Raloxifene is a second-generation selective estrogen receptor modulator (SERM) used primarily for the prevention and treatment of postmenopausal osteoporosis. It acts as an estrogen agonist on bone and lipid metabolism while acting as an estrogen antagonist on breast and uterine tissue. It is a non-hormonal, oral therapy that reduces the risk of vertebral fractures.
Adult: 60 mg orally once daily, with or without food.
Note: Tablet should be swallowed whole with a glass of water. Can be taken at any time of the day, with or without food. If a dose is missed, it should be taken as soon as remembered on the same day. Two tablets should not be taken on the same day. Calcium (1000-1500 mg/day) and Vitamin D (400-800 IU/day) supplementation is recommended unless contraindicated.
Raloxifene binds to estrogen receptors (ER) with high affinity, resulting in differential expression of estrogen-regulated genes in various tissues. It acts as an estrogen agonist in bone (increasing mineralization, reducing resorption) and on lipid metabolism (decreasing LDL cholesterol). It acts as an estrogen antagonist in breast and uterine tissue, blocking the proliferative effects of estrogen.
Pregnancy: Pregnancy Category X. Contraindicated. Raloxifene may cause fetal harm. Can cause fetal abnormalities and loss of pregnancy. Exclude pregnancy before starting therapy. Advise use of effective non-hormonal contraception in perimenopausal women.
Driving: Raloxifene has no known influence on the ability to drive and use machines. However, patients experiencing dizziness, vertigo, or leg cramps should exercise caution.
| Warfarin | Raloxifene may modestly decrease prothrombin time. Monitor INR closely when starting or stopping raloxifene. | Moderate |
| Cholestyramine | Significantly reduces the absorption and enterohepatic cycling of raloxifene by ~60%. Administer at least 2 hours before or 4-6 hours after cholestyramine. | Major |
| Ampicillin, Amoxicillin | May reduce enteric hydrolysis of raloxifene glucuronides, potentially decreasing enterohepatic cycling and efficacy. | Moderate |
| Systemic Estrogens (Oral, Transdermal) | Concomitant use is not recommended. May interfere with the SERM activity and safety profile. | Major |