AROMASIN 25 MG 30 TAB

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Description

 AROMASIN 25 MG 30 TABS

  • Aromasin treats postmenopausal women with oestrogen receptor positive invasive early breast cancer (EBC), following 2 – 3 years of initial adjuvant tamoxifen therapy.

 

 

Active Ingredient of Aromasin 

exemestane

 

Pharmaceutical form

Coated tablet, Round, biconvex, off-white coated tablet marked 7663 on one side.

 

Therapeutic Indications of Aromasin 

  • Aromasin treats postmenopausal women with oestrogen receptor positive invasive early breast cancer (EBC), following 2 – 3 years of initial adjuvant tamoxifen therapy.
  • Aromasin treats advanced breast cancer in women with natural or induced postmenopausal status whose disease has progressed following anti-oestrogen therapy. Efficacy has not been demonstrated in patients with oestrogen receptor negative status.

 

Method of Administration and doses of Aromasin 

Adult and elderly patients

Take one 25 mg tablet of Aromasin once daily, preferably after a meal.

In patients with early breast cancer, treatment with Aromasin should continue until completion of five years of combined sequential adjuvant hormonal therapy (tamoxifen followed by Aromasin), or earlier if tumor relapse occurs.

In patients with advanced breast cancer, treatment with Aromasin should continue until tumour progression is evident.

HCP don’t need to make dose adjustments for patients with hepatic or renal insufficiency.

 

Drug Interactions with Aromasin 

In vitro evidence showed that the drug is metabolised through cytochrome P450 CYP3A4 and aldoketoreductases and does not inhibit any of the major CYP isoenzymes. A clinical pharmacokinetic study shows that the specific inhibition of CYP3A4 by ketoconazole has no significant effects on the pharmacokinetics of exemestane.

 

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 shows a reduction by 54% and Cmax by 41%.

Since the clinical relevance of this interaction has not been evaluated, the co-administration of medicinal products, 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 Aromasin.

Aromasin should be used cautiously with medicinal products that are metabolised via CYP3A4 and have a narrow therapeutic window. There is no clinical experience of the concomitant use of Aromasin with other anticancer medicines.

Don’t take Aromasin with oestrogen-containing medicines as these would negate its pharmacological action.

 

Special Populations

Pregnancy

No clinical data on exposed pregnancies are available with Aromasin. Studies on animals have shown reproductive toxicity. Pregnant Women shouldn’t take Aromasin.

 

Breast-feeding

Breastfeeding women shouldn’t take Aromasin. However, there are no enough studies to show whether it presents in human milk or not.

 

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.

 

Age

No significant correlation between the systemic exposure of Aromasin and the age of subjects has been observed.

 

Renal impairment

In patients with severe renal impairment (CLcr <30 ml/min) the systemic exposure to exemestane was 2 times higher compared with healthy volunteers.

Dose adjustment is not necessary.

 

Hepatic impairment

In patients with moderate or severe hepatic impairment the exposure of exemestane is 2-3 fold higher compared with healthy volunteers. Given the safety profile of exemestane, dose adjustment is not necessary.

 

 

Side effects of exemestane

Hot flushes
Fatigue
Headache
Insomnia
Sweating increased
Gynaecological
Dizziness
Nausea
Osteoporosis
Vaginal hemorrhage
Other primary cancer
Vomiting
Visual disturbance
Thromboembolism
Osteoporotic fracture
Myocardial infarction

 

Mechanism of Action

Exemestane is an irreversible, steroidal aromatase inhibitor, structurally related to the natural substrate androstenedione. Oestrogen deprivation through aromatase inhibition is an effective and selective treatment for hormone dependent breast cancer in postmenopausal women. In postmenopausal women, Aromasin p.o. significantly lowered serum oestrogen concentrations starting from a 5 mg dose, reaching maximal suppression (>90%) with a dose of 10-25 mg.

 

Exemestane does not possess any progestogenic or oestrogenic activity. A slight androgenic activity, probably due to the 17-hydro derivative presents mainly due to high doses. In multiple daily doses trials, Aromasin had no detectable effects on adrenal biosynthesis of cortisol or aldosterone, when measuring before or after ACTH challenge, thus demonstrating its selectivity with regard to the other enzymes involved in the steroidogenic pathway.

 

 

Pharmacokinetic Properties
Absorption

After oral administration of Aromasin tablets, exemestane is absorbed rapidly. The fraction of the dose absorbed from the gastrointestinal tract is high. The absolute bioavailability in humans is unknown, although it is anticipated to be limited by an extensive first pass effect. A similar effect resulted in an absolute bioavailability in rats and dogs of 5%. After a single dose of 25 mg, maximum plasma levels of 18 ng/ml  after 2 hours. Concomitant intake with food increases the bioavailability by 40%.

Distribution

The volume of distribution of exemestane is ca 20000 l. The kinetics is linear and the terminal elimination half-life is 24 h. Binding to plasma proteins is 90% and is concentration independent. Exemestane and its metabolites do not bind to red blood cells.

Exemestane does not accumulate in an unexpected way after repeated dosing.

Elimination

Exemestane is metabolized by oxidation of the methylene moiety on the 6 position by CYP3A4 isoenzyme and/or reduction of the 17-keto group by aldoketoreductase followed by conjugation. The clearance of exemestane is ca 500 l/h, not corrected for the oral bioavailability.

The metabolites are inactive or the inhibition of aromatase is less than the parent compound.

The amount excreted unchanged in urine is 1% of the dose. In urine and faeces equal amounts (40%) of C-labeled exemestane were eliminated within a week.

 

Is it approved to use Aromasin in a cycle for Bodybuilding ?

Aromasin must not be used for purposes other than breast cancer. FDA doesn’t approve it for other indications.

Aromasin contains the active ingredient exemestane, which is a steroid. Aromasin works by binding to aromatase, the enzyme in the body responsible for turning testosterone  into estrogen. This increases the level of testosterone in the body, which has similar effects to testosterone replacing therapy.

Using Aromasin for this purpose is a misuse of drugs.

 

Aromasin Vs Arimidex

Similar to Aromasin, Arimidex treats certain types of early and advanced breast cancer. But the dosages for these drugs are different.

Arimidex (anastrozole) and Aromasin (exemestane) are nonsteroidal aromatase inhibitors that treat breast cancer in postmenopausal women. Women whose cancer has progressed after taking tamoxifen can take Arimidex and Aromasin.

The recommended dosage for Aromasin is one 25-milligram (mg) tablet once per day after a meal.

However, the dosage for Arimidex is one 1-mg tablet once per day, with or without food.

 

 

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