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Anti-Estrogen Profiles
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Anti-Estrogen Profiles - 11-02-2011, 11:43 AM

Arimidex (Anastrozole)



Anastrozole

Tetramethyl-5-(1H-1,2,4-triazol-1ylmethyl) 1,3-benzenediacetionitrile
Molecular Formula C17H19N5
Molecular Weight 293.37
CAS Registry Number 120511-73-1
Melting point
81-82 ēC

Although Arimidex does increase testosterone levels slightly in the body, it is more often used in conjunction with other steroids to lower estrogen in the body. Many anabolic steroids will convert, or aromatize, in the body into estrogen, which causes many of the unwanted side effects like bloating and acne. Arimidex is one of the best compounds to lower the aromatizing effect of steroids.

There are some concerns with using an aromatase inhibitor such as this during prolonged steroid treatment however. While it will effectively reduce estrogenic side effects, it will also block the beneficial properties of estrogen from becoming apparent (namely its effect on cholesterol values). Studies have clearly shown that when an aromatase inhibitor is used in conjunction with a steroid such as testosterone, suppression of HDL (good) cholesterol becomes much more pronounced. Apparently estrogen plays a role in minimizing the negative impact of steroid use. Since the estrogen receptor antagonist Nolvadex is shown not to display an anti-estrogenic effect on cholesterol values, it is certainly the preferred from of estrogen maintenance for those concerned with cardiovascular health.

Arimidex has another principle drawback, namely the great price of this drug. Tablets can easily sell for $10 each, becoming quite costly with regular use. Clearly the price of an ancillary drug can be much greater than the steroids themselves, a situation destined not to be popular with recreational bodybuilders. Competitors on the other hand are likely to welcome this item. It can ward off the side effects of strong androgen therapy much better than Nolvadex and/or Proviron, making heavy cycles much more comfortable. As the number of countries manufacturing this drug increases, we may be able to look forward to a reduction in price. Privately compounded versions of “liquid Arimidex” have also been formulated “for research purposes” are also available. Generic tabs are also available and these two forms represent a very cost-effective alternative for buying the brand name drug.


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Last edited by K1; 05-28-2012 at 03:35 PM.
   
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Aromasin (Exemestane)
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Aromasin (Exemestane) - 11-02-2011, 11:44 AM



Exemestane

6-Methylenandrosta-1,4-diene-3,17-dione; 10,13-Dimethyl-6-methylidene-7,8,9,10,11,12,13,14,15,16-decahydrocyclopenta[a]phenanthrene-
Molecular Formula C20H24O2
Molecular Weight 296.40
CAS Registry Number 107868-30-4
Melting point 155.13 ēC

Exemestane is a steroidal suicide aromatase inhibitor. It isvery similar in structure and action to formestane, although it is significantly more potent in comparison. As a class of drugs, aromatase inhibitors offer an anti estrogenic effect by blocking the enzyme responsible for synthesizing estrogens. Exemestane is approved by the FDA for the treatment of breast cancer in women, specifically in post menopausal patients whose cancer has progressed following therapy with tamoxifen (nolvadex). Male bodybuilders and athletes often use the drug for non approved purposes, namely to counter the estrogenic side effects associated with the use of aromatizable anabolic/androgenic steroids. This may include gynecomastia, fat buildup, and water retention. Exemestane is one of the most potent aromatase inhibitors presently available. The most commonly cited date reports a lowering of estrogen around 85% on average in clinical studies with women. Exemestane was developed by Pharmacia & Upjohn, which gained FDA approval for sale of the drug in late 1999. They introduced it under the Aromasin brand name in early 2000. Although the drug proved to be effective in doses as low as 2.5mg per day in some patients, the company developed it in a standard and near universally effective dosage of 25mg per tablet. The company has since introduced the drug to many other nations under the same trade name of Aromasin.

