Raloxifene, sold under the brand name Evista among others, is a medication used to prevent and treat osteoporosis in postmenopausal women and those on glucocorticoids. For osteoporosis it is less preferred than bisphosphonates. It is also used to reduce the risk of invasive estrogen receptor positive breast cancer in postmenopausal women at increased risk. Raloxifene is a selective estrogen receptor modulator that acts as an estrogen agonist in bone and lipid metabolism and as an antagonist in breast and uterine tissues, reducing bone resorption and favorably altering bone mineral density; it is administered orally, commonly 60 mg once daily, has low absolute bioavailability due to first pass glucuronidation, undergoes extensive enterohepatic recycling, and is primarily eliminated as glucuronide conjugates, with a terminal half-life in the range of about 27 to 32 hours in healthy adults.
Parent: Raloxifene
Parent: Raloxifene
Parent: Raloxifene
Parent: Raloxifene
Parent: Raloxifene / Raloxifene Hydrochloride
Parent: Raloxifene
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Parent: Raloxifene
Manufacturing and stability control for raloxifene API and finished dosage forms focuses on limiting process- and degradation-related impurities monitored by validated HPLC and LC-MS methods; commonly applied specification limits are individual unidentified impurities not more than 0.2 percent w/w and total impurities not more than 1.0 percent w/w, with specified known related compounds typically limited to 0.1 to 0.2 percent depending on toxicity profiling and regulatory guidance. Typical identified related compounds and metabolites that are monitored include hydroxylated and dealkylated analogs such as 6-hydroxy-raloxifene, raloxifene N-oxide, desalkylated derivatives, and sulfated/glucuronidated conjugates; potential genotoxic or mutagenic impurities are controlled to ICH M7-derived limits and residual solvents and heavy metals are controlled to relevant pharmacopeial limits.
Raloxifene is used to prevent and treat osteoporosis in postmenopausal women and in patients receiving chronic glucocorticoid therapy; it also reduces the risk of developing invasive estrogen receptor positive breast cancer in postmenopausal women who are at increased risk.
If by gyno you mean gynecologic conditions generally, raloxifene is not a treatment for common benign gynecologic conditions such as fibroids or polycystic ovarian syndrome; it has tissue-selective estrogen antagonist activity in breast and uterine tissue, and its effects on menstrual bleeding are not the target of therapy.
Key disadvantages include increased risk of venous thromboembolism and possibly stroke in certain populations, common adverse effects such as hot flashes and leg cramps, lack of proven efficacy for vertebral fracture prevention that matches some bisphosphonates for nonvertebral fracture reduction, contraindication in pregnancy and lactation, and interactions or reduced benefit when combined with estrogen therapies.
Avoid coadministration with estrogen-containing hormone replacement therapies when the goal is breast cancer risk reduction since estrogen can antagonize raloxifene breast effects; bile acid sequestrants such as cholestyramine and colestipol may reduce raloxifene absorption so separate dosing is recommended; be cautious with concomitant agents that alter glucuronidation pathways or enterohepatic circulation, and evaluate thrombotic risk when combining with drugs that increase clotting risk.
