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CLASSIFICATION(S): Antineoplastic, hormone PREGNANCY CATEGORY: D Rx: Arimidex.

USES (1) First-line treatment in postmenopausal women with advanced or locally advanced breast cancer whose disease is hormone receptor positive or hormone receptor unknown. (2) Advanced breast cancer in postmenopausal women with progression of the disease following tamoxifen therapy. (3) Adjuvant treatment of postmenopausal early breast cancer that is hormone receptor positive. NOTE: Clients with negative tumor estrogen receptors and those who do not respond to tamoxifen are rarely helped by anastrozole. ACTION/KINETICS Action Growth of many breast cancers is due to stimulation of estrogen receptors by estrogens. In postmenopausal women the main source of circulating estrogen is conversion of androstenedione to estrone by aromatase in peripheral tissues with further conversion to estradiol. Anastrozole is a nonsteroidal aromatase inhibitor that significantly decreases serum estradiol levels. Has no effect on formation of adrenal corticosteroids or aldosterone. Pharmacokinetics Well absorbed from the GI tract; food does not affect the extent of absorp1 tion. t /2, terminal: About 50 hr in postmenopausal women. Steady-state levels reached in about 7 days of once daily dosing. Metabolized by the liver and both unchanged drug (about 10%) and metabolites are excreted through the urine. Plasma protein binding: 40%. SPECIAL CONCERNS Causes changes in circulating levels of progesterone, androgen, and estro-

gens. Use with caution during lactation. Safety and efficacy have not been determined in children. SIDE EFFECTS Most Common GI disturbances, hot flashes, vasodilation, nausea, asthenia, back pain, pain, peripheral edema, bone pain, increased cough, dyspnea, headache. GI: N&V, diarrhea, constipation, abdominal pain, anorexia, dry mouth, increased appetite, GI disturbances, anorexia, GI disorder, dyspepsia. CNS: Headache, paresthesia, dizziness, depression, somnolence, confusion, insomnia, anxiety, nervousness, hypertonia, lethargy, mood disturbances. CV: Hypertension, vasodilation, ischemic CV disease, venous thromboembolic events, DVT events, ischemic CV event, MI, angina pectoris, hypertension, thrombophlebitis. Musculoskeletal: Asthenia, back/bone pain, myalgia, arthralgia, arthrosis, arthritis, osteoporosis, joint pain/stiffness, pathological fracture, fracture (hip, spine, wrist). Respiratory: Dyspnea, increased cough, pharyngitis, sinusitis, bronchitis, rhinitis. Dermatologic: Hot flushes, rash, sweating, hair thinning, pruritus, erythema multiforme, Stevens-Johnson syndrome (rare). GU: Vaginal hemorrhage, UTI, breast pain, vaginal dryness, vaginal bleeding during first few weeks after changing from hormone therapy, breast pain, vulvovaginitis, vaginal discharge, endometrial cancer. Hematologic: Anemia, leukopenia, leukorrhea. Body as a whole: Pain, edema, weight gain or loss, flu syndrome, fever, asthenia, malaise, accidental injury, infection. Miscellaneous: Peripheral edema, lymphedema, pelvic/chest/neck pain, infection, tumor flare, increased appetite, cataracts. LABORATORY TEST CONSIDERATIONS GGT, AST, ALT, alkaline phosphatase, total and LDL cholesterol. HOW SUPPLIED Tablets: 1 mg. DOSAGE TABLETS First-line treatment of advanced or locally advanced breast cancer. AdIV = Intravenous

C = see color insert

H = Herbal

E = sound alike drug

or 3 hr after meals. Consume fluids; ensure adequate hydration. 2. Drug works by lowering blood estradiol concentrations, which may decrease size and growth of the tumor 3. Use reliable birth control; may cause fetal harm and impair fertility. 4. Drug may cause dizziness; alcohol or certain medicines may worsen these symptoms. Report unusual side effects, increased SOB/pain. 5. May experience vaginal bleeding esp. during first two weeks of change over from other hormonal therapy; report continued bleeding immediately. May experience rash, hot flashes, itching, and skin lesions. 6. Keep all F/U to evaluate response to therapy and adverse SE. OUTCOMES/EVALUATE Control of malignant cell proliferation

vanced breast cancer following tamoxifen therapy. Adjuvant treatment of early breast cancer. 1 mg daily.

ADMINISTRATION/STORAGE 1. Glucocorticoid or mineralocorticoid therapy is not required. 2. For first-line therapy, continue treatment until tumor regression evident. 3. For adjuvant treatment of early breast cancer, treatment is long-term (up to 5 years). 4. Dosage adjustment not necessary with hepatic or renal dysfunction. ASSESSMENT 1. Note disease progression, last tamoxifen therapy; rate pain level. 2. Obtain/monitor BP, CBC, renal and LFTs, and pregnancy test. Check cholesterol, bone mineral density. CLIENT/FAMILY TEACHING 1. Take as directed at same time daily; usually on empty stomach 1 hr before

Bold Italic = life threatening side effect

= black box warning

W = Available in Canada