Aromasin 25 (exemestane) works as a steroidal aromatase inhibitor, functioning to reduce estrogen production by blocking the enzyme responsible. It was developed for postmenopausal women battling cancer and in particular need of aggressive therapy, where first-line medications have not worked successfully. On the average, Aromasin 25 (exemestane) has an 85% rate for estrogen suppression, which makes it effective for treating cancer since certain cancers grow due to the body’s estrogen supply. Cut the estrogen and you help slow down the cancer. As for steroids use, Aromasin 25 is a good option because male bodybuilders don’t have to worry about aromatization, the conversion of estrogen in the body, which is then responsible for side effects like acne, water retention, and gynecomastia. It is also not too harsh on blood lipids which make it great for long cycles. Since it also raises testosterone levels, it also makes Aromasinor a great component of a Post-Cycle-Therapy.
The recommended dose of exemestane is one film-coated tablet (25 mg) to be taken orally once a day, preferably after a meal.
In patients with early breast cancer, treatment with exemestane should continue until completion of five years of combined sequential adjuvant hormonal therapy (tamoxifen followed by exemestane), or earlier if tumour relapse occurs.
In patients with advanced breast cancer, treatment with exemestane should continue until tumour progression is evident.
No dose adjustments are required for patients with hepatic or renal impairment (see section 5.2).
Not recommended for use in children and adolescents
Exemestane is contraindicated in
– patients with hypersensitivity to the active substance or to any of the excipients listed in section 6.1.
– pre-menopausal women.
– pregnant or lactating women.
4.4 Special warnings and precautions for use
Exemestane 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.
Exemestane should be used with caution in patients with hepatic or renal impairment.
Exemestane tablets contain glucose and should not be administered to patients with rare glucose-galactose malabsorption.
Aromasin 25 is a potent oestrogen lowering agent, and a reduction in bone mineral density (BMD) and an increased fracture rate has been observed following administration (see section 5.1). At the commencement of adjuvant treatment with exemestane, women with osteoporosis or at risk of osteoporosis should have treatment baseline bone mineral health assessment, based on current clinical guidelines and practice. Patients with advanced disease should have their bone mineral density assessed on a case by case basis. Although adequate data to show the effects of therapy in the treatment of the bone mineral density loss caused by exemestane are not available, patients treated with exemestane should be carefully monitored and treatment for, or prophylaxis of, osteoporosis should be initiated in at risk patients.
Routine assessment of 25 hydroxy vitamin D levels prior to the start of aromatase inhibitor treatment should be considered, due to the high prevalence of severe deficiency in women with early breast cancer (EBC). Women with Vitamin D deficiency should receive supplementation with Vitamin D.
4.5 Interaction with other medicinal products and other forms of interaction
In vitro evidence showed that the drug is metabolised through cytochrome P450 (CYP) 3A4 and aldoketoreductases (see section 5.2) and does not inhibit any of the major CYP isoenzymes. In a clinical pharmacokinetic study, the specific inhibition of CYP 3A4 by ketoconazole showed no significant effects on the pharmacokinetics of exemestane. Probably CYP3A4 catalyses a secondary route of metabolism of exemestane.
In an interaction study with rifampicin, a potent CYP450 inducer, at a dose of 600 mg daily and a single dose of exemestane 25 mg, the AUC of exemestane was reduced by 54% and Cmax by 41%. Since the clinical relevance of this interaction has not been evaluated, the co-administration of drugs, such as rifampicin, anticonvulsants (e.g. phenytoin and carbamazepine) and herbal preparations containing Hypericum perforatum (St John’s Wort) known to induce CYP3A4 may reduce the efficacy of exemestane.
Exemestane should be used cautiously with drugs that are metabolised via CYP3A4 and have a narrow therapeutic window. There is no clinical experience of the concomitant use of exemestane with other anticancer drugs.
Exemestane should not be co-administered with oestrogen-containing medicines as these would negate its pharmacological action.
4.6 Fertility, pregnancy and lactation
No clinical data on exposed pregnancies are available with exemestane. Studies on animals have shown reproductive toxicity. Exemestane is therefore contraindicated in pregnant women.
It is not known whether exemestane is excreted into human milk. Exemestane should not be administered to lactating woman.
Women of perimenopausal status or child-bearing potential
The physician needs to discuss the necessity of adequate contraception with women who have the potential to become pregnant including women who are perimenopausal or who have recently become postmenopausal, until their postmenopausal status is fully established (see sections 4.3 and 4.4).
4.7 Effects on ability to drive and use machines
Drowsiness, somnolence, asthenia and dizziness have been reported with the use of the drug. Patients should be advised that, if these events occur, their physical and/or mental abilities required for operating machinery or driving a car may be impaired.
4.8 Undesirable effects
Exemestane was generally well tolerated across all clinical studies conducted with exemestane at a standard dose of 25 mg/day, and undesirable effects were usually mild to moderate.
The withdrawal rate due to adverse events was 7.4% in patients with early breast cancer receiving adjuvant treatment with exemestane following initial adjuvant tamoxifen therapy.
The most commonly reported adverse reactions were hot flushes (22%), arthralgia (18%) and fatigue (16%).
The withdrawal rate due to adverse events was 2.8% in the overall patient population with advanced breast cancer. The most commonly reported adverse reactions were hot flushes (14%) and nausea (12%).
Most adverse reactions can be attributed to the normal pharmacological consequences of oestrogen deprivation (e.g. hot flushes).
The reported adverse reactions from clinical studies and post-marketing experience are listed below by system organ class and by frequency. http://konozahealthbiotech.com