Progestins, Estrogens, & Androgens Flashcards
GNRH from the hypothalamus stimulates the pituitary to release what?
LH and FSH
LH and FSH stimulate the ovary to do what?
progesterone, estrogens, follicular growth and ovulation
The placenta releases progesterone, estrogen, or chorionic gonadotropin, what does the CG cause in the ovary?
Causes ovary to release progesterone, estrogens, follicular growth, and ovulation.
Does progesterone and ovulation inhibit or increase release of GNRH and LH and FSH from the hypothalamus and pituitary? What about estrogens and follicular growth?
- inhibits
2. Increases and inhibits???
Is estradiol, gonadotropins or progesterone increased right at ovulation?
estradiol and gonadotropins(LH and FSH)
What cells is progesterone made in? Estradiol?
Theca cells
In both theca and granulosa, but mostly granulosa
What are the effects of estradiol on the following- 1. mammary glands 2. endometrium 3. vaginal epithelium 4 bone 5. HDL and LDL 6. Thromboembolism 7. Cancer 8. Progesterone receptors
- stim. growth and development during pub.
- promote prolif. during follicular phase
- promote prolif
- block resorption
- Up HDL, Down LDL
- Increase risk and stroke
- increase risk of endometrial and breast
- Increase
What are the effects of progesterone on the following-
- endometrium
- menstruation
- cervical mucus
- body temperature
- mammary gland
- promotes develop. during luteal phase
- main determinant of onset
- Decreases the amount of mucus and increases viscosity
- increases basal temp.
- stim growth and development during preg.
What are the effects of progesterone on the following-
- Uterus
- mineralcorticoids
- essential for maintenance of pregnancy
2. weak mineralcorticoid antagonist
Is progesterone or estradiol rapidly inactivated when given orally?
Both are
[Synthetic analogs are more useful but they
may cross‐react with other steroid receptors
(progesterone, estrogen, androgen,
mineralocorticoid) and act as agonists or
antagonists]
What is an environmental contaminant with estrogen-like effects?
bisphenol A
What main drugs are given for contraception? suppression of the HPG axis? replacement therapy? Abortion? Ovulation induction
- P, E, SPRM
- P, E
- P, E SERMS
- P antagonist
- E antagonists and aromatase inhibitors
What main drugs are used for breast cancer therapy?
SERMS, aromatase inhibitors
What is the most effective non-hormonal contraceptions? How does it work?
Cooper IUD (Paragard) spermicidal but may also prevent implantation
How do the progestin only contraceptions stop pregnancy? 2
- prevent fertilization by decreasing the amount
and increasing the viscosity of cervical mucus - prevent ovulation by inhibiting the
hypothalamus and the pituitary
Progestins + estrogen birth control usually uses what 2 chemicals?
norethindrone and ethinyl estradiol
What is the main mechanism of action for the progestin + estrogen type birth control?
- prevent ovulation by inhibiting the pituitary and thalamus
[OPPOSITE OF PROGESTIN ONLY] - decreasing the amount
and increasing the viscosity of cervical mucus
What are some health benefits of progestin + estrogen birth control? 3
- decreased ovarian cysts $ fibrocystic breasts
- decreased incidence of endometrial and ovarian cancer
- Increase HDL and down LDL
Is progestin only or progestin+estrogen continuous administration only? main effect on the pituitary/hypothalamus? has irregular menstural periods or absence of menstrual periods? absence of period?
- progestin only
- Progestin +estrogen
- progestin only
- both (estrogens do when they are given continuous)
What is the efficacy of the combination type contraceptives reduced by?
antibiotics of the rifampin family and some anticonvulsants
What percentage of pregnancies unintended? is it higher in younger women? how many are terminated by abortion? How many women used contraception the month they had the abortion? what percent of women in reproductive age have used emergency contraception?
