Brand and Other Names:Arimidex
- Classes: Antineoplastics, Aromatase Inhibitor
Dosing & Uses
Dosage Forms & Strengths
- 1 mg PO once daily; continue until tumor progression
- Adjuvant treatment: 1 mg PO qDay; optimal duration unknown; 5 years in clinical trials
May be taken with or without food
Mild-to-moderate impairment or stable hepatic cirrhosis: Dose adjustment not necessary
Severe hepatic impairment: Not studied
Use not recommended
Serious - Use Alternative
Significant - Monitor Closely
Hot flashes (12-36%)
Mood disturbances (19%)
Nausea and vomiting (19%)
Bone pain (11%)
Increased cough (11%)
Accidental injury (10%)
Back pain (10%)
Peripheral edema (10%)
Abdominal pain (9%)
Breast pain (8%)
Urinary tract infection (8%)
Chest pain (7%)
Flu syndrome (6%)
Breast neoplasm (5%)
Vaginal bleeding (5%)
Fractures of spine, hip, or wrist (4%)
Ischemic cardiovascular disease (4%)
Vaginal hemorrhage (4%)
Deep vein thrombosis (2%)
Endometrial cancer (intact uterus at baseline) (2%)
Ischemic cerebrovascular event (2%)
Weight gain (2%)
Hepatitis; increased alkaline phosphatase, aminotransferases, gamma-glutamyl transferase, and bilirubin
Allergic reactions, including angioedema, urticaria, and anaphylaxis
Rash, including mucocutaneous disorders (eg, erythema multiforme, Stevens-Johnson syndrome)
Myalgia, trigger finger, and hypercalcemia (with or without increase in parathyroid hormone)
May cause fetal harm or loss; use is contraindicated in women who are or may become pregnant
Increased incidence of ischemic cardiovascular events in women with preexisting ischemic heart disease; use only if benefits greatly outweigh risks
Decreases lumbar spine and total hip bone mineral density; increased risk of fractures and osteoporosis
Elevated serum cholesterol reported; monitor closely
Affords no clinical benefit to premenopausal women with breast cancer
Increased risk of ischemic cardiovascular events in patients with pre-existing ischemic cardiac disease
Pregnancy & Lactation
Pregnancy category: X
Lactation: Unknown whether drug is excreted in milk; not recommended given potential for serious adverse reactions in nursing infants
A:Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B:May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C:Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D:Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X:Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA:Information not available.
Mechanism of Action
Selective nonsteroidal aromatase inhibitor; prevents conversion of androstenedione to estrone and estradiol in peripheral tissues, thereby significantly lowering serum estradiol concentrations; has no effect on adrenal corticosteroids or aldosterone
Peak plasma concentration: 2 hr without food; 5 hr with food
Onset: 24 hr (70% reduction); 2 weeks (80% reduction)
Time to steady-state levels: 7 days
Protein bound: 40%
Metabolized in liver via N-dealkylation, hydroxylation, and glucuronidation (85%)
Metabolite: Triazole (inactive)
Enzymes inhibited: CYP1A2, CYP2C9, CYP3A4 (at high concentrations; inhibition not significant at usual dose)
Half-life: 50 hr
Excretion: Urine (10%)
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