Saturday, December 1, 2012

Amphetamines Are Performance Enhancing Drugs

Millard Baker made a very perspective comment concerning the peloton of the eighties, they allegedly were not too focused on enhancing oxygen transport to the mitochondria, or increasing the levels of red blood cells which also transport oxygen, or beating the drug testers with forty-nine point nine percent hematocrit levels, or enhancing their performance with human growth hormones. However, the transition was in process with blood doping pioneer Francesco Conconi, who was accused of providing human growth hormones and doped blood to the Italian Olympic Team as far back as 1980.

There is confusion as to the advent of the blood dopers, but it is certain that in 1984 Francesco Moser, aided by Francesco Conconi and his star student Michele Ferrari, blood doped to break Eddy Merckx's 1972 one hour world record ride.  Of course, Francesco Moser also built an unconventional bicycle equipped with moon disc wheels, which improved aerodynamic properties that were considered an unfair advantage over the conventional safety bicycle design.  The UCI finally determined that these aerodynamics could not be allowed, and Moser's record was subsequently rescinded.  Naturally, this reminds one of the 1989 Tour de France final time trial, Versailles to Paris, where Greg LeMond used questionable aerodynamic additions that were not only allowed but probably proved to be decisive.  Of course, Laurent Fignon had a decisive aerodynamic disadvantage with his ponytail flapping in the wind.

But for the accomplished rouleur, a cyclist who has all the requisite talents of time trialist, sprinter, climber, ace lieutenant; the man or woman who chases down the breaks, sets the tempo, eats wind, protects the team leader; there probably was not much investment into the newly evolving unconventional methods of cheating.  Most of the small fry probably relied upon the old conventional methods of amphetamine or cocaine abuse which had been in practice since the days of Maurice Garin.  But, there is no need to plead ignorance to the fact that team doctors knew that increases in oxygen transport from autologous blood transfusions increased performance in long term endurance sports or the fact that cycling teams were using blood transfusions to gain an unfair competitive advantage.  After all, Jacques Anquetil understood that the Tour de France can't be won on mineral water alone.  There must be additions, sympathomimetic amines, for example.  In 1967 Jacques Anquetil broke his own world record ride but he refused to submit to the newly instituted doping testing.  From Wikipedia:

In 1967, 11 years later, Anquetil again broke the hour record, at 47.493 km, but the record was disallowed because he refused to take the newly-introduced post-race doping test.[8] He objected to what he saw as the indignity of having to urinate in a tent in front of a crowded velodrome and said he would take the test later at his hotel. The international judge ruled against the idea and a scuffle ensued that involved Anquetil's manager, Raphaël Géminiani.

Cycling reported:[9]
Wonderful Jacques Anquetil has broken the world hour record as he said he would... and then ran into official trouble when he refused to take a trackside dope test demanded by the Italian authorities. An Italian Dr. Giuliano Marena asked for the urine sample, but Anquetil refused and asked him to come to his hotel. Dr. Marena refused and, after waiting a couple of hours at the track, left town to go home to Florence. Anquetil said at his hotel: 'I didn't and don't intend to escape the test, but it must take place under circumstances far different from those at the velodrome. I'm still here and ready to undergo the test.' While Italian officials talked of taking the matter to the UCI, Dr. Tanguy of the FFC [French cycling federation] took a sample from Anquetil on his return to Rouen, pointing out afterward that it would be valid up to 48 hours after the record attempt. But Raphaël Géminiani, his manager, had all but lost his temper with the Italian medical man and had tried to throw him out of the cabin, though Jacques had remonstrated mildly. Later he said that he understood the tests would be valid for up to 48 hours and said he was trying to locate another doctor for the test.[9]

Wonderful are these examples of cheaters who refuse to submit to dope tests after setting inhuman athletic records.  Remember, that the man who laughed at mineral water as an acceptable supplement won five Tour de France titles; none of which have been deleted from the record books.

But no matter.  These diversionary tales of yore, the cocaine users, and amphetamine abusers, would be considered cheaters by any rational definition, but do we live in a rational world?  Apparently not.  There seems to have emerged into the discussion a dispute over what class of drugs constitutes performance-enhancing drugs. For example, I heard a raging debate on a nationally syndicated sports talk show the other day where the host insisted that Dexedrine was not a performance-enhancing drug, and when the caller insisted that amphetamines were performance-enhancing drugs, the host called the caller an idiot.  There is some debate as to the action of amphetamines but it is clear that amphetamines increase the levels of catecholamines in the brain and thus could be considered a performance-enhancing drug.  From drugs.com:

Mechanism of action/Effect:

Amphetamines are sympathomimetic amines {12} {13} {14} {15} that increase motor activity and mental alertness {14}, and diminish drowsiness and a sense of fatigue {14}.

