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

Evista

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

(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

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 ?
Previous data have demonstrated that ospemifene inhibits breast cancer cell growth in in vitro cultures as well as experimental animals (6) and inhibits proliferation of human breast tissue epithelial cells, (7) with such breast effects similar to tamoxifen and raloxifene. Thus, although one would not choose ospemifene as a primary treatment, or risk-reducing agent, for breast cancer, the direction of its activity in breast tissue is indisputable and is likely the reason that in the European Union, unlike in the United States, it is approved to treat dyspareunia from VVA of menopause in women with a prior history of breast cancer.
The treatment team decides to consult Endocrinology to further investigate the feasibility of starting raloxifene (Table 3) because of their experience using this medication to manage osteoporosis.
Two of the SERMs, namely, tamoxifen and raloxifene, have shown promising results in bipolar disorder and schizophrenia, respectively.
Raloxifene, ibandronate, and teriparatide have not been shown to reduce the risks of all types of fractures, so they are not recommended as first-line therapy.
Raloxifene can also be given as an alternative for women with a uterus.
When raloxifene made by Eli Lilly under the trade name of Evista entered the market in 1997, its global sales value in the first year reached up to 285 million, making it the second most successful product of Eli Lilly.
Prevention is an important tool in the fight against breast cancer, and two drugs--tamoxifen (Nolvadex) and raloxifene (Evista)--are currently first-line weapons in that war.
24, 2014, 1 year after the USPSTF first issued a "B" rating also, for use of the selective estrogen receptor modulators, tamoxifen, or raloxifene for women at high-risk for breast cancer and low risk for side effects.
Experimental group 1 ([C.sub.1]) : Amount of drug was based on their weight, they received 30 mg raloxifene tablet dissolved in 1 ml of distilled water.
The drug, either in the form of tamoxifen or raloxifene, could help more than 488,000 women in England and Wales dramatically slash their risk of breast cancer.