The aromatase inhibitor is structurally similar to the natural steroid hormone androstenedione.
In postmenopausal women, estrogens are produced primarily by converting androgens to estrogens under the action of the aromatase enzyme in peripheral tissues. The mechanism of action of exemestane is due to irreversible binding to the active fragment of aromatase, which leads to inactivation of the enzyme.
Exemestane does not possess progestagenic and estrogenic activity. When used in high doses, only a slight androgenic activity appears. Has no effect on the biosynthesis of cortisol and aldosterone in the adrenal glands.
A slight increase in the levels of LH and FSH in serum is observed even at low doses of exemestane. This effect, however, is uncharacteristic for the drugs of this pharmacological group. It probably develops on the principle of feedback, at the level of the pituitary: a decrease in the concentration of estrogen stimulates the secretion of gonadotropins in the pituitary gland also in postmenopausal women.
Side effects of exemestane:
- increase the level of bad cholesterol in the blood
- abdominal pains
- hot flashes
- skin rash
- increased sweating
Precautions for the substance of Exemestane
Do not prescribe women with premenopausal endocrine status (efficacy and safety of the drug in this group of patients has not been studied). In patients with hepatic or renal failure, dose adjustment is not required. It is not recommended for use in children. During treatment, one should refrain from occupations that require concentration and speed of psychomotor reactions (when the drug was used, symptoms such as drowsiness, asthenia, and dizziness were noted).