Estrogens and progestins Flashcards

1
Q

steroidogenesis in the ovary is regulated by what compounds?

A

LH and FSH (gonadotropins)

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2
Q

which cells are required for estradiol synthesis?

A

theca and granulosa

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3
Q

what are the features of follicular phase of ovarian cycle?

A
  1. high frequency, low amplitude LH secretion
  2. estrogen rises
  3. endometrial proliferation
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4
Q

what is the main feature of ovulation? which day does it occur?

A

estrogen induced gonadotropin surge

day 14

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5
Q

what are the features of the luteal phase of the ovarian cycle?

A
  1. rise in estrogen and progesterones

2. endometrial differentiation under control of progesterone

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6
Q

which hormone is absolutely required for ovulation?

A

LH

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7
Q

what is the effect of estrogen on the endometrium?

A

endometrial proliferation

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8
Q

what is the effect of progesterone on the endometrium?

A

endometrial differentiation
preparation for implantation
decrease uterine contractions

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9
Q

how does progesterone influence glucose metabolism?

A

leads to glucose intolerance

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10
Q

which hormone is the key regulator during the luteal phase of the menstrual cycle?

A

progesterone

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11
Q

which hormone is the key regulator during the follicular phase of the menstrual cycle?

A

estrogen

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12
Q

what are the effects of estrogen on lipids?

A

decrease LDL
increase HDL
increase TGs

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13
Q

what is the effect of estrogen on bone?

A

antiresorptive

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14
Q

what is the effect of estrogen on the liver?

A

increase plasma proteins

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15
Q

what are the effects of estrogen on the blood?

A

increase coag factors

decrease antithrombin

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16
Q

what is important about ethinyl estradiol?

A

addition of ethinyl group to estrogen increases half life up to 13-27 hours

17
Q

what are the risks of long term estrogen plus progesterone in healthy postmenopausal women?

A

increased coronary heart disease
increased stroke
increased PE
increased invasive breast cancer

18
Q

what is the main mechanism of estrogen use on contraception?

A

negative feedback pressure on HPG axis

suppresses LH surge

19
Q

what is responsible for suppression of acne in birth control?

A

estrogenic component of BC preparations

20
Q

how does estrogen inhibit acne?

A

inhibits steroidogenesis

decreases free testosterone concentrations

21
Q

what are the adverse effects of estrogen?

A

breast tenderness
endometrial hyperplasia
increased blood coagulation

22
Q

in which situation can you use estrogen alone for hormone replacement therapy?

A

hysterectomy - no risk of endometrial cancer

23
Q

what are the two backbone molecules for the progestins?

A

progesterone

19-nortestosterone

24
Q

what are the important progestins?

A

medroxyprogesterone (MPA)
norethindrone
norgestrel

25
Q

how do progestins differ from estrogens for ovulation? what about for BC in general? why?

A

progestins are less efficacious than estrogens at suppressing ovulation

for BC, they are just as efficacious

progestin effect on cervical glands (increasing viscosity)

26
Q

what are the therapeutic uses for progestins?

A

contraceptives
HRT
dysmenorrhea
endometriosis

27
Q

what is the risk of unchallenged estrogen use?

A

continued proliferation

28
Q

what is the rationale for progestin use in HRT?

A

decrease risk of endometrial hyperplasia caused by estrogens

29
Q

what is the rationale for progestin use in dysmenorrhea?

A

decrease endometrial mass and PG production

30
Q

what is the rationale for progestin use in endometriosis?

A

decrease endometrial proliferation by regulating ER expression and stimulating differentiation of endometrial cells

31
Q

what are the adverse effects of progestin use?

A
breakthrough bleeding 
impaired glucose tolerance 
hirsutism 
acne 
lipid metabolism
32
Q

what are the general MOAs of combined estrogen-progestin BC and progestin-only pills or implants?

A
  1. prevent pituitary release of hormones that stimulate ovulation
  2. suppress LH and FSH surge
  3. alter cervical mucus
  4. alter endometrium
33
Q

which oral BC pill is progestin only?

A

norethindrone

34
Q

what are the contraindications of estrogen containing contraceptives?

A
  1. known or suspect breast cancer
  2. thromboembolic disorders
  3. liver disease
  4. CV disease hx
  5. smokers 35 yo or older