Aromasin
Aromasin: instructions for use and reviews
- 1. Release form and composition
- 2. Pharmacological properties
- 3. Indications for use
- 4. Contraindications
- 5. Method of application and dosage
- 6. Side effects
- 7. Overdose
- 8. Special instructions
- 9. With impaired renal function
- 10. For violations of liver function
- 11. Use in the elderly
- 12. Drug interactions
- 13. Analogs
- 14. Terms and conditions of storage
- 15. Terms of dispensing from pharmacies
- 16. Reviews
- 17. Price in pharmacies
Latin name: Aromasin
ATX code: L02BG06
Active ingredient: Exemestan (Exemestanum)
Producer: Pfizer Manufacturing Deutschland (Germany)
Description and photo update: 2019-07-08
Prices in pharmacies: from 1131 rubles.
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Aromasin is a synthetic anticancer drug used to treat advanced breast cancer in women in induced or natural postmenopausal women.
Release form and composition
The drug is produced in the form of white sugar-coated tablets with an engraving “7663” on one side (15 pcs. In a blister, 1, 2, 6 blisters in a cardboard box).
The active ingredient is exemestane, in 1 tablet - 25 mg.
Excipients: crospovidone, mannitol, polysorbate 80, hypromellose, hydrated colloidal silicon dioxide, magnesium stearate, microcrystalline cellulose, sodium carboxymethyl starch.
Pharmacological properties
Pharmacodynamics
Exemestane belongs to irreversible steroidal aromatase inhibitors, the structure of which resembles the natural substance androstenedione.
In postmenopausal women, estrogens are produced mainly as a result of the conversion of androgens to estrogens under the influence of the aromatase enzyme in peripheral tissues. Prevention of estrogen formation by inhibiting aromatase is considered to be an effective and selective method of therapy for hormone-dependent breast cancers in postmenopausal women.
Exemestane irreversibly binds to the active component of the enzyme, which leads to its inactivation. According to confirmed data, the use of Aromasin in postmenopausal women lowers the level of estrogen in the serum when taking a dose of 5 mg or more, and the maximum decrease (more than 90%) is observed when the drug is prescribed at a dose of 10-25 mg. In postmenopausal women diagnosed with breast cancer, who receive 25 mg of exemestane daily, the total aromatase content in the body is reduced by 98%.
For exemestane estrogenic and progestogenic activity is not characteristic. Revealed only a slight androgenic activity, mainly when taking high doses. The substance does not participate in the processes of biosynthesis of aldosterone and cortisol in the adrenal glands, which proves the selectivity of the drug. Therefore, replacement therapy with mineralocorticoids and glucocorticoids is not necessary. When prescribing the drug, even in small doses, a slight increase in the content of luteinizing hormone and follicle-stimulating hormone in the blood serum is observed. This is due to the fact that a decrease in the level of estrogen in the body stimulates the production of gonadotropins in the pituitary gland also in postmenopausal patients.
Pharmacokinetics
After oral administration, exemestane is rapidly absorbed, mainly from the gastrointestinal tract. The absolute bioavailability of the substance has not been established, but there are suggestions that it depends on the extensive effect of the "first pass" through the liver. With a single dose of 25 mg, the maximum plasma exemestane content of 17 ng / ml is reached after 2 hours. When the drug is taken with food, its bioavailability increases by 40%.
The pharmacokinetic parameters are characterized by a linear relationship. The terminal half-life is approximately 24 hours. The active component of Aromasin binds to plasma proteins by approximately 90%. There is no binding of exemestane and its metabolites to erythrocytes. Repeated intake does not lead to an unpredictable accumulation of the substance.
The biotransformation of exemestane is carried out by oxidation of the methylene group in the 6th position under the influence of the CYP3A4 isoenzyme and / or reduction of the 17-keto group under the influence of aldoketo reductase with further conjugation. Exemestane metabolites are either inactive or less active in aromatase inhibition than the parent compound.
Exemestane is excreted in the urine and feces during the week in approximately equal amounts (about 40%). 0.1–1% of the substance is excreted in the urine unchanged.
The age of the patient and the systemic effects of Aromasin are not directly related. In patients with severe renal failure (creatinine clearance less than 30 ml / min), the systemic effect of the drug is 2 times higher, however, dose adjustment is not required. In patients with moderate to severe hepatic insufficiency, the systemic effect of the drug is 2-3 times higher, but there is no need for dose adjustment.
