Gonadal hormones Flashcards
anastrozole
inhibits aromatase
- decrease effects of estrogen
ketoconazole
inhibits desmolase
letrozole
aromatase inhibitor
exemestane
aromatase inhibitor
fulvestrant
SERD
drospirennone
progestin
desogestrel
progestin
toremifene
SERM
clomiphene
SERM
norethindrone
progestin
norgestrel
progestin
mestranol
estrogen
nafarelin
GnRH analog
goserelin
GnRH analog
Ganirelix
GnRH anatagonist
mifepristone
antiprogestin
oxandrolone
androgen
stanozolol
androgen
fluoxymesterone
androgen
nandrolone
androgen
oxymetholone
androgen
danazol
androgen
finasteride
5-alpha reducatase inhibitor
flutamide
androgen receptor antagonist
bicalutamide
androgen receptor antagonist
nilutamide
androgen receptor antagonist
cyproterone
androgen receptor antagonist
spironolactone
androgen receptor antagonist
ketoconazole
steroid synthesis inhibitor
estradiol vs estrone vs estriol - which is most potent
estradiol
ethinyl estradiol MOA
stimulation of estrogen receptors = change rate of transcription
relies on P450
ethinyl estradiol use
prevent osteoporosis
HRT
OCP
hypogonadism
ethinyl estradiol AE
breakthrough bleeding thromboembolism gallbladder diz hyperTG HTN depression
post menopausal women: breast CA, endometrial hyperplasia
**pro-thrombotic drug - blocks AT3
taken with p450 inducer = breakthrough bleeding, dec contraceptive efficacy
mestranol
prodrug - converted to ethinyl estradiol
dietthlstilbestrol
nonsteroidal estrogen agonist used in pregnancy – can lead to infertility and vaginal cancer
estrogen esters
long acting estrogens - given IM and used for hypogonadism in young females
weekly patch
ethinyl estradiol + norelgestromin
monthly vaginal ring
ethinyl estradiol + etonogestrel
IUD
L-norgestrel
subcutaneous implant
etonogestrel
depot IM
medroxyprogesterone
postcoital contraceptive
L-norgestrel, combined oral contraceptive
tx for intractable dysmenorrhea
conjugated estrogens ethinyl estradiol OCP depot inejction GnRH agnoist
infertility tx
progesterone* clomiphene hMG and hCG GnRH analogs bromocriptine
endometriosis tx
OCP
depot injection
GnRH agonist
danazol
osteoporosis in postmenopausal women
conjugated estrogens
estradiol
raloxifene
hirsutism
combined OCP
spirinolactone
flutamide
GnRH agonist
progesterone functions
stimulate endometrial glandular secretion
pro-gestation
dec myometrial contraction
inc body temp
thick cervical mucus
prevent endometrial hyperplasia
norgestrel AE
weight gain
dec in bone density
low HDL, inc LDL, HTN
drospirenone
progestin of spironolactone derivative
tamoxifen
SERM - estrogen antag at breast and CNS. agonist in endometrium, liver and bone
tamoxifen AE
hot flush
thromboembolism
endometrial hyperplasia
raloxifene vs tamoxifene
protect against osteoporosis
antagonist effects in breast and CNS and endomterium
**bone density increases with raloxifene
clomiphene
induced ovulation
ER antagonist effect in pituitary = gonadotropin secretion increased
clomiphene AE
hyperstimulation of ovary = hypertrophy
multiple pregnancy
hot flush, n/v, weight gain
fulvestrant MOA
estrogen antagonist in all tissues = SERD
fulvestrant use
tx for hormone responsive breast CA that is resistant to first lines
IM admin
fulvestrant AE
hot flush, HA, injection site reactions
anastrozole MOA
inhibits aromatase = dec estrogen synthesis
anastrozole use
tx for hormone responsive breast CA
oral admin
anastrozole AE
musculoskeletal disorder, dec bone density, hot flushes
joint sxs: spondylosis, osteoarhtritis, disk herniation
letrozole
similar to anastrozole
exemestane
irreversible aromatase inhibitor
leuprolide use
ovarian suppresion control ovarian hyperstimulation central precocious puberty block endogenous puberty in transgender adv prostate cancer
Leuprolide AE
continued use - may show signs of hypogonadism
light headed, HA, nausea
GnRH analogs
goserelin histrelin nafarelin triptorelin gonadorelin
ganirelix MOA
GnRH antagonist
ganirelix use
prevention of premature LH surges during controlled ovulation hyperstimulation
cetrorelix
similar to ganirelix
degarelix
used for adv prostate CA
Danazol
partial agonist of progestin and androgen receptors
*p450 inhibtior
danazol use
endometriosis
fibrocystic breast
danazol AE
acne
hirsutism
weight gain
menstrual disturbance
mifepristone
antiprogestin
progestin and glucocorticoid blocker
mifepristone use
abortion
dihydrotestosterone vs testosterone vs androstenedione - potency?
DHT most potent
what drug is used for wasting syndromes?
testosterone - helps with weight gaining
oral testosterone
fluoxymesterone
methyltestosterone
long acting androgens for parenteral admins
testosterone esthers
finasteride use
BPH
male patterned hair loss
oral admin
finasteride AE
impotence
gynecomastia
dutasteride
similar to finasteride
flutamide MOA
competitive inhibition of androgen receptor
flutamide use
adv prostate cancer
flutamide AE
gynecomastia
hot flush
impotence
hepatotoxicity
bicalutamide
flutamide like - lower liver toxicity risk
nilutamide
flutamide like - lower liver toxicity risk
cyproterone
used in hirsutism and to decrease excessive sexual drive in men