Gonadal Steroids Flashcards
(127 cards)
0
Q
metabolism of natural estrogen
A
more rapid inactivation in liver
1
Q
oral estrogen forms
A
ESTRADIOL
ETHYNIL ESTRADIOL
CONJ EQUINE ESTRADIOL
2
Q
synthetic estrogen metabolism
A
less rapid degradation
3
Q
binds mainly to SHBG
less to albumin
A
ESTRADIOL
4
Q
bind extensively to albumin
A
ETHYNIL ESTRADIOL
5
Q
distribution of oral estrogen
A
rapidly and extensively
6
Q
responsible for the unwanted effects of estrogen such as increase in clotting factors and inc in plasma Triglycerides
A
ENTEROHEPATIC CIRCULATION
7
Q
intramuscular estrogen
A
ESTRADIOL VALERATE
estrogen + straight chain fa
8
Q
intramuscular estrogen advantage
A
prolonged half life
can be given on a weekly or monthly basis
9
Q
lesser hepatic effects compared to orally admin
A
transdermal patch
10
Q
greater systemic absorption which can produce systemic effects
A
vaginal administration
11
Q
effects of estrogen on endometrium
A
proliferatove -> endometrial hyperplasia
12
Q
effects of estrogen on cervical mucus
A
watery, mucoid, stretchable -Spinbarkeit
13
Q
estrogen on mammary glands
A
stromal and ductal devt
pigmentation of nipples and areola
14
Q
estrogen on adipose tissue
A
female distribution pattern
15
Q
estrogen on bones
A
pubertal linear growth
epiphyseal closure
16
Q
estrogen on liver
A
inc coagulation factors 2,7,9,10
dec protein C, S, antithrombin
inc binding proteins SHBG,TBG,CBG
17
Q
estrogen on bile
A
inc cholesterol secretion
dec bile acid secretion
-inc formation of gallstones
18
Q
estrogen on plasma lipids
A
⬆HDL
⬇️LDL
slight decrease in total serum cholesterol
inc TAG
19
Q
estrogen on kidneys
A
Sodium and water retention
20
Q
use of estrogen
A
replacement therapy
- hypogonadism
- menopause
contraception
21
Q
deficiency in sex hormones and the ovaries are non functioning
A
Turner’s syndrome
22
Q
most important progestin in humans
precursor of estrogens, androgens, adrenocortical steroids
A
PROGESTERONE
23
Q
absorption of PROGESTERONE
A
rapid
24
hepatic metabolism of PROGESTERONE to
PREGNANEDIOL
25
PROGESTERONE is conjugated with
GLUCORONIC acid
26
effect of progesterone on reproductive tract
secretory endometrium
⬇️uterine contractility
thick, scanty cervical mucus
27
progesterone on breast
proliferation in acini
| vs ESTROGEN on stroma and ducts
28
PROGESTERONE on plasma lipids
⬆️LDL
| slight ⬇️HDL
29
PROGESTERONE on brain
resets hypothalamic thermostat- increase heat production
30
PROGESTERONE on HP function
⬇️GNRH pulse frequency➡️suppressed Gn release
31
synthetic progestins
C21 progestins- PREGNANES
19-nortestosterone derivatives- ESTRANES
19-nortestosterone derivatives- GONANES
spironolactone analog- DROSPIRENONE
32
most chemically and pharmacologically related to progesterone
C21 progestins - PREGNANES
33
pregnanes- HYDROXYPOGESTERONE CAPROATE admin
IM due to first pass hepatic metabolism
34
MPA MEDROXYPROGESTERONE ACETATE admin
oral- HRT
IM- every 3 months for contraception
SC- for contraception
35
19 NT derivatives- ESTRANES
NORETHINDRONE
36
major effect of NORETHINDRONE
from androgenic to progestational
| - removal of carbon at position 19
37
strong antigonadotropic activity of NORETHINDRONE
⬆️ affinity to testosterone
suppress gonadotropin release
contraceptive effect
38
norethindrone AE
acne
| hirsutism
39
19nt derivatives GONANES
| a further modification of testosterone
LEVONORGESTREL
40
LEVONORGESTREL androgen activity
minimal or absent
41
