Taming Thermogenesis for Weight Loss
by Dallas Clouatre, Ph.D.
 As most dieters have discovered through sad experience, just cutting back on the number of calories eaten is not the ticket to success. Usually the diet has not been underway for very long before energy levels plummet and the desire for old, familiar foods gets the upper hand. What’s worse, after the diet ends, the weight can come roaring back. Thermogenic weight loss products are advertised on TV, in magazines and even at carts in local malls as the solution to these
problems. The majority of us are familiar with the claims: speed up your metabolism; increase your energy levels; keep the lean while burning the fat; and so forth and so on. Lots of products make these claims, but the ingredients list is usually very short. Ephedrine and caffeine are almost always at the heart of these thermogenic products.
Thermogenesis refers to the increase in the body’s production of energy as heat which is triggered by nutritional and biochemical means. One of the chief drawbacks of calorie-restricted diets is their tendency to lower the body’s rate of energy production. Those who are prone to obesity already tend to have lower basal metabolic rates (BMR) on a pound-for-pound basis than those who are thin, and obesity itself promotes a lowering of the BMR. There is also something called diet-induced thermogenesis. After eating, most normal weight individuals see a lasting rise in energy production amounting to approximately 10 percent of their prior metabolic rates. For reasons not well understood, the overweight, women in particular, do not experience this increase in heat
production. Correcting a “low metabolism” certainly looks like a panacea for dieters. The pertinent questions are whether this can be done and whether it can be done safely.
The Ephedrine Promise:
The Theory
Ephedrine products are everywhere. Currently popular are the “stacks” EC and ECA. (“Stacking” refers to using more than one active ingredient at a time.) EC stands for ephedrine and caffeine; ECA stands for ephedrine, caffeine and aspirin. All three of these ingredients can come from a variety
of different natural sources as well as from synthetic products. Many readers will recognize the Chinese herb Ma huang as the chief natural source of the ephedrine family of compounds, albeit there are other minor sources, such as Sida cordifolia. Herbal extracts supplying ephedrine alkaloids are fairly commonly “spiked” with synthetic pseudoephedrine. Ma huang itself contains one or more still unidentified compounds which extend the active life of ephedrine through a mechanism similar to that of
caffeine. Of course only a full-spectrum extract (usually standardized for six percent ephedrine alkaloids) will contain these other compounds.
Caffeine sources include guarana, maté and kola (cola) as well as the better-known coffee and black and green teas. Quite a number of studies have been conducted with the related compound known as theophylline. As for aspirin, this is the popular name for acetyl-salicylic acid. Willow bark is one natural source of salicin, a compound similar to aspirin. Its extracts are not nearly as concentrated as aspirin, and very few
thermogenic products which contain willow bark extracts contain enough to have any effect.
Ephedrine has been the subject of a great many studies, either alone or in combination with caffeine. Caffeine taken by itself does not have any special benefits for weight loss, yet it is quite significant in its ability to extend the effects of ephedrine. Aspirin and ephedrine in combination have also been tried and aspirin, like caffeine, extends the effects of ephedrine. Whether salicin from willow bark also supplies this benefit is hotly debated and apparently has not been properly tested. However, both aspirin and salicin have the further benefit of increasing the body’s internal “thermostat” so that the increased production of heat, which is typical of thermogenic products, does not set off alarms in the body.
What are the primary effects of ephedrine plus caffeine? Ephedrine-based combinations chiefly reduce appetite. For most
individuals, between 75 and 80 percent of the impact of taking an ephedrine and caffeine product will come from appetite suppression. However, at fairly high dosages ephedrine plus caffeine can cause a significant increase in the number of calories burned per day. In one test published just this year, 50 mg of ephedrine was given to volunteers three times per day. Under controlled conditions and using very precise monitors to measure energy expenditure it was found that 3.6 percent more energy was expended in a 24-hour
period when the subjects were taking the ephedrine. Several years ago a similar experiment was conducted in which 22 mg of ephedrine plus 30 mg caffeine and 50 mg theophylline three times per day was taken. This combination increased the number of calories burned by eight percent per day.
These results give an indication of the impact of caffeine in extending the life of ephedrine in the body. Moreover, an increased energy expenditure of eight percent per day, if it continued with chronic use, would amount to the loss of about 15 pounds per year.
Other benefits include correcting defects in diet-induced thermogenesis and helping to preserve lean tissue during dieting.
In one sense our bodies are a bit like car engines; we produce heat as a byproduct and the faster we run, the hotter we get. However, thermogenesis has a special meaning. It refers to a cycle involving a type of fat known as “brown fat” which only produces heat when activated by a particular receptor, the beta-3 adrenoreceptor. Current research shows that ephedrine has very little direct action upon beta-3 receptors. However, continued use of ephedrine over a period of months does appear to enhance brown-fat thermogenesis.
