Comparative Pharmacology
Head-to-head clinical analysis: ANASTROZOLE versus ARIMIDEX.
Peer-Reviewed Evidence
Head-to-head clinical analysis: ANASTROZOLE versus ARIMIDEX.
ANASTROZOLE vs ARIMIDEX
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Anastrozole is a selective non-steroidal aromatase inhibitor. It inhibits the conversion of androgens to estrogens in peripheral tissues, thereby reducing circulating estradiol levels. It has no intrinsic progestogenic, androgenic, or estrogenic activity.
Aromatase inhibitor; inhibits conversion of androgens to estrogens by binding to aromatase enzyme, reducing estrogen levels in tissues.
1 mg orally once daily
1 mg orally once daily
None Documented
None Documented
Terminal elimination half-life: ~46 hours (range 30–60 hours). Clinically, steady-state reached after ~10 days; once-daily dosing maintains therapeutic concentrations.
Clinical Note
moderateAnastrozole + Digoxin
"Anastrozole may decrease the cardiotoxic activities of Digoxin."
Clinical Note
moderateAnastrozole + Digitoxin
"Anastrozole may decrease the cardiotoxic activities of Digitoxin."
Clinical Note
moderateAnastrozole + Deslanoside
"Anastrozole may decrease the cardiotoxic activities of Deslanoside."
Clinical Note
moderateAnastrozole + Acetyldigitoxin
"Anastrozole may decrease the cardiotoxic activities of Acetyldigitoxin."
Terminal elimination half-life ~50 hours (range 30-60 hours); supports once-daily dosing.
Primarily hepatic metabolism (85%): N-dealkylation, hydroxylation, and glucuronidation. Renal excretion of metabolites: ~10% unchanged drug in urine. Fecal elimination: ~10% as metabolites.
Primarily hepatic metabolism via N-dealkylation and glucuronidation; ~80% excreted in feces, <10% unchanged in urine.
Category D/X
Category C
Aromatase Inhibitor
Aromatase Inhibitor