Aromasin

"Aromasin" (exemestane) is a drug that belongs to the class of aromatase inhibitors. It is used in oncology to treat breast cancer in women after menopause. Breast cancer in this category of patients often depends on estrogens for its growth.

Aromasin reduces estrogen levels in postmenopausal women by blocking the action of the enzyme aromatase, which converts androgens to estrogens in fat and other tissues. Because breast cancer can be sensitive to estrogen, reducing estrogen levels in the body may slow the growth and spread of the tumor.

The drug is usually taken as a tablet, usually daily. The dosage and duration of treatment are determined by the doctor based on the patient's specific situation and the characteristics of the breast cancer.

Indications Aromasin

• In postmenopausal women with hormone-dependent breast cancer:

  • As primary therapy after surgery (adjuvant therapy) to reduce the risk of recurrence.
  • As a therapy for metastatic breast cancer.

• In women with breast cancer whose disease progresses after tamoxifen therapy.

Release form

The drug "Aromasin" is produced in the form of tablets for oral (internal) administration. Tablets usually have different dosages, which allows the doctor to choose the optimal treatment regimen depending on the individual characteristics of the patient and the characteristics of the disease.

Available dosages may vary depending on the country and manufacturer, but are typically 25 mg or 50 mg.

The tablets are usually packaged in blisters or bottles, which ensures convenience and accuracy of drug dosage.

Pharmacodynamics

The pharmacodynamics of "Aromasin" is related to its ability to inhibit the aromatase enzyme, which is involved in the conversion of androgens into estrogens. Exemestane is a third-generation non-steroidal selective aromatase inhibitor.

Aromatase is an enzyme that catalyzes the conversion of androgens such as testosterone to estrogens, especially estradiol, in adipose tissue and other tissues of the body, including tumor tissue in breast cancer patients.

By acting as an aromatase inhibitor, exemestane reduces the level of estrogens in a woman's body, which leads to inhibition of the growth of estrogen-dependent breast tumors.

Thus, the main mechanism of action of Aromasin is to block the formation of estrogens in postmenopausal women, which helps in the treatment and prevention of the growth of cancer cells sensitive to estrogens and reduces the risk of recurrence of breast cancer.

Pharmacokinetics

• Absorption: Exemestane is absorbed from the gastrointestinal tract rapidly and completely after oral administration. It is usually taken daily.
• Distribution: Exemestane is well distributed throughout the body tissues, including adipose tissue. The volume of distribution is approximately 15 liters.
• Metabolism: Exemestane undergoes metabolism in the liver to form active metabolites. The main metabolite, 17-dehydroexemestane, also has aromatase inhibitory properties.
• Excretion: The main route of excretion of exemestane and its metabolites from the body is through the kidneys and bile.
• Elimination half-life: The elimination half-life of exemestane is approximately 24 hours. However, its active metabolites may have a longer half-life.

Dosing and administration

For the treatment of breast cancer in postmenopausal women:

• The recommended dose of Aromasin is 25 mg daily.
• The tablet is usually taken daily, preferably at the same time with or after meals.

Use Aromasin during pregnancy

• Reproductive toxicity:

  • Studies in rats and rabbits have shown that exemestane may cause reproductive toxicity. In studies with oral administration of exemestane in rats, increases in resorptions and decreases in fetal body weight were observed at doses exceeding the pharmacologically active dose (Beltrame et al., 2001).

• Mechanism of action:

  • Exemestane is a steroidal aromatase inhibitor that irreversibly blocks the conversion of androgens to estrogens. This results in a significant reduction in estrogen levels in the body, which is important for the treatment of hormone-dependent breast cancer in postmenopausal women (Geisler et al., 1998).

• Clinical studies:

  • In clinical trials in postmenopausal women with breast cancer, exemestane was highly effective in reducing estrogen levels and was well tolerated. However, there are no data on its use during pregnancy, as the drug is not intended for use in pregnant women (Robinson, 2008).

• Recommendations for use:

  • Exemestane is contraindicated during pregnancy and lactation due to the risk of serious adverse effects on the fetus, including potential for teratogenicity. The drug should only be used in postmenopausal women for the treatment of breast cancer (Clemett & Lamb, 1998).

Contraindications

• Pregnancy and breastfeeding: The drug is contraindicated for use in pregnant and lactating women, as it may harm the development of the fetus or child.
• Hypersensitivity: If the patient has a known hypersensitivity to exemestane or other components of the drug, its use is also contraindicated.
• Premenopausal Conditions: Aromasin is intended for use in postmenopausal women only and is not recommended for use in women before menopause.
• Conditions requiring estrogen therapy: If a patient requires estrogen therapy (for example, for the treatment of osteoporosis), Aromasin may be contraindicated.
• Severe liver dysfunction: Since exemestane is metabolized in the liver, it may be contraindicated in patients with severe liver dysfunction.

Side effects Aromasin

• Headache: Mild to moderate headache may occur.
• Hypercholesterolemia: Increased levels of cholesterol in the blood.
• Hypertension: Increased blood pressure.
• Joint and muscle pain: Pain and discomfort in the joints and muscles may occur.
• Heat: You may experience a feeling of heat or hot flashes.
• Drowsiness or insomnia: Some patients may experience drowsiness, while others may experience insomnia.
• Decreased bone density: Decreased bone density may occur, increasing the risk of osteoporosis and fractures.
• Decreased appetite: Some patients may experience decreased appetite.
• Depression or mood: Some patients may experience mood disturbances, including depression or anxiety.
• Gastrointestinal disorders: Diarrhea, nausea, vomiting, dyspepsia or constipation may occur.

Overdose

An overdose of "Aromasin" may lead to an increase in the side effects described earlier, such as headache, hypercholesterolemia, hypertension, joint and muscle pain, fever and others.

Interactions with other drugs

• Estrogens: Using estrogens with Aromasin may reduce its effectiveness because they may compete for aromatase binding sites.
• CYP3A4 enzyme inducers: Drugs that are CYP3A4 enzyme inducers (eg, rifampicin, carbamazepine, phenytoin) can accelerate the metabolism of Aromasin and reduce its concentration in the blood.
• CYP3A4 enzyme inhibitors: Drugs that are CYP3A4 enzyme inhibitors (eg, ketoconazole, atazanavir, clarithromycin) may slow down the metabolism of Aromasin and increase its concentration in the blood.
• Warfarin and other anticoagulants: Aromasin may increase the effect of anticoagulants, which may lead to increased anticoagulant effect and increased risk of bleeding.

Storage conditions

• Store the drug at room temperature, protected from moisture and direct sunlight.
• Avoid storing the medicine in places exposed to high temperatures or humidity, such as bathrooms.
• Keep Aromasin out of reach of children, preferably in a closed package.
• Check the expiration date of the drug and do not use it after the expiration date.
• If the instructions for use indicate that the drug should be stored in the refrigerator, it should be stored at a temperature of 2°C to 8°C.