Letrozole 25 (Femara)

Description

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Letrozole is a non-steroidal selective third generation aromatase inhibitor. The structure and activity of this compound are very similar to that of Arimidex (anastrozole), and it is prescribed for similar medical purposes. More specifically, U.S. prescribing guidelines for letrozole recommend it be used for the treatment of postmenopausal women with estrogen receptor-positive or estrogen receptor-unknown (unsure if the cancer is responsive to estrogen) breast cancer. It is typically used as a second line of treatment after an estrogen-receptor antagonist like tamoxifen has failed to elicit a desirable response, although it is sometimes initiated as the first course of therapy depending on the circumstances. Male bodybuilders and athletes find value in letrozole for its ability to mitigate the estrogenic side effects associated with the use of aromatizable anabolic/androgenic steroids, such as gynecomastia, fat buildup, and visible water retention.

Letrozole represents one of the newer achievements in a long line of drugs targeting aromatase inhibition. It is among the most potent estrogen-lowering drugs developed to date, and has an effect significantly stronger than non-selective first generation aromatase inhibitors like Teslac and Cytadren. The dosage of each tablet of Femara is 2.5 milligrams, which according to product information was sufficient to lower estrogen levels by an average of 78% during clinical trails. The drug, however, appears to often remain quite effective in lower doses. The package insert for the product itself comments that during clinical studies doses as low as .1 and .5 milligrams produced 75 and 78% estrogen inhibition, respectively in many patients. The recommended dose, likewise, reflects a level that seems to elicit a desired level of inhibition in nearly all patients. A large number of people may, therefore, respond well to lower doses of the drug.

Administration:

The recommended dose of letrozole is one 2.5 mg tablet administered once per day, without regard to meals. When used (off-label) to mitigate the estrogenic side effects of anabolic/androgenic steroid use or increase muscle definition, male athletes and bodybuilders often take 1.25 mg to 2.5 mg per day. In some cases a dosage of a half of a tablet (1.25 mg) taken every other day is sufficient to prevent the onset of estrogenic side effects.

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