Description
Aromatase inhibitors (a group of drugs including Anastrozole) are hormone antagonists, they act by inhibiting the synthesis of the enzyme necessary for the production of hormones. The active ingredient in the composition of the drug – anastrozole suppresses estradiol (female hormone), but has no effect on cortisol, gonadotropin and aldosterone.
The antitumor agent contains an active component that is a selective (selectively acting) non-steroidal aromatase inhibitor. In postmenopausal women, estradiol is produced from androstenedione and estrone with the participation of this enzyme. Reducing its levels treats breast cancer. Anastrozole is able to lower the amount of circulating hormone by 80%. The drug does not have progestagenic, estrogenic and androgenic activity.
After taking tablets orally, the active component is rapidly absorbed from the gastrointestinal tract and reaches maximum plasma concentration in two hours, provided that the drug was taken on an empty stomach. Food decreases the rate of absorption of anastrozole, but not the extent. The active substance binds to plasma proteins by 40%, does not cumulate (does not accumulate).
Metabolism of the drug occurs in the liver by dealkylation, hydroxylation and glucuronidation. The main metabolite triazole is determined in plasma and urine, is not an aromatase inhibitor. The substance itself and its metabolites are excreted by urine within three days after administration. With stabilized liver cirrhosis, impaired renal function, the clearance of anastrozole does not change. There are no differences in the pharmacokinetics of the active component in postmenopausal women.
Indications for use
Specialists can prescribe Anastrozole for men – the drug is used in bodybuilding. Indications for the use of the drug in women are:
Treatment of advanced breast cancer in postmenopause;
therapy of invasive estrogen-positive breast cancer at early stages with positive hormone receptors;
comprehensive treatment of estrogen-positive breast cancer at early stages after adjuvant therapy with Tamoxifen for 2-3 years.
How to take Anastrozole
Tablets are intended for oral administration in a dosage of 1 mg once/day. The dosage has no dependence on age (in the elderly also 1 mg once a day). Dose correction is not carried out in case of slight or moderate impairment of liver and kidney functions. The course of therapy with Anastrozole is determined by the doctor individually, it can last for a long time (up to several years).
Anastrozole in bodybuilding
The drug inhibits the production of estrogens, so it can be used in bodybuilding in long-term courses of steroid hormones to reduce the negative effects of female sex hormones. Additionally, the medication removes unnecessary amounts of water from the body, allows you to achieve a clear relief. Anastrozole suppresses the problem of breast enlargement (gynecomastia) in men. For female bodybuilders, the drug is not recommended.
It is recommended to take tablets in the morning on an empty stomach, so that the active substance is more quickly absorbed and digested. In 10 days after taking anabolics you should take an estradiol test, after which you should start taking Anastrozole at a dose of 0.5 mg/day (when using Sustanon or anabolics containing testosterone enanthate, the tests should be taken in 3-4 weeks).
Reviews
There are no reviews yet.