Letrozole (Letrozole/Femara)

Femara is the brand name of Novartis Pharmaceuticals of letrozole, a compound classified as a non-steroidal selective third generation aromatase inhibitor. It is indicated for postmenopausal women with estrogen receptor-positive or estrogen-receptor unknown breast cancer.

The third-generation drugs have dislodged the non-selective aromatase inhibitors, such as Teslac and Cytadren, for the simple fact that former are more potent and more effective than the latter.

Femara is of the same class of drugs as Arimidex. And liike Arimidex, Femara is used as second-line treatment for the aforementioned disease if it does not respond to tamoxifen therapy. There are cases, however, when both Femara and Arimidex are used as initial pharmaceutical options.

The ability of Femara to effectively lower estrogen levels is what attracts bodybuilders to this relatively new drug. Femara offers benefits to individuals who are prone to estrogenic side effects when they are using anabolic-androgenic steroids. These side effects include bloating, water retention and gynecomastia.

Because of their potency aromatase inhibitors provide drawbacks to bodybuilders. Anti-estrogens, such as Nolvadex and Clomid, only inhibit the activity of the hormone estrogen while Femara effectively blocks its production. And this can have harmful effects on the body because estrogen is not entirely an injurious hormone.

Estrogen actually refers to a group of chemically similar hormones, which include estrone, estriol, and estradiol (the most abundant). Although it is commonly referred to as the primary female sex hormone, estrogen is also present in males. However, its function in males is not yet clearly determined.

Estrogen plays significant role in many chemical and structural processes in the body as enumerated below. Remember that estrogen’s function is not limited to the following processes; however, these are relatively more important in bodybuilding.

• Structural changes (promotion of the growth and development of female secondary sexual characteristics)
• Protein synthesis (increases hepatic production of binding proteins)
• Metabolism (accelerates body’s metabolism, burns fat)
• Lipid profile (increases HDL, triglyceride; decreases LDL, fat deposition)
• Fluid balance (salt/sodium, water retention)
• Hormonal (increases growth hormone; increases cortisol, SHBG)

Total restriction of estrogenic activity can result to negative reactions, particularly in the aspect of lipid metabolism. Aromatase inhibitors are known to elevate HDL (bad cholesterol) and decrease LDL (good cholesterol).

The recommended dosage of Femara is one tablet a day (2.5 milligrams), which can lower estrogen levels by 78%, as shown in clinical trials. However, anecdotal feedback reports that it can still be effective even taken at a much lower dose – a 0.5 milligram a day can elicit ideal estrogen inhibition.

Side effects of Femara include dizziness, fatigue, hot flashes, and muscle and joint pains. Long term use of this drug can cause osteoporosis resulting to bone fractures.