The Prototypical "Anti-Estrogen"...Tamoxifen
Tamoxifen is the oldest anti-estrogen and the first in a host of later drugs to follow that were initially intended to block the effects of estrogen in estrogen dependent breast cancer in females. Tamoxifen has the longest track record and a very safe one. We all know that the world of bodybuilding has used many a tamoxifen pill.
Most of us also know how tamoxifen works. Remember the two classes of anti-estrogens, one is by attaching to the receptor itself (and thereby occupying the receptor from linking up with regular estrogen), and the other is to block the actual production of estrogen by binding up the aromatase enzyme. Tamoxifen, or Nolvadex as its trade name does not block the aromatase enzyme, but occupies the estrogen receptor and lessens the amount of real estrogen active in the body. After all, Nolvadex/Tamoxifen itself, is, a weak estrogen.
What many of you may not know, is that tamoxifen/nolvadex at the time of this writing is being investigated as a drug that appears to offer many advantages for men in decreasing cardiovascular risk. How great would that be? One of our ancilliary drugs having a function that actually protects us from some of the negative effects our 'other' drugs may cause? Wow! You want to know how? This is really interesting stuff...well if you are a muscle and physiology geek at all like me, you might like to know what goes on in our bodies from all of our crazy practices.
Well, at least two major benefits tamoxifen has shown in clinical trials. Number one, tamoxifen lowers TNF-alpha (huh?) in more than a few studies. Who cares? TNF-alpha is a major inflammatory substance that increases inflammation in the entire body, specifically the arterial system. If you keep it low, the arterial system is under less stress. It is a rare find for a drug to decrease this substance since most drugs have toxic effects which contribute to raising TNF-alpha.
Secondly, tamoxifen has been shown to lower C-Reactive Protein or CRP in both men and women who use it for therapeutic purposes. CRP is the main big gun that is loaded up by many other substances in the body including TNF-alpha. Once CRP begins to elevate, you are in trouble. Most medical authorities agree that the old cardiovascular risk marker homocysteine, is now a thing of the past compared to the implications of a high CRP. High CRP, high risk factor for cardiovascular mortality, even if you are lean and in shape. CRP is the universal bad guy with respect to heart risk.
Tamoxifen, by having a lowering affect on TNF-alpha and CRP, along with a few other harmful substances in the body, may very soon prove to be a legitimate anti-aging and cardioprotective drug. If it does, you will find mainstream medicine catching on slowly and more and more aging men with a prescription from their GP for nolvadex or a compounded generic tamoxifen in the US, and many other areas of the world.
The dose needed? Only around 10mg/day.