Composition
Active ingredients:
exemestane 25 mg.
Auxiliary substances:
mannitol,
hypromellose,
polysorbate 80,
crospovidone,
colloidal hydrated silicon dioxide,
microcrystalline cellulose,
sodium carboxymethyl starch,
magnesium stearate.
Composition of the sugar shell:
hypromellose,
simethicone emulsion,
macrogol 6000,
magnesium carbonate,
titanium dioxide,
methyl p-hydroxybenzoate,
polyvinyl alcohol,
sucrose.
Pharmacological action
Pharmacodynamics
An irreversible steroid aromatase inhibitor, similar in structure to the natural substance androstenedione. In postmenopausal women, estrogens are produced primarily by the conversion of androgens to estrogens under the action of the aromatase enzyme in peripheral tissues. Blocking estrogen production by inhibiting aromatase is an effective and selective treatment for hormone-dependent breast cancer in postmenopausal women. The mechanism of action of Aromazin® is due to the fact that it irreversibly binds to the active fragment of the enzyme, causing its inactivation.
In postmenopausal women, Aromasin ® significantly reduces the concentration of estrogens in the blood serum, starting with a dose of 5 mg, and the maximum reduction (>90%) is achieved with doses of 10-25 mg. In postmenopausal women diagnosed with breast cancer who received 25 mg of the drug daily, the total level of the aromatase enzyme in the body decreased by 98%.
Exemestane does not have progestogenic and estrogenic activity. Only insignificant androgenic activity is detected, mainly when used in high doses.
Aromazin® 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 the content of LH and FSH in the blood serum, which is characteristic of drugs of this pharmacological group and probably develops on the principle of feedback at the pituitary level: a decrease in the concentration of estrogens stimulates the secretion of gonadotropins in the pituitary gland also in postmenopausal women.
Pharmacokinetics
Suction
After oral use, exemestane is rapidly absorbed, mainly from the gastrointestinal tract. 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 25 mg, Cmax in plasma is 17 ng / ml and is reached after 2 hours. Simultaneous food intake increases the bioavailability of the drug by 40%.
The pharmacokinetic parameters of exemestane are linear.
Distribution
Binding to plasma proteins is approximately 90%. Exemestane and its metabolites do not bind to red blood cells. When repeated use of unpredictable accumulation of exemestane is not observed.
Metabolism
The process of biotransformation of exemestane is carried out by oxidation of the methylene group in position 6 under the action of the SUR 3 A 4 isoenzyme and/or reduction of the 17-keto group under the action of aldoketoreductase, followed by conjugation. The metabolites of exemestane are either inactive or less active in aromatase inhibition than the parent compound.
Deduction
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 unchanged in the urine.
Pharmacokinetics in special clinical cases
There is no significant association between systemic exposure to the drug and age.
In patients with severe renal insufficiency (CC
In patients with moderate or severe hepatic insufficiency, the systemic effect of exemestane is 2-3 times higher, but no dose adjustment is required.
Indications
- Common breast cancer in women, in natural or induced postmenopausal women with the progression of the disease on the background of anti-estrogen therapy and the progression of the disease after repeated application of different types of hormonal therapy;
- adjuvant therapy of early breast cancer in postmenopausal women with estrogen-receptor positive or of unknown receptor status, after 2-3 years of initial adjuvant therapy with tamoxifen, with the aim of reducing the risk of recurrence (distant or regional), and contralateral breast cancer.
Use during pregnancy and lactation
Aromazin® is contraindicated for use during pregnancy and lactation.
Contraindications
- Premenopausal endocrine status;
- pregnancy;
- lactation (breastfeeding);
- hypersensitivity to exemestane or to any other component of the drug.
With caution: the drug should be used in case of impaired liver or kidney function.
Side effects
Undesirable effects when using the drug at a dose of 25 mg / day are insignificant or moderate.
Adverse reactions are listed below, distributed by body system and frequency:
- very often ( > 10%);>
- often ( > 1%, >< 10%);
- infrequently ( > 0,1%, >< 1%);
- rare ( > 0.01%, >
From the digestive system: very often-nausea; often-anorexia, abdominal pain, vomiting, constipation, dyspepsia, diarrhea.
From the central and peripheral nervous system: very often – insomnia, headache; often-depression, dizziness, carpal tunnel syndrome.
From the cardiovascular system: very often – hot flashes.
Dermatological reactions: very often – sweating; often-rash, alopecia.
From the musculoskeletal system: very often – joint and musculoskeletal pain.
Other: very often-increased fatigue; often-pain of unspecified localization, peripheral edema or swelling of the legs.
Approximately 20% of patients (especially those with baseline 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 there was no concomitant increase in the incidence of viral infections.
Sometimes there was an increase in the activity of liver enzymes and alkaline phosphatase, mainly in patients with liver and bone metastases, as well as in the presence of other liver lesions (it was not established whether these changes were associated with taking the drug or not).
Interaction
Preparations containing estrogens, when used simultaneously with Aromasin, completely neutralize its pharmacological effect.
Exemestane is metabolized by CYP3A4 and aldoketoreductases and does not inhibit any of the major CYP isoenzymes.
Specific inhibition of CYP3A4 by ketoconazole does not significantly affect 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, so no dose adjustment is required.
How to take, course of use and dosage
Assign inside. For adults and elderly patients, the recommended dose is 25 mg 1 time / day, preferably after a meal.
In early breast cancer, treatment with the drug is recommended to continue until the total duration of consecutive adjuvant hormone therapy reaches 5 years. Treatment of patients with advanced breast cancer is long-term. Aromasin treatment should be discontinued if there are signs of tumor progression or if contralateral breast cancer occurs.
In case of hepatic or renal insufficiency, no dose adjustment is required.
It is not recommended to use the drug in children.
Overdose
Symptoms: A single dose of the drug that could cause life-threatening symptoms has not been determined. 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.
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.
Special instructions
Aromasin® should not be prescribed to women with premenopausal endocrine status, therefore, in cases where this is clinically justified, postmenopausal status should be confirmed by determining the level of LH, FSH and estradiol.
Aromasin® should not be administered concomitantly with drugs containing estrogens.
Influence on the ability to drive vehicles and other mechanisms that require increased concentration of attention
Patients should be warned about the possibility of drowsiness, asthenia and dizziness during Aromasin treatment. If these symptoms occur, patients are advised to refrain from driving a car or engaging in other potentially dangerous activities that require increased concentration of attention and speed of psychomotor reactions.
Form of production
Film-coated tablets
Storage conditions
At a temperature not exceeding 30 °C
Shelf life
3 years
Active ingredient
Exemestane
Conditions of release from pharmacies
By prescription
Dosage form
Tablets
Purpose
For women, For adults as prescribed by a doctor
Indications
Breast Cancer, Cancer
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