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TweetFulvestrant: Safer than Nolvadex?
What if there was a drug available in an injectable form that can control estrogen related side effects that often occur from anabolic steroid use?
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The way anabolic steroids and other performance enhancing drugs are used today compared to when they were first introduced to the sports world many decades ago, has changed dramatically.
Today, there is a much better understanding of how these chemicals work, and there are simply more drugs available. In the 70’s and 80’s a bodybuilder’s steroid cycle generally consisted of testosterone, methandienone, nandrolone, and methenolone enanthate when it was available. It is rumored that Arnold stacked these steroids together while competing. It is also rumored that Arnold had access to European steroids like Primobolan, when other competitors in the US had to rely on a limited selection of steroids that originated in Mexico.
During this time, the most common anti-estrogen used was Nolvadex, and there was really not much else available to combat elevated estrogen levels that accompany steroid use. This was a time before arimidex, letrozole, and the other anti-estrogens that are common today; Fulvestrant, for example, which looks (to me) to be one of the safest and most effecitve.
Bodybuilders that take anabolic steroids are always looking for that new steroid or performance enhancing drug that yields the largest reward with minimal side effects.Often times a bodybuilder will take high doses of testosterone or other steroids to pack on more muscle mass, and then add other drugs like Arimidex or Exemastane to reduce estrogen levels, which are usually elevated with higher steroid doses. Taking oral steroids such as Anadrol, Winstrol, or Dianabol have been known to be taxing on the liver, and this is usually a concern to anyone taking these compounds. However, the potential dangers of long-term administration of anti-estrogenic or anti-aromatase drugs have been almost ignored completely.
Tamoxifen (Nolvadex) has been shown to greatly increase the risk of fatty liver disease. Recent human studies have shown that tamoxifen treated women had a 3 times the risk of developing liver disease, which appeared as soon as 3 months at only 20mg per day(1). Nolvadex was first developed to treat breast cancer in women, and there is a favorable trade-off when risking liver disease to treat breast cancer, but the trade-off is certainly not favorable when the medication is not being taken to treat a deadly disease.
The body metabolizes oral and injectable medications differently, and this is the primary reason that Nolvadex and other oral anti-estrogenic/anti-aromatase drugs have the potential for liver toxicity. Oral medications require first pass metabolism where it is metabolized in the gut and the liver before being delivered into the bloodstream. After the first pass, the medication is transported through the blood to other tissue where it is absorbed. Some of the drug will continue on and will require a second pass through the liver. Injectable medications bypass first pass metabolism and will be delivered directly to the bloodstream where it will require just the second pass. While avoiding the first pass, most injectable medications are less likely to cause liver toxicity.
What if there was a drug available in an injectable form that can control estrogen related side effects that often occur from anabolic steroid use? Being an injectable would avoid first pass metabolism that occurs with oral medications, which would be much less taxing on the liver. An injectable medication effective in eliminating excess estrogen does exist, and it is known as fulvestrant. This drug was first introduced as a medication to treat breast cancer over a decade ago, and it has been used to treat women with breast cancer that did not respond well to treatment involving oral tamoxifen. It is in a class of medications called estrogen receptor antagonists, and it is able to eliminate the action of estrogen after blocking available estrogen receptors.
A 250mg monthly injection of fulvestrant has shown to be as effective as 1mg of Arimidex or 2.5mg of Femara per day at lowering estrogen in the body. This drug was first marketed under the trade name Falsodex, and even though the studies behind the drug have panned out well, a hefty price tag has slowed the momentum of this drug. Treatment using Falsodex has a cost that is about ten times greater than Arimidex or Femara. As with most drugs, when the original patent expires on Falsodex, a generic version will be available, which will greatly reduce the price. There might even be versions available in the European or Asian markets at this time.
Khalid A Osman; Meissa M Osman; Mohamed H Ahmed (2007). “Tamoxifen-induced non-alcoholic steatohepatitis: where are we now and where are we going?”. Expert opinion on drug safety 6 (1)
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