Aromasin, as it is most commonly called, is a very potent AI which works by blocking the aromatase enzyme in the body. This drug was originally developed to help fight breast cancer in women by reducing estrogen which some believe to aid in cancer cell growth. While not quite as strong as Letrozole, aromasin is considerably stronger than Anastrozole. Studies done with this substance typically show around an 85% reduction in estrogen levels in the body. This can be very useful to bodybuilders who are using aromatizing compounds such as testosterone. Typically, one will begin the use of aromasin the same day they begin their cycle. It is also important to note that Aromasin has shown to be very effective at increasing testosterone and IGF levels in the body. Because of this, this drug is also very useful during PCT regime when one is trying to restore natural testosterone levels in order to avoid a post cycle "crash". It is important to keep doses of aromasin reasonable, as too much estrogen suppression can result in hindered muscle gains and loss of sex drive. One 25mg tablet a day should be sufficient for effectively keeping estrogen related sides out of the picture, or for effectively raising natural testosterone levels during PCT.

Exemestane reaches peak plasma concentrations within 2 hours following the oral administration of a 25 mg dose. The active life of the drug is between 24 and 30 hours. This is significant since it is quite shorter than for the non-steroidal inhibitors. A single oral dose of 25 milligrams of exemestane causes a relatively long-lasting reduction in plasma and urinary estrogen levels, with maximal suppression occurring approximately 2 to 3 days after dosing and persists for about 4 to 5 days.It has been shown that 25 milligrams of exemestane is basically just as effective as 50 milligrams at suppressing estrogen, raising testosterone levels, and levels of IGF. It is therefore unnecessary to go higher in doses than 25 milligrams per day. Due to the active life of the compound exemestane should be administered roughly once every twenty-four hours. Users often start the drug on the first or second week of steroid use and continue to take it throughout the cycle and for a few weeks afterwards in order to prevent any type of estrogen rebound.


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Last edited by K1; 05-28-2012 at 03:37 PM.
   
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Clomid (clomiphene citrate)
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Clomid (clomiphene citrate) - 11-02-2011, 11:44 AM



Clomiphene citrate is an anti estrogenic drug that is prescribed to women to treat anovulatory infertility (inability to ovulate). In clinical medicine it is specifically referred to as a nonsteroidal ovulatory stimulant. The drug works by interacting with estrogen receptors, often in an antagonistic manner, in various tissues of the body including the hypothalamus, pituitary, ovary, en***etrial, vagina, and cervix. One main focus is that the drug will oppose the negative feedback of estrogens on the hypothalamic pituitary ovarian axis, enhancing the release of gonadotropins (LH and FSH). This surge in gonadotropins may cause egg release, ideally leading to conception. Clomiphense is very similar in structure to the popular drug nolvadex. Clomiphene citrate is a fertility drug with a substantial history of use in the United States. It first gaiined widespread acceptance during the early 1970s, and has been a drug common to the fertility practice ever since. The drug is now considered a standard medication for certain forms of fertility therapy, and has been adopted as such far outside the United States border. The drug is now presently available in most nations worldwide. The most two popular brand names for clomiphene citrate are Clomid and Serofen, although the drug can be found under numerous other trade names as well.

Clomid, as it is most often called, is one of the most popular PCT drugs today, and is a staple of most bodybuilder's protocol. Clomid is typically prescribed for women to aid in ovulation. In men, the application of Clomid causes an elevation of follicle stimulating hormone and luteinizing hormone. As a result, natural testosterone production is also increased. This effect is obviously beneficial to the athlete, especially at the conclusion of a cycle when endogenous testosterone levels are subnormal. Clomid will gradually raise testosterone levels over its period of intake. Clomid is typically prescribed for women to aid in ovulation. In men, the application of Clomid causes an elevation of follicle stimulating hormone and luteinizing hormone. As a result, natural testosterone production is also increased. This effect is obviously beneficial to the athlete, especially at the conclusion of a cycle when endogenous testosterone levels are subnormal. Clomid will gradually raise testosterone levels over its period of intake. Clomid is also effective as an anti-estrogen. With the intake of Clomid, the athlete gets the dual effect of blocking out some of the effects of estrogen, while also increasing endogenous testosterone production.

