Arimidex is brand name for anastrozole, an oral antiestrogen. Arimidex inhibits the enzyme aromatase in the adrenal glands that produces the estrogens (estradiol and estrone) and thereby lowers their levels.
While officially indicated for women, this drug has proven effective in the off-label use of reducing estrogens (in particular and more importantly, estradiol) in men. Excess estradiol in men can cause benign prostatic hyperplasia, gynecomastia, and symptoms of hypogonadism. Some athletes and body builders will also use anastrozole as a part of their steroid cycle to reduce and prevent symptoms of excess estrogens; in particular, gynecomastia and water retention.
Study data currently suggests that dosages of 0.5mg to 1mg a day reduce serum estradiol by about 50% in men, which differs from the typical reduction in postmenopausal women. However the reduction may be different for men with grossly elevated estradiol (clinical data is currently lacking).
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Side effects, that may go away during treatment, include weakness, nausea, headache, hot flashes, pain, vomiting, cough, or diarrhea. If they continue or are bothersome, check with your doctor. Check with your doctor as soon as possible if you experience a sore throat or fever. If you notice other effects not listed above, contact your doctor, nurse, or pharmacist.
There was no evidence of teratogenicity in rats administered doses up to 1.0 mg/kg/day. In rabbits, anastrozole caused pregnancy failure at doses equal to or greater than 1.0 mg/kg/day (about 16 times the recommended human dose on a mg/m2 basis); there was no evidence of teratogenicity in rabbits administered 0.2 mg/kg/day (about 3 times the recommended human dose on a mg/m2 basis).
Clinical trials have been conducted with ARIMIDEX, up to 60 mg in a single dose given to healthy male volunteers and up to 10 mg daily given to postmenopausal women with advanced breast cancer; these dosages were well tolerated. A single dose of ARIMIDEX that results in life-threatening symptoms has not been established. In rats, lethality was observed after single oral doses that were greater than 100 mg/kg (about 800 times the recommended human dose on a mg/m2 basis) and was associated with severe irritation to the stomach (necrosis, gastritis, ulceration, and hemorrhage).
In an oral acute toxicity study in the dog the median lethal dose was greater than 45 mg/kg/day.