In attention-deficit hyperactivity disorder, amphetamines decrease motor restlessness and enhance the ability to pay attention.

The exact mechanism of action has not been established. However, in animals, amphetamines facilitate the action of dopamine and norepinephrine by blocking reuptake from the synapse, inhibit the action of monoamine oxidase (MAO), and facilitate the release of catecholamines. An increase in locomotor activity at relatively low doses and an increase in stereotypic behavior with a concomitant decrease in activity at higher doses appear to be due to stimulation of mesocorticolimbic and nigrostriatal dopaminergic pathways. Dextroamphetamine may also stimulate inhibitory autoreceptors in the substantia nigra and ventral tegmentum. {01}

Some studies support the theory that amphetamine exerts a dual effect on the striatal dopaminergic nerve terminal, thus explaining the paradoxical effects of amphetamines. Amphetamines may selectively facilitate the dopaminergic transmission by promoting the release of recently synthesized dopamine from a reserpine-resistant pool and, in addition, may inhibit the classical dopaminergic neurotransmission involving the calcium-dependent depolarization-evoked release of dopamine from reserpine-sensitive storage sites. {02}

Cocaine increases the neurotransmitter dopamine in the synaptic cleft through autoreceptor blockade, but this is only one method of reuptake inhibition.  Autoreceptors act as a feedback loop; the presynaptic neuron is attempting through this feedback loop to maintain synaptic neurotransmitter homeostasis.  Once the feedback is disrupted through the autoreceptor blockade, the presynaptic neuron increases the quantity of dopamine in the synaptic cleft through depletion of storage granules, which generates long term depolarization in the postsynaptic neuron.  Long term potentiation of postsynaptic neurons that are catecholamine-dependent has been demonstrated to enhance performance.  It has been postulated that the central nervous system neurotransmitter norepinephrine regulates drive, and that dopamine regulates reinforcement of behavior.  Amphetamines are stereoisomers designated [+] dextro and [-] levorotatory.  "Dexedrine (dextroamphetamine sulfate) is the dextro-isomer of the compound d, l-amphetamine sulfate," having the longest half-life, and the most potent longest lasting effects.  "Adderall (amphetamine-dextroamphetamine mixed salts) tablets contain d-amphetamine and l-amphetamine salts in the ratio of 3:1," which would reduce the potency of the drug, and theoretically the performance-enhancing effects.  However, there is a caveat to this logic, hyperarousal has a tendency to decrease performance both physically and cognitively.

Of course, if the drugs are not modern: Adderall, Provigil, or Ritalin, and they were not abused by the legends, Jacques Anquetil or Eddy Merckx in cycling, or Babe Ruth in baseball, as the nationally syndicated radio show host claimed; then they have no performance-enhancing benefits.  No matter that amphetamines and similar central nervous system stimulants were the most abused drugs in cycling and baseball during the sixties, seventies, and eighties.

But even the legends used performance-enhancing drugs, Eddy Merckx tested positive for fencamfamin a central nervous system stimulant during the 1969 Giro d' Italia and was given the boot.

Here is another example.  Though the exchange between cycling legends Gino Bartali and Fausto Coppi is hilarious, the discussion does reveal the acceptance of amphetamine use at the time.  Quoting: Seven Deadly Sins, David Walsh, Atria Books, 2012.

Gino Bartali: "Do cyclists take the la bomba [amphetamine]?"
Fausto Coppi: "Yes, and those who claim otherwise, it's not worth talking to them about cycling."
Gino Bartali: "And you, did you take la bomba?"
Fausto Coppi: "Yes, whenever it was necessary."
Gino Bartali: "And when was it necessary?"
Fausto Coppi: "Almost all the time!" P.59

Then, of course, there was British rider Tommy Simpson, who sadly died on the moonscape of Mont Ventoux during the 1967 Tour de France, so high on amphetamines that he did not know he had ridden beyond his physical capacity.  Tommy Simpson collapsed just a few kilometers from the summit of Mont Ventoux, his jersey pockets were full of amphetamine tablets, more amphetamines were found in his luggage at his hotel.

So come on.  Do your homework before you shoot your mouth next time.  Amphetamines are performance-enhancing drugs and that is why they are on the prohibited list.

Warning: Too much amphetamine arousal can have counterproductive adverse effects that will diminish performance in both cognitive, and physical areas, and chronic abuse will produce a syndrome that exactly mimics paranoid schizophrenia.

1 comment:

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