Raloxifene

Raloxifene

A drug that belongs to the family of drugs called selective estrogen receptor modulators (SERMs) and is used in the prevention of osteoporosis in postmenopausal women. Raloxifene is also being studied as a cancer-prevention drug.

Information about Raloxifene

Raloxifene (ral ox' i feen) is a selective estrogen receptor modulator that has estrogen-like effects (agonism) on bone and the cardiovascular system but antiestrogen activity (antagonism) on breast and uterus tissue.  This differential activity takes advantage of the beneficial effects of estrogens on bone in decreasing bone resorption and turnover and thus preventing osteoporosis, while avoiding the potential harmful effects of estrogen stimulation of breast and uterine tissue. 

Mechanism of action of Raloxifene

In several large clinical trials, raloxifene was shown to increase bone mineral density and prevent bone fractures in postmenopausal women at high risk for osteoporosis, while decreasing serum cholesterol levels (both total and LDL) and without stimulating breast and uterine growth. 

FDA approval information for Raloxifene

Raloxifene was approved for treatment and prevention of postmenopausal osteoporosis in the United States in 1997, and indications were expanded in 2007 to include reduction of risk of breast cancer in postmenopausal women with osteoporosis as well as those at high risk of breast cancer.  Raloxifene is available in tablets of 60 mg generically and under the brand name Evista, and the recommended dose is 60 mg daily. 

Side effects of Raloxifene

side effects are not common, but can include hot flashes, leg cramps, peripheral edema, arthralgias and sweating.  Rare, but potentially severe adverse events include deep venous thrombosis, pulmonary embolism and ischemic strokes, side effects that it shares with estrogen. 

Obstetrical and Gynecological Agents

• Emergency contraceptive agents
  • Levonorgestrel, Ulipristal

• Estrogens and Oral contraceptives

• • Selective estrogen receptor modulators
    • Bazedoxifene, Ospemifene, Raloxifene
  • Infertility agents

• Antiestrogens
  • Clomiphene, Letrozole, Tamoxifen

• Gonadotropins
  • Chorionic gonadotropin, Follicle stimulating hormone, Luteinizing hormone, Human gonadotropin releasing hormone

• Pregnancy termination agents
  • Mifepristone
• Progesterone and the Progestins

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