Aromasin coated pills 25mg N30
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Active ingredients
Exemestane
Release form
Pills
Composition
Active ingredient: Eksemestanan active substance concentration (mg): 25 mg
Pharmacological effect
An irreversible steroid aromatase inhibitor, similar in structure to the natural substance androstenedione. In postmenopausal women, estrogens are produced mainly by the conversion of androgens into estrogens by the action of the aromatase enzyme in peripheral tissues. Blocking the formation of estrogen by inhibiting aromatase is an effective and selective treatment for hormone-dependent breast cancer in postmenopausal women. The mechanism of action of the drug Aromazin due to the fact that it irreversibly binds to the active fragment of the enzyme, causing its inactivation. In postmenopausal women, Aromasin reliably reduces the concentration of estrogen in the blood serum, starting with a dose of 5 mg, and the maximum decrease (more than 90%) is achieved with the use of doses of 10-25 mg. In postmenopausal patients with a diagnosis of breast cancer who received 25 mg of the drug daily, the total level of the enzyme aromatase in the body decreased by 98%. Exemestane does not have progestogenic and estrogenic activity. Only minor androgenic activity is detected, mainly when used in high doses. Aromasin does not affect the biosynthesis of cortisol and aldosterone in the adrenal glands, which confirms the selectivity of the drug. In this regard, there is no need for replacement therapy with glucocorticoids and mineralocorticoids. When using the drug, even in low doses, there is a slight increase in serum LH and FSH levels, which is characteristic of drugs of this pharmacological group and probably develops on the basis of feedback at the level of pituitary: a decrease in the concentration of estrogen stimulates the secretion of gonadotropins in the pituitary gland also in postmenopausal women.
Pharmacokinetics
Absorption is rapidly absorbed, mainly from the gastrointestinal tract. The absolute bioavailability of the drug has not been established. It is assumed that it is limited by the extensive effect of the first passage through the liver. With a single dose of the drug in a dose of 25 mg Cmax in plasma is 17 ng / ml and is achieved after 2 hours.Simultaneous ingestion of food increases the bioavailability of the drug by 40%. The pharmacokinetic parameters of exemestane are linear. The distribution of plasma proteins is approximately 90%. Exemestane and its metabolites do not bind to red blood cells. When repeated administration of unpredictable cumulation of exemestane is not observed. Metabolism The process of biotransformation of exemestane is carried out by oxidation of the methylene group in 6 positions under the action of the isoenzyme CYP3A4 and / or reduction of the 17-keto group under the action of aldocetoreductase with subsequent conjugation. The metabolites of exemestane are either inactive or less active in relation to the inhibition of aromatase than the original compound. Injection The final T1 / 2 is approximately 24 hours. Approximately equal amounts of exemestane (about 40%) are excreted in the urine and feces during the week. From 0.1 to 1% is excreted in the urine unchanged. Pharmacokinetics in special clinical situations There is no marked connection between systemic exposure and age. In patients with severe renal failure (CC less than 30 ml / min), systemic exposure to exemestane is 2 times higher, however, dose adjustment is not required. In patients with moderate or severe liver failure, the systemic exposure to exemestane is 2-3 times higher, but dose adjustment is not required.
Indications
Common breast cancer in women in natural or induced postmenopause with the progression of the disease on the background of anti-estrogenic therapy, as well as with the progression of the disease after repeated use of various types of hormonal therapy; adjuvant treatment of early breast cancer in postmenopausal women with estrogen-positive receptors or with unknown receptor status, after completion of 2–3 years of initial adjuvant therapy with tamoxifen, in order to reduce the risk of recurrence (long-term or regional), as well as contralateral breast cancer .
Contraindications
Hypersensitivity to exemestane or to any other component of the drug; premenopausal endocrine status; pregnancy and lactation. With caution Impaired liver or kidney function.
Precautionary measures
Do not exceed the recommended dose. The drug should be used with caution in case of impaired liver or kidney function.
Use during pregnancy and lactation
Aromasin is contraindicated for use during pregnancy and lactation.
Dosage and administration
Inside. Elderly adults and patients The recommended dose is 25 mg 1 time per day, preferably after meals. In patients with early breast cancer, treatment with the drug is recommended to continue until the total duration of sequential adjuvant hormone therapy reaches 5 years. Treatment of patients with advanced breast cancer is a long-term. If there are signs of progression of a tumor disease or if a contralateral breast cancer appears, treatment with Aromasin should be discontinued. Hepatic or renal failure Dose adjustment is not required. Children are not recommended for use in children.
Side effects
In general, Aromasin is well tolerated; undesirable effects when using the drug in a dose of 25 mg / day are insignificant or moderately pronounced. The following are undesirable reactions distributed by body systems and frequency: very often (more than 10%), often (more than 1%, less than 10%), infrequently (more than 0.1%, less than 1%), rarely (more than 0.01%, less than 0.1% ). On the part of the digestive system: very often - nausea; often - anorexia, pain in the abdomen, vomiting, constipation, dyspepsia, diarrhea. From the central and peripheral nervous system: very often - insomnia, headache; often - depression, dizziness, carpal tunnel syndrome. From the vascular system: very often - flushes. From the skin and skin appendages: very often - sweating; often - rash, alopecia. From the musculoskeletal system: very often - joint and musculoskeletal pains. Other: very often - increased fatigue; often - pain of unspecified localization, peripheral edema or leg edema. Approximately 20% of patients (especially patients with initial lymphopenia) experienced a periodic decrease in the number of lymphocytes. However, the average number of lymphocytes in these patients did not change significantly over time, and a concomitant increase in the incidence of viral infections was not observed. Sometimes there was an increase in liver enzymes and alkaline phosphatase, mainly in patients with metastasis to the liver and bone, as well as in the presence of other lesions liver (not established, whether these changes are associated with taking the drug or not).
Overdose
A single dose of the drug that could cause life-threatening symptoms has not been established. The use of exemestane in a single dose of up to 800 mg in healthy women and in a daily dose of up to 600 mg in postmenopausal women with advanced breast cancer was well tolerated. The treatment: there are no specific antidotes. If necessary, symptomatic therapy should be carried out, as well as regular monitoring of vital functions and careful monitoring.
Interaction with other drugs
Drugs containing estrogens, while being used with Aromasin, completely level up its pharmacological action. Exemestanan is metabolized under the influence of CYP3A4 and aldoketoreductases and does not inhibit any of the major CYP isoenzymes. Specific inhibition of CYP3A4 by ketoconazole does not have a significant effect on the pharmacokinetics of exemestane. Despite the established pharmacokinetic interaction of exemestane with rifampicin, a strong inducer of CYP3A4, the pharmacological activity of Aromasin (estrogen suppression) remains unchanged, therefore, dose adjustment is not required.
special instructions
Aromasin should not be prescribed to women with premenopausal endocrine status, therefore, in cases where it is clinically justified, postmenopausal status should be confirmed by determining the level of LH, FSH and estradiol. and management of patients. Patients should be warned about the possibility of drowsiness, asthenia and dizziness during the treatment with Aromasin. If these symptoms occur, it is recommended that patients refrain from driving and other potentially hazardous activities that require increased concentration and psychomotor reactions.