Dosing and uses of Evista (raloxifene)
Adult dosage forms and strengths
tablet
- 60mg
Osteoporosis in Post-menopausal Women
60 mg PO qDay
Breast Cancer
Prevention; risk reduction of invasive breast cancer in postmenopausal women at high risk for invasive breast cancer
60 mg PO qDay for 5 years
Dosing Modifications
Moderate to severe renal impairment: Caution; safety and efficacy not established
Mild hepatic impairment: Safety and efficacy not established
Dosing Considerations
High risk of breast cancer is defined as at least 1 breast biopsy showing lobular carcinoma in situ (LCIS) or atypical hyperplasia, 1 or more first-degree relatives with breast cancer, or a 5-year predicted risk of breast cancer >1.66% (based on the modified Gail model)
Limitations of use for breast cancer risk reduction
- There are no data available regarding the effect on invasive breast cancer incidence in women with inherited mutations (BRCA1, BRCA2), so specific recommendations on the effectiveness of raloxifene cannot be made
- Not indicated for the treatment of invasive breast cancer or reduction of the risk of recurrence
- Not indicated for reduction in the risk of noninvasive breast cancer
Pediatric dosage forms and strengths
Not recommended
Evista (raloxifene) adverse (side) effects
>10%
Hot flashes (8-29%)
Flu syndrome (14-15%)
Cramps/muscle spasm (6-12%)
Arthralgia (11-16%)
Infection (11%)
1-10%
Insomnia (6%)
Vomiting (5%)
Sinusitis (10%)
Venous thromboembolism (1-2% )
Bronchitis (10%)
Pharyngitis (8%)
Breast pain (4%)
Gastroenteritis (<3%)
Diaphoresis (3%)
Frequency not defined
Deep vein thrombosis
Cerebrovascular accident
Thrombosis of retinal vein (rare)
Pulmonary embolism
Decreased fibrinogen
Warnings
Black box warnings
Increased risk of deep vein thrombosis and pulmonary embolism has been reported with this drug
Women with active or past history of venous thromboembolism should not take this drug
Increased risk of death due to stroke occurred in a trial in postmenopausal women with documented coronary heart disease or at increased risk for major coronary events
Consider risk-benefit balance in women at risk for stroke
Contraindications
Pregnancy, lactation
Active history of thromboembolic disorders
Women who could become pregnant
Cautions
Discontinue 72 hours prior to and during prolonged immobilization
Increased risk of stroke, deep vein thrombosis/pulmonary embolism
Supplemental calcium and vitamin D recommended
Triglyceride levels may increase in women with history of triglyceride elevation in response to oral estrogens
Taper off estrogen treatment, then wait month before starting raloxifene
Examine unexplained uterine bleeding
Concurrent estrogen treatment
Hepatic dysfunction
Premenopausal use not recommended
Pregnancy and lactation
Pregnancy category: X
Lactation: Excretion in milk unknown; contraindicated
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Evista (raloxifene)
Mechanism of action
Selective estrogen receptor modulator; estrogenlike effects on bone (decreases bone resorption; increases bone density) and lipid (decrease in LDL); antiestrogenic in uterus, breast
Absorption
Bioavailability: 2%
Absorption: 60%
Onset: 8 wk
Distribution
Protein bound: >95%
Vd: 2348 L/kg
Metabolism
Extensively undergoes first-pass metabolism in the liver to glucuronide conjugates
Metabolites: Raloxifene-4 glucuronide, raloxifene-6 glucuronide (inactive)
Elimination
Half-life: 27.7-32.5 hr
Excretion: Feces (>93%); urine (<0.2%)