LEVANOGESTREL moa
potent gonadotropin inhibitor
42
antimineralocorticoid
| androgen receptor antagonist
spironolactone analog- DROSPIRENONE
43
effects on DROSPIRENONE
⬇️water retention and breast tenderness : bloated and painful
improves skin appearance
44
uses of progestins
hormone replacement therapy
❤️contraception-⬇️GnRH
endometriosis, dysmenorrhea tx
relief of hot flushes when estrogen is CI
45
WHI estrogen + progestin tx
| higher incidence of
breast CA
| heart attack, stroke, thromboembolism
46
WHI estrogen + progestin tx
| lower incidence of
fracture
| colorectal cancer
47
US FDA approved indications for estrogen-progestin therapy
treat vasomotor symptoms
menopausal genital atrophy- topical
prevention of osteoporosis- consider non estrogen tx
48
EP replacement therapy CI
```
thromboembolic disorders
breast or endometrial neoplasms
hepatic or gallbladder disease
undiagnosed genital bleeding
DM
HPN
migraine
```
49
HRT regimens: cyclic
1st half: estrogen
2nd half: estrogen + progestin
drug free: menstrual bleeding
50
HRT regimen: Continuous
if symptomatic during estrogen free days
(-) uterus: estrogen only
(+) uterus: estrogen + progestin
51
oral contraceptive types
combined estrogen + progestin
progestin only
emergency contraception
52
COC mechanism of contraception
prevent ovulation-synergystic actions
53
progestin in COC effect on hypothalamus
⬇️frequency of GnRH pulses
54
effect of COC estrogen on pituitary
suppression of FSH release
| -no maturation of graafian follicle
55
COC progestin effect on pituitary
inhibition of estrogen- induced LH surge
56
COC combo on pituitary
⬇️pituitary responsiveness to GnRH
57
COC effects
prevent ovulation
produce thick cervical mucus
endometrial atrophy
altered tubal support
58
high dose COC
> or equal to 50mcg ETHYNIL estradiol
59
low dose COC
30-35 mcg
60
very low dose COC
20-25 mcg
61
monthly cycle COC
* 21 days active pills + 7 days active pills
| * 24 days active pills + 4 days inactive pills
62
extended cycle COC
84 days active pills + 7 days inactive- quarterly menstrual periods
63
no period COC
28 active pills per pack, no inactive pills
| continuous intake
64
fixed amount of estrogen and progestin
monophasic COC
65
more closely approximates the estrogen progestin ratios that occur during the menstrual cycle
biphasic COC
66
three dosage formulation that also mimics the menstrual cycle
triphasic COC
67
doses vary 4x each 28 day treatment cycle
quadriphasic COC
68
mild AE of COC
```
nausea
mastalgia
edema
breakthrough bleeding
headache
```
69
moderate COC AE
weight gain
hirsutism
amenorrhea
prolactinemia or prolactinoma
70
severe COC AE
```
venous thromboembolism
MI-obese, HPN, smokers
⬆️risk of stroke: women >35
hepatic adenoma
gallbladder disease
breast cancer
```
71
absolute CI to COC
```
history
carcinoma of the breast, female repro tract
abnormal undiagnosed vaginal bleeding
liver tumors or impaired fxn
pregnancy
```
72
relative CI to COC
migraine
HPN
DM
cholestatic jaundice of pregnancy
73
PROGESTIN only dose
28 day packs all active
74
PROGESTIN only oral contraceptive effect
⬇️menstrual blood loss and cramps
75
uses of PROGESTIN only
breastfeeding
| CI estrogen- smokers,HPN,migraine
76
PROGESTIN only AE
acne
| irregular bleeding
77
not recommended for long term contraception
EMERGENCY CONTRACEPTIVE PILLS
78
emergency contraceptive forms
PROGESTIN only
SPRM- selective progesterone receptor modulator
Yuzpe regimen
79
