Exemestane is an irreversible steroidal estrogen blocker similar in structure to the natural steroid androstenedione, its action is expressed by blocking the enzymes Aromex 25mg responsible for the synthesis of estrogen.
Irreversible steroidal aromatase inhibitor, similar in structure to the natural substance androstenedione.
In postmenopausal women, estrogens are produced primarily by converting androgens to estrogens under the action of the aromatase enzyme in peripheral tissues. Blocking the formation of estrogen by inhibiting aromatase is an effective and selective method for treating hormone-dependent breast cancer in postmenopausal women. The mechanism of action of the drug Aromazin is due to the fact that it irreversibly binds to the active fragment of the enzyme, causing its inactivation. In postmenopausal women, Aromasin significantly reduces serum estrogen concentration, starting at a dose of 5 mg, with a maximum reduction (> 90%) achieved with doses of 10-25 mg. In postmenopausal patients diagnosed with breast cancer who received 25 mg of the drug daily, the total level of the aromatase enzyme in the body was reduced by 98%.
Exemestane does not possess progestagenic and estrogenic activity. Only minor androgenic activity is revealed, mainly when used in high doses.
Aromazine has no effect on the biosynthesis of cortisol and aldosterone in the adrenal glands, which confirms the selectivity of the drug. In this regard, there is no need for replacement therapy with glucocorticoids and mineralocorticoids.
With the use of the drug, even in low doses, a slight increase in the content of LH and FSH in the blood serum is observed, which is characteristic for the preparations of this pharmacological group and probably develops on the basis of feedback at the pituitary level: a decrease in the concentration of estrogen stimulates the secretion of gonadotropins in the pituitary gland also Women in postmenopausal women.
Aromasin vs. Arimidex
Preparations containing estrogens, when applied simultaneously with Aromazine completely neutralize its pharmacological effect.
Exemestane undergoes metabolism under the influence of CYP3A4 and aldoketoreductases and does not inhibit any of the major CYP isoenzymes. The specific inhibition of CYP3A4 by ketoconazole has no significant effect aromadex on the pharmacokinetics of exemestane. Despite the established pharmacokinetic interaction of exemestane with rifampicin, a strong inducer of CYP3A4, the pharmacological activity of Aromazine (suppression of estrogens) remains unchanged, so dose adjustment is not required.