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PMCOL 343 > progestogen > Flashcards

progestogen Flashcards

1
Q

what is progesterone

A

the most important progestogen

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2
Q

what is the most important progestogen

A

progesterone

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3
Q

what is progestogen

A

class of steroid hormones that bind to and activate the progesterone receptor

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4
Q

what is the site of progesterone release in females

A
  • corpus luteum in 2nd part of menstrual cycle
  • placenta (pregnant)
  • small from adrenal gland
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5
Q

what is the site of progesterone release in males

A

testis and adrenal cortex

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6
Q

does progesterone bind to albumin

A

yes

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7
Q

does progesterone bind to SHBG

A

no

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8
Q

where is progesterone metabolized

A

in the liver

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9
Q

what pathway is progesterone in (mineralocorticoid, glucocorticoid or sex steroid)

A

mineralocorticoid actually!!!

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10
Q

what is the plasma half life of progesterone

A

5 mins actually

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11
Q

what are 3 main actions of progesterone in females

A
  • preperation for ovum implantation
  • negative feedback
  • thermogenic effect
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12
Q

how do progesterone prepare for ovum implantation

A
  • decrease estrogen endometrial proliferation
  • grow endometrial blood vessels
  • more viscous cervical mucus, less alkaline and less welcoming for sperm
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13
Q

what does progesterone do to estrogen-driven endometrial proliferation and how

A

decreases by stimulating differentiation, leading to the development of secretory endometrium

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14
Q

what does progesterone to do endometrial blood vessels

A

cause growth

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15
Q

what does progesterone to do cervical mucus (3)

A

makes it more viscous, less alkaline and less welcoming to sperm

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16
Q

what does progesterone to do negative feedback

A

reduces frequency of GnRH pulses

reduce gonadotrophin release from gonadotropes

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17
Q

what does progesterone to do GnRH pulses

A

reduces frequency of pulses from GnRH neurons

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18
Q

what does progesterone to do gonadotrophin release

A

reduce gonadotrophin release from gonadotropes

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19
Q

what does progesterone to do body temperature

A

increases it by 0.5 celcius

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20
Q

when does progesterone increase body temp

A

ovulating until the end of cycle

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21
Q

what is the mechanism of action of progesterone

A

progesterone receptors

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22
Q

what does progesterone do to male reproduction

A

no major effect

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23
Q

what does progesterone do to male mood

A

may cause aggression in rats towards infants

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24
Q

what are 3 therapeutic uses of progesterone

A

birth control, gynecological disorders, postmenopausal hormone replacement

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25
Q

how is progesterone used in birth control

A

either alone or with estrogen

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26
Q

how is progesterone used in gynecological disorders

A

dysmenorrhea and endometriosis

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27
Q

what is dysmenorrhea

A

painful cramps

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28
Q

how does progesterone help with dysmenorrhea

A

reduces estrogen induced contractions

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29
Q

how does progesterone help with endometriosis

A

oppose estrogen so less proliferation and bleeding and symptoms

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30
Q

how does progesterone help with postmenopausal hormone replacement

A

in combo with estrogen to prevent endometrial hyperplasia and reduce risk of endometrial carcinoma

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31
Q

what is the mechanism of action of antiprogesterone (mifepristone RU486)

A

competitive progesterone receptor antagonist

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32
Q

what happens if you administer antiprogesterone (mifepristone RU486) at early pregnancy

A
  • blockage of progesterone receptor in uterus leads to detachment of blastocyst
  • sensitize uterus to prostaglandins (contractions)
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33
Q

what does antiprogesterone (mifepristone RU486) sensitize the uterus to

A

prostaglandings

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34
Q

what does antiprogesterone (mifepristone RU486) do to ovulation (2 how)

A

inhibits

  • blocks graffian follicle growth
  • counteracts positive feedback action of estradiol on gonadotrophin release
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35
Q

what does antiprogesterone (mifepristone RU486) do to graffian follicle

A

inhibits growth

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36
Q

antiprogesterone (mifepristone RU486) gonadotrophin release

A

counteracts the positive feedback action of estradiol on gonadotrophin release

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37
Q

what does antiprogesterone (mifepristone RU486) do to secretory endometrium

A

impairs its development, discourages implantation

38
Q

what is a main use for antiprogesterone (mifepristone RU486)

A

termination of early pregnancy

39
Q

what happens with prostaglandins at the uterus

A

more contraction

40
Q

what is antiprogesterone (mifepristone RU486) often given with and when and why

A

a prostaglandin analogue 48 hours later (induces contraction and labour)

41
Q

how is antiprogesterone (mifepristone RU486) used as emergency contraception + how does it work

