Park lecture 3

Question 1

Most important progestin in humans

Answer 1

Progesterone

Question 2

What is an effect of progesterone being so featureless

Answer 2

All other hormones can be synthesized from progesterone, but due to this there will be some cross reactivity.

Question 3

Where is progesterone produced

Answer 3

ovary, testes, adrenal gland

Question 4

during follicular phase only_________ is produced. During Luteal phase, _________&__________ is produced

Answer 4

Estrogen
Estrogen & progesterone

Question 5

When are the two times progesterone is synthesized in large quantity

Answer 5

Large quantities of progesterone is synthesized by corpus luteum in luteal phase and placenta during pregnancy

Question 6

Why are synthetic progesterone’s used over progesterone?

Answer 6

Half life of progesterone is 5 minutes (that is why synthetic progestins are used)

Question 7

How is progesterone inactivated inside the body?

Answer 7

Inactivated by hydrolysis of ketone

Question 8

When progesterone is excreted in urine, it is converted into______ and conjugated with______

Answer 8

Pregnanediol, glucuronic acid

Question 9

physiological effect of progesterone on menstruation cycle

Answer 9

Causes maturation of endometrium following ovulation

Question 10

Metabolic effect of progesterone

Answer 10

Increase basal insulin levels and insulin response to glucose

Question 11

effect of progesterone on glycogen storage

Answer 11

Increases glycogen storage in liver

Question 12

Why do women gain weight during pregnancy

Answer 12

Because progesterone promotes storage of progesterone in liver

Question 13

What does aldosterone do in the body

Answer 13

Increases the amount of Na+ reuptake, increasing the amount of water retained.

Question 14

Relationship between progesterone and aldosterone

Answer 14

Progesterone binds to aldosterone receptor and antagonizes its function

Question 15

Effect of progesterone on Na+ levels

Answer 15

Since progesterone antagonizes aldosterone, Na+ levels will decrease in the body.

Question 16

Name 5 uses of Progesterone

Answer 16

-Hormonal contraception
-HRT in combination with estrogen
-Endometriosis prevention
-Dysmenorrhea
-bleeding disorders

Question 17

Why is progesterone used in HRT in combination with estrogens

Answer 17

Progesterone decreases some adverse effects of estrogens

Question 18

which hormone promotes endometrial growth, which hormone suppresses it

Answer 18

Estrogen promotes
progesterone suppresses

Question 19

What addition to the structure of progestins would add oral activity

Answer 19

C17-a ethynyl moiety

Question 20

What addition of structure is required for activity

Answer 20

C-18 Methyl or Ethyl are required for activity

Question 21

Which substitution in progestins has the highest activity but poor oral availability

Answer 21

C-17 B acetyl

Question 22

Which substituents in progestins are used for oral preparations

Answer 22

17-b OH or esters

Question 23

What substituent is essential for activity

Answer 23

Ketone at C3

Question 24

_______ alone is necessary for the growth of endometrium

Answer 24

Estrogen

Question 25

Introducing which hormone will not allow endometrium to grow fully.

Answer 25

Progesterone

Question 26

giving which hormone will stop menstrual cycle completely

Answer 26

progesterone

Question 27

1st generation progestin drug names

Answer 27

Norethindrone Ethynodiol diacetate

Question 28

17 ethinyl group use?

Answer 28

Increases bioavailability

Question 29

replacement f 17-acetyl with OH use?

Answer 29

Increases bioavailability

Question 30

2nd gen drug names

Answer 30

Lenonorgestrel Norgestimate

Question 31

Active isomer of norgestrel

Answer 31

Levonorgestrel

Question 32

What drug is a pro drug that is converted into levonorgestrel invivo

Answer 32

Norgestimate

Question 33

3rd gen progestin drug names

Answer 33

Desogestrel Etonogestrel

Question 34

Which 3rd gen drug is a prodrug

Answer 34

Desogestrel

Question 35

Desogestrel is rapidly metabolized to

Answer 35

Etonogestrel

Question 36

4th gen drug names

Answer 36

Drosperinone

Question 37

Which drug has weak progesterone activity

Answer 37

Progesterone

Question 38

which drug has antimineralcorticoid activity

Answer 38

drosperinone

Question 39

What drug negates side effects of ethynyl estradiol in combination therapy

Answer 39

drosperinone

Question 40

Which drug has antiandrogenic activities

Answer 40

Drosperinone

Question 41

Why do progestins frequently have androgenic effect?

Answer 41

They bind to androgen receptor due to dimilar structure as testosterone

Question 42

why do progestins frequently have hormonal activities other than progesteronic effects

Answer 42

Due to i/a with steroid receptors

Question 43

which progestin drug has powerful androgen effects

Answer 43

Lenonorgestrel

Question 44

Most commonly used combination of estrogen drugs

Answer 44

ethynyl estradiol and progestins

Question 45

Difference between monophasic vs diphasic & triphasic

Answer 45

Monophasic indicates progesterone levels are constant throughout all 21 days, while biphasic and triphasic increases weekly

Question 46

How is ovulation inhibited

Answer 46

By production of estrogens and progestins

Question 47

effect of oral contraceptive on uterus

Answer 47

Change in cervical mucus and in uterine endometrium

Question 48

How does oral contraception affect cervical mucus and uterine endometrium

Answer 48

Decrease in likelihood of conception and implantation

Question 49

effect of oral contraceptive on breast (combination only)

Answer 49

Stimulation of breasts and supression of lactation

Question 50

mild adverse effects of oral contraceptive (estrogenic)

Answer 50

HTN, nausea, edema, breast fullness

Question 51

mild adverse effects of oral contraceptives (progesterone)

Answer 51

increase in appetite, fatigue, breast regression

Question 52

What is a moderate adverse effect of oral contraception more common in progesterone only contraceptive

Answer 52

Irregularity in menstruation

Question 53

What are some other moderate adverse effects of oral contraceptives

Answer 53

Amenorrhea weight gain, acne, hirsutism

Question 54

severe adverse effects of oral contraceptive due to estrogen?

Answer 54

Venous thromboembolic disease

Question 55

severe adverse effects of oral contraceptives due to progestin

Answer 55

Myocardial infraction