Endometrial hyperplasia
Increased risk of endometrial cancer in a woman with a uterus who uses unopposed estrogens; bazedoxifene/conjugated estrogens has been shown to reduce the risk of endometrial hyperplasia, which may be a precursor to endometrial cancer.
Adequate diagnostic measures, including directed or random endometrial sampling when indicated, should be undertaken to rule out malignancy in postmenopausal women with undiagnosed persistent or recurring abnormal genital bleeding.
Estrogens and estrogen agonist/antagonists are known to increase risk of thromboembolism, including DVT, PE, and stroke
Discontinue 4-6 weeks before surgery that is associated with increased risk of thromboembolism, or during periods of prolonged immobilization
Retinal vascular thrombosis reported
Estrogens may exacerbate pre-existing hypertriglyceridemia and lead to pancreatitis
Caution with history of cholestatic jaundice associated with past estrogen use or with pregnancy
Do not use with conditions that predispose to hyperkalemia
Use caution in individuals with severe hypocalcemia
Indication
Menopausal Vasomotor Symptoms, Osteoporosis
Contra Indication
Undiagnosed abnormal uterine bleeding
Known, suspected, or past history of breast cancer
Known or suspected estrogen-dependent neoplasia
Active DVT, PE, or history of these conditions
Active arterial thromboembolic disease (eg, stroke, MI) or history of these conditions
Hypersensitivity (eg, anaphylaxis, angioedema) to estrogens, bazedoxifene, or any ingredients
Known hepatic impairment or disease
Known protein C, protein S, or antithrombin deficiency or other known thrombophilic disorders
Pregnancy, women who may become pregnant, and nursing mothers; may cause fetal harm when administered to a pregnant woman
FDA has not yet classified the drug into a specified pregnancy category.
Mode of Action
Bazedoxifene: Selective estrogen receptor modulator (SERM); estrogen-like effects on bone (increase bone density) and lipids (decrease LDL); antiestrogenic in uterus and breast (reduces risk of endometrial hyperplasia that can occur with conjugated estrogens)
Conjugated estrogens: Replaces endogenous estrogen
Interaction
N/A
Pregnancy Category Note
Pregnancy
Contraindicated for use in pregnant women; not indicated for use in females of reproductive potential
There are no data with the use of conjugated estrogens in pregnant women; however, epidemiologic studies and meta-analyses have not found an increased risk of genital and non-genital birth defects (including cardiac anomalies and limb-reduction defects) following exposure to combined hormonal contraceptives before conception or during early pregnancy
There are no available data on bazedoxifene use in pregnant women to inform a drug associated risk of adverse developmental outcomes
Based on animal data, bazedoxifene administration may adversely affect female fertility; ;owever, clinical fertility studies with bazedoxifene not conducted
Animal data
Animal studies have shown that oral bazedoxifene administered during period of organogenesis to pregnant rats or rabbits at 0.3 and 2 times, respectively, exposure at maximum recommended dose, can cause fetal harm; based on mechanism of action, bazedoxifene may block important functions that estrogen has during all stages of pregnancy
Lactation
Not indicated for use in females of reproductive potential
Estrogens are present in human milk and can reduce milk production in breast-feeding females; this reduction can occur at any time but is less likely to occur once breast-feeding is well-established
There are no data on presence of bazedoxifene in either human or animal breast milk, effect on breastfed infant, or on milk production; based on mechanism of action, bazedoxifene may block important functions that estrogen has in mammary tissue during lactation
Adult Dose
Oral
Menopausal Vasomotor Symptoms
Indicated for vasomotor symptoms associated with menopause
20 mg/0.45 mg (1 tablet) once daily
Osteoporosis
Indicated for prevention of postmenopausal osteoporosis
20 mg/0.45 mg (1 tablet) once daily
Hepatic impairment: Contraindicated
Child Dose
N/A
Renal Dose
Renal impairment: Not evaluated, and therefore not recommended
Administration
May take with or without food
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The information provided herein are for informational purposes only and not intended to be a substitute for professional medical advice, diagnosis, or treatment. Please note that this information should not be treated as a replacement for physical medical consultation or advice. Great effort has been placed to provide accurate and comprehensive data. However, Medicart along with its authors and editors make no representations or warranties and specifically disclaim all liability for any medical information provided on the site. The absence of any information and/or warning to any drug shall not be considered and assumed as an implied assurance of the Company.