Description

Active-Life: Less than 24 hours

Drug Class: Anti-estrogen/estrogen antagonist (Oral)

Average Reported Dosage: 0.5-2.5 mg daily

Acne: None

Water Retention: No

High Blood Pressure: Rare (not normally attributed to the drug itself)

Liver Toxic: Yes

Letrozole is a non-steroidal selective third generation aromatase inhibitor, which is being sold under the brand name Femara by the international drug-manufacturing firm Novartis. It is used to treat postmenopausal women with estrogen receptor-positive or estrogen receptor-unknown (unsure if the cancer is responsive to estrogen) breast cancer.The structure and activity of this compound are very similar to that of Arimidex (anastrozole), which is approved in the United States for the same purpose. Femara is typically used as a second line of treatment, after an estrogen-receptor antagonist like tamoxifen has failed to elicit a desirable response (although at times it is used as a first line option as well).

Femara and Arimidex represent the newest achievements in a long line of drugs targeting aromatase inhibition. These are amongst the most potent estrogen-lowering drugs made to date, working far more effectively than the non-selective first generation aromatase inhibitors, like Teslac and Cytadren, to come before them. The dosage of each tablet of Femara is 2.5 milligrams, which according to the product insert was sufficient to lower estrogen levels by 78% during clinical trails.The drug, however, appears to still be extremely effective in much lower doses. The package insert for the product itself comments that during clinical studies doses of .1 and .5 milligram produced 75% and 78% estrogen inhibition, respectively. When it comes to a product like this, typically the recommended dose reflects what seems to work for almost everyone who takes it. A large number of people may respond extremely well to lower doses, however, to make sure each patient is receiving the proper benefit of the drug a standard effective dosage unit is ascertained and used.

It is important to point out that there are some disadvantages to using an aromatase inhibitor over mixed estrogen agonist/antagonists (anti-estrogen) like Nolvadex and Clomid, the most notable being unwanted (negative) alterations in cholesterol values (strong HDL suppression in particular). This is because estrogen is tied to HDL cholesterol synthesis and LDL metabolism, and aromatase inhibitors block total estrogenic action. Clomid and Nolvadex, on the other hand, tend to produce an estrogenic increase in good cholesterol values, as they are active estrogens in the liver. If I you are just trying to prevent estrogenic side effects like gynecomastia, bloating and excess water retention in general, these agents are probably better choices (they do the same job and are safer on your cholesterol levels). But if you want that really

tight, dry, defined look that is often so sought after when you are cutting, Nolvadex or Clomid are not quite going to cut it (excuse the unintentional pun). In such cases, I think you will find Femara to serve you well.

At the pharmacy, 30 tablets will cost you a little under $200. This comes out to about $6.50 each tablet, roughly the same price you are going to pay for Arimidex. Like Arimidex, each tablet can be broken up if you desire to stretch out the value of the drug. In fact, with studies showing maximum inhibition in some patients with doses as low as 1/2 milligram, each 2.5 milligram tablet can be broken up in to as many as 5 separate doses (perhaps even more). But the typical use amongst bodybuilders is to cut the tabs in half, and take one every other day (unless needed daily). In terms of overall power, Femara seems to be a little bit more potent the Arimidex, at least by most peoples’estimations. If both agents were available for the same price, Femara would probably be the one I would go for.

(Letrozole) is an oral non-steroidal aromatase inhibitor that has been introduced for the adjuvant treatment of hormonally-responsive breast cancer.

Estrogens are produced by the conversion of androgens through the activity of the aromatase enzyme. Letrozole blocks production of estrogens in this way by competitive, reversible binding to the heme of its cytochrome P450 unit. The action is specific, and Letroplex does not reduce production of mineralo- or corticosteroids. In contrast, the antiestrogenic action of tamoxiplex, the major medical therapy prior to the arrival of aromatase inhibitors, is due to its interfering with the estrogen receptor, rather than inhibiting estrogen production.