Off-label: Oxymetholone

       Oxymetholone - commonly known as Anadrol, Anapolon, A-bombs, and a few other names - is widely considered one of the big guns in the world of AAS. It was one of the early anabolics used widely in medicine  and caught on in the sporting world quickly for one reason: the stuff works like magic. If you are familiar with doping in sports you are familiar with the classic description of 'drol as a powerful and fast acting strength and size booster that comes with alot of water weight and side effects. And minus a few misconceptions, the popular idea of the drug is fairly accurate. But there is an element of mystery behind oxymetholone also. Partly this is because of the almost mythic status it has obtained as strength and physique athletes sing the Ballad of the Gainz, but in part it's also due to the misconceptions being cultivated and maintained in the pupular dialogue. In this short post I want to list and address a few things that contribute to the confusion. Some of these are flat-out myths, while others are areas we don't fully understand yet. As a reminder let's keep in mind this is for educational purposes and is not meant as a guide or as advocacy for the use of illicit ergogenics. My aim is to educate only, and as this is a topic of frequent debate both in the world of atheltics and the world of physiology research it fits in nicely here.

1. Oxymetholone converts rapidly to estrogen. False. So false. In fact oxymetholone cannot interact with the aromatase enzyme at all, and thus it cannot be converted into estrogen in any amount or at any pace.

 

2. Oxymetholone is not suppressive to the HPTA. Another myth. It clearly disrupts the HPTA heavily, as evidenced by the numerous studies in which it does precisely that.

 

3. Oxymetholone is a xenoestrogen. It's been noted that oxymethelone bears some structural similarity to estradiol and therefore hypothesized that it may possess inherent estrogenic qualities by stimulating the estrogen receptor itself instead of by converting to estrogen via aromatization. While this would seem to explain some reports of side-effects and treatment of them with selective estrogen receptor modulators literature on the topic is conspicuously absent. To date no substantial evidence has surfaced that indicates oxymetholone has any binding affinity for the estrogen receptor, although studies examining metabolites have not examined this in depth and further study is needed to rule out the possibility of estrogenic metabolites of the parent drug.

 

4.  Oxymetholone is a progestin. Another hypothesis lacking evidence at this point. There are no examples in the literature that I could find showing clear evidence for progestagenic activity.

 

       So how do we explain the side effects and the case reports and the popular folklore? The short answer is that right now we don't. Explanations range from a rumor-driven placebo effect in the doping community to alterations of glucose metabolism to metabolites with novel actions. We need to keep studying to find out.