The Facts About Ephedra and Ephedrine

For over 2000 years an "innocuous" green herb, known as Ma-Huang, has been used by physicians in the Far East to treat a variety of ailments.  They range from the discomforts of a common cold to congestive heart failure.  

Experts in the field of Traditional Chinese Medicine such as Yong Ping Jiang, Chair of the Dept. of Oriental Medicine of Minnesota College, have attempted to enlighten the lay person as to the proposed capabilities (which includes fat loss) of this ancient herb [1].

As you may have guessed, Ma-Huang and ephedra is one and the same thing.  And while it may have been a staple of Chinese Medicine for centuries, it hasn't been embraced by all here in the West.

In 2004 the Federal Drug Administration (FDA) banned ephedra and ephedra containing supplements; although many over-the-counter medicines containing ephedrine and pseudoephedrine (two stimulating compounds found in the ephedra herb) escaped the ban.

While the ban was over ruled just a year later, it has since been upheld and the current stance of the FDA is that consumers should not take ephedra (the herb) or ephedrine (the synthetic version) in any dose as a supplement.  

It is also banned by many athletic governing bodies. 

But despite its controversy, anecdotal reports claim that it is a powerful and effective fat loss aid.  Let's see whether there's any scientific research to bolster those claims.


What Is Ephedra Used for?

Ephedra sinica, ephedra intermedia, and ephedra equisentina are the main species of ephedra.

Ephedrine, pseudoephedrine, norephedrine, and norpseudoephedrine are the compounds, or alkaloids, derived from the stem of the ephedra sinica (the most potent of them being ephedrine). 

The versatility of ephedrine includes an ability to stimulate the central nervous system, relax and dilate respiratory pathways [3], cause thermogenesis [4], vasoconstriction, as well as control the activity of the hypothalamus. Its properties have been recognised by the pharmaceutical industry and it has been used to develop a range of products from nasal decongestants to asthma inhalers.

Ephedrine has been used illicitly as a stimulant, like caffeine,  prior to physical activity and to improve concentration for studying and exams.

Ephedrine can be used to make methylamphetamine (a class-A drug in the UK) by chemical reduction, which has made it a highly sought-after chemical precursor within the illegal drugs trade [2].

Of course, the use that has sparked most interest in the supplement industry is that of fat loss...


Ephedra and Fat Loss

A number of controlled studies have looked into the effect of ephedra and ephedrine on weight loss.  Very often ephedra is combined with caffeine and sometimes aspirin, which is thought to have a more potent effect.

One recent, short-term study found that those taking an ephedra/caffeine supplement lost about 1kg per month (over 6 months) more than a group taking a placebo.  The dosage was 90mg of ephedra and 192mg of caffeine per day, which lead to no adverse side effects [3].

An older study compared four groups of obese people [4] - one taking just caffeine (200mg 3xday), one taking just ephedrine (20mg 3xday), one taking both ephedrine and caffeine together (20/200mg 3xday) and one taking a placebo.  

The group taking both ephedrine and caffeine together lost the most weight over approximately 6-months.  However, all groups lost similar amounts of weight as they were on a calorie controlled diet, and in fact the placebo group lost more weight than the ephedrine group alone.  It's important to note that the ephedrine-caffeine group reported negative side effects including vertigo and an increased heart rate.

An ephedrine-caffeine combination seems to work by increasing the metabolic rate [5,6] and by also suppressing appetite (as measured by a natural reduction in calorie consumption [7].  What's more interesting is that the combination may also help to preserve muscle mass so that a large percentage of weight loss is in the form of fat [8]. 

You may have heard of the fat loss pill called Xenadrine.  The original version of Xenadrine (called Xenadrine RFA-1) has now been discontinued.  It contained both ephedrine, derived directly from Mu Huang, and caffeine.  

A study measuring the effect of 2 daily servings of Xenadrine RFA-1 (total of 40mg ephedrine/200mg caffeine) found that they lost more fat and less muscle than the placebo group.  Both groups followed the same diet and exercise programme designed to help weight loss [9].

A similar study reported similar results with the Xenadrine RFA-1 group losing more fat and gaining more muscle.  Although the difference was statistically significant, it's important to put it into context - the Xenadrine RFA-1 group lost less than 6 pounds of fat over 6 weeks [10].

Other studies have also shown that ephedrine, and ephedrine plus caffeine in combination, can help to increase the rate and amount of fat loss while preserving muscle [11,12]. 


Performance Enhancement

A 1999 study examined whether a combination of 375mg of caffeine 75mg of ephedrine could improve performance in a 3.3km running test (carrying weighted gear) carried out by Forces personnel in Canada.  On average the recruits completed the test almost 1 minute faster following the caffeine and ephedrine stack [16].

In an maximal test lasting for a similar amount of time, subjects taking both caffeine and ephedra lasted nearly 5 minutes longer before exhaustion (taking caffeine of ephedra alone led to an increase of around 2 minutes before exhaustion) [17]. 

When exercise duration was longer (10km run carrying 11kg of gear) ephedrine reduced time to completion slightly [18].

Ephedrine and caffeine taken prior to a resistance training session can also boost performance [19].  In this study, systolic blood pressure was significantly raised with ephedrine consumption.


Ephedra Safety

An analysis of 140 reports of serious events attributed to ephedra and ephedrine was completed Haller and colleagues.  In total, 31% of those reports were considered highly likely to be caused by taking ephedra alkaloids.  31% of the cases were deemed to be "possibly related" [13]. 

Adding caffeine to ephedra seems to increase the likelihood of adverse effects.  Caffeine alone can raise systolic blood pressure [14] and ephedrine alone can raise heart rate [15].  Unsurprisingly, taken together they can raise both heart rate and systolic blood pressure [14].

