Exemestane - instructions for use, analogs, reviews and release forms (25 mg Teva tablets) of a drug for the treatment of breast or breast cancer in adults, children and pregnancy. Composition

In this article, you can read the instructions for using the drug Exemestane. There are reviews of visitors to the site - consumers of this medication, as well as opinions of doctors of experts on the use of Exemestane in their practice. A big request is to actively add their feedback on the drug: the medicine helped or did not help get rid of the disease, which were observed complications and side effects, possibly not declared by the manufacturer in the annotation. Analogues of Exemestan in the presence of existing structural analogues. Use for the treatment of breast or breast cancer in adults, children, as well as during pregnancy and lactation. Composition of the preparation.

Exemestan - antitumor agent, aromatase inhibitor, similar in structure 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.

Composition

Exemestane + auxiliary substances.

Pharmacokinetics

After oral administration, it is rapidly absorbed from the gastrointestinal tract (GIT). With a single dose of 25 mg after meals, the maximum concentration is reached within 2 hours. The food improves the absorption: the level of exemestan in blood plasma achieved is 40% higher than after taking an empty stomach.

Exemestane is widely distributed in tissues. Binding to plasma proteins is about 90%, the degree of binding does not depend on the total concentration.

After repeated doses of 25 mg per day, the plasma concentration of the unchanged substance was similar to that after a single dose.

Exemestane is characterized by high clearance, mainly due to metabolism.As a result, numerous secondary metabolites are formed, but the amount of each is very small compared to the administered dose. With regard to the inhibition of aromatase, these metabolites are either inactive or less active than the unaltered substance.

It is excreted in the urine and with feces. Excretin and its metabolites are excreted from the body mainly within 1 week. Less than 1% is excreted in the urine unchanged.

Indications

• treatment of advanced breast cancer in women in natural or induced postmenopausal women who have progression of the disease on the background of anti-estrogen therapy.
• hormonal therapy for advanced breast cancer in women in natural or induced postmenopausal women who have a progression of the disease on the background of therapy with either non-steroid aromatase inhibitors or progestins.

Forms of release

The tablets covered with a cover of 25 mg.

Instructions for use and dosing regimen

If administered orally, the recommended dose for adults and elderly patients is 25 mg once daily, preferably after meals.

In patients in the early stages of breast cancer, Exemestan should be treated until the completion of a five-year combined sequential adjuvant hormone therapy or the occurrence of relapses of a tumor disease.

In patients with advanced breast cancer, treatment should continue until the progression of the tumor is obvious.

Side effect

• fatigue;
• dizziness;
• headache;
• insomnia;
• depression;
• asthenia (general weakness);
• nausea;
• abdominal pain;
• anorexia (pathological desire to lose weight);
• constipation;
• dyspepsia (indigestion);
• tides (paroxysmal sensations of heat);
• skin rash;
• alopecia (baldness);
• decrease in the level of lymphocytes;
• thrombocytopenia (decrease in the number of platelets);
• leukopenia (decrease in the number of leukocytes);
• edema of the feet, swelling of the legs;
• increased sweating.

Contraindications

• pregnancy;
• lactation (breastfeeding);
• hypersensitivity to eksemestan.

Application in pregnancy and lactation

Exemestane is contraindicated in pregnancy and lactation.

Use in children

It is not recommended for use in children.

special instructions

It should not be used in women with premenopausal endocrine status, as the effectiveness and safety of the drug in this category of patients was not evaluated. In cases where the need for application is clinically justified, postmenopausal status should be confirmed by determining the level of LH (luteinizing hormone), FSH (follicle-stimulating hormone) and estradiol.

In patients with initial lymphopenia, the risk of a decrease in the number of lymphocytes is increased. An increase in the indices of functional hepatic tests in the serum and an increase in the level of alkaline phosphatase was noted mainly in patients with metastases to the liver and bone, as well as in the presence of other liver lesions.

Impact on the ability to drive vehicles and manage mechanisms

When performing work related to the need for concentration of attention and high speed of psychomotor reactions, patients should be aware that with the application of Exemestane, drowsiness and dizziness may occur.

Drug Interactions

Preparations containing estrogens, when used simultaneously with eksemestanom completely level its pharmacological effect.

Until now, there have been no studies of the interaction of exemestane with other drugs. The results of in vitro studies have shown that exemestane is metabolized under the influence of the CYP3A4 isoenzyme and aldoketoreductases and does not inhibit any of the major CYP isoenzymes. In a clinical pharmacokinetic study, it was found that specific inhibition of the CYP3A4 isoenzyme by Ketoconazole does not cause significant changes in the pharmacokinetic parameters of exemestane. However, it is impossible to exclude a possible decrease in the concentration of exemestane in plasma under the influence of preparations that are inducers of the isoenzyme CYP3A4.

Analogues of the drug Exemestan

Structural analogs for the active substance:

• Aromasine;
• Aromeston;
• Exemestan TL;
• Teemestan Teva.

Analogues on the curative effect (remedies for the treatment of breast cancer):

• Abitaxel;
• Abraxan;
• Avastin;
• Alkeran;
• Aminoglutethimide;
• Anastrozole;
• Arimidex;
• Buserelin;
• Velba;
• Vepezid;
• Anastrozole;
• Vincristine;
• Mitomycin;
• Tamoxifen;
• Vinelbin;
• Vincristine;
• Vinorelbine;
• Gemcitabine;
• Herceptin;
• Depostat;
• Doxorubifer;
• Doxorubicin;
• Zitazonium;
• Zoladex;
• Zometa;
• Ikzempra;
• Intaksel;
• Kabetsin;
• Carboplatin;
• Kelix;
• Xeloda;
• Leukeran;
• Letrozole;
• Lomustine;
• Methotrexate;
• Miltex;
• Mitoxantrone;
• Mitotax;
• Novanthron;
• Novofen;
• Nolvadex;
• Octreotide;
• Omnadren;
• Oncotron;
• Paclitaxel;
• Paxen;
• Provera;
• Rubid;
• Selana;
• Sinestrol;
• Tayverb;
• Taxol;
• Taxotere;
• Tamoxen;
• Tamoxifen;
• Tautax;
• Treksan;
• Femara;
• Photosens;
• Ftorafur;
• Fluorouracil;
• Halavan;
• Holoksan;
• Cyclophosphane;
• Cytohem;
• Cytoxan;
• Egistrazole;
• Extrase;
• Aldesine;
• Endoxane;
• Epirubicin;
• The Estrolet;
• Etoposide;
• Etrusil;
• Yutaksan.

Review of the oncologist-mammalogist

The drug Exemestine I assign to patients in natural or induced postmenopausal. The drug is highly effective in advanced breast cancer if the disease progresses after an anti-estrogen treatment or if the malignant neoplasm does not respond to progestin or non-steroidal aromatase inhibitors. There are relatively few manifestations in Exemestan, the drug is well tolerated by women. Treatment schedule is simple - 1 tablet once a day. Therapy continues for the time being, there are clearly signs of progression of the cancerous tumor.

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