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Pharmacology > Gonadal Steroids > Flashcards

Gonadal Steroids Flashcards

0
Q

metabolism of natural estrogen

A

more rapid inactivation in liver

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1
Q

oral estrogen forms

A

ESTRADIOL
ETHYNIL ESTRADIOL
CONJ EQUINE ESTRADIOL

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2
Q

synthetic estrogen metabolism

A

less rapid degradation

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3
Q

binds mainly to SHBG

less to albumin

A

ESTRADIOL

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4
Q

bind extensively to albumin

A

ETHYNIL ESTRADIOL

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5
Q

distribution of oral estrogen

A

rapidly and extensively

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6
Q

responsible for the unwanted effects of estrogen such as increase in clotting factors and inc in plasma Triglycerides

A

ENTEROHEPATIC CIRCULATION

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7
Q

intramuscular estrogen

A

ESTRADIOL VALERATE

estrogen + straight chain fa

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8
Q

intramuscular estrogen advantage

A

prolonged half life

can be given on a weekly or monthly basis

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9
Q

lesser hepatic effects compared to orally admin

A

transdermal patch

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10
Q

greater systemic absorption which can produce systemic effects

A

vaginal administration

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11
Q

effects of estrogen on endometrium

A

proliferatove -> endometrial hyperplasia

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12
Q

effects of estrogen on cervical mucus

A

watery, mucoid, stretchable -Spinbarkeit

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13
Q

estrogen on mammary glands

A

stromal and ductal devt

pigmentation of nipples and areola

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14
Q

estrogen on adipose tissue

A

female distribution pattern

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15
Q

estrogen on bones

A

pubertal linear growth

epiphyseal closure

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16
Q

estrogen on liver

A

inc coagulation factors 2,7,9,10
dec protein C, S, antithrombin
inc binding proteins SHBG,TBG,CBG

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17
Q

estrogen on bile

A

inc cholesterol secretion
dec bile acid secretion
-inc formation of gallstones

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18
Q

estrogen on plasma lipids

A

⬆HDL
⬇️LDL
slight decrease in total serum cholesterol
inc TAG

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19
Q

estrogen on kidneys

A

Sodium and water retention

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20
Q

use of estrogen

A

replacement therapy

  • hypogonadism
  • menopause

contraception

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21
Q

deficiency in sex hormones and the ovaries are non functioning

A

Turner’s syndrome

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22
Q

most important progestin in humans

precursor of estrogens, androgens, adrenocortical steroids

A

PROGESTERONE

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23
Q

absorption of PROGESTERONE

A

rapid

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24
Q

hepatic metabolism of PROGESTERONE to

A

PREGNANEDIOL

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25
Q

PROGESTERONE is conjugated with

A

GLUCORONIC acid

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26
Q

effect of progesterone on reproductive tract

A

secretory endometrium
⬇️uterine contractility
thick, scanty cervical mucus

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27
Q

progesterone on breast

A

proliferation in acini

vs ESTROGEN on stroma and ducts

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28
Q

PROGESTERONE on plasma lipids

A

⬆️LDL

slight ⬇️HDL

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29
Q

PROGESTERONE on brain

A

resets hypothalamic thermostat- increase heat production

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30
Q

PROGESTERONE on HP function

A

⬇️GNRH pulse frequency➡️suppressed Gn release

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31
Q

synthetic progestins

A

C21 progestins- PREGNANES
19-nortestosterone derivatives- ESTRANES
19-nortestosterone derivatives- GONANES
spironolactone analog- DROSPIRENONE

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32
Q

most chemically and pharmacologically related to progesterone

A

C21 progestins - PREGNANES

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33
Q

pregnanes- HYDROXYPOGESTERONE CAPROATE admin

A

IM due to first pass hepatic metabolism

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34
Q

MPA MEDROXYPROGESTERONE ACETATE admin

A

oral- HRT
IM- every 3 months for contraception
SC- for contraception

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35
Q

19 NT derivatives- ESTRANES

A

NORETHINDRONE

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36
Q

major effect of NORETHINDRONE

A

from androgenic to progestational

- removal of carbon at position 19

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37
Q

strong antigonadotropic activity of NORETHINDRONE

A

⬆️ affinity to testosterone
suppress gonadotropin release
contraceptive effect

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38
Q

norethindrone AE

A

acne

hirsutism

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39
Q

19nt derivatives GONANES

a further modification of testosterone

A

LEVONORGESTREL

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40
Q

LEVONORGESTREL androgen activity

A

minimal or absent

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41
Q

LEVANOGESTREL moa

A

potent gonadotropin inhibitor

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42
Q

antimineralocorticoid

androgen receptor antagonist

A

spironolactone analog- DROSPIRENONE

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43
Q

effects on DROSPIRENONE

A

⬇️water retention and breast tenderness : bloated and painful
improves skin appearance

