Class: Selective Estrogen Receptor Modulator
Dosage Forms. Tablet: 60 mg
Common FDA Label Indication, Dosing, and Titration.
1. Breast cancer, invasive, in postmenopausal women at high risk; prophylaxis: 60 mg po daily
2. Postmenopausal osteoporosis, prevention or treatment: 60 mg po daily
Off-Label Uses. None
MOA. Raloxifene is a selective estrogen receptor modulator (SERM) and binds to estrogen receptors, resulting in activation of estrogenic pathways in some tissues (agonism) and blockade of estrogenic pathways in others (antagonism). The agonistic or antagonistic action of raloxifene depends on the extent of recruitment of coactivators and corepressors to estrogen receptor (ER) target gene promoters. Raloxifene appears to act as an estrogen agonist in bone, decreasing bone resorption and bone turnover, increasing BMD.
Drug Characteristics: Raloxifene
Medication Safety Issues: Raloxifene
Drug Interactions: Raloxifene
Adverse Reactions: Raloxifene
Efficacy Monitoring Parameters. DEXA scan for increased bone mineral density, mammography showing absence of breast cancer.
Toxicity Monitoring Parameters. Weight gain, shortness of breath, symptoms of stroke, DVT (swelling of the leg, redness, pain); triglycerides.
Key Patient Counseling Points. Raloxifene increases the risk of blood clots, especially during the first 4 mo of therapy. Avoid sitting for long periods and be aware of the symptoms of deep vein thrombosis. If taking for osteoporosis, consider calcium and vitamin D supplementation.
Clinical Pearls. Tamoxifen and raloxifene are equivalent in efficacy of preventing breast cancer; however, raloxifene causes less endometrial hyperplasia, thromboembolic events, and cataracts. Medication guide required at dispensing.