RaloxifeneRx

Trade Names: Evista

Drug Class: Selective estrogen receptor modulator

Preparations: 60-mg tablet

Dose/Administration: Osteoporosis: 60 mg  by mouth daily

Indications: Treatment and prevention of osteoporosis in postmenopausal women; reduction in risk of invasive breast cancer in high risk women

Mechanism of Action: Acts on some estrogen receptors and blocks others; acts as an estrogen receptor agonist to prevent bone loss

Contraindications: Pregnancy or planned pregnancy (not intended for use in premenopausal women), hypersensitivity, history of thromboembolism including DVT, pulmonary embolism, retinal vein thrombosis

Precautions: Increased risk of thromboembolism, renal or hepatic impairment, may increase triglycerides, increased risk of stroke in women with coronary heart disease

Pregnancy Risk: X

Adverse Effects
Common: Hot flashes, arthralgia, edema
Less Common: Fever, migraine, insomnia, myalgia, cramps, thromboembolism, thrombophlebitis, pulmonary embolism, hypertriglyceridemia

Drug Interactions
Cholestyramine: decreased raloxifene concentrations
Estrogens: avoid

Patient Instructions: Increased risk of blood clots.

Comments: Selective estrogen receptor modulators such as raloxifene preferentially act on estrogen receptors outside the uterus and breast. Raloxifene, unlike estrogens, does not increase the risk of breast cancer; in fact, it reduced the risk. Unlike hormone replacement therapy, hot flashes do not improve; they may get worse. Calcium and vitamin D supplemented if intake inadequate. Greater effect on vertebral than non-vertebral fracture risk.

Clinical Pharmacology: Absorbed (60%) but rapidly glucuronidated so that oral bioavailability is poor (2%). Extensive hepatic metabolism; half-life 30 hours.

Cost: $$$$