Bazedoxifene

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[edit] BRAND NAMES

[edit] STRUCTURE

Bazedoxifene.jpg

[edit] MECHANISM OF ACTION

Osteoporosis happens when not enough new bone grows to replace the bone that is naturally broken down. Gradually, the bones become thin and fragile, and more likely to break. Osteoporosis is more common in women after the menopause, when the levels of the female hormone estrogen fall, since estrogen helps to keep bones healthy. Approximately 40% of 50-year-old women will experience an osteoporosis-related fracture during their remaining lifetimes and bone loss is particularly rapid for the first 10 years after menopause.

Bazedoxifene, is a selective estrogen receptor modulator (SERM). It acts as an AGONIST of the estrogen receptor on bone and as an estrogen ANTAGONIST in uterine and breast tissues.

Replacement therapy with Bazedoxifene reverse the excessive resorption of bone and increase bone mineral density (BMD) in postmenopausal women with osteoporosis.

[edit] INDICATIONS

  • Treatment and prevention of osteoporosis in postmenopausal women. A significant reduction in the incidence of vertebral fractures has been demonstrated; efficacy on hip fractures has not been established.

[edit] DOSAGE

The recommended dose is one tablet (20 mg) taken once a day, at any time of day, with or without food. Patients may also receive calcium and vitamin D supplements if they do not get enough from their diet. Bazedoxifene is intended for long-term use.

[edit] CONTRAINDICATIONS

  • Women of child-bearing potential
  • Active or past history of venous thromboembolism, including deep vein thrombosis, pulmonary embolism (a blood clot in the lungs), and retinal vein thrombosis.
  • Hypersensitivity to Bazedoxifene.

[edit] WARNINGS AND PRECAUTIONS

  • Venous Thromboembolism: Increased risk of deep vein thrombosis, pulmonary embolism, and retinal vein thrombosis. Discontinue use prior to and during prolonged immobilisation (e.g., post-surgical recovery, prolonged bed rest), and therapy should be resumed only after the patient is fully ambulatory
  • Premenopausal Women: Use is not recommended.
  • Hepatic Impairment: Use is not recommended.
  • Hypertriglyceridemia: Bazedoxifene may increase serum triglyceride levels; therefore, caution should be exercised in patients with known hypertriglyceridemia.

[edit] INTERACTIONS

[edit] PREGNANCY AND LACTATION

  • Bazedoxifene is only for use in postmenopausal women.
  • Nursing mothers: It is not known whether bazedoxifene is excreted in human milk. Bazedoxifene is not intended for use in breast-feeding women.

[edit] SIDE EFFECTS

The most common side effects (seen in more than 10% of patients) are hot flushes and muscle spasms.

Other common adverse reactions include hypersensitivity, somnolence, dry mouth , urticaria, peripheral edema, increased blood triglycerides and elevated transaminases (ALT and AST)

[edit] RELATED LINKS

How osteoporosis develops

[edit] BIBLIOGRAPHY

[edit] REFERENCES