It appears that ephedrine is less likely to cause negative side effects compared to the ephedra herb in it's natural state.  Ephedra, or Ma Huang varies greatly in potency depending on how and where it is grown and contains other compounds extracted during the synthesis of ephedrine.  The fact that ephedrine is used in clinical trials and that subjects are health-screened prior to participation may be why there are fewer adverse events in the literature.

You should bear in mind that in many of the trials that show the positive effects of ephedra, some of the subjects complained of, and even dropped out due to, side effects.  Many doctors fear that taking ephedrine or ephedra without medical supervision can lead to serious cardiac events in people who may have heart disease without knowing it.   


Summary

Ephedra and ephedrine do seem to have a definite effect of weight loss.  Moreover, it seems to achieve the elusive goal of fat loss while retaining muscle mass.

However, the extent to which it works is much less than is often portrayed in the media and anecdotally. And, as with any supplement or drug, nothing comes close to the potency of proper diet and exercise. 

It also seems to enhance certain athletic activities and has been banned by many sports governing bodies.

There are reports, both anecdotally and in the literature of negative side effects, although these may be less severe when ephedrine is used instead of ephedra and when taken under close supervision.  Even so, the potential for serious harm has lead several countries to ban its use as a supplement. 

If you really want to take a supplement to give your exercise and diet programme a boost (albeit a small one), caffeine alone has research to back it and is undoubtedly safer when used correctly.  

References

1. Yong Ping Jiang, DOM, PhD http://www.ephedra.nu/medicine_6.html

2. http://en.wikipedia.org/wiki/Ephedrine.  Accessed 15th Dec. 2007. 

3. Boozer C, Daly P, Homel P, Solomon J, Blanchard D, Nasser J, Strauss R, Meredith T (2002). "Herbal ephedra/caffeine for weight loss: a 6-month randomized safety and efficacy trial". Int J Obes Relat Metab Disord 26 (5): 593-604.

4. Toubro, S., Astrup, A.V., Breum, L., & Quaade, F. (1993). Safety and efficacy of long-term treatment with ephedrine, caffeine and an ephedrine/caffeine mixture. International Journal of Obesity, 17, S69-72

5.Rosenbaum, M., Hirsch, J., & Leibel, R.L. (2000). Effects of changes in body weight on carbohydrate metabolism, catecholamine excretion, and thyroid function. American Journal of Clinical Nutrition, 71 , 1421-1432

6. Astrup, A., Breum, L., & Toubro, S. (1995). Pharmacological and clinical studies of ephedrine and other thermogenic agonists. Obesity Research,  3, S537-S540

7. Dulloo, A.G., & Miller, D.S. (1987). Reversal of obesity in the genetically obese fa/fa Zucker rate with an ephedrine/methylxanthines thermogenic mixture. Journal of Nutrition, 117, 383-389

8. Astrup, A., Buemann, B., Christensen, N.J., Toubro, S., Thorbek, G., Victor, O.J., & Quaade, F. (1992). The effect of ephedrine/caffeine mixture on energy expenditure and body composition in obese women. Metabolism, 41, 686-688

9. Kalman, D.S., Colker, C.M., Shi, Q., & Swain, M.A. (2000). Effects of a weight-loss aid in healthy overweight adults: Double-blind, placebo-controlled clinical trial. Current Therapeutic Research, 61, 199-205

10. Armstrong, W.J., Johnson, P., & Duhme, S. (2001). The effect of commercial thermogenic weight loss supplement on body composition and energy expenditure in obese adults. Journal of Exercise Physiology, 4, 28-34

11. Greenway, F.L., De Jonge, L., Blanchard, D., Frisard, M., & Smith, S.R. (2004). Effect of a dietary herbal supplement containing caffeine and ephedra on weight, metabolic rate, and body composition. Obesity Research, 12, 1152-1157

12. Boozer, C.N., Nasser, J.A., Heymsfield, S.B., Wang, V., Chen, G., & Solomonm, J.L. (2001). An herbal supplement containing Ma Huang-Guarana for weight loss: a randomized, double blind trial. International Journal of Obesity, 25,-324

13. Haller, C.A., & Benowitz, N.L.. (2000). Adverse cardiovascular and central nervous system events associated with dietary supplements containing ephedra alkaloids. New England Journal of Medicine, 343, 1833-1838

14. Haller, C.A., Jacob, P., & Benowitz, N.L. (2004). Enhanced stimulant and metabolic effects of combined ephedrine and caffeine. Clinical Pharmacology and Therapeutics, 75, 259-273

15. Drew, C.D., Knight, G.T., Hughes, D.T., Bush, M. (1978). Comparison of the effects of D-(-)-ephedrine and L-(+)-pseudoephedrine on the cardiovascular and respiratory systems in man. British Journal of Clinical Pharmacology, 6, 221-225

16. Bell, D.G., & Jacobs, I. (1999). Combined caffeine and ephedrine ingestion improves run times of Canadian Forces Warrior Test. Aviation, Space and Environmental Medicine, 70, 325-329

17. Bell, D.G., Jacobs, I., & Zamecnik, J. (1998). Effects of caffeine, ephedrine and their combination on time to exhaustion during high-intensity exercise. European Journal of Applied Physiology and Occupational Physiology, 77, 427-433

18. Bell, D.G., McLellan, T.M., & Sabiston, C.M. (2002). Effect of ingesting caffeine and ephedrine on 10-km run performance. Medicine and Science in Sports and Exercise, 34, 344-349

19. Jacobs, I., Pasternak, H., & Bell, D.G. (2003). Effects of ephedrine, caffeine, and their combination on muscular endurance. Medicine and Science in Sports and Exercise, 35, 987-994