Anastrozole (arimidex)

Anastrozole (arimidex)

Molecular formula: C17H19N5
Molecular weight: 293.37
Molecular Structure:
 
CAS : 120511-73-1
Appearance: an off-white color crystalline powder
Use: It can be used to the treatment of Breast cancer
Standard: Enterprise Standard
Package: 25KG/Drum

Anastrozole (INN) (marketed under the trade name Arimidex by AstraZeneca) is a non-steroidal aromatase-inhibiting drug approved for treatment of breast cancer after surgery, as well as for metastasis in both pre and post-menopausal women. The severity of breast cancer can be increased by estrogen, as sex hormones cause hyperplasia, and differentiation at estrogen receptor sites. Anastrozole works by inhibiting the synthesis of estrogen. The patent on Arimidex by AstraZeneca expired June 2010.
It is on the World Health Organization's List of Essential Medicines, a list of the most important medications needed in a basic health system.

Mechanism of action
Anastrozole binds reversibly to the aromatase enzyme through competitive inhibition, inhibits the conversion of androgens to estrogens in peripheral tissues (extra-gonadal).

Side effects
Bone weakness has been associated with anastrozole. Women who switched to anastrozole after two years on tamoxifen reported twice as many fractures as those who continued to take tamoxifen (2.1% compared to 1%).Bisphosphonates are sometimes prescribed to prevent the osteoporosis induced by aromatase inhibitors. The level of circulating estradiol is likely causal here and not the anastrozole itself, and so the dose will determine likelihood of osteoporosis (estradiol inhibits osteoclasts, which resorb bone).

Usage in men
Anastrozole has been tested for reducing estrogens, including estradiol, in men.Excess estradiol in men can cause benign prostatic hyperplasia, gynecomastia, and symptoms of hypogonadism. It can also contribute to increased risk of stroke, heart attack, chronic inflammation, prostate enlargement and prostate cancer. Some athletes and body builders use anastrozole as part of their steroid cycle to reduce and prevent symptoms of excess estrogen--gynecomastia, emotional lability and water retention.Study data suggests dosages of 0.5 mg to 1 mg a day reduce serum estradiol by approximately 50% in men, which differs in postmenopausal women

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