Pharmacological action – antitumor, inhibitory synthesis of estrogens. It is active against estrogen-dependent breast tumors in postmenopausal women. Androstenedione – the main source of circulating estrogens in postmenopausal women, in peripheral tissues is converted to estrone, and then to estradiol, this process takes place with the participation of the aromatase enzyme. The mechanism of action of anastrozole is associated with the inhibition of aromatase (a selective non-steroidal inhibitor) in peripheral tissues, incl. Fatty, which leads to a decrease in the amount of estradiol. When anastrozole is treated at the recommended dose of 1 mg per day, the level of estradiol is reduced by 70% within 24 hours, by 80% after 14 days. Suppression of serum estradiol levels is maintained for 6 days after discontinuation of daily intake of 1 g of anastrozole. A decrease in the level of circulating estradiol has a therapeutic effect in breast tumors in postmenopausal women. With daily intake of doses of 3, 5 and 10 mg, anastrozole had no effect on the secretion of cortisol and aldosterone. Anastrozole did not show direct progestogen, androgenic and estrogenic activity in animals, but it altered the levels of circulating progesterone, androgens and estrogens.
Effects of taking Anastrozol
- Significant reduction in the level of aromatization (up to 80% of the initial level).
- Strong inhibitory effect.
- Blocking the level of estrogen.
- Rapid action of the drug. The maximum concentration of the active substance in the blood is observed after 2 hours after administration, which allows very quickly to suppress the process of aromatization.
- It is very effective for athletes prone to aromatization.
Dosing and Administration
Inside, the tablet is swallowed whole, washed down with water. Recommended use at the same time.
The daily dose for adults, including the elderly, is 1 mg 1 time per day. If signs of disease progression appear, the drug should be discontinued. With adjuvant therapy, the recommended duration of treatment is 5 years.
If there is a mild or moderate renal dysfunction, no dose adjustment is required.
If the liver function is mild, no dose adjustment is required.
Side Effects of Anastrozol
When hypersensitive individual active ingredient, and also significantly exceeded the recommended dosages, the following side effects of anastrozole: drowsiness, polymorphic erythema, asthenia, various allergic reactions, headache, vomiting, nausea, diarrhea, skin rash. Do not use Anastrozol for people who have problems with the cardiovascular system. The drug effectively counteracts estrogenic side effects, but at the same time it blocks the beneficial properties of estrogen (suppression of “good” cholesterol), which can lead to heart problems. Athletes who have CCC disease should consult a sports doctor or, in extreme cases, use the course Tamoxifen.