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31 Cards in this Set
- Front
- Back
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what takes testosterone to DHT
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5 - alpha- reductase
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Name the 7 classes of hormonal agents
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Selective estrogen receptor modulators (SERMs)
Aromatase inhibitors Estrogen receptor down-regulators Gonadotropin hormone-releasing agonists Anti-androgen GnRH antagonists Progestins |
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What signals comes from the hypothalamus to signal the anterior pituitary to release LH and FSH
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LH Releasing Hormone
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Testosterone can make (2)
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Androstenedione or 17 B Estradiol
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What hormone allows Estrone to go back and forth to 17 B Estradiol
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Aromatase
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Step 1 estrogen receptor bound what happens in step 2 (2)
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Disassociation of Hsp90 from ER and confirmational change and dimerization of ER
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what are the 4 types of estrogen receptor - DNA interactions
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classic, non-direct DNA binding, Ligand-Independent Genomic Action, Non-Genomic Mechanism
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which estrogen receptor-DNA interaction involves protein kinase cascade leading to phosphorylation of ER at ERE
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Ligand-Independent Genomic Action
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what is the MOA of LH-RH agonist & Aromatase inhibitors
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Block Estrogen/Testoterone formation
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What are the 3 types of Intervention
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Block Estrogen/Testoterone formation, Receptor Antagonism, Feed Back Inhibition
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what is the "trick" of LHRH
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continual stimulation which lead to receptor down reguation
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which LHRH agonist is usually used for both prostate and breast cancer treatment
frequency |
Goserelin (Zoladex)
q28 days |
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Name a steriodal third generation Aromatase Inhibitor
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Exemestane (Aromasin)
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Name 2 non- steriodal third generation Aromatase Inhibitor
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Anastrozole (Arimidex)
Letrozole (Femara) |
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Whats wrong with Cytadren
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leads to adrenal suppression because it blocks aromatase as well as several other steriod forming enzymes
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Aromatase Inhibitors blocks the formation of
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Estrogens so lots of androgens left
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Name a Estrogen Receptor Antagonist
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Fulvestrant Injection (Faslodex)
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Which SERM is used for treatment and prevention of breast cancer
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Tamoxifene (Nolvadex)
Toremifene (Fareston)- rarely used |
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What SERMs are used for breast cancer prevention
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Raloxifene (Evista)
Tamoxifene (Nolvadex) |
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benefit of raloxifene over tamoxifene
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less risk of endometrial cancer
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con of raloxifene as compared to tamoxifene
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not as good as tamoxifene for NON-invasive breast cancer
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what drug needs monitoring when using with Tamoxifene
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warfarin
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taking ______s with Tamoxifene can reduce it's efficacy
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CYP 2D6 INHIBitors
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what is a drug that should be co-administered with Androgen Receptor Antagonist
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LHRH agonist
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Name 3 Androgen Receptor Antagonist
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Biclutamide- qd
Flutamide- q8h Nilutamide- qd and 5xdose after 30days |
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how could giving estrogen to breast cancer patients work?
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high doses alter mitosis and estrogen receptor density in breast cancer
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what effects does giving estrogen in prostate cancer
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Decreased LH, FSH, and testosterone
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what is the major concern with estrogen therapy
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thromboembolism
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MOA of Progestins
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Known to decrease FSH, LH, testosterone, and estrogen. may also change receptor densities & alter hormone production
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Both progestins and estrogens are used in ___
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Metastatic prostate and breast cancer
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name 2 progestin therapies
its place in therapy |
Megesterol Acetate (Megace)
Medroxyprogesterone Acetate (Depo-Provera)- qwk for 6wk then qmo 3rd or 4th line in breast CA or adv. uterine CA |
