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Although banned by the NFL, NCAA and International Olympic Committee, dietary supplements containing ephedrine are still consumed by athletes and the general public, often in the hopes that it will aid weight loss or provide a stimulant-induced performance edge. To find out the latest on this common dietary supplement, we asked Ellen Coleman, RD, MA, MPH, a nutrition consultant for the Los Angeles Lakers and Anaheim Angels, to research the most current findings regarding this drug.
We hope you find this information useful.
Bob Murray, PhD, FACSM
Director, Gatorade Sports Science Institute
Ephedrine-Containing Supplements
April, 2003
Ellen Coleman, RD, MA, MPH
In many competitions, the difference between winning and losing can occur in one play or the divisions of seconds. So it is not surprising that athletes may want to utilize ephedrine-containing supplements to improve their performance, have more energy or decrease their body fat. Unfortunately, athletes who use ephedrine may risk getting more than they bargained for from the drug. While it may help them run farther and faster, it can also make them prey to the myriad of negative—even potentially life-threatening—side effects. The fact is ephedrine use is controversial at best. Especially when you consider that the NFL, NCAA and International Olympic Committee have all taken steps to keep it off the playing fields. And now, the FDA is getting into the discussion.
What is Ephedrine
So what exactly is ephedrine? Classified as a sympathomimetic drug (a beta-1 and beta-2 adrenergic receptor agonist), it’s a central nervous system stimulant that increases serum levels of norepinephrine. The herbs ma huang, ephedra sinica and Sida cordifolia contain ephedrine, which structurally is similar to amphetamines.1
Ephedrine is an effective bronchodilator due to its stimulation of beta–2 receptors in the lungs. However, it also stimulates beta-1 receptors in the heart and causes dose-dependent increases in heart rate and blood pressure. Drugs that are more selective beta-2 agonists are generally preferred for treatment of asthma.1
Ephedrine’s Role in Athletic Performance and Weight Loss
Ephedrine’s appeal to users rests in the fact that it may do one or all of the following three things, depending on the individual:
Improve athletic performance by stimulating the central nervous system and by increasing heart rate and contraction force via activation of the beta-1 receptors.
Suppress appetite by increasing norepinephrine release through stimulation of adrenergic pathways in the hypothalamus.1
Promote weight loss by increasing thermogenesis and resting energy expenditure via stimulation of the muscle beta-2 receptors to increase substrate metabolism.
Combining the drug with caffeine and aspirin (called the "ECA stack"), as some users do in the belief that it will enhance its effectiveness as a weight loss agent, may add significantly to the risk. In this context, ephedrine stimulates the release of norepinephrine, which stimulates the release of adenosine and the synthesis of prostaglandins by the activated tissue. Adenosine and prostaglandins both inhibit the effect of norepinephrine. Caffeine opposes the effect of adenosine and so increases norepinephrine release. Aspirin inhibits the synthesis of prostaglandins and so enhances the effect of norepinephrine.1
Side Effects
What users may not understand or take seriously when they seek the performance enhancing benefits of the supplement are the adverse effects it can produce. Ephedrine raises heat production and body temperature and may increase the athlete’s risk of developing a heat injury during exercise in warm weather. In addition to increased heat production, other effects may include dizziness, headache, gastrointestinal distress, irregular heartbeat, and heart palpitations to heart attack, stroke, seizures, psychosis and even death.
These side effects can vary among individuals and occasions and don't always depend on how much is consumed. Also, combining caffeine (from coffee, Guarana, mate, or any other source) with ephedrine-containing products (such as those mentioned earlier) greatly increases the risks.2,3
If the knowledge of these adverse effects isn’t enough to deter users, the International Olympic Committee, the National Collegiate Athletic Association (NCAA) and the National Football League (NFL) are hoping some of their recent policies banning the drug—and suspending players for doping—will be.
Research Findings
Still, are these organizations’ concerns about ephedrine really valid? In December of 2000, a study commissioned by the Food and Drug Administration (FDA) set out to answer that question by examining the adverse cardiovascular and central nervous system events associated with dietary supplements containing ephedra alkaloids.
In the study, records from 140 ephedra users who experienced complications (heart attack, stroke, seizure and death) between 1997 and 1999 were reviewed. These users were young and healthy—and some had only been taking ephedrine for a few days. 2
The researchers found that:
One-third of the patients’ complications were definitely or probably caused by ephedrine use.
Another third of the problems were possibly caused by ephedrine.
In one-fifth of the cases there was not enough information to determine the cause.
