Untitled Deck Flashcards

(50 cards)

1
Q

Which of the following is the most potent naturally occurring estrogen?

A

Estradiol

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2
Q

What enzyme is responsible for the aromatization of ring A in estrogens?

A

Aromatase (CYP19)

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3
Q

The steroidal nucleus “Estrane” contains how many carbon atoms?

A

18

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4
Q

Which ring fusion pattern is most common in natural steroid hormones?

A

Trans/Trans/Trans

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5
Q

The oral inactivity of estradiol is primarily due to what process?

A

Degradation of ring D and first-pass metabolism

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6
Q

Estradiol exerts negative feedback directly on which pituitary hormone?

A

FSH

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7
Q

Which estrogen is most abundant in urine?

A

Estriol

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8
Q

The steroid class “Cholestane” contains how many carbon atoms?

A

27

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9
Q

In natural hormones, the A/B ring fusion is typically _____?

A

Trans

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10
Q

Which synthetic estrogen has a 17α-ethinyl group that prevents rapid oxidation?

A

Ethinyl estradiol

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11
Q

The hormone with structure Estra-1,3,5(10)-triene-3,17β-diol is _____?

A

Estradiol

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12
Q

Aromatization in estrogens occurs in which ring?

A

Ring A

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13
Q

Why is mestranol used in oral contraceptives?

A

It is a prodrug of ethinyl estradiol

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14
Q

The steroid “Pregnane” forms the base skeleton of which hormone class?

A

Progestins

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15
Q

Name a depot (IM) estradiol ester formulation.

A

Estradiol benzoate

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16
Q

CYP11A1 converts cholesterol into which immediate product?

A

Pregnenolone

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17
Q

Which substituent increases oral bioavailability of estradiol?

A

Ethinyl group

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18
Q

What structural feature of estrogens is essential for activity?

A

Aromatic ring A

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19
Q

Which estrogen is formed predominantly by the placenta during pregnancy?

A

Estriol

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20
Q

Reduction of the C17 keto group during metabolism yields which estrogen?

A

Estradiol

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21
Q

Which estradiol ester has the longest IM duration of action?

A

Estradiol cypionate

22
Q

Which component of Premarin is derived from pregnant mares?

23
Q

Estradiol benzoate is best described as what type of preparation?

A

Esterified depot formulation

24
Q

Using conjugated estrogens as sodium sulfate esters primarily serves to _____?

A

Attenuate estrogenic potency (reduce activity until hydrolyzed)

25
Ethinyl estradiol assay commonly uses what analytical method?
Titration with NaOH after AgNO₃ addition
26
Clomiphene’s anti-estrogenic effect is most prominent in which sites?
Uterus and hypothalamus
27
Which geometric isomer of clomiphene is anti-estrogenic?
Trans (E)
28
Name the non-steroidal estrogen used in prostate cancer therapy.
Diethylstilbestrol (DES)
29
Diethylstilbestrol’s highest potency lies in which isomer?
Trans
30
Fosfosterol was designed to act primarily as what?
A selective cancer-cell binder
31
Dienestrol is administered by which route to treat vaginal atrophy?
Vaginal cream
32
The primary endogenous source of estrone is _____?
Ovaries and adrenal glands
33
What chemical feature distinguishes mestranol from ethinyl estradiol?
A methylated hydroxyl group
34
Compared with its 17β-epimer, estradiol 17α is _____ potent.
Much less active
35
Estriol is considered the _____ potent natural estrogen.
Least
36
The steroid backbone “Androstane” contains how many carbons?
19
37
Which SERM carries the lowest risk of uterine cancer?
Raloxifene
38
Which estrogen possesses –OH groups at both C3 and C17β?
Estradiol
39
What core structure is key for estrogen-receptor binding in many SERMs?
Triphenylethylene core
40
In raloxifene, the terminal nitrogen is typically _____ to boost stability.
Incorporated into a ring (cyclic)
41
Which estrogen is most abundant in serum but not the most potent?
Estrone
42
What key difference makes fulvestrant unlike typical SERMs?
It triggers degradation of the estrogen receptor
43
Fulvestrant’s anti-estrogenic action results from what mechanism?
Receptor dimerization inhibition and degradation
44
The long lipophilic chain of fulvestrant is attached at which carbon?
C6
45
Fulvestrant is primarily indicated for which condition?
Metastatic hormone-receptor-positive breast cancer
46
Which enzyme converts androstenedione to estrone?
Aromatase (CYP19)
47
Letrozole’s aromatase-inhibitory activity relies on which ring system?
Triazole ring
48
CYP2D6 metabolizes which selective estrogen-receptor modulator?
Tamoxifen
49
Endoxifen is the active metabolite derived from which parent drug?
Tamoxifen
50
Before prescribing tamoxifen, genetic testing may be needed for what?
CYP2D6 polymorphism