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44
Q

uses of progestins

A

hormone replacement therapy
❤️contraception-⬇️GnRH
endometriosis, dysmenorrhea tx
relief of hot flushes when estrogen is CI

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45
Q

WHI estrogen + progestin tx

higher incidence of

A

breast CA

heart attack, stroke, thromboembolism

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46
Q

WHI estrogen + progestin tx

lower incidence of

A

fracture

colorectal cancer

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47
Q

US FDA approved indications for estrogen-progestin therapy

A

treat vasomotor symptoms
menopausal genital atrophy- topical
prevention of osteoporosis- consider non estrogen tx

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48
Q

EP replacement therapy CI

A 
thromboembolic disorders
breast or endometrial neoplasms
hepatic or gallbladder disease
undiagnosed genital bleeding
DM
HPN
migraine
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49
Q

HRT regimens: cyclic

A

1st half: estrogen
2nd half: estrogen + progestin

drug free: menstrual bleeding

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50
Q

HRT regimen: Continuous

A

if symptomatic during estrogen free days
(-) uterus: estrogen only
(+) uterus: estrogen + progestin

51
Q

oral contraceptive types

A

combined estrogen + progestin
progestin only
emergency contraception

52
Q

COC mechanism of contraception

A

prevent ovulation-synergystic actions

53
Q

progestin in COC effect on hypothalamus

A

⬇️frequency of GnRH pulses

54
Q

effect of COC estrogen on pituitary

A

suppression of FSH release

-no maturation of graafian follicle

55
Q

COC progestin effect on pituitary

A

inhibition of estrogen- induced LH surge

56
Q

COC combo on pituitary

A

⬇️pituitary responsiveness to GnRH

57
Q

COC effects

A

prevent ovulation
produce thick cervical mucus
endometrial atrophy
altered tubal support

58
Q

high dose COC

A

> or equal to 50mcg ETHYNIL estradiol

59
Q

low dose COC

A

30-35 mcg

60
Q

very low dose COC

A

20-25 mcg

61
Q

monthly cycle COC

A
  • 21 days active pills + 7 days active pills

* 24 days active pills + 4 days inactive pills

62
Q

extended cycle COC

A

84 days active pills + 7 days inactive- quarterly menstrual periods

63
Q

no period COC

A

28 active pills per pack, no inactive pills

continuous intake

64
Q

fixed amount of estrogen and progestin

A

monophasic COC

65
Q

more closely approximates the estrogen progestin ratios that occur during the menstrual cycle

A

biphasic COC

66
Q

three dosage formulation that also mimics the menstrual cycle

A

triphasic COC

67
Q

doses vary 4x each 28 day treatment cycle

A

quadriphasic COC

68
Q

mild AE of COC

A 
nausea
mastalgia
edema
breakthrough bleeding
headache
69
Q

moderate COC AE

A

weight gain
hirsutism
amenorrhea
prolactinemia or prolactinoma

70
Q

severe COC AE

A 
venous thromboembolism
MI-obese, HPN, smokers
⬆️risk of stroke: women >35 
hepatic adenoma
gallbladder disease
breast cancer
71
Q

absolute CI to COC

A 
history 
carcinoma of the breast, female repro tract
abnormal undiagnosed vaginal bleeding
liver tumors or impaired fxn
pregnancy
72
Q

