?

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

Which of the following estrogens is derived from pregnant mares' urine?

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

Which of the following is NOT a type of estrogen receptor?

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

How does 4-hydroxytamoxifen affect transcription of estrogen-responsive genes in breast tissue?

<p>It inhibits transcription (D)</p> Signup and view all the answers

What is the role of CYP2D6 in the metabolism of tamoxifen?

<p>It metabolizes tamoxifen into its more potent metabolites (D)</p> Signup and view all the answers

What is the effect of tamoxifen on the endometrium?

<p>It acts as a partial agonist (B)</p> Signup and view all the answers

What is the effect of tamoxifen on bone tissue?

<p>It has anti-osteoporotic effects (D)</p> Signup and view all the answers

What is the risk of poor metabolizers of tamoxifen?

<p>They have poorer clinical outcomes (D)</p> Signup and view all the answers

What is raloxifene used for in postmenopausal women?

<p>Treatment of osteoporosis and breast cancer (A)</p> Signup and view all the answers

What is the type of drug that tamoxifen and raloxifene belong to?

<p>Selective estrogen receptor modulators (SERMs) (D)</p> Signup and view all the answers

What is the role of CYP2D6 in the metabolism of tamoxifen for patients with variant forms of the gene?

<p>They metabolize tamoxifen slower (C)</p> Signup and view all the answers

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