Raloxifene

Pronunciation

(ral OKS i feen)

U.S. Brand Names

Evista®

Synonyms

Keoxifene Hydrochloride; Raloxifene Hydrochloride

Generic Available

Canadian Brand Names

Evista®

Use

Prevention and treatment of osteoporosis in postmenopausal women

Pregnancy Risk Factor

Pregnancy Implications

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

Lactation

Contraindicated

Contraindications

Hypersensitivity to raloxifene or any component of the formulation; active thromboembolic disorder; pregnancy (not intended for use in premenopausal women)

Warnings/Precautions

Use caution in patients with history of or at high risk for 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; women with a history of elevated triglycerides in response to treatment with oral estrogens (or estrogen/progestin). Discontinue at least 72 hours prior to and during prolonged immobilization (postoperative recovery or prolonged bedrest).

Adverse Reactions

Note: Has been associated with increased risk of thromboembolism (DVT, PE) and superficial thrombophlebitis; risk is similar to reported risk of HRT

2%:

Cardiovascular: Chest pain

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

<1%: Hypertriglyceridemia (in women with a history of increased triglycerides in response to oral estrogens)

Postmarketing and/or case reports: Retinal vein occlusion

Overdosage/Toxicology

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.

Drug Interactions

Decreased effects: Ampicillin and cholestyramine decreases raloxifene absorption

Ethanol/Nutrition/Herb Interactions

Ethanol: Avoid ethanol (may increase risk of osteoporosis).

Mechanism of Action

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 (decreases total and LDL-cholesterol but does not raise triglycerides), but it has the potential to block some estrogen effects such as those that lead to breast cancer and uterine cancer

Pharmacodynamics/Kinetics

Onset of action: 8 weeks

Absorption: ~60%

Distribution: 2348 L/kg

Protein binding: >95% to albumin and -glycoprotein

Metabolism: Extensive first-pass effect

Bioavailability: ~2%

Half-life elimination: 27.7-32.5 hours

Excretion: Primarily feces; urine (0.2%)

Dosage

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

Monitoring Parameters

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.

Patient Education

Inform prescriber of all prescriptions, OTC medications, or herbal products you are taking, and any allergies you have. Do not take any new medication during therapy unless approved by prescriber. Avoid alcohol (ethanol may increase risk of osteoporosis). 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 menopausal hot flashes or flushing (cool environment may reduce hot flashes). May cause flu-like symptoms at beginning of therapy (these will resolve with use); GI disturbances (eg, nausea, vomiting, dyspepsia - small, frequent meals, frequent mouth care, chewing gum, or sucking lozenges may help); or joint pain (consult prescriber for approved analgesic). Report immediately any pain, redness, warmth, or cramping in leg muscles; sudden chest pain; or respiratory difficulty. Report fever, acute migraine, insomnia or emotional depression, unusual weight gain (>5 lb/week), unresolved gastric distress, urinary infection or vaginal burning or itching, or unusual cough. Pregnancy/breast-feeding precautions: Inform prescriber if you are pregnant. For use in postmenopausal women only. Do not breast-feed.

Additional Information

The decrease in estrogen-related adverse effects with the selective estrogen-receptor modulators in general and raloxifene in particular should improve compliance and decrease the incidence of cardiovascular events and fractures while not increasing breast cancer.

Dental Health: Effects on Dental Treatment

No significant effects or complications reported

Dental Health: Vasoconstrictor/Local Anesthetic Precautions

No information available to require special precautions

Mental Health: Effects on Mental Status

May cause insomnia or depression

Mental Health: Effects on Psychiatric Treatment

None reported

Dosage Forms

Tablet, as hydrochloride: 60 mg

References

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.

International Brand Names

Biofem® (AR); Bonmax® (IN); Celvista® (TH); Ciclotran® (AR); Evista® (AR, AT, AU, BE, BR, CA, CH, CL, CO, CR, CZ, DE, DK, DO, ES, FI, FR, GB, GT, HN, HR, HU, ID, IE, IL, IT, MX, NL, NO, NZ, PA, PH, PL, PT, RO, RU, SE, SG, SI, SV, TR, TW, YU, ZA); Ketidin® (AR); Optruma® (DE, ES, FI, FR, IT, PT); Raxeto® (AR)

A.D.A.M., Inc. is accredited by URAC, also known as the American Accreditation HealthCare Commission (www.urac.org). URAC's accreditation program is the first of its kind, requiring compliance with 53 standards of quality and accountability, verified by independent audit. A.D.A.M. is among the first to achieve this important distinction for online health information and services. Learn more about A.D.A.M.'s editorial process . A.D.A.M. is also a founding member of Hi-Ethics (www.hiethics.com) and subscribes to the principles of the Health on the Net Foundation (www.hon.ch).

The information provided herein should not be used during any medical emergency or for the diagnosis or treatment of any medical condition. A licensed medical professional should be consulted for diagnosis and treatment of any and all medical conditions. Call 911 for all medical emergencies. Links to other sites are provided for information only -- they do not constitute endorsements of those other sites. © 1997-2007 A.D.A.M., Inc. Any duplication or distribution of the information contained herein is strictly prohibited.

Home > Medical Reference > Complementary Medicine