relative CI to COC

A

migraine
HPN
DM
cholestatic jaundice of pregnancy

73
Q

PROGESTIN only dose

A

28 day packs all active

74
Q

PROGESTIN only oral contraceptive effect

A

⬇️menstrual blood loss and cramps

75
Q

uses of PROGESTIN only

A

breastfeeding

CI estrogen- smokers,HPN,migraine

76
Q

PROGESTIN only AE

A

acne

irregular bleeding

77
Q

not recommended for long term contraception

A

EMERGENCY CONTRACEPTIVE PILLS

78
Q

emergency contraceptive forms

A

PROGESTIN only
SPRM- selective progesterone receptor modulator
Yuzpe regimen

79
Q

emergency contraceptive pill that contaisn LEVONORGESTEL

A

progestin only pills

80
Q

progestin only pills must be talen

A

within 72 hours of unprotected sex

81
Q

PLAN b otc dose

A

2 pills taken 12 hours apart within 3 days

82
Q

plan B one step OTC dose

A

single dose, greater compliance

83
Q

SPRM - Ella contains

A

ullipristal : partial agonist

84
Q

SPRM is effective for

A

5 days (120hours) after coitus

85
Q

SPRM dose

A

1 tab single dose

86
Q

YUZPE regimen contain

A

high dose estrogen + progestin pills : COC

87
Q

yuzpe regimen taken within

A

72 hours of unprotected coitus

88
Q

yuzpe regimen dose

A

2 doses 12 hours apart

89
Q

inge table contraceptives

A

MPA or medroxyprogesterone acetate

90
Q

MPA dosing

A

IM or SC. every 3 months

91
Q

MPA ae

A 
irregular spotting or bleeding
⬆️LDL
⬇️HDL
⬇️bone density
delayed return of ovulation
92
Q

transdermal contraceptive releases estrogen and progestin for

A

7 days

93
Q

transdermal contraceptive dosing

A

one patch per week for 3 weeks

no patch for 1 week&raquo_space; menstrual period

94
Q

subdermal implant : IMPLANON form

A

single 4 cm rod releases progestin

95
Q

IMPLANON is removed after

A

3 years

96
Q

intrauterine contraceptive MIRENA releases

A

LEVONORGESTREL for 5 years

97
Q

CVR: NUVARING contains

A

estrogen and progestin

98
Q

NUVARING is left in place for

A

3 weeks

99
Q

most of circulating testosterone is bound to

A

Sex hormone binding globulin or SHBG

100
Q

5 alpha reductase converts testosterone to

A

DHT

101
Q

aromatase converts testosterone to

A

ESTRADIOL

adipose tissues, liver hypothalamus

102
Q

DHT in males is responsible for

A 
puberty
inc activity of sebaceous glands 
inc lean body mass
inc skeletal muscle growth
closure of epiphysis
103
Q

androgens stimulate the secretion of

A

erythropoietin for rbC production

104
Q

Androgens decrease HDL levels, favoring

A

atherosclerosis

105
Q

oral androgens

A

ESTER FORM TESTOSTERONE UNDECANOATE

ALKYKL DERIVATIVE STANOZOLE

106
Q

parenteral androgen

A

ester form TESTOSTERONE CYPLONATE

alkyl derivative NANDROLONE

107
Q

preparation of androgen that exhibit prolonged absorption can be administered weekly

A

parenteral form of Androgen

108
Q

androgen prep that bypass first pass effect

A

trandermal Androgen

109
Q

by pass first effect,tablet is placed at incisor

A

Transbucca androgen

110
Q

transbuccal androgen is taken

A

12 hours apart

111
Q

uses of androgen

A

replacement therapy for male hypogonadism
protein anabolic agent
gynecologic disorders
androgen abuse in sports

112
Q

androgen in male hypogonadism

A

preferred prep is testosterone

restores or induces virillization

113
Q

DANAZOL causes

A

atrophy of lesion in endometriosis

114
Q

increases strength, aggressiveness, competitive edge are seen on

A

androgen use in sports

115
Q

ANDROGENS AE

A

masculinizing effects
hepatic
prostatic enlargement
decrease HDL, increased LDL

116
Q

selective estrogen receptor modulators have tissue selective effects

A

agonist - bone, liver

antagonist- breast and endometrium

117
Q

has both agonist and antagonist action

A

RALOXIFENE

118
Q

RALOXIfene use

A

prevent or treat osteoporosis

breast cancer prophylaxis

119
Q

RALPXIFENE

A

hot flushes
leg cramps
DVt

120
Q

ANASTROZOLE MOA

A

aromatase inhibitor

121
Q

FULVESTRANT MOA

A

estrogen receptor antagonist

122
Q

used for TAMOXIFEN resistant breast tumors

A

ANASTROZOLE

FULVESTRANT

123
Q

5 alpha reductase inhibitors

A

FINASTERIDE : type 2

DUTASTERIDE : type 1,2

124
Q

FINASTERIDE and DUTASTERIDE are used for

A

BPH

androgenic alopesia- FINASTERIDE

125
Q

moa of FLUTAMIDE

A

andorgen receptor antagonist

126
Q

FLUTAMIDE use

A

treatment of prostatic cancer

Pharmacology (8 decks)

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