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Pharm > Estrogens and Progestins > Flashcards

Estrogens and Progestins Flashcards

1
Q

What are the two cells in the female that produce estrogen?

A

Theca and granulosa cells

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2
Q

What are the enzymes that are needed to convert cholesterol to estrogen?

A

3 beta HSD
17 hydroxylase
17, 20 hydroxylase

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3
Q

What is the enzyme that converts androstenedione to testosterone?

A

17 beta HSD

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4
Q

What is the enzyme that converts androstenedione or testosterone to estrone/estradiol?

A

Aromatase

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5
Q

What is the function of estrogen on the endometrium?

A

Proliferation

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6
Q

What are the metabolic effects of estrogen?

A

Decrease LDL, increase HDL, and increase Triglycerides

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7
Q

What is the effect of estrogen on bones?

A

Antiresorptive

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8
Q

What is the effect of estrogen on the liver?

A

Increase plasma proteins

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9
Q

What is the effect of estrogen on the blood?

A

Increased expression of coagulation factors, decreased antithrombin

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10
Q

What is the effect of estrogen in the menstrual cycle?

A

Key regulator during follicular phase

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11
Q

What is the role of estrogen in the HPA axis?

A

Feedback regulation for steroidogenesis and ovulation

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12
Q

What is the role of progesterone in the HPA axis?

A

Feedback regulation for steroidogenesis and ovulation

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13
Q

What is the effect of progesterone on the endometrium? Uterine contractions?

A

Causes endometrial differentiation, and preparation for implantation

Decreases uterine contractions

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14
Q

What is the effect of progesterone the cervical glands?

A

Increases cervical mucus viscosity

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15
Q

What is the effect of progesterone in the menstrual cycle?

A

Key regulator during the luteal phase

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16
Q

What cells does LH bind to? What does this cause?

A

Theca cells to increase Testosterone and androstenedione

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17
Q

What cells does FSH bind to? What does this cause? What enzyme is present in these cells?

A

Granulosa cells to increase estrone and estradiol

Aromatase

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18
Q

When do estrogen and progesterone exert a negative feedback? Positive?

A 
Negative = most of the time
Positive = mid ovarian cycle (around day 14)
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19
Q

What causes the surge in LH mid cycle?

A

Surge in estrogen

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20
Q

What causes the release of the ova from the mature follicle?

A

Surge is estrogen

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21
Q

What maintains the LH levels late in menstruation?

A

Corpus luteum

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22
Q

What happens during the follicular phase of the menstrual cycle? (2)

A

High frequency, low amplitude LH secretion
Estrogen rises
Endometrial proliferation

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23
Q

What happens during the luteal phase of the menstrual cycle? (2)

A
  • Rise in estrogens and progesterone

- Endometrial differentiation under control of progesterone

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24
Q

Which hormone controls endometrial proliferation, and which controls the maintenance/secretory phase?

A

Proliferation = estrogen

Maintenance/secretory phase = progesterone

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25
Q

What happens to estrogen levels in the luteal phase of menstruation?

A

Progesterone levels rise

Estrogen levels fall from their peak, but remain elevated

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26
Q

What is the MOA of most steroids?

A

Bind to intracellular receptor, that then migrates into the nucleus

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27
Q

What is the effect of progesterone on lipid and glucose levels? Estrogen?

A

Progesterone = Increases LDL and fat deposition, Increases fasting Glucose levels

Estrogen = decrease LDL, increase HDL, increase fats

28
Q

What is the steroid that causes insulin intolerance?

A

Progesterone

29
Q

What is the effect of progesterone on prostaglandin production in the uterus? Why is this significant?

A

Decreases, which helps maintain the relaxed state of the uterus

30
Q

What are the three primary natural steroids?

A

Estradiol
Estrone
Estriol

31
Q

What are the two primary synthetic estrogens?

A

Ethinyl estradiol

Mestranol

32
Q

What is the primary nonsteroidal synthetic estrogen?