While these results illustrate the risks associated with ephedrine, the results of research illustrate its effectiveness. According to research:
A combination of ephedrine and caffeine (0.8 to 1.0 mg of ephedrine per kg and 4 to 5 mg of caffeine per kg consumed 1½ hours before exercise) may improve both anaerobic and high-intensity aerobic performance.4,5
Combining ephedrine and caffeine (20 mg ephedrine and 200 mg caffeine, consumed three times per day) with a low calorie diet (1,000 calories) may also help to promote weight loss in obese individuals. 6,7
Federal Investigations
Despite its effectiveness, in June of 2002, Health and Human Services Secretary Tommy Thompson called for an extensive scientific review of ephedrine to address health concerns associated with its use. The Rand Corporation is conducting this comprehensive review of the existing science on ephedrine and the National Institutes of Health will use this information to evaluate the safety of the product.8
In October of 2002, Secretary Thompson also urged the FDA to recommend strong mandatory warning labels for ephedrine-containing products. The FDA is working on proposed regulations regarding Good Manufacturing Practices for dietary supplements. These measures do not preclude further actions as a result of the Rand Corporation’s review of ephedrine. In addition, the FDA announced a new program to analyze all herbal ephedrine products to ensure that they contain natural (not synthetic) ingredients as required by law. It is illegal for companies to market non-herbal synthetic ephedrine products as dietary supplements.9.
Conclusion
Although ephedrine may improve athletic performance, the risks associated with this supplement far outweigh the benefits. Supplements containing ephedrine will not enable athletes to reach their goals. Sound nutrition, hydration and training programs will.
Ellen Coleman works with athletes at The S.P.O.R.T. Clinic in Riverside, Calif., and she is a nutrition consultant for the Los Angeles Lakers and Anaheim Angels.
References
1 Rawson ES, Clarkson PA. Ephedrine as an ergogenic aid. Performance-enhancing Substances in Sport and Exercise. Ed Bahrke MS, Yesalis CE. Human Kinetics. 2002.
2 Haller CA, Benowitz NL. Adverse cardiovascular and central nervous system events associated with dietary supplements containing ephedra alkaloids. N Engl J Med. 343:1833-8, 2000.
3 Public Citizen Health Research Group. Petition to the Food and Drug Administration (FDA) requesting the ban of production and sale of dietary supplements containing ephedrine alkaloids. (HRG Publication #1590). http://www.citizen.org/publications/release.cfm?ID=7053
4 Bell DG, McLellan TM, Sabiston CM. Effect of ingesting caffeine and ephedrine on 10-km run performance. Med Sci Sports Exerc. 34:344-9, 2002.
5 Bell DG, Jacobs I, Ellerington K. Effect of caffeine and ephedrine ingestion on anaerobic exercise performance. Med Sci Sports Exerc. 33:1399-403, 2001.
6 Astrup A, Breum L, Toubro S, Hein P, Quaade F. The effect and safety of an ephedrine/caffeine compound compared to ephedrine,caffeine and placebo in obese subjects on an energy restricted diet. A double blind trial. Int J Obes Relat Metab Disord. 16(4):269-77, 1992.
7 Astrup A, Buemann B, Christensen NJ, Toubro S, Thorbek G, Victor OJ, Quaade F. The effect of ephedrine/caffeine mixture on energy expenditure and body composition in obese women. Metabolism. 41:686-8, 1992.
8 Food and Drug Administration. FDA News: Statement from FDA Deputy Commissioner Crawford regarding Metabolife. August 15, 2002. http://www.fda.gov/bbs/topics/NEWS/2002/NEW00828.html
9 Food and Drug Administration. FDA News: Secretary Thompson urges strong warning labels for ephedra. October 8, 2002. http://www.fda.gov/bbs/topics/NEWS/2002/NEW00844.html
We hope you find this information useful.
Bob Murray, PhD, FACSM
Director, Gatorade Sports Science Institute
Ephedrine-Containing Supplements
April, 2003
Ellen Coleman, RD, MA, MPH
In many competitions, the difference between winning and losing can occur in one play or the divisions of seconds. So it is not surprising that athletes may want to utilize ephedrine-containing supplements to improve their performance, have more energy or decrease their body fat. Unfortunately, athletes who use ephedrine may risk getting more than they bargained for from the drug. While it may help them run farther and faster, it can also make them prey to the myriad of negative—even potentially life-threatening—side effects. The fact is ephedrine use is controversial at best. Especially when you consider that the NFL, NCAA and International Olympic Committee have all taken steps to keep it off the playing fields. And now, the FDA is getting into the discussion.
What is Ephedrine
So what exactly is ephedrine? Classified as a sympathomimetic drug (a beta-1 and beta-2 adrenergic receptor agonist), it’s a central nervous system stimulant that increases serum levels of norepinephrine. The herbs ma huang, ephedra sinica and Sida cordifolia contain ephedrine, which structurally is similar to amphetamines.1
Ephedrine is an effective bronchodilator due to its stimulation of beta–2 receptors in the lungs. However, it also stimulates beta-1 receptors in the heart and causes dose-dependent increases in heart rate and blood pressure. Drugs that are more selective beta-2 agonists are generally preferred for treatment of asthma.1
Ephedrine’s Role in Athletic Performance and Weight Loss
Ephedrine’s appeal to users rests in the fact that it may do one or all of the following three things, depending on the individual:
Improve athletic performance by stimulating the central nervous system and by increasing heart rate and contraction force via activation of the beta-1 receptors.
