Raloxifene Hydrochloride
Pronouncation: (ral-OX-ih-FEEN)Class: Selective estrogen receptor modulator
Trade Names:
Evista
- Tablets 60 mg
Pharmacology
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The biological actions of raloxifene are mediated largely through binding to estrogen receptors, which results in activation of certain estrogenic pathways and blockade of others. Raloxifene decreases resorption of bone and reduced biochemical markers of bone turnover to the premenopausal range. Effects on bone are manifested as reductions in the serum and urine levels of bone turnover markers, decreases in bone resorption based on radiocalcium kinetics studies, increases in bone mineral density, and decreases in incidence of fractures. Raloxifene also effects lipid metabolism, decreasing total and LDL cholesterol levels but does not increase triglyceride levels or change total HDL cholesterol levels.
Pharmacokinetics
Absorption
Absorbed rapidly after oral administration. Bioavailability is 2%.
Distribution
Vd is 2348 L/kg. Protein binding is 95%. Binds albumin and alpha-1-acid glycoprotein.
Metabolism
Extensive first pass metabolism to glucuronide conjugates.
Elimination
Primarily excreted in feces. Less than 0.2% is excreted unchanged in urine. Cl (oral) is 44.1 L/kg/h and t ½ is 27.7 to 32.5 h. Chronic dosing Cl is 40 to 60 L/kg/h.
Special Populations
CirrhosisPlasma 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.
Contraindications
Women who are or may become pregnant; women with active or history of venous thromboembolic events, including deep venous thrombosis, pulmonary embolism, and retinal vein thrombosis; allergy to raloxifene or other constituents of the tablet; coadministration of cholestyramine.
Dosage and Administration
Adult womenPO 60 mg every day.
Storage/Stability
Store at controlled room temperature.
Drug Interactions
CholestyramineMajor reduction in absorption and enterohepatic cycling of raloxifene; avoid concurrent use.
Highly protein-bound drugs (eg, clofibrate, indomethacin, naproxen, ibuprofen, diazepam, diazoxide)May displace raloxifene from protein-binding sites, increasing the effects of raloxifene.
WarfarinRaloxifene may decrease anticoagulant effect.
Laboratory Test Interactions
None well documented.
Adverse Reactions
Cardiovascular
Hot flashes.
CNS
Migraine; depression; insomnia.
Dermatologic
Rash; sweating.
EENT
Sinusitis; pharyngitis; laryngitis.
GI
Nausea; dyspepsia; vomiting; flatulence; gastroenteritis; abdominal pain.
Genitourinary
Vaginitis; UTI; cystitis; leukorrhea; endometrial disorder.
Respiratory
Cough; pneumonia.
Miscellaneous
Infection; flu-syndrome; leg cramps; chest pain; fever; weight gain; edema; arthralgia; myalgia; arthritis.
Precautions
Pregnancy
Category X .
Lactation
Undetermined.
Children
Safety and efficacy not established.
Hepatic Function
Safety and efficacy not evaluated in patients with severe hepatic function impairment.
Breast abnormality
Investigate any unexplained breast abnormality during therapy.
Concurrent estrogen therapy
Concurrent use with systemic estrogens is not recommended.
Endometrium
Because raloxifene does not affect endometrial proliferation unexplained uterine bleeding should be investigated as clinically indicated.
History of breast cancer
Raloxifene has not been adequately studied in women with history of breast cancer.
Lipid metabolism
Raloxifene lowers serum total and LDL cholesterol but does not affect total HDL or triglycerides.
Premenopausal use
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.
Patient Information
- 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 if a dose is missed, to start taking the drug on the normal schedule as soon as possible. Do not make up for the missed dose.
- 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: pain in groin or calves; leg swelling; sudden chest pain; shortness of breath or coughing blood; abnormal vaginal bleeding; breast lumps; sudden vision problems.
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Prevention of Osteoporosis, Prevention of Breast Cancer, Osteoporosis