emergency contraceptive pill that contaisn LEVONORGESTEL
progestin only pills
80
progestin only pills must be talen
within 72 hours of unprotected sex
81
PLAN b otc dose
2 pills taken 12 hours apart within 3 days
82
plan B one step OTC dose
single dose, greater compliance
83
SPRM - Ella contains
ullipristal : partial agonist
84
SPRM is effective for
5 days (120hours) after coitus
85
SPRM dose
1 tab single dose
86
YUZPE regimen contain
high dose estrogen + progestin pills : COC
87
yuzpe regimen taken within
72 hours of unprotected coitus
88
yuzpe regimen dose
2 doses 12 hours apart
89
inge table contraceptives
MPA or medroxyprogesterone acetate
90
MPA dosing
IM or SC. every 3 months
91
MPA ae
```
irregular spotting or bleeding
⬆️LDL
⬇️HDL
⬇️bone density
delayed return of ovulation
```
92
transdermal contraceptive releases estrogen and progestin for
7 days
93
transdermal contraceptive dosing
one patch per week for 3 weeks
| no patch for 1 week >> menstrual period
94
subdermal implant : IMPLANON form
single 4 cm rod releases progestin
95
IMPLANON is removed after
3 years
96
intrauterine contraceptive MIRENA releases
LEVONORGESTREL for 5 years
97
CVR: NUVARING contains
estrogen and progestin
98
NUVARING is left in place for
3 weeks
99
most of circulating testosterone is bound to
Sex hormone binding globulin or SHBG
100
5 alpha reductase converts testosterone to
DHT
101
aromatase converts testosterone to
ESTRADIOL
| adipose tissues, liver hypothalamus
102
DHT in males is responsible for
```
puberty
inc activity of sebaceous glands
inc lean body mass
inc skeletal muscle growth
closure of epiphysis
```
103
androgens stimulate the secretion of
erythropoietin for rbC production
104
Androgens decrease HDL levels, favoring
atherosclerosis
105
oral androgens
ESTER FORM TESTOSTERONE UNDECANOATE
| ALKYKL DERIVATIVE STANOZOLE
106
parenteral androgen
ester form TESTOSTERONE CYPLONATE
| alkyl derivative NANDROLONE
107
preparation of androgen that exhibit prolonged absorption can be administered weekly
parenteral form of Androgen
108
androgen prep that bypass first pass effect
trandermal Androgen
109
by pass first effect,tablet is placed at incisor
Transbucca androgen
110
transbuccal androgen is taken
12 hours apart
111
uses of androgen
replacement therapy for male hypogonadism
protein anabolic agent
gynecologic disorders
androgen abuse in sports
112
androgen in male hypogonadism
preferred prep is testosterone
| restores or induces virillization
113
DANAZOL causes
atrophy of lesion in endometriosis
114
increases strength, aggressiveness, competitive edge are seen on
androgen use in sports
115
ANDROGENS AE
masculinizing effects
hepatic
prostatic enlargement
decrease HDL, increased LDL
116
selective estrogen receptor modulators have tissue selective effects
agonist - bone, liver
| antagonist- breast and endometrium
117
has both agonist and antagonist action
RALOXIFENE
118
RALOXIfene use
prevent or treat osteoporosis
| breast cancer prophylaxis
119
RALPXIFENE
hot flushes
leg cramps
DVt
120
ANASTROZOLE MOA
aromatase inhibitor
121
FULVESTRANT MOA
estrogen receptor antagonist
122
used for TAMOXIFEN resistant breast tumors
ANASTROZOLE
| FULVESTRANT
123
5 alpha reductase inhibitors
FINASTERIDE : type 2
| DUTASTERIDE : type 1,2
124
FINASTERIDE and DUTASTERIDE are used for
BPH
| androgenic alopesia- FINASTERIDE
125
moa of FLUTAMIDE
andorgen receptor antagonist
126
FLUTAMIDE use
treatment of prostatic cancer
