Wednesday, September 4, 2013

Cytadren anti-estrogen profiles

Cytadren


Aminoglutethimide is mainly identified as an inhibitor of adrenocortical steroid synthesis. Its primary function is to block the conversion of cholesterol to pregnenolone, which is required for the biosynthesis of adrenal glucocorticoids, mineral corticoids, estrogens, and androgens. Aminoglutethimide is a nonspecific inhibitor, and also blocks several other steps in steroid synthesis including hydroxylation at C-11, C-18, and C-21, and the aromatization of androgen to estrogens, The drug may be used clinically to treat estrogen dependent breast cancer, and to treat Cushing’s syndrome, which is a condition where the body overproduces the hormone cortical. The effect that Aminoglutethimide can have on cortical and estrogen production is what makes this a drug of interest to athletes and bodybuilders. The drug also works by inhibiting cortical production. While cortical is an essential hormone for life, its levels may also vary greatly within “normal” ranges depending on the individual, their training and dietary status. Aminoglutethimide was FDA approved as an anticonvulsant drug in 1960 under the main trade name of Cytadren. Side effects were common with treatment, however, including drowsiness, dizziness, and partial loss of motor control. In 1966 reports of adrenal insufficiency subsequent to Aminoglutethimide use were reported. The drug was withdrawn from the U.S market as an anticonvulsant that same year due to its recently understood effects on the adrenal gland. The drug is most commonly supplied in tablets of 250mg.

In terms of research conducted in athletes or those looking to use the drug for athletic or cosmetic purposes, there is of course very little as is the case with many drugs used by bodybuilders and strength athletes. For this reason we are left to extrapolate the best methods to use aminoglutethimide from anecdotal information as well as trying to form the available research to fit into our needs. A significant aspect of aminoglutethimide is that along with its ability to inhibit both cortisol and aromatization, it also suppresses the production of adrenal androgens. Obviously this would be a negative for someone that was not using exogenous hormones, but since it is unlikely that athletes or other steroid users would be administering aminoglutethimide without also using anabolic steroids this is likely not to be a concern for most. The cortisol inhibiting effect of aminoglutethimide is short lived in the body due to the body’s ability to adapt to the action of the drug. By lowering the natural production of cortisol the body will begin to produce adrenocorticotropic hormone. The hormone sparks an increase in cortisol production in the body to help normalize its levels causing the action of the drug to become basically moot. It is believed by some that if one staggers their use of the drug to a schedule similar to two days on and then two days off that this may be enough to ward off the body’s response to the lowered cortisol levels while still reaping the benefit of partial suppression. There is little research to indicate that this is true however. It appears that there is a significant risk of hepatoxicity with aminoglutethimide when used over extended periods of time even at relatively moderate dosages. For this reason lengthy use of the drug would not be recommended for most users and even short cycles of it are likely to increase liver values.

Athletes and bodybuilders looking to take Cytadren for the suppression of cortisol usually take the drug in a dosage of 1000mg per day for a period of 2-3 weeks or less. A schedule of 2 days on and 2 days off may be used in an effort to extend the effectiveness of the drug for extended periods of time.

More...




Monday, September 2, 2013

Teslac testolactone anti-estrogen profiles

Teslac  testolactone



Testolactone is a first generation non selective steroidal aromatase inhibitor, used clinically to treat estrogen dependent breast cancer. Its exact mode of function is unknown, but it is believed to inhibit the aromatase enzyme in a noncompetitive and irreversible manner. If so, this would be an activity that is very similar to that of Lentaron. This might also explain why cessation of the drug does not provide an immediate restoration of normal estrogen production.
Like formestane, it takes several days after ceasing use for the body to replenish its enzyme levels. Testolactone was first approved by the FDA as a prescription drug back in 1970. It was an early anti estrogenic drug, exhibiting a moderately pronounced effect but failing to reach levels of high clinical success. As other more successful medications began to surface for the treatment of breast cancer, testolactone would not see the success that had been planned for it. Currently, the United States is the only country where the product has not been discontinued. Testolactone is most commonly supplied in tablets of 50mg.

Even though the drug no longer being utilized for its originally intended purpose, testolactone still offers several unique advantages for steroid users. First, research has shown that the compound can effectively treat and prevent gynecomastia. This is seemingly accomplished by way of aromatase inhibition as opposed to the estrogen agonist/antagonist mechanism that tamoxifen citrate accomplished this effect with. The second benefit that strength athletes, bodybuilders and other who make use of performance-enhancing drugs could experience by taking testolactone is the ability of the compound to help increase the natural testosterone production of users.

This increase is prompted by several physiological mechanisms. In several studies it has been demonstrated that not only is the level of testosterone increased in users significantly, but that this is likely caused by the ability of the compound to also increase the levels of androstenedione, luteinizing hormone and follicle stimulating hormone in the body. Obviously all of this would suggest that testolactone offers several advantages to those with suppressed natural testosterone production, with male steroid users coming off of anabolic steroids clearly being this group. Returning to the aromatase inhibition action of testolactone, the effects of this drug are similar to those of other aromatase inhibitors.

 That is to say that testolactone can help to minimize aromatization and lowers the levels of circulating estradiol. However the level to which testolactone can accomplish this is somewhat clouded due to contradictory research. For example, one study indicated that administering one gram of testolactone to a group of healthy men for nine days resulted in only a twenty five percent decline in the level of circulating estradiol. However another study found that users taking one gram of the compound over only six days cut their estradiol levels in half. So while it can be concluded that testolactone will lower the level of circulating estradiol, there is no definitive answer as to exactly how effective it truly is. As for controlling aromatization, testolactone has been shown to reduce it by up to ninety five percent in some cases.

While testolactone has been shown to be an effective compound for the treatment and prevention of gynecomastia, the main benefit it can offer users is during post-cycle therapy when they are trying to regain natural testosterone production by the body. The ability to help increase the natural production of testosterone, as well as the precursors to testosterone, would undoubtedly serve a user well when he is attempting to re-start and raise his hormonal production to their regular levels.

More...