Indication: For the prevention of osteoporosis in post-menopausal women
Pharmacology: Raloxifene, a selective estrogen receptor modulator (SERM) of the benzothiophene class, is similar to tamoxifen in that it produces estrogen-like effects on bone and lipid metabolism, while antagonizing the effects of estrogen on mammary tissue. Raloxifene decreases bone resorption, increases bone mineral density (BMD) and decreases incidence of fractures. Raloxifene is used in the prevention of postmenopausal osteoporosis and breast cancer.
Mechanism Of Action: Raloxifene binds to estrogen receptors, resulting in differential expression of multiple estrogen-regulated genes in different tissues. Raloxifene produces estrogen-like effects on bone, reducing resorption of bone and increasing bone mineral density in postmenopausal women. Raloxifene also antagonizes the effects of estrogen on mammary tissue and blocks uterotrophic responses to estrogen.
Absorption: Approximately 60% of an oral dose is absorbed, but presystemic glucuronide conjugation is extensive. Absolute bioavailability of raloxifene is 2.0%
Interactions:
DrugBank: Interactions for Raloxifene
Interactions for Raloxifene:
Cholestyramine: Cholestyramine causes a 60% reduction in the absorption and enterohepatic cycling of
raloxifene and should not be coadministered with EVISTA.
Warfarin: The coadministration of EVISTA and warfarin has not been assessed under chronic
conditions. However, 10% decreases in prothrombin time have been observed in single-dose studies. If EVISTA is given
concurrently with warfarin, prothrombin time should be monitored.
Other Highly Protein-Bound Drugs: Raloxifene is more than 95% bound to plasma proteins. In vitro,
raloxifene did not affect the binding of warfarin, phenytoin, or tamoxifen. Caution should be used when EVISTA is
coadministered with other highly protein-bound drugs, such as clofibrate, indomethacin, naproxen, ibuprofen,
diazepam, and diazoxide.
