Question 1

Antiestrogens

Accepted Answer

Antiestrogens are drugs that block ERs, and hence only work against cells that are ER positive. Benefits derive from depriving tumor cells of the growth-promoting influence of estrogen. Three antiestrogens—tamoxifen, toremifene, and fulvestrant—are approved for adjuvant treatment. Of these, tamoxifen is by far the most widely used.

Question 2

Tamoxifen - use

Accepted Answer

Used for established breast cancer disease and for reducing occurrence in high-risk patients Adjuvant therapy after surgery Treatment of metastatic disease

Question 3

Aromatase Inhibitors

Accepted Answer

The aromatase inhibitors are used to treat ER-positive breast cancer in postmenopausal women. These drugs block the production of estrogen from androgenic precursors, and thereby deprive breast cancer cells of the estrogen they need for growth. Aromatase inhibitors do not block production of estrogen by the ovaries, and hence are of little benefit in premenopausal women. In fact, aromatase inhibitors may cause a compensatory rise in estradiol in premenopausal patients. Aromatase inhibitors are more effective than tamoxifen and have a different toxicity profile. Unlike tamoxifen, aromatase inhibitors pose no risk of endometrial cancer and only rarely cause thromboembolism. However, they can increase the risk of fractures and have been associated with moderate to severe myalgias.

Question 4

Anastrozole - use

Accepted Answer

Used to treat ER-positive breast cancer in postmenopausal women

Question 5

Localized Prostate Cancer

Accepted Answer

Surgery + Radiation. (Optional Drug Treatment)

Question 6

Metastatic Prostate Cancer

Accepted Answer

Drug Treatment, Castration

Question 7

Androgen Deprivation Therapy

Accepted Answer

Lowers testosterone production Drugs used to block testosterone receptors Slows progression, increases comfort Gonadotropin Releasing Hormone Agonists Gonadotropin Releasing Hormone Antagonists

Question 8

Gonadotropin-Releasing Hormone Agonists

Accepted Answer

The gonadotropin-releasing hormone (GnRH) agonists suppress production of androgens by the testes—but not by the adrenal glands and prostate cancer cells. Currently, four GnRH agonists are available: leuprolide, triptorelin, goserelin, and histrelin. All four are indicated for cancer of the prostate. In addition, leuprolide is used for endometriosis

Question 9

Leuprolide - use

Accepted Answer

Advanced prostate cancer Palliation, not cure, is primary benefit

Question 10

Gonadotropin-Releasing Hormone Antagonists

Accepted Answer

Like the GnRH agonists, the GnRH antagonists suppress production of androgens by the testes. However, in contrast to the GnRH agonists, the GnRH antagonists do not produce an initial tumor flare. Currently, only one GnRH antagonist—degarelix—is available.

Question 11

Degarelix - use

Accepted Answer

palliative therapy of advanced prostate cancer in men who are not candidates for a GnRH agonist, and who do not want surgical castration Suppress production of androgens Do not produce initial tumor “flare”

Question 12

Leuprolide - mechanism of action

Accepted Answer

Stimulates pituitary to release ICSH (TestisAndrogens). After initial surge, pituitary becomes desensized to stimulationreduced ICSH Cotreatment with an androgen receptor blocker Prevents surge effects Blocks androgens produced by other sources

Question 13

Leuprolide - adverse effects

Accepted Answer

Generally well tolerated Hot flashes Testosterone loss may aggravate bone pain and urinary obstruction Concurrent treatment with androgen receptor blocker can minimize these effects

Question 14

Degarelix - mechanism of action

Accepted Answer

blockade of GnRH receptors in the anterior pituitary, which decreases release of luteinizing hormone and follicle-stimulating hormone, which in turn deprives the testes of the stimulus they need for testosterone production.

Question 15

Degarelix - adverse reactions

Accepted Answer

hot flashes, reduced libido, erectile dysfunction, gynecomastia, decreased muscle mass, decreased bone mass with associated increased risk of fractures and injection site reactions.

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Week 7 - Chapter 103 Anticancer Drugs II Flashcards

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