Brand name: Aromasin
Active ingredient ( generic name): Exemestane
Manufacturer: Pfizer
Importer: Behestan Darou
Pharmacotherapeutic group: anti-neoplastic agent
Pharmaceutical form: 25mg coated tablets
Pharmacodynamic:
Exemestane is an irreversible, steroidal aromatase inhibitor, structurally related to the natural substrate androstenedione. In post-menopausal women, oestrogens are produced primarily from the conversion of androgens into oestrogens through the aromatase enzyme in peripheral tissues. Oestrogen deprivation through aromatase inhibition is an effective and selective treatment for hormone dependent breast cancer in postmenopausal women.
Exemestane does not possess any progestogenic or oestrogenic activity. A slight androgenic activity, probably due to the 17-hydro derivative, has been observed mainly at high doses. In multiple daily doses trials, Aromasin had no detectable effects on adrenal biosynthesis of cortisol or aldosterone, measured before or after ACTH challenge, thus demonstrating its selectivity with regard to the other enzymes involved in the steroidogenic pathway.
Pharmacokinetic:
Aromasin absorption is rapidly and concomitant intake with oily food increases the bioavailability.
Binding to plasma proteins is 90% and the terminal elimination half-life is 24h and it’s metabolized by
Oxidation and conjugation. Aromasin and its metabolites (mostly inactive) excrete in liver and kidney.
Uses and Administration:
Aromasin is indicated for the adjuvant treatment of postmenopausal women with oestrogen receptor positive invasive early breast cancer, following 2 – 3 years of initial adjuvant Tamoxifen therapy. For treatment of advanced breast cancer if tumors relapse occur.
The recommended dose of Aromasin is one 25 mg tablet to be taken once daily, preferably after a meal.
No dose adjustments are required for patients with hepatic or renal insufficiency.
Adverse reaction:
Common side effects of Aromasin are:
Hot flashes, Nausea, fatigue, increased sweating and dizziness; less common are headache, insomnia, anorexia, depression, vomiting, constipation, dyspepsia, peripheral oedema and elevated liver enzymes.
Contraindication:
No specific contraindication is reported. Aromasin should not be co-administered with oestrogen-containing medicines as these would negate its pharmacological action.
Warnings and precautions:
Aromasin should not be administered to women with pre-menopausal endocrine status. Therefore, whenever clinically appropriate, the post-menopausal status should be ascertained by assessment of LH, FSH and oestradiol levels.
Aromasin should be used with caution in patients with hepatic or renal impairment.
Aromasin tablets contain sucrose and should not be administered to patients with rare hereditary problems of fructose intolerance, glucose-galactose malabsorption or sucrase-isomaltase insufficiency.
Aromasin tablets contain methyl-p-hydroxybenzoate which may cause allergic reactions (possibly delayed).
Aromasin is a potent oestrogen lowering agent, and a reduction in bone mineral density and an increased fracture rate-has been observed following administration. During adjuvant treatment with Aromasin, women with osteoporosis or at risk of osteoporosis should have their bone mineral density formally assessed by bone densitometry at the commencement of treatment. Although adequate data to show the effects of therapy in the treatment of the bone mineral density loss caused by Aromasin are not available, treatment for osteoporosis should be initiated in at risk patients. Patients treated with Aromasin should be carefully monitored.
Pregnancy and lactation:
Aromasin is in group D, therefore should not be administered by pregnant or lactating women.
Storage temperature: Room temperature (15-30 C).
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