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REPRO > PHARM_prostate cancer > Flashcards

PHARM_prostate cancer Flashcards

1
Q

name the androgen receptor blockers (3)

A

bicalutamide
flutamide
nilutamide

AR-B-UTAMIDE

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2
Q

name the targeted alkylator used to treat prostate cancer

A

estramustine

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3
Q

name the GnRH agonists (4)

A

goserelin
histrelin
leuprolide
triptorelin

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4
Q

name the GnRH antagonist

A

degarelix

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5
Q

name the 17-alpha inhibitor

A

abiraterone

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6
Q

what is 1st line treatment for prostate cancer?

A

combined androgen blockade-medical or surgical castration plus a pure anti-androgen

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7
Q

how do the GnRH agonists treat prostate cancer?

A

they cause down regulation of the GnRH receptor on the pituitary gland & ultimately decreased prod. of FSH & LH
-serum levels of testosterone fall at 2-4 wks

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8
Q

a gain of function in prostatic cancer in what enzyme can cause a lot of conversion of DHEA –>DHT

A

3-betahydroxysteroid dehydrogenase

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9
Q

what is something you worry about when treating prostate cancer with hormone therapy?

A

the development of a super androgen receptor that can respond to lower levels or even function as a ligand-independent receptor

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10
Q

what is something you worry about when using GnRH agonists when treating prostate cancer?

A

initial transient dz flare (avoided by 2-4 wks of AR blockers)

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11
Q

the GnRH agonists can cause a hypoandrogenic state when given by injection, which includes what kinds of symptoms?

A

decreased bone mineral density–>spinal compression
elevated triglycerides; weight gain; DM–>CVD
reduced libido; sex dysfunction; gynecomastia–>sexually related

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12
Q

how does degarelix work?

A

reversible GnRH receptor antagonist given by SC injection

  • reduced LH & FSH secretion
  • reach castrate Testosterone levels w/i 3 days
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13
Q

what are some of the AEs of degarelix that are consistent with hypoandrogenic state?

A
  • hot sweats, weight gain

- htn, arthralgia, chills, fatigue, impotence

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14
Q

what are some of the AEs of degarelix that are not consistent with a hypoandrogenic state?

A

QT prolongation & elevated hepatic enzyme levels (reversible)

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15
Q

how does estramustine work?

A

conjugated drug which carries alkylating agent attached to an estradiol structure
-binds Estramustine binding protein (EBP) on prostate CA-inhibits microtubules, promoting dis-assembly & G2/M arrest-produces DNA strand breakage

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16
Q

how is estramustine administered?

A

oral

17
Q

what are some of the common AEs of estramustine?

A

GI upset, gynecomastia, mastalgia & impotence

18
Q

what may happen with estramustine therapy as a result of the elevated estradiol levels?

A

edema, thromboembolism, MI, PE or stroke

19
Q

flutamide has a BBW for what?

A

hepatotoxicity/failure

20
Q

nilutamide has a BBW for what?

A

respiratory insufficiency

21
Q

all the androgen receptor blockers are teratogens except for what drug?

A

nilutamide

22
Q

bicalutamide has selectivity for blocking which receptors?

A

prostate>central

23
Q

flutamide blocks which androgen receptors?

A

prostate

24
Q

nilutamide blocks which androgen receptors?

A

prostate & central

25
Q

what type of adverse effects do all the androgen receptor blockers have in common?

A

all produce AEs of hypoandrogenic state

26
Q

how does sipuleucel-T work?

A

autologous cellular immunotherapy designed to stimulate T-cell immunity against prostatic acid phosphatase

  • pt APCs (leukapheresis) cultured w/ recombinant PAP-GM-CSF
  • APCs take up antigen, process & express fragments on surface
  • Product (w/ immune cells) reinfused
27
Q

what are some of the AEs of sipuleucel-T?

A

mild infusion rxns; fever/chills/dyspnea; GI effects like N/V
-Paresthesias, citrate toxicity & fatigue

28
Q

how does Abiraterone work?

A

CYP17 inhibitor (prevents production of androgens)

29
Q

what are some of the AEs of abiraterone?

A

produces increased mineralocorticoid state

  • HTN, hypokalemia, & fluid retention
  • caution w/ pre-existing CV issues
30
Q

how do you reduce the symptoms of an increased mineralocorticoid state with abiraterone?

A

use corticosteroid to suppress ACTH drive

31
Q

should we use finasteride and dutasteride to prevent prostate cancer?

A

NO

32
Q

what are the conventional drugs used to treat prostate cancer?

A

docetaxel and carbazitaxel (poor substrate for P-gp, penetrates BBB) and mitoxantrone (+prednisone) which is used for palliation of severe pain

33
Q

which conventional chemotherapeutic used to treat prostate cancer is a poor substrate for P-gp and penetrates the BBB?

A

carbazitaxels

REPRO (13 decks)

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