(an AS troe zole)
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Arimidex: 1 mg
Generic: 1 mg
Brand Names: U.S.
- Antineoplastic Agent, Aromatase Inhibitor
Potent and selective nonsteroidal aromatase inhibitor. By inhibiting aromatase, the conversion of androstenedione to estrone, and testosterone to estradiol, is prevented, thereby decreasing tumor mass or delaying progression in patients with tumors responsive to hormones. Anastrozole causes an 85% decrease in estrone sulfate levels.
Well absorbed; extent of absorption not affected by food
Extensively hepatic (~85%) via N-dealkylation, hydroxylation, and glucuronidation; primary metabolite (triazole) inactive
Feces; urine (urinary excretion accounts for ~10% of total elimination, mostly as metabolites)
Onset of Action
Onset of estradiol reduction: 70% reduction after 24 hours; 80% after 2 weeks of therapy
Time to Peak
Plasma: ~2 hours without food; 5 hours with food
Duration of Action
Duration of estradiol reduction: 6 days
Special Populations: Renal Function Impairment
Renal clearance is decreased proportionally with CrCl and was approximately 50% lower in those with severe renal function impairment (CrCl less than 30 mL/minute per 1.73 m2); this reduced total body clearance by 10%.
Special Populations: Hepatic Function Impairment
Oral clearance was approximately 30% lower in those with stable hepatic cirrhosis, but plasma concentrations were within normal range.
Use: Labeled Indications
First-line treatment of locally-advanced or metastatic breast cancer (hormone receptor-positive or unknown) in postmenopausal women
Adjuvant treatment of early hormone receptor-positive breast cancer in postmenopausal women
Treatment of advanced breast cancer in postmenopausal women with disease progression following tamoxifen therapy
Treatment of recurrent or metastatic endometrial or uterine cancers, treatment of recurrent ovarian cancer
Hypersensitivity to anastrozole or any component of the formulation; use in women who are or may become pregnant
Canadian labeling: Additional contraindications (not in U.S. labeling): Lactating women
Breast cancer, advanced: Adults: Postmenopausal females: Oral: 1 mg once daily; continue until tumor progression
Breast cancer, early (adjuvant treatment): Adults: Postmenopausal females: Oral: 1 mg once daily. Note: The American Society of Clinical Oncology (ASCO) guidelines for Adjuvant Endocrine Therapy of Hormone-Receptor Positive Breast Cancer (Focused Update) recommend a maximum duration of 5 years of aromatase inhibitor (AI) therapy for postmenopausal women; AIs may be combined with tamoxifen for a total duration of up to 10 years of endocrine therapy. Refer to the guidelines for specific recommendations based on menopausal status and tolerability (Burstein, 2014).
Breast cancer, risk reduction (off-label use): Postmenopausal females ≥40 years: Oral: 1 mg once daily for 5 years (Cuzick, 2014)
Dosage adjustment in renal impairment: No dosage adjustment necessary.
Dosage adjustment in hepatic impairment:
Mild to moderate impairment or stable hepatic cirrhosis: No dosage adjustment necessary.
Severe hepatic impairment: There are no dosage adjustments provided in the manufacturer’s labeling (has not been studied).
May be administered with or without food. Hazardous agent; use appropriate precautions for handling and disposal (NIOSH 2014 [group 1]).
Store at 20°C to 25°C (68°F to 77°F).
Amodiaquine: CYP2C8 Inhibitors may increase the serum concentration of Amodiaquine. Avoid combination
Estrogen Derivatives: May diminish the therapeutic effect of Anastrozole. Avoid combination
Methadone: Aromatase Inhibitors may increase the serum concentration of Methadone. Monitor therapy
Tamoxifen: May decrease the serum concentration of Anastrozole. Consider therapy modification
TiZANidine: CYP1A2 Inhibitors (Weak) may increase the serum concentration of TiZANidine. Management: Avoid these combinations when possible. If combined use cannot be avoided, initiate tizanidine at an adult dose of 2 mg and increase in 2-4 mg increments based on patient response. Monitor for increased effects of tizanidine, including adverse reactions. Consider therapy modification
Cardiovascular: Vasodilatation (25% to 36%), ischemic heart disease (4%; 17% in patients with pre-existing ischemic heart disease), hypertension (2% to 13%), angina pectoris (2%; 12% in patients with pre-existing ischemic heart disease), edema (7% to 11%)
Central nervous system: Fatigue (19%), mood disorder (19%), headache (9% to 18%), pain (11% to 17%), depression (2% to 13%)
Dermatologic: Skin rash (6% to 11%)
Endocrine & metabolic: Hot flash (12% to 36%)
Gastrointestinal: Gastrointestinal distress (29% to 34%), nausea (11% to 20%), vomiting (8% to 13%)
Neuromuscular & skeletal: Weakness (13% to 19%), arthritis (17%), arthralgia (2% to 15%), back pain (10% to 12%), ostealgia (6% to 12%), osteoporosis (11%)
Respiratory: Pharyngitis (6% to 14%), dyspnea (8% to 11%), increased cough (7% to 11%)
1% to 10%:
Cardiovascular: Peripheral edema (5% to 10%), chest pain (5% to 7%), venous thrombosis (2% to 4%; including pulmonary embolism, thrombophlebitis, retinal vein thrombosis), myocardial infarction (1%)
