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7361 Hem/Onc Block 3 > Hormonal > Flashcards

Hormonal Flashcards

1
Q

___ are c18 steroids with an aromatic A ring formed by CYP19 enzyme known as aromatase

a. progestins
b. estrogens
c. androgens

A

b. estrogens

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2
Q

The most potent endogenous estrogen is __, but __ is the major circulating estrogen.

a. estrone (E1), estradiol (E2)
b. estradiol (E1), estrone (E2)
c. estradiol (E2), estrone (E1)

A

c. estradiol (E2), estrone (E1)

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3
Q

Activation of ___ receptors leads to the increase or decrease of there transcription of multiple target genes

A

estrogen

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4
Q

Dysregulation of __ signaling fuels the growth of certain types of tumors

A

estrogen

termed HR+ breast cancer

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5
Q

Aromatase inhibitors are used to block estrogen production by the ovaries

a. true
b. false

A

b. false

can be used to block synthesis of estrogens in the periphery, but are not effective in blocking estrogen production by the ovaries

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6
Q

Tamoxifen drug class?

A

selective estrogen receptor (SERM)

directly blocks binding of estrogens to estrogen receptors, and is an option for premenopausal pts

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7
Q

Tamoxifen is an option for postmenopausal pts

a. true
b. false

A

b. false

PREmenopausal pts

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8
Q

Tamoxifen is highly ___

a. hydrophilic
b. lipophilic

A

b. lipophilic

contributes to its high protein binding (> 98%) and long terminal half life (5-7 days)

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9
Q

Poor CYP___ metabolizers may benefit less from tamoxifen therapy

A

2D6

pts taking concomitant meds that are strong CYP2D6 inhibitors may benefit less from tamoxifen therapy

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10
Q

Tamoxifen is generally well tolerated, the most frequent side effect is ___

A

hot flashes

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11
Q

Tamoxifen stimulates the proliferation of ___ cells

A

endometrial

causes thickening of the endometrium, and increases the risk for developing endometrial cancer

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12
Q

What is the most frequent side effect of the SERM tamoxifen?

A

hot flashes

generally well tolerated

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13
Q

___ aromatase inhibitors are steroidal and bind irreversibly at the androgen binding site

a. type I
b. type II

A

a. type I

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14
Q

Which type of aromatase inhibitor binds irreversibly?

A

type I

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15
Q

which type of aromatase inhibitor binds reversibly?

A

type II

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16
Q

___ aromatase inhibitors are non-steroidal and bind reversibly to the heme of the enzyme.

a. type I
b. type II

A

b. type II

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17
Q

Type I aromatase inhibitor:

___ is a synthetic derivative of androstenedione where changes in the A/B ring system make the A ring electrophilic and able to form a covalent bond with the enzyme.

A

exemestane

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18
Q

What is the most common AE of exemestane?

A

hot flashes

generally well tolerated

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19
Q

Exemestane places pts at a greater risk for what condition?

A

osteoporosis

causes loss in bone density

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20
Q

___ are type II aromatase inhibitors

a. exemestane
b. anastrozole
c. letrozole

select all that apply

A

b, c

Type II aromatase inhibitors are non-steroidal and bind reversibly to the heme of the enzyme

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21
Q

Two most common AEs of the type II aromatase inhibitors anastrozole and letrozole?

A

hot flashes

night sweats

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22
Q

The type II aromatase inhibitors anastrozole and letrozole can cause what condition?

A

osteoporosis

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23
Q

Selective estrogen receptor degraders (SERD) are always ___

a. agonistic
b. antagonistic

A

b. antagonistic

devoid of estrogenic activity in all tissues

In addition to blocking estrogen receptor activation, a SERD makes the estrogen receptor a target for proteolytic degradation, thereby reducing the total number of receptors present

24
Q

What drug class if fulvestrant?

