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48 Cards in this Set

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Where is estrogen produce in men and post-menopausal women?
Adipose Tissue
Where in the ovary is estradiol produces
In granulosa cells from androgen secreted by thecal cells
Major ciculating homrmon in postmenopausal women and men is
Estrone

Estradiol in premenopausal
Difference between estrogen binding to sex steroid binding globulin and albumin
SSBG is high affinity, low capacity

Albumin is low affinity, high capacity
Estrogen effect on progestin receptors
Estrogen stimulates progesterone receptors in endometerial tissue, so progesterone can counter act effects of estrogen
Difference between natural, synthetic and conjugated estrogens
Conjugate can be taken orally, the rest are transdurmal or IV, IM
Use of Estrogens
Birth control
Replacement therapy
Hypogonadotropic females
Uterine bleeding

Also for prostatic carcioma (inhibit GnRH)
Estrogen and Progestin in replacement therapy. When do you use one or both?
If uterus is present, need progestin to prevent edometerial hyperplasia and cancer.

No uterus, estrogen alone is ok
Negative Side Effects of Estrogen therapy
26% increase in breat cancer (>5 yrs)
Increase risk of cardiovascular disease
Increase in stroke, clots
Increase cholesterol and gall bladder disease
Postive side effects of Estrogen therapy
Few hip fractures
Decrease colorectal cancer (37%)
Contraindications to estrogen therapy
Breast or endometerial cancer
Endometriosis
Vaginal Bleeding
Pregnany
DVTs
Hypertension
Liver disease
Estrogen and hot flashes
Good more moderate to sever hot flashes

Use behavior modification for mild hot flashes
Two antiestrogen drugs
Clomiphene Citrate
Tamoxifen
Clomiphene Citrate
Inhibits estrogen receptor feedback at pituitary

Increase amplitude of LH and FSH to treat fertility
Estrogen receptor blocker for infertility
Clomiphene Citrate
Tamoxifen
Blocks estrogen receptors in breast cancer cells

Acts as agonist for bone density and lipoprotein profiles
Side effects of Tamoxifen
Like menopause

May increase risk of endometrial cancer
Aromatase inhibitor
Anastrozole
Letrozole
Exemestane

Blocker conversion of cholesterol to estrogen in adipose tissue
2nd line drug for breast cancer
Anastrozole
Letrozole
Exemstane

Not as effective has Tamoxifen
Aromataze inhibitors in pre vs post menopausal women
Work only on adipose, so more effective in post menopausal women
Raloxifene
Full estrogen antagonist on breast and uterus

Agonist at all other sites.
Full anatagonist of estrogen in the breast and uterus, but acts as an agonist elsewhere
Raloxifene
Three places where progesterone is produced
Corpus Luteum
Fetal Placenta
Adrenals
CNS effects of progesterone
respiratory stimulant
Thermogenenisis
High doses, anesthertic properties
Medroxyprogesterone acetate
Progesterone commonly used in hormone replacement regimen
Norethindrone
Norgestrel
Nogestimate
Desogestrel
Progesterones used in OCP
Use of progesterone
Birth Control
Replacement therapy
Suprresion of Estrogen (bleeding, endometriosis, estrogen dependent cancers)
Diagnositic Tests
Side Effects of Progesterone
Weight gain
Hirsutism
Libidi change
Bad for cholesterol
Contraindications for progesterone replacment therapy
Hepatic Disease
Suspected pregnancy
Undiagnosed vaginal bleeding
Antiprogesterone drug and its use
Mifepristone for abortions
Trade off with OCP
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
Plan B
High dose estrogen plus levonorgestrel for morning after contraception

Causes N/V
Levonorgestrel
Progestin in Plan B morning after pill
Absolute CI's to OCP
Clotting disorder
MI
Hyperlipidemia
Carcinom of breat or Uterus
Vaginal Bleeding
Pregnancy
History of Liver tumors
What is testosterone bound to in seminiferous tubules
Androgen binding globulin
Where testosterone is efficiently converted to 5-HT
Prostate, scrotal skin, hair follicles and brain
Danazol
Testosterone Alkyl for Angioneurotic Edema

Increase inhbitor of edema and restors complement factors

Also for Endometriosis
Testosterone for angioneuortic edema
Danazol
Use for androgen replacement therapy
Induce puberty in hypogonadotrophic hypogonadism
Treat short stature (though may cause epiphyseal plate to fuse earlier)
Most common testosterone ester
Testosterone enanthate
Side effects of testosterone
Virilizing effects (women and children)
Feminizing effects in men (more converted to estrogen)
Liver disease and edema
Flutamide
Testosterone receptor blocker

used for prostate cacner, but needs to be given with GnRH analog to prevent secondary increase in testosterone (blocks feedback inhibition)
Cyporterone acetate
Oraly active test receptor antagonist

Not in US, but used for precocious puberty, baldness, and inhibition of libido in dangerous men
Testosterone blocker for prostate cancer. Give with GnRH analog
Flutamide
Inhibitors of androgen synthesis
Ketoconazole
Spironolactone

Inhibit P450, which lowers testosterone, but compensation and short action limit their effectiveness
5 alpha reductase inhibitor
Finasteride

For BPH, and baldness (Propecia)
Propecia
Finasteride

5alpha reductase inhibitor
Finasteride
5 alpha reducatse inhibitor for BPH and baldness