Gonad hormones Flashcards
gonadorelin (GnRH)
pulasatile release stimulates pituitary gonadotrophs to release LH and FSH
sustained non pulse inhibits LH and FSH release
synthetic GnRH
leuprolide
GnRH analog (modified peptide = longer HL)
goserelin
GnRH analog (modified peptide = longer HL)
nafarelin
GnRH analog (modified peptide = longer HL)
ganirelix
GnRH antagonist
same goes for all the other relix drugs
urofillotropin
gonadotropin (FSH) analog
found in urine of post men women
fillotropin alfa
gonadotropin (FSH) analog
recombinant
lutropin alfa
gonadotropin (LH) analog
recombinant
chorionic gonadotropin (hCG)
gonadotropin
- produced by placenta (LH >> FSH)
- Can activate both LH and FSH receptors but the LH activity is much stronger
- Can be used to stimulate ovulation and spermatogenesis but mostly its going to make steroid hormones (LH)
- made by placenta
- Can activate both LH and FSH receptors but the LH activity is much stronger
choriogonadotropin alfa
gonadotropin
- produced by placenta (LH >> FSH)
- Can activate both LH and FSH receptors but the LH activity is much stronger
- Can be used to stimulate ovulation and spermatogenesis but mostly its going to make steroid hormones (LH)
- recombinant
- Can activate both LH and FSH receptors but the LH activity is much stronger
menotropins (hMG)
gonadotropin
- FSH and LH activity (full FSH and LH - does both equally )
- Human menopausal gonadotropin (hMG)
Estradiol (E2)
natural estrogen
major product of the ovary
Estrone (E1)
natural estrogen
estriol (E3)
natural estrogen
estropitate
natural purified crystalized estrone
estrogen cypionate
natural estrogen
metabolically resistant prohormones with improved bioavilability and HL
conjugated estrogens
natural estrogen
- Equine (derived from horses) estrogen sulfate sodium salts blended to standardized activity
- High potency
- These are technically natural - but they are natural for horses
ethinyl estradiol
syntehtic estrogen
- Undergoes extensive hepatic metabolism
- More active than natrual estronges
- Common in oral contraceptives
diethystibestrol
estrogen
diethystibestrol (DES)
synthetic estrogen
- Was used to prevent preg complications - but cuased a variety of complications in exposed famale offspring
- Carcinoma of vagina amoung other things
- DES daughters - may have to ask women if their mothers were exposed to this drug
esterified estrogens
estrogen
progesterone
progestin
antiestrogenic
antimineralocorticoid
IM
medroxyprogesterone
progestin
androgenic
antiestrogenic
PO or IM
norethindrone
progestin
1st gen analog
androgenic
antiestrogenic
anabolic
PO
levonorgestrel
progestin
plan B
2nd gen
androgenic
antiestrogenic
anabolic
PO
desogestrol
progestin
3rd gen
little other effects - the cleanest progestin we have
PO
drospirenone
progestin
estrogenic
antimineralocorticoid
PO
tamoxifen
SERM
used in breast cancer
toremifine
SERM - partial agonist partial antagonist
used in breast cancer
raloxifene
SERM
used in osteoporosis
bazedoxefine
SERM
used for relieving men symptoms - in combo with conjugated estrogens
clomiphene
SERM
ovulation induction
increases LH and FSH release by blocking negative feedback by estrogen
this is an oral drug - women who are trying to get preg may try this before some other treatments (hCG) - becuase its easyer to take
fulvestrant
estrogen antagonist
used in tamoxifen resistant breast cancer
mefipristone
RU486
- Post coital contraceptive
- Abortifacient in combination with misprostol or PGE1 - basically don’t support the pregnancy and expels the conceived embryo
- Also a glucorticoid antagonist
anatrozole
aromatase inhibitor (blocks the last enzyme in the path to produce estrogen)
non steroidal
letrozole
aromatase inhibitor (blocks the last enzyme in the path to produce estrogen)
non steroidal
exemestane
aromatase inhibitor (blocks the last enzyme in the path to produce estrogen)
steroidal
irreversible - long lasting
danazol
other estrogen and progesterone inhibitors
used to suppress ovarian function
testosterone
androgen
1:1 androgen:anabolic activity
methyltestosterone
androgen
1:1 androgen:anabolic activity
oral
fluoxymestrone
androgen
1:2 androgen:anabolic activity
oral
oxandrolone
androgen
1:13 androgen:anabolic activity
most anabolic that we have
the illegal ones are more anabolic
oral
testosterone cypionate
androgen
testosterone esters
1:1 androgen:anabolic activity
IM
ketoconazole
Steroid synthesis inhibitor
used for prostate cancer and men with excess testosterone secretion
inhibits gonadal steroid synth - increases estrogen: testosterone ratio -> gynecomastia
abiraterone
Steroid synthesis inhibitor
used for prostate cancer and men with excess testosterone secretion
17a-hydroxylase inhibitor
finasteride
Steroid synthesis inhibitor
used for prostate cancer and men with excess testosterone secretion
5a-hydroxylase inhibitor - decreased DHT
dutasteride
Steroid synthesis inhibitor
used for prostate cancer and men with excess testosterone secretion
5a-hydroxylase inhibitor
long HL
cyproterone
androgen receptor inhibitor
used for hirsutism in women and excessive sexual desire in men (chemical castration)
flutamide
competitive antagonist of the androgen receptors
spironolactone
androgen receptor inhibitor
competes with DHT as well as aldosterone
