Reproductive Flashcards
most potent form of endogenous estrogen in women
estradiol
- other forms have 1/10th the potency
do synthesized estrogens have more or less bioavailability?
more because less first pass metabolism by liver
therapeutic uese of estrogen
hormone replacement in post-menopausal women
contraception
benefits of HRT
- decreased vasoactive responsiveness = less hot flashes and night sweats
- prevention/tx of postmenopausal atrophy of tissues
- benefits sleep quality
- estrogen decreases resorption of bone decreasing osteoporosis
risks of exogenous estrogen
stroke blood clots ovarian ca endometrial ca breast ca
medroxyprogesterone acetate (depo)
injected birth control
10 months
increased risk of breast ca and dementia if taken with premarin
WHI - E + P trial arm
estrogen + progestin (prempro) = increased MI stroke DVT and PE breast ca colorectal ca fewer fractures
bio-identical hormones
alternative to oral CEE and MPA
- cream, patch, etc
Bi-est
TriEst
estriol: estradiol 80:20 - better option
estriol: estradiol: estrone 80:10:10
Premarin
conjugated estrogen
alters gene transcription
SE: vaginal bleeding, breast tenderness, increased risk of DVT, increased atherosclerosis and CAD, uterine and breast ca
when can you give HRT with unopposed estrogen?
only if hysterectomy otherwise it will cause endometrial hyperplasia
progestins
synthetic progesterone used alone for contraception or with estrogen
8 types
drospirenone/yaz/Yasmin
synthetic progestin
4th generation progestin gonane
derived from 17a-spironlactone, not 19
3 mg drospirenone and 20mcg ethinyl estradiol
*need to test K levels before and a few months into tx because it can cause K retention
medroxyprogesterone/provera/ depo-provera IM
synthetic variant of progesterone
progesterone only
contraceptive, HRT, dysfunctional uterine bleeding
increases LDL and decreases HDL
used to block hormonal aggravation of tissue with endometriosis
*chemically castrate sex offenders
contraindicated with DVT Ca, causes birth defects
- can cause metabolic disturbances
- at high doses can use to treat ca
OCP and depression/anxiety
alter/lower serotonin which can lead to anxiety and depression
benefits of OCPs
decreased risk of colorectal ca
decreased PID, dysmenorrhea, acne, PCOS, and PMS
OCPs and breast cancer risk
slight increase in risk during and 10 years after use
no increased risk 10 or more years after stopping
- decrease in risk of ovarian ca
what drugs reduce the efficacy of OCPs?
antibiotics
st johns wart
medroxyprogesterone/depoprovera
many benefits
don’t use for more than 2 years due to increased risk of osteoporosis
the use of oral contraceptives decreases risk of endometrial and ovarian cancer by what percent?
50%
80% after 10 years of use
risk of drospirenone?
6-7 times the risk of developing thromboembolism
2 times risk of women taking levonorgestrel
drospirenone properties
- anti-mineralcorticoid effect reduces water retention and bloating
- also treats premenstrual dysphoric disorder
depo-sub-q provera 104
104mg aqueous suspension of medroxyprogesterone acetate.
31% less than original
how does depo-provera work?
high dose progestin inhibits follicular devleopment, preventing ovulation
- decreases GnRH -> decreases release of FSH and LH
benefits and risks of depo/medroxyprogesterone
- reduces risk of endometrial ca by 80%, no increased risk of DVT, stroke, MI.
- menstrual irregularities, abd discomfort, weight changes, hair loss, depression, nervousness, delayed return of fertility, bone less!
Implanon
subdermal progestin implant
remove after 3 years
ortho-evra
discontinued due to thrombolic events
transdermal patch
- middle layer contains 150ugm norelgestromin and 20 ugm ethinyl estradiol
- new patch every week for 3 weeks and then 1 week off
IUDs
what types and doses?
ParaGard - copper, no hormones (impairs sperm mobility)
Mirena - mg progestine and 52 mg levongestrel (20mcg/day)
Liletta - progestine and 52 mg levongestrel (20mcg/day)
Skyla - progestine and 13.5mg levongestrel (14 mcg.day)
effectiveness of IUDs
0.7%
Plan B
Levongestrel 1. mg as 2 750 ug doses 12 hours apart or as one single dose
works up to 72 hours after sexual intercourse
Ulipristal acetate/Ella One
SPRM progestin receptor modulator
morning after pill
given up to 5 days (120 hours) after intercourse
60% effective
Mifepristone/mifeprex
abortion pill
synthetic steroid compound used in first two months of pregnancy
progestin antagonist - blocks receptors
85% success rate
Clomiphene/Clomid
selective estrogen receptor modulator
infertility/amenorrhea
binds estrogen receptor sites in brain -> increased GnRH release -> increased LH and FSH stimulating ovulation
testonsterone MOA
alteration of gene transcription
metabolized to dihydrotestosterone or estrogen
androgenic (male sex hormones) and anabolic (protein metabolism) effects.
Leuprolide/lupron
anti-androgenic hormone and anti-estrogenic hormone
prostate ca, precocious puberty, endometriosis and uterine fibroids, IVF
decreased libido, impotence, nausea, vomitting, hot flashes, nigth sweats, osteoporosis