Brainscape's Knowledge GenomeTM

Browse over 1 million classes created by top students, professors, publishers, and experts.


See full index

Therapeutics > Park lecture 2 > Flashcards

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.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

What cells produce estrogen

A

Granulosa cells

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

What produces both estrogen and progesterone

A

Corpus luteum

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

1st two weeks before ovulation is called

A

Follicular phase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Last two weeks after ovulation is called

A

luteal phase

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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)
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Explain what happens during early follicular phase

A

Estrogen suppresses the production of FSH

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Explain what happens during late follicular phase

A

Estrogen stimulates the surge of LH and FSH.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

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

A

Ovulation and formation of corpus luteum

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

What happens in luteal phase

A

Estrogen and progesterone suppress LH and FSH

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

What would happen if FSH levels are continuously high?

A

Another follicle could grow, leading to multiple eggs being released

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Remember the graphs for estrogen, progesterone, LH and FSH

A
How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Androstenedione acted on by aromatase will form

A

estrone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

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

A

Estrone

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

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

A

True

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
18
Q

Where is estrogen metabolized?
where is it excreted?

A

Metabolized in liver, excreted in urine.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
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.

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
21
Q

Endometrial effects of estrogen

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
22
Q

Effect of estrogen on bone

A

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

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
23
Q

Effect of estrogen on transcortin and SHBG

A

Stimulates synthesis

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
24
Q

Effects of estrogen on cholesterol levels

A

Increase HDL
Decrease LDL

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
25
Q

Effects of Estrogen on blood coagulation

A

Enhancement of blood coagulation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
26
Q

Effect of estrogen on CNS

A

affects mood

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
27
Q

consequences of enterohepatic circulation

A

high ratio of hepatic to peripheral effect

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
28
Q

4 clinical uses of estrogen

A

HRT in post menopausal women
Osteoporosis
Hormonal contraception
replacement therapy in patients with primary hypogonadism (ovary not functioning)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
29
Q

3 ways estrogen helps post menopausal women in hormone replacement therapy

A

Relief of CNS disturbances(hot flash, sweating)
Relief of symptoms resulting from urogenital atrophy (vaginal dryness)
relief from psychological effects (mood swings)

30
Q

List adverse effects of estrogen

A

uterine bleeding
breast cancer
endometrial carcinoma
Nausea, headache, fluid retention, weight gain

31
Q

What is the major cause of post menopausal uterine bleeding. Why?

A

Estrogen therapy
Due to endometrial hyperplasia

32
Q

What can we do to avoid post menopausal bleeding and endometrial carcinoma in estrogen therapy?

A

Administration of progestin

33
Q

Why does the use of progestin prevent uterine bleeding in estrogen therapy

A

In maturation phase of the menstrual cycle, estrogen and progesterone are produced together to help the maturation of endometrium.

34
Q

What is progestin?

A

An analog of progesterone

35
Q

What effect does progestin have on prevention of breast cancer in estrogen therapy?

A

No effect

36
Q

What are three required structural features in estrogenic cpds

A

Aromaticity in far left ring
17B-OH group
OH at 3 position

37
Q

Use of ether in estrogenic cpds at C3

A

Ethers can mask OH groups, which are readily hydrolyzed invivo

38
Q

16 OH on estrogenic cpd effect

A

Decrease activity

39
Q

Use of 17a-ethynyl substituent in estrogenic cpd

A

blocks metabolism and allows for oral activity

40
Q

Use of ester on 17B position

A

Can temporarily block OH group for drug delivery,

41
Q

how do 17 a-alkylated estrogens increase half life and enhance bioavailability

A

Prevent conversion to estrone

42
Q

effect of esterification on 17-B carbon? How will this change the administration of drug?

A

Decreases solubility of the drug, allows for a slower absorption from injection site (depot), less frequent injections

43
Q

in non-steroidal estrogens, what is the use of the far left amine substituted side?

A

Blocks helix-12 and leads to antagonist/serm activity

44
Q

What is required for agonist activity in non-steroidal estrogens

A

OH group in top right aromatic ring

45
Q

What is the purpose of the double bond in the middle of non steroidal estrogens?

A

Rigid core is needed to maintain proper space.

46
Q

What should the distance be between the two hydroxy groups in non steroidal estrogens

A

10-12 angstroms

47
Q

Use of OH at lower position in nonsteroidal estrogens

A

enhances activity

48
Q

Name two non steroidal estrogens and their uses

A

Diethyl stilbestrol-prevents miscarriage, may cause adenocarcinoma in women exposed in utero
Chlorotrianisene- Post partum breast engorgement

49
Q

What is a SERM (agonist or antagonist?)

A

Partial agonist (blocks action of stronger estrogens)

50
Q

Are SERMs estrogenic or antiestrgenic

A

Estrogenic in some and anti estrogenic in others

51
Q

Action of helix 12

A

Vital for the recruitment of co-activators

52
Q

action of helix 12 with an agonist

A

covers binding pocket and recruits co-activators.

53
Q

How does SERM interact with helix 12? What effect does this have?

A

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
Q

Most common partial estrogen agonist(SERM)

A

Tamoxifen (prodrug, OH groups added invivo)

55
Q

Anti estrogenic actions of tamoxifene

A

Treats breast cancer
Prevents breast cancer in high risk women

56
Q

Estrogenic actions of tamoxifene

A

Increases risk for thrombolic events
prevents osteoporosis
weak estrogen agonist at endometrial cells (stimulate endometrial growth and increases bleeding)

57
Q

SERMS all end with

A

-ifene

58
Q

Difference in action between raloxifene and tamoxifene

A

Raloxifene does not stimulate endometrial cells

59
Q

SERM that does not end with -ifene

A

Clomiphene

60
Q

Use of clomiphene

A

Increases LH and FSH secretion

61
Q

How does clomiphene lead to the increase of LH and FSH secretion

A

inhibits negative estradiol feedback

62
Q

What does clomiphene treat

A

poly cystic ovary syndrome

63
Q

Adverse effect of clomiphene

A

Multiple births

64
Q

difference between SERM and SERD

A

SERM is a partial agonist, so they still have estrogenic effect
SERD is an antagonist.

65
Q

Example of SERD drug

A

Fluvestrant

66
Q

When are SERD drugs used over SERM

A

When resistance has been built up to SERM by breast cancer patients

67
Q

Use of Aromatase enzyme

A

Catalyzes conversion of testosterone to 17B-estradiol

68
Q

what are aromatase inhibitors used for

A

Block biosynthesis of estrogens

69
Q

Why are aromatase inhibitors used for ovulation induction

A

aromatase inhibitors lower estrogen levels
negative feedback is less
FSH level increases.
stimulates ovulation

70
Q

aromatase inhibitors can be used to treat

A

gynecomastia

Therapeutics (46 decks)

Brainscape helps you reach your goals faster, through stronger study habits.
© 2024 Bold Learning Solutions. Terms and Conditions