Ralofen®
Raloxifene
tablet
Treatment and prevention of postmenopausal osteoporosis
Mechanism of Action:
Raloxifene is an estrogen agonist/antagonist (a selective estrogen receptor modulator [SERM]); selective binding activates estrogenic pathways in some tissues and antagonizes estrogenic pathways in other tissues. Raloxifene acts like an estrogen agonist in the bone to prevent bone loss and has estrogen antagonist activity to block some estrogen effects in the breast and uterine tissues. Raloxifene decreases bone resorption, increasing bone mineral density and decreasing fracture incidence.
Method of Administration:
Osteoporosis, postmenopausal, fracture risk reduction: 60 mg once daily
Risk reduction for invasive breast cancer in postmenopausal females: Oral: 60 mg once daily.
Notes
Contraindications:
History of or current venous thromboembolic disorders (including DVT, PE, and retinal vein thrombosis); pregnancy
Interactions:
Bile Acid Sequestrants: May decrease the absorption of Raloxifene. Management: Consider separating the doses of raloxifene and bile acid sequestrants by at least 4 hours. Risk D: Consider therapy modification
Fluoroestradiol F18: Selective Estrogen Receptor Modulators may diminish the diagnostic effect of Fluoroestradiol F18. Management: Image patients with fluoroestradiol F-18 prior to starting systemic endocrine therapies that block the estrogen receptor. Use of fluoroestradiol F-18 should not delay indicated treatment. Risk D: Consider therapy modification
Levothyroxine: Raloxifene may decrease the absorption of Levothyroxine. Management: Consider separating doses of raloxifene and levothyroxine by several hours. Monitor for reduced effects of levothyroxine and reduced serum concentrations of thyroxine if raloxifene and levothyroxine are used concomitantly. Risk D: Consider therapy modification
Ospemifene: Selective Estrogen Receptor Modulators may enhance the adverse/toxic effect of Ospemifene. Ospemifene may also enhance adverse/toxic effects of other Selective Estrogen Receptor Modulators. Selective Estrogen Receptor Modulators may diminish the therapeutic effect of Ospemifene. Ospemifene may also diminish the therapeutic effects of other Selective Estrogen Receptor Modulators. Risk X: Avoid combination
Pregnancy and Lactation:
Raloxifene is contraindicated during pregnancy.
It is not known if raloxifene is present in breast milk.
Raloxifene is not indicated for use in females of reproductive potential.
Warning and Precaution:
- Breast cancer history: The use of raloxifene has not been adequately studied in females with a prior history of breast cancer.
- Cardiovascular disease: The risk of death due to stroke is increased in postmenopausal females with coronary heart disease or at increased risk for major coronary events; consider risks versus benefits in females at risk for stroke. Do not use for primary or secondary prevention of cardiovascular disease. Assess risks versus benefits in females at risk for stroke (eg, prior stroke, transient ischemic attack, atrial fibrillation, hypertension, smokers).
- Hepatic impairment: Use with caution in patients with hepatic impairment; safety and efficacy have not been established.
- Hypertriglyceridemia: Females with a history of marked elevated triglycerides (>5.6 mmol/L or >500 mg/dL) in response to treatment with oral estrogens (or estrogen/progestin) may also develop elevated triglycerides when treated with raloxifene; monitor triglycerides.
- Renal impairment: Use with caution in patients with moderate to severe renal impairment; safety and efficacy have not been established.
- Uterine bleeding: Investigate unexplained uterine bleeding.
Adverse Reactions:
Cardiovascular: Peripheral edema (3% to 14%)
Endocrine & metabolic: Hot flash (8% to 29%)
Infection: Infection (11%)
Neuromuscular & skeletal: Arthralgia (11% to 16%), leg cramps (≤12%), muscle spasm (≤12%)
Respiratory: Flu-like symptoms (14% to 15%)
Storage:
Store below 30ºC and protect from light and moisture.