Heptaminol? Where do they even find this stuff

Carlos Sastre won the Tour de France yesterday, but the whole race has been marred by incidents of sports doping. First, Riccardo Ricco was caught using a form of Epo called CERA. Now another biker named Dmitriy Fofonov tested positive for a drug called heptaminol.

Heptaminol made me raise an eyebrow, primarily because I had never heard of it before. I am beginning to wonder where these bikers even find this stuff. I kid you not: it took me a while to even find information on it. Most drug databases I checked don't even have an entry for it.

It is on the list of WADA prohibited substances. Here is a summary on it (from here):

Heptaminol. This is a cardiac stimulant with predominantly positive inotropic actions (Berthiau et al., 1989), and also has a pressor effect in cats (Grobecker and Grobecker, 1976). It has been used to treat low blood pressure and orthostatic hypotension (Boismare and Boquet, 1975), with reported 'unexpected' adverse effects (Pathak et al., 2005). Its actions may involve NA [noradrenaline] release by action at the transporter (Grobecker and Grobecker, 1976; Delicado et al., 1990), but it may also have effects on Ca2+ channels to increase intracellular calcium (Peineau et al., 1992). (Links in original.)

Orthostatic hypertension is when you get low blood pressure when you stand up -- sometimes leading to fainting. It has several causes including autonomic failure (when your nervous system does not respond to changes in blood pressure by constricting blood vessels) from neurodegenerative disease, peripheral neuropathy from diabetes, or from heart output problems like congestive heart failure. Anyway, I sincerely doubt that Fofonov has any of those if he is participating in the Tour de France.

Presumably Fofonov took it as an upper, but I'm skeptical it would have been effective at improving performance. It may have raised his blood pressure through increasing sympathetic tone, but like 6 other things regulate blood pressures and I am not certain that there is a direct relationship between blood pressure and performance. At high enough doses it could cause tachycardia -- which might improve performance by increasing heart output -- but it also might cause atrial fibrillation -- which definitely would hurt performance. (A summary of adverse drug reactions here.) Also, I don't get the sense that heptaminol has many CNS actions, so I don't how it would provide a mental edge.

So here is my question: are these bikers taking anything they can get their hands on without regard to whether the drug is effective at improving performance? If we are going to take anything, why not DayQuil? (Phenylephrine is incidentally not on the list of prohibited substances.) Why not NoDoze? (Caffeine is also not on the list.) I doubt those would work either, but hey as long as we are trying...

That is certainly the sense I am getting. I mean, I get it when they take Epo. I think they should know that they will eventually be caught, but at least Epo is probably effective. I just don't understand why they would gamble with their career using a drug that might not even work.

What shocks me about people who indulge in sports doping is not that they would dare. It is that they seem to be going about it in a shockingly stupid way -- ignoring both the methods of testing and the likely actions of the drug.

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"So here is my question: are these bikers taking anything they can get their hands on without regard to whether the drug is effective at improving performance?"

The answer to do that would be: "Yes." Like most professional athletes, cyclists leave school at an early age to become full time professionals. Add to that that there is relative little money in professional cycling and that a few good results can easily lead to that better contract. So cyclists are an easy prey for whatever miracle cure shady quacks try to sell them.

"What shocks me about people who indulge in sports doping is not that they would dare. It is that they seem to be going about it in a shockingly stupid way -- ignoring both the methods of testing and the likely actions of the drug."

That's what gets me as well. But everyone thinks they can beat the system.

I imagine that the market for dopants has certain features that encourage dubious experimentation as well. If a drug is popular enough, long enough, the odds are that they'll cook up and use a test for it, making it less safe to use.
Add to that the fact that all this is underground(not necessarily too far under; but still) so evaluation of effectiveness is going to end up being a matter of N=1 study populations, rumor, and whatnot, with the only firm data being the stuff filtering in from studies of these compounds in therapeutic contexts(which, while very helpful, are incomplete for athletic purposes).

It is probably not too much unlike the market for recreational drugs. There are some staples, which are known to work; but quite easy to test for, and an impressive, if often scientifically misguided, proliferation of weird stuff around the edges, driven by the constant demand for things to get high on that haven't been banned yet. The number of crazy things that've popped up under the "designer drug" label suggests that this type of regulatory pressure creates very strong tendencies to diversify.

This might be a silly question: why, if no advantage can be gained from taking the drug, is it on the WADA-list?

A lot of times bikers, athletes and others will use masking agents to hide other drugs. Sometimes these "dummy drugs" will have a longer life cycle than the stimulating reactant. It's all about timing, and for Fofonov he simply didn't get it right - for better or worse.

It seems that the sport of biking itself will never get rid of this craze on drugs until there is a more realistic view of what the Tour is. People are always trying to better a time, improve upon last year, etc - when in fact, there is no way you can compare since the race is so variable.

My 0.02.

H.G.G.

No, not orthostatic hypertension....orthostatic hypotension

By tjcantwell (not verified) on 25 Aug 2008 #permalink