Exemestane is a fairly popular aromatase inhibitor that most closely resembles the structure of the steroid hormone androstenedione. It has no estrogenic or progestogenic activity. In fact, when taken even in large doses, only pronounced and negligible anti-estrogenic androgenic activity is possible. However, it does not affect the biosynthesis of aldosterone and cortisol in the adrenal glands.
Be aware that when taking exemestane, there may be a slight increase in serum levels of the hormones FSH and LH (seen even at low doses). This beneficial effect would apparently develop according to the feedback principle (a decrease in estrogen content leads to an increase in the secretion of gonadotropins in the pituitary gland).
And more useful information: the antiestrogenic exemestane, as the official description suggests, is rapidly absorbed from the gastrointestinal tract after ingestion. With a single dose of 25 milligrams, Cmax is 18 ng / ml (achieved within the first 2 hours). Food can increase the already good absorption: the level of the drug in the blood when taken after a meal is about 40% higher than when taken on an empty stomach.
After reaching Cmax, the level of the active substance gradually begins to decrease, while the final T½ is about 24 hours. It should be noted that after the administration is completed, exemestane is widely distributed in tissues. Plasma protein binding is approximately 90% (total concentration does not affect the degree of binding).
For what purposes is the antiestrogen exemestane used in medical practice?
Indications for use in this area are as follows:
During hormone therapy for advanced breast cancer in natural or induced postmenopausal women who have active disease despite treatment with progestogens or non-steroidal aromatase inhibitors;
During treatment of advanced breast cancer in postmenopausal or naturally postmenopausal women who experience disease progression despite antiestrogen therapy.
And for what purposes do athletes use eczema preparations? Here everything is a little simpler than in medicine. Like other blockers described, this drug is used by athletes primarily to prevent or eliminate estrogenic side effects, particularly gynecomastia associated with AAS drug use.
If we talk about its exact use, then we notice at first that it is better to take exemestane, as the official description suggests, after meals, and this applies not only to sports but also to medicine. The dosages largely depend on the method of application. If you are using the drug prophylactically, 12.5 mg every other day or 25 mg every other day is sufficient. If you resort to taking it when there are signs of aromatization, the dose should be higher – 25 mg per. day.
What side effects can exemestane cause? We answer that due to its intake, fatigue, dizziness, insomnia, nausea, skin rash, a feeling of heat and some other abnormalities.