A

Diethylstilbestrol

33
Q

Natural steroid, synthetic steroid, or nonsteroidal synthetic: Estradiol

A

Natural

34
Q

Natural steroid, synthetic steroid, or nonsteroidal synthetic: ethinyl estradiol

A

Synthetic

35
Q

Natural steroid, synthetic steroid, or nonsteroidal synthetic: Estrone

A

Natural

36
Q

Natural steroid, synthetic steroid, or nonsteroidal synthetic: estriol

A

Natural

37
Q

Natural steroid, synthetic steroid, or nonsteroidal synthetic: Mestranol

A

Synthetic

38
Q

Natural steroid, synthetic steroid, or nonsteroidal synthetic: diethylstilbestrol (DES)

A

Nonsteroidal synthetic

39
Q

What is the benefit of ethinyl estradiol over regular estrogen?

A

Markedly increased half-life, and much lower dose needed

40
Q

What is conjugated equine estrogens (Premarin) used for?

A

Hormone replacement therapy

41
Q

Why is exogenous estrogen used in menopause?

A

Maintain bone density
Suppress hot flashes
Suppress urogenital atrophy

42
Q

What are the four major side effects of exogenous estrogen use over the long term? When do these present?

A
  1. CHD
  2. Stroke
  3. PE
  4. Invasive breast CA

Present years later

43
Q

What are the two protective effects of exogenous estrogen?

A

Decreases colorectal cancer and hip fractures

44
Q

What is the way estrogen works as a contraceptive?

A

Suppresses ovulation via negative feedback pressure on HPG axis

45
Q

How does estrogen work in treating acne? (2)

A
  • Suppress steroidogenesis

- Increases SHBG production by the liver, thereby decreasing testosterone concentrations

46
Q

What determines if a birth control pill increases or decreases acne?

A

More progesterone component usually means more acne

47
Q

What are the usual side effects of estrogen?

A

breast tenderness
endometrial hyperplasia
Increased blood coagulation

48
Q

What causes the increased migraine risk with exogenous estrogen use?

A

May indicate altered blood flow

49
Q

What causes the increased risk of cholestasis with exogenous estrogen use?

A

Changes secretion of cholesterol into bile

50
Q

What likely mediates the increased risk of developing breast CA with birth control?

A

Progestin, not estrogen

51
Q

What is the one clear example where you can administer estrogen alone without concern of endometrial hyperplasia and cancer?

A

If they’ve had a hysterectomy

52
Q

What is the MOA of estrogen causing cancer?

A

Trophic effect of hormones and ROS production during metabolism

53
Q

How does estrogen increase blood coagulation?

A

Decreases antithrombin

Increases factors II VII IX and X

54
Q

How does estrogen cause bloating?

A

Loss of intravascular fluid

55
Q

What are the two major parent steroids of progesterone?

A

Progesterone itself

19-nortestosterone

56
Q

What is the progestin that is derived from progesterone?

A

Medroxyprogesterone acetate

57
Q

What are the progestins that are derived from 19-nortestosterone?

A

Norethindrone, norgestrel and other nor compounds

58
Q

What is Medroxyprogesterone acetate (MPA) usually used for?

A

Commonly combined with estrogen for HRT

59
Q

What is norethindrone usually used for?

A

Combinational or progestin only hormone contraception

60
Q

What is norgestrel usually used for?

A

Combinational or progestin only hormone contraception

61
Q

True or false: you never give estrogen alone for birth control

A

True

62
Q

What is the MOA of progestins as a contraceptive?

A

Inhibits HPA axis (80% of the time)

Increases cervical mucous viscosity

63
Q

Progestins are only effective at inhibiting the HPA axis about 80% of the time, yet are more effective than estrogen alone for contraception. Why are they still very effective as a contraceptive (and not because they’re usually combined with estrogen)

A

Because they increase cervical mucous viscosity.

64
Q

What is the MOA of using progestins to treat dysmenorrhea?

A

Decreases endometrial mass and decreases prostaglandin production

65
Q

What is the MOA of using progestins to treat endometriosis?

A

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

66
Q

Why are progestins used in HRT?

A

Decreases the risk of endometrial hyperplasia caused by estrogens

67
Q

How does progesterone decrease the pain associated with uterine contractions?

A

Decrease prostaglandin production

Pharm (73 decks)

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