estrogens conjugated/bazedoxifene

Adult Dosing

Moderate to severe vasomotor symptoms associated with menopause

1 tab PO Daily

Prevention of postmenopausal osteoporosis

1 tab PO Daily

Note:

Women taking therapy for prevention of postmenopausal osteoporosis should consider supplemental calcium and/or vitamin D to their diet if daily intake is inadequate
If a dose is missed, take it as soon as remembered unless it is almost time for the next scheduled dose; do not take 2 doses at the same time

Pediatric Dosing

Safety and effectiveness in pediatric patients have not been established

[Outline]

Adult Dosing
Pediatric Dosing

Indications ⬆ ⬇

Treament of moderate to severe vasomotor symptoms associated with menopause
Prevention of postmenopausal osteoporosis

Note:

Therapy is only indicated in women with uterus

Contraindications ⬆ ⬇

Hypersensitivity to any of the ingredients of the product
Undiagnosed abnormal uterine bleeding
Known, suspected, or past history of breast cancer
Known or suspected estrogen-dependent neoplasia
Active deep venous thrombosis, pulmonary embolism, or hx
Active arterial thromboembolic disease or hx
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
Women > 75 years

Black Box Warnings ⬆ ⬇

Do not take additional estrogens with the therapy
Increased risk of endometrial cancer has been reported in women with a uterus who uses unopposed estrogens. Therapy decreases the risk of endometrial hyperplasia, which may be a precursor to endometrial cancer. Adequate diagnostic measures, especially random endometrial sampling should be considered to rule out malignancy in postmenopausal women with undiagnosed persistent or recurring abnormal genital bleeding
Estrogen therapy is contraindicated for prevention of cardiovascular disease or dementia
Increased risk of stroke and DVT in postmenopausal women has been reported in Women’s Health Initiative (WHI) estrogen-alone substudy during 7.1 years of treatment with daily oral conjugated estrogens at dose 0.625 mg alone, relative to placebo
Increased risk of probable dementia in postmenopausal women >65 yrs have been reported with WHI Memory Study (WHIMS) estrogen-alone ancillary study of the WHI during 5.2 years of treatment with daily conjugated estrogens at dose 0.625 alone, relative to placebo. It is not known whether this finding applies to younger postmenopausal women
Estrogens should be prescribed at the lowest effective doses and for the shortest duration consistent with treatment goals and risks for the individual woman

Dosing Adjustment ⬆ ⬇

Renal Dose Adjustment

Renal impairment: Dose adjustments not defined

Hepatic Dose Adjustment

Hepatic impairment: Contraindicated

Warnings/Precautions ⬆ ⬇

Do not take drugs containing progestins, additional estrogens, or additional estrogen agonist/antagonists while on therapy (US Black Box Warning)
Cardiovascular disorders, including venous thromboembolism, pulmonary embolism, stroke, coronary heart disease and retinal vascular thrombosis have been reported with therapy. Discontinue the therapy 4-6 weeks before surgery that is associated with increased risk of thromboembolism, or during periods of prolonged immobilization
Malignant neoplasms, including endometrial cancer, breast cancer, and ovarian cancer have been occured with therapy
Women with BMI >27 may have an increased risk of endometrial hyperplasia
Risk of gallbladder disease requiring surgery is reported in postmenopausal women receiving estrogens
Retinal vascular thrombosis has been reported in patients receiving estrogens, Consider discontinuation of medication if there is sudden partial or complete loss of vision, proptosis, diplopia, or migraine. If the eye examination reveals papilledema or retinal vascular lesions, then discontinue permanently
Rare cases of substantial increases in blood pressure have been reported with therapy
Estrogens may elevate levels of plasma triglycerides in women with pre-existing hypertriglyceridemia leading to pancreatitis. Discontinue if this develops.
Estrogen administration leads to increased thyroid-binding globulin (TBG) levels; hence women dependent on thyroid hormone replacement therapy who are also receiving estrogens may require increased thyroid hormone doses, therefore such women should monitor for thyroid function to maintain their free thyroid hormone levels
Drug may cause fluid retention, hence therapy should be carefully prescribed in patients with cardiac dysfunction or renal impairment
Therapy may worsen symptoms of angioedema in women with hereditary angioedema
Therapy may worsen asthma, diabetes mellitus, epilepsy, migraine/porphyria, systemic lupus erythematosus, and hepatic hemangiomas and should be used cautiously with these conditions

Cautions: Use cautiously in :

History of cholestatic jaundice
Hypoparathyroidism
Asthma
Diabetes mellitus
Epilepsy
Migraine
Porphyria
Systemic lupus erythematosus
Hepatic hemangiomas

Pregnancy/Breast Feeding ⬆ ⬇

Pregnancy Category:X

Breastfeeding: Safety unknown

Adverse Reactions ⬆ ⬇

CNS:Dizziness
GI: Nausea, diarrhea, dyspepsia, upper abdominal pain, oropharyngeal pain
MUSC: Muscle spasms, neck pain

Clinical Pharmacology ⬆ ⬇

Bazedoxifene

Selective estrogen receptor modulator; is an estrogen agonist/antagonist that acts as an agonist in some estrogen-sensitive tissues and an antagonist in others (e.g., uterus)
Metabolized by liver, glucuronidation major metabolic pathway
Excreted in feces (85%) and urine ( <1%)
Half-Life: 30 hours.

Conjugated estrogens

Steroids and steroid derivatives; enter the cells of responsive tissues and interact with protein receptor, and subsequently increases the rate of synthesis of DNA, RNA, and some proteins
Metabolized by liver
Excreted in urine
Half-Life: 17 hours

Brands and Availability ⬆ ⬇