raloxifene

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raloxifene

 [ral-ok´sĭ-fēn]
a selective estrogen receptor modulator that has estrogenlike effects on bone, increasing bone mineral density, and lipid metabolism, lowering total and LDL cholesterol; it has no effect on breast or uterine tissue. Administered orally as the hydrochloride salt for the prevention of postmenopausal osteoporosis.

raloxifene

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

Treatment and prevention of osteoporosis in postmenopausal women; reduction of invasive breast cancer risk in postmenopausal women with osteoporosis; reduction of invasive breast cancer risk in postmenopausal women at high risk for invasive breast cancer

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.

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.

ral·ox·i·fene

(ral-ox'ĭ-fēn),
A selective estrogen receptor modulator (SERM) that has estrogen-agonistic effects on bone and lipid metabolism but estrogen-antagonistic effects on breast and uterus; used in the prophylaxis of osteoporosis after menopause.

Raloxifene is a benzothiophene derivative that binds to estrogen receptor sites. Besides conferring protection against osteoporosis after menopause, it has been shown to improve bone mineral density and reduce the risk of fractures in established osteoporosis. The reduction in fracture risk is greater than would be expected from the increase in bone density. Unlike tamoxifen, which also reduces osteoporosis risk, raloxifene does not heighten the risk of endometrial cancer. Although raloxifene increases bone mineral density to a lesser degree than estrogen, it reduces the risk of breast cancer rather than increasing it as estrogen does. Hence it may be preferred for women who fear breast cancer or are at high risk for it. Like hormone replacement therapy with estrogen-progestogen, raloxifene decreases LDL cholesterol, fibrinogen, and lipoprotein Lp(a), thus increasing HDL cholesterol without raising triglycerides. It has no effect on the risk of adverse cardiovascular events (myocardial infarction, unstable angina, stroke) in women at normal risk before therapy, but significantly reduces the risk of adverse outcomes in women with a prior history of myocardial infarction, coronary artery bypass graft, or percutaneous transluminal coronary angioplasty, and in those with several risk factors combined (for example, diabetes mellitus, hyperlipidemia, hypertension, cigarette smoking). Raloxifene does not relieve hot flashes; in fact, it causes them in 25% of patients. It is contraindicated in pregnancy and in women with a history of thromboembolism.

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.

raloxifene

(rə-lŏk′sĭ-fēn′)
n.
A selective estrogen receptor modulator, C28H27NO4S, used in the form of its hydrochloride primarily to treat and prevent osteoporosis in postmenopausal women.

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.

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.

ral·ox·i·fene

(ră-lox'i-fēn)
A selective estrogen receptor modulator (SERM) that has estrogen-agonistic effects on bone and lipid metabolism but estrogen-antagonistic effects on breast and uterus; used in the prophylaxis of osteoporosis after menopause.

raloxifene

A non-steroidal selective oestrogen receptor modulator drug that produces oestrogen antagonist effects in some tissues and oestrogen agonist effects in others. There are at least two different oestrogen receptors and the proportions of these differ in different tissues. It is hoped that raloxifene may be useful in breast cancer and osteoporosis without raising the risk of coronary heart disease

ral·ox·i·fene

(răl-ox'i-fēn)
Selective estrogen receptor modulator with estrogen-agonistic effects on bone and lipid metabolism.
References in periodicals archive ?
Raloxifene hydrochloride, a selective estrogen receptor modulator: Safety assessment of effects on cognitive function and mood in postmenopausal women.
The patent protecting the dosing regimen of administering 60 mg/day Raloxifene hydrochloride in the treatment and prevention of osteoporosis is considered to further constrain generic entry until March 2014.
Raloxifene hydrochloride is the active ingredient in Evista[R], Eli Lilly's immediate release tablets for osteoporosis.
Food and Drug Administration (FDA) seeking approval to market a raloxifene hydrochloride tablet.
Raloxifene hydrochloride is the active ingredient in Evista(R), Eli Lilly's immediate release tablets for osteoporosis.
Raloxifene hydrochloride is the active ingredient in Evista(R), Eli Lilly and Company's immediate release tablets for osteoporosis.
In addition to CDT-based raloxifene hydrochloride, we also previously announced that we are initiating development of a CDT-based ondansetron hydrochloride formulation.
Barr filed an ANDA for Raloxifene Hydrochloride 60 mg tablets with the U.