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Park lecture 2 Flashcards

1
Q

Why are estrogen levels in women never constant? why do they fluctuate

A

Estrogen has positive and negative feedback. If only negative like testosterone, it would remain constant.

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2
Q

What cells produce estrogen

A

Granulosa cells

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3
Q

How is corpus luteum formed

A
  • FSH stimulates growth of 1 follicle.
    Becoming larger and larger and becoming primary and then secondary follicle
  • After 2 weeks it is fully mature (graafian follicle) and it ruptures
  • Oocyte is released and travels to uterus
  • The follicle becomes corpus luteum and stays for 2 weeks
  • if pregnancy does not occur, they disappear
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4
Q

What produces both estrogen and progesterone

A

Corpus luteum

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5
Q

1st two weeks before ovulation is called

A

Follicular phase

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6
Q

Last two weeks after ovulation is called

A

luteal phase

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7
Q

Explain the change in endometrium during menstruation

A
  • Day 1 is the start of menstruation, so endometrium collapses and is discharged (menstruation)
  • Once Estrogen is produced by follicle, it stimulates growth of uterus (proliferative phase)
  • Estrogen and progesterone is produced by corpus luteum and they help maturation of endometrium
    (secretary phase)
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8
Q

Explain what happens during early follicular phase

A

Estrogen suppresses the production of FSH

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9
Q

Explain what happens during late follicular phase

A

Estrogen stimulates the surge of LH and FSH.

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10
Q

The surge of LH and FSH in late follicular phase leads to

A

Ovulation and formation of corpus luteum

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11
Q

What happens in luteal phase

A

Estrogen and progesterone suppress LH and FSH

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12
Q

What would happen if FSH levels are continuously high?

A

Another follicle could grow, leading to multiple eggs being released

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13
Q

Remember the graphs for estrogen, progesterone, LH and FSH

A
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14
Q

Androstenedione acted on by aromatase will form

A

estrone

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15
Q

If we have too much 17b-estradiol in our system, what is it converted into to lower?

A

Estrone

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16
Q

T/F
Estrogen is not 1 compound. It is any cpd with estrogenic ability

A

True

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17
Q

Name 3 estrogens and how potent they are

A

17b estradiol- most potent
estrone- less potent
estriol- Less potent. Dominant form during pregnancy

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18
Q

Where is estrogen metabolized?
where is it excreted?

A

Metabolized in liver, excreted in urine.

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19
Q

explain enterohepatic circulation

A

Conjugated estrogen (broken down) in bile can be hydrolyzed in intestine and reabsorbed. They go through liver multiple times

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20
Q

What kind of ROA of estrogens have high ratio of hepatic to peripheral effect. What can we do to avoid it?

A

Oral administration. Can be avoided by RA that avoid first pass liver effect.

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21
Q

Endometrial effects of estrogen

A

Development of endometrial lining during menstrual lining.
Prolonged exposure leads to hyperplasia of endometrium and abnormal bleeding

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22
Q

Effect of estrogen on bone

A

Decreases bone resorption. (decreases in estrogen levels can lead to osteoporosis)

