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30 Cards in this Set

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