Product Name: Exemever
Active substance: Exemestane
The antitumor agent, an inhibitor of estrogen synthesis, has anti-estrogenic, androgenic and cytostatic effect. Blocks estrogen formation by inhibiting aromatase irreversibly binds to the active site of the enzyme causing its inactivation. Do not have progestin and estrogen activity. It has no effect on the synthesis of cortisol and aldosterone in the adrenal glands. According to the principle of feedback increases the secretion of LH and FSH by the pituitary gland (decrease the concentration of estrogen stimulates the secretion of gonadotropins by the pituitary gland). Absorption - high (food improves absorption), bioavailability - low. TCmax - 2 h, Cmax for a single dose of 25 mg - 18 ng / ml. Has the effect of "first pass" through the liver. Metabolized by oxidation of the methylene group with the participation of isoenzyme CYP3A4 and / or by reducing the 17-keto group with the participation of aldoketoredukt to form a pharmacologically inactive or less active metabolites. T1 / 2 - 24 hours is well distributed in tissues (large volume of distribution). Relationship to plasma proteins - 90%. Excreted by the kidneys and through the intestines.
Common breast cancer among women in natural or induced postmenopausal women: the progression of the disease during the anti-estrogen therapy (including non-steroidal aromatase inhibitors), progestin (hormone therapy III of the series). Adjuvant treatment of early breast cancer in postmenopausal women with estrogen-receptor positive or unknown receptor status, after a 2-3-year initial adjuvant tamoxifen therapy, to reduce the risk of recurrence (distant or regional) and contralateral breast cancer.
Contraindications and Cautions:
Hypersensitivity, pregnancy, lactation, infancy. The caution. Premenopausal endocrine status. Post-menopausal status should be confirmed by determining the concentration of LH, FSH and estradiol. During the period of treatment must be careful when driving and occupation of other potentially hazardous activities that require high concentration and speed of psychomotor reactions.
"Tides" of blood to the upper body and face, increased sweating; fatigue, dizziness, headache, insomnia, depression, a syndrome of "carpal tunnel"; skin rash; lymphopenia, thrombocytopenia, leukopenia; abdominal pain, loss of appetite, nausea, vomiting, constipation, dyspepsia, diarrhea, increased activity of "liver" transaminases and alkaline phosphatase; alopecia, peripheral edema; arthralgia, myalgia, ossalgiya, pain unspecified location.
Inside, 25 mg 1 time a day after meals. In the treatment of advanced breast cancer treatment should be continued until tumor progression or development of contralateral breast cancer. Treatment of early breast cancer continue to until the total duration of successive adjuvant hormonal therapy reaches five years.
Rifampicin (inductor CYP3A4) reduces the concentration that does not lead, however, to decrease the pharmacological activity of exemestane. Antagonism with estrogens.
Store in a dry place protected from light, at a temperature of 15-25 ° C. Keep out of the reach and sight of children.