Gonadal Flashcards
concept: Describe clinical presentation in 17 alpha-hydroxylase deficiency
decreasd androgens, cortisol
increased mineralcorticoids
XY - cryptorchidism and indistinct genitalia – give androgens, glucocorticoids and anti hypertensives
XX - outwardly female with normal internal but no secondary charcteristics — give estrogens and anti hypertensives
concept: 21 hydroxylase deficiency
decreased BP icnreased K, increased renin and volume depletion
pseudohermaphroditism in females
tx: fliuds, salt repletion and give cortisl to decreased ACTH
concept: 11 hydrozxylase deficiency
increased sex hormones, decreased cortisol and mineralcorticoids but increased 11 deoxycorticosterone
increased BP
overmasculinization
tx: estrogens and HTN (same as 11)
Which is the most potent: estriol, estrone, estradiol
estradiol because has the most letters
concept: effects of estronge on a) coagulation b) lipid profile c) hormone levels d) cholesterol
a) procoagulation state - increases II, VII, IX, X, XII and decreases antithrombin II, prot C and S
b) favours lipid profile
c) increases binding protein; free level fo hormone unaffected
d) increases cholesterol in bile - formation of gall stone
List the clinically used estrogens please
estradiol conjugated estrogen ethinyl estradoil quinestrol estrone
What is mestranol
prodrug converted to ethinyl estradiol (in some contraceptives)
Benefits of HRT please
reduced hot flashed
reudeced bone fracture and loss
decreased urogenital atrophy
A/se of HRT/estrogens
thromboembolism changes in lipid/carb metabolism increased risk of high bp increased incidence of breast and endometrial cnacers migraine cholestasis mood changes
What is Diethylstilbestrol (DES)?
a nonsteroidal estrogen agonist
‘‘des daughters’’
Name the absolute contraindications of estrogen use!!!
1) history of thromboembolism
2) breast and endometrial cancer
3) pregnancy
4) liver disease
Tamoxifen - repeat from boen
antag @ breat
ag @ bone
ag @ liver
ag @ endometrium
USED @ breast cancer treatment
a/se of tamoxifen
antag - hot flushes
ag - thrombosis
increased risk of endometrial cacners
Toremifene
used in metastatic breast cancer
Raloxifene
antag @ breast
ag @ bone
no effect @ endo
therefore, no increased risk of endometrial cancer, hurahh!!
Use of Raloxifene
prophylaxis vrs breast cancer in high risk patients
prevention fo osteoporosis
Name an estrogen receptor antagonist in all tissues
Fulvestrant
used of Fulvestrant
estrogen receptor antag
used @ breast cancer in tamoxifen resistant patients
a/se of fulvestrant
hot flushes
injection site reactions
headache
List the aromatase inhibitors
letrozole
anastrozole
exemestane - irreversible
Use of letrozole, anastrozole, exemestane
aromatase inhibitors
second line for breast cancer to tamoxifen
MOA Clomiphene
estrogen antag @ hypothalamus and anterior pituitary –> prevents feedback inhibito fo GnRh by hypothalamus –> continued release of GnRH from hypothalamus –> LH and FSH from pituitary –> ovulation
Uses of clomiphene
treatment of infertility
A/se of clomiphene
ovarian hyperstimulation syndrome
ovarian elargment
multiple pregnancy
visual disturbances
affect of progesterone on gallbladder…rando
decreases gall bladder contraction
effects of progesterone at high levels
suppresses gonadotropin secretion – anovulation
List the progestins
medroxyprogesterone and NORgestrel and NORethindrone
List the antiprogestins
mifepristone
SHARK flashback –> used to treat inoperable ectpoic ACTh syndrome (inhibits glucocorticoi and progesterone receptors)
List some newer preps with less androgenic effects than classic progesterones ( medroxyprogesterone, norgestrol and nor ethindrone)
desoGESTREL
norelGESTROmine
etonoGESTREL
norGESTimate
GESTROL - less like a gentlemen. . . .
What is DROSPIRENONE?
spironolactone ( aldosterone antaga with some anti androgenic activity)
used to treat acne in feamles
acne in females treatment
drospirenone - spironolactone derivaitive (hirsutism, aldosternoisn, diuretic) that antagonizes aldosterone
a/se progestins @ long term use
weight gain depression oedema acne decreasd HDL hypertension thrombophlebitis cholestatic juandice
Mifepristone MOA
competitive inhibitor of progesterone and glucocorticoids
uses of mifepristone
morning after pill - abortificant
inoperable ectopic ACTH syndrome
Danazol = ?
inhibitor P450 in gonadal steroid synthesis
partial agonist of progestin, androgen, glucocorticoids
Use of danazol
endometriosis
fibrocystic disease of breast
a/se danazol
parial agonist at progestin, andronge, glucocorticoids
hepatitis - abnormal liver function
since a modified androgen – masculizing effects ie acne (despiranone), hirsutism (spironolactone), menstrual distoruabcnes
which is more potent androstenedione, testosterone, DHT
DHT
Compare and contrast the actions of testosterone and DHT
testosterone:
- wolffian duct
- boen formation
- muscle growth
- spermatogenesis
VRS
DHT
- growth of external genitalia
- prostate growth
- scalp hair loss - remember jerrys story abotu this
- acne – OCP
- facial/body hair
List synthetic androgens please
-OLONE
oxandrolone stanozolol fluxymesterone** this one is bolded oxymetholone nandrolone OLONE
how can you use androgens to be clinically helpful?
hypogonasim
increase bone density
increase muscle mass (positive nitrogen balance)
some cases of aplastic anaemia
admin route of androgens
oxandrolon, stanozolol, fluxymesterone, oxymetholon, nandrolone
transdermal
IM
one bolded a/se of androgens
hepatic adenomas
List the androgen receptor antagonists
U-T-AMIDE
flutamide
bicalutamide
nilutamide
UTAMIDE
use of flutamide, bicalutamide, nilutamide
LUTAMIDE
used with GnRH analogs to decrease initial tumour flare ups of prostate carcinoma
Finasteride MOA
5 alpha reductase inhibitors –> inhibits conversion of testosterone to DHT
use of finasteride
BPH
promotes hair growth
a/se finasteride
gynecomastia and impotence
Ketoconazole
inhibits 17, 20 desmolase
(no gonadal no adrenal hormones)
cushing, prostate cancer
GnRH analogs list please
leuprolide
goserelin
nafarelin
continuous does of leuprolide, goserelin and nafarelin
down regulates GnRH receptors in pituiturat
Used of leuprolide, goserelin and nafarelin
prostate cancer
uterine fibroids
precocious puberty
list other drugs with anti androgenic action
spironlactone ( hirsutism, aldosternosim, diuretic)
cimetidine
cyproterone acetate
uses of : leuprolide and flutamide
flutamide (androgen receptor antag)
leuprolide (GnRH analog)
prostate cancer
Bicalutamide
a nonsteroidal antiandrogenic
prostate cancer
hirsutism
Nilutamide
used for prostate cance
SHARK: prostate cancer
leuprolide
flutamide
nilutamide
Spironolactone and cyropterone
hirsutism
BPH and male patterned baldness
finasteride (5alpha reductase inhibitor)
Ketoconazole
inhibits 17,20 desmolase
treats cushing and met prostati cancer.
How do finasteride and dutasteride help with benign prostatic hyperplasia?
5 alpha reductase inhibitors that decrease size of prostate
How do terazosin, doxazosin, tamsulosin, and alfuzosin help in BPH?
reduce tension fo prostatic smooth muscle in prostate, capsule, neck
