Drugs Information Online
Drugs and diseases reference index

Drugs and diseases reference index

Drugs A-Z List

Diseases & Conditions A-Z List

Herbs & Supplements

Medical Dictionary

Full Article

Popular Drugs

Popular Diseases & Conditions

Drugs reference index «Anastrozole»



Pronunciation: (an-AS-troe-zole)Class: Aromatase inhibitor

Trade Names:Arimidex- Tablets 1 mg


A selective nonsteroidal aromatase inhibitor. It lowers serum estradiol concentrations.



Absorption is rapid, with T max at about 2 h. Food decreases C max by 16% and delays T max to 5 h.


40% protein bound.


Metabolized in the liver (N-dealkylation, hydroxylation, and glucuronidation) via CYP1A2, CYP2C8/2C9, and CYP3A4.


Half-life is approximately 50 h; approximately 10% is excreted in the urine. Approximately 85% undergoes hepatic metabolism.

Special Populations

Renal Function Impairment

Renal Cl decreased proportionally with CrCl and was approximately 50% lower in those with severe renal function impairment (CrCl less than 30 mL/min per 1.73 m 2 ); this reduced total body Cl by 10%. No dosage adjustment is needed for renal impairment.

Hepatic Function Impairment

Oral Cl was approximately 30% lower in those with stable hepatic cirrhosis, but plasma concentrations were within normal range. Dosage adjustment is not necessary. Has not been studied in patients with severe hepatic impairment.


The pharmacokinetics of anastrozole are not affected by age.


Safety and efficacy not established.

Indications and Usage

Advanced breast cancer in postmenopausal women with progression following tamoxifen therapy; first-line treatment of postmenopausal women with hormone receptor–positive or hormone receptor unknown locally advanced or metastatic breast cancer; for adjuvant treatment of postmenopausal women with hormone receptor–positive early breast cancer.

Unlabeled Uses

Male infertility.


Women who are or plan to become pregnant; premenopausal women; patients who have shown hypersensitivity reaction to the drug or any of the excipients.

Dosage and Administration

Breast CancerAdults

PO 1 mg every day with or without food.

Unlabeled UsesMale Infertility

PO 1 mg once daily for a mean duration of 4.7 mo (range, 1 to 24 mo).


Store tablets at controlled room temperature (68° to 77°F).

Drug Interactions


Estrogens may diminish the actions of anastrozole. Coadministration is not recommended.

May reduce blood estradiol levels. This may affect the efficacy of oral contraceptives.


Coadministration is not recommended.

Laboratory Test Interactions

Elevations of gamma glutamyltransferase (GGT) levels have been observed among patients with liver metastases.

Adverse Reactions


Vasodilation (36%); hypertension (13%); ischemic CV disease, thromboembolic disease (4%); venous thromboembolic events (3%); deep venous thromboembolic events, ischemic cerebrovascular event (2%).


Asthenia, mood disturbances (19%); headache (18%); depression (13%); insomnia (10%); dizziness (8%); paraesthesia (7%); anxiety (6%); hypertonia (3%); lethargy (1%).


Rash (11%); sweating (5%); erythema multiforme, mucocutaneous disorder, Stevens-Johnson (postmarketing).


Pharyngitis (14%); cataract specified (6%).


GI disturbance (34%); nausea (20%); vomiting (11%); abdominal pain, constipation, diarrhea (9%); anorexia (8%); dyspepsia, GI disorder (7%); dry mouth (6%).


Breast pain, UTI (8%); vulvovaginitis (6%); breast neoplasm, vaginal hemorrhage (5%); vaginal discharge, vaginitis (4%); leucorrhea (3%); vaginal dryness (2%).


Lymphedema (10%); anemia (4%); leukopenia (postmarketing).


Increased alkaline phosphatase, ALT, AST, bilirubin, GGT; hepatitis (postmarketing).


Allergic reactions including anaphylaxis, angioedema, and urticaria (postmarketing).


Edema (11%); peripheral edema (10%); hypercholesterolemia, weight gain (9%).


Musculoskeletal events (36%); arthritis (17%); arthralgia (15%); back pain, bone pain (12%); osteoporosis (11%); fracture (10%); arthrosis, pelvic pain (7%); joint disorder, myalgia (6%).


Dyspnea, increased cough (11%); sinusitis (6%); bronchitis (5%).


Hot flashes (36%); pain (17%); accidental injury (10%); infection (9%); chest pain, flu syndrome (7%); cyst, neoplasm (5%); tumor flare (3%).



Monitor cholesterol levels and BMD periodically.


Category X .




Safety and efficacy not established.

Bone effects

May decrease BMD.

Cardiac effects

Consider the risks and benefits in patients with preexisting ischemic heart disease.


May increase serum cholesterol levels.

Estrogen receptor–negative

Patients who did not respond to tamoxifen rarely respond to anastrozole.

Patient Information

  • Advise patient that medication can be taken without regard to meals, but to take with food if GI upset occurs.
  • Advise women that anastrazole may cause fetal harm. Advise patients to avoid becoming pregnant.
  • Instruct patient to immediately report any of the following to the health care provider: dizziness or fainting, pain in groin or calves, sharp chest pain or sudden shortness of breath, sudden severe headache, vision or speech problems, weakness or numbness of arms or legs.
  • Advise patient that drug may cause dizziness and to use caution while driving or performing other tasks requiring mental alertness.
  • Advise patient that this medicine may decrease bone strength, which may increase the risk of fractures.
  • Advise patient with preexisting ischemic heart disease of the increased risk of CV events.
  • Advise patients that this medication may increase cholesterol.

Copyright © 2009 Wolters Kluwer Health.

  • Anastrozole MedFacts Consumer Leaflet (Wolters Kluwer)
  • Anastrozole Detailed Consumer Information (PDR)
  • anastrozole Advanced Consumer (Micromedex) - Includes Dosage Information
  • Arimidex Prescribing Information (FDA)
  • Arimidex Consumer Overview

Comment «Anastrozole»