Antiestrogens & antiprogestins Flashcards
Antiestrogens (2 groups)
Estrogen receptor antagonists Aromatase inhibitors (estrogen synthesis inhibitors)
Estrogen receptor antagonists (6 drugs)
Clomiphene Tamoxifen Raloxifene Toremifene Ospemifene Bazedoxifene
Clomiphene - indication
Anovulatory infertility (polycystic ovary disease)
Which estrogen receptor antagonist is used indicated for breast cancer?
Tamoxifen
Tamoxifen - MoA and adverse effects
Both estrogenic and antiestrogenic effects. Antagonist in breast –> inh breast cancer proliferation, agonist in endometrial tissue
Endometrial cancer
Vaginal bleeding
Hot flashes
Raloxifene - indications
Osteoporosis and reduces risk of breast cancer in postmenopausal women
Raloxifene - MOA
Estrogen-like effects on bone and lipid metabolism, antagonistic effect on breast and uterine tissue
Aromatase inhibitors (2 drugs)
Anastrozole
Letrozole
First-line treatment of locally advanced or metastatic breast cancer in postmenopausal women
Estrogen synthesis inhibitors (anastrozole & letrozole
Aromatase inhibitors - adverse effects
Hot flashes
Vaginal bleeding
Back pain
Antiprogestins (1 drug)
Mifepristone
Mifepristone - indications
Medical termination of pregnancy through 49 days gestation
Cushing’s syndrome
Hyperglycemia
Mifepristone treatment is followed by
A prostaglandin (usually misopristol)
Mifepristone - adverse effects
Heavy uterine bleeding
Clomiphene - MoA and Adverse effects
Weak estrogen agonist and moderate estrogen antagonist. Increases FSH and LH, induce follicle maturation and ovulation
Multiple births and hot flashes
