By Josh Hodnik
Disclaimer: This article is being published for educational and entertainment purposes. The information in this article does not constitute sound medical advice, nor does the author or this website condone the use of PED’s, Anabolic Steroids or any other drugs. Always seek the advice of a skilled Medical Practitioner before considering the use of any drugs whatsoever.
The way anabolic steroids and other performance enhancing drugs (PEDs) are used today, compared to when they were first introduced to the sporting world many decades ago, has changed dramatically. Today there is a much better understanding of how these chemicals work, and there are also more drugs available. In the ’70s and 80’s a bodybuilder’s steroid cycle generally consisted of testosterone, methandienone, nandrolone, and methenolone enanthate – when it was available.
During this time, the most common anti-oestrogen used was Nolvadex, and there was really not much else available to combat the elevated oestrogen levels that accompany steroid use. This was a time before Arimidex, Letrozole, and the other anti-oestrogens that are common today, including Fulvestrant, which looks (to me) to be one of the safest and most effective.
Bodybuilders who take anabolic steroids are always looking for that new steroid or PED that will yield the largest reward, but they also want minimal side effects. Often times a bodybuilder will take high doses of testosterone or other steroids in an attempt to pack on more muscle mass, and will then add other drugs like Arimidex or Exemastane to reduce the associated rise in oestrogen levels and limit the side effects. Taking oral steroids such as Anadrol, Winstrol, or Dianabol are also known to tax the liver, which is usually a concern to anyone taking these compounds. However, the potential dangers of long-term administration of anti-oestrogenic or anti-aromatase drugs have been almost completely ignored.
Tamoxifen (Nolvadex) has been shown to greatly increase the risk of fatty liver disease. Recent human studies have shown that tamoxifen-treated women had three times the risk of developing liver disease, which appeared as soon as three months after commencement, at doses of only 20mg per day. Nolvadex was first developed to treat breast cancer in women, and there is a favourable trade-off when risking liver disease to treat breast cancer. However, this trade-off is certainly not favourable when the medication is not being taken to treat a potentially deadly disease.
The body metabolises oral and injectable medications differently. This is the primary reason why Nolvadex, and other oral anti-oestrogenic/anti-aromatase drugs, have the potential for liver toxicity. Oral medications require first-pass metabolism, where it is metabolised 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 as they are delivered directly to the bloodstream, where it will only go through the second pass process. As they avoid the first pass, most injectable medications are less likely to cause liver toxicity.
But what if there was a drug available in an injectable form that could control the oestrogen-related side effects that arise from anabolic steroid use? The truth is that an injectable medication that is effective in eliminating excess oestrogen does exist, and it’s known as Fulvestrant. This drug was first introduced as a medication to treat breast cancer over a decade ago, and it has also been used to treat women with breast cancer who did not respond well to treatments with oral Tamoxifen. It is in a class of medications called oestrogen receptor antagonists, which means it is able to eliminate the action of oestrogen by blocking available oestrogen receptors.
A 250mg monthly injection of Fulvestrant has shown to be as effective at lowering oestrogen in the body as 1mg of Arimidex or 2.5mg of Femara per day. 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.