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Estrogens and Progestins Flashcards

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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
What happens to estrogen levels in the luteal phase of menstruation?
Progesterone levels rise | Estrogen levels fall from their peak, but remain elevated
26
What is the MOA of most steroids?
Bind to intracellular receptor, that then migrates into the nucleus
27
What is the effect of progesterone on lipid and glucose levels? Estrogen?
Progesterone = Increases LDL and fat deposition, Increases fasting Glucose levels Estrogen = decrease LDL, increase HDL, increase fats
28
What is the steroid that causes insulin intolerance?
Progesterone
29
What is the effect of progesterone on prostaglandin production in the uterus? Why is this significant?
Decreases, which helps maintain the relaxed state of the uterus
30
What are the three primary natural steroids?
Estradiol Estrone Estriol
31
What are the two primary synthetic estrogens?
Ethinyl estradiol | Mestranol
32
What is the primary nonsteroidal synthetic estrogen?
Diethylstilbestrol
33
Natural steroid, synthetic steroid, or nonsteroidal synthetic: Estradiol
Natural
34
Natural steroid, synthetic steroid, or nonsteroidal synthetic: ethinyl estradiol
Synthetic
35
Natural steroid, synthetic steroid, or nonsteroidal synthetic: Estrone
Natural
36
Natural steroid, synthetic steroid, or nonsteroidal synthetic: estriol
Natural
37
Natural steroid, synthetic steroid, or nonsteroidal synthetic: Mestranol
Synthetic
38
Natural steroid, synthetic steroid, or nonsteroidal synthetic: diethylstilbestrol (DES)
Nonsteroidal synthetic
39
What is the benefit of ethinyl estradiol over regular estrogen?
Markedly increased half-life, and much lower dose needed
40
What is conjugated equine estrogens (Premarin) used for?
Hormone replacement therapy
41
Why is exogenous estrogen used in menopause?
Maintain bone density Suppress hot flashes Suppress urogenital atrophy
42
What are the four major side effects of exogenous estrogen use over the long term? When do these present?
1. CHD 2. Stroke 3. PE 4. Invasive breast CA Present years later
43
What are the two protective effects of exogenous estrogen?
Decreases colorectal cancer and hip fractures
44
What is the way estrogen works as a contraceptive?
Suppresses ovulation via negative feedback pressure on HPG axis
45
How does estrogen work in treating acne? (2)
- Suppress steroidogenesis | - Increases SHBG production by the liver, thereby decreasing testosterone concentrations
46
What determines if a birth control pill increases or decreases acne?
More progesterone component usually means more acne
47
What are the usual side effects of estrogen?
breast tenderness endometrial hyperplasia Increased blood coagulation
48
What causes the increased migraine risk with exogenous estrogen use?
May indicate altered blood flow
49
What causes the increased risk of cholestasis with exogenous estrogen use?
Changes secretion of cholesterol into bile
50
What likely mediates the increased risk of developing breast CA with birth control?
Progestin, not estrogen
51
What is the one clear example where you can administer estrogen alone without concern of endometrial hyperplasia and cancer?
If they've had a hysterectomy
52
What is the MOA of estrogen causing cancer?
Trophic effect of hormones and ROS production during metabolism
53
How does estrogen increase blood coagulation?
Decreases antithrombin | Increases factors II VII IX and X
54
How does estrogen cause bloating?
Loss of intravascular fluid
55
What are the two major parent steroids of progesterone?
Progesterone itself | 19-nortestosterone
56
What is the progestin that is derived from progesterone?
Medroxyprogesterone acetate
57
What are the progestins that are derived from 19-nortestosterone?
Norethindrone, norgestrel and other nor compounds
58
What is Medroxyprogesterone acetate (MPA) usually used for?
Commonly combined with estrogen for HRT
59
What is norethindrone usually used for?
Combinational or progestin only hormone contraception
60
What is norgestrel usually used for?
Combinational or progestin only hormone contraception
61
True or false: you never give estrogen alone for birth control
True
62
What is the MOA of progestins as a contraceptive?
Inhibits HPA axis (80% of the time) | Increases cervical mucous viscosity
63
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)
Because they increase cervical mucous viscosity.
64
What is the MOA of using progestins to treat dysmenorrhea?
Decreases endometrial mass and decreases prostaglandin production
65
What is the MOA of using progestins to treat endometriosis?
Decreases endometrial proliferation by regulating ER expression and stimulating differentiation of endometrial cells
66
Why are progestins used in HRT?
Decreases the risk of endometrial hyperplasia caused by estrogens
67
How does progesterone decrease the pain associated with uterine contractions?
Decrease prostaglandin production

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