The Importance Of Anti-estrogens

mercredi 31 juillet 2013

The Importance Of Anti-estrogens



Anastrozole (Arimidex ®) is the aromatase inhibitor of choice. The drug is appropriately used when using substantial amounts of aromatizing steroids, or when one is prone to gynecomastia and using moderate amounts of such steroids. Arimidex does not have the side effects of aminoglutethimide (Cytadren ®) and can achieve a high degree of estrogen blockage, much moreso than Cytadren ®. It is possible to reduce estrogen too much with Arimidex, and for this reason blood tests, or less preferably salivary tests, should be taken after the first week of use to determine if the dosing is correct. As an aromatase inhibitor, Arimidex's mechanism of action -- blocking conversion of aromatizable steroids to estrogen -- is in contrast to the mechanism of action of anti-estrogens such as clomiphene (Clomid ®) or tamoxifen (Nolvadex ®), which block estrogen receptors in some tissues, and activate estrogen receptors in others. During a cycle, if using Arimidex, there is generally no need to use Clomid as well, but (as mentioned in the section on Clomid) there may still be benefits to doing so





Letrozole (Femara)



Active Life: 2-4 days

Drug Class: Aromatase inhibitor (Oral)

Average Dose: 0.5 - 2.5 mg/day

Acne: Yes

Water Retention: No

High Blood Pressure: May reduce bp when using aronatizable steroids

Liver Toxic: Yes, dose dependant

Decrease HPTA function: No



Femara (generic name is letrozole) is a new drug developed for the treatment of advanced breast cancer in women. Femara is the second in a new class of third-generation selective oral aromatase inhibitors.. 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. This is the basic premise behind Nolvadex, except this drug blocks the action and not production of estrogen. The effects of Femara can be quite dramatic to say the least. A daily dose of one tablet (2.5 mg) can produce estrogen suppression greater than 80 % in treated patients. With the powerful effect this drug has on hormone levels, it is only to be used (clinically) by post-menopausal women whose disease has progressed following treatment with Nolvadex. Side effects like hot flushes and hair thinning can be present, and would no doubt be much more severe in pre-menopausal patients.



For the steroid using male athlete, Femara shows 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 Femara appears able to do the job much more efficiently, and with less hassle. Its use is only now catching on, but early reports have been excellent. A single tablet daily, the same dose use clinically, seems to be all one needs for an exceptional effect (some even report excellent results with only 1/4 tablet daily). 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 the one drug halting estrogen conversion and the other blocking 5-alpha reduction (testosterone, methyltestosterone and Halotestin only), 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 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 does not display an anti-estrogenic effect on cholesterol values, it is the preferred from of estrogen maintenance for those concerned with cardiovascular health.



Femara has another principle drawback, namely the great price of this drug. Tablets can be quite costly with regular use, but it can ward off the side effects of strong androgens 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 Femara have also been formulated "for research purposes" and are currently circulating the black market. Generic tabs are also available and these two forms represent a very cost-effective alternative for buying the brand name drug.





CLOMID

Clomiphene Citrate
(Clomid)



This drug is not a steroid; it is a synthetic estrogen used as a fertility drug. In men it can work as both an anti-estrogen, and a gonadotropic stimulant. Male steroid users find that it can work quite well to prevent gynecomastia while taking steroids that aromatise. It also is used to bring the body's natural testosterone levels back up to normal after a steroid cycle. The clomid acts directly on the pituitary gland to stimulate more gonadotropins. Women have used this drug to reduce the amount of estrogen in their systems, usually to harden up before a show. But in some cases women suffer estrogen deficiencies that can cause a number of side effects. No adverse reactions have been seen in males who used this drug. It can be quite effective, but is not favoured over HCG or Nolvadex in these areas. A dosage of 50 milligram per day for short cycles is most often seen.



Clomid typically come in 50 mg tablets in boxes of between 10 - 25 per box in blister packs. Clomid is a synthetic estrogen used to induce ovulation in women. Bodybuilders typically use Clomid as an anti-estrogen and to stimulate testosterone production when coming off a steroid cycle. Clomid causes an elevation of follicle stimulating hormone and luteinizing hormone. As a result, natural testosterone production is also increased. After a steroid cycle, testosterone production is suppressed. If testosterone levels are not brought to normal, a dramatic loss in size and strength may occur. Clomid is an excellent drug for preventing this crash.



