Raloxifene is a selective estrogen receptor modulator (SERM). It acts as an estrogen receptor agonist in the bones. On the other hand, it acts as an estrogen receptor antagonist on the breast and uterus.
Raloxifene has a similar effect as estrogen in bones by inhibiting osteoclast differentiation, which leads to decreased bone resorption.
Raloxifene has an antiestrogenic activity in the breast tissue and endometrium. The antagonist effect in endometrial tissue does not increase the risk of endometrial cancer development. This is different from other SERMs such as tamoxifen, which acts as a partial agonist on the endometrium and results in an increased risk of endometrial cancer.
Osteoporosis is most commonly seen in postmenopausal patients and is characterized by the deficiency of estrogen. Raloxifene acts as an agonist on estrogen receptors in the bone and will preserve bone mineral density in patients with osteoporosis. This treatment will help to prevent complications such as fracture.
Raloxifene has antiestrogenic activity in breast tissue, making it useful in reducing the risk of breast cancer. It can decrease the incidence of invasive breast cancer by up to 72%.
Raloxifene is the most studied SERM for the treatment of uterine fibroids. Data is still limited, but it has been shown to decrease the size of fibroids.
One of the most common side effects of raloxifene is hot flashes. It occurs in roughly 10% of patients.
Raloxifene increases the risk of deep vein thrombosis (DVT), pulmonary embolism, and retinal vein thrombosis. These complications can occur within the first four months of treatment. If the patient has a history of thrombosis, raloxifene should be avoided. Raloxifene should be discontinued at least 72 hours before and during immobilization (e.g., post-surgical recovery).
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