Raloxifene

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Raloxifene belongs to a group of non-hormonal medicines called Selective Estrogen Receptor Modulators (SERMs).

Raloxifene mimics some of the helpful effects of estrogen after the menopause. Raloxifene reduces the risk of vertebral fractures in women with postmenopausal osteoporosis. A reduction in the risk of hip fractures has not been shown.

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[edit] BRAND NAMES

[edit] STRUCTURE

Raloxifene.jpg

[edit] MECHANISM OF ACTION

Osteoporosis happens when not enough new bone grows to replace the bone that is naturally broken down. Gradually, the bones become thin and fragile, and more likely to break. Osteoporosis is more common in women after the menopause, when the levels of the female hormone estrogen fall, since estrogen helps to keep bones healthy. Approximately 40% of 50-year-old women will experience an osteoporosis-related fracture during their remaining lifetimes and bone loss is particularly rapid for the first 10 years after menopause when the compensatory increase in bone formation is inadequate to keep up with resorptive losses.

Raloxifene, is a selective estrogen receptor modulator (SERM). It acts as an AGONIST of the estrogen receptor on bone and partially on cholesterol metabolism (decrease in total and LDL-cholesterol) and as an estrogen ANTAGONIST in uterine and breast tissues.

Replacement therapy with Raloxifene reverse the excessive resorption of bone, reduce the incidence of vertebral fractures, preserve bone mass and increase bone mineral density (BMD) in postmenopausal women with osteoporosis.

[edit] INDICATIONS

  • Treatment and prevention of osteoporosis in postmenopausal women.
  • Reduction in risk of invasive breast cancer in postmenopausal women with osteoporosis. (FDA)
  • Reduction in risk of invasive breast cancer in postmenopausal women at high risk for invasive breast cancer. (FDA)

[edit] DOSAGE

The recommended dose is one tablet (60 mg) taken once a day, with or without food. Patients may also receive calcium and vitamin D supplements if they do not get enough from their diet. Raloxifene is intended for long-term use.

[edit] CONTRAINDICATIONS

  • Pregnancy and lactation
  • Active or past history of venous thromboembolism, including deep vein thrombosis, pulmonary embolism (a blood clot in the lungs), and retinal vein thrombosis.
  • Hypersensitivity to Raloxifene.

[edit] WARNINGS AND PRECAUTIONS

  • Venous Thromboembolism: Increased risk of deep vein thrombosis, pulmonary embolism, and retinal vein thrombosis. Discontinue use 72 hours prior to and during prolonged immobilization.
  • Death Due to Stroke: Increased risk of death due to stroke occurred in a trial in postmenopausal women with documented coronary heart disease or at increased risk for major coronary events. No increased risk of stroke was seen in this trial. Consider risk-benefit balance in women at risk for stroke.
  • Cardiovascular Disease: Raloxifene should not be used for the primary or secondary prevention of cardiovascular disease.
  • Premenopausal Women: Use is not recommended.
  • Hepatic Impairment: Use with caution.
  • Concomitant Use with Systemic Estrogens: Not recommended.
  • Hypertriglyceridemia: If previous treatment with estrogen resulted in hypertriglyceridemia, monitor serum triglycerides

[edit] INTERACTIONS

  • Cholestyramine: Raloxifene should not be co-administered with cholestyramine (or other anion exchange resins), which significantly reduces the absorption and enterohepatic cycling of raloxifene.

[edit] PREGNANCY AND LACTATION

  • Pregnancy Category X (US). Raloxifene should not be used in women who are or may become pregnant.
  • Nursing Mothers: Raloxifene should not be used by lactating women. It is not known whether this drug is excreted in human milk. Because many drugs are excreted in human milk, caution should be exercised when raloxifene is administered to a nursing woman

[edit] SIDE EFFECTS

Common side effects are hot flushes, sweating, flu-like symptoms, leg cramps, peripheral edema and arthralgia

[edit] RELATED LINKS

How osteoporosis develops

[edit] BIBLIOGRAPHY

[edit] REFERENCES