Bazedoxifene/​Conjugated Estrogens

DEA Class; Rx

Common Brand Names; Duavee

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

Should not take progestins, additional estrogens, or additional estrogen agonist/antagonists

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

Absolute risk of dementia with estrogen-alone use vs placebo from the Women’s Health Initiative was 37 versus 25 cases per 10,000 women-years; relative risk was 1.49 A 2- to 4-fold risk of gallbladder disease requiring surgery is reported in postmenopausal women receiving estrogens

Retinal vascular thrombosis reported

Substantial increases in blood pressure described in a small number of case reports in women receiving estrogens; this effect was not observed in a large, randomized, placebo-controlled clinical study

Estrogens may exacerbate pre-existing hypertriglyceridemia and lead to pancreatitis

Caution with history of cholestatic jaundice associated with past estrogen use or with pregnancy

Estrogen administration leads to increased thyroid-binding globulin (TBG) levels; women dependent on thyroid hormone replacement therapy who are also receiving estrogens may require increased thyroid hormone doses; patients dependent on thyroid hormone replacement therapy who are also receiving estrogens may require increased doses of thyroid replacement therapy; these patients should have their thyroid function monitored in order to maintain their free thyroid hormone levels in an acceptable range

May cause fluid retention

May exacerbate asthma, diabetes mellitus, epilepsy, migraine, porphyria, systemic lupus erythematosus, and hepatic hemangiomas

Estrogens are metabolized partially by CYP3A4 and therefore coadministration with inhibitors and inducers of this isoenzyme may increase risk of toxicity or alter therapeutic effect

Bazedoxifene undergoes metabolism by UGT enzymes in the intestinal tract and liver; coadministration with UGT inducers may reduce bazedoxifene exposure/efficacy and therefore increase risk of endometrial hyperplasia

Do not use with conditions that predispose to hyperkalemia

Retinal vascular thrombosis reported in patients receiving estrogens; discontinue medication pending examination if there is sudden partial or complete loss of vision, or a sudden onset of proptosis, diplopia, or migraine; if examination reveals papilledema or retinal vascular lesions, estrogens should be discontinued

There are, possible risks that may be associated with use of progestins with estrogens compared to estrogen-alone regimens, including a possible increased risk of breast cancer, adverse effects on lipoprotein metabolism (e.g., lowering HDL, raising LDL), and impairment of glucose tolerance

Use caution in individuals with severe hypocalcemia

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

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