Index of drugs

Supplementary treatment in postmenopausal women with invasive early breast cancer with the presence of estrogen receptors after 2-3 years of initial adjuvant treatment with tamoxifen. Treatment of advanced breast cancer in women during natural or post-menopausal treatment in whom the disease has progressed after antioestrogen therapy. Exestin was not shown to be effective in patients who have not detected estrogen receptors in tumor cells.

1 tabl powl. contains 25 mg of exemestane.

Anti-cancer drug - an irreversible, steroidal aromatase inhibitor, structurally similar to the naturally occurring androstendione. Blocks the biosynthesis of estrogen by inhibiting aromatase. Decreased estrogen concentration is an effective and selective way to treat hormone-dependent breast cancer in postmenopausal women. It has no estrogenic or progestogen activity, while low androgenic activity was observed as a result of high doses of the drug. After oral administration, the drug is rapidly and extensively absorbed from the gastrointestinal tract. The absolute bioavailability of the drug is unknown in humans (most likely it is limited by a strong first-pass effect). Administration of the drug with food increases the bioavailability. After a single dose of 25 mg, the maximum plasma concentration is achieved after 2 hours. The drug is 90% bound to plasma proteins. Exemestane and its metabolites are associated with red blood cells. It is metabolized by oxidation with CYP3A4 and / or keto reduction by aldoketoreductase followed by a coupling process. Metabolites are inactive or less sensitive to aromatase than the parent compound. The drug is excreted from the body in equal parts with urine and faeces. T_0,5 drug is 24 hours.

Hypersensitivity to the active substance or any of the other ingredients of the medicine. Women before menopause. Pregnancy and breastfeeding.

Before starting treatment, the activity of LH, FSH and serum estradiol should be determined to ensure that the patient is post-menopausal. Exemestane should be used with caution in patients with impaired liver or kidney function. Due to the risk of bone mineral density decrease and increased fracture incidence, at the beginning of exemestane adjuvant treatment in women with osteoporosis or a high risk of osteoporosis, the bone mineral density should be assessed by densitometry. Patients should be monitored for reduction in bone density and, if necessary, osteoporosis treatment should be instituted. It is not recommended for use in children and adolescents.

The drug is contraindicated during pregnancy and stone breastfeeding. The doctor should discuss the need to use adequate contraception, a patient who could potentially become pregnant, including perimenopausal women, or women who have recently been through the menopause, until they are fully sure that the patient is after menopause.

Very often: insomnia, headache, hot flushes, nausea, increased sweating, joint pain and musculoskeletal pain (including joint pain and less often: limb pain, osteoarthritis, backache, arthritis, myalgia and stiffness) joints), feeling of excessive fatigue. Common: anorexia, depression, dizziness, carpal tunnel syndrome, abdominal pain, vomiting, constipation, dyspepsia, diarrhea, rash, alopecia, osteoporosis, fractures, pain, peripheral edema. Uncommon: drowsiness, weakness. Severe thrombocytopenia and leukopenia have been reported rarely in patients with advanced breast cancer. An occasional decrease in the number of lymphocytes in the blood has been observed, especially in those with pre-existing lymphopenia in approximately 20% of patients receiving exemestane; however, the average number of lymphocytes in these patients did not change significantly over time and there was no increase in the frequency of coexisting viral infections. This type of activity was not observed in patients treated in the early stages of breast cancer development.There was a slight increase in blood parameters including liver enzymes, bilirubin and alkaline phosphatase. In the early breast cancer study, the incidence of ischemic heart changes in the arms with exemestane and Tamoxifen was 4.5% vs. 4.2%. There were no significant differences in the incidence of cardiac complications including arterial hypertension (9.9% vs. 8.4%), myocardial infarction (0.6% vs. 0.2%) and heart failure (1.1 % vs. 0.7%). In the early breast cancer study, exemestane was associated with a higher incidence of hypercholesterolemia compared to tamoxifen (3.7% vs. 2.1%). In a separate, randomized, double-blind clinical trial of postmenopausal women with early-stage low-risk breast cancer treated with exemestane or placebo for 24 months, exemestane was associated with a reduction in serum HDL-cholesterol of 7-9% on average, compared with an increase of 1% in the placebo group. There was also a 5-6% decrease in apolipoprotein A1 in the exemestane group, compared to a reduction of 0-2% in the placebo group. In both groups, the effect on other analyzed lipid parameters (total cholesterol, LDL cholesterol, triglycerides, apolipoprotein B and lipoprotein A) was very similar. The clinical significance of these results is not explained. In the early breast cancer study, a higher incidence of gastric ulcer was observed in the arm with exemestane compared to the tamoxifen arm (0.7% and <0.1%, respectively). Most patients receiving exemestane who had a stomach ulcer, received NSAIDs or reported previous history of peptic ulcer disease. Side effects seen after the medicine has been marketed: hepatitis, including cholestatic hepatitis.

Orally. Adults, also elderly patients: the recommended dose is 1 tablet. once a day, preferably after a meal. In patients with early breast cancer, treatment should be continued for 5 years as a supplement to previous tamoxifen therapy or be terminated earlier if tumor recurs. In patients with advanced breast cancer, treatment with exemestane should be continued until a definite tumor progression is observed. No dosage adjustment is required in patients with renal or hepatic impairment.