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20.04.2012


The testosterone effect of ibuprofen

The painkillers ibuprofen and diclofenac probably cause a temporary boost in testosterone levels, if the results of a 2009 Finnish-Swedish in vitro study published in Steroids are anything to go by. The study also shows that some synthetic testosterone users are able to mislead doping hunters by using these over-the-counter drugs.


Two key enzymes in the breakdown of testosterone are UGT2B17 and UGT2B15. They attach sugar groups to the testosterone molecules, which enables the kidneys to eliminate them. You can read more about this in Chapter 10 of our Anabolics Book. If the enzymes work less hard then there might just be more testosterone circulating in your body.

In some people the enzyme UGT2B17 works less well, or doesn't work at all. These people can use high doses of testosterone without them showing up in a doping test. In the usual test for testosterone, doping hunters look at the ratio between glycosylated testosterone and glycosylated epitestosterone in the urine. If the UGT2B17 enzyme isn't working, the urine contains relatively little sugared testosterone [structural formula shown below]. The glycosylation of epitestosterone is the work of a different enzyme.

Testosterone Glucuronide
The researchers wanted to know what the effect is on the glycosylation of testosterone of the anti-inflammatory painkillers [NSAIDs] diclofenac and ibuprofen, as these are widely used in the sports world. They added testosterone to enzyme producing liver cells in a test tube, and then proceeded to add increasing concentrations of diclofenac and ibuprofen. They then measured the amount of sugared testosterone and epitestosterone that was created. Both painkillers inhibited the glycosylation of testosterone – but not that of epitestosterone.







If you take 800 mg ibuprofen, an hour later there'll 13-35 micrograms of the stuff in one millilitre of your blood. That's 0.06-0.12 micromoles. As you can see above, this should have an effect. This might therefore be a partial explanation for the anabolic effect of anti-inflammatories such as ibuprofen in elderly – and not in younger – athletes.

Older athletes should be able to boost their testosterone level temporarily by taking ibuprofen. Certainly if they take it after training, when the muscle cells are sucking anabolic hormones out of the bloodstream, ibuprofen might have an ergogenic effect. [Hmm. We wonder whether there's some naturally occurring substance that works in the same way as ibuprofen…]

So taking diclofenac or ibuprofen makes normal athletes resemble athletes who don't have the UGT2B17 enzyme. If these athletes inject synthetic testosterone, then the conventional doping test for testosterone may not work properly.

But the effect is bigger in athletes who don't have the UGT2B17 enzyme. In them UGT2B15 partially takes over the work of UGT2B17 and this enzyme also works less well when diclofenac and ibuprofen are present. This means that in practice these athletes can happily use testosterone without doping hunters getting wind of it, thanks to ibuprofen and diclofenac.

"These results warrant further studies in order to assess the inhibitory potential that these and other NSAIDs may have on testosterone glucuronidation in vivo, as well as in other drug–drug, drug–xenobiotics and drug–endobiotics interactions", the researchers write. "Such studies are on-going at our laboratory in healthy volunteers."

If you’re thinking about experimenting with a combination of synthetic testosterone and ibuprofen or diclofenac, read first the article published by researchers at Kingston University in 2010. They suspect that this combination can cause kidney damage in people who don't have the UGT2B17 enzyme. [Subst Abuse Treat Prev Policy. 2010 Apr 29; 5:7.]

Source:
Steroids. 2009 Nov;74(12):971-7.

More:
Ibuprofen helps immune cells build up muscle tissue 09.08.2010
'Right' gene lets you inject testosterone without getting caught by doping test 25.04.2009
Ibuprofen and acetaminophen are anabolic for seventy year olds 24.08.2008