Female repro pharm Flashcards
general adverse effects of progestins
Headache
breakthrough bleeding
androgenic actions, acne hirsuitism
decreases estrogen driven endometrial proliferation and leads to development of secondary endometrium
progesterone
contraindications estrogens
pregnancy
estrogen dependent cancers
undiagnosed uterine bleeding
thromboembolic disorders
spironolactone analogue
indications and side effects
Drospirenone
indications: pregnancy prevention, PMDD, moderate acne vulgaris
side effects - antimineralcorticoid activity
K should be monitored for hyperkalemia
therapuetic uses for progestins
Hormonal contraceptives
Post menopause hormone replacement (only with estrogen)
diagnosis of secondary amenorrhea
endometrial hyperplasia
progesterone analog, (injected+oral)
medroxprogesterone
natural estrogens
17b estradiol
estrone
estriol
progesterone binds what in plasma
corticosteroid binding globulin
albumin
some progestins bind SHBG
anti estrogen that inhibits action of strong estrogens via inhibition of feedback (pituitary hypothalamus) thus increasing pulsitile gonadotropin release amplitude
Clomiphene
mechanism and indication Raloxifene
side effects
SERM estrogen agonist in bone
Use: reudce rate of bone loss (osteopororsis prophylaxis) risk reduction for invasive breast cancer
side effects: (estrogenic) reduces total cholesterol, hot flashes, increases thrombosis, leg cramps (does NOT cause endometrial thickening as Tamoxifene)
therapeutic approaches for postmenopausal replacement
estrogen/progetin combo (intact uterus)
estrogen only (post hysterectomy)
Clomiphene mechanism
inhibits action of strong estrogens via inhibition of feedback at pituitary and hypothalamus
causes increase in GnRH pulse amplitude
phsyiological effects of estrogen on endometrium
enhance cervical mucus and increases water content
promotes endometrial proliferation
increases tubule contractility favoring rhythmic contractions of myometrium
indication, mechanism, side effects ulipristal
Emergency contraception
selective progesterone receptor mdoulator > inhibits LH release > inhibits LH induced folliculr rupture in ovary when taken 5 days after intercourse (inhibits ovulation)
side effects - headache, abd pain
synthetic estrogens
ehtinyl estradiol
mestranol
decreases the frequency of GnRH pulses, critical for suppressing gonadotropin release
progesterone
estrogen skeletal effects
skeletal maturation
epiphyseal plate closure
postive effects on bone mass
adverse effects estrogens
Gall bladder disease (due to increase cholesterol content in bile)
oral estrogens increase risk of thromboembolic disease
nausea and vomiting on initial use
breast swelling
migrane headaches
SERMS
Tamoxifen
Raloxifene
Alternatives to estrogen for the treatment of osteoporosis
raloxifene
alendronate (bisphosphonate)
progesterone derivative, etyinyl substituent at C17 slows hepatic metabolism to reduce firsts pass
progesterone derivative, racemic mixture, 13 ethyl subtituent results in potent progestin with less androgenic activity
norethindrone
Norgestrel
therapeutic uses of estrogens
combination oral contraceptives
post-menopause hormone replacement therapy
failure of pituitary function and and ovarian development
half life progesterone
minutes
relative strength of natural estrogens
estradiol > estrone > estriol
Tamoxifen mechanism and idication
side effects
SERM: mixed estrogenic and anti estrogenic effects (esp breast)
use: treatment and preventionof breast cancer (ER positive)
side effects (estrogenic) hot flashes, endometrial poliferation (risk of endometrial cancer)
increased thromboembolic disease
antiresoptive effect on bone
emergency contraceptive regimens
Levonorgeestrel + ethinyl estradiol (2 doses)
Levonorgesrel alone (2 doses)
Ulipristal
Aromatase inhibitors, specific mechanism, indication and side effects
Letrozole+Anastrozole: non steroidal reversible inhibitors of aromatase (reduce T>estradiol, Androstenedion>Estrone)
Exemestane: suicide inhibitor
use: treat breast cancer, ovulation induction (off-label)
side effects: hot flashes
inidcation, mechanism Mfepristone (Ru-486)
side effects
abortifacient
competitive progesterone receptor modulator (mainly antagonist)
competitively binds receptor, causing decidual breakdown leading to placental detachment.
snetizies myometrium to contractile actions of prostaglandins for expulsion
vaginal bleeding
