SERMs

Selective estrogen receptor modulator (SERM)

Raloxifene is a selective estrogen receptor modulator (SERM) that is given to postmenopausal women. It appears to act on bone as an estrogen agonist. In uterine and breast tissue, the nonsteroidal compound exerts an estrogen antagonist effect. Multiple estrogen/SERM receptors, capable of reacting with multiple response elements, appear to exist within cell nuclei and permit the differential effects of SERMs on various tissues. They select specific estrogen receptors in the body and either stimulate or depress an estrogen-like response. In other words, SERMs cause estrogen-like responses in certain tissues

while preventing estrogen-like responses in other parts of the body.

There are no cures for osteoporosis, but raloxifene can help reduce the effects of the condition. Raloxifene can prevent bone loss throughout the body, increase bone density, and reduce the risk of hip and spinal fractures.

Unlike estrogen, raloxifene does not appear to increase the risk of uterine cancer or breast cancer. On the other hand, it will not simultaneously treat menopausal symptoms as estrogen does. In addition to treating bone loss, raloxifene has also been shown to: reduce levels of LDL and total cholesterol.

Unfortunately raloxifene can increase menopausal symptoms flushing and transpiration and cause leg cramps. Rare side effects include blood clots (similar to estrogens).

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The clinical effect of raloxifene on bone density will become apparent after: