from what i understand your body converts test to estrogen when there is an excess amount of test (not enough receptors for the test) because the excess test becomes free radicals and destroys vital organs.
i also understand that males need some estrogen for bone mass and other ****.
so when someone takes a anti-estrogen, and your body responds by attempting to produce more estrogen, does it go about by producing so much test that there would be an excess amount to convert to estrogen or does it simply produce some test (not excess) and aromatize that test. basically, can your body alter your test to estrogen conversion percentage.
This is the long version of it but please note the final paragraph for a summary.
Receptor blockers
Clomiphene (Clomid) and tamoxifen (Nolvadex) are the most popular drugs of this class. They are more precisely referred to as "selective estrogen receptor modulators." This is because their mode of action is not so simple as merely blocking the estrogen receptor. Estrogen receptors require not only hormone but also activation of regions of the receptor called AF-1 and AF-2. AF-1, to be activated, requires phosphorylation, while AF-2 can be activated by any of a number of cofactors, such as IGF-1.
As it happens, clomiphene and tamoxifen are estrogen receptor antagonists (blockers) in cells that depend on activation of the AF-2 region, while in cells which activate AF-1, these compounds are estrogens.
In some cells these drugs activate one of the types of estrogen receptor (ERa ) but are antagonists of the other type (ERb ).
The result is that these compounds are antiestrogenic in breast tissue, fat tissue, and in the hypothalamus, which is what we want in bodybuilding, but are estrogenic in bone tissue and with respect to favorable effect on blood lipid profile, both of which are, again, desirable. They also appear to have some estrogenic effect on mood, though this may be in only parts of the brain (the matter is not studied.)
Cyclofenil is a similar drug to the above two. Clomiphene will do everything that the other two will do, but for some unknown reason, has been found more effective than tamoxifen both medically and in bodybuilding for increasing LH production.
Raloxifene (Evista) is a new selective estrogen receptor modulator that, for women, has the advantage of being an antiestrogen in the uterus, whereas clomiphene and tamoxifen are estrogens in that tissue. For this reason, the latter two drugs can promote uterine cancer, while raloxifene actually should help prevent it, and is therefore a superior drug for women. It is not known how effective it may be in increasing LH production.
While on high dose androgens it is impossible to maintain LH production in any case, and clomiphene can do no good in that regard. As androgen levels return to normal, however, a dose of 50 mg/day of clomiphene if estrogen levels are reasonable, or 100 mg/day if estrogen levels are high, is usually effective in restoring natural testosterone production.
Because the drug has a long half-life, when one takes 50 mg/day the amount in the system is not only the 50 mg just taken, but also approximately another 250 mg from previous days. Thus, to immediately arrive at the therapeutic level, one would take 300 mg (50 mg six times) on the first day, and then continue with 50 mg/day.
A small percentage of individuals suffer vision problems from use of clomiphene, which is generally reversible upon discontinuance. These persons, of course, should not use the drug after discovering the problem.
It also must be pointed out that these are prescription drugs, and should be obtained and used only by precription with medical advice, though the selective estrogen receptor modulators have excellent safety records.
After a cycle, it is reasonable to continue clomiphene use until at least four weeks after the last injection of long acting ester, or at least two weeks after the last use of an oral, or until natural testosterone production is clearly back to normal, whichever comes last.
Conclusion
Other than acne and accelerated hair loss, the two most common problems of AAS use are gynecomastia and difficulty in recovering natural testosterone production. Antiestrogenic drugs can effectively address both problems and are safe for most individuals. Ideally, if aromatizable drugs are used, the problem is corrected at the source by limiting production of estrogen by using an aromatase inhibitor. However, it is also effective to use a selective estrogen receptor modulator such as Clomid. The latter drug is also of particular use in helping to restore natural testosterone production after a cycle.