25
___ is an estradiol analog with a lipophilic side chain at the 7-position
fulvestrant
26
What enables the long duration of action of fulvestrant?
it is lipophilic and very insoluble once monthly dosing
27
Activation of __ receptors increases or decreases the transcription of multiple target genes a. estrogen b. androgen
b. androgen
28
Dysregulation of androgen signaling fuels the growth of __ cancer
prostate
29
Inhibition of what CYP blocks testosterone biosynthesis?
CYP17
30
4 approaches to limit the ability of androgens to cause prostate cancer?
- GnRH agonists down regulate GnRH receptors - GnRH antagonists block GnRH receptors - CYP17 inhibitors block testosterone biosynthesis - androgen receptor antagonists block androgen receptors
31
GnRH agonists are modified analogs of GnRH with changes to the AA residues at positions __ and __ that lead to increased receptor affinity and resistance to enzymatic degradation
6, 10 GnRH agonists: - leuprolide - histrelin - triptorelin - goserelin
32
Which GnRH agonist is a biodegradable implant?
goserelin other implants must be removed
33
GnRH agonists: After one week the continuous GnRH receptor activation causes negative feedback and down regulation, decreasing LH and FSH with testosterone reaching castation levels (<50ng/dL) after ___ weeks
3-4
34
GnRH agonists: During the ___, the increased testosterone levels may stimulate prostate cancer growth and lead to a flare in symptoms
transient surge
35
Degarelix is a GnRH ___ a. agonist b. antagonist
b. antagonist
36
__ is a 10 AA peptide that contains 3 proteinogenic AA residues and 7 residues that are synthetic AA derivatives
degarelix
37
What is the MOA of the GnRH antagonist degarelix?
competes directly wit GnRH for binding site on anterior pituitary gland where its binding inhibits release of LH and FSH causing drop in serum testosterone
38
How is the GnRH antagonist degarelix administered? a. IM b. SC c. IV
b. SC forms a depot for continuous delivery, making it suitable for once monthly dosing
39
With the GnRH antagonist degarelix pts reach castration level of testosterone about ___ days after the initial dose and avoid the flare phenomenon seen with GnRH agonists
3
40
GnRH antagonists: ___ is a small molecule (non-peptide) competitive antagonist of GnRH receptors that is available as a once daily oral tablet a. degarelix b. relugolix
b. Relugolix
41
The GnRH antagonist relugolix is a substrate of what transporter?
P-gp strong inhibitors/inducers of P-gp should be avoided if possible
42
Which CYP catalyzes two important reactions in the biosynthesis of testosterone and DHT?
CYP17
43
CYP17 inhibition can prevent synthesis of testosterone in ___ a. peripheral tissues b. tumors c. none of the above d. a and b
d. a and b
44
CYP17 inhibitors should be administered with low dose ___
glucocorticoids ex. prednisone
45
A double bond at what position is critical for irreversible inhibition of CYP17?
C16-C17
46
An acetate ester instead of a hydroxyl at the C3 position is hydrolyzed in vivo to what active metabolite?
abiraterone
47
The CYP17 inhibitor abiraterone is a strong inhibitor of what CYP?
CYP2D6 can increase the exposure of drugs metabolized by CYP2D6
48
What drug class competes directly with DHT for the binding site on androgen receptors and inhibits the activation of gene transcription targets?
non-steroidal anti-androgens (NSAA)
49
What drug class is bicalutamide?
non-steroidal anti-androgen (NSAA)
50
non-steroidal anti-androgen: Which bicalutamide enantiomer is directly glucuronidated and rapidly cleared? a. S-enantiomer b. R-enantiomer
a. S-enantiomer
51
non-steroidal anti-androgen: Which bicalutamide enantiomer is first oxidized by CYP3A4 prior to conjugation and has an elimination half life of one week? a. S-enantiomer b. R-enantiomer
b. R-enantiomer
52
non-steroidal anti-androgen: Which bicalutamide enantiomer has higher plasma concentrations at steady state? a. S-enantiomer b. R-enantiomer
b. R-enantiomer 100x higher
53
Enzalutamide drug class?
non-steroidal anti-androgen (NSAA)
54
non-steroidal anti-androgen: Which is an active metabolite too enzalutamide that has equal AR potency and terminal half life to enzalutamide? a. M1 b. M2
b. M2 t1/2 = 7.8 to 8.6 days
55
The non-steroidal anti-androgen enzalutamide is a strong inducer of CYP___ and moderate inducer of CYP ___ and CYP___
3A4, 2C9, 2C19 avoid use with drugs that are metabolized by these enzymes and have narrow therapeutic indices

7361 Hem/Onc Block 3 (9 decks)

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