Aromasin is an irreversible steroid aromatase inhibitor, which in its structure resembles the natural substance of androstenedione.
In the body of a woman who survives the postmenopausal period, the production of estrogens is mainly through the conversion into androgens estrogen under the influence of the aromatase enzyme. By blocking the production of estrogen through inhibition of aromatase, it is possible to provide effective treatment of hormone-dependent breast cancer in women during the postmenopause.
The Aromasin agent acts by binding the active substance to the active fragment of the enzyme. As a consequence, its inactivation occurs. Under the influence of Aromasin, the concentration of estrogens in the blood in postmenopausal women decreases. This process is noted when taking a dose of 5 mg, the most pronounced decrease is observed when taking doses of 10-25 mg.
According to the available studies, in women from this category who received 25 mg of medication daily, the content of the aromatase enzyme decreased by 98%.
Exemestane does not demonstrate progestagenic and estrogenic activity. If the drug is used in large doses, there is a slight androgenic activity.
The drug does not affect the biosynthesis of aldosterone and cortisol in the adrenal glands, which confirms its selective effect. In this regard, there is no need for replacement therapy with glucocorticoids and mineralocorticoids.
Aromasin is called the real “killer of aromatase.” The principle of action of this drug is that it blocks the enzymes responsible for the synthesis of estrogens.
In medicine, this drug is used to treat breast cancer in post-menopausal women in cases when Tamoxifen treatment failed. Bodybuilders and other athletes found application of this drug in their activities. Many experienced athletes consider Aromasin the most effective aromatase inhibitor. This drug suppresses at least 85% of estrogens. And it is worth noting that the process of suppression is irreversible.
Aromazin during the steroid cycle prevents side effects that can cause flavoring steroids. It is worth noting that the action of Aromasin is radically different from the usual for many athletes Tamoxifen. As is known, Tamoxifen does not have any influence on the process of aromatization. It simply begins to interact with cellular estrogen receptors, not allowing estrogen to join them and form a bond. Exemestane acts on the process of aromatization and suppresses it. The structure of Aromasin is very similar to the steroid of natural origin androstenedione. The principle of action of Exemestane is that it irreversibly binds the active enzymes to hormones. As a result, hormones lose their activity. Aromasin does not possess estrogenic, not progestogenic, activity. But it is characterized by mild androgenic activity.
Aromasin – is a treatment for hormone-dependent breast cancer in women. The active substance of the drug is eksemestan, which blocks the transformation of certain hormones in the body. It is known that in the menopause (natural or provoked) the health of a woman is noticeably changing – the condition and functions of many organs and systems are being reconstructed. So, for example, “female sex hormone” estrogen begins to be produced in tissues, by converting the “male sex hormone” – androgen. It stimulates the conversion of the enzyme aromatase. At the same time, estrogen can provoke the development of malignant tumors. The drug Aromasin, acting on aromatase, stops the conversion of androgen into estrogen. In this case, the agent itself is not hormonal. Such treatment can inhibit the oncological process.
Aromasin is used when:
A common hormone-dependent breast cancer. Including, after the application of hormone therapy;
Chemotherapy for early cancer of this type, designed to prevent relapse of the disease. Including, after a long course of Tamoxifen;
Form of production of Aromasin – tablets. Most often, the scheme includes taking one tablet a day. Drug instruction Aromasin shows that it is better to drink after eating. The duration of the course can be measured over the years. If the disease begins to progress or contralateral cancer is detected (swelling in the second mammary gland) – treatment with this drug is stopped.
Contraindicated Aromasin with:
Patient therapy in the pre-menopause;
Pregnancy, lactation and in childhood;
In the annotation to the drug there is a detailed list of possible undesirable effects arising during treatment. We will quote those that, according to the results of clinical studies, are most common – more than 10% of patients. So, very frequent side effects of Aromasin are: nausea, headaches, insomnia, sweating and flushing, pain in the muscles and joints. A fifth of all women taking this drug periodically had a drop in the number of lymphocytes in their blood, but then it increased.
Studies have shown that even taking very high doses of Aromasin did not cause dangerous conditions, both in patients and in healthy subjects
Exemestane was developed by Pharmacia & Upjohn (Pharmacia), which received approval from the FDA to sell the drug in late 1999. In early 2000, the company launched a drug called Aromasin. Although in some patients the drug is effective already at such low doses as 2.5 mg per day, the company has developed a standard and universally effective dosage of 25 mg per tablet. Since then, the company has started production of the drug in many other countries under the same trade name.
Side effects of Aromasin can manifest itself quite often and to varying degrees. So, an athlete can face such unpleasant consequences as:
– increased sweating,
– dizziness and headache,
– skin rash,
– Insomnia, etc.
In one athlete, side effects can manifest themselves intensely, while in another the drug can be used absolutely painlessly. Everything depends on the individual’s sensitivity to the active substance of the drug. But, as a rule, when the recommended dosage is observed, the side effects of Aromasin do not appear at all, or manifest to an insignificant degree.
Exemestane (Natco Pharma)£65.20