Exemestane

Exemestane in bodybuilding and beyond

Exemestane is a popular aromatase inhibitor with a structure most similar to the steroid hormone androstenedione. It has no estrogenic or progestagenic activity. In fact, when taking it, even in high doses, only pronounced anti-estrogenic and minor androgenic activity is possible. However, it has no effect on aldosterone and cortisol biosynthesis in the adrenal glands.

Note that when exemestane is taken, there may be a slight increase in serum FSH and LH hormone levels (observed even with low doses). This beneficial effect seems to develop according to a feedback principle (a reduction of estrogen leads to an increase of gonadotropin secretion in the pituitary gland).

Exemestane tablets

And a little more useful information: the anti-estrogen exemestane, as the official description suggests, is absorbed fairly quickly from the gastrointestinal tract after ingestion. When a single 25-milligram dose is taken, the Cmax is 18 ng/ml (reached in the first 2 hours). Food can improve already good absorption: blood levels are approximately 40% higher when taken after a meal than when consumed on an empty stomach.

After reaching Cmax, the level of active substance starts to decrease gradually, with a final T½ of about 24 hours. Note that once administration has taken place, exemestane is widely distributed in the tissues. Binding to plasma proteins is approximately 90 per cent (total concentration is not affected by the degree of binding).

For which purposes the anti-estrogen exemestane is used in medical practice

Its indications for use in this field are as follows:

• During hormonal therapy for advanced breast cancer in women in natural or induced postmenopause who have advanced disease despite treatment with progestins or non-steroidal aromatase inhibitors;
• During treatment of advanced breast cancer in women in induced or natural postmenopause who have advanced disease despite treatment with anti-estrogenic agents.
  

And for what purposes are exemestane-based products used by athletes? It's a little simpler than in medicine. Just like the other blockers described, this drug is primarily used by athletes to prevent or eliminate estrogen side effects, in particular gynaecomastia, associated with taking AAS drugs.

Speaking about how exactly it is used, let us first note that taking exemestane, as the official description suggests, is best done after meals, and this applies not only to sports, but also to medicine. The doses depend a great deal on the mode of administration. If you are taking it as a prophylactic agent, 12.5 mg every other day or 25 mg every other day will suffice. If you take it at signs of flavouring, the dosage should be higher, 25 mg per day.

Side effects of Exemestane

You may experience fatigue, dizziness, insomnia, nausea, skin rashes, fever and some other abnormalities.