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Anastrozole

Anastrozole, sold under the trade name Arimidex among others, is a medication used in addition to other treatments for breast cancer. More

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Description

Anastrozole, sold under the trade name Arimidex among others, is a medication used in addition to other treatments for breast cancer.

Generic Name

Anastrozole

Chemical names

Anastrozole, Anastrazole, Arimidex, Anastrozol

Brand names

Altraz, Altrol, Anabrez, Anaday, Anazol, Anzucia, Arimidex, Armilon, Armotraz, Azoleres, Redest, Stazonex

IUPAC name

2-[3-(1-cyano-1-methylethyl)-5-(1H-1,2,4-triazol-1-ylmethyl)phenyl]-2-methylpropanenitrile

Pharmacokinetics

  • Absorption: Oral
  • Distribution: 40% protein binding
  • Metabolism: Hepatic
  • Excretion: Via urine

Actions

It is selectively inhibits aromatase, aromatase inhibition leads to a decrease in tumor concentration of estrogen and serum, leading to a delayed progression of tumor growth or decreased tumor mass in some women.

Dosage/Dosage form

1 mg daily oral

Therapeutic uses

  • For adjuvant treatment of hormone receptor positive breast cancer, as well as hormonal treatment of advanced breast cancer in post-menopausal women. 
  • McCune-Albright syndrome
  • Has also been used to treat pubertal gynecomastia

Adverse effects/Side effects

Hot flushes, vaginal dryness, vaginal bleeding, rash, hair thinning, anorexia, myalgia, nausea, vomiting, diarrhoea, headache, arthralgia, bone fractures, oedema, asthenia, fever, flu-like syndrome, weight gain, leucopenia, dizziness, drowsiness, abnormal liver enzyme values, thrombophloebitis, anaphylaxis.

Interaction

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

Contraindications

Hypersensitivity, Pregnancy. Premenopausal women and lactation

Storage

Store at 20-25°C oral dosage forms

Information

Molecular weight

293.3663

Molecular formula

C17H19N5

CAS number

120511-73-1

Precautions

  • Bone mass density test should be conducted at the start of the therapy and at regular intervals thereafter.
  • Moderate or severe hepatic impairment
  • Laboratory test for menopause if status is doubtful.