Suppress appetite by increasing norepinephrine release through stimulation of adrenergic pathways in the hypothalamus.1
Promote weight loss by increasing thermogenesis and resting energy expenditure via stimulation of the muscle beta-2 receptors to increase substrate metabolism.
Combining the drug with caffeine and aspirin (called the "ECA stack"), as some users do in the belief that it will enhance its effectiveness as a weight loss agent, may add significantly to the risk. In this context, ephedrine stimulates the release of norepinephrine, which stimulates the release of adenosine and the synthesis of prostaglandins by the activated tissue. Adenosine and prostaglandins both inhibit the effect of norepinephrine. Caffeine opposes the effect of adenosine and so increases norepinephrine release. Aspirin inhibits the synthesis of prostaglandins and so enhances the effect of norepinephrine.1
Side Effects
What users may not understand or take seriously when they seek the performance enhancing benefits of the supplement are the adverse effects it can produce. Ephedrine raises heat production and body temperature and may increase the athlete’s risk of developing a heat injury during exercise in warm weather. In addition to increased heat production, other effects may include dizziness, headache, gastrointestinal distress, irregular heartbeat, and heart palpitations to heart attack, stroke, seizures, psychosis and even death.
These side effects can vary among individuals and occasions and don't always depend on how much is consumed. Also, combining caffeine (from coffee, Guarana, mate, or any other source) with ephedrine-containing products (such as those mentioned earlier) greatly increases the risks.2,3
If the knowledge of these adverse effects isn’t enough to deter users, the International Olympic Committee, the National Collegiate Athletic Association (NCAA) and the National Football League (NFL) are hoping some of their recent policies banning the drug—and suspending players for doping—will be.
Research Findings
Still, are these organizations’ concerns about ephedrine really valid? In December of 2000, a study commissioned by the Food and Drug Administration (FDA) set out to answer that question by examining the adverse cardiovascular and central nervous system events associated with dietary supplements containing ephedra alkaloids.
In the study, records from 140 ephedra users who experienced complications (heart attack, stroke, seizure and death) between 1997 and 1999 were reviewed. These users were young and healthy—and some had only been taking ephedrine for a few days. 2
The researchers found that:
One-third of the patients’ complications were definitely or probably caused by ephedrine use.
Another third of the problems were possibly caused by ephedrine.
In one-fifth of the cases there was not enough information to determine the cause.
While these results illustrate the risks associated with ephedrine, the results of research illustrate its effectiveness. According to research:
A combination of ephedrine and caffeine (0.8 to 1.0 mg of ephedrine per kg and 4 to 5 mg of caffeine per kg consumed 1½ hours before exercise) may improve both anaerobic and high-intensity aerobic performance.4,5
Combining ephedrine and caffeine (20 mg ephedrine and 200 mg caffeine, consumed three times per day) with a low calorie diet (1,000 calories) may also help to promote weight loss in obese individuals. 6,7
Federal Investigations
Despite its effectiveness, in June of 2002, Health and Human Services Secretary Tommy Thompson called for an extensive scientific review of ephedrine to address health concerns associated with its use. The Rand Corporation is conducting this comprehensive review of the existing science on ephedrine and the National Institutes of Health will use this information to evaluate the safety of the product.8
In October of 2002, Secretary Thompson also urged the FDA to recommend strong mandatory warning labels for ephedrine-containing products. The FDA is working on proposed regulations regarding Good Manufacturing Practices for dietary supplements. These measures do not preclude further actions as a result of the Rand Corporation’s review of ephedrine. In addition, the FDA announced a new program to analyze all herbal ephedrine products to ensure that they contain natural (not synthetic) ingredients as required by law. It is illegal for companies to market non-herbal synthetic ephedrine products as dietary supplements.9.
Conclusion
Although ephedrine may improve athletic performance, the risks associated with this supplement far outweigh the benefits. Supplements containing ephedrine will not enable athletes to reach their goals. Sound nutrition, hydration and training programs will.
Ellen Coleman works with athletes at The S.P.O.R.T. Clinic in Riverside, Calif., and she is a nutrition consultant for the Los Angeles Lakers and Anaheim Angels.
References
1 Rawson ES, Clarkson PA. Ephedrine as an ergogenic aid. Performance-enhancing Substances in Sport and Exercise. Ed Bahrke MS, Yesalis CE. Human Kinetics. 2002.
2 Haller CA, