Hormones Pharm part I, Linger Flashcards
What are the estrogens we have for drugs
conjugated E- premarin
estradiol valerate
ethinyl estradiol
mestranol
what are the progestin drgus
desogestrel(inactive etonogestrel(active)
drospinenone
medroxyprogresterone, norethindrone, norgestimate
norgestrel (L-norgestrel, levonorgestrel)
what are the E and P inhibitors
Mifepristone
what are the selective E R modulators
raloxifene
tamoxifen
toremifene
what are the selective E R downregulators
clomiphene
fulvestrant
what are the aromatase inhibitors
anastrazole
exemestane
letrozole
how do synthetic E work
bind to the SHBG and lower affinity to albumin so there is more unfound E around
why are vaginal and transdermal modes for effective for giving E
because avoid the first pass metabolism of the liver
MOA E
binds ER and activates gene transcription
how do E Receptros work
homodimerize and bind promoter regions or bind to other transcription factors which bind to the promoter regions
endometrial effects of E
bleeding and shedding
continuous exposure will lead to hyperplasia of the endometrium leading to abnormal bleeding patterns
metabolic effects of E
decrease rate of bone resoprtion because promotes apoptosis of osteoclasts
stimulate adipose tissude production of letpin
stimulates increase production of the cortisol globulin, thyroxine binding globulin, sex hormone binding protein
increase HDL and TG, reduce LDL
vascular effects of E
enhance coagulability of blood
increases factors II CII IX and X, decrease antithrombin III
icnrease plasminogen
When do we use E for Tx
primary hypogonadism
postmenopausal hormone replacement
suppress ovulation in patients with intractable dysmenorrhea or suppress ovarian function in cases of hirsutism and excessive ovary androgen secretion
E and P replacement decreases risk of what
osteoporotic fractures of hip vertebrae, and wrist
adverse effects estrogens
uterine bleeding, breast and endometrial cancer
nausea, breast tenderness, hyperpigmentation, increased migraine frequency, cholestasis, gallbladder disease and HTN
how is endometrial hyperplasia from administration of E prevented
give progestin too
does adding P to E Tx prevent breast cancer
not, may actually increase risk of breast cancer
Contraindications to E
patients with E dependent neoplasms (endometrial carcinoma and breast cancer)
patients with unDx genital bleeding, liver disease, history of thromboembolic disorder and heavy smokers