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Anastrozole

ARIMIDEX

Pronunciation: an-AS-troe-zoel

Anastrozole ballicule: receptor binding, kinetics and half-life diagram
Mechanism of action: Anastrozole ballicule
Anastrozole ARIMIDEX mascot mnemonic cartoon
Visual mnemonic: Anastrozole mascot
“An Astro Arm-o-dex”

What it isAromatase inhibitor blocking peripheral estrogen synthesis; hormone receptor-positive breast cancer in postmenopausal women.

Why this oneUnlike steroidal exemestane, it is reversible and nonsteroidal; it lacks tamoxifen's endometrial-cancer and thrombosis liabilities.

What limits itAccelerated bone loss and arthralgia; monitor density. It is ineffective before menopause unless ovarian function is suppressed.

Anastrozole molecular structure (skeletal formula)
Molecular structure: Anastrozole

FDA-approved for

FDA label

FDA dosingPopulationStartTargetMax
Breast cancer (adjuvant early-stage, or advanced) in postmenopausal womenPostmenopausal women1 mg QD1 mg QD1 mg QD

Renal No adjustment needed

Hepatic Mild-to-moderate impairment: no change; severe impairment: not studied.

Instructions

Available strengths

Cautions

Adverse reactions

Pregnancy May cause fetal harm based on animal findings and mechanism of action; embryo-fetal toxicities in rats; advise effective contraception.

Lactation No data on presence in human milk; because of tumorigenicity in animal studies, breastfeeding is not recommended.

Cost

Anastrozole (ARIMIDEX)
What pharmacies pay · NADAC 9/30/26
Strength#/mogeneric $/moCostPlus
1 mgtab30 qd$4.25offered

Generic entry2010

NO BOXED WARNINGS

Principal riskAccelerated bone loss and arthralgia

Classes and tags

Clinical profile

Therapeutic safety burden2 / 4
Overdose danger2 / 4
Weight-gain liability0 / 4
Sedation liability0 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk3 / 4

Legacy pregnancy categoryMultiple / indication-, trimester- or formulation-dependent

Defining liabilityThrombotic, metabolic, hepatic, skeletal or reproductive toxicity varies by hormonal target.

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