raloxifene

raloxifene /ral·ox·i·fene/ (ral-ok´sĭ-fēn) a selective activator of estrogen receptors that increases bone mineral density and decreases total and LDL cholesterol without affecting breast and uterine tissue; used as the hydrochloride salt for the prevention of postmenopausal osteoporosis.

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ra·lox·i·fene (r-lks-fn)

n.

A selective estrogen receptor modulator that acts as both an estrogen agonist and antagonist. It is usually used to treat and prevent osteoporosis in postmenopausal women.

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raloxifene,

a selective estrogen receptor modulator.

indication It is used to prevent osteoporosis in postmenopausal women.

contraindications Pregnancy, lactation, and known hypersensitivity to raloxifene prohibit its use.

adverse effects Adverse effects include insomnia, migraines, depression, hot flashes, diarrhea, anorexia, cramps, vaginitis, urinary tract infection, leukorrhea, endometrial disorder, breast pain, rash, sweating, weight gain, peripheral edema, arthralgia, myalgia, leg cramps, arthritis, sinusitis, pharyngitis, increased cough, pneumonia, and laryngitis. Nausea is a common side effect.

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raloxifene Warning - Hazardous drug!

Evista

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

➣ Osteoporosis in postmenopausal women

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.

Route	Onset	Peak	Duration
P.O.	Unknown	6 hr	Unknown

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

☞ 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.
☞ 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.

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raloxifene

Evista^® Osteoporosis An SERM–selective estrogen receptor modulator, that ↑ bone density–less extensively than estrogen, ↓ total cholesterol and LDL-C, ↓ risk of breast CA;. Cf Tamoxifen Contraindications Pregnancy, nursing, active or prior venous thromboses Pros Lacks estrogenic effects on breast and uterus Adverse effects Hot flashes, leg cramps, DVT, PTE, retinal vein thrombosis. See Calcium channel blocker, MORE, Osteoporosis, STAR. Cf Biphosphonates.