41 Questions
Which statement accurately describes Tamoxifen's mechanism of action?
Tamoxifen competes with estradiol for ER binding.
What distinguishes Fulvestrant in terms of its mechanism of action?
Fulvestrant is a competitive antagonist that interferes with ER dimerization.
Why is Fulvestrant considered a potent anti-estrogen?
Fulvestrant degrades ER and does not allow estrogen signaling.
Which of the following correctly describes Fulvestrant's structure?
Fulvestrant is a non-aromatic estradiol-derivative.
What role does Fulvestrant play in estrogen receptor-positive metastatic breast cancer treatment?
Fulvestrant degrades estrogen receptors and blocks estrogen signaling.
Which characteristic makes Fulvestrant different from Tamoxifen?
Fulvestrant binds to ER competitively with estradiol, while Tamoxifen degrades ER.
What distinguishes Fulvestrant from being an agonist on estrogen receptors?
Fulvestrant does not induce estrogen receptor degradation.
Why is Fulvestrant considered a potent pure estrogen antagonist?
Fulvestrant blocks and degrades estrogen receptors effectively.
Which component of representative oral contraceptives is known for potentially interfering with enterohepatic cycling of EE, reducing its efficacy?
Quinestrol
What role does the ethinyl group play in 17a-ethinylestradiol (EE)?
Blocks oxidative metabolism at the D-ring
Which type of estradiol derivative shows prolonged activity due to deposition in adipose tissue, where it is slowly released and converted to EE?
Mestranol
Which type of estrogens contain one or two additional double bonds in the steroidal B ring, leading to potentiation of estrogenic activity?
Conjugated Equine Estrogens
What is the primary reason for the metabolic stability of 17a-ethinylestradiol (EE)?
Ethinyl substituent's effect on oxidative metabolism
Which metabolites of 17a-ethinylestradiol undergo enterohepatic recycling?
3-O-glucoronide and 3-O-sulfate
How do antibacterial agents affect the enterohepatic cycling of EE when used as a major oral contraceptive?
Reduce contraceptive efficacy of EE
'Metabolic O-demethylation' is primarily associated with the estrogenicity of which EE-ether derivative?
[EE]-ether derivatives (mestranol, quinestrol)
'Chemically inert ethinyl-C17 substituent blocks oxidative metabolism at the D-ring' refers to which synthetic steroidal estrogen?
[EE] Synthetic steroidal estrogens with prolonged activity
Which of the following is the most water-soluble estrogen receptor ligand?
Fulvestrant
Which medication is approved by the FDA for preventing breast cancer in women at high risk?
Tamoxifen
Which compound is a prodrug metabolized in the liver by the cytochrome P450 isoform CYP2D6?
Tamoxifen
Which medication is a third-generation aromatase inhibitor?
Anastrozole
Which medication is a pure anti-oestrogen?
Fulvestrant
Which medication is used for the treatment of early and advanced estrogen receptor positive breast cancer?
Tamoxifen
Which medication is used to prevent osteoporosis with breast and endometrial safety?
Raloxifene
Which medication is a Selective Estrogen Receptor Modulator (SERM)?
Raloxifene
Which of the following estrogenic agents can undergo enterohepatic recycling?
Estropipate
What is the primary route of administration for hormonal replacement therapy (HRT) for the treatment of menopausal symptoms?
Oral
Which of the following is an example of an estrogen-only HRT?
Estradiol acetate
Which of the following medications is used to treat symptoms of menopause using a transdermal patch?
Estradiol
What is the purpose of adding a progestin to estrogen in HRT for the treatment of menopausal symptoms?
To reduce the risk of endometrial cancer associated with estrogen therapy
Which of the following is NOT a common side effect of estrogen therapy?
Hair loss
Which of the following estrogens is derived from pregnant mares' urine?
Equilin
Which of the following is NOT a type of estrogen receptor?
ERδ
How does 4-hydroxytamoxifen affect transcription of estrogen-responsive genes in breast tissue?
It inhibits transcription
What is the role of CYP2D6 in the metabolism of tamoxifen?
It metabolizes tamoxifen into its more potent metabolites
What is the effect of tamoxifen on the endometrium?
It acts as a partial agonist
What is the effect of tamoxifen on bone tissue?
It has anti-osteoporotic effects
What is the risk of poor metabolizers of tamoxifen?
They have poorer clinical outcomes
What is raloxifene used for in postmenopausal women?
Treatment of osteoporosis and breast cancer
What is the type of drug that tamoxifen and raloxifene belong to?
Selective estrogen receptor modulators (SERMs)
What is the role of CYP2D6 in the metabolism of tamoxifen for patients with variant forms of the gene?
They metabolize tamoxifen slower
Explore the metabolic pathways and pharmacokinetics of 17a-Ethinylestradiol, a stable oral estrogen compound with a duration of action of 14-28 days. Learn about its metabolites, enterohepatic recycling, and how antibacterial agents can potentially interfere with its metabolism.
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