The Ephedrine Promise: The Evidence for Weight Loss
Ephedrine/caffeine combination and variations on this theme do work to increase weight loss beyond that found with dieting alone. For instance, in one two-month trial which tested the ECA stack versus placebo without a diet, those taking the ECA stack lost three times as much weight (4.8 pounds) as those taking the placebo (1.5 pounds). This study’s participants took 50 mg of caffeine and 110 mg of aspirin along with 25 mg of ephedrine three times per day for the first four weeks and 50 mg of ephedrine for the last four weeks of the trial.
Another study tested the effects of 20 mg of ephedrine and 200 mg of caffeine taken three times per day with a 1200 calorie diet as compared to the same diet and 15 mg of
D-fenfluramine taken twice per day. The subjects in this trial were 20 to 80 percent over their ideal weights. After 15 weeks the ephedrine + caffeine group had lost 18.3 pounds whereas the D-fenfluramine subjects had lost 15.2 pounds. This 20 percent greater weight loss was not statistically significant because of the size of the group being tested. Interestingly, in those subjects who were the most overweight (40 percent or more over their ideal weights), ephedrine + caffeine was statistically superior to D-fenfluramine in its weight loss benefits. In this group, those taking the EC stack lost 29 percent more weight (19.8 versus 15.4 pounds).
Oddly enough there have been no trials to directly test whether ephedrine + caffeine
+ aspirin actually works significantly better than just ephedrine + caffeine, the combination used in virtually all of the clinical trials. Similarly, insofar as the author is aware, no one has tested 10 mg ephedrine + 100 - 200 mg of caffeine taken before meals against 20 mg ephedrine + 200 mg of caffeine to see how great the difference in weight loss is under normal circumstances.
More is not necessarily better where ephedrine is concerned. In terms of increasing calories burned, in one test 10 mg of ephedrine by itself was more effective than
20 mg of ephedrine alone or 20 mg of ephedrine plus 100 mg of caffeine, and it was equal to 10 mg ephedrine plus 200 mg of
caffeine. The reason for this seemingly odd result is that increasing the level of ephedrine without adding caffeine also greatly increases the body’s feedback loop designed to deactivate the compound. Maximal effect in increasing the metabolism was found using
20 mg of ephedrine and 200 mg of caffeine.
Ephedrine: The Down Side
It should be understood that the traditional medical systems of neither China nor India, both of which have employed ephedrine sources for thousands of years, approve of the chronic consumption of large amounts of metabolic stimulants. In part this is because these products work by causing the release of elevated amounts of neurotransmitters. Unfortunately our nerve tissues are perhaps the most difficult of all tissues to regenerate. Doing things which lead to the generation of free
radicals in neurological tissues is not generally
a good idea. There may be no obvious declines in mental functioning in the short term, but what about 40 years from now?
Anyone taking ephedrine-based products should also take plenty of antioxidant compounds, as well. Similarly, in traditional herbal systems, strong stimulants are usually balanced with herbs which support the functions of the adrenal glands, for instance, licorice and dioscorea.
The warnings which accompany ephedrine products deserve to be read closely. Adverse effects from ephedrine use are common
experiences in some gyms and ephedrine
clearly is subject to habituation and to dependency. Chest pain in adolescents going to
emergency rooms is often ephedrine related. Those with hypertension, diabetes, thyroid disease, enlarged prostate and a number of other
conditions should consult a doctor before using any ephedrine-based product. Drug interactions may occur with monoamine oxidase inhibitors (MAO inhibitors) and clonidine, a drug used to treat hypertension. Caffeine and theophylline may pose special problems for those suffering from peptic ulcers. The addition of aspirin arguably makes this combination safer than it would be without the aspirin, but aspirin, of course, has its own down side, such as gastrointestinal discomfort and damage. Aspirin leads to a mild loss of blood in approximately 70 percent of users and can lead to
iron-deficiency anemia in some individuals. The loss of oxygen-carrying capacity by the blood is a factor which athletes should
consider as well.
The impact of ephedrine/caffeine products can be boosted in a number of ways which will not be discussed here. The problem with increasing the impact of the stimulants is that unwanted side effects increase at the same time. Likewise, greater stimulation may lead to faster habituation and to a quicker development of dependency.
Thermogenic Alternatives
Although few dieters realize it, there are good alternatives to the ephedrine/caffeine combination. These items often bring with them benefits not limited to thermogenesis and weight loss. Here are some items worth trying.
