021315 female pharm Flashcards
physiological effects of estrogen
- enhances skeletal maturation and epiphyseal growth plate closure
- feedback regulation of gonadotropin release
- positive effects on bone mass
- increases clotting
- changes bile composition (increases saturation of bile with cholesterol-can cause gallstones)
- increases amt of cervical mucus and water content (facilitates sperm penetration of cervix)
- promotes endometrial proliferation
- increases tubal contractility and favors uterine myometrium contractions
progesterone and estrogen bioavailability
low oral bioavailability
half life of minutes due to first pass effect
physiologic effects of progesterone
- decreases frequency of GnRH pulses (suppresses gonadotropin release)
- decreases estrogen-driven endothemetrial proliferation and leads to development of secretory endomerium
- changes cervical mucous to scant viscid material (sperm has difficulty penetrating)
- maintenance of pregnancy
main determinant for onset of menstruation
abrupt decline in progesterone at end of cycle
mestranol is converted by the body to
ethinyl estradiol
ethinyl estradiol
synthetic estrogen orally bioavailable (limits first pass effect)
uses of estrogen
combination oral contraceptives (ethinyl estradiol or mestranol)
postmenopausal hormone replacement (equine estrogens, estradiol)
failure of pituitary fxn and ovarian development
adverse and toxic effects of estrogen
gallbladder disease oral estrogens increase risk of thromboembolic dis nausea and vomiting-initial use breast swelling migraine
contraindications to estrogen use
pregnancy
estrogen-dependent cancers
undiagnosed uterine bleeding
thromboembolic disorders
clomiphene
racemic mixture of two isomers (weak estrogen agonist and potent antagonist)
use of clomiphene
induce ovulation (infertility due to anovulation)
MOA of clomiphene
inhibits action of stronger estrogens–inhibiting feedback on pituitary and hypothalamus. increases pulsatile gonadotropin release amplitude
side effects of clomiphene, tamoxifen, raloxifene, aromatase inhibitors
hot flashes
SERMs MOA
mixed estrogenic and antiestrogenic effects (tissue specific)
it’s anti-estrogenic in breast
use of tamoxifen
tx and prevention of breast cancer
raloxifene MOA
estrogen agonist in bone
use of raloxifene
prophylaxis of osteoporosis
breast cancer
aromatase inhibitors
letrozole
anastrozole
exemestane
suicide inhibitor that irreversibly inactivates aromatase
exemestane
uses of aromatase inhibitors
breast cancer
medroxyprogesteron
progesterone analog
norethindrone
19 nortestosterone derivative
primarily progestational rather than androgenic activity
ethinyl subsituent at C17 slows hepatic metabolism
norgestrel
racemic mixture of inactive isomer and active isomer Levonorgestrel
13 ethyl substituent results in more potent progestin with less androgenic activity than norethindrone
drospirenone
spironolactone analogue
has ANTI-MINERALCORTICOID and progestin activity
use of drospirenone
pregnancy prevention
emotional and physical symptoms of premenstural dysphoric disorder (to reduce tendency toward edema)
moderate acne vulgaris
uses of progestins
hormonal contraceptives
post menopausal hormone replacement therapy (with an estrogen b/c want to limit the proliferation that would occur with estrogen alone)
others-secondary amenorrhea, endometrial hyperplasia
adverse effects of progestins
headache
breakthrough bleeding
androgenic actions-acne, hirsutism
mifepristone
competitive progesterone receptor modulator. mainly an antagonist
use of mifepristone
pregnancy termination
MOA of mifepristone
causes decidual breakdown
sensitizes myometrium to contractile actions of PGs
how is mifepristone administered
in combo with PG (misoprostol) to ensure expulsion of blastocyst
ulipristal
selective progesterone receptor modulator
partial agonist
use of ulipristal
emergency contraception
MOA of ulipristal
inhibits ovulation by inhibiting LH release which inhibits LH-induced follicular rupture in ovary
emergency contraception
combined oral contraceptives (levonorgestrel and ethinyl estradiol)
levonorgestrel alone
ulipristal
