For the prevention and treatment of osteoporosis in postmenopausal women*: One 60 mg tablet given once a day without regard to meal or time of day.
For the reduction in risk of invasive breast cancer in postmenopausal women with osteoporosis and/or at high risk for invasive breast cancer*: One 60 mg tablet given once a day.
*The following are risk factors for developing postmenopausal osteoporosis: Caucasian or Asian descent, slender body build, early estrogen deficiency, smoking, alcohol consumption, low calcium diet, sedentary lifestyle, and family history of osteoporosis. The greater number of risk factors, the greater probability of developing postmenopausal osteoporosis.
**The following are risk factors for invasive breast cancer; female gender, advancing age, family history of breast cancer (first-degree relative), previous breast biopsy, advanced age at first live birth, early age of menarche, history of atypical hyperplasia or lobular carcinoma in situ, and increased breast density.
Pharmacology/Pharmacokinetics:
Raloxifene is a selective estrogen receptor modulator. Decreases in estrogen levels after menopause lead to bone reabsorption and bone loss. Raloxifene decreases bone resorption by producing an estrogen-like effect on bones. It also possesses estrogen-like activity on lipid metabolism (decrease in total and LDL cholesterol levels). Raloxifene is an estrogen antagonist in uterine and breast tissue. Plasma elimination half-life after an oral dose is 27.7 hours. Metabolism occurs via glucuronide conjugates and excretion occurs through the feces. 95% is bound to plasma proteins.
Drug Interactions:
Cholestyramine significantly reduces the bioavailability of raloxifene. Because of protein binding use caution with diazepam, clofibrate, indomethacin, naproxen, ibuprofen, and diazoxide.
Contraindications/Precautions:
Contraindicated in women who are or may become pregnant and in women with active or past history of venous thromboembolic events, including deep vein thrombosis, pulmonary embolism, and retinal vein thrombosis. Because of the risk of thromboembolic events, discontinue therapy at least three days before patients become immobile (e.g., surgical recovery and prolonged bed rest) and resume only after the patient becomes fully ambulatory. Patients should be advised against prolonged restrictions of movement during travel. Pregnancy Category X.
Adverse Effects:
Hot flashes, leg cramps, weight gain, peripheral edema, sinusitis, rash, and sweating.
Discontinue 72 hours prior to and during periods of prolonged immobilization.
Avoid prolonged restrictions of movement during travel.
It is advisable to take calcium and vitamin D supplements if dietary intake is inadequate.
May be taken without regard to meals.
Report any signs of blood clots to a physician. These include pains in the calves or leg swelling, sudden chest pain, shortness of breath or coughing blood, or changes in vision.
Discontinue therapy and consult physician if pregnancy is suspected.
If a dose is missed, take it as soon as possible and return to dosing schedule.
Store in a cool, dry place away from sunlight and children.