acts on the anterior piruitary gland to inhibit the release of FSH
activin moa
acts to stimulate the release of FSH
where is aromatase synthesized
ovary and placenta
after menopause where does the majority of circulating estrogen come from
adipose tissue
a little comes from adrenal cortex
common precursor to testosterone & estrogen synthesis
antiproliferative effect on female endometrium
promotes endometrial lining to secrete
required for maintenance of pregnancy
progestins
general mechanisme of hormones
in the plasma progestins, androgens and estrogens bind to sex hormone binding globulin (SHBG) and albumin
the unbound fraction diffuses into cells and bind to the nuclear hormone receptor subfamily
3 main AE of estrogens
endometrial hyperplasia & carcinom
breast cancer
N/V
2 indications of estorgen postmenopausal therapy
hot flushes
sleep disturbances
what do you need to watch out for with vaginal estrogens
100% absorbed because they bypass first pass effect. watch for overdosing
major progestin in humans and purpose
progesterone - acts prior to gestation to prepare the uterus for implantatoin of a fertilized ovum
T 1/2
therapeutic uses of progestins
postmenopausal hormone therapy to counteract the AE's of estrogen
dysmenorrhea
endometriosis
SERM
used to treat estrogen (+) breast cancer
AE - hot flushes, endometrial cancer
tamoxifen - nolvadex
SERM
does not activate estrogen receptor in the endometrium
ind - approved for osteoporosis
raloxifene - evista
anti-estrogen
luteolytic property
ind - abortificant
emergency post-coital contraceptive
single dose 600mg
miefpristone - RU486
aromatase inhibitors 4
ind - breast cancer
precocious pregnancy
anastrozole
letrozole
fadrozole
exemestane
aromatase inhibitor
ind-treat breast cancer in tamoxifen resistant individuals
moa - pure estrogen receptor antagonist
fulvestrant - faslodex
ovulation inducer
moa - partial agonist at estrogen receptors
AE - hot flushes, multiple pregnancy
CI - enlarged ovaries
clomiphene - clomid
estrogen & progesterone
ind - treats endometriosis, fibrocystic disease of the breast
moa - suppress pituitary ovarian axis
AE - weight gain, edema, decreased breast size, acne, hot flushes, changes in libido
caution in hepatic disease
danazol
3 layers of the prostate and makeup
glands or epithelial tissue
androgen dependent - 25% of BPH
smooth muscle tissue - 75% of prostate
a1-adrenergic receptors
capsule shell
a1-adrenergic receptors
5a-reductase ihibitor
moderately effective in reducing BPH <50g
peak onset in 6 mo
pregnancy catergory X
AE - sexual dysfunction
finasteride - propecia
5a-reductase inhibitor
inhibits both type I & II
faster and more complete decrease in DHT
dutasteride - avodart
antiandrogen
receptor inhibitor
used to treat prostatic carcinoma
flutamide
antiandrogen
receptor inhibitor
used to treat hirsutism
cyproterone
spironolactone - aldactone
antiandrogen
receptor inhibitor
ind - prostate cancer