Estrogen/Progestin Antagonists Flashcards
Selective Estrogen Receptor Modulators (SERMs)
Clomiphene
Tamoxifen
Raloxifene
Aromatase Inhibitors
Anastrazole
Letrozole
GnRH agonist
Leuprolide
GnRH receptor antagonist
Ganirelix
Cetrorelix
Treatment of anovulatory infertility
Clomiphene
Weak estrogen agonist
MOA of Clomiphene
Blocks ER in hypothalamus and pituitary, increasing FSH and LH Secretion → inducing follicle development and ovulation
A/E of Clomiphene
Multiple births
Tamoxifen
Tamoxifen → 4-hydroxytamoxifen (30-100x affnity to FR)
Estrogen antagonist: breast tissue and CNS
Estrogen agonist: endometrium, liver and bone
Prevention and adjuvant treatment of hormone-responsive breast cancer
Tamoxifen
S/E of Tamoxifen
Hot flushes, thromboembolism, endometrial hyperplasia
Approved for osteoporosis and prevention of breast cancer in postmenopausal women
Raloxifene
Antagonist effects in breast, CNS, and endometrium
Agonist effects in the liver
First line treatment for locally advanced or metastatic breast cancer in postmenopausal women
Aromatase inhibitors
Anastrazole
Letrozole
Adjuvant treatment of hormone-responsive breast cancer
Anastrazole
Aromatase inhibitor used for treatment of anovulatory infertility
Letrozole
Weak cytochrome P450 inhibitor and partial agonist of progestin and androgen receptors
Danazol