Trade Names:Evista- Tablets 60 mg
Actions mediated largely through binding to estrogen receptors, which results in activation of certain estrogenic pathways and blockade of others. Appears to act as an estrogen agonist in bone. Decreases bone resorption and turnover, increases bone mineral density.
Absorbed rapidly after oral administration. Bioavailability is 2%.
Vd is 2348 L/kg. Protein binding is 95%. Binds albumin and alpha-1 acid glycoprotein.
Extensive first-pass metabolism to glucuronide conjugates.
Primarily excreted in feces. Less than 0.2% is excreted unchanged in urine. Cl (oral) is 44.1 L/kg•h and half-life is 27.7 to 32.5 h. Chronic dosing Cl is 40 to 60 L/kg•h.
Raloxifene concentrations are elevated in renal impairment. Use with caution.Hepatic Function Impairment
Raloxifene Cl is reduced in patients with hepatic impairment; the pharmacokinetics were not studied in patients with moderate or severe hepatic impairment. Use with caution.Elderly
No differences in pharmacokinetics were found in the age range 42 to 84 yr.Gender
No differences in pharmacokinetics between men and women.Race
No differences in pharmacokinetics have been identified based on race.Cirrhosis
Plasma concentrations increase 2.5 times. Safety and efficacy have not been evaluated any further.
For the prevention and treatment of osteoporosis in postmenopausal women; reduction in the risk of invasive breast cancer in postmenopausal women with osteoporosis; reduction in the risk of invasive breast cancer in postmenopausal women at high risk of invasive breast cancer.
Treatment of uterine leiomyomas; treatment of pubertal gynecomastia; prevention of bone loss in men with prostate cancer.
Women who are or may become pregnant; breast-feeding mothers; women with active or history of venous thromboembolic events, including deep vein thrombosis (DVT), pulmonary embolism, and retinal vein thrombosis; allergy to raloxifene or other constituents of the product.
PO 60 mg every day.
Store at 59° to 86°F.
Major reduction in absorption and enterohepatic cycling of raloxifene; avoid concurrent use.Estrogens
Safety and efficacy of coadministration not established; concurrent use is not recommended.Highly protein-bound drugs (eg, clofibrate, diazepam, diazoxide, ibuprofen, indomethacin, naproxen)
May displace raloxifene from protein-binding sites, increasing the effects of raloxifene.Warfarin
Raloxifene may decrease anticoagulant effect.
None well documented.
Hot flashes (29%); migraine, syncope, varicose vein (2%); stroke, venous thromboembolism sometimes fatal (postmarketing).
Headache (9%); depression, insomnia (6%); vertigo (4%); hypesthesia, neuralgia (2%).
Rash (6%); sweating (3%).
Pharyngitis (7%); conjunctivitis, laryngitis (2%); retinal vein occlusion (postmarketing).
Nausea (9%); abdominal pain, diarrhea (7%); dyspepsia (6%); vomiting (5%); flatulence, gastroenteritis, GI disorder (3%).
Cystitis (5%); breast pain, UTI, vaginal bleeding, vaginitis (4%); endometrial disorder, leucorrhea, urinary tract disorder, uterine disorder, vaginal hemorrhage (3%).
Weight gain (9%); peripheral edema (5%).
Arthralgia (16%); myalgia (8%); leg cramps (7%); arthritis, tendon disorder (4%).
Bronchitis, rhinitis, sinusitis (10%); increased cough (9%); pneumonia (3%).
Flu syndrome (15%); infection (11%); chest pain, fever (4%); chest pain (3%).
Increased risk of DVT and pulmonary embolism have been reported. Women with active or past history of venous thrombosis should not take raloxifene.Stroke
The risk of death due to stroke may be increased in postmenopausal women with documented coronary heart disease or at increased risk of major coronary events.
Monitor triglyceride plasma levels in women with a history of marked hypertriglyceridemia in response to treatment with oral estrogen or estrogen plus progestin.
Category X .
Contraindicated in breast-feeding women.
Safety and efficacy not established.
No overall differences in safety and efficacy have been reported between patients older than 65 yr of age and younger subjects.
Use with caution in patients with moderate or severe renal impairment.
Use with caution in patients with hepatic impairment.
Investigate any unexplained breast abnormality during therapy.
Not for use for the primary or secondary prevention of CV disease.
Concurrent use with systemic estrogens is not recommended.
Raloxifene has not been adequately studied in women with history of breast cancer.
Women with a history of marked hypertriglyceridemia in response to treatment with oral estrogen or estrogen plus progestin may develop increased triglyceride levels with raloxifene therapy.
Safety and efficacy not established. Use is not recommended.
Safety and efficacy not established.
Increased risk of thromboembolic events.
Dizziness, leg cramps.
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