Aromex (Exemestane) Steroid-generation aromatase inhibitor III, similar in structure to androstenedione. Crystalline powder from white to white with a yellowish tinge. It is soluble in N, N-dimethylformamide, soluble in methanol, practically insoluble in water.
It inhibits aromatase (irreversibly binds to the active site of the enzyme and causing its inactivation) and blocks the formation of estrogens. Has anti-estrogenic effects, does not possess progestogenic and estrogenic activity does not affect the synthesis of cortisol and aldosterone in the adrenal glands. Scientists from the UK claim: In high doses, it shows little androgenic activity (due to the 17-gidroproizvodnym). It increases the level of LH and FSH on the feedback principle: reducing the concentration of estrogen stimulates the secretion of gonadotropins in the pituitary gland, as UK ahtletes say.
It is dose-dependent decrease in estrone, estradiol, and estrone sulfate. Reduction of estrogen concentrations in the serum of postmenopausal women is shown at a dose of 5 mg and reaches a maximum (reduction by more than 90%) at a dose of 10-25 mg (maximum reduction in estrogen levels is observed for 3 days). In postmenopausal women with breast cancer when taking exemestane 25 mg / day reduced the overall level of aromatase by 98%.
Side effects of Aromex
- From the nervous system and sensory organs: fatigue, dizziness, headache, insomnia, depression.
- From the digestive tract: nausea, anorexia, constipation or indigestion, abdominal pain, increased liver transaminases (predominantly in patients with liver metastases and bone, the presence of other liver lesions).
- Allergic reactions: skin rash.
- Other: hot flushes, sweating, alopecia, peripheral edema (feet and legs), thrombocytopenia and leukopenia, lymphopenia.