Gonadal Hormones and Inhibitors Flashcards
Androgen Receptor Antagonist
Flutamide, Bicalutamide, Nilutamide
Cyproterone, Cyproterone Acetate
Androgen Synthesis Inhibitor/5-Alpha Reductase Inhibitor
Finasteride
Dutasteride
MOA: FINASTERIDE
inhibits 5 alpha reductase enzyme that converts testosterone to DHT (most potent form)
Anabolic Steroids
Oxandrolone, Nandrolone Decanoate
Used in male hypogonadism
Androgens - Testosterone, Methyltestosterone, Testosterone Cypionate, Oxymetholone, Mesterolone
Used in illegal performance enhancement by athletes
Anabolic Steroids
oxandrolone, nandrolone decanoate
Used in Prostate CA
Flutamide, Bicalutamide, Nilutamide
Used in hirsutism
Cyproterone, Cyproterone acetate
Used in BPH
Finasteride, Dutasteride
SERM
Tamoxifen
Toremifene
Raloxifene
Clomiphene
Aromatase Inhibitors
Anstrozole
Letrozole
Exemestane
Ovarian Inhibitor (Anti-Androgen)
Danazol
GNRH AGONISTS
Leuprolide Gonadorelin Goserelin Histrelin Nafarelin Triptorelin
GNRH ANTAGONISTS
Ganirelix
Cetrorelix
Abarelix
Degarelix
Glucocorticoid and Progesterone Receptor Antagonist
Mifepristone
Use: Tamoxifen, Toremifene
Hormone-responsive Breast Cancer
ER+ PR+
Use: Raloxifene
Osteoporosis
preferred
increases bone mineral density without estrogenic effects on endometrial tissue
Use: Clomiphene
Induction of ovulation
antagonizes estrogen receptors in the pituitary thus inhibiting the negative feedback by estrogen = increase LH and FSH
Enzyme that converts Testosterone to Estrogen (Estradiol)
Aromatase
Irreversible aromatase inhibitor
Exemestane
Pharmacologic antagonist of glucocorticoid and progesterone receptors used in medical abortion
Mifepristone
AE of Tamoxifen
Increased risk for endometrial hyperplasia, endometrial CA, DVT
AE of Raloxifene
Increased risk for DVT
Side effect of Clomiphene
Multiple pregnancies (10%)
Increased risk of low-grade ovarian cancer with long term use