What it's for (Indications)
- Recommended for post-menopausal women to reduce the risk of non-traumatic vertebral fractures, for the prevention and treatment of osteoporosis, and for the reduction of the risk of invasive breast cancer.
Dosage Information
| Type | Guideline |
|---|---|
| Standard | The recommended dosage is one 60 mg raloxifene hydrochloride tablet orally once daily. It may be administered any time of day without regard to meals. For the treatment or prevention of osteoporosis, supplemental calcium and/or vitamin D should be added to the diet if daily intake is inadequate. Postmenopausal women typically require an average of 1500 mg/day of elemental calcium and 400-800 IU daily of vitamin D. |
Safety & Warnings
Common Side Effects
- Common adverse reactions observed in clinical trials (affecting >2% of patients and more frequently than placebo) include hot flashes (also known as hot flushes), leg cramps, peripheral edema, flu syndrome, arthralgia, and sweating.
- Patients experiencing these symptoms for a prolonged period should consult their physician.
Serious Warnings
- Black Box Warning: WARNING: INCREASED RISK OF VENOUS THROMBOEMBOLISM AND DEATH FROM STROKE. Increased risk of deep vein thrombosis and pulmonary embolism have been reported with raloxifene hydrochloride tablets. Women with active or past history of venous thromboembolism should not take raloxifene hydrochloride tablets. Increased risk of death due to stroke occurred in a trial.
- Patients should ensure adequate intake of vitamin D and calcium while on this medication.
- Driving should be avoided if this medicine affects one's ability to drive.
- Alcohol consumption should be avoided.
- An increased risk of deep vein thrombosis and pulmonary embolism has been reported.
- An increased risk of death due to stroke has also occurred in clinical trials, particularly in women with a history of stroke or transient ischemic attack.
- Caution is advised in patients with risk factors for venous thromboembolism.
How it Works (Mechanism of Action)
Raloxifene is an estrogen agonist/antagonist, commonly referred to as a selective estrogen receptor modulator (SERM). Its biological actions are largely mediated through binding to estrogen receptors, resulting in activation of estrogenic pathways in some tissues (agonism) and blockade in others (antagonism). The specific action depends on the extent of recruitment of coactivators and corepressors to estrogen receptor (ER) target gene promoters. Raloxifene acts as an estrogen agonist in bone, decreasing bone resorption and turnover, increasing bone mineral density (BMD), and decreasing fracture incidence. Preclinical data and clinical trials demonstrate that raloxifene acts as an estrogen antagonist in uterine and breast tissues, lacking estrogen-like effects on these organs.