SARMs and the Liver by Jerry Brainum 6/20

 

 

I've written about selective androgen receptor modulator drugs or SARMs in past issues of Applied Metabolics. SARMs are experimental drugs that have never been approved by any official health agency for human use, but are nonetheless freely available on the Internet. As I noted in my previous articles about SARMs, there is much hype and hyperbole expressed about them over the web in both discussion forums and on sites that sell the drugs. But as with many other things that are available exclusively on the Internet, what you pay for isn't always what you get. In one of my articles, I recounted a study in which 50 SARMs were purchased on various websites. The products were then analyzed to determine whether the content matched the product labels. In this survey, 50% of the drugs proved to be either mislabeled, didn't contain the potency listed on the label, or in some cases, contained a completely different substance.

The big selling point about SARMs is that they provide many of the anabolic effects of anabolic steroid drugs, but provide far less of an androgenic effect. Anabolic steroids themselves are synthetic versions of testosterone, with many of the oral versions chemically modified to resist premature breakdown in the liver. For example, if you ingested testosterone orally, most of the dose would be degraded in the liver in about 30 minutes. But the oral steroids resist such breakdown and can accumulate to a degree in the liver. Indeed, that is the main problem with oral anabolic steroids. The anabolic effects of testosterone include increasing and maintaining bone mass, as well as promotion of increased muscle mass along with a decrease of body fat. While the androgenic effects of testosterone are often called "bad," they are important. Among these effects are the growth of sexual organs, body hair, and the deeper voice that is characteristic of men. This explains why when women use large doses of anabolic steroids, a common and unfortunately permanent side effect is a deeper voice that is caused by the drugs increasing the thickening of their vocal cords. Other androgenic effects of testosterone are less desirable. These include acne development, prostate gland enlargement, and male pattern baldness.

The fact that testosterone provides both anabolic and androgenic effects has been known since the discovery of testosterone by German scientists in 1934. While the anabolic effects of testosterone are considered useful, such as for maintaining muscle mass and bone mass, the androgenic effects are not. As such, this led scientists to develop new drugs that would emphasize the anabolic effects of testosterone while eliminating or at least minimizing the androgenic effects. The scientists were also aware that testosterone is rapidly degraded in the liver when ingested orally, so sought to produce a version that would survive the liver breakdown. As such, they came up with methyltestosterone in 1934. However, methyl testosterone proved far too androgenic, which set . . .