Central nervous system: Insomnia (2% to 10%), dizziness (5% to 8%), paresthesia (5% to 7%), anxiety (2% to 6%), confusion (2% to 5%), drowsiness (2% to 5%), malaise (2% to 5%), nervousness (2% to 5%), carpal tunnel syndrome (3%), hypertonia (3%), cerebrovascular insufficiency (2%), lethargy (1%)
Dermatologic: Alopecia (2% to 5%), pruritus (2% to 5%), diaphoresis (1% to 5%)
Endocrine & metabolic: Hypercholesterolemia (9%), increased serum cholesterol (9%), weight gain (2% to 9%), increased gamma-glutamyl transferase (2% to 5%), weight loss (2% to 5%)
Gastrointestinal: Constipation (7% to 9%), diarrhea (7% to 9%), abdominal pain (6% to 9%), anorexia (5% to 8%), dyspepsia (7%), gastrointestinal disease (7%), xerostomia (4% to 6%)
Genitourinary: Mastalgia (2% to 8%), urinary tract infection (2% to 8%), pelvic pain (5% to 7%), vulvovaginitis (6%), vaginal dryness (1% to 5%), vaginal hemorrhage (1% to 5%), vaginal discharge (4%), vaginitis (4%), leukorrhea (2% to 3%)
Hematologic & oncologic: Lymphedema (10%), breast neoplasm (5%), neoplasm (5%), anemia (2% to 5%), leukopenia (2% to 5%), tumor flare (3%)
Hepatic: Increased serum alkaline phosphatase (2% to 5%), increased serum ALT (2% to 5%), increased serum AST (2% to 5%)
Infection: Infection (2% to 9%)
Neuromuscular & skeletal: Bone fracture (1% to 10%), arthrosis (7%), myalgia (2% to 6%), neck pain (2% to 5%), pathological fracture (2% to 5%)
Ophthalmic: Cataract (6%)
Respiratory: Flu-like symptoms (2% to 7%), sinusitis (2% to 6%), bronchitis (2% to 5%), rhinitis (2% to 5%)
Miscellaneous: Accidental injury (2% to 10%), cyst (5%), fever (2% to 5%)
<1% (Limited to important or life-threatening): Anaphylaxis, angioedema, cerebral infarction, cerebral ischemia, dermal ulcer, endometrial carcinoma, erythema multiforme, hepatitis, hepatomegaly, hypercalcemia, hypersensitivity angiitis (including anaphylactoid purpura [IgA vasculitis]), jaundice, joint stiffness, pulmonary embolism, retinal thrombosis, skin blister, skin lesion, Stevens-Johnson syndrome, tenosynovitis (stenosing), urticaria
Concerns related to adverse effects:
• Decreased bone mineral density: Due to decreased circulating estrogen levels, anastrozole is associated with a reduction in bone mineral density (BMD); decreases (from baseline) in total hip and lumbar spine BMD have been reported. Patients with preexisting osteopenia are at higher risk for developing osteoporosis (Eastell, 2008). When initiating anastrozole treatment, follow available guidelines for bone mineral density management in postmenopausal women with similar fracture risk; concurrent use of bisphosphonates may be useful in patients at risk for fractures.
• Hypercholesterolemia: Elevated total cholesterol levels (contributed to by LDL cholesterol increases) have been reported in patients receiving anastrozole; use with caution in patients with hyperlipidemias. Cholesterol levels should be monitored/managed in accordance with current guidelines for patients with LDL elevations.
• Hepatic impairment: Plasma concentrations in patients with stable hepatic cirrhosis were within the range of concentrations seen in normal subjects across all clinical trials. Has not been studied in patients with severe hepatic impairment.
• Ischemic disease: Patients with preexisting ischemic cardiac disease have an increased risk for ischemic cardiovascular events.
• Pregnancy: Use is contraindicated in women who are or may become pregnant.
• Premenopausal women: Anastrozole offers no clinical benefit in premenopausal women with breast cancer.
• Hazardous agent: Use appropriate precautions for handling and disposal (NIOSH 2014 [group 1]).
Bone mineral density; total cholesterol and LDL
Breast cancer risk reduction (off-label use): Bone mineral density at baseline, mammograms, and clinical breast exam at baseline and at least every 2 years (Cuzick, 2014)
Pregnancy Risk Factor
Adverse events were observed in animal reproduction studies. Anastrozole is contraindicated in women who are or may become pregnant (may cause fetal harm if administered during pregnancy). Use in premenopausal women with breast cancer does not provide any clinical benefit.
• Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)
• Patient may experience flushing, nausea, arthralgia, joint edema, insomnia, pharyngitis, or back pain. Have patient report immediately to prescriber signs of depression (ie, suicidal ideation, anxiety, emotional instability, illogical thinking), signs of hepatic impairment, signs of hypercalcemia, excessive weight gain, edema of extremities, strength differences from one side to another, difficulty speaking or thinking, change in balance, blurred vision, severe headache, paresthesia, arrhythmia, mood changes, significant dizziness, syncope, polyuria, difficult urination, considerable asthenia, enlarged lymph nodes, vaginal hemorrhaging, vaginitis, severe angina, or significant dyspnea (HCAHPS).
• Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.
Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.
More about anastrozole
- Other brands: Arimidex