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Pharmacology part B > Hormones > Flashcards

Hormones Flashcards

1
Q

classical pathway of hormones

A

released from cells then circulate the blood bound to sex hormone binding globulin. unbound enter cytoplasm of target tissue cells where they ind to the hormone recept which translocates to the nucleus and changes gene trasncription

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2
Q

potency of estrogen

A

E2 > E1 > E3

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3
Q

estrogen effects

A 
sexual maturation and growth 
development of endometrial lining 
maintain skin and blood vessels
decrease bone reabsorption 
alters liver 
enhances coagulability of blood 
induces synthesis of estrogen and progesterone receptors
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4
Q

progesterone is a precursor to

A

estrogens
androgens
adrenocortical steroids

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5
Q

progesterone effects

A

downregulat estrogen receptor and suppresses estrogenic stimulation of endometrium
induce maturation adn secretory changes in endometrium

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6
Q

what effects does progesterone metabolites have on the brain

A

anxiolytic and hypnotic effect

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7
Q

what receptor does progesterone antagonize and result

A

mineralcorticoid receptor

decrease sodium resorption and water retention

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8
Q

what is the hypothalamic pituitary gonadal axis responsible for in men and women

A

female - regulates menstrual cycle

male - regulate testosterone production and spermatogenesis

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9
Q

role of gonadotropin releasing hormone secreted from the hypothalmus

A

stimulates anterior pituitary to secrete LH and FSH which stimulate E and P formation in females and spermatogenesis and testosterone production in males

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10
Q

estrogen containing contraceptives are contraindicated in

A 
over 35 who smoke 
hypertension 
diabetes with severe vascular disease
history of stroke
migraines 
risk factors for CVD
breast, cervical, ovarian,endometrial cancer 
active liver disease
thromboembolic disorder 
pregnancy
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11
Q

what is the most important mecahnism of action of HC

A

suppression of gonadotropin secretion

dose dependent inhibition of ovulation

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12
Q

MOA of HC

A

inhibits development of dominant follicle by suppressing FSH
endometrail less suitable
thickening of cervical mucus
impair tube motility

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13
Q

reason for ethinyl sub to estradiol

A

inhibits first pass metabolism and increases potency

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14
Q

describe first generation progestins

A

affinity for progesterone androgen receptors

medium androgen activity

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15
Q

describe second generation progestins

A

increeased affinity for progestine and androgen receptors
strong androgen and anti-estrogen activity increases acne and weight gain
lower VTE risk?

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16
Q

describe third generation progestins

A

greater affinity for progesterone receptors
low androgen activity
higher VTE risk?

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17
Q

describe unclassfied progestins

A

bind primarly to progesterone receptors
anti-androgenic
higher VTE risk

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18
Q

first gen progestin example

A

norethindrone

ethynodiol diacetate

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19
Q

second gen progestin example

A

levonorgestrel

norgestrel

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20
Q

third gen progestin example

A

norgestimate

desogestrel

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21
Q

unclassified progestin example

A

ddrospirenone

cyproterone acetate

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22
Q

metabolism of ethinyl estradiol and progestins

A

first pass hepatic metabolism by CYP 3A4

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23
Q

benefits of oral contraceptives that arent well none

A 
treat PCOS 
reduce pelvic inflammatory disease
reduce ectopic pregnancoes 
improve endometriosis 
reduce risk of ovarian and endometrial  cancer
reduce benign breast disease 
prtective against colon cancer 
maintain bone mineral density 
decrease risk of fibroids
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24
Q

too much estrogen effects

A

nausea
breast tenderness
headache
bloatin

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25
Q

too little estrogen effects

A

spotting

breakthrough bleeding early cycle

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26
Q

too much progestin effects

A 
breast tenderness 
headache
fatigue
mood changes
bloating
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27
Q

too little progestin effects

A

breakthrough bleeding late cycle

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28
Q

too much androgen effects

A 
weight gain 
acne 
hhirsutism 
increased LDL 
decreased HDL
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29
Q

what is chloasma

A

irreversible darkening/pigmentation of facial skin exacerbated by sunlight

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30
Q

risks with hormonal contraception

A 
venous thromboembolism 
MI 
stroke 
gallbladder disease
breast cancer
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31
Q

medications which may cause contraceptive failure dur to induction of CYP enzymes

A 
anticonvulsants 
antifungals 
antibiotics 
HIV meds
st johns wort 
bile acid sequestrants
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32
Q

medications which may increase OC activity

A

CYP 3A4 inhibitors: fluconazole, grapefruit juice

vitamin C

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33
Q

what is effective birth control in obese women

A

ring

depo-provera

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34
Q

progestin on pill should be used in

A 
over 35 smokers
obese
migraine
thromboembolic or CV disease history 
post partum 
breast feeding 
endometriosis
35
Q

MOA of mini pill

A

thicken cervial mucus
lower FSH and LH peaks
alter endometrium
impair sperm motility

36
Q

depo provera MOA

A

suppresses ovulation

increase cervical mucus atrophy of endometrium

37
Q

side effect of depo provera

A 
headache 
weight gain 
decreased libido 
mood changes
decreased BMD
delay of ovulation 9 months after last dose
38
Q

do progestin products increase CV, stroke, MI, or VTE risk

A

no

39
Q

progestin only IUS MOA

A

decrease estrogen and progestron receptors and strong antiproliferative effect
weak foreign bod reaction
thickens cervical mucus

