Drug Guide
Bazedoxifene Acetate; Estrogens, Conjugated
Classification
Therapeutic: Hormone Modulator / Estrogen Therapy
Pharmacological: Selective Estrogen Receptor Modulator (SERM) / Estrogen receptor agonist
FDA Approved Indications
- Prevention of osteoporosis in postmenopausal women at risk of fracture
- Treatment of moderate to severe vasomotor symptoms associated with menopause (for conjugated estrogens)
Mechanism of Action
Bazedoxifene acts as a selective estrogen receptor modulator (SERM), exerting estrogen-agonistic effects on bone and lipid metabolism and antagonistic effects on the uterine tissue, thereby reducing the risk of endometrial hyperplasia. Conjugated estrogens supply estrogenic activity to alleviate menopausal symptoms and prevent osteoporosis.
Dosage and Administration
Adult: One tablet daily (containing 20 mg bazedoxifene and 0.45 mg conjugated estrogens)
Pediatric: Not indicated
Geriatric: No specific dose adjustment; use with caution in older patients
Renal Impairment: No specific adjustment needed
Hepatic Impairment: Use caution; no specific dose adjustment, but hepatic function should be monitored
Pharmacokinetics
Absorption: Well absorbed orally with food recommended
Distribution: Bound primarily to serum albumin
Metabolism: Extensively metabolized in the liver via conjugation, hydroxylation, and glucuronidation
Excretion: Excreted primarily in feces and urine
Half Life: Approximately 20 hours for bazedoxifene; conjugated estrogens half-life varies
Contraindications
- History of venous thromboembolism (VTE)
- Known or suspected estrogen-dependent neoplasia
- Undiagnosed abnormal genital bleeding
- Pregnancy
Precautions
- History of liver disease, coagulopathy, smoking, cardiovascular disease; monitor for hypertension, VTE, and other thromboembolic events
Adverse Reactions - Common
- Hot flashes (Common)
- Leg cramps (Common)
- Nausea (Common)
Adverse Reactions - Serious
- Venous thromboembolism (Less common)
- Endometrial hyperplasia or carcinoma (if not prescribed with progestin) (Rare)
- Stroke or cardiovascular events (Rare)
Drug-Drug Interactions
- Other estrogenic or anti-estrogenic agents
- Anticoagulants
- Benzodiazepines
Drug-Food Interactions
N/ADrug-Herb Interactions
N/ANursing Implications
Assessment: Monitor for signs of thromboembolism, cardiovascular issues, and abnormal bleeding.
Diagnoses:
- Risk for thromboembolic events
- Impaired uterine bleeding
Implementation: Administer orally, preferably with meals. Educate patient on symptoms of thromboembolism.
Evaluation: Assess for adverse effects, symptom management, and osteoporosis risk reduction.
Patient/Family Teaching
- Take medication exactly as prescribed.
- Report symptoms of blood clots (leg swelling, chest pain, sudden headache).
- Maintain regular follow-up appointments.
- Discuss risks and benefits of therapy.
Special Considerations
Black Box Warnings:
- Increased risk of thromboembolic events (DVT, PE, stroke)
Genetic Factors: None specific
Lab Test Interference: May affect liver function tests and lipid panels
Overdose Management
Signs/Symptoms: Nausea, vomiting, abdominal pain, bleeding, thromboembolic events
Treatment: Supportive care, symptomatic treatment, anticoagulation therapy if indicated, contact poison control.
Storage and Handling
Storage: Store at room temperature, away from moisture and light
Stability: Stable for 24 months when stored properly