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Unit 1: Pharm > Hormone Agonists and Antagonists > Flashcards

Hormone Agonists and Antagonists Flashcards

Technically, not all the drugs in this group are properly antagonists - some are agonists that compete with hormones for a receptor, while the true antagonists interact with the ligand to prevent receptor binding, and still others have both agonist and antagonist actions. To make the cards flow better, I refer to all drugs in this category simply as "hormone antagonists." Please don't hate me!

1
Q

Hormone antagonists are currently used to treat what 3 types of cancers?

A

Lymphomas/leukemias, breast cancer, and prostate cancer

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2
Q

What group of hormone antagonist drugs is used to treat lymphomas and leukemias?

A

Glucocorticoids

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3
Q

List 3 different types of hormone antagonists that are used to treat breast cancer.

A

SERMs (Selective Estrogen-Receptor Modulators), SERDs (SER Downregulators), and aromatase inhibitors

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4
Q

Complete androgen ablation therapy requires 2 different kinds of hormone antagonists. What are these 2 categories?

A

GnRH analogs and nonsteroidal androgen-receptor blockers

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5
Q

Name the 2 glucocorticoid hormone antagonists.

A

Prednisone and dexamethasone

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6
Q

Which hormone antagonist is a SERM (selective estrogen-receptor modulator)?

A

Tamoxifen

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7
Q

Which hormone antagonist is a SERD (selective estrogen-receptor downregulator)?

A

Fulvestrant

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8
Q

What are the 4 aromatase inhibitors?

A

Aminoglutethamide, anastrozole, letrozole, and exemestane

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9
Q

What are the 2 GnRH analogs?

A

Leuprolide and goserelin

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10
Q

Name the 2 nonsteroidal androgen-receptor blockers.

A

Flutamide and bicalutamide

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11
Q

By what mechanism do the glucocorticoids inhibit cancer?

A

They inhibit lymphocyte mitosis

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12
Q

Which hormone antagonist is used to treat ALL, as well as Hodgkins, non-Hodgkins, multiple myeloma, and CLL.

A

Prednisone

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13
Q

How is dexamathasone typically used?

A

In conjunction with radiation therapy, to reduce edema in brain and spinal cord tumors

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14
Q

As a group, the hormone antagonists are notable for not inducing what common chemotherapy side-effect?

A

They do not cause myelosuppression

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15
Q

Which hormone antagonist, which can be administered orally, is the most widely used anti-estrogen therapy?

A

Tamoxifen

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16
Q

Tamoxifen therapy is unfortunately accompanied by hot flushes, alopecia, and increased risk of what 2 events?

A

Increased risks of endometrial cancer and of thromboembolism

17
Q

How do tamoxifen and fulvestrant compare in terms of their mechanistic effect on ERs (estrogen/estradiol receptor)?

A

Fulvestrant binds ER with ~100x greater affinity than tamoxifen does, and reduces overall ER levels while tamoxifen stabilizes or even increases ER expression.

18
Q

List 3 circumstances in which tamoxifen might be used.

A

For metastatic ER-positive breast cancer, as adjuvant therapy following breast tumor excision, or for prevention in high-risk (strong family history) patients

19
Q

Even though we refer to the “hormone antagonists” as a class of cancer drugs, only 1 breast cancer drug is a true “anti-estrogen” antagonist that blocks estrogen from its receptor without displaying any agonist activity. Which drug is this?

A

Fulvestrant

20
Q

Which aromatase inhibitor is a first-line therapy for treating ER(+) breast cancer in postmenopausal women?

A

Anastrozole

21
Q

What is an obvious, must-not-miss feature that should be found for a cancer before it is treated with estrogen or androgen inhibiting drugs?

A

The cancer must be ER(+) or AR(+)

22
Q

Which first generation estrogen inhibitor has fallen out of favor because it is relatively weak and has significant toxicity?

A

Aminoglutethamide

23
Q

Which aromatase inhibitor is a steroidal inhibitor, meaning that it binds covalently and irreversibly?

A

Exemestane

24
Q

Which estrogen inhibitors are used only on postmenopausal women?

A

Fulvestrant, anastrozole, letrozole, and exemestane

25
Q

What receptor do leuprolide and goserelin bind to, and what hormones are not released as a result?

A

Binds GnRH receptor, inhibiting FSH and LH release

26
Q

What 2 hormone antagonists work by competing with androgen for AR binding?

A

Flutamide and bicalutamide

Unit 1: Pharm (10 decks)

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