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30 Cards in this Set
- Front
- Back
Estrogens MOA
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binds to estrogen response slements on various genes and regulates their transcription resulting in protein synthesis affects vary by cell type and location
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Physiological effects of estrogens
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femal maturation, development of vagina, uterus, fallopian tubes, secondary sex traits, and development of endometrial lining
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Metabolic effects of estrogens
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decreases bone resorption, increases HDL and decreases LDL and total cholesterol, decreases bile acids, and alters production and activity of binding proteins
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Side effects of estrogens
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increases factors 2,7,9, and 10 and decreases antithrombin III, edma, induce synthesis of progesteron receptors, and behavorial effects
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Why can't you take 17-estradiol beta orally?
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Nature estrogens and their esters are not effectives orally due to sinificant first pass hepatic metabolism and are excreted renally and biliary
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Conjugated Equine Estrogens how are they administered and what do they treat?
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oral, menopause
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How is estradiol (17) given?
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transdermally, menopause
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How are the esters given (-ate)
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injection, menopause
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Side effects of etrogens as a drug
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nausea, vomiting, anorexia, weight gain, chloasma, hypertension, decreased glucose tolerance, thromboembolism, cancer growth (breast, uterine but does not cause them), migraine headache (increased risk of stroke), GERD
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Uses for estrogen drugs
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failure of ovarian development, menopause (HRT)--in combo with progestin if still have uterus, osteoporosis but bisphosphonates are preferred, dysmenorrhea, oral contraception
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Raloxifene MOA
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estrogen agonist in bone, antagonist in breast and endometrium
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Raloxifene uses
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osteoporosis, reduce breast cancer risk
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Raloxifene side effects
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hot flashes, leg cramps, increased incidence of venous thrombeombolism
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Tamoxifen MOA
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Pro durg, blocks estrogen in breast tissue, agonist in bone, liver, and endometrium (may increase uterine cancer but benefit outweighs risk)
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Tamoxifen use
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inhibition of growth of estrogen dependent breast tumors. Can get resistance only use for 5 yrs
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Clomiphene
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strogen receptor antagonist
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Clomiphene MOA
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decreases signal of estrogen to the hypothalamus so there is increase in the release of GnRH and which leads to increase in LH and FSH
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Clomiphene uses
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infertility, fibrocystic breast disease
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Fulvestrant
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E2 receptor antagonist used to treat metastatic breast cancer
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Anastrozole, Letrozole, Exemestan
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block the actions or production of estrogen
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Anastrozole, Letrozole, Exemestan MOA
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decrease estrogen synthesis by inhibiting aromaste enzyme
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Anastrozole, Letrozole, Exemestan uses
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breast cancer, decrease risk of endometrium cancer, increases risk of osteoporosis
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Danazol MOA
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suppresses LH and FSH which decreases estrogen and progesterone
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Danazol uses
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endometriosis
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Medroxyprogesterone acetate administration
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IM, PO
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Medroxyprogesterone acetate uses
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dysfunctional uterine bleeding, dysmenorrhea (in combo with estrogen), edometriosis, edometrial carcinoma, oral contraception
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Medroxyprogesterone acetate
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Progestin
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Medroxyprogesterone acetate adverse effects
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weight gain, camps, acne, pigmentation changes, drowsiness, and depression
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Mifepristone
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progesterone antagonist
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Mifepristone uses
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used to terminate early pregnancy
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