Teva exemestane (aromasin)

Description

Information about the drug

Exemestane is a synthetic steroid drug that belongs to aromatase inhibitors. The mechanism of action of this drug is to inhibit the aromatase enzyme, which provides the conversion in the tissues from androstenedione to estrol, from which estradiol is subsequently formed, which leads to inhibition of the action of estrogens on sensitive cells of the body. The consequence of this is primarily the inhibition of the growth of estrogen-dependent malignant tumors of the breast without estrogenic, androgenic and gestagenic activity, as well as without affecting the receptors of mineralocorticoids and glucocorticoids.

Exemestane also promotes testosterone levels in men and reduces the side effects of anabolic steroids, which is why it is often used by bodybuilders to build muscle. This medicine was approved by FDA for applying during the early treatment of breast cancer.

Thanks to the property to suppress estrogenic activity this drug is widely used in sports. Its main users are athletes who apply aromatizing Androgenic Anabolic Steroids (AAS).

This product differ from similar one, it is very powerful and leave behind all competitors. The principle of its action differs too – it hasn’t influence on the estrogens, but prevents its production on the organism. This drug’s action is as effective that estrogens level on the organism decreases to 15%.

This product is on the area from 1999, produced in oral tablets in the dosage 25mg.

Pharmacology

Exemestane does not have progestogen and estrogenic activity. When used in high doses, only slight androgenic activity is manifested. It does not affect the biosynthesis of cortisol and aldosterone in the adrenal glands.

A slight increase in serum LH and FSH levels is noted even at low doses of exemestane. This effect, however, is uncharacteristic for drugs of this pharmacological group. Probably, it develops according to the feedback principle, at the level of the pituitary gland: a decrease in the concentration of estrogen stimulates the secretion of gonadotropins in the pituitary gland also in postmenopausal women.

Exemestan is rapidly absorbed after oral administration, but the availability of this drug is only 42%. The maximum concentration of the drug in the blood is reached within 1.2-2.9 hours after taking of the drug. The drug binds well (90%) to plasma proteins. There are no data on the penetration of exemestane across the placental barrier and into breast milk. The drug is metabolized in the liver to form inactive and inactive metabolites. Exemestane is excreted in the body with both urine and faeces, mainly as metabolites. The half-life of the drug is 24 hours, and this time does not change with impaired liver and kidney function.

Applying

There 2 schedules of applying for active AAS-users:

1. Use this drug together with the course of AAS;
2. Applying in post-course therapy (PCT).

Applying on the course: The dosage is 12.5mg (a half of the tablet) after the meal once in two days.

Applying on PCT: This drug is also used once in two days, but in the larger doses – 25mg during 10 days. After this time the dosage decreased in 2 times and then the drug applied 2 weeks. Make a pause after the course of Aromasin.

Full duration shouldn’t be more than 4 weeks.

Side effects

In the case of correct applying this medicine will help you to overcome estrogenic side effects effectively. Aromasin gets athletes rid of such disorders as: Gynecomastia (unnatural growth of mammary glands); Accumulation of fat deposits in female shape (on the stomach, waist and hips); Excess water accumulation in the organism.

Following the recommendations of this drug using you will not feel any side symptoms. But violating the dosage or course duration you can notice next effects:

• Allergic reactions and on the part of the skin – skin rash, itching, alopecia, fever, cough, increased sweating.
• From the digestive system – abdominal pain, vomiting, diarrhea or constipation, decreased appetite.
• From the nervous system – headache, drowsiness, depression, dizziness, insomnia, paresthesia.
• From the cardiovascular system – hypertension.

Changes in laboratory tests – lymphopenia, thrombocytopenia, leukopenia, increased levels of livers enzymes in the blood

Contact your physician immediately, if you have experience any of the following symptoms:

• Shortness of breath or difficulty breathing
• Having thoughts or feeling like you may want to harm yourself or others

Attention

• Before starting Exemestane use, make sure you tell your doctor about any other medications you are taking (including herbal remedies, vitamins, etc.).
• Exemestane can decrease bone mineral density due to decreases in estrogen levels. Your physician may monitor your bone mineral density and can prescribe vitamin D supplements, Ca²⁺ supplements, or other medications to prevent osteoporosis and possible bone fractures.
• Do not receive any vaccination and immunization without your physician’s approval while taking Exemestane.
• Use contraceptives, and do not conceive a child (get pregnant) while taking Exemestane. Barrier methods of contraception, for example condoms, are recommended.
• Drinking alcoholic beverages should be kept to a minimum or avoided completely.
• Take Exemestane after a meal; at the same time every day.

Exemestane should not be prescribed to women with premenopausal endocrine status (the effectiveness and safety of the drug in this group of patients has not been studied). During taking of Exemestane, one should refrain from classes that require concentration and speed of psychomotor reactions (when using the drug, symptoms such as drowsiness, asthenia and dizziness were noted).

Warning!

This drug is medical product and requires following recommendations of using and storing. It should be stored in the cool dark place, avoiding direct sunlight. It’s also necessary to prevent applying this drug by children.

You MUST consult with your attending physician before you start using this drug. We also ask you to take into account that this drug may cause some side effects, some of them can be life-threatening. If you notice any disturbing symptoms you should to contact with your physician. In some cases, it is necessary to stop taking the drug for a while. Also you must inform your doctor if you taking this drugs with other medicines. So physician can prescribe proper treatment and help to avoid any unpleasant adverse effects.