Pronunciation: ral-OX-i-FEEN HYE-droe-KLOR-ide
Class: Selective estrogen receptor modulator
- 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.
Special PopulationsRenal Function Impairment
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.
Indications and Usage
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.
Dosage and AdministrationAdult women
PO 60 mg every day.
- May be taken any time of day without regard to meals.
- For reduction in risk of invasive breast cancer, the optimum duration of treatment is not known.
- For osteoporosis treatment or prevention, add supplemental calcium and/or vitamin D to the diet if daily intake is inadequate.
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.
Laboratory Test Interactions
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 estrogen therapy
Concurrent use with systemic estrogens is not recommended.
History of breast cancer
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.
Use in men
Safety and efficacy not established.
Venous thromboembolic events
Increased risk of thromboembolic events.
Dizziness, leg cramps.
- Advise patient to read package insert before starting therapy and each time the prescription is refilled.
- Advise patient that drug is taken once a day without regard to meals.
- Advise patient that this drug is for postmenopausal women only. It should not be given to men or premenopausal women to prevent osteoporosis.
- Advise patient that estrogen therapy comes as a pill, patch, or injection, and should not be used in conjunction with this drug.
- Advise patient that drug does not reduce hot flashes and may actually cause hot flashes in women who are closer to menopause.
- Instruct patient to take supplemental calcium (1,500 mg) and vitamin D (400 international units) daily if dietary intake is not adequate.
- Encourage patient to perform weight-bearing exercises and avoid behaviors that promote osteoporosis (eg, alcohol consumption, cigarette smoking).
- Advise patient to avoid prolonged restrictions of movement during travel.
- Advise patient that medication will need to be discontinued 72 h or more prior to any event that would cause prolonged immobilization (eg, postsurgical recovery) and can only be restarted once patient is fully mobile.
- Instruct patient to report the following symptoms to health care provider: abnormal vaginal bleeding, breast lumps, leg swelling, pain in groin or calves, shortness of breath or coughing up blood, sudden chest pain, sudden vision problems.
- Advise patients to have breast exams and mammograms performed before starting therapy and regularly thereafter.
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