Showing posts with label gynecomastia. Show all posts
Showing posts with label gynecomastia. Show all posts

Friday, August 30, 2013

Nolvadex tamoxifen citrate anti-estrogen profiles

Nolvadex tamoxifen citrate



Tamoxifen citrate is a non steroidal anti estrogenic drug, used widely in clinical medicine. It is specifically a selective estrogen receptor modulator of the triphenylethylene family, and posses both estrogen agonist and antagonist properties. As such, it may act as an estrogen in some tissues while acting as an anti-estrogen in others. In breast tissue the drug is a strong anti estrogen and as a result is commonly used in the treatment of estrogen related breast cancer in women. Tamoxifen citrate was first developed in 1962 by the pharmaceutical company ICI. It was made commercially available in the United States not long after, but its initial use was for the treatment of female infertility, a purpose for which the drug does not seem ideally suited for. It was not until 1977 that the FDA approved the drug for use in the United States for the treatment of breast cancer. The drug has been sold by ICI in a number of worldwide markets under the brand name of Nolvadex. The drug is most commonly supplied in tablets containing either 10mg of 20mg of the drug.

In terms of its use in steroid users, tamoxifen citrate can help in two ways. Firstly due to the binding affinity of the compound it is able to help in the prevention of gynecomastia. Tamoxifen will compete with estrogen for the estrogen receptors in certain tissues, including the breast, and if it can bind to the receptor estrogen will not have an opportunity to interact with receptor and therefore gynecomastia should not be able to develop. When using anabolic steroids that can convert to estradiol (estrogen) this protection against gynecomastia can be invaluable. However it should be noted that tamoxifen citrate will not eliminate the estrogen or disallow the conversion to occur. Instead it attempts to counteract the effects of circulating estrogen in the body in those tissues that the drug effects. Therefore there is no evidence that tamoxifen citrate has any effects counteracting estrogenic side effects that are unrelated to the tissues that are not in the breast, liver or bone. Namely there is no real causal connection to any reduction in water retention and acne in users that begin taking tamoxifen citrate as it relates to estrogen. The second, and possibly more beneficial, aspect of tamoxifen citrate for steroid users is its ability to increase the production of luteinizing hormone and follicle stimulating hormone, and therefore increasing testosterone. This ability is why it is often used by steroid users during their post-cycle therapy. There are numerous studies that indicate that tamoxifen citrate can increase the levels of these hormones quite dramatically. Tamoxifen citrate does this by blocking the negative feedback inhibition caused by estrogen at the hypothalamus and pituitary, and this in turn will help to increase the production of these hormones. Unlike clomiphene citrate, tamoxifen citrate has also been shown to increase luteinizing hormone responsiveness to gonadotropin releasing hormone. Clomiphene citrate can lower this responsiveness over time. One of the possible side effects associated with use of tamoxifen citrate is the possible reduction of insulin-like growth factor levels. If these levels are reduced this could suppress the gains an individual can make slightly. However this reduction, if it actually exists, would not be overly significant with gains in muscle mass only being marginally reduced for the most part.

When it comes to dosing for combating gynecomastia that has begun to form, there is very little research. The limited research that does exist does point to the fact that doses of 20-40mgs per day are effective in treating the existing condition. However, anecdotally users have reported sometimes using doses of 60-80mgs per day. For use during post-cycle therapy users have anecdotally indicated that doses ranging between 20 and 40mgs per day are average. These doses have been shown to significantly raise levels of testosterone, luteinizing hormone and follicle stimulating hormone.

More...




Wednesday, August 28, 2013

Femara letrozole anti-estrogen profiles

Femara  letrozole



Letrozole is a non steroidal selective third generation aromatase inhibitor. The structure and activity of this compound are very similar to that of Arimidex, and is prescribed for similar medical reasons. More specifically, United States prescribing guidelines for leptosome recommend it to be used for the treatment of postmenopausal women with estrogen receptor positive or estrogen receptor unknown breast cancer. It is typically used as a second line of treatment after an estrogen receptor antagonist like tamoxifen has failed to elicit a describable response, although it is sometimes initiated as the first course of therapy depending on the circumstances. Male bodybuilders and athletes find value in leptosome for its ability to mitigate the estrogenic side effects associated with the use of aromatically anabolic/androgenic steroids, such as gynecomastia, fat buildup, and visible water retention. The U.S FDA approved leptosome for prescription sale in 1997, where it is sold by the pharmaceutical company Novartis under the brand name of Femara. The company also markets the drug in over 70 nations worldwide. The drug is most commonly supplied in dosages of 2.5mg.

In terms of how this drug can be used to the benefit of bodybuilders and strength athletes, letrozole is primarily used to ward any estrogenic side effects caused by the administration of anabolic steroids. Letrozole has been show to have the capability of reducing the level of estrogen in users' bodies by up to 96-98%. This would seemingly be enough in itself to make the compound a desirable one with which steroid users would be interested in. However letrozole also has been shown to increase the amount of luteinizing hormone, follicle stimulating hormone, and sex hormone binding globulin in users. When you combine these attributes with the fact that it will help protect against gynecomastia, water retention and other estrogenic side effects letrozole obviously can fulfill many users' needs. There are some animal studies that have suggested that letrozole can help to reduce or even eliminate pre-existing gynecomastia as well. Of course there are some limits to this research as it has never been conducted using human subjects but it does demonstrate that there may be a mechanism by which this could occur. Anecdotally some users have reported that they have experienced a reduction in their own pre-existing gynecomastia, but of course these reports have their limits as they were not conducted with the scientific controls in place. Interestingly, it takes approximately 60 days to get a steady blood plasma level of letrozole once administration of the drug begins. This may necessitate that a user begin using the compound prior to beginning their cycle if they wish for the effects to be at full strength once their cycle begins. This may also hinder the ability of the compound to respond quickly if a user begins administration of the drug to counteract some side effects that have appeared quickly.

The maximum dosage that a user would want to use would be 2.5mgs per day. It has been shown in numerous studies that this dosage will eliminate nearly all of the estrogen in the body in nearly all individuals. Any dose that is higher than this would simply be unneeded. Despite the ability to increase the amount of luteinizing hormone, follicle stimulating hormone, and sex hormone binding globulin in users letrozole can be counterproductive if used during post-cycle therapy. This is due to the ability of the compound to drive estrogen levels too low during use. Once the compound is discontinued this can result in a "rebound effect" in estrogen levels with these becoming quite high, something that should be avoided during or after post-cycle therapy. Anastrozole could be seen as an alternative to letrozole in this capacity as it seemingly does not have such a potent effect. The detrimental effect that letrozole has on blood lipid levels is another reason why many will avoid it's use during post-cycle therapy

More...