raloxifene
ra·lox·i·fene
R5033600 (rə-lŏk′sĭ-fēn′)ra•lox•i•fene
(rəˈlɒk səˌfin)n.
n.
raloxifene
raloxifene
[ral-ok´sĭ-fēn]raloxifene
Pharmacologic class: Nonsteroidal benzothiophene derivative
Therapeutic class: Selective estrogen receptor modulator, bone resorption inhibitor
Pregnancy risk category X
Action
Binds to estrogen receptors, activating estrogen pathways and increasing bone mineral density. These effects decrease bone resorption and turnover.
Availability
Tablets: 60 mg
Indications and dosages
➣ Treatment and prevention of osteoporosis in postmenopausal women; reduction of invasive breast cancer risk in postmenopausal women with osteoporosis; reduction of invasive breast cancer risk in postmenopausal women at high risk for invasive breast cancer
Adults: 60 mg P.O. daily
Off-label uses
• Prophylaxis of cardiovascular disease
Contraindications
• Hypersensitivity to drug or its components
• History of thromboembolic events
• Premenopausal women
• Females of childbearing age
• Pregnancy or breastfeeding
• Children
Precautions
Use cautiously in:
• altered lipid metabolism, hepatic dysfunction
• concurrent estrogen therapy (use not recommended)
• immobilized patients and others at increased risk for thromboembolic events.
Administration
• Give with or without food.
Adverse reactions
CNS: depression, insomnia, vertigo, syncope, hypoesthesia, migraine, neuralgia
CV: chest pain, peripheral edema, varicose veins, deep-vein thrombosis, thrombophlebitis
EENT: conjunctivitis, sinusitis, rhinitis, pharyngitis, laryngitis
GI: nausea, vomiting, diarrhea, abdominal pain dyspepsia, flatulence, gastroenteritis
GU: urinary tract infection or disorder, cystitis, vaginitis, leukorrhea, endometrial disorder, vaginal hemorrhage
Musculoskeletal: leg cramps, joint pain, myalgia, arthritis, tendon disorder
Respiratory: cough, pneumonia, bronchitis, pulmonary embolism
Skin: rash, diaphoresis
Other: weight gain, hot flashes, infection, pain, flulike symptoms
Interactions
Drug-drug. Cholestyramine: reduced raloxifene absorption
Highly protein-bound drugs (such as diazepam, diazoxide, lidocaine): interference with binding of these drugs
Warfarin: decreased prothrombin time
Drug-diagnostic tests. Albumin, apolipoprotein B, calcium, fibrinogen, inorganic phosphate, low-density lipoproteins, platelets, protein, total cholesterol: decreased levels
Apolipoprotein A1; corticosteroid-binding, sex steroid-binding, and thyroid-binding globulin: increased levels
Patient monitoring
See Watch for thromboembolic events, especially during first 4 months of therapy.
• Stay alert for other adverse effects, particularly leg cramps, other musculoskeletal complaints, and respiratory disorders.
• Assess bone mineral density test results.
• Monitor for unexplained vaginal bleeding.
Patient teaching
• Tell patient she may take with or without food.
• Instruct patient to read package insert before starting drug and then periodically.
See Teach patient to recognize and immediately report symptoms of blood clots.
• Instruct patient to stop taking drug 3 days before anticipated period of prolonged immobility, and to restart it only after she regains normal mobility.
• Tell patient that drug may cause hot flashes, but that these are normal effects.
• Advise patient to report unexplained vaginal bleeding or leg cramps.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.
ral·ox·i·fene
(ral-ox'ĭ-fēn),Raloxifene is a benzothiophene derivative that binds to estrogen receptor sites. Besides conferring protection against osteoporosis after menopause, it has been shown to improve bone mineral density and reduce the risk of fractures in established osteoporosis. The reduction in fracture risk is greater than would be expected from the increase in bone density. Unlike tamoxifen, which also reduces osteoporosis risk, raloxifene does not heighten the risk of endometrial cancer. Although raloxifene increases bone mineral density to a lesser degree than estrogen, it reduces the risk of breast cancer rather than increasing it as estrogen does. Hence it may be preferred for women who fear breast cancer or are at high risk for it. Like hormone replacement therapy with estrogen-progestogen, raloxifene decreases LDL cholesterol, fibrinogen, and lipoprotein Lp(a), thus increasing HDL cholesterol without raising triglycerides. It has no effect on the risk of adverse cardiovascular events (myocardial infarction, unstable angina, stroke) in women at normal risk before therapy, but significantly reduces the risk of adverse outcomes in women with a prior history of myocardial infarction, coronary artery bypass graft, or percutaneous transluminal coronary angioplasty, and in those with several risk factors combined (for example, diabetes mellitus, hyperlipidemia, hypertension, cigarette smoking). Raloxifene does not relieve hot flashes; in fact, it causes them in 25% of patients. It is contraindicated in pregnancy and in women with a history of thromboembolism.