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 fatty tissue and other tissues. Because breast cancer can be sensitive to estrogen, reducing estrogen levels in the body can slow the growth and spread of the tumor.

The drug is usually taken in tablet form, usually daily. The dosage regimen and duration of treatment are determined by the doctor depending 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 therapy for metastatic breast cancer.

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

Release form

The drug "Aromasin" is available 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 by country and manufacturer, but are typically 25 mg or 50 mg.

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

Pharmacodynamics

The pharmacodynamics of "Aromasin" is associated with its ability to inhibit the enzyme aromatase, 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, into estrogens, especially estradiol, in adipose tissue and other tissues of the body, including tumor tissue in patients with breast cancer.

Acting as an aromatase inhibitor, exemestane reduces the level of estrogen 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 estrogen in postmenopausal women, which helps in the treatment and prevention of the growth of estrogen-sensitive cancer cells and reduces the risk of breast cancer recurrence.

Pharmacokinetics

• Absorption: Exemestane is absorbed from the gastrointestinal tract quickly and completely after oral administration. It is usually taken daily.
• Distribution: Exemestane is well distributed throughout body tissues, including adipose tissue. The distribution volume is approximately 15 liters.
• Metabolism: Exemestane undergoes metabolism in the liver to form active metabolites. The main metabolite, 17-dihydroexemestane, 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.
• Half-life: The half-life of exemestane from the body 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 exemestane in rats, increases in resorptions and decreases in fetal body weight were observed at doses above pharmacologically active doses (Beltrame et al., 2001).

• Mechanism of action:

  • Exemestane is a steroidal aromatase inhibitor that irreversibly blocks the conversion of androgens to estrogens. This leads to a significant decrease 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 on postmenopausal women with breast cancer, exemestane showed high effectiveness in reducing estrogen levels and was well tolerated. However, there is 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 to the fetus, including the potential for teratogenicity. The drug should only be used in postmenopausal women to treat breast cancer (Clemett & Lamb, 1998).

Contraindications

• Pregnancy and breastfeeding: The drug is contraindicated for use in pregnant and breastfeeding 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: Aromasin is intended for use only in postmenopausal women and is not recommended for use in premenopausal women.
• Conditions requiring estrogen use: If the patient requires treatment with estrogen (for example, in the treatment of osteoporosis), Aromasin may be contraindicated.
• Severe hepatic impairment: Because exemestane is metabolized in the liver, it may be contraindicated in patients with severe liver impairment.

Side effects Aromasin

• Headache: Mild to moderate headache may occur.
• Hypercholesterolemia: Increased cholesterol levels in the blood.
• Hypertension: Increased blood pressure.
• Joint and muscle pain: Pain and discomfort in the joints and muscles may occur.
• Fever: You may feel hot or flushed.
• Drowsiness or insomnia: Some patients may experience drowsiness and others may experience insomnia.
• Decreased bone density: There may be a decrease in bone density, which increases 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, indigestion, or constipation may occur.

Overdose

An overdose of Aromasin can lead to increased side effects described earlier, such as headache, hypercholesterolemia, hypertension, joint and muscle pain, fever and others.

Interactions with other drugs

• Estrogen: The use of estrogens together with Aromasin may reduce its effectiveness, as they may compete for binding sites with aromatase.
• CYP3A4 enzyme inducers: Drugs that are CYP3A4 enzyme inducers (for example, 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 (for example, 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 result in increased anticoagulant effect and increased risk of bleeding.

Storage conditions

• Store the drug at room temperature, protected from humidity and direct exposure to sunlight.
• Avoid storing the drug in places exposed to high temperatures or humidity, such as bathrooms.
• Keep "Aromasin" out of the 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 to store the drug in the refrigerator, it should be stored at a temperature of 2°C to 8°C.