Anastrozole is an anti-estrogenic drug developed to treat advanced breast cancer in women. Specifically, it is the first of a new class of third generation selective oral aromatase inhibitors. It acts by blocking the aromatase enzyme, subsequently blocking estrogen production in the body. Because many breast cancer cells are stimulated by oestrogen, reducing the levels of this hormone in the body may slow the progression of the disease. This is also the main use of tamoxifen or Nolvadex , except that Nolvadex blocks the action of oestrogen at the receptor rather than its actual endogenous production. The effect of anastrozole can be very significant, as a daily dose of 1 mg (usually 1 tablet) can cause estrogen suppression of more than 80% in treated patients. Given its powerful effect on hormone levels, this drug is usually only prescribed to post-menopausal women. Side-effects such as hot flashes and hair thinning can occur during therapy and will be much more serious in premenopausal patients. For male athletes taking steroids, anastrozole is used to minimise the side effects of elevated estrogen levels resulting from the use of anabolic/androgenic steroids. Compared to traditional methods, anastrozole is much more effective at controlling estrogen.
How it is supplied:
Anastrozole is most commonly supplied in 1mg tablets.
Anastrozole is classified as a selective non-steroidal aromatase inhibitor. It has a chemical designation of benzenediacetonitrile.
Common side effects associated with aromatase inhibitor use include hot flashes, joint pain, weakness, fatigue, mood changes, depression, increased blood pressure, swollen hands/legs and headache. Aromatase inhibitors may also reduce bone mineral density, which may lead to osteoporosis and an increase in fractures in predisposed patients. Some people may also react to taking the drug with gastrointestinal side effects, including nausea and vomiting. Aromatase inhibitors can harm the development of the unborn foetus, so they should not be taken or used during pregnancy. When aromatase inhibitors are taken by men (not as prescribed) to reduce estrogenicity during long-term steroid use, they can increase the risk of cardiovascular disease (CVD) by inhibiting some of the beneficial effects of estrogen on cholesterol values. Studies have shown that when aromatizable steroids, such as testosterone enanthate, are taken in combination with an aromatase inhibitor, the suppression of HDL (good) cholesterol levels becomes much more pronounced. Because the estrogen receptor agonist/antagonist Nolvadex® usually has no such anti-estrogenic (negative) effect on cholesterol levels, it is generally preferred to aromatase inhibitors for estrogen maintenance by male bodybuilders and athletes who are concerned about cardiovascular health. However, today it is not the correct protocol of using tamoxifen as the purpose of anti-estrogens is different in contrast to aromatase inhibitors.
Anastrozole is approved by the FDA for the adjunctive treatment of postmenopausal women with hormone receptors.
In early-stage breast cancer, first-line treatment for postmenopausal women with locally advanced metastatic hormone receptor-positive or unknown breast cancer, and treatment of advanced breast cancer in postmenopausal women with disease progression following tamoxifen therapy. In all cases, a dosage of 1 mg daily is prescribed until disease progression has stopped. When used to mitigate the estrogenic side effects of anabolic/androgenic steroids, male athletes and bodybuilders typically take between 0.5 mg and 1 mg of anastrozole daily. In some cases half a tablet (0.5 mg) taken every other day is sufficient to reduce estrogen accumulation. When used with easily aromatizable androgens such as methandrostenolone or testosterone, gynecomastia and water retention are often effectively blocked. In addition, anastrozole use can reduce fat mass, which can also be related to estrogen levels. As a result, muscles and physique become firmer and more refined, which makes this drug of interest for dieting/drying as well.
It should be noted that food has no effect on absorption of anastrozole, so the drug can be taken during or between meals.