No

Selective Estrogen Receptor Modulator (SERM)

Prevention and treatment of osteoporosis in postmenopausal women

X

Raloxifene should not be used by pregnant women or by women planning to become pregnant in the immediate future

Pregnancy; prior hypersensitivity to raloxifene; active thromboembolic disorder; not intended for use in premenopausal women

History of venous thromboembolism/pulmonary embolism; patients with cardiovascular disease; history of cervical/uterine carcinoma; renal/hepatic insufficiency (however, pharmacokinetic data are lacking); concurrent use of estrogens

greater than or equal to 2%:

Central nervous system: Migraine, depression, insomnia, fever

Dermatologic: Rash

Endocrine & metabolic: Hot flashes

Gastrointestinal: Nausea, dyspepsia, vomiting, flatulence, gastroenteritis, weight gain

Genitourinary: Vaginitis, urinary tract infection, cystitis, leukorrhea

Neuromuscular & skeletal: Leg cramps, arthralgia, myalgia, arthritis

Respiratory: Sinusitis, pharyngitis, cough, pneumonia, laryngitis

Miscellaneous: Infection, flu syndrome, diaphoresis

Incidence of overdose in humans has not been reported. In an 8-week study of postmenopausal women, a dose of raloxifene 600 mg/day was safely tolerated. No mortality was seen after a single oral dose in rats or mice at 810 times the human dose for rats and 405 times the human dose for mice. There is no specific antidote for raloxifene.

Decreased effects: Ampicillin and cholestyramine decreases raloxifene absorption

A selective estrogen receptor modulator, meaning that it affects some of the same receptors that estrogen does, but not all, and in some instances, it antagonizes or blocks estrogen; it acts like estrogen to prevent bone loss and improve lipid profiles, but it has the potential to block some estrogen effects such as those that lead to breast cancer and uterine cancer

Onset of action: 8 weeks

Distribution: 2348 L/kg

Protein binding: >95% to albumin and a-glycoprotein

Metabolism: Extensive first pass metabolism

Bioavailability: ~2%

Half-life: 27.7-32.5 hours

Elimination: Primarily in the feces and 0.2% renal

Adults: Female: Oral: 60 mg/day which may be administered any time of the day without regard to meals

Radiologic evaluation of bone mineral density (BMD) is the best measure of the treatment of osteoporosis; to monitor for the potential toxicities of raloxifene, complete blood counts should be evaluated periodically.

May cause insomnia or depression

None reported

No information available to require special precautions

No effects or complications reported

May be taken at any time of day without regard to meals. This medication is given to reduce incidence of osteoporosis; it will not reduce hot flashes or flushing. You may experience flu-like symptoms at beginning of therapy (these may resolve with use). Mild analgesics may reduce joint pain. Rest and cool environment may reduce hot flashes. Report fever; acute migraine; insomnia or emotional depression; unusual weight gain; unresolved gastric distress; urinary infection or vaginal burning or itching; chest pain; or swelling, warmth, or pain in calves. Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant. Do not breast-feed.

Tablet, as hydrochloride: 60 mg

Delmas PD, Bjarnason NH, Mitlak BH, et al, "Effects of Raloxifene on Bone Mineral Density, Serum Cholesterol Concentrations, and Uterine Endometrium in Postmenopausal Women," N Engl J Med, 1997, 337(23):1641-7.

Draper MW, Flowers DE, Huster WJ, et al, "A Controlled Trial of Raloxifene (LY139481) HCl: Impact on Bone Turnover and Serum Lipid Profile in Healthy Postmenopausal Women," J Bone Miner Res, 1996, 11(6):835-42.

Heaney RP and Draper MW, "Raloxifene and Estrogen: Comparative Bone-Remodeling Kinetics," J Clin Endocrinol Metab, 1997, 2(10):3425-9.