For the most part users will maintain doses of the drug between 25mgs to 150mgs per day on a consistent basis. Often times users will "frontload" the compound using doses of between 200-300mgs on the first day of their post-cycle therapy and then reduce the subsequent doses. However the side effects associated with large doses of the compound may hinder some individuals' abilities to do this. Some users also advocate tapering the dose of clomiphine citrate during the last few weeks of administration. However this is more a practice that is based upon theory rather than solid medical evidence of it's productivity. In terms of dosing length it seems that at least 3 weeks of clomiphine citrate therapy is recommended by users. Of course each has their own preferences along with individual recovery schedules. Also the types of compounds used and the duration of a cycle will of course influence the time it takes for a user to recover and the need for a lengthy post-cycle therapy.


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Last edited by K1; 05-28-2012 at 05:19 PM.
   
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Cytadren (aminoglutethimide)
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Cytadren (aminoglutethimide) - 11-02-2011, 11:45 AM



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.


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Last edited by K1; 05-28-2012 at 05:20 PM.
   
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Evista (raloxifene)
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Evista (raloxifene) - 11-02-2011, 11:45 AM



Raloxifene hydrochloride is a second generation selective estrogen receptor modulator (SERM) of the benzothiophene family. This drug is similar in its effects to the drug tamoxifen (nolvadex), exhibiting estrogen receptor antagonist properties in some tissues while acting as an estrogen receptor agonist in others. The main point of variation between the two drugs is their tissue selectivity. While raloxifene hydrochloride is a strong anti-estrogen in breat and uterine tissues, it appears to be estrogenic in bone. This allows it to protect bone density, mimicking the effects of endogenous estradiol. This is quite different than nolvadex, which is anti estrogenic in both breast and bone. In a role that novel for an anti-estrogen, raloxifene was approved by the FDA for the prevention and treatment of osteoporosis in post menopausal women. It is also being investigated for several other potential uses, including the treatment and prevention of cardiovascular disease. Raloxifene was developed by Eli Lilly & Company, and the FDA approved for U.S sale in 1997. Its first indictated use was as that of an osteoporosis treatment, owing to its ability to increase bone density. In 2007, the FDA expanded the indicated uses for the drug to include reducing the risk of invasive breast cancer in two populations. Today, the drug is a fairly popular drug in clinical medicine, and is approved for sale in over 50 countries. The most common brand name is Evista and ***inates the global market.

There is some evidence that raloxifene hydrochloride may actually be more effective for the treatment of gynecomastia than is the drug nolvadex. In one study it was shown that while both tamoxifen citrate and raloxifene hydrochloride had relatively similar rates of success in reducing the size of gynecomastia in pubertal males, raloxifene hydrochloride had a higher rate of effectively reducing the size to noticeably significant smaller levels. Obviously when one is faced with the option of choosing which compound to use when a treatment for gynecomastia is needed this should indicate that raloxifene hydrochloride may indeed be the more effective choice. A second benefit of raloxifene hydrochloride is that it seemingly has the ability to lower low-density lipoprotein and total cholesterol levels in users. The drug is able to accomplish this by way of its agonist actions on lipid metabolism. However it appears that these effects may be marginal at best and may not be all that significant in terms of the health of the user. However in a minority of studies there is some evidence that improvements in cholesterol levels can be quite significant and should improve the health of the user. It appears that more research needs to be conducted in this area before any proclamations can be made about the effect of this drug on the cardiovascular health of users. Combine this with the fact that anabolic steroid use will have a significant impact on cholesterol levels and any attempt at reaching a conclusion about this issue for bodybuilders and strength athletes is even further away. For now the use of this drug for cholesterol lowering effects is questionable. A far less contentious issue is the ability of raloxifene hydrochloride to raise the levels of follicle stimulating hormone, luteinizing hormone and testosterone levels in male users. Like tamoxifen citrate, clomiphine citrate and toremifene citrate raloxifene hydrochloride has been demonstrated to help raise the levels of these hormones when they are suppressed. The research regarding the ability of raloxifene hydrochloride to raise testosterone levels in males is limited when compared to both clomiphine citrate and tamoxifen citrate so it is difficult to compare their effects in this regard.

