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38 Cards in this Set
- Front
- Back
List the 3 physicological effects of estrogens
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1. Female maturation
2. Developemnt of secondary sex charcteristics 3. Growth and closure of epiphysis |
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What do estrogens do to the endometrium?
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Stimulate development of lining
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List 4 metabolic effects of estrogens
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1. decrease bone resorption
2. alter production/activity of binding proteins 3. alter composition of plasma lipids (positive effects) 4. decrease secretion of bile acids |
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What do estrogens do to blood coagulation?
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Increase factors 2, 7, 9, 10
Decrease antithrombin 3 |
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Can natural estrogens be taken orally?
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No, because of first pass of liver.
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How are estrogens excreted?
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Renal and biliary excretion
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The oral estrogens are what forms?
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Conjugated estrogens
Esterfied estrogens Micronized Estriopipate |
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What is the most common AE of estrogens?
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Nausea
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Replacement therapy of estrogens are used to treat?
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Failure of ovarian development
Menopause |
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What is targeted for estrogen treatment of menopause?
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1. atrophic vaginits (topical)
2. osteoporosis |
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What is an herbal drug used to treat hot flashes?
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Black cohash (don't use in people who have breast cancer)
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Raloxifene blocks is in agonist in:
Antagonist in: |
Agonist in bone
Antagonist in breasts nad endometrium |
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What are some AE of Raloxifene?
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Hot flashes
Leg cramps Venous thrombeombolism |
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What are the two therapeutic uses of Raloxifene?
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Prevent osteoporosis and breast cancer in post-menopausal women
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Name some SERM drungs
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Raloxifene
Tamoxifen |
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Tamoxifen is agonist in:
Antagonist in: |
Agonist in bone, liver, endometrium (not cool)
Antagonist in breasts |
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Tamoxifen must be activate in metabolism by
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CYP2D6
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Name an antiestrogen
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Clomiphene
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How does Clomiphene work?
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Bind to cytoplasmic estrogen receptor which decreases feedback inhibition on GnRH which results in release of LH and FSH
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What are two thing Clomiphene is used for?
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Infertility
Fibrocytic breast cancer |
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Name an E2 receptor antagonist
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Fulvestrant
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What is Fulvestrant used for
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Metastatic breast cancer
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These three drugs block the production of estrogen
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anastrozole
letrozole exemestan |
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What is MOA of anastrozole, letrozole, exemestan?
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Inhibit aromatase enzyme
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What do anastrozole, letrozole, exemestan treat?
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Breast cancer
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There is a higher risk of ___ when on anastrozole, letrozole, and exemestan?
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Osteoporosis
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Danzol MOA
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Suppress LH and FSH thus estrogen production
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Danzol is used to treat
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Endometriosis
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Danzol may increase the risk of
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ovarian cancer
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Which progestin should you know?
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Medroxyprogeterone acetate
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What secrets progestin?
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CL
Placenta |
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What do progestin do to endometrium?
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Develop secretory endometrium
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Excretion of progestins?
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Urine
Feces |
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What are the two activities of medoxyprogesterone acetate?
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+ androgenic
+ antiestrogenic |
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What are some of the therapeutic effects of progestins?
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Dysfuntional uterine bleeding
Dysmenorrhea Endometriosis Endometrial carcinoma |
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What is a progestin antagonist?
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Mifepristone
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What is Mifepristone used for?
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Terminate pregnancies (along with misoprostol)
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What do you need to watch for in Mifepristone?
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Excessive vaginal bleeding
Ectopic pregancny Systemic bacterial infections |