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.</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.</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.</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.</p> Signup and view all the answers

    Why is Fulvestrant considered a potent pure estrogen antagonist?

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

    Which metabolites of 17a-ethinylestradiol undergo enterohepatic recycling?

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

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

    <p>Fulvestrant</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</p> Signup and view all the answers

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

    <p>Tamoxifen</p> Signup and view all the answers

    Which medication is a third-generation aromatase inhibitor?

    <p>Anastrozole</p> Signup and view all the answers

    Which medication is a pure anti-oestrogen?

    <p>Fulvestrant</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</p> Signup and view all the answers

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

    <p>Raloxifene</p> Signup and view all the answers

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

    <p>Raloxifene</p> Signup and view all the answers

    Which of the following estrogenic agents can undergo enterohepatic recycling?

    <p>Estropipate</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</p> Signup and view all the answers

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

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

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

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

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

    <p>Equilin</p> Signup and view all the answers

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

    <p>ERδ</p> Signup and view all the answers

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

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

    What is the effect of tamoxifen on the endometrium?

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

    What is the effect of tamoxifen on bone tissue?

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

    What is the risk of poor metabolizers of tamoxifen?

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

    What is raloxifene used for in postmenopausal women?

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

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