HRT, Selective Estrogen Response Modifiers

Question 1

Selective Estrogen Response Modifiers (SERM)

Answer 1

Steroid analogs, “mixed agonist-antagonist” properties
“tissue-specific)
Full agonists in some tissues, full antagonists in others
NOT “partial agonists”

Question 2

Raloxifene

Answer 2

Agonist at: bone/osteoporosis (good), lipids/heart dz (good), clotting factors/stroke (bad)
Antagonist at: breat/cancer (good), uterus/cancer (good), menopausal symptoms (bad)
Oral
First SERM
Agonist on bone, antagonist for Breast CA prevention
Lacks uterine CA risk
Antagonist on breat
Improves blood lipid profiles
Disadvantages: causes hot flashes, increased clotting/thrombosis risk
Useful only for OSTEOPOROSIS part of menopause

Question 3

Tamoxifen

Answer 3

Agonist at: bone/osteoporosis (good), lipids/heart dz (good), uterus/cancer (bad), clotting factors/stroke (bad)
Antagonist at: breast/cancer (good), menopausal symptoms (bad)
Oral
Antagonist on breast only (major use)
Agonist effects on other tissues
Breast CA preventive therapy
May decrease osteoporosis, improve blood lipid profiles, decrease heart dz risk
Disadvantages: increased uterine Ca, increased thrombosis risk, hot flashes

Question 4

Bisphosphonates

Answer 4

Decrease bone resorption

Useful for osteoporosis