By JERRY BRAINUM Iron Man Magazine
Overview of papers related to sports and bodybuilding pharmacology presented at the conference.
A few interesting papers were presented at the 2011 meeting of the American College of Sports Medicine. Here is an overview of those related to sports and bodybuilding pharmacology that were presented at the conference.
Does DHEA really work?
Dehydroepiandrosterone is an adrenal steroid hormone that circulates in the blood in higher concentrations than any other steroid hormone. Its precise function is still a matter of debate, but most researchers agree that it’s a precursor substance of other steroid hormones in the body. As such, enzymes are able to convert DHEA into estrogen and testosterone. Numerous published studies have shown that it also exerts considerable health benefits, including better immune response and the ability to fight excess cortisol. Older people who have higher DHEA levels are also more vigorous and youthful, an effect attributed to the higher levels of insulinlike growth factor 1 that are linked to normal DHEA levels. With age, DHEA drops, and some have suggested that supplementing with DHEA can have a fountain-of-youth effect in those over age 40.
So far, however, studies have shown more beneficial effects of DHEA in animals than humans. One reason is that the animals tested either don’t produce DHEA or produce only small amounts. So, when you give them DHEA, you get a pronounced effect. For example, DHEA provides potent fat-loss effects in most rodents. In humans the effect has proved disappointing, although one study did show a loss of abdominal and deep, visceral abdominal fat in older people who had been deficient in DHEA. From a bodybuilding perspective, DHEA is of interest because of its capacity for being converted into testosterone.
Even so, several studies have shown that DHEA is more reliably converted into testosterone in women than in men. In women’s bodies a lot of the androgens produced are the result of DHEA conversion into testosterone, and women also produce only about a tenth as much testosterone as men. In men the studies have shown that DHEA more often is converted into a metabolite of testosterone called dihydrotesterone, or DHT, which is itself a by-product of testosterone metabolism. The enzyme 5-alpha reductase converts testosterone into DHT, which can be problematic since it’s associated with male pattern baldness, acne and prostate enlargement.
It would appear that DHEA is useless for bodybuilding purposes, except perhaps for women who want to boost their testosterone a bit. Still, a study presented at the 2011 ACSM conference casts new light on the effects of DHEA in men who lift weights. Eight young adults and eight middle-aged adults received either a 50-milligram dose of DHEA or a placebo 12 hours before a bout of high-intensity exercise. Unfortunately, the researchers didn’t disclose the sex of the subjects, so we don’t know how many were men and how many were women, which, obviously, might have affected the outcome of the study.
In any case, the subjects engaged in intermittent cycling at 100 percent of their maximum oxygen intakes, an intensity comparable to high-intensity weight training. The researchers collected blood samples before exercise and at five and 15 minutes after exercise. The hormones observed included DHEA-S, the circulating form of DHEA; cortisol; testosterone; free, or active, testosterone; and lutenizing hormone.
As expected, DHEA significantly boosted DHEA-S in both the young and middle-aged subjects. Total testosterone wasn’t affected, but free testosterone went up after exercise in the younger group. The authors explained that testosterone may have been exhausted by the intense exercise in the younger group, and the body wasn’t able to produce any to replace it. Given DHEA, however, the body rapidly converted it into free testosterone, which implies that taking DHEA before intense training may provide an enhanced active testosterone boost. There was no discussion of why the DHEA didn’t affect the middle-aged subjects. Since the sampling was small, it needs to be replicated, perhaps using a free-weight protocol, before we can authoritatively state that DHEA may increase free testosterone during intense training.
Geranium Effects on Blood Pressure
Many current sports supplements touted to boost performance and fat loss include an ingredient called 1,3 dimethylamylamine, which is said to come from the oils of geranium, a plant. It’s often combined with caffeine, a mix that’s thought to be a potent stimulator. As such, “geranamine,” as it’s called, is quite popular for use in preworkout supplements. Some so-called experts have gone on record saying that geranamine is comparable in structure to ephedrine, an incorrect assertion. Ephedrine also has stimulant and fat-mobilizing effects, but it was removed from the market several years ago because of unfounded concerns that its use could lead to strokes or heart attacks.
Ephedrine worked by promoting the release of epinephrine and norepinephrine, collectively known as the catecholamines. Among their properties was the ability to set off a cascade in fat cells that leads to the release of fat from the cells; however, the catecholamines are also known as the “fight or flight” hormones and are released in abundance during high-stress conditions. When they are released, they tend to cause a constriction of blood vessels that leads to a rise in blood pressure. For those not already afflicted with high blood pressure or heart disease, the temporary rise in blood pressure induced by ephedrine was harmless. After all, blood pressure also rises temporarily when you lift heavy weights. Even so, ephedrine was contraindicated for those with existing high blood pressure or heart disease—but many ignored the warning in their quest to lose bodyfat or get a shot of energy for an impending workout. Even worse, some people thought that since ephedrine was sold over the counter, it must be innocuous, and they increased the recommended dosage considerably.
As the old pharmaceutical dictum states, “Only the dose determines the poison,” so people suffered such serious side effects as heart attacks and strokes. No one who was healthy—without a preexisting condition—or who did not overdose got any side effects other than perhaps minor muscle tremor or insomnia, if they took the supplement at night. Still, the Food and Drug Administration felt that people could not be trusted to protect themselves, and it removed ephedrine from market sales. The fact that a few studies had shown that ephedrine and caffeine were superior at producing weight loss than existing drugs for that purpose also likely played a role in the FDA action. The agency’s charter declares that a primary goal is to protect the profits of the pharmaceutical industry.
Ever since the removal of ephedrine, companies have scampered looking for a suitable alternative. One of the more recent such alternatives is geranamine, but you have to wonder, Just how safe is it? As I’ve pointed out in the past, many supplements touted to contain geranamine actually contain a discarded old drug that was known to boost blood pressure. The object of a study presented at the ACSM meeting was to see if the current geranamine supplements, especially when combined with caffeine, would affect blood pressure. Ten young adults took one of the following combinations in a fasted state on different days:
1) 250 milligrams of caffeine
2) 50 milligrams of geranamine
3) 75 milligrams of geranamine
4) 250 milligrams of caffeine and 50 milligrams of geranamine
5) 250 milligrams of caffeine and 75 milligrams of geranamine
The researchers took measurements of heart rate and systolic and diastolic blood pressure, as well as another measure of blood pressure called rate pressure product, or RPP, before the subjects got any of the supplements and at 30, 60, 90 and 120 minutes afterward. They also measured plasma epinephrine and norepinephrine at an hour and two hours after ingestion.
The results showed that heart rate wasn’t affected by either caffeine alone or any combination of caffeine and geranamine. But blood pressure and RPP were higher, depending on the dosage. Specifically, systolic blood pressure rose by 20 percent and diastolic blood pressure went up 17 percent, along with a 9 percent increase in RPP, with the combination of 250 milligrams of caffeine and 75 milligrams of geranamine an hour after the subjects took it. The catecholamines, epinephrine and norepinephrine, were not affected. What’s interesting about this is that unlike ephedrine, the catecholamines were not involved in the rise in blood pressure. Nor was the heart rate affected. So what did cause blood pressure to go up with the greatest dose? That remains for future research to determine.