Hellekant Antineoplastics Flashcards

1
Q

What is goserelin?

A

GnRH receptor agonist

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2
Q

What is leuprolide?

A

GnRH agonist

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3
Q

What is Degarelix?

A

GnRH receptor antagonist

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4
Q

What tissues produce 5 alpha reductase?

A

Prostate, external genitalia, skin

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5
Q

What is the MOA of finasteride?

A

5 alpha reductase inhibitor; inhibits conversion of testosterone to DHT

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6
Q

What is the MOA of dutasteride?

A

5 alpha reductase inhibitor; prevents conversion of testosterone to DHT

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7
Q

What 5 alpha reductase inhibitor has a trophic effect on the prostate?

A

Dutasteride

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8
Q

What is abiraterone?

A

17 alpha hydroxylase and 17,20-lyase inhibitor; prevents testosterone synthesis

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9
Q

What tissues does testosterone target?

A

Muscle, seminal vesicle, epididymis, bone

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10
Q

What is the MOA of bicalutamide?

A

Blocks androgen receptors

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11
Q

What is the MOA of flutamide?

A

Blocks androgen receptors

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12
Q

In treatment of prostate cancer, leuprolide is administered with what for the first few weeks? Why?

A

Leuprolide (GnRH agonist) is administered with androgen receptor blocker (eg bicalutamide) to prevent early GnRH stimulation

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13
Q

What is aminoglutethimide?

A

Blocks pregnenolone synthesis

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14
Q

What drug blocks 17 alpha hydroxylase and is used in the treatment of prostate cancer?

A

Abiraterone

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15
Q

What is anastrazole?

A

Aromatase inhibitor

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16
Q

What is the MOA of anastrazole?

A

Inhibit aromatase, preventing the conversion of testosterone to estradiol 17 beta and androstendione to estrone

17
Q

What is exemestane?

A

Irreversibly inhibitor of aromatase

18
Q

What is fluvestrant?

A

Selective estrogen downregulator; inhibits all ER actions and causes ER degradation following SERD binding

19
Q

What is tamoxifen?

A

SERM; antagonist at breast, agonist and uterus and bone

20
Q

What is an AE due to tamoxifen use?

A

Endometrial cancer due to agonism at the uterus

21
Q

What is Raloxifene?

A

SERM; antagonist at breast and uterus; agonist at bone

22
Q

What is tormifene?

A

SERM; antagonist at breast; no effect on bone, ? On uterus

23
Q

What SERM is an antagonist at the breast and uterus, but is an agonist at the bone?

A

Raloxifene

24
Q

What is letrozole?

A

Aromatase inhibitor