Anastrozole (Arimidex)

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Chemical structure

Chemical structure AnastrozoleAnastrozole – refers to anti-estrogen drugs and is synthesized specifically for the treatment of a common disease among women today – breast cancer. Anastrozole was the first medicine that got into the class of aromatase inhibitors of the 3rd generation. Anastrozole is able to reversibly bind aromatase with a competitive inhibition pathway, and the drug inhibits the conversion of androgens to estrogens that are found in peripheral tissues. The drug has its name in the chemical language – 1,3 benzene-diacetonitrile, a, a, a ‘, a’-tetramethyl-5- (1 H-1, 2,4-triazol-1-ylmethyl), formula C17H19N5. The molecular weight is 293.366 g / mol. Tamoxifen citrate (Nolvadex) is also often used for this purpose, which blocks the effect of estrogen on receptors, and does not affect the endogenous synthesis of its own estrogen by the body. The drug Anastrozole can have a significant effect on the level of estrogen in the body. So, for example, the use of only 1 mg (most often this is one tablet) per day can cause a process in which estrogen will be suppressed in 80% of patients and more. Given the powerful effect of the drug on the hormone level, it is mainly prescribed to women only during the postmenopausal period.

Historical reference

Anastrozole was developed by Zeneca Pharmaceuticals, and by the end of 1995 it was approved for use in the US. The drug was conceived as a means of a new generation that will be used to treat still-treatable breast cancer in women. For the same purpose, a drug called Tamoxifen was previously used for a long time. In order to move away from the already established trends in this area, there were compelling reasons. Very soon after the appearance, Anastrozole was included in a global double-blind study of a multicenter, which was based in Rome. During the study, an assessment was made of the use of Anastrozole and Tamoxifen, alone or in combination. The study involved 9,366 women in the postmenopausal period after surgery for the treatment of breast cancer. Based on the results, a significant advantage of the drug Anastrozole in front of Tamoxifen was revealed. After such treatment, a significant number of patients experienced regression of the disease, and overall survival rates were also raised. After the results of the study were published in 2002, the drug Anastrozole is known as a new tool for the treatment of additional breast cancer in women during the postmenopause. Then he begins to gain popularity among men – athletes, due to the fact that he can strongly suppress estrogen.

Pharmacological action (according to the manufacturer)

It is a selective (or selective) aromatase inhibitor of a non-steroidal nature. During postmenopause, estradiol is largely derived from estrone, the production of which occurs in peripheral tissues when converted from androstenedione (with the participation of the aromatase enzyme). With a decrease in the volume of circulating estradiol in women with breast cancer, there is a therapeutic effect. During postmenopause in the female body, anastrozole at a dosage of 1 mg per day can reduce the level of estradiol by 80%. Anastrozole is not progestogen, androgenic and estrogenic. When used in the recommended dose for therapy, the drug will not affect the process of producing cortisol and aldosterone.

Properties of Anastrozole

ArimidexArimidex will definitely be interested in athletes who use steroids. Previously, before it was invented, they were fighting against estrogen with nolvadex and proviron. With a combined course, they gave a good effect. Unlike them, Arimidex solo has a much greater effect, and therefore becomes very popular. The use of one, and sometimes even ½ tablets gives an amazing result. When using highly aromatized drugs, side effects, for example, in the form of gynecomastia and water retention, are easily blocked. If you combine armibode with proscore (finasteride), you will minimize the side effects, the occurrence of which is associated with the use of ligaments of highly aromatizing agents and agents capable of converting to dihydrotestosterone. Significantly improve the muscles, because it will leave unnecessary water.

As with the long-term use of any drug, problems with the use of aromatase inhibitors may occur. Arimidex can well reduce side effects of an estrogenic nature, but at the same time, there is a blocking of useful properties of estrogen, for example, suppression of “good” cholesterol. If there are problems in the cardiovascular system of Nolvadex, because it is blocking the estrogen receptors.

Application of Anastrozole

Admission (for men):

To suppress the effects of aromatization, athletes should take from 500 μg to 1 mg of anastrozole per day.

Admission (for women):

Exclusively for medical reasons

Side Effects of Anastrozole

In general, the side effects associated with taking aromatase inhibitors include hot flushes, soreness of joints, general weakness, fatigue, sudden mood swings, depression, high blood pressure, swelling of the hands / feet, and headaches. It is also possible to reduce the level of bone mineral density, which can lead to osteoporosis and increase the risk of fractures. Sometimes there may be problems in the gastrointestinal tract, as well as nausea and vomiting. Strictly forbidden to use during pregnancy, tk. it is possible to disrupt the development of the fetus. When using drugs of this kind by men to reduce estrogen for a long time can lead to the development of cardiovascular diseases because of containing the positive effect of estrogen on the level of cholesterol. In the course of the studies, it was found that when combining steroids that tended to aromatize (eg, testosterone enanthate) together with an aromatase inhibitor, then apparent suppression of HDL cholesterol (high-density lipoproteins, “good” cholesterol) begins to manifest. Since tamoxifen does not generally have the same negative effect on the amount of cholesterol, it is more popular among men – athletes with a problematic cardiovascular system, rather than aromatase inhibitors.