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Therapeutics > Park lecture 3 > Flashcards

Park lecture 3 Flashcards

1
Q

Most important progestin in humans

A

Progesterone

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2
Q

What is an effect of progesterone being so featureless

A

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

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3
Q

Where is progesterone produced

A

ovary, testes, adrenal gland

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4
Q

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

A

Estrogen
Estrogen & progesterone

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5
Q

When are the two times progesterone is synthesized in large quantity

A

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

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6
Q

Why are synthetic progesterone’s used over progesterone?

A

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

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7
Q

How is progesterone inactivated inside the body?

A

Inactivated by hydrolysis of ketone

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8
Q

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

A

Pregnanediol, glucuronic acid

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9
Q

physiological effect of progesterone on menstruation cycle

A

Causes maturation of endometrium following ovulation

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10
Q

Metabolic effect of progesterone

A

Increase basal insulin levels and insulin response to glucose

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11
Q

effect of progesterone on glycogen storage

A

Increases glycogen storage in liver

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12
Q

Why do women gain weight during pregnancy

A

Because progesterone promotes storage of progesterone in liver

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13
Q

What does aldosterone do in the body

A

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

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14
Q

Relationship between progesterone and aldosterone

A

Progesterone binds to aldosterone receptor and antagonizes its function

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15
Q

Effect of progesterone on Na+ levels

A

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

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16
Q

Name 5 uses of Progesterone

A

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

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17
Q

Why is progesterone used in HRT in combination with estrogens

A

Progesterone decreases some adverse effects of estrogens

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18
Q

which hormone promotes endometrial growth, which hormone suppresses it

A

Estrogen promotes
progesterone suppresses

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19
Q

What addition to the structure of progestins would add oral activity

A

C17-a ethynyl moiety

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20
Q

What addition of structure is required for activity

A

C-18 Methyl or Ethyl are required for activity

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21
Q

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

A

C-17 B acetyl

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22
Q

Which substituents in progestins are used for oral preparations

A

17-b OH or esters

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23
Q

What substituent is essential for activity

A

Ketone at C3

24
Q

_______ alone is necessary for the growth of endometrium

A

Estrogen

25
Q

Introducing which hormone will not allow endometrium to grow fully.

A

Progesterone

26
Q

giving which hormone will stop menstrual cycle completely

A

progesterone

27
Q

1st generation progestin drug names

A

Norethindrone
Ethynodiol diacetate

28
Q

17 ethinyl group use?

A

Increases bioavailability

29
Q

replacement f 17-acetyl with OH use?

A

Increases bioavailability

30
Q

2nd gen drug names

A

Lenonorgestrel
Norgestimate

31
Q

Active isomer of norgestrel

A

Levonorgestrel

32
Q

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

A

Norgestimate

33
Q

3rd gen progestin drug names

A

Desogestrel
Etonogestrel

34
Q

Which 3rd gen drug is a prodrug

A

Desogestrel

35
Q

Desogestrel is rapidly metabolized to

A

Etonogestrel

36
Q

4th gen drug names

A

Drosperinone

37
Q

Which drug has weak progesterone activity

A

Progesterone

38
Q

which drug has antimineralcorticoid activity

A

drosperinone

39
Q

What drug negates side effects of ethynyl estradiol in combination therapy

A

drosperinone

40
Q

Which drug has antiandrogenic activities

A

Drosperinone

41
Q

Why do progestins frequently have androgenic effect?

A

They bind to androgen receptor due to dimilar structure as testosterone

42
Q

why do progestins frequently have hormonal activities other than progesteronic effects

A

Due to i/a with steroid receptors

43
Q

which progestin drug has powerful androgen effects

A

Lenonorgestrel

44
Q

Most commonly used combination of estrogen drugs

A

ethynyl estradiol and progestins

45
Q

Difference between monophasic vs diphasic & triphasic

A

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

46
Q

How is ovulation inhibited

A

By production of estrogens and progestins

47
Q

effect of oral contraceptive on uterus

A

Change in cervical mucus and in uterine endometrium

48
Q

How does oral contraception affect cervical mucus and uterine endometrium

A

Decrease in likelihood of conception and implantation

49
Q

effect of oral contraceptive on breast (combination only)

A

Stimulation of breasts and supression of lactation

50
Q

mild adverse effects of oral contraceptive (estrogenic)

A

HTN, nausea, edema, breast fullness

51
Q

mild adverse effects of oral contraceptives (progesterone)

A

increase in appetite, fatigue, breast regression

52
Q

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

A

Irregularity in menstruation

53
Q

What are some other moderate adverse effects of oral contraceptives

A

Amenorrhea
weight gain, acne, hirsutism

54
Q

severe adverse effects of oral contraceptive due to estrogen?

A

Venous thromboembolic disease

55
Q

severe adverse effects of oral contraceptives due to progestin

A

Myocardial infraction

Therapeutics (46 decks)

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