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5 Hormones and Antagonists
Abramson Hanley
25
Pharmacology
Professional
01/08/2011

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Cards

Term
Types of hormone treatments
Definition
Aromatase inhibitors
Antiandrogens
Progestins
SERMs and estrogen antagonists
GnRH agonists and antagonists
Adrenocortical hormones
Term
Aromatase
Definition
Enzyme used to synthesize estrogen from androgen
Term
Major site of estrogen synthesis in premenopausal women
Definition
Ovary
Term
Estrogen synthesis is postmenopausal women
Definition
Estrogens are synthesized from androstenedione in the adrenal gland and undergoes aromatization mainly in adipose tissue
Term
Exemestane (Aromasin)
Definition
Aromatase inhibitor used for the treatment of disseminated breast cancer in postmenopaulsal women

Reacts irreversibly with aromatase
Term
Testolactone (Teslac)
Definition
Aromatase inhibitor devoid of androgenic activity that is used to treat disseminated breast cancer in postmenopausal women
Term
2 types of aromatase inhibitors
Definition
1) Based on steroidal nucleus
2) Non-steroidal inhibitors
Term
Letrozole (Femara)
Definition
Nonsteroidal aromatase inhibitors containing a triazole ring

Treats advanced breast cancer in postmenopausal women (not pre)
Term
Anasozole (Arimidex)
Definition
Nonsteroidal aromatase inhibitor for advanced and early stage breast cancer in posmenopausal women
Term
Aminoglutethimide (Cytadren)
Definition
Aromatase inhibitor used to treat advanced breast cancer (not as selective as others)

Also involves first step in the synthesis of adrenocortical steroid - the conversion of cholesterol to pregnenolone which is used to treat Cushing's Syndrome

Treats Cushing's syndrome
Term
3 Antiandrogens
Definition
1) Flutamide
2) Nilutamide
3) Bicalutamide

They all inhibit translocation of the androgen receptor from the cytoplasm to the nucleus of target cells
Term
Flutamide (Eulexin)
Nilutamide (Nilandron)
Bicalutamide (Casodex)
Definition
Antiandrogen (anilid derivative) used in conjunction with GnRH analog for metastatic prostate cancer
Term
2 Progestational agents
Definition
1) Megestrol acetate (Megace)
2) Medroxyprogesterone acetate (Depo-Provera)
Term
Megestrol acetate (Megace)
Medroxyprogsterone acetate (Depo-Provera)
Definition
Progestins used as second-line hormonal therapy for metastatic hormone-depdent breast cancer and management of endometrial carcinoma previously treated by surgery and radiotherapy
Term
SERMs
Definition
Selective estrogeneceptor modulators aka estrogen agonist/antagonists
Term
Tamoxifen (Nolvadex)
Definition
SERM that acts as estrogen agonists in bone, brain and liver but estrogen antagonists in the breast

Treatment of choice for postmenopausa women with ER+ metastatic breast cancer or following primary tumor therapy

Also approved for long-term use in women with high risk of developing breast cancer

However, have increased risk of endometrial cancer
Reduce risk of CV disease in postmenopausal women
Term
Toremifene (Fareston)
Definition
SERM used in metastatic breast cancer in postmenopausal women with ER + or ER unknown tumors
Term
Raloxifene (Evista)
Definition
SERM used for its antiresorptive effect on bone

Currently the subject of large study STAR (Study of Tamoxifen and Raloxifene) to prevent breast cancer

Approved to reduce the risk of invasive breast cancer in postmenopausal women
Term
Fulvestrant (Faslodex)
Definition
pure estrogen antagonist
treat ER+ metastatic breast cancer in postmenopausal women who are resistant to tamoxifen
Term
GnRH agonists
Definition
Produces LH and FSH which in turn cause gonads to synthesize and release androgens, progesterone, and estrogen

GnRH agonists will supress hormonal production through negative feedback
Term
Leuprolide acetate (Lupron)
Definition
GnRH agonists used in advanced prostate cancer**
(Also endometriosis, uterine fibroids, central precocious puberty)
Term
Flare effect
Definition
GnRH initial administration causes an immediate and sustained release of LH and FSH

LH and FSH supression and reduction of androgenic and estrogenic effects after 10 days
Term
Abarelix (Plenaxis)
Definition
GnRH antagonist used I.M to treat advanced prostate cancer

No initial flare-up but cause serious allergic reactions (Withdrawal from market in 2006)
Term
Degarelix (Firmagon)
Definition
GnRH antagonist similar to abarelix but does not cause serious allergic reaction for Advanced prostate cancer
Term
Glucocorticoids
Definition
Adrenocortical steroid which suppress mitosis in lymphocytes used to treat acute leukemia in children and malignant lymphoma in children and adults

Prednisone is preferred glucocorticoid
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