When used by athletes and bodybuilders to mitigate the side effects of anabolic/androgenic steroids, the most common dosage is 30-60mg per day during the course of the steroid cycle.


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Last edited by K1; 05-28-2012 at 05:31 PM.
   
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Fareston (toremifene citrate)
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Fareston (toremifene citrate) - 11-02-2011, 11:46 AM



Toremifene citrate is an anti-estrogenic drug, specifically classified as a selective estrogen receptor modulator (SERM) with mixed agonist and antagonist properties. It is a non steroidal triphenylethylene derivative, similar in structure to both the drugs nolvadex and clomid. Toremifen citrate is used for the treatment of breast cancer in postmenopausal women with the estrogen receptor positive or estrogenic receptor unknown tumors. It works by attaching to the estrogen receptor in various tissues in a competitive manner, blocking endogenous estrogen from exerting biological activity. Toremifene citrate was first approved by the FDA as a prescription drug in 1997. It is sold in the U.S under the Fareston brand name, which is made by the pharmaceutical company Gtx Inc. Fareston is also available in over 25 other countries worldwide. Fareston is most commonly supplied in tablets of 88.4mg, which are labeled and equate to 60mg of toremifene base.

The difficulty in using toremifene citrate is the lack of research conducted using human subjects, and specifically male subjects. While it is possible to apply most of what is known about the other selective estrogen receptor modulators to toremifene citrate, independent research conducted with the drug itself is invaluable and therefore a risk is taken when using the drug because of the lack of information. Unfortunately toremifene citrate is possibly the least researched selective estrogen receptor modulator, with the possible exception of raloxifene.
Despite the lack of human-based research available, in terms of its use in steroid users, toremifene citrate can help in two ways. Firstly due to the binding affinity of the compound it is able to help in the prevention of gynocomastia. Toremifene citrate 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 gynocomastia should not be able to develop. When using anabolic steroids that can convert to estradiol (estrogen) this protection against gynocomastia can be invaluable. However it should be noted that toremifene 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 toremifene citrate has any effects counteracting estrogenic side effects that are unrelated to the tissues not affected by the drug. Namely there is no real causal connection to any reduction in water retention and acne in users that begin taking toremifene citrate as it relates to estrogen.The second, and possibly more beneficial, aspect of toremifene 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. Toremifene citrate would accomplish 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. Currently there is no available research that directly links toremifene citrate to being able to raise testosterone levels in male users, however due to the nearly identical mechanisms that both tamoxifen and toremifene citrate use and the reactions that they produce in the body, it would be easy to extrapolate that both drugs should have similar effects in this respect as well. Anecdotally users have reported good results with toremifene citrate and say that they are at least comparable that those of tamoxifen citrate.

Athletes and bodybuilders will usually take around 60-100 mg per day of toremifene per day which is equal to roughly 20-40mg per day of the drug nolvadex.


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Last edited by K1; 05-28-2012 at 05:33 PM.
   
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Faslodex
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Faslodex - 11-02-2011, 11:46 AM



Fulvestrant is a highly selective estrogen receptor antagonist. It exerts its action in the body not by targeting the production of estrogen, but by preventing it from exerting activity on the body. It does this by binding available estrogen receptors in a competitive manner, making them unavailable for circulating estrogens. This mode of action is very similar to Nolvadex and Clomid, although unlike these two agent fulvestrant does not have mixed agonist/antagonist properties. It is a pure estrogen receptor antagonist. This agent also stands out as the first inject able estrogen antagonist to catch the attention of the athletic and bodybuilding world. Although not widely used here, when applied it may be effective drug for mitigating the side effects of excess estrogen caused by anabolic/androgenic steroid use such as gynecomastia, fat buildup, and increased water retention. Fulvestrant was developed by the pharmaceutical company AstraZeneca. It was approved as a prescription drug in the U.S in 2002, and is sold under the brand name of Faslodex. The drug is indicated for the treatment of estrogen receptor positive breast cancer with disease progression following traditional anti estrogen treatment with drugs such as nolvadex. The company has since expanded its market for Faslodex to include over a dozen countries worldwide.

Fulvestrant is very potent as an anti estrogen, significantly more so than earlier medications like nolvadex and clomid. Although it targets estrogen at its receptor and not its production, it can still produce an environment of low estrogencity on par with strong aromatase inhibition. One study, for example shows fulvestrant to be as effective in arimidex in treating breast cancer patients who have already failed with first line endocrine treatments. Another shows the drug prevents tumor cell turnover and growth significantly more effectively than tamoxifen citrate. Studies investigating the physiological response to fulvestrant note that the drug actually down regulates estrogen receptor concentrations. Furthermore, it also tends to down regulate progesterone receptor concentrations. Fulvestrant does not cross the blood brain barrier, and for this reason is believed to produce fewer neurological side effects such as hot flashes, mood alterations, and low energy. The most common side effects associated with the drug include gastrointestinal disturbances such as nausea, vomiting, constipation, ab***inal pain, and diarrhea. Other common adverse effects include headache, back pain, hot flashes, and sore throat. Less common side effects include rash, loss of strength, urinary-tract infections, venous thromboembolism, liver enzyme elevations, vaginal bleeding, muscle pain, and low white blood cell count. Injection side reactions may also occur. Anti estrogens can harm the development of unborn fetuses and should not be taken by pregnant women. The drug is most commonly supplied in pre-filled syringes containing 50mg/ ml.

Fulvestrant is FDA approved for the treatment of hormone receptor positive metastatic breast cancer in postmenopausal women with disease progression following anti estrogen therapy. The recommended dose is 250mg administered intramuscularly per month as a single 5ml injection or two 2.5ml injections. When used off label to mitigate the estrogenic side effects of anabolic/androgenic steroid use, male athletes and bodybuilders may find a similar dose as is used for medical reasons to be effective for their needs.


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Last edited by K1; 05-28-2012 at 05:34 PM.
   
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Femara (letrozole)
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Femara (letrozole) - 11-02-2011, 11:47 AM



Letrozole is a non steroidal selective third generation aromatse 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 unkown brest cancer. It is typically used as a second line of treatment after an estrogen receptor antagonist like tamoxifen has failed to elicit a deseribale 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 mitigatge 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 Femera. 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 lutenizing 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 gynocomastia, 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 gynocomastia 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 gynocomastia, 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 lutenizing 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
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Nolvadex (tamoxifen citrate)
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Nolvadex (tamoxifen citrate) - 11-02-2011, 11:48 AM



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 gynocomastia. 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 gynocomastia should not be able to develop. When using anabolic steroids that can convert to estradiol (estrogen) this protection against gynocomastia 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 etrogenic 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 clomiphine citrate, tamoxifen citrate has also been shown to increase luteinizing hormone responsiveness to gonadotropin releasing hormone. Clomiphine 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 gynocomastia 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.


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Teslac (testolactone)
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Teslac (testolactone) - 11-02-2011, 11:48 AM



Testolactone is a first generation non selective steroidal aromatase inhibitor, used clinically to treat estrogen dependant breast cancer. Its exact mode of funciton is unkown, 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 gynocomastia. 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, leutenizing 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 estadiol, 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 gynocomastia, 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.


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02-04-2013, 05:17 PM

I've always heard that Aromasin is the best way to go during the cycle. Are you of the same opinion?
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02-17-2013, 05:05 AM

I'm seeing good results on 25mgs a day I just wonder if I'm suppressing my estrogen levels too low that I'm suppressing gains
   
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Ralox - 03-27-2014, 02:01 PM

Hey guys I'm new on this board, I wanted to know if it would be a good idea to use tamos only to reverse gyno?
   
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Anti-Estrogen Profiles
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Anti-Estrogen Profiles - 03-27-2014, 02:11 PM

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05-01-2015, 02:15 PM

Great read on the different AIs. Be careful with Letro, guys, since it is VERY strong. You do not want to lose ALL your E2 - that would suck.
   
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