Classifications: antineoplastic; nonsteroidal aromatase inhibitor; Therapeutic: antineoplastic
Pregnancy Category: D
1 mg tablets
Anastrozole is a potent and selective nonsteroidal aromatase inhibitor that converts estrone to estradiol. It lowers serum
estrogen levels in postmenopausal women without interfering with adrenal steroid synthesis.
Inhibiting the biosynthesis of estrogens is one way to deprive tumors of estrogens, and thus restrict tumor growth.
Early and advanced breast cancer in postmenopausal women.
Pregnancy (category D), lactation, premenopausal women, postmenopausal hormone replacement therapy; severe hepatic disease,
Mild to moderate hepatic disease.
Route & Dosage
Adult: PO 1 mg once daily
- Give on an empty stomach, 1 h before or 2 h after meals, because food affects extent of absorption.
- Store at 20°25° C (68°77° F).
Adverse Effects (≥1%)CNS:
Asthenia, headache, hot flushes, pain, dizziness, depression
, confusion, anxiety, nervousness. CV:
Chest pain, hypertension, thrombophlebitis, edema. GI: Diarrhea,
nausea, vomiting, constipation
, abdominal pain, anorexia, dry mouth, increased liver function tests (ALT, AST, GGT). Respiratory: Dyspnea
, cough, pharyngitis, bronchitis
, rhinitis, sinusitis
Rash, peripheral edema, pelvic pain, flu-like syndrome
Rapidly absorbed from GI tract. Distribution:
40% protein bound. Metabolism:
85% metabolized in liver to inactive metabolites. Elimination:
10% excreted unchanged; 60% as metabolites in urine. Half-Life:
Assessment & Drug Effects
- Lab Tests: Monitor periodically liver enzymes, CBC with differential, alkaline phosphatases, total cholesterol, and lipid
- Assess for hypertension, complications of edema, thrombotic events, and signs of liver toxicity.
Patient & Family Education
- Recognize common adverse effects and seek information on measures to control discomfort.
- Seek medical attention if you experience chest pain, calf pain, or shortness of breath; unexplained loss of appetite or nausea;