Information about the drug
Femara (Letrozole) are tablets for oral using. The drug was made to prevent the development of the breast cancer. The principle of action is in the inhibiting of the enzyme aromatase. It is a non-steroidal inhibitor of aromatase, an enzyme with the participation of which estrogen synthesis occurs in women in the postmenopausal period. Aromatase promotes the conversion of androgens synthesized in the adrenal glands (primarily androstenedione and testosterone) into estrone and estradiol. The inhibition of aromatase activity is realized by competitive binding to the subunit of this enzyme, the cytochrome P450 hem, which leads to a decrease in estrogen biosynthesis in all tissues, including in tissues of estrogen-dependent tumors.
The suppressing of the functioning of aromatase is the most effective way to combat with estrogen in the organism. The necessity to fight with estrogens appears for athletes who use androgenic anabolic steroids. As a rule, this group of drugs contains testosterone (the male sex hormone). Testosterone is processed into other compounds in the organism, interacting with various enzymes natural testosterone is able to turn into the more powerful compound, dihydrotestosterone, and hormones which are more characteristic for the female body (estrogens).
The interaction with the enzyme aromatase leads to the emergence of an excessive amount of female sex hormones in the male body. An excess of estrogens can lead to the so-called feminization of the male body — this is manifested by the number of symptoms that make the male body look like the female: breast growth (gynecomastia); the deposition of fats on the hips and stomach (by female type); accumulation of large amounts of water in the body; changes in mood.
The blockade of estrogen biosynthesis does not lead to the accumulation of androgens, which are the precursors of estrogens. While taking letrozole, there were no changes in the concentrations of luteinizing and follicle-stimulating hormones in the blood plasma, changes in the thyroid gland function, changes in the lipid profile, and an increase in the frequency of myocardial infarction and strokes.
Anti-estrogen drugs should be used to control the amount of female hormones and to prevent these symptoms. Depending on the power of the course of androgenic anabolic steroids, there are two types of drugs made to fight estrogen. They have different strength and principle of action. The weaker type of drugs is anti-estrogens, as a rule, these drugs were made for light and non-measured steroids courses (with a moderate amount of natural testosterone), their principle of action is to interact with estrogen receptors (they occupy receptors, excluding the interaction of real estrogens with them).
Another type of inhibitors of aromatase prevents the process of aromatization, effectively controlling the level of estrogens. Such medicines are more suitable for more powerful courses of steroids and allow the applying of higher doses of testosterone without fear of the development of side effects associated with estrogenic activity.
The drug can be used as on the course of applying AAS, as during the post course therapy. After oral administration, it is completely absorbed, bioavailability approaches 100%. In the vascular bed, more than half (60%) binds to proteins (mainly to albumin) and accumulates in red blood cells. Small changes in the rate of absorption are regarded as not having clinical significance, therefore letrozole can be taken regardless of food intake.
Common dose in the period of using steroid drugs is 0.5 mg per day or in day. You should focus on such approximate dosages – this is 0.25-0.35 mg Letrozole per day for every 250 mg of testosterone per week, but not more than 1 mg per day To find out the most optimal dose it is necessary to make regular estrogen tests. The course and dosage of letrozole are selected individually, based on data from a blood test and at the same time taken drugs (in particular, steroid derivatives).
This schedule is used to apply Mar-Letrozole during the post course therapy: the first 10 days used really big dose 2.5 mg (1 tablet), but then used only 0.5 mg per day during the next 2-3 weeks.
It is necessary to notice that individual way to choose the correct dosage is very important, as minimal presence of female hormones in male’s body is a necessity. Estrogens are responsible for the many chemical processes and have major influence on the user’s mood and sexual activity.
This drug should be applied only following the recommendations and under the control of medical workers, in case of violation of the dosage regimen and doses you can notice next effects:
- Weakness, bad mood, prostration,
- Nausea and vomiting,
- Pain in the joints, itchiness, back pain,
- Increased blood pressure, severe headache, or dizziness, or loss of consciousness, or impaired vision,
- With prolonged use, this drug may cause bone fragility (osteoporosis).
Letrozole can cause a typical picture of estrogen deficiency, including osteoporosis, atrophy, decreased libido, erectile dysfunction and pain during intercourse.
Under the influence of letrozole, a decrease in the ability to concentrate is possible, therefore, during the treatment period, it is recommended to avoid driving vehicles and other potentially dangerous activities.
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This drug is a medical product and requires following recommendations of its usage and storage. It should be stored in the cool dark place, avoiding direct sunlight. It’s also necessary to keep this drug out of children`s reach!
You MUST consult with your attending physician before you start using this drug. We also ask you to take into account that this drug may cause some side effects. Some of them can be life-threatening. If you notice any disturbing symptoms you should to contact with your physician. In some cases, it is necessary to stop taking the drug for a while. Also, you must inform your doctor if you taking MAR-LETROZOLE with other medicines. So physician can prescribe proper treatment and help you to avoid any unpleasant adverse effects.