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Part 5: Hormones and Antagonists
Dr. Abramson Handout
32
Pharmacology
Graduate
01/06/2011

Additional Pharmacology Flashcards

 


 

Cards

Term
Estrogens are synthesized in the body from androgens (principally androstenedione) via the action of a cytochrome  P450 complex known as...
Definition
aromatase
Term
In PREmenopausal women, the main site of aromatization and estrogen synthesis is in the ______.
Definition
ovary
Term
In POSTmenopausal women, estrogens are synthesized from androstenedione in the ______ ______, and undergoes aromatization mainly in the _____ _____.
Definition

adrenal gland

adipose tissue

Term
Two aromatase inhibitors that are structurally based on the steroid nucleus are ______ and ______.
Definition

exemestane (Aromasin) and

testolactone (Teslac)

Term
Exemestane and testolactone are used in the treatment in _______ _______ ________ in ____menopausal women.
Definition

disseminated breat cancer

POST

Term
Does exemestane react reversibly or irreversibly with aromatase?
Definition
irreversibly
Term
Two aromatase inhibitors that are non-steroidal in structure are ______ and ______.
Definition

letrozole (Femara) and

anastrozole (Arimidex)

Term
Letrozole and anastrozole are used in the treatment of _______ and ______ ______ breast cancer in ___menopausal women.
Definition

advanced and early stage

POST

Term
This drug blocks the first step in the synthesis of adrenocorticoid steroids, the conversion from cholesterol to pregnenolone.
Definition
aminoglutethimide (Cytadren)
Term
Name the three antiandrogen drugs.
Definition
flutamide (Eulexin), nilutamide (Nilandron) and bicalutamide (Casodex)
Term
Antoandrogens are used in the treatment of what type of cancer?
Definition
Metastatic prostate cancer
Term
What is the MOA of antiandrogen drugs?
Definition
they inhibit translocation of the androgen receptor from the cytoplasm to the nucleus of target cells
Term
Name the 2 progestin drugs available.
Definition
megestrol acetate (Megace) and medroxyprogesterone acetate (Depo-Provera)
Term
What types of cancer are progestins used for treatment?
Definition
metastatic hormone-dependent breast cancer and in the management of endometrial carcinoma previously treated by surgery and radiotherapy
Term
List another use for the progestins.
Definition
Appetite stimulant
Term
What does SERM stand for?
Definition
Selective estrogen receptor modulators
Term
What is another name for SERMs?
Definition
EAAs (estrogen agonist/antagoinsts)
Term
These 2 drugs act as estrogen agonists in the bone, brain, and liver and also act as estrogen antagonists in the breast.
Definition

tamoxifen (Nolvaldex) and

toremifene (Fareston)

Term
________ is the endocrine treatment of choice in POSTmenopausal women with ER+ metastatic breast cancer or following primary tumor therapy.
Definition
tamoxifen
Term
______ is a SERM/EAA that is used for its antiresorptive effect on bone.
Definition
raloxifene (Evista)
Term
In 2007, raloxifene was FDA approved to reduce the risk of what type of cancer?
Definition
invasive breast cancer in postmenopausal women
Term
This drug is a pure estrogen antagonist in all tissues.
Definition
fulvestrant (Faslodex)
Term
Fulvextrant is approved for treatment in what type of cancer?
Definition
ER+ metastatic breast cancer in postmenopausal women. It is useful in women who are resistant to tamoxifen treatment.
Term
GnRH releases what hormones from the anterior pituitary? This action, in turn, causes the gonade to synthesize and release androgens, progesterone, and estrogens.
Definition
luteinizing hormone (LH) and follicle stimulating hormone (FSH)
Term
Leuprolide (Lupron) is a GnRH agonist used in the treatment of what type of cancers/conditions?
Definition

advanced prostate cancer

endometriosis

uterine fibroids

central precocious puberty

 

Term
Goserelin (Zoladex) is a GnRH agonist used in the treatment of which type of cancer/conditions?
Definition

advanced prostate cancer

endometriosis

advanced breat cancer

Term
Triptorelin pamoate (Treistar) is a GnRH agonist used in the treatment of which type of cancer?
Definition
advanced prostate cancer
Term
Histrelin (Vantas) is a GnRH agonist used in the treatment of which type of cancer?
Definition
advanced prostate cancer
Term
Upon administration of GnRH agonists, what side effect/adverse reaction occurs?
Definition
immediate and sustained release of LH and FSH, producing a so called "flare effect" that last for about 10 days
Term
Degarelix (Firmagon) is a GnRH antagonist used in the treatment of what type of cancer?
Definition
advanced prostate cancer
Term
This drug class is useful in the treatment of acute leukemia in children and malignant lymphoma in children and adults.
Definition
adrenocortical steroids (glucocorticoids)
Term
This drug is used in the treatment of Cushing's syndrome.
Definition
aminoglutethimide (Cytadren)
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