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Repro Pharm - Keith > Treatment of Prostate Cancer > Flashcards

Treatment of Prostate Cancer Flashcards

1
Q

MOA of bicalutamide

A

androgen receptor blocker. mostly in prostate (less central). Has some slight agonist activity in other tissues but mainly antagonist.

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2
Q

ADE of bicalutamide

A

GI toxicity, hot flashes, aches/pains
Hepatotoxicity
Teratogen

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3
Q

MOA of flutamide

A

androgen receptor Antagonist. Exclusively in prostate. (FLUTE-amide works only on your flute)
GI toxicity, hot flashes, aches/pains
hepato

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4
Q

ADE of flutamide

A

black box warning for hepatotoxicity/failure
blood dysacria
GI toxicity, hot flashes, aches/pains
Teratogen

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5
Q

MOA of nicalutamide (nilutamide)

A

androgen receptor blocker of prostate AND central

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6
Q

ADE of nicalutamide (nilutamide)

A 
Black box warning for respiratory insufficiency and interstitial penumonitis.
HF and HTN
Blood dysacria
Increased light to dark transition time.
GI toxicity, hot flashes, aches/pains
Hepatotoxicity
NOT A TERATOGEN - NULL-utamide
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7
Q

MOA of estramustine

A

Estrogen+nitrogen mustard that alkylates.
binds EBP on prostate CA.
inhibits microtubules, promoting disassembly and G2/M arrest.
Produces DNA strand breakage.
Has estrogenic effects.
Depressess testosterone levels via negative feedback on HP axis

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8
Q

ADE of estramustine

A

Has estrogenic effects similar to estradiol -> Edema, thromboembolism, MI, PE, and stroke.

GI, gynecomastia, mastalgia, impotence

elevated hepatic enzymes and hyperbilirubinemia

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9
Q

MOA of goserelin

A

GnRH agonist. SubCu.
down regulation of GnRH receptor on pituitary decreases FSH and LH. Serum levels of testosterone drop to castrate levels within 2-4 weeks.

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10
Q

ADE of goserelin

A

transient disease flare (give androgen receptor blocker)
CV effects - edema, HTN, MI
CNS - headache, fatigue, depression, seizures
Elevated TGs, weight gain
Reduced libido
gynecomastia
hepatotoxicity rarely

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11
Q

MOA of histrelin

A

GnRH agonist, SC injection.
down regulation of GnRH receptor on pituitary decreases FSH and LH. Serum levels of testosterone drop to castrate levels within 2-4 weeks.

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12
Q

ADE of histrelin

A 
transient disease flare (give androgen receptor blocker)
CV effects - edema, HTN, MI
CNS - headache, fatigue, depression, seizures, suicide (HYSTERIA-lin)
Elevated TGs, weight gain
Reduced libido
gynecomastia
hepatotoxicity rarely
CATEGORY X TERATOGEN
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13
Q

MOA of leuprolide

A

GnRH agonist. IM/SC injections.
down regulation of GnRH receptor on pituitary decreases FSH and LH. Serum levels of testosterone drop to castrate levels within 2-4 weeks.

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14
Q

ADE of leuprolide

A 
transient disease flare (give androgen receptor blocker)
CV effects - edema, HTN, MI
CNS - headache, fatigue, depression, seizures
Elevated TGs, weight gain
Reduced libido
gynecomastia
hepatotoxicity rarely
CATEGORY X TERATOGEN
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15
Q

MOA of triptorelin

A

GnRH agonist. IM injection.
down regulation of GnRH receptor on pituitary decreases FSH and LH. Serum levels of testosterone drop to castrate levels within 2-4 weeks.

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16
Q

ADE of tripttorelin

A 
transient disease flare (give androgen receptor blocker)
CV effects - edema, HTN, MI
CNS - headache, fatigue, depression, seizures
Elevated TGs, weight gain
Reduced libido
gynecomastia
hepatotoxicity rarely
CATEGORY X TERATOGEN
17
Q

MOA of degarelix

A

reversible GnRH receptor antagonist. SC injection. reduces LH and FSH secretion and drops testosterone to castrate levels within 3 days.

18
Q

ADE of degarelix

A 
hot sweats
HTN
Elevated hepatic enzymes 
QT prolongation
wiegh tgain, arthralgia, chills, fatigue
impotence
19
Q

MOA of abiraterone

A

CYP17 inhibitor (17a-hydroxylase inhibitor) prevents testosterone production and shunts towards mineralocorticoids.

20
Q

ADE of abiraterone

A

Increases mineralocorticoids causing HTN and fluid retention.
Contraindicated with preexisting CV issues.
Give with corticosteroids to suppress ACTH drive.
Elevated hepatic enzymes.
Category X teratogen (female partner precautions required)

21
Q

MOA of sipuleucel-T

A

Autologous (from-self) immunotherapy that stimulates T-cell immunity against prostatic acid phosphatase (PAP).
Made of pateint APCs cultured with recombinant PAP-GM-CSF. Product is reinfused with T, B and NK cells.

22
Q

ADE of sipuleucel-T

A

paresthesias, citrate toxicity and fatigue.

infusion reactions, fever/chills/dispnea, GI effects like N/V

23
Q

Where are the two sources of androgens acting in the prostate?

A

testicular testosterone
and
Locally produced DHT from adrenal produced dehydroepiandrosterone (DHEAS)

24
Q

What are the effects of ERa on prostate? ERb?

A

ERa mediates abberant proliferation, inflammation and malignancy.

ERb promotes antiproliferative, anti-inflammatory, and anticarcinogenic effects.

Repro Pharm - Keith (11 decks)

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