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23
Q

Effect of estrogen on transcortin and SHBG

A

Stimulates synthesis

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24
Q

Effects of estrogen on cholesterol levels

A

Increase HDL
Decrease LDL

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25
Effects of Estrogen on blood coagulation
Enhancement of blood coagulation
26
Effect of estrogen on CNS
affects mood
27
consequences of enterohepatic circulation
high ratio of hepatic to peripheral effect
28
4 clinical uses of estrogen
HRT in post menopausal women Osteoporosis Hormonal contraception replacement therapy in patients with primary hypogonadism (ovary not functioning)
29
3 ways estrogen helps post menopausal women in hormone replacement therapy
Relief of CNS disturbances(hot flash, sweating) Relief of symptoms resulting from urogenital atrophy (vaginal dryness) relief from psychological effects (mood swings)
30
List adverse effects of estrogen
uterine bleeding breast cancer endometrial carcinoma Nausea, headache, fluid retention, weight gain
31
What is the major cause of post menopausal uterine bleeding. Why?
Estrogen therapy Due to endometrial hyperplasia
32
What can we do to avoid post menopausal bleeding and endometrial carcinoma in estrogen therapy?
Administration of progestin
33
Why does the use of progestin prevent uterine bleeding in estrogen therapy
In maturation phase of the menstrual cycle, estrogen and progesterone are produced together to help the maturation of endometrium.
34
What is progestin?
An analog of progesterone
35
What effect does progestin have on prevention of breast cancer in estrogen therapy?
No effect
36
What are three required structural features in estrogenic cpds
Aromaticity in far left ring 17B-OH group OH at 3 position
37
Use of ether in estrogenic cpds at C3
Ethers can mask OH groups, which are readily hydrolyzed invivo
38
16 OH on estrogenic cpd effect
Decrease activity
39
Use of 17a-ethynyl substituent in estrogenic cpd
blocks metabolism and allows for oral activity
40
Use of ester on 17B position
Can temporarily block OH group for drug delivery,
41
how do 17 a-alkylated estrogens increase half life and enhance bioavailability
Prevent conversion to estrone
42
effect of esterification on 17-B carbon? How will this change the administration of drug?
Decreases solubility of the drug, allows for a slower absorption from injection site (depot), less frequent injections
43
in non-steroidal estrogens, what is the use of the far left amine substituted side?
Blocks helix-12 and leads to antagonist/serm activity
44
What is required for agonist activity in non-steroidal estrogens
OH group in top right aromatic ring
45
What is the purpose of the double bond in the middle of non steroidal estrogens?
Rigid core is needed to maintain proper space.
46
What should the distance be between the two hydroxy groups in non steroidal estrogens
10-12 angstroms
47
Use of OH at lower position in nonsteroidal estrogens
enhances activity
48
Name two non steroidal estrogens and their uses
Diethyl stilbestrol-prevents miscarriage, may cause adenocarcinoma in women exposed in utero Chlorotrianisene- Post partum breast engorgement
49
What is a SERM (agonist or antagonist?)
Partial agonist (blocks action of stronger estrogens)
50
Are SERMs estrogenic or antiestrgenic
Estrogenic in some and anti estrogenic in others
51
Action of helix 12
Vital for the recruitment of co-activators
52
action of helix 12 with an agonist
covers binding pocket and recruits co-activators.
53
How does SERM interact with helix 12? What effect does this have?
SERM has an extra long arm that stretches out of the binding pocket and interferes with docking of helix 12. No co activator recruitment.
54
Most common partial estrogen agonist(SERM)
Tamoxifen (prodrug, OH groups added invivo)
55
Anti estrogenic actions of tamoxifene
Treats breast cancer Prevents breast cancer in high risk women
56
Estrogenic actions of tamoxifene
Increases risk for thrombolic events prevents osteoporosis weak estrogen agonist at endometrial cells (stimulate endometrial growth and increases bleeding)
57
SERMS all end with
-ifene
58
Difference in action between raloxifene and tamoxifene
Raloxifene does not stimulate endometrial cells
59
SERM that does not end with -ifene
Clomiphene
60
Use of clomiphene
Increases LH and FSH secretion
61
How does clomiphene lead to the increase of LH and FSH secretion
inhibits negative estradiol feedback
62
What does clomiphene treat
poly cystic ovary syndrome
63
Adverse effect of clomiphene
Multiple births
64
difference between SERM and SERD
SERM is a partial agonist, so they still have estrogenic effect SERD is an antagonist.
65
Example of SERD drug
Fluvestrant
66
When are SERD drugs used over SERM
When resistance has been built up to SERM by breast cancer patients
67
Use of Aromatase enzyme
Catalyzes conversion of testosterone to 17B-estradiol
68
what are aromatase inhibitors used for
Block biosynthesis of estrogens
69
Why are aromatase inhibitors used for ovulation induction
aromatase inhibitors lower estrogen levels negative feedback is less FSH level increases. stimulates ovulation
70
aromatase inhibitors can be used to treat
gynecomastia

Therapeutics (46 decks)

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