Clomid is also an estrogen that works very well as an anti-estrogen. The reason that it works is that Clomid is a weak estrogen. It will typically bind to the estrogen receptors not allowing the harsher estrogens that are a byproduct of a testosterone cycle from attaching to the receptors. This signifigantly cuts down on the risks of bad side effects such as gyno. Cycling bodybuilders will suffer from an elevated estrogen level at the conclusion of a cycle. A high estrogen levels and low testosterone levels can be a disasterous combination. 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. As far as side effects go, Clomid is a fairly safe drug. At the worst, you will get bloating, stomach pains, blurred vision, headaches, nausea, and dizzyness.



Effective Dose

The common dosage in male bodybuilders is 50- 100 mgs. per day taken for up to two weeks at a time. Most of the time you will be back to normal by 1 week of usage but it never hurts to take a little extra just to be on the safe side. You need to take Clomid with meals as well.



Street Price

This product is really expensive in US pharmacies so the black market price is high as well. It will sell for between $2 - 4 per tablet.



Stacking Info

This product is usually taken along with HCG. HCG is taken for a week or two first since its effects will start within a few hours of injection. Then Clomid is taken for a few weeks since Clomid helps regenerate the entire testosterone producing cycle whereas HCG only has direct testosterone stimulating effects on the LH (luteinizing hormone) production to stimulate testosterone production.





NOLVADEX

Tamoxifen Citrate
(Nolvadex)



This drug is a potent nonsteroidal anti-estrogen. It is intended for use in estrogen dependent tumors, i.e. breast cancer. Steroid users take Nolvadex to prevent the effects of estrogen in the body. This estrogen is most often the result of aromatizing affect of steroids. It can aid in preventing edema, gynecomastia, and female pattern fat distribution, all of which might occur when a man?s estrogen levels are too high. Also these affects can occur when androgen levels are too low, making estrogen the predominant hormone. This can occur when endogenous androgens have been suppressed by the prolonged use of exogenous steroids in combination with cutting of these exogenous sources. Nolvadex works by competitively binding to target estrogen sites like the breast.



This drug is not toxic nor have any side effects been seen in athletes who used the drug as an anti-estrogen. This drug is the most popular anti-estrogen among steroid users by far. Although this drug does not turn out to be 100% effective for everyone, it does seem to exhibit some level of effectiveness for all. It works so well for some bodybuilders, they can take untraditional drugs like Dianabol or Anadrol right up to a contest as long as they stack it with Nolvadex. It would seem wise to take this drug in conjunction with any steroid cycle. Most reported a dosage of 10mg to 20mg daily got the job done. Availability of Nolvadex has been fair on the black market.



Nolvadex is very comparable to Clomid, behaves in the same manner in all tissues, and is a mixed estrogen agonist/antagonist of the same type as Clomid. The two molecules are also very similar in structure.



It is not correct that Nolvadex reduces levels of estrogen: rather, it blocks estrogen from estrogen receptors and, in those tissues where it is an antagonist, causes the receptor to do nothing.



The claim that Nolvadex reduces gains should not be taken too seriously. The fact is that any number of bodybuilders have made excellent gains while using Nolvadex. The belief that it reduces gains seems to stem from the fact that the scientific literature reports a slight reduction in IGF-1 (individuals using anabolic steroids were not studied though) from use of Nolvadex. Thus, Dan Duchaine reported that it reduces IGF-1 and therefore reduces gains. However, if this effect exists at all, it must be very minor, due to the excellent gains that many have made, and from the fact that no one has noticed any such thing from Clomid, which has the same activity profile.



However, I would not be surprised if one were to tell a steroid user that Clomid reduced his gains, he would immediately become afraid that Clomid reduced his gains (please note that no one I have ever heard of has noticed this.) Not having been so misled, however, he would not conclude this from his results. But if an authority publishes that such an effect occurs, whether it does or not it can become self-fulfilling by biasing the user.



The fact that Nolvadex will reduce water retention may result in the user agreeing that gains are less, since weight gain is less, thus reinforcing the bias. Many bodybuilders take 10-20 mg of Nolvadex each day for the last month prior to a bodybuilding contest to help reduce water retension and increase muscle hardness.

by muscleup





via World Class Bodybuilding Forum http://www.worldclassbodybuilding.com/forums/f484/the-importance-of-anti-estrogens-133962/

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