Immune altering and hormonal therapy - 23 to 33 Flashcards

1
Q

How does hormonal therapy work in cancer?

A

Steroid hormones bind steroid responsiveness element on DNA
Binding activates or promotes gene expression, usually growth factors

Hormone-response elements remain so that in presence of hormone, oncogenes can drive tumor growth

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2
Q

How do glucocorticoids work in cancer?

A

Suppress white blood cells, used in acute lymphoblastic leukemias to decrease leukemic cells

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3
Q

How do anti-estrogens work in cancer?

A

Used in breast, uterine, cervix, ovaries

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4
Q

How do anti-androgens work in cancer?

A

Used in testicular and prostate cancers

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5
Q

What is Tamoxifen?

A

Estrogen partial agonist (SERM), competes with estrogen for receptor binding

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6
Q

Indications for Tamoxifen?

A

Estrogen dependent breast tumors

Also used to reduce risk of developing breast tumors in women with strong family history, premenopausal women given for 5 years, postmenopausal 2 years

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7
Q

Tamoxifen toxicities

A

Hot flashes, nausea, vomiting, myelosuppression, pulmonary embolism

Linked to endometrial cancer and blood clots

Positive estrogenic effects on bone and cholesterol tho!

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8
Q

What is Toremifene?

A

Tamoxifen analog

Increases TNFB to decrease cell proliferation/decrease cell growth

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9
Q

Indication for Toremifene?

A

Estrogen dependent breast cancer

Looking at prostate cancer prophylaxis

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10
Q

Tamoxifen toxicities?

A

Similar response/adverse effects to tamoxifen

Hot flashes, nausea, vomiting, myelosuppression, pulmonary embolism

Linked to endometrial cancer and blood clots

Positive estrogenic effects on bone and cholesterol tho!

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11
Q

What is Raloxifene?

A

Selective estrogen receptor modulator (SERM’s)
Estrogen effect in bone, CV system
Antagonist in Breast, uterine tissue

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12
Q

Indication for Raloxifene

A

Mostly used in osteoporosis
FDA approved to reduce breast cancer risk in postmenopausal women with osteoporosis and postmenopausal at high risk for breast cancer

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13
Q

Raloxifene toxicities?

A

Increased incidence of thromboembolism, hot flashes, muscle cramps, teratogenic in animals

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14
Q

What is Fulvestrant?

A

Selective estrogen receptor down regulator (SERD’s)

Pure anti-estrogen, down regulates estrogen receptor

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15
Q

How is Fulvestrant administered?

A

Monthly IM injection

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16
Q

Fulvestrant indications?

A

Postmenopausal hormone sensitive metastatic breast cancer

17
Q

Toxicities associated with Fulvestrant?

A
Nausea
Asthenia
Pain
Vasodilation
Headache
18
Q

What is Anastrazole, Letrozole?

A

Nonsteroidal competitive aromatase inhibitors (decrease 98.1% of estrogen)

19
Q

How are anastrazole, letrozole administered?

A

Oral

20
Q

Indications for anastrazole, letrozole?

A

All women with postmenopausal estrogen sensitive breast cancer should receive aromatase inhibitors

21
Q

Anastrazole, letrozole toxicities?

A

Nausea, hot flashes, hair thinning, muscle pain, less CV events than tamoxifen

22
Q

What is Exemestane?

A

Irreversible steroidal aromatase suicide inhibitor (reduces estrogen by 98%)

23
Q

Indications for Exemestane?

A

Used in postmenopausal ER + breast cancer in women after 2-3 years of Tamoxifen, or for 5 years by itself

24
Q

Toxicities with Exemestane?

A
Nausea
Hot flashes
Edema
Fatigue
Less frequent gynecological symptoms
More common visual disturbances and bone fractures
25
Q

What are flutamide, nilutamide, and bicalutamide?

A

Synthetic nonsteiroidal anti androgens

26
Q

Indications for flutamide, nilutamide, and bicalutamide

A

Prostate cancer

27
Q

MOA for flutamide, nilutamide, and bicalutamide?

A

Bind androgen receptor to block testosterone stimulation of cancer cells, usually given with Leuprolide or goserelin

28
Q

Toxicities with flutamide, nilutamide, and bicalutamide?

A

Gynecomastia
GI distress
Decreased libido
Vasomotor flushing

29
Q

What are Leuprolide, Goserelin, Histrelin, Triptorelin?

A

Analogs of GnRH
They occupy LHRH receptor in pituitary continuously, desensitize and inhibit release of FSH and LH
FSH and LH are responsible for testosterone release

30
Q

How are Leuprolide, Goserelin, Histrelin, Triptorelin administered?

A

Daily SubQ or monthly depot

31
Q

Toxicities of Leuprolide, Goserelin, Histrelin, Triptorelin?

A
Impotence
Hot flashes
Gynecomastia
Nausea
Vomiting
32
Q

What is Nafarelin?

A

Nasal spray formulation of the GnRH analogs