Sex hormones & Gonadotropins Flashcards
(25 cards)
Leuprolide
GnRH agonist- long acting, initial inc release then suppresses LF/FSH.
Tx: shut down HPG axis- infertility, prostate/breast ca, delay precocious puberty, endometriosis, PCOS, uterine leiomyomas
Adv: menopausal sx, testes atrophy, ovarian cyst
PROSTATE CA: use w/ antiandrogens at first!!!!
Gonadorelin
GnRH agonist, short acting, for infertility.
Not in the US
Nafarelin
GnRH agonist- long acting, initial inc release then suppresses LF/FSH.
Tx: shut down HPG axis- infertility, prostate/breast ca, delay precocious puberty, endometriosis, PCOS, uterine leiomyomas
Adv: menopausal sx, testes atrophy, ovarian cyst
PROSTATE CA: use w/ antiandrogens at first!!!!
Goserelin
GnRH agonist- long acting, initial inc release then suppresses LF/FSH.
Tx: shut down HPG axis- infertility, prostate/breast ca, delay precocious puberty, endometriosis, PCOS, uterine leiomyomas
Adv: menopausal sx, testes atrophy, ovarian cyst
PROSTATE CA: use w/ antiandrogens at first!!!!
Cetrorelix
GnRH antagonist- supp release of LH (low dose), FSH (high dose)
4-5d tx, no initial Gn surge
Tx: endometriosis, ART
Ganirelix
GnRH antagonist- supp release of LH (low dose), FSH (high dose)
4-5d tx, no initial Gn surge
Tx: endometriosis, ART
Urofollitropin
purified FSH
stim ovaries and estrogen, drives spermatogenesis
Follitropin-a
Follitropin-b
rFSH
Expensive, no urine contaminants
stim ovaries and estrogen, drives spermatogenesis
hMG
Human menopausal gonadotropins- LH+FSH but used as FSH
stim ovaries and estrogen, drives spermatogenesis
Menotropins
LH+FSH but used as FSH
stim ovaries and estrogen, drives spermatogenesis
hCG
Human chorionic gonadotropins, similar structure to LH, longet T1/2
IM admin
Sg dose to induce ovulaiton, inc Testosterone in males (up to a yr)
Choriogonadotropin-a
recombinant hCG- acts as LH
SC admin
Sg dose to induce ovulaiton, inc Testosterone in males (up to a yr)
Lutropin
Recombinant LH
Only for combo c follitropin-a (rFSH)
Sg dose to induce ovulaiton, inc Testosterone in males (up to a yr)
Estradiol
(Estrace, Estraderm)
Estrogen- endogenous
not orally active -cream/patch
Ethinyl estradiol
Mestranol
Synthetic estrogen
Combo oral contraceptives
Premarin
Conjugated estrogen - equine
HRT
Cenestin
Conjugated estrogen - soy
HRT
Diethylstilbestrol (DES)
Non-steroid - estrogenic activity
CI in pregnancy
Tamoxifen
Estrogen agonist in uterus/bone, antagonist in breast
DOC: premenopausal estrogen dependent breast CA (prevent bone loss), no hot flash relief
Adv: risk of uterine CA, dec HDL, hot flashes, n/v
CI: thromboembolism, breast feeding
Toremifene (Fareston)
Estrogen agonist in uterus/bone, antagonist in breast (tamoxifen like)
For high HDL
Raloxifene (Evista)
Estrogen agonist in bone/liver, antagonist in breast/uterus
To prevent postmeno osteoporosis (inc bone density)
Adv: hot flashes, DVT, leg cramps
Clomiphene (Clomid)
Estrogen antagonist in hypothalamus (inc LH/FSH, no neg feedback)
Agonist elsewhere
DOC infertility (women c intact HPG)
Adv: mltp preg, hot flashes, HA, constipation, allergic, hair loss, enlarge ovaries
Fulvestrant (Faslodex)
Pure estrogen receptor agonist
For tamoxifen resistant tumors
Adv: hot flashes, GI, HA, back pain, pharyngitis
Anastrozole (Arimidex)
Letrozole (Femara)
Non-steroidal comp inhibitor of aromatase (only estrogen synth inhibit)
DOC: postmeno breast CA. 2nd line: postmeno breast CA that progressed w/ tamoxifen.
Adv: menopausal sx, bone fractures, jnt pain
CI: premenopausal, pregancy
