Reproductive pharmacology Flashcards
What is the mechanism of action of luprolide
GnRH agonist- binds GnRH membrane receptor on pituitary gonadotrope cells.
Usually given in long acting form that eliminates pulsatility and thus causes decreased gonadotropin production
What are indications for GnRH agonists or antagonists?
- testing for precocious or delayed puberty
- suppressing precocious puberty
- endometriosis
- prostate cancer
- decrease endogenous ovarian function to use exogenous ovulation indcution
What are side effects of GnRH agonists?
signs of hypogondadism- hot flashes, bone loss, low libido, amenorrhea
What is a difference in the response to GnRH agonists vs antagonists?
agonists do cause LH/ FSH flare then inhibition
antagonists cause immediate inhibition with no flare
What would be an indication for pulsatile administration of GnRH?
treatment of hypogonadotropic hypogonadism due to hypothalamic dysfunction, ex Kallman syndrome
Daily injections of exogenous ______ stimulate ovarian follicle development
FSH
Injection of hCG (or LH) triggers ______
LH surge, ovulation, and progesterone production
________ are used to treat prolactinomas
dopamin agonists like cabergoline, bromocriptine
Describe the cellular location and biochemistry of the estrogen receptor
nuclear location
bound to heat shock proteins that dissociate upon estrogen binding
receptor dimerizes then can bind estrogen response element in DNA
_______ is a weak estrogen produced by the placenta
estriol
____ is the principle ovarian estrogen; _____ is an estrogen common in post-menopause
estradiol/ estrone
What is the source of most estrogen in post-menopausal women
peripheral aromatization of adrenal androgens
What is the effect of estrogen at bone?
maintains bone mass
stimulates closure of epiphyses
What is the effect of estrogen in the liver?
Stimulates production of SHBG, thyroid hormone binding globulin, and blood clotting factors
What are therapeutic uses of estrogens?
- tx estrogen deficiency in premature ovarian failure, menopause
- prevention, treatment of osteoporosis
- contraception
If estrogen is given therapeutically without opposing progesterone, there is increased risk of __________
endometrial carcinoma
What is the mechanism of action of clomiphene citrate?
Inhibits estrogen binding in the hypothalamus and anterior pituitary, preventing the normal feedback regulation and causing increased secretion of GnRH and gonadotropins, stimulating ovarian follicle development
technically has weak agonist effects, but clinically acts as a pure antagonist