A

single low dose up to 120 hours after

inhibiting or delaying ovulation

42
Q

what is in the combined oral contraceptive pill

A

estradiol and progestogen

43
Q

what is a monophasic preperation

A

meaning there is the same hormone for each pill

44
Q

what is a tri or biphasic preperation

A

2 or 3 types of pills with different estrogen: progestin ratio

45
Q

what is the efficacy of combined pills

A

99%

46
Q

what are 5 beneficial effects of combined pill

A
  • decreased pregnancy and mother death
  • decrease iron deficiency anemia + PMS
  • less ovarian and endometrial cancer
  • less dysmenorrhea or irregularity
  • improved acne
47
Q

why is there less ovarian and endometrial cancer with combined pill

A

less gonadotrophin release

48
Q

why is there less acne with combined pill

A

inhibition of gonadotrophin release leads to reduction in androgen production

49
Q

what does the combined pill do to LH and FSH secretion

A

decrease

50
Q

what does decreased LH and FSH secretion from the combined pill cause

A

suppression of ovarian follicle development and prevention of ovulation

51
Q

what does progestogen do to cervical mucous and what does this cause

A

makes it thick so sperm cant penetrate

52
Q

what does progestogen do to endometrium and what does this cause

A

antiproliferative on endometrium to discourage implantation

53
Q

what are 2 main untoward effects of combined pill

A

vascular disorders and cancer

54
Q

what vascular disorders happen with combined pill

A

venous thrombosis, myocardial infarction, cerebrovascular disease

55
Q

who has the highest risk of vascular disorders with combined pill

A 
smokers
women over 35
obese
diabetic
long term users
56
Q

what cancers happen more with with combined pill

A

breast

57
Q

does breast cancer happen more with with combined pill

A

yes

58
Q

does cervical cancer happen more with with combined pill

A

no

59
Q

what GI disorders can happen with combined pill

A

small increase risk of cholestatic jaundice, gallbladder disease and hepatic adenoma

60
Q

what mental disorder can happen with combined pill

A

depression in 6%

61
Q

what skin disorders can happen with combined pill

A

skin pigmentation (darker)

62
Q

what can happen with combined pill to period

A

amenorrhea (if too much suppression)

63
Q

what can happen with combined pill to weight

A

gain due to androgenic effect of synthetic progestogen

64
Q

what can happen with combined pill to swelling

A

edema

65
Q

what can happen with combined pill to vaginal infection

A

increase

66
Q

what can happen with combined pill to head hurt

A

migraine wah

67
Q

when is progestogen only pill the drug of choice

A

with severe dysmenorrhea (and when estrogen use is undesirable)

68
Q

what are 3 disadvantages to progestogen only pill

A

must be taken daily
less reliable contraceptive
may cause irregular bleeding

69
Q

how can progestogen only or combined be used for emergency contraception

A

both act by preventing or delating mid cycle LH surge (negative feedback mechanism) to suppress ovulation

70
Q

what are selective progesterone receptor modulators

A

emergency contraception drugs

71
Q

are progestogen only or combined OR selective progesterone receptor modulators more effective as emergency contraception

A

selective progesterone receptor modulators

72
Q

how do selective progesterone receptor modulators work

A

block progesterone binding to receptors

73
Q

what do selective progesterone receptor modulators do to follicle and how

A

delays maturation (cause they need progesterone receptors)

74
Q

why is selective progesterone receptor modulators better than combined or prog only

A

because it can delay ovulation even on the day of the LH peak !! (thats too late for the other ones)

75
Q

can selective progesterone receptor modulators delay ovulation on the same day as LH peak

A

yeff

76
Q

can combined or prog only delay ovulation on the same day as LH peak

A

nope

77
Q

what are analogs of gonadotrophin releasing hormone

A

GnRH super-agonists or antagonists (substitution of specific amino acids in GnRH)

78
Q

what are benefits of GnRH analogs

A
  • increase degradation resistance
  • high GnRH receptor binding
  • longer receptor occupancy
  • more convenient routes of administration
79
Q

how often is endogenous GnRH released and from where

A

60-90 mins from hypothalamus

80
Q

what does continous high levels of GnRH cause

A

desensitization of pituitary GnRH receptors nd inhibition of gonadotrophin release

81
Q

what does it mean to be a GnRH super agonist

A

very high GnRH receptor binding affinity

82
Q

what is a therapeutic use of GnRH analogues

A

infertility in women

83
Q

how do you treat infertility in women

A

pulsatile GnRH and anti-estrogen (Clomiphene)

or

exogenous gonadotrophins + GnRH agonist or antagonist

84
Q

what happens when you use pulsatile GnRH and anti-estrogen (Clomiphene) together + why

A

more gonadotrophin secretion (Decrease negative feedback on gonadotropes) and stimulation of ovulation

85
Q

what 2 things happen with exogenous gonadotrophin use for infertility

A

longer ovarian stimulation so increase # of mature follicles

86
Q

what happens when you use continuous GnRH agonist or GnRH antagonist

A

less endogenous gonadotrophin secretion so less risk of premature endogenous LH surge (more mature follicles, increase fertility)

87
Q

how do you do male contraception

A

continous GnRH agonist or antagonist in conjunction with testosterone

88
Q

ia T alone or with GnRH more effective for contraception

A

together

89
Q

what is good post partum contraceptive + why

A

GnRH analogues (because clots are v common after giving birth)

90
Q

is GnRH anaogue safe for baby in milk

A

yes cause the analogue has no biological activity in milk

91
Q

what are some other uses of GnRH anaglues

A

suppress hormone levels, like

  • prostate cancer
  • breast cancer
  • endometriosis
  • uterine fibroids
  • hirsutism
  • children with GnRH dependent precocious puberty

PMCOL 343 (31 decks)

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