Anastrozole
Anastrozole
Arimidex
Experience
No personal reports yet
No clinical reports yet
Log in to add your own experience.
Problems
No problems yet. Be the first to suggest one.
+ Add a problemTitration strategies
No titration strategies yet. Be the first to suggest one.
Effects
No effects listed yet. Be the first to suggest one.
Relevant anecdote
No anecdotes yet. Share a relevant one.
Relevant Literature
No literature entries yet.
Log in to submit relevant literature.
Summary
Common uses
Adjuvant treatment of hormone receptor-positive breast cancer in postmenopausal women0, Advanced ER-positive breast cancer (postmenopausal)0, Breast cancer risk reduction (selected high-risk postmenopausal women)0
Pharmacy
Starting dose
1 mg PO once daily
Preparations
1 mg tablets
US FDA Max
1 mg/d
Pharmacology
Routes
Oral
Onset
Estrogen suppression within days; clinical effect over months
Duration
24 hours
Half-life
~50 hours[1]
Bioavailability
High (oral; not significantly affected by food)[1]
Pregnancy
Contraindicated in pregnancy (only used in postmenopausal women); D class historically.[citation needed]
Legal status
Rx-only in US
Purported mechanism
Anastrozole is a selective non-steroidal aromatase inhibitor; it reversibly binds the CYP19 (aromatase) enzyme that converts adrenal androgens to estrogens in peripheral tissues (the principal source of estrogen after menopause), producing >97% estrogen suppression in postmenopausal women.0 Not effective in premenopausal women because ovarian aromatase is gonadotropin-driven and not adequately suppressed by AI alone. Adverse effects reflect estrogen withdrawal: hot flashes, arthralgias (the "AI joint syndrome"), vaginal dryness, accelerated bone loss (DEXA monitoring; bisphosphonate/denosumab co-therapy common), and modestly increased ischemic CV events in some analyses[1].
References
- ↑ 1.0 1.1 1.2 FDA Prescribing Information, Arimidex (anastrozole), AstraZeneca, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2010/020541s026lbl.pdf