endocrine Flashcards
Estradiols
estradiol cypionate
Premarin
ethinyl estradiol
biological affection of estradiols
female tract development
secondary sexual characteristic
reduce secretion of gonadotropin from pituitary
increase triglyceride, reduce LDL, increase HDL
increase coagulation of blood protein
diethylstilbestrol
we do not use it anymore
it was use unsuccessfully to prevent miscarriage
it causes severe toxicity
ectopic pregnancy
infertility
vaginal adenocarcinoma
DES daughter
have increase risk of develop breast cancer and cervical caner
DES son
have increase risk of develop cryptorchidism
hypospadias
transgenderism, gender dysphoria
emergency contraception / post coital contraceptive
( morning after pill )
prevent pregnancy if given within 72 hours
can be combination of estrogen and progestin
or progestin only
progesterone only product have fewer side effects
action - inhibit ovulation before LH surge
decrease receptivity in uterine tube endometrium
altered cervical mucous gland function
monophasic or
mulitphasic with placebo week ( sugar pill to get period )
oral estrogen
Non-contraceptive use
Tx for hypogonadism in sound females
Hormone replacement therapy in females with premature ovarian failure or surgical removal
Hormone replacement therapy in postmenopausal females
side effect of oral contraceptive agent / oral estrogen
increase risk of endometrial cancer ( prevented by combining with progestin )
increase risk in breast cancer (postmenopausal women)
increase in CV risk in postmenopausal women
toxicity / overdose effect of oral contraceptive agent / oral estrogen
nausea
great tenderness
migraine
thromboembolic disease
gallbladder disease
Hypertriglyceridemia
hypertension
progestins
progesterone is the major progestin in human
induces secretion of endometrium, healthy endometrium for pregnancy
medroxyprogesterone
prototypical oral synthetic progestin
synthetic progestin doesn’t support pregnancy
inhibit ovulation
in HRT use as adjunct to reduce the risk of endometrium cancer
side effect of progestin
affect carb metabolism
stimulate fat deposits
dec HDL
reduce boen density ( long term)
delayed ovulation after cessation
suppress GnRH and LH, FSH
Selective Estrogen Receptor Modulator ( SERMs)
Tamoxifen, Toremifene
Estrogen receptor antagonist in breast tissue - reduce risk of breast cancer
estrogen receptor agonist in endometrial tissue - promote endometrial hyperplasia
increase risk of endometrial cancer
side effect of SERMs
as antagonist - hot flash
as agonist - increase risk of venous thromboembolism
- increase risk of endometrial cancer
Selective Estrogen Receptor Modulator ( SERMs)
Raloxifene
approved of prevention and treatment of osteoporosis
antagonist effect - reduce breast cancer risk
agonist effect - no estrogenic effect on endometrial tissue ( unlike tamoxifen)
Selective Estrogen Receptor Modulator ( SERMs)
Bazedoxifene
use for menopause symptoms and osteoporosis prevention
Selective Estrogen Receptor Modulator ( SERMs)
Clomiphene
reduces negative feedback in pituitary increase LH and FSH
induce ovulation in anovulatory women
Pure estrogen receptor antagonist
Fulvestrant
use in breast cancer with resistance to tamoxifen
use in women with breast cancer with endometrial risk factor
non-steroidal competitive aromatase inhibitor ( synthesis inhibitors )
anastrozole, letrozole
irreversible aromatase inhibitor
Exemestane