- about 50%
- near 80%
- 40%
- 50%
- 10%
How much more of the progestrin (norgestrel) alone pill do we need for post-coital contraceptives? what does it prevent? oral & prescription? how does it work?
- 2-4x
- ovulation
- oral and no prescription
- suppression of the hypothalamic‐pituitarygonadal
axis.
What are the side effects of post-coital progestin?
nausea/vomit headache dizzy breast tenderness abdominal and leg cramps
What selective progesterone receptor modulator is used in ELLA for post-coital? when must it be used? is it more or less effective than norgesterel? how does it work? Is prescription needed?
- ulipristal
- used within 5 days
- more effective and longer efficacy
4.Inhibits ovulation by antagonizing the actions of
progesterone on the granulosa cell progesterone
receptor. This action of progesterone is needed for
follicular rupture - Prescription necessary
Can you use Copper IUD paragaurd post coital”?
YEs
What can be used to to suppress the hypothalamic-pituitary‐
ovarian axis in the treatment of dysmenorrhea,
and endometriosis.?
Progestrins
What are used as
replacement therapy in ovarian dysfunction?
progestrin/estrogen combo
What are used as
replacement therapy for the treatment of
postmenopausal symptoms and postmenopausal
osteoporosis: lowest effective dose and for the shortest
duration possible>
Progestrin/estrogen combo
What is the only agonist of breast tissue SERM?
Estradiol
What is the only antagonist of bone SERM?
clomiphene/fluvestrant
What is the only antagonist of CV system SERM?
clomiphen/fluvestrant
What SERMS are antagonistic to the endometrium? neutral?
- clomiphene/fluvestrant & bazedoxifene
2. raloxifene and ospemifene
What is the only antagonist to vaginal epithelium SERM? neutral?
- clomiphene fluvestrant
2. raloxifene
What is roloxifenes big advantage over tamoxifen?
not being an agonist in endometrium
When given early in the menstrual cycle what do the clomiphene and fulvestrants do?
induce ovulation- antagonize the inhibitory effects of estrogen on the pituitary and hypothalamus
What are aromatase inhibitors useful for? can they be steroidal or non-steroidal?
- treat breast cancer and induce ovulation
2. Both
What can RU486 be used for other than abortion?
glucocorticoid antagonist and is
approved to be used as such in the treatment of
individuals with Cushing’s and type 2 diabetes
What does LH and FSH increase in the testes? Do they feedback inhibit the HPA axis?
- Androgens (testosterone and dihydrotestosterone)
2. Yes
What cells ini the testes form testosterone and estradiol?
leydig cells
What takes cholesterol to pregenelone? what takes testosterone to estradiol? what takes testosterone to dihydrotestosterone?
- cholesterol side chain cleavage
- aromatase
- 5 alpha-reductase
Review the following actions of androgens
- Virilization of the urogenital tract during development
- puberty
- maintenance of secondary sexual characteristics
- essential for spermatogenesis
- promote anabolic reactions
Testosterone is ineffective when given orally, how
can it be administered?
transdermally (ANDROGEL®) or as buccal tablets (STRIANT®).
How can testosterone esters be given?
intramuscularly
What can be given orally that is an analog of testosterone? what is the problem though?
17 alpha alkylated androgen (danazole)
but they have more side effects such as liver toxicity
What is androgen therapy used for?
Replacement therapy in male hypogonadism
treatment of some catabolic states such as muscle wasting
REview the side effects of androgen therapy
Virilization, feminization, suppression of HPA, edema, jaundice, hepatic carcinoma
What do we screen for ovulation? pregnancy?
LH
CG
What do we use FSH for? CG for?
Induce follicular growth
induce ovulation
BOTH ARE INJECTIONS
gonadorelin in a synthetic GnRH that does what?
stimulates gonatotropin secretion
What does luprolide do?
– After and initial stimulation of gonadotropin secretion they suppress it (desensitization). – Therefore these are used to suppress gonadotropin secretion (like GnRH antagonists). Injectable
