Letrozole is a nonsteroidal selective inhibitor of a third-generation aromatase. The structure and activity of the drug is similar to Arimidex (Anastrazole), and appointed for the same indications. In particular, letrozole recommended for postmenopausal syndrome treatment with estrogen receptor positive or estrogen receptor-unknown breast cancer. Usually used as second-line drug of choice after unsuccessful treatment of estrogen receptor antagonist tamoxifen, although, depending on the circumstances, and may be selected as a first line drug. Male bodybuilders and other athletes have found their own benefit in the use of letrozole, thanks to its ability to mitigate / eliminate estrogenic side effects associated with taking aromatizing anabolic-androgenic steroids, such as gynecomastia, increased body fat, water retention, etc.
Letrozole is among the latest achievements in the field of combating directed inhibition of aromatase. At the moment, the most powerful drug lowers levels of estrogen in the blood, it has a much stronger effect in comparison with such a non-selective inhibitors of aromatase like Cytadren and Teslac. The dosage of each tablet Femara is equal to 2.5 mg, and if you believe the product description, then this drug could reduce estrogen levels by 78% in clinical trials. The drug, however, appears to remain often very effective in lower dosages. Leaflet inside the packaging tells us that just as in clinical trials the dose equal to 0.1mg and 0.5mg led to a decrease in estrogen levels by 75% and 78%, respectively, in many patients. However, it is recommended dose can achieve the desired effect in all patients. But be that as it may, the huge number of people as well and respond to the use of lower dosages.
The US FDA approved prescription letrozole for sale as early as 1997, since it is sold by the pharmaceutical company Novartispod Femara trade mark. Novartisudalos expand sales in more than 70 countries in which this drug was also approved. Today Femarayavlyaetsya dominant drug around the world, particularly in countries such as: Argentina, Australia, Belgium, Brazil, Canada, Chile, Czech Republic, France, Germany, Greece, Hong Kong, India, Netherlands, New Zealand, Italy, South Africa, Switzerland and Russia. Novartistak letrozole also sells under the brand name Femarv Finland, Denmark, Norway and Sweden. In addition, letrozole can be found under other brands, such as: Fempro (India), Oncolet (India), Trozet (India), Insegar (Spain), Aromek (Poland), LAMETTA (Poland), Cendalon (Argentina) Fecinole (Argentina), and Kebirzol (Argentina). But given the high level of efficiency and a strong marketing support, Femarai Femarostayutsya most popular products on the basis of letrozole worldwide.
Letrozole usually comes in tablets with a dose equal to 2.5 mg.
Letrozole is classified as a non-steroidal selective inhibitor of a third-generation aromatase. Its chemical name – 4,4 ‘- (1H-1,2,4-triazole-1-yl-methylene) dibenzonitril.
The most common side effects of aromatase inhibitor reception are: joint pain, weakness, fatigue, mood changes, depression, high blood pressure, swelling of hands / feet, and headache. An aromatase inhibitor can also reduce the degree of mineralization of bone density that can lead to osteoporosis and increased chance of fractures in susceptible patients. Some people may respond to medication gastrointestinal disorders including nausea and vomiting. Aromatase inhibitors may harm the unborn fetus, so do not start receiving during pregnancy. When used by men to reduce the effects of estrogen on the long-term course of steroid aromatase inhibitor may increase the risk of cardiovascular disease by reducing some of the beneficial effects of estrogen on the amount of cholesterol. Studies have shown that when used in conjunction with an aromatase inhibitor, testosterone enanthate, HDL suppression (good) cholesterol is considerable. Therefore, as tamoxifen does not have such a negative effect on cholesterol levels, that it should give preference to men prone to cardiovascular disease.
Letrozole is approved by the FDA for:
- Adjuvant therapy of postmenopausal women with a positive diagnosis on breast cancer early stages;
- Adjuvant therapy of postmenopausal women with a positive diagnosis of breast cancer early stages taking tamoxifen for 5 years;
- Treatment of locally rasprostnёnnogo or metastatic breast cancer as first-line therapy;
- Treatment of advanced breast cancer therapy with an anti-estrogen.
The recommended daily dose is the one receiving 2.5 mg tablet, regardless of the meal. When used to mitigate the estrogenic side effects of steroids on the course, or to increase muscle definition, male athletes and bodibldery usually have to take 1.25 mg or 2.5 mg daily. In many cases, it will be enough and receiving 1.25 mg every other day, to prevent the majority of the side effects associated with high levels of estrogen.