Bazedoxifene

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Selective estrogen receptor modulator


Chemical structure of Bazedoxifene

Bazedoxifene is a medication that belongs to the class of drugs known as selective estrogen receptor modulators (SERMs). It is primarily used in the treatment of osteoporosis in postmenopausal women. Bazedoxifene functions by mimicking the effects of estrogen on bone density, thereby reducing the risk of fractures.

Pharmacology[edit | edit source]

Bazedoxifene acts as an estrogen agonist on bone and lipid metabolism, while acting as an estrogen antagonist on uterine and breast tissues. This dual action helps in maintaining bone density and reducing the risk of breast and uterine cancer, which can be a concern with estrogen replacement therapy.

Mechanism of Action[edit | edit source]

Bazedoxifene binds to estrogen receptors and modulates their activity. In bone tissue, it acts as an agonist, promoting bone density and strength. In breast and uterine tissues, it acts as an antagonist, blocking the proliferative actions of estrogen, which helps in reducing the risk of cancer in these tissues.

Clinical Use[edit | edit source]

Bazedoxifene is primarily indicated for the prevention and treatment of osteoporosis in postmenopausal women. It is often used in combination with conjugated estrogens to provide a comprehensive approach to managing menopausal symptoms and preventing bone loss.

Dosage and Administration[edit | edit source]

Bazedoxifene is administered orally, typically in a daily dose. The specific dosage may vary based on the combination with other medications and the individual patient's needs.

Side Effects[edit | edit source]

Common side effects of bazedoxifene include hot flashes, leg cramps, and an increased risk of venous thromboembolism. It is important for patients to discuss their medical history with their healthcare provider to assess the risk of these side effects.

Contraindications[edit | edit source]

Bazedoxifene is contraindicated in women with a history of venous thromboembolism, active or past history of breast cancer, and in those with known hypersensitivity to the drug.

3D molecular model of Bazedoxifene

Research and Development[edit | edit source]

Bazedoxifene has been studied in various clinical trials to assess its efficacy and safety in the treatment of osteoporosis. Ongoing research is exploring its potential use in other conditions related to estrogen deficiency.

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Contributors: Prab R. Tumpati, MD