Exemestane

Exemestane

An anti-tumour drug, aromatase inhibitor, similar in structure to the natural steroid hormone androstenedione.

In postmenopausal women, estrogens are produced mainly by the conversion of androgens to estrogens by the aromatase enzyme in peripheral tissues. The mechanism of action of Exemestane is due to irreversible binding to the active aromatase fragment, resulting in inactivation of the enzyme.

Exemestane has no progestogenic or estrogenic activity. When used in high doses, only slight androgenic activity is seen. There is no effect on cortisol and aldosterone biosynthesis in the adrenal glands.

Slight increases in serum LH and FSH levels are observed even at low doses of exemestane. This effect, however, is uncharacteristic of drugs in this pharmacological group. It probably develops in a feedback loop at the pituitary level: a decrease in estrogen concentration stimulates gonadotropin secretion in the pituitary also in postmenopausal women.

Dosage regimen

The method of administration and the dosage regime of a particular drug depend on its form of release and other factors. The optimum dosing regimen is determined by the doctor. It should be strictly followed in accordance with the dosage form used for the particular drug indications and the dosing regimen.

When administered orally, the recommended dosage for adults and elderly patients is 25 mg once daily, preferably after meals. Treatment should be continued until there are signs of tumour progression, after which it is recommended to adjust the treatment.

No dose adjustment is necessary in the case of hepatic or renal impairment.

Side effects

• CNS disorders: common - fatigue, dizziness; sometimes - headache, insomnia, depression, asthenia.
• The digestive system: frequently - nausea, sometimes - abdominal pain, anorexia, constipation, dyspepsia, rarely - increased liver function tests in serum, increased alkaline phosphate level.
• Endocrine system: often - hot flashes (hot flashes).
• Dermatological reactions: possible - skin rash, alopecia.
• Blood system: often - decreased lymphocyte count; rarely - thrombocytopenia, leukopenia.
• Metabolism: possible - peripheral edema (edema of feet, shins).
• Other: often - increased sweating.

Special directions

It should not be used in women with premenopausal endocrine status because the evaluation of the efficacy and safety of the drug in this category of patients has not been carried out. Postmenopausal status should be confirmed by determining LH, FSH and oestradiol levels in those cases where it is clinically indicated.

Patients with baseline lymphopenia are at increased risk of reduced lymphocyte counts. Increased serum liver function tests and elevated alkaline phosphate levels have been reported mainly in patients with liver and bone metastases as well as in patients with other liver lesions.

It is not recommended for use in children.

Effect on driving and operating ability

Patients should be aware that drowsiness and dizziness may occur when performing work requiring concentration and high speed of psychomotor reactions.

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