SERMs - Clomid,Clomiphene,Nolvadex,Tamoxifene,Evista,Raloxifene

SERMS are great for first line defense against male estrogenic side effects. I say first line defense against gynecomastia because they generally peak in the bloodstream very quickly (withing a few hours) and directly help to block estrogen's effects on the estrogen receptor. Clomid/clomiphen,Nolvadex/tamoxifene,Evista/raloxifene,Fareston/toremifene and others make up this class of drugs. By doing this, you get a rapid effect of the drug on the estrogen receptor as compared to waiting until an aromatase inhibitor (AI) kicks in.

Aromatase inhibitors are great, and many times much more potent in decreasing estrogenic effects overall, but take a while to start working. The reason for this, is that the AI must first get into the bloodstream, elevate, then find aromatase and begin to either bind to it - reversibly or irreversibly. Conversely, these drugs get into the bloodstream, elevate to a good level rapidly, and then begin to saturate and block estrogen receptors.

So, if you are having a gyno attack or super water-logged from estrogenic bloating, you will want to first take a good SERM to begin to lessen your side effects ASAP.

There have been many of these antagonist drugs invented since the original days of Nolvadex for breast cancer in women, but there are four main ones known and used today. They are Nolvadex (tamoxifen), Clomid (clomiphene), Evista (Raloxifene), and Fareston (toremifene). Chemically, there are two main categories which these SERMS fall into. They are triphenylethylene and benzothiophene groups. Raloxifene is the only drug of the four SERMS which is a benzothiophene. The other three drugs are triphenylethylenes. This is the primary structure and backbone of the drug and does not play a huge difference in the effectiveness of the drug.

The half-life of the drug in question probably has a lot to do with it even though the literature does not seem to address this. Raloxifene being the only benzo, also has the shortest half-life of all drugs in this class-27.5hours vs 5 days and longer for the other drugs. Obviously, this will effect dosing and has implications for frequency of dosing as well. Let's get into this with a discussion on the updated 2008 version(s) of what is in the literature for each drug... SERMs Clomid Update Toremifene Update Nolvadex Update

Male Health Benefits of Tamoxifen

Raloxifene Update