RALOXIFENE HYDROCHLORIDE
(ra-lox'i-feen)
Evista
Classifications: hormone and synthetic substitute; selective estrogen receptor antagonist/agonist
Prototype: Tamoxifen
Pregnancy Category: X

Availability

60 mg tablets

Actions

Tamoxifen analog that exhibits selective estrogen receptor antagonist activity on uterus and breast tissue. Prevents tissue proliferation in both sites. Decreases bone resorption and increases bone density. Decreases serum total cholesterol and LDL cholesterol without lowering HDL cholesterol or triglycerides.

Therapeutic Effects

Indicated by increased bone mineral density, lowers serum total cholesterol and LDL cholesterol.

Uses

Prevention and treatment of osteoporosis in postmenopausal women.

Contraindications

Active thromboembolic event; hypersensitivity to raloxifene; pregnancy (category X), lactation, children.

Cautious Use

Concurrent use of raloxifene and estrogen hormone replacement therapy and lipid-lowering agents.

Route & Dosage

Prevention or Treatment of Osteoporosis
Adult: PO 60 mg q.d.

Administration

Oral

Adverse Effects (1%)

Body as a Whole: Infection, flu-like syndrome, leg cramps, fever, arthralgia, myalgia, arthritis. CNS: Migraine headache, depression, insomnia. CV: Hot flashes, chest pain, peripheral edema, decreased serum cholesterol. GI: Nausea, dyspepsia, vomiting, flatulence, GI disorder, gastroenteritis, weight gain. Respiratory: Sinusitis, pharyngitis, cough, pneumonia, laryngitis. Skin: Rash, sweating. Urogenital: Vaginitis, UTI, cystitis, leukorrhea, endometrial disorder, breast pain, vaginal bleeding.

Interactions

Drug: Concomitant use of estrogens not recommended; absorption reduced by cholestyramine.

Pharmacokinetics

Absorption: 60% absorbed, absolute bioavailability 2%. Metabolism: Extensive first-pass metabolism in liver. Elimination: Excreted primarily in feces. Half-Life: 27.7–32.5 h.

Nursing Implications

Assessment & Drug Effects

Patient & Family Education


Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug