Anti-Estrogens or Aromatase Inhibitors (AI)

Arimidex (Anastrozole)

Arimidex (generic name is anastrozole) is a very new drug developed for the treatment of advanced breast cancer in women. Anastrozole is a Selective Androgen Receptor Modulator (SARM) because it is a compound that acts directly on the androgen receptor. It acts by blocking the enzyme aromatase, subsequently blocking the production of estrogen. Since many forms of breast cancer cells are stimulated by estrogen, it is hoped that by reducing amounts of estrogen in the body the progression of such a disease can be halted. A daily dose of one tablet (1mg) can produce estrogen suppression greater than 80% in treated patients.

For the steroid using male athlete, Arimidex shows a great potential. Up to this point, drugs like Nolvadex and Proviron have been our weapons against excess estrogen. These drugs, especially in combination, do prove quite effective. But Arimidex appears to do the job much more efficiently and with less hassle. A single tablet daily, seems to be all one needs for an exceptional effect (some even report excellent results with only 1/4 tablets taken every day or every other day). When used with strong, readily aromatizing androgens such as Dianabol or testosterone, gynecomastia and water retention can be effectively blocked. In combination with Propecia (Finasteride), we have a great advance. With one drug halting estrogen conversion and the other blocking 5-alpha reduction (testosterone), related side effects can be effectively minimized. Here the strong androgen testosterone could theoretically provide incredible muscular growth, while at the same time being as tolerable as nandrolone. Additionally the quality of the muscle should be greater, the athlete appearing harder and much more defined without holding excess water.

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 estrogen from becoming apparent (namely its effects 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 form of estrogen maintenance for those concerned with cardiovascular health.

Aromasin (Exemestane)

Aromasin is a steroidal suicide aromatase inhibitor, it is called a Selective Androgen Receptor Modulator because it is a compound that acts directly on the androgen receptor. Exemestane works to lower estrogen production in the body by blocking the enzyme responsible for synthesizing these hormones. Aromasin is for the treatment of breast cancer, specifically in post-menopausal women whose cancer has progressed following therapy with a first line agent such as tamoxifen.

Aromasin may perhaps be the most effective aromatase inhibitor available to date. While Femara and Arimidex boast of estrogen suppression around the 78-80% in their packaging inserts, Aromasin reports it can lower estrogen as much as 85% on average. Feedback from bodybuilders tends to support the preference for Aromasin over other anti-estrogens, so this my very well be the case. Regardless of which one is the true “king” aromatase inhibitor, all of the newer pharmaceutical agents, Arimidex, Femara, and Aromasin, should be looked at as extremely effective for reducing estrogen synthesis in the body. A possible 10% difference in inhibition between the weakest and the strongest of the three is really not going to amount to all that much during your next cycle. If you are looking at one of these agents to prevent gynecomastia and help you lose fat and water on your next cycle, they are all going to do a good job for you. If you absolutely need the best agent, my money would be on this one.

It is important to point out that there are some disadvantages to using an aromatase inhibitor over mixed estrogen agonist/antagonists (anti-estrogen) like Nolvadex and Clomid, the most notable being unwanted (negative) alterations in serum cholesterol values. This is because estrogen is tied with HDL (good) cholesterol synthesis and LDL (bad) cholesterol metabolism, and aromatase inhibitors block estrogenic action. Clomid and Nolvadex, on the other hand, tend to exert a positive influence on cholesterol values, as they are both active estrogens in the liver. If you are trying to prevent estogenic side effects like gynecomastia, bloating and excess water retention in general, these agents are probably better choices (they do the same job and are safer on your cholesterol levels).

Aromasin is very potent and can be used at lower dosages than the recommended 25mg daily. In fact, studies have shown maximum estrogen suppression in some patients with as little as 2.5mg per day. That is not a recommendation to smash each tablet into 10 little pieces, but it does make the current armchair advice of taking 1/2 a tablet every day or two seem well justified.

Clomid (Clomiphene Citrate)

Clomid is the brand name for the drug clomiphene citrate, it is called a Selective Estrogen Receptor Modulator (SERM) because it is a compound that acts directly on the estrogen receptor. The drug is not an anabolic steroid but a prescription drug generally prescribed to woman as a fertility aid due to the fact that it shows ability to stimulate ovulation. Clomid is a chemically synthetic estrogen with both agonist/antagonist properties. In certain target tissues is can block the ability of estrogen to bind with its corresponding receptor. Its clinical use is therefore to oppose the negative feedback of estrogens on the hypothalamic-pituitary-ovarian axis, which enhances the release of luteinizing hormone (LH) and follicle stimulating hormone (FSH).

Clomid when taken for athlete purposes does not offer a tremendous benefit to women. However, in men the negative feedback on the hypothalamic-pituitar-testicular axis will cause an elevation in both FSH and (primarily) LH which will result in an increase in natural testosterone level production. This affect can be beneficial to the athlete at the end of a steroid cycle when endogenous testosterone levels are depressed. If endogenous testosterone levels are not restored quickly, a dramatic loss in size and strength is likely to occur. This is due to the fact that without testosterone (or other androgens), the catabolic hormone cortisol becomes the dominant force affecting muscle protein synthesis (quickly bringing about a catabolic metabolism). Often referred to as the post-steroid crash, it can quickly eat up much of your newly acquired muscle. Clomid can play a crucial role in preventing this crash in athletic performance. As for woman, the only real use for Clomid is the possible management of endogenous estrogen levels near contest time. This can increase fat loss and muscularity, particularly in female troubles areas such as this hips and thighs.

Male athletes generally find that a daily intake of 50 -150mg over a four to six week period will bring endogenous testosterone production back to an acceptable level. This raise in testosterone should occur slowly but evenly throughout the period of intake. Studies have shown that a dose of 150mg of Clomid will raise your testosterone levels by around 150%.

Clomid can also help with elevated levels of estrogen during a cycle. A high estrogen level puts an athlete in serious risk of developing gynecomastia, which is an obvious unwanted side effect. With the intake of Clomid, the athlete can reduce the risk of developing gynecomastia. The drug also can ward of excess water/fat retention with the minimized estrogen activity. Unfortunately this is not always the case however, and many find it necessary to addition another anti-estrogenic drug. The most common adjunct is Proviron, an oral DHT used to competitively lower aromatase activity and raise the androgen to estrogen ratio.

As for toxicity and side effects, Clomid is considered a very safe drug. Bodybuilders seldom report any problems, but listed possible side effects do include hot flashes, nausea, dizziness, headaches and temporarily blurred vision. Such side effects usually only appear in females however, as they feel the effects of estrogen manipulation much more readily than men.

Femara (Letrozole)

Letrozole is a non-steroidal third generation aromatase inhibitor. It is a Selective Androgen Receptor Modulator (SARM) because it is a compound that acts directly on the androgen receptor. It is used to treat postmenopausal women with estrogen receptor-positive or estrogen receptor-unknown (unsure if the cancer is responsive to estrogen) breast cancer. The structure and activity of this compound are very similar to that of Arimidex (Anastrozole). Femara is typically used as a second line of treatment, after an estrogen-receptor antagonist like tamoxifen has failed to elicit a desirable response (although at times it is used as a first line option as well).

Femara and Arimidex represent the newest achievements in a long line of drugs targeting aromatase inhibition. These are amongst the most potent estrogen-lowering drugs made to date, working far more effectively than the non-selective first generation aromatase inhibitors, like Teslac and Cytadren, to come before them. The dosage of each tablet of Femara 2.5 milligrams, which according to the product insert was sufficient to lower estrogen levels by 78% during clinical trials. The drug, however, appears to still be extremely affective in much lower dosages. The package insert for the product itself comments that during clinical studies doses of .1 and .5 milligram produced 75% and 78% estrogen inhibition, respectively. When it comes to a product like this, typically the reflects what seems to work for almost everyone who takes it. A large number of people may respond extremely well to lower doses, however, to make sure each patient is receiving the proper benefit of the drug a standard effective dosage unit is ascertained and used.

It is important to point out that there are some disadvantages to using an aromatase inhibitor over mixed estrogen agonist/antagonists (anti-estrogen) like Nolvadex and Clomid, the most notable being unwanted (negative) alterations in serum cholesterol values. This is because estrogen is tied with HDL (good) cholesterol synthesis and LDL (bad) cholesterol metabolism, and aromatase inhibitors block estrogenic action. Clomid and Nolvadex, on the other hand, tend to exert a positive influence on cholesterol values, as they are both active estrogens in the liver. If you are trying to prevent estrogenic side effects like gynecomastia, bloating and excess water retention in general, these agents are probably better choices (they do the same job and are safer on your cholesterol levels). But if you want that really tight, dry, defined look that is often sought after when you are cutting, Nolvadex or Clomid are not quite going to cut it. In such cases, I think you will find Femara to serve you well.

Like Arimidex, each tablet can be broken up if you desire to stretch out the value of the drug. In fact, with studies showing maximum inhibition in some patients with doses as low as 1/2 milligram, each 2.5 milligram tablet can be broken up in to as many as 5 separate doses (perhaps even more). But the typical use amongst bodybuilders is to cut the tabs in half, and take one every other day (unless needed daily). In terms of overall power, Femara seems to be a little bit more potent than Arimidex, at least by most people’s estimations. If both agents are available for the same price, Femara would probably be the one to would go for.

Nolvadex (Tamoxifen Citrate)

Nolvadex is the trade name for the drug tamoxifen citrate, it is an estrogen agonist/antagonist which competitively binds to estrogen receptors in various target tissues. With the tamoxifen molecule bound to this receptor, estrogen is blocked from exerting any action, and an anti-estrogenic effect is achieved. Nolvadex is called a Selective Estrogen Receptor Modulator (SERM) because it is a compound that acts on the estrogen receptor. It should be noted that when one uses nolvadex, since the drug acts to only block the estrogen, your total body estradiol level will increase as there are less receptors that are in a free state to be bound to. It should also be noted that Nolvadex will block most of the estrogen however some will still bind to the estrogen receptors.

Tamoxifen citrate is an antagonist at estrogen receptor in the breast, and a agonist at the estrogen receptor in the uterus. Antagonist meaning inhibiting the affect of estrogen and agonist meaning to stimulate the effect of estrogen in the various tissues. Many forms of breast cancer are responsive to estrogen, the result of tamoxifen citrate used to treat this condition is a very effective form of treatment, as tamoxifen citrate inhibits the estrogen effect in the breast tissue.

Nolvadex is used by bodybuilders that use anabolic/androgenic steroids that aromatase and convert to estrogen. The excess estrogen can result in unwanted side effects, one which is of main concern is gynecomastia or the development of female breast tissue in men. The first symptoms of this are the appearance of swelling or a small lump under the nipple. If left to progress it can turn into a very unsightly development of tissue, often an irreversible occurrence without surgery. This estrogen can also lead to an increase in the levels of water retained by the body. The result here can be a notable loss of definition, the muscles beginning to look smooth and bloated due to the retention of subcutaneous fluid. Fat storage may also be increased as estrogen levels rise. This hormone is the primary reason woman have a higher body fat percentage, and different fat distribution (hips/thighs) than men. Steroid users sensitive to estrogen side effects should have an anti-estrogen on hand when taking problematic steroids to minimize the impact of side effects. It is also to note that when estrogen and body fat levels are normal, administering Nolvadex (both Men and Woman) can increase the look of hardness and definition in muscles.Tamoxifen citrate shows ability to increase the production of FSH (follicle stimulating hormone) and LH (luteinizing hormone) in the male body. This is accomplished by blocking negative feedback inhibition caused by estrogen at the hypothalamus and pituitary, which fosters the release of the mentioned pituitary hormones. Since a higher level of LH can stimulate the Leydig’s cells in the testes to produce more testosterone, Nolvadex can have a positive impact on one’s serum testosterone level. This “testosterone stimulating” effect is an added benefit when preparing to finish a steroid cycle. Since most anabolic/androgenic steroids will suppress endogenous testosterone production, Nolvadex can help restore a balance of hormone levels. Studies have shown that a dose of 20mg of Nolvadex will raise your testosterone levels by around 150%, therefore the use of Nolvadex on a post cycle therapy can greatly aid recovery.

A typical dosage of tamoxifen citrate is around 10 to 30mg, the amount being taken correspondent to the effect desired. It is best to begin with a low dosage of nolvadex and work up to the amount required, as to avoid taking an unnecessary amount. The time in which Nolvadex is started also relies on individual needs of the user. If an athlete with a known sensitivity to estrogen is starting a strong steroid cycle, Nolvadex should probably be added soon after the cycle has been initiated. If estrogen is probably not going to be a major problem during the cycle (but will likely be after), Nolvadex is administered around the time exogenous steroid levels will drop. It will be continued for some weeks after, until the point when natural testosterone is thought to be at an acceptable level.Nolvadex is also and estrogen agonist in the liver, capable of activating the estrogen receptor mimicking the actions of this sex hormone in this region of the body. As such it can have a markedly positive impact on HDL (good) cholesterol values, as does estrogen. Many similarly use this drug to counter some of the negative consequences of steroid use in regards to cholesterol values and cardiac risk, as steroids often suppress HDL and raise LDL levels considerably.

It has been reported by many however that Nolvadex seems to slightly reduce the gains made during a steroid cycle. It appears that many anabolic/androgenic steroids will exhibit their most powerful anabolic effect when accompanied by a sufficient level of estrogen. This may be one reason why gains made with a strong androgen like testosterone are usually much more pronounced than when using an anabolic that aromatizes to a lower degree. It therefore seems like good advice to be aware of how much Nolvadex is actually needed before committing to it during a cycle.

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