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48 Cards in this Set
- Front
- Back
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Where is estrogen produce in men and post-menopausal women?
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Adipose Tissue
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Where in the ovary is estradiol produces
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In granulosa cells from androgen secreted by thecal cells
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Major ciculating homrmon in postmenopausal women and men is
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Estrone
Estradiol in premenopausal |
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Difference between estrogen binding to sex steroid binding globulin and albumin
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SSBG is high affinity, low capacity
Albumin is low affinity, high capacity |
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Estrogen effect on progestin receptors
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Estrogen stimulates progesterone receptors in endometerial tissue, so progesterone can counter act effects of estrogen
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Difference between natural, synthetic and conjugated estrogens
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Conjugate can be taken orally, the rest are transdurmal or IV, IM
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Use of Estrogens
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Birth control
Replacement therapy Hypogonadotropic females Uterine bleeding Also for prostatic carcioma (inhibit GnRH) |
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Estrogen and Progestin in replacement therapy. When do you use one or both?
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If uterus is present, need progestin to prevent edometerial hyperplasia and cancer.
No uterus, estrogen alone is ok |
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Negative Side Effects of Estrogen therapy
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26% increase in breat cancer (>5 yrs)
Increase risk of cardiovascular disease Increase in stroke, clots Increase cholesterol and gall bladder disease |
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Postive side effects of Estrogen therapy
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Few hip fractures
Decrease colorectal cancer (37%) |
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Contraindications to estrogen therapy
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Breast or endometerial cancer
Endometriosis Vaginal Bleeding Pregnany DVTs Hypertension Liver disease |
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Estrogen and hot flashes
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Good more moderate to sever hot flashes
Use behavior modification for mild hot flashes |
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Two antiestrogen drugs
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Clomiphene Citrate
Tamoxifen |
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Clomiphene Citrate
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Inhibits estrogen receptor feedback at pituitary
Increase amplitude of LH and FSH to treat fertility |
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Estrogen receptor blocker for infertility
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Clomiphene Citrate
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Tamoxifen
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Blocks estrogen receptors in breast cancer cells
Acts as agonist for bone density and lipoprotein profiles |
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Side effects of Tamoxifen
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Like menopause
May increase risk of endometrial cancer |
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Aromatase inhibitor
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Anastrozole
Letrozole Exemestane Blocker conversion of cholesterol to estrogen in adipose tissue |
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2nd line drug for breast cancer
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Anastrozole
Letrozole Exemstane Not as effective has Tamoxifen |
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Aromataze inhibitors in pre vs post menopausal women
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Work only on adipose, so more effective in post menopausal women
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Raloxifene
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Full estrogen antagonist on breast and uterus
Agonist at all other sites. |
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Full anatagonist of estrogen in the breast and uterus, but acts as an agonist elsewhere
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Raloxifene
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Three places where progesterone is produced
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Corpus Luteum
Fetal Placenta Adrenals |
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CNS effects of progesterone
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respiratory stimulant
Thermogenenisis High doses, anesthertic properties |
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Medroxyprogesterone acetate
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Progesterone commonly used in hormone replacement regimen
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Norethindrone
Norgestrel Nogestimate Desogestrel |
Progesterones used in OCP
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Use of progesterone
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Birth Control
Replacement therapy Suprresion of Estrogen (bleeding, endometriosis, estrogen dependent cancers) Diagnositic Tests |
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Side Effects of Progesterone
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Weight gain
Hirsutism Libidi change Bad for cholesterol |
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Contraindications for progesterone replacment therapy
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Hepatic Disease
Suspected pregnancy Undiagnosed vaginal bleeding |
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Antiprogesterone drug and its use
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Mifepristone for abortions
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Trade off with OCP
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No increase in heart disease, stroke
Some increase in DVTS and HTN Increase in Hepatic and Gall Bladder disease Decrease in endometerial cancer, ovarian cancer |
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Plan B
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High dose estrogen plus levonorgestrel for morning after contraception
Causes N/V |
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Levonorgestrel
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Progestin in Plan B morning after pill
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Absolute CI's to OCP
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Clotting disorder
MI Hyperlipidemia Carcinom of breat or Uterus Vaginal Bleeding Pregnancy History of Liver tumors |
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What is testosterone bound to in seminiferous tubules
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Androgen binding globulin
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Where testosterone is efficiently converted to 5-HT
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Prostate, scrotal skin, hair follicles and brain
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Danazol
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Testosterone Alkyl for Angioneurotic Edema
Increase inhbitor of edema and restors complement factors Also for Endometriosis |
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Testosterone for angioneuortic edema
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Danazol
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Use for androgen replacement therapy
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Induce puberty in hypogonadotrophic hypogonadism
Treat short stature (though may cause epiphyseal plate to fuse earlier) |
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Most common testosterone ester
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Testosterone enanthate
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Side effects of testosterone
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Virilizing effects (women and children)
Feminizing effects in men (more converted to estrogen) Liver disease and edema |
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Flutamide
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Testosterone receptor blocker
used for prostate cacner, but needs to be given with GnRH analog to prevent secondary increase in testosterone (blocks feedback inhibition) |
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Cyporterone acetate
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Oraly active test receptor antagonist
Not in US, but used for precocious puberty, baldness, and inhibition of libido in dangerous men |
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Testosterone blocker for prostate cancer. Give with GnRH analog
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Flutamide
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Inhibitors of androgen synthesis
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Ketoconazole
Spironolactone Inhibit P450, which lowers testosterone, but compensation and short action limit their effectiveness |
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5 alpha reductase inhibitor
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Finasteride
For BPH, and baldness (Propecia) |
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Propecia
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Finasteride
5alpha reductase inhibitor |
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Finasteride
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5 alpha reducatse inhibitor for BPH and baldness
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