Indications for use
- Treatment of advanced breast cancer in women in induced or natural postmenopause (drug treatment is indicated after undergoing various types of hormonal therapy, as well as in cases of disease progression against the background of antiestrogen therapy);
- Adjuvant therapy for early breast cancer in postmenopausal women with estrogen-positive receptors (after completion of initial adjuvant tamoxifen therapy to reduce the risk of recurrence).
Contraindications
According to the instructions, Aromasin is contraindicated for women with premenopausal endocrine status, as well as with hypersensitivity to the active substance or to other components of the drug.
The use of the drug is contraindicated during pregnancy, lactation, and also in childhood.
Instructions for the use of Aromasin: method and dosage
Tablets are taken 1 pc. after meals 1 time per day.
In the early stages of breast cancer, the duration of treatment should be at least 5 years.
In cases of progression of the disease, the use of the drug should be discontinued.
Side effects
The drug can cause nausea, insomnia, headache, hot flashes, sweating, joint and muscle pain.
Much less often when taking the drug may be observed: anorexia, constipation, dizziness, pain of unspecified localization, leg edema, pain in the abdomen, alopecia, dyspepsia, vomiting, depression, diarrhea, carpal tunnel syndrome, rash, peripheral edema.
Overdose
A single dose of Aromasin that can lead to the development of fatal symptoms has not been established. Taking the drug 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 extensive breast cancer does not cause side effects.
There are no specific antidotes. If necessary, symptomatic therapy is performed. Patients who have taken high doses of Aromasin should remain under medical supervision for some time. Regular monitoring of vital signs is also recommended.
special instructions
No dose adjustment is required for renal or hepatic impairment.
Do not take the drug at the same time as medicinal products containing estrogens.
Influence on the ability to drive vehicles and complex mechanisms
Patients should be warned about the possibility of side effects such as dizziness, drowsiness and asthenia during the course of therapy. If these symptoms occur, it is recommended to refrain from driving and engaging in other potentially hazardous activities that require special concentration and immediate reactions.
With impaired renal function
The drug is used with caution in patients with impaired renal function.
For violations of liver function
The drug is prescribed with caution in case of liver dysfunction.
Use in the elderly
For elderly patients, the recommended dose of Aromasin is 25 mg once a day, preferably after meals.
Drug interactions
Estrogen-containing drugs completely neutralize the pharmacological action of Aromasin. Its active substance is metabolized by cytochrome P450 CYP3A4 and aldoketoreductases, therefore it is not able to inhibit any of the main CYP isoenzymes.
Ketoconazole specifically inhibits the CYP3A4 isoenzyme, however, no confirmed effect of this on the pharmacokinetics of exemestane has been identified. Although exemestane interacts pharmacokinetically with rifampicin, a potent inducer of the CYP3A4 isoenzyme, the pharmacological action of Aromasin remains unchanged, so no dose adjustment is required.
Analogs
The structural analogs of Aromasin include the drugs Aromeston and Exemestan-Teva.
Storage conditions and periods
Store at a temperature not exceeding 30 ° C.
The shelf life is 3 years.
Terms of dispensing from pharmacies
Dispensed by prescription.
Reviews about Aromasin
Most of the patients leave favorable reviews about Aromasin, noting that it is well tolerated. However, some patients complain of side effects of the drug, expressed in hot flashes, insomnia, nausea, pain in the back and joints. The prevailing opinion is that the drug is very effective for cancer, but it can only be taken as prescribed by a doctor.
Price for Aromasin in pharmacies
Depending on the region, the price of Aromasin averages 1,500-2,500 rubles per pack of 30 tablets.
Aromasin: prices in online pharmacies
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Drug name Price Pharmacy |
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Aromasin 25 mg film-coated tablets 30 pcs. 1131 RUB Buy |
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Aromasin tablets p.p. 25mg 30 pcs. 2248 RUB Buy |
Anna Kozlova Medical journalist About the author
Education: Rostov State Medical University, specialty "General Medicine".
Information about the drug is generalized, provided for informational purposes only and does not replace the official instructions. Self-medication is hazardous to health!
