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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
too little estrogen effects
spotting | breakthrough bleeding early cycle
26
too much progestin effects
``` breast tenderness headache fatigue mood changes bloating ```
27
too little progestin effects
breakthrough bleeding late cycle
28
too much androgen effects
``` weight gain acne hhirsutism increased LDL decreased HDL ```
29
what is chloasma
irreversible darkening/pigmentation of facial skin exacerbated by sunlight
30
risks with hormonal contraception
``` venous thromboembolism MI stroke gallbladder disease breast cancer ```
31
medications which may cause contraceptive failure dur to induction of CYP enzymes
``` anticonvulsants antifungals antibiotics HIV meds st johns wort bile acid sequestrants ```
32
medications which may increase OC activity
CYP 3A4 inhibitors: fluconazole, grapefruit juice | vitamin C
33
what is effective birth control in obese women
ring | depo-provera
34
progestin on pill should be used in
``` over 35 smokers obese migraine thromboembolic or CV disease history post partum breast feeding endometriosis ```
35
MOA of mini pill
thicken cervial mucus lower FSH and LH peaks alter endometrium impair sperm motility
36
depo provera MOA
suppresses ovulation | increase cervical mucus atrophy of endometrium
37
side effect of depo provera
``` headache weight gain decreased libido mood changes decreased BMD delay of ovulation 9 months after last dose ```
38
do progestin products increase CV, stroke, MI, or VTE risk
no
39
progestin only IUS MOA
decrease estrogen and progestron receptors and strong antiproliferative effect weak foreign bod reaction thickens cervical mucus
40
drug interactiosn with IUS
no becuase local action
41
side effecs of IUS
mood change decreased libido become amenorrheic
42
when is fertility restored in IUS
after removal
43
emergency contraception MOA
thickens cervical mucus inhibits ovulation alters endometrium
44
mifepristone MOA
competitively binds to both progesterone receptors blocking the effects
45
combo of misoprostol and mifepristone effective how many days after pregnnacy
50 days
46
mistoprostol MOA
prostaglandin analogue | promotes contractions
47
effects of mifepristone
``` degenerates endometrium decrease embryo support soften and dilate crevix promote release of prostaglandins increase uterine contractions ```
48
adverse effects of mifepristone
``` vaginal bleeding abdominal pain cramping nausea vomiting diarrhea ```
49
what is methotrexate used for in canada
ectopic pregnancies
50
what are ovulation inducers and what are they used for
anti-estrogens | women with anovulatory cycles and polycystic ovarian syndrome
51
what is clomiphene citrate
selective estrogen receptor modulator
52
clomiphene citrate MOA
competitive inhibitor of estrogen receptors in hypothalamus | agonist and antagonist depending on target tissue
53
what does clomiphene citrate do in the hypothalamus
inhibits negative estrogenic feedback, increases GnRH release causes growth of ovarian follicles with subsequent ovulation
54
what is letrozole
an aromatase inhibitor
55
letrozole MOA
blocks conversion of testosterone and androsteinedione to E2/E1 decreasing the negative estrogenic feedback at pituitary resulting in increased FSH output
56
example of a gonadotropin releasing hormone agonist
leuprolide acetate
57
uses of leuprolide acetate
endometriosis uterine fibroids advanced prostate cancer
58
leuprolide MOA
interrupts normal pulsatile stimulation of GnRH receptors inhibiting FSH and Lh secretion thereby suppressing the production of estrogen and testosterone
59
adverse effects of leuprolide acetate
menopausal symptoms | hot flashes
60
define final menstrual period
12 months of amennorhea in women with a uterus that occurs between 45-58 years old
61
abrupt menopause cause by
oophorectomy (remove ovaries) radiation to pelvis chemo
62
premature menopause requires
hormone therapy until age 51
63
when does perimenopause occur
2-8 years prior to final menstrual period
64
what is the hypothesis of thermoregulatory dysfunction in menopause
disturbance in thermoneutral zone in hypothalamus | increased sensitivity to core body temp changes causes vasomotor symptoms
65
cause of the narrowing of thermoneutral zone
elevated sympathetic activation through alpha 2 adrenergic receptors
66
best treatment for menopausal symptoms
exogenous estrogen widens the thermoneutral zone
67
common combo with systemic estrogen if uterus intact
progestogens to prevent hyperplasia and possible uterine cancer
68
continuous regimen for menopause
estrogen and progestogen continuously | causes unpredictable bleeding
69
sequential regimen for menopause
estrogen continuous progestogen pulses for 10 days per month causes predictable bleeding
70
two types of progestogen used in post menopause
micronized progesterone or | medroxyprogesterone acetate
71
what are vaginal estrogen therapries
local treatment of urogenital atrophy due to low estrogen levels that restores urogenital health in 3 months
72
examples of selective estrogen receptor modulators
tamoxifen - breast cancer | raloxifene - osteoporosis
73
where does tamoxifen act
antagonist in breast | agonist in endometrium and bone
74
where does raloxifene act
antagonist at breast and endometrium | agonist at bone
75
what does clomiphene do
ovulation inducer in fertility treatment ER antagonist in hypothalamus partial agonist in ovaries
76
example of a selective progestin receptor modulator
ulipristal acetate
77
use of selective progestin receptor modulator
treatment of moderat to severe signs of uterine fibroids in women eligible for surgery
78
selective progestin receptor modulator MOA
prevents progesterone from binding to the PR | direct effect of endometrium and fibroids
79
effect of selective progestin receptor modulator
reduces the size of uterine firoids by inhibiting cell proliferation adn inducing apoptosis decreased bleeding improved Hgb decrease pain
80
LH purpose in men
interacts with receptors on leydig cells in the testes to enhance testosterone synthesis
81
FSH purpose in men
act on receptors in the sertoli cells in testes to regulate spermatogenesis enhances synthesis of aromatase enzymes that converts testosterone to E2
82
why do they say testosteron acts as 3 hormones
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
symptoms of androgen deficiency
``` 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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