Term
| Estrogens are synthesized in the body from androgens (principally androstenedione) via the action of a cytochrome P450 complex known as... |
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Definition
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Term
| In PREmenopausal women, the main site of aromatization and estrogen synthesis is in the ______. |
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Definition
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Term
| In POSTmenopausal women, estrogens are synthesized from androstenedione in the ______ ______, and undergoes aromatization mainly in the _____ _____. |
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Definition
adrenal gland
adipose tissue |
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Term
| Two aromatase inhibitors that are structurally based on the steroid nucleus are ______ and ______. |
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Definition
exemestane (Aromasin) and
testolactone (Teslac) |
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Term
| Exemestane and testolactone are used in the treatment in _______ _______ ________ in ____menopausal women. |
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Definition
disseminated breat cancer
POST |
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Term
| Does exemestane react reversibly or irreversibly with aromatase? |
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Definition
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Term
| Two aromatase inhibitors that are non-steroidal in structure are ______ and ______. |
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Definition
letrozole (Femara) and
anastrozole (Arimidex) |
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Term
| Letrozole and anastrozole are used in the treatment of _______ and ______ ______ breast cancer in ___menopausal women. |
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Definition
advanced and early stage
POST |
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Term
| This drug blocks the first step in the synthesis of adrenocorticoid steroids, the conversion from cholesterol to pregnenolone. |
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Definition
| aminoglutethimide (Cytadren) |
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Term
| Name the three antiandrogen drugs. |
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Definition
| flutamide (Eulexin), nilutamide (Nilandron) and bicalutamide (Casodex) |
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Term
| Antoandrogens are used in the treatment of what type of cancer? |
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Definition
| Metastatic prostate cancer |
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Term
| What is the MOA of antiandrogen drugs? |
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Definition
| they inhibit translocation of the androgen receptor from the cytoplasm to the nucleus of target cells |
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Term
| Name the 2 progestin drugs available. |
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Definition
| megestrol acetate (Megace) and medroxyprogesterone acetate (Depo-Provera) |
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Term
| What types of cancer are progestins used for treatment? |
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Definition
| metastatic hormone-dependent breast cancer and in the management of endometrial carcinoma previously treated by surgery and radiotherapy |
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Term
| List another use for the progestins. |
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Definition
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Term
| What does SERM stand for? |
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Definition
| Selective estrogen receptor modulators |
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Term
| What is another name for SERMs? |
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Definition
| EAAs (estrogen agonist/antagoinsts) |
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Term
| These 2 drugs act as estrogen agonists in the bone, brain, and liver and also act as estrogen antagonists in the breast. |
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Definition
tamoxifen (Nolvaldex) and
toremifene (Fareston) |
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Term
| ________ is the endocrine treatment of choice in POSTmenopausal women with ER+ metastatic breast cancer or following primary tumor therapy. |
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Definition
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Term
| ______ is a SERM/EAA that is used for its antiresorptive effect on bone. |
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Definition
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Term
| In 2007, raloxifene was FDA approved to reduce the risk of what type of cancer? |
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Definition
| invasive breast cancer in postmenopausal women |
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Term
| This drug is a pure estrogen antagonist in all tissues. |
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Definition
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Term
| Fulvextrant is approved for treatment in what type of cancer? |
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Definition
| ER+ metastatic breast cancer in postmenopausal women. It is useful in women who are resistant to tamoxifen treatment. |
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Term
| GnRH releases what hormones from the anterior pituitary? This action, in turn, causes the gonade to synthesize and release androgens, progesterone, and estrogens. |
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Definition
| luteinizing hormone (LH) and follicle stimulating hormone (FSH) |
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Term
| Leuprolide (Lupron) is a GnRH agonist used in the treatment of what type of cancers/conditions? |
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Definition
advanced prostate cancer
endometriosis
uterine fibroids
central precocious puberty
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Term
| Goserelin (Zoladex) is a GnRH agonist used in the treatment of which type of cancer/conditions? |
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Definition
advanced prostate cancer
endometriosis
advanced breat cancer |
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Term
| Triptorelin pamoate (Treistar) is a GnRH agonist used in the treatment of which type of cancer? |
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Definition
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Term
| Histrelin (Vantas) is a GnRH agonist used in the treatment of which type of cancer? |
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Definition
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Term
| Upon administration of GnRH agonists, what side effect/adverse reaction occurs? |
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Definition
| immediate and sustained release of LH and FSH, producing a so called "flare effect" that last for about 10 days |
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Term
| Degarelix (Firmagon) is a GnRH antagonist used in the treatment of what type of cancer? |
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Definition
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Term
| This drug class is useful in the treatment of acute leukemia in children and malignant lymphoma in children and adults. |
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Definition
| adrenocortical steroids (glucocorticoids) |
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Term
| This drug is used in the treatment of Cushing's syndrome. |
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Definition
| aminoglutethimide (Cytadren) |
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