Green Tea
Already known as a powerful antioxidant, green tea extract can also help dieters to
burn off excess pounds. Dr. Abdul Dulloo of the Institute of Physiology at the University
of Fribourg in Switzerland maintains that the extract may be a safe improvement on traditional diet drugs because its benefits are “not accompanied by an increase in heart rate.”
In a study published in the December 1999 issue of the American Journal of Clinical Nutrition and reported widely by Reuters health news service, Dr. Dulloo and other investigators measured the 24-hour energy expenditure of 10 healthy men receiving three doses of caffeine (50 mg), green tea extract (containing 50 mg caffeine and 90 mg epigallocatechin) or a “dummy” placebo per day. Compared with placebo, treatment with green tea was associated with a “significant increase” (+ 4 percent) in daily energy expenditure.
This effect was not linked to the relatively small amounts of caffeine found in tea, since subjects receiving amounts of caffeine similar to those found in green tea displayed no change in daily energy output. Some researchers believe that the antioxidants found in green tea in the
form of catechin polyphenols somehow extend the active life of the body’s own fat-burning hormone noradrenaline. Whatever the mechanism involved, green tea, unlike ephedrine, is apparently safe for overweight and obese
individuals who suffer from hypertension and other cardiovascular conditions.
Green tea is available in extract form, but it is worth a try as a substitute for other
caffeine-containing beverages. Try drinking a couple of cups of green tea with each meal. Green tea’s major health benefits, such as
protection against some forms of cancer, appear with the consumption of three to five cups per day. However, dieters should bear
in mind that this form of tea still contains
caffeine and they should limit other sources of caffeine accordingly.
Thermogenic Spices
As indicated above, a metabolic dysfunction which is common in the overweight is the failure to experience diet-induced thermogenesis (DIT). This mealtime increase in metabolism is responsible for burning a significant number
of calories each day. Just as importantly, the overweight often suffer from poor digestion and poor digestion itself may encourage weight gain by water retention due to an increase in low-level chronic immune response to partially-digested proteins. Fortunately both the below par DIT and the poor digestion can be dealt with at the same time. In one study performed in England, adding one teaspoon of hot pepper sauce and one teaspoon of hot mustard to each meal was found to raise subjects’ metabolic rate by as much as 25 percent.
Thyroid Support
Bouts of dieting can cause the function of
thyroid to decrease, and this in turn will lead to an increase in weight. However, there are ways to improve thyroid output and the activity of the thyroid hormone. Both the Indian herb known as guggul and special phosphate salts have been used for just this purpose. One clinically-tested patented combination of these and other ingredients is already on the market.
Coenzyme Q-10
As I pointed out several years ago in my book Anti-Fat Nutrients, about one-half of those who are overweight do not seem to have adequate amounts of the antioxidant and energy nutrient CoQ-10 available in their systems. For the 50 percent of the overweight to whom this fact applies, supplementing with CoQ-10 will improve weight loss. The typical dosage for this purpose is 100 to 150 mg per day.
5-HTP
5-Hydroxytryptophan (5-HTP) is a building block for the neurotransmitter serotonin, which helps to regulate the body’s satiety
signals. Clinical experiments performed in Europe have confirmed that 5-HTP can help to reduce appetite and thus improve weight loss. Try 50 to 200 mg three times per day before meals and use the lowest dose which seems to help after a week’s trial. The 5-HTP can be combined with L-tyrosine, 100 to 250 mg three times per day, to support thyroid function and the production of other brain neurotransmitters. Again, start with the lowest dose of L-tyrosine and be prepared to cut back the dosage. Some individuals find that this amino acid can cause headaches and increase their blood pressure.
Blood Sugar Control
The regulation of blood sugar levels and insulin response are important components in any supplement plan intended to help with dieting. Dieters should consider taking a good multi-mineral supplement to support blood sugar control. This supplement should include chromium (600 mcg per day if regulation is a major issue), magnesium, manganese and zinc. In truth, mineral supplementation is not a bad idea for the rest of us who do not want to gain extra weight in the first place.
Conclusion
Although there is no doubt that ephedrine/
caffeine-based products can be used successfully to aid in weight loss, dieters should keep firmly in mind that there is a very real down side to
the use of such stimulants. Those with diabetes and cardiovascular issues should be especially cautious.
Even in otherwise healthy individuals the risks of becoming somewhat dependent
upon such products are evident. However, ephedrine/caffeine-based products are not the only options for achieving thermogenesis and, in general, increasing one’s metabolism. Other options exist which may lack the “kick-in-the-seat-of-the-pants” wallop of the ephedrine and caffeine combination yet which do work, nevertheless, and work safely. These solutions may turn out to be more
successful in the long term than is the quick fix of ephedrine/caffeine.
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