Anastrozole – refers to the anti-androgenic drugs and synthesized specifically dlyalecheniya frequent today among women of the disease – breast cancer. Anastrozole was the first drug that has got into the class of aromatase inhibitors 3rd generation. Anastrozole is capable of reversibly binding aromatase path using competitive inhibition, as well as a preparation process inhibits the conversion of androgens to estrogens, which are located in peripheral tissues.
The drug has its own chemical name in English – 1,3benzenediatsetonitril, a, a, a ‘, a’-tetramethyl-5- (1 H-1, 2,4triazol-1-ylmethyl), C17H19N5 formula. The molecular weight of 293,366 g / mol. In such applications also often used tamoxifen citrate (Nolvadex), which blocks the effect of estrogen receptors and does not affect the synthesis of endogenous estrogen own body. Details
The drug Anastrozole can have a significant impact on the level of estrogen in the body. For example, the use of 1 mg (usually one tablet) per day can cause a process in which the estrogen is suppressed at 80% or more of patients. Given that has a powerful effect on hormonal drug, it is mainly women prescribed exclusively postmenopausal.
Anastrozole was developed by Zeneca Pharmaceuticals, and the end of 1995 received approval for use in the United States. Medicine was conceived as a new generation tool that will be used for the treatment of more operations to be breast cancers in women. With the same purpose for a long time previously used a drug called Tamoxifen. In order to move from the already well-established trends in this area needed good reasons. Very soon after the emergence of Anastrozole included in a global somatotropin dosage, multicenter, double-blind study destination, which was based in Rome. During the study, evaluated on the use of anastrozole and tamoxifen, alone or combining. In a study of 9366 women took part in postmenopausal after surgery for breast cancer treatment.
According to the results it showed a statistically significant superior efficacy of anastrozole over tamoxifen. After such treatment, a significant number of patients showed regression of the disease, but also increases overall performance for survival.
After the results of the study were published in 2002, the drug Anastrozole received fame as a new tool for the treatment of breast cancer additionality in postmenopausal women. Then he begins to gain popularity among men – athletes, due to the fact that can strongly suppress estrogen. Read more
Mode of action (according to the manufacturer)
Is selective (or selective) non-steroidal aromatase inhibitor nature. During menopause, estradiol largely obtained from estrone, which output occurs in peripheral tissues for the conversion of androstenedione (involving aromatase enzyme). When reducing the volume of circulating estradiol in women with breast cancer therapeutic effect is manifested. During a post-menopausal female body anastrozole in a dosage of 1 mg per day can reduce the level to 80% of estradiol.
The drug Anastrozole is not peculiar progestogenic, androgenic and estrogenic activity. When used at the recommended dose for the treatment of a doctor, the drug has no effect on the process of production of cortisol and aldosterone.
Armideks uniquely interested in athletes who use steroids. Earlier, before it was invented against estrogen fought using Nolvadex and Proviron. When combined course they gave a good effect. In contrast, Arimidex solo has a far greater effect, and therefore become very popular. Use one, and sometimes even ½ tablet gives a stunning result.
When applying silnoaromatiziruyuschihsya drug side effects, such as gynecomastia and water retention, easily blocked. When combined with armideks PROSCAR (finasteride), will minimize the side effects, the occurrence of which involves the use of chords silnoaromatiziruyuschihsya funds and capable of conversion to dihydrotestosterone. Significantly improve the musculature, because excess water will go.
As for sufficiently prolonged administration of any drug, aromatase inhibitors when used may cause problems. Arimidex well able to reduce the side effects of estrogen character, but at the same time, blocking occurs and useful properties of estrogen, such as, the suppression of the “good” cholesterol. If there are problems in the cardio – Nolvadex vascular system, because it carries out the estrogen receptor blockage. Details
- Reception (for men):
To suppress the effects aromatization athletes sufficiently accept from 500 .mu.g to 1 mg of anastrozole per day.
- Reception (for women):
Exclusively for medical reasons
Side effects of anastrozole
Mainly to the side effects that arise when taking aromatase inhibitors include hot flashes, joint pain, weakness, fatigue, mood swings, depression, high blood pressure, swelling of hands / feet, as well as headaches. It is also possible decline in bone mineral density, as a result may develop osteoporosis and increased risk of fractures. Sometimes problems can occur in the gastrointestinal tract, as well as nausea and vomiting.
It is strictly forbidden to use during pregnancy, because can disrupt fetal development. When using this type of drugs by men to reduce estrogen for a long time can lead to the development of cardio – vascular diseases due to containment positive impact of estrogen on cholesterol. Studies have found that if we combine steroids having a tendency to aromatization (e.g. testosterone enanthate) together with an aromatase inhibitor begins to show a clear inhibition of HDL (high density lipoproteins, the “good” cholesterol).
Since Tamoxifen basically has such a negative influence on the amount of cholesterol, it is more popular among men – athletes problematic cardio – vascular system than aromatase inhibitors.
Indications for drug use
Breast cancer in postmenopausal women.
Contraindications for medical use
Premenopausal expressed renal insufficiency (creatinine clearance less than 20 ml / min), moderate and clearly marked hepatic impairment, pregnancy and lactation, infancy, hypersensitivity to anastrozole.