Bazedoxifene
- Atc Codes:G03XC02
- CAS Codes:198481-33-3
- PHARMGKB ID:198481-33-3
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Genes that may be involved
- Substrate of
- Drug Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Conbriza; Czech Republic: Conbriza; Estonia: Conbriza; Finland: Conbriza; Germany: Conbriza; Greece: Conbriza; Ireland: Conbriza; Lithuania: Conbriza; Luxembourg: Conbriza; Malta: Conbriza; Netherlands: Conbriza; Poland: Conbriza; Portugal: Conbriza; Romania: Conbriza; Slovakia: Conbriza; Slovenia: Conbriza; Spain: Conbriza; Sweden: Conbriza.
Drug combinations
Chemistry
Bazedoxifene Acetate: C~32~H~38~N~2~O~5~. Mw: 530.65. (1) Acetic acid;1-[[4-[2-(azepan-1-yl)ethoxy]phenyl]methyl]-2-(4-hydroxyphenyl)-3-methylindol-5-ol; (2) 1-(p-(2-(Hexahydro-1H-azepin-1-yl)ethoxy)benzyl)-2-(p-hydroxyphenyl)-3-methylindol-5-ol monoacetate; (3) 1H-Indol-5-ol, 1-((4-(2-(hexahydro-1H-azepin-1-yl)ethoxy)phenyl)methyl)-2-(4-hydroxyphenyl)-3-methyl-, monoacetate. CAS-198481-33-3.
Pharmacologic Category
Estrogen Agonists-Antagonists; Selective Estrogen Receptor Modulator. (ATC-Code: G03XC02).
Mechanism of action
Bazedoxifene acts as both an estrogen-receptor agonist and/or antagonist, depending upon the cell and tissue type and target genes. Bazedoxifene decreases bone resorption and reduces 5 biochemical markers of bone turnover to the premenopausal range. These effects on bone remodeling lead to an increase in bone mineral density (BMD), which in turn contributes to a reduction in the risk of fractures. Bazedoxifene functions primarily as an estrogen-receptor antagonist in uterine and breast tissues.
Therapeutic use
Treatment of postmenopausal osteoporosis in women at increased risk of fracture.
Pregnancy and lactiation implications
Only for use in postmenopausal women. Contraindicated in women of child-bearing potential. Not intended for use in breast-feeding women.
Unlabeled use
Contraindications
Hypersensitivity to the active substance or to any of the excipients. Active or past history of venous thromboembolic events, including deep vein thrombosis, pulmonary embolism, and retinal vein thrombosis. Only for use in postmenopausal women. Bazedoxifene must not be taken by women of child-bearing potential. Unexplained uterine bleeding. Patients with signs or symptoms of endometrial cancer.
Warnings and precautions
Not recommended in women at increased risk for venous thromboembolic events. Its safety in premenopausal women has not been established, and its use is not recommended. Any uterine bleeding during therapy should be fully investigated. May increase serum triglyceride levels. Not recommended for treatment or prevention of breast cancer. Contains lactose (patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicinal product).