Progestins, Estrogens, & Androgens Flashcards

1
Q

GNRH from the hypothalamus stimulates the pituitary to release what?

A

LH and FSH

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2
Q

LH and FSH stimulate the ovary to do what?

A

progesterone, estrogens, follicular growth and ovulation

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3
Q

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

A

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

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4
Q

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?

A
  1. inhibits

2. Increases and inhibits???

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5
Q

Is estradiol, gonadotropins or progesterone increased right at ovulation?

A

estradiol and gonadotropins(LH and FSH)

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6
Q

What cells is progesterone made in? Estradiol?

A

Theca cells

In both theca and granulosa, but mostly granulosa

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7
Q
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
A
  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
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8
Q

What are the effects of progesterone on the following-

  1. endometrium
  2. menstruation
  3. cervical mucus
  4. body temperature
  5. mammary gland
A
  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.
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9
Q

What are the effects of progesterone on the following-

  1. Uterus
  2. mineralcorticoids
A
  1. essential for maintenance of pregnancy

2. weak mineralcorticoid antagonist

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10
Q

Is progesterone or estradiol rapidly inactivated when given orally?

A

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]

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11
Q

What is an environmental contaminant with estrogen-like effects?

A

bisphenol A

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12
Q

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

A
  1. P, E, SPRM
  2. P, E
  3. P, E SERMS
  4. P antagonist
  5. E antagonists and aromatase inhibitors
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13
Q

What main drugs are used for breast cancer therapy?

A

SERMS, aromatase inhibitors

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14
Q

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

A
Cooper IUD (Paragard)
spermicidal but may also prevent implantation
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15
Q

How do the progestin only contraceptions stop pregnancy? 2

A
  1. prevent fertilization by decreasing the amount
    and increasing the viscosity of cervical mucus
  2. prevent ovulation by inhibiting the
    hypothalamus and the pituitary
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16
Q

Progestins + estrogen birth control usually uses what 2 chemicals?

A

norethindrone and ethinyl estradiol

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17
Q

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

A
  1. prevent ovulation by inhibiting the pituitary and thalamus
    [OPPOSITE OF PROGESTIN ONLY]
  2. decreasing the amount
    and increasing the viscosity of cervical mucus
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18
Q

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

A
  1. decreased ovarian cysts $ fibrocystic breasts
  2. decreased incidence of endometrial and ovarian cancer
  3. Increase HDL and down LDL
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19
Q

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?

A
  1. progestin only
  2. Progestin +estrogen
  3. progestin only
  4. both (estrogens do when they are given continuous)
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20
Q

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

A

antibiotics of the rifampin family and some anticonvulsants

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21
Q

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?

A
  1. about 50%
  2. near 80%
  3. 40%
  4. 50%
  5. 10%
22
Q

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?

A
  1. 2-4x
  2. ovulation
  3. oral and no prescription
  4. suppression of the hypothalamic‐pituitarygonadal
    axis.
23
Q

What are the side effects of post-coital progestin?

A
nausea/vomit
headache
dizzy
breast tenderness
abdominal and leg cramps
24
Q

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?

A
  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
25
Q

Can you use Copper IUD paragaurd post coital”?

A

YEs

26
Q

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

A

Progestrins

27
Q

What are used as

replacement therapy in ovarian dysfunction?

A

progestrin/estrogen combo

28
Q

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

A

Progestrin/estrogen combo

29
Q

What is the only agonist of breast tissue SERM?

A

Estradiol

30
Q

What is the only antagonist of bone SERM?

A

clomiphene/fluvestrant

31
Q

What is the only antagonist of CV system SERM?

A

clomiphen/fluvestrant

32
Q

What SERMS are antagonistic to the endometrium? neutral?

A
  1. clomiphene/fluvestrant & bazedoxifene

2. raloxifene and ospemifene

33
Q

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

A
  1. clomiphene fluvestrant

2. raloxifene

34
Q

What is roloxifenes big advantage over tamoxifen?

A

not being an agonist in endometrium

35
Q

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

A

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

36
Q

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

A
  1. treat breast cancer and induce ovulation

2. Both

37
Q

What can RU486 be used for other than abortion?

A

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

38
Q

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

A
  1. Androgens (testosterone and dihydrotestosterone)

2. Yes

39
Q

What cells ini the testes form testosterone and estradiol?

A

leydig cells

40
Q

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

A
  1. cholesterol side chain cleavage
  2. aromatase
  3. 5 alpha-reductase
41
Q

Review the following actions of androgens

A
  1. Virilization of the urogenital tract during development
  2. puberty
  3. maintenance of secondary sexual characteristics
  4. essential for spermatogenesis
  5. promote anabolic reactions
42
Q

Testosterone is ineffective when given orally, how

can it be administered?

A
transdermally (ANDROGEL®) or as
buccal tablets (STRIANT®).
43
Q

How can testosterone esters be given?

A

intramuscularly

44
Q

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

A

17 alpha alkylated androgen (danazole)

but they have more side effects such as liver toxicity

45
Q

What is androgen therapy used for?

A

Replacement therapy in male hypogonadism

treatment of some catabolic states such as muscle wasting

46
Q

REview the side effects of androgen therapy

A

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

47
Q

What do we screen for ovulation? pregnancy?

A

LH

CG

48
Q

What do we use FSH for? CG for?

A

Induce follicular growth
induce ovulation

BOTH ARE INJECTIONS

49
Q

gonadorelin in a synthetic GnRH that does what?

A

stimulates gonatotropin secretion

50
Q

What does luprolide do?

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