Progestins, Estrogens, & Androgens

Question 1

GNRH from the hypothalamus stimulates the pituitary to release what?

Answer 1

LH and FSH

Question 2

LH and FSH stimulate the ovary to do what?

Answer 2

progesterone, estrogens, follicular growth and ovulation

Question 3

The placenta releases progesterone, estrogen, or chorionic gonadotropin, what does the CG cause in the ovary?

Answer 3

Causes ovary to release progesterone, estrogens, follicular growth, and ovulation.

Question 4

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?

Answer 4

1. inhibits

2. Increases and inhibits???

Question 5

Is estradiol, gonadotropins or progesterone increased right at ovulation?

Answer 5

estradiol and gonadotropins(LH and FSH)

Question 6

What cells is progesterone made in? Estradiol?

Answer 6

Theca cells

In both theca and granulosa, but mostly granulosa

Question 7

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

Answer 7

1. stim. growth and development during pub.
2. promote prolif. during follicular phase
3. promote prolif
4. block resorption
5. Up HDL, Down LDL
6. Increase risk and stroke
7. increase risk of endometrial and breast
8. Increase

Question 8

What are the effects of progesterone on the following-

1. endometrium
2. menstruation
3. cervical mucus
4. body temperature
5. mammary gland

Answer 8

1. promotes develop. during luteal phase
2. main determinant of onset
3. Decreases the amount of mucus and increases viscosity
4. increases basal temp.
5. stim growth and development during preg.

Question 9

What are the effects of progesterone on the following-

1. Uterus
2. mineralcorticoids

Answer 9

1. essential for maintenance of pregnancy

2. weak mineralcorticoid antagonist

Question 10

Is progesterone or estradiol rapidly inactivated when given orally?

Answer 10

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]

Question 11

What is an environmental contaminant with estrogen-like effects?

Answer 11

bisphenol A

Question 12

What main drugs are given for contraception? suppression of the HPG axis? replacement therapy? Abortion? Ovulation induction

Answer 12

1. P, E, SPRM
2. P, E
3. P, E SERMS
4. P antagonist
5. E antagonists and aromatase inhibitors

Question 13

What main drugs are used for breast cancer therapy?

Answer 13

SERMS, aromatase inhibitors

Question 14

What is the most effective non-hormonal contraceptions? How does it work?

Answer 14

Cooper IUD (Paragard)
spermicidal but may also prevent implantation

Question 15

How do the progestin only contraceptions stop pregnancy? 2

Answer 15

1. prevent fertilization by decreasing the amount
   and increasing the viscosity of cervical mucus
2. prevent ovulation by inhibiting the
   hypothalamus and the pituitary

Question 16

Progestins + estrogen birth control usually uses what 2 chemicals?

Answer 16

norethindrone and ethinyl estradiol

Question 17

What is the main mechanism of action for the progestin + estrogen type birth control?

Answer 17

1. prevent ovulation by inhibiting the pituitary and thalamus
   [OPPOSITE OF PROGESTIN ONLY]
2. decreasing the amount
   and increasing the viscosity of cervical mucus

Question 18

What are some health benefits of progestin + estrogen birth control? 3

Answer 18

1. decreased ovarian cysts $ fibrocystic breasts
2. decreased incidence of endometrial and ovarian cancer
3. Increase HDL and down LDL

Question 19

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?

Answer 19

1. progestin only
2. Progestin +estrogen
3. progestin only
4. both (estrogens do when they are given continuous)

Question 20

What is the efficacy of the combination type contraceptives reduced by?

Answer 20

antibiotics of the rifampin family and some anticonvulsants

Question 21

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?

Answer 21

1. about 50%
2. near 80%
3. 40%
4. 50%
5. 10%

Question 22

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?

Answer 22

1. 2-4x
2. ovulation
3. oral and no prescription
4. suppression of the hypothalamic‐pituitarygonadal
   axis.

Question 23

What are the side effects of post-coital progestin?

Answer 23

nausea/vomit
headache
dizzy
breast tenderness
abdominal and leg cramps

Question 24

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?

Answer 24

1. ulipristal
2. used within 5 days
3. 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
4. Prescription necessary

Question 25

Can you use Copper IUD paragaurd post coital"?

Answer 25

YEs

Question 26

What can be used to to suppress the hypothalamic-pituitary‐ ovarian axis in the treatment of dysmenorrhea, and endometriosis.?

Answer 26

Progestrins

Question 27

What are used as | replacement therapy in ovarian dysfunction?

Answer 27

progestrin/estrogen combo

Question 28

What are used as replacement therapy for the treatment of postmenopausal symptoms and postmenopausal osteoporosis: lowest effective dose and for the shortest duration possible>

Answer 28

Progestrin/estrogen combo

Question 29

What is the only agonist of breast tissue SERM?

Answer 29

Estradiol

Question 30

What is the only antagonist of bone SERM?

Answer 30

clomiphene/fluvestrant

Question 31

What is the only antagonist of CV system SERM?

Answer 31

clomiphen/fluvestrant

Question 32

What SERMS are antagonistic to the endometrium? neutral?

Answer 32

1. clomiphene/fluvestrant & bazedoxifene | 2. raloxifene and ospemifene

Question 33

What is the only antagonist to vaginal epithelium SERM? neutral?

Answer 33

1. clomiphene fluvestrant | 2. raloxifene

Question 34

What is roloxifenes big advantage over tamoxifen?

Answer 34

not being an agonist in endometrium

Question 35

When given early in the menstrual cycle what do the clomiphene and fulvestrants do?

Answer 35

induce ovulation- antagonize the inhibitory effects of estrogen on the pituitary and hypothalamus

Question 36

What are aromatase inhibitors useful for? can they be steroidal or non-steroidal?

Answer 36

1. treat breast cancer and induce ovulation | 2. Both

Question 37

What can RU486 be used for other than abortion?

Answer 37

glucocorticoid antagonist and is approved to be used as such in the treatment of individuals with Cushing’s and type 2 diabetes

Question 38

What does LH and FSH increase in the testes? Do they feedback inhibit the HPA axis?

Answer 38

1. Androgens (testosterone and dihydrotestosterone) | 2. Yes

Question 39

What cells ini the testes form testosterone and estradiol?

Answer 39

leydig cells

Question 40

What takes cholesterol to pregenelone? what takes testosterone to estradiol? what takes testosterone to dihydrotestosterone?

Answer 40

1. cholesterol side chain cleavage 2. aromatase 3. 5 alpha-reductase

Question 41

Review the following actions of androgens

Answer 41

1. Virilization of the urogenital tract during development 2. puberty 3. maintenance of secondary sexual characteristics 4. essential for spermatogenesis 5. promote anabolic reactions

Question 42

Testosterone is ineffective when given orally, how | can it be administered?

Answer 42

``` transdermally (ANDROGEL®) or as buccal tablets (STRIANT®). ```

Question 43

How can testosterone esters be given?

Answer 43

intramuscularly

Question 44

What can be given orally that is an analog of testosterone? what is the problem though?

Answer 44

17 alpha alkylated androgen (danazole) but they have more side effects such as liver toxicity

Question 45

What is androgen therapy used for?

Answer 45

Replacement therapy in male hypogonadism treatment of some catabolic states such as muscle wasting

Question 46

REview the side effects of androgen therapy

Answer 46

Virilization, feminization, suppression of HPA, edema, jaundice, hepatic carcinoma

Question 47

What do we screen for ovulation? pregnancy?

Answer 47

LH | CG

Question 48

What do we use FSH for? CG for?

Answer 48

Induce follicular growth induce ovulation BOTH ARE INJECTIONS

Question 49

gonadorelin in a synthetic GnRH that does what?

Answer 49

stimulates gonatotropin secretion

Question 50

What does luprolide do?

Answer 50

``` – After and initial stimulation of gonadotropin secretion they suppress it (desensitization). – Therefore these are used to suppress gonadotropin secretion (like GnRH antagonists). Injectable ```