40
Q

drug interactiosn with IUS

A

no becuase local action

41
Q

side effecs of IUS

A

mood change
decreased libido
become amenorrheic

42
Q

when is fertility restored in IUS

A

after removal

43
Q

emergency contraception MOA

A

thickens cervical mucus
inhibits ovulation
alters endometrium

44
Q

mifepristone MOA

A

competitively binds to both progesterone receptors blocking the effects

45
Q

combo of misoprostol and mifepristone effective how many days after pregnnacy

A

50 days

46
Q

mistoprostol MOA

A

prostaglandin analogue

promotes contractions

47
Q

effects of mifepristone

A 
degenerates endometrium 
decrease embryo support
soften and dilate crevix
promote release of prostaglandins 
increase uterine contractions
48
Q

adverse effects of mifepristone

A 
vaginal bleeding 
abdominal pain 
cramping
nausea 
vomiting
diarrhea
49
Q

what is methotrexate used for in canada

A

ectopic pregnancies

50
Q

what are ovulation inducers and what are they used for

A

anti-estrogens

women with anovulatory cycles and polycystic ovarian syndrome

51
Q

what is clomiphene citrate

A

selective estrogen receptor modulator

52
Q

clomiphene citrate MOA

A

competitive inhibitor of estrogen receptors in hypothalamus

agonist and antagonist depending on target tissue

53
Q

what does clomiphene citrate do in the hypothalamus

A

inhibits negative estrogenic feedback, increases GnRH release causes growth of ovarian follicles with subsequent ovulation

54
Q

what is letrozole

A

an aromatase inhibitor

55
Q

letrozole MOA

A

blocks conversion of testosterone and androsteinedione to E2/E1 decreasing the negative estrogenic feedback at pituitary resulting in increased FSH output

56
Q

example of a gonadotropin releasing hormone agonist

A

leuprolide acetate

57
Q

uses of leuprolide acetate

A

endometriosis
uterine fibroids
advanced prostate cancer

58
Q

leuprolide MOA

A

interrupts normal pulsatile stimulation of GnRH receptors inhibiting FSH and Lh secretion thereby suppressing the production of estrogen and testosterone

59
Q

adverse effects of leuprolide acetate

A

menopausal symptoms

hot flashes

60
Q

define final menstrual period

A

12 months of amennorhea in women with a uterus that occurs between 45-58 years old

61
Q

abrupt menopause cause by

A

oophorectomy (remove ovaries)
radiation to pelvis
chemo

62
Q

premature menopause requires

A

hormone therapy until age 51

63
Q

when does perimenopause occur

A

2-8 years prior to final menstrual period

64
Q

what is the hypothesis of thermoregulatory dysfunction in menopause

A

disturbance in thermoneutral zone in hypothalamus

increased sensitivity to core body temp changes causes vasomotor symptoms

65
Q

cause of the narrowing of thermoneutral zone

A

elevated sympathetic activation through alpha 2 adrenergic receptors

66
Q

best treatment for menopausal symptoms

A

exogenous estrogen widens the thermoneutral zone

67
Q

common combo with systemic estrogen if uterus intact

A

progestogens to prevent hyperplasia and possible uterine cancer

68
Q

continuous regimen for menopause

A

estrogen and progestogen continuously

causes unpredictable bleeding

69
Q

sequential regimen for menopause

A

estrogen continuous
progestogen pulses for 10 days per month
causes predictable bleeding

70
Q

two types of progestogen used in post menopause

A

micronized progesterone or

medroxyprogesterone acetate

71
Q

what are vaginal estrogen therapries

A

local treatment of urogenital atrophy due to low estrogen levels that restores urogenital health in 3 months

72
Q

examples of selective estrogen receptor modulators

A

tamoxifen - breast cancer

raloxifene - osteoporosis

73
Q

where does tamoxifen act

A

antagonist in breast

agonist in endometrium and bone

74
Q

where does raloxifene act

A

antagonist at breast and endometrium

agonist at bone

75
Q

what does clomiphene do

A

ovulation inducer in fertility treatment
ER antagonist in hypothalamus
partial agonist in ovaries

76
Q

example of a selective progestin receptor modulator

A

ulipristal acetate

77
Q

use of selective progestin receptor modulator

A

treatment of moderat to severe signs of uterine fibroids in women eligible for surgery

78
Q

selective progestin receptor modulator MOA

A

prevents progesterone from binding to the PR

direct effect of endometrium and fibroids

79
Q

effect of selective progestin receptor modulator

A

reduces the size of uterine firoids by inhibiting cell proliferation adn inducing apoptosis
decreased bleeding
improved Hgb
decrease pain

80
Q

LH purpose in men

A

interacts with receptors on leydig cells in the testes to enhance testosterone synthesis

81
Q

FSH purpose in men

A

act on receptors in the sertoli cells in testes to regulate spermatogenesis
enhances synthesis of aromatase enzymes that converts testosterone to E2

82
Q

why do they say testosteron acts as 3 hormones

A

direct action affects lean muscle mass and strength
conversion to DHT amplifies action on external genitalia and sexual ahir
conversion to estradiol acts on bone, stimulates sexual function and decreases body fat

83
Q

symptoms of androgen deficiency

A 
low libido 
decreased morning erections 
loss of body hair 
low bone mineral density 
gynecomastia 
small testes

Pharmacology part B (17 decks)

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