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Reproductive Pharm > Drugs for Prostate Cancer > Flashcards

Drugs for Prostate Cancer Flashcards

1
Q

What is unique pharmacologically about prostate Cancer?

A

Prostate cancer is the most hormone sensitive of all cancers. Also one must take into account 2 sources of androgens (Testis and Adrenals).

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2
Q

What is the first line treatment for prostate cancer?

A

Medical or surgical castration plus pure anti androgen drug is the first line treatment. Radiation may be an alternative treatment.

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3
Q

What are some drug targets for prostate cancer therapy?

A

Pituitary release of ACTH/LH
CYP17A1 (17-hyroxylase)
Androgen receptors

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4
Q

What are the GnRH agonists that are used to treat prostate cancer?

A

Goserelin
Histarelin
Leuprolide
Triptorelin

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5
Q

What is the MOA for the GnRH agonists in treating prostate cancer?

A

Continuous GnRH downregulates GnRH receptors thus decreasing the production of LH/FSH. The result is lower levels of sex hormones. However, there is an initial increase in GnRH receptor activation which can cause a disease flare.

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6
Q

What are some adverse effects which are common to the GnRH class?

A 
Decreased bone density
increased triglycerides
Weight gain
Sexual dysfunction, gynecomastia, 
Pregnancy Category X
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7
Q

Which GnRH agonists can be given SC?

A

Goserelin
Histarelin
Leuprolide

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8
Q

Which GnRh agonists can be given IM?

A

Leuprolide

Triptorelin

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9
Q

What adverse effects are unique to Histarelin?

A

Seizure

Suicide

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10
Q

WHat adverse effects are unique to Leuprolide?

A

MI

CHF

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11
Q

What is the MOA of Degarelix?

A

Degarelix is a GnRH antagonist. Has the same long term effect as the GnRH agonists, except there is no initial disease flare and castration occurs in 3 days.

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12
Q

How is Degarelix administered?

A

SC

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13
Q

What adverse effects are associated with Degarelix?

A

More important:
Elevated LFTs, Hepatotoxicity
QT prolongation, HTN

Less Important:
Hot flashes
Injection site rxn
impotence 
Arthralgia
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14
Q

Which drugs are the androgen receptor blockers?

A

Bicalutamide
Enzalutamide
Flutamide
Nilutamide

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15
Q

What is the MOA of the androgen receptor blockers?

A

Obviously they block the effects of stimulatory effects of Testosterone and DHT on the tumor. (stupid question)

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16
Q

What are some common adverse effects of the Androgen receptor blockers?

A

GI Toxicity
Hot flashes
Arthralgia/Myalgia
Teratogenic (except Nilutamide)

17
Q

What is unique about Bicalutamide?

A

Bicalutamide is an agonist and an antagonist with more effect in the prostate than centrally. Also known for CYP interactions

18
Q

What is unique about Enzalutamide?

A 
Enzalutamide has effects both in the prostate and centrally. 
Unique adverse effects include:
Seizures
URTI
Male teratogenicity
19
Q

What is unique about Flutamide?

A

Flutamide has effect in the prostate only. Unique adverse effects include Hepatotoxicity (BBW), and blood dyscrasias.

20
Q

What is Unique about Nilutamide?

A 
Nilutamide has effect in both the prostate and centrally.
Unique adverse effects include:
Interstitial pneumonitis
CHF/HTN
Blood dyscrasias
photosensitivity.
21
Q

What is Estramustine?

A

Estramustine is an estrogen with an alkylator attached to it.

22
Q

What is the MOA of Estramustine?

A

Binds estrogen binding protein on prostate cancer and delivers the alkylator which inhibits microtubules and causes DNA strand breaks.

23
Q

What adverse effects are associated with Estramustine?

A 
PE/DVT, MI, Stroke
GI tox
gynecomastia, mastalgia
Impotence, edema
increase LFTs.
24
Q

What is the MOA of Sipuleucel?

A

Sipuleucel involves taking the patients APCs, modifying them, and then putting them back in. They new APCs stimulate T cell immunity to prostatic acid phosphatase.

25
Q

What adverse effects are associated with Sipuleucel?

A

Parathesia,
Citrate toxicity
GI disturbance
Dyspnea

26
Q

What is the MOA of Abiraterone?

A

Abiraterone inhibits 17-hydroxylase. This prevents the production of DHEA and Androstenedione.

27
Q

What adverse effects are associated with Abiraterone?

A 
Increased mineralcorticoids (Suppress with ACTH)
Increased LFTs
CAT X (use condoms b/c semen may spread drug)
28
Q

Why aren’t 5-alpha-reductase inhibitors used to treat prostate cancer?

A

b/c they increase the risk of cancer (possibly?)

29
Q

What is the difference in the various estrogen receptors in the prostate?

A

Estrogen receptor Alpha promotes inflammation and malignant proliferation
Estrogen receptor beta is anti-inflammatory and reduces proliferation

30
Q

What is the conventional chemotherapeutic therapy for metastatic prostate cancer?

A

Taxanes

Mitoxantrone (used for palliation in severe Dz)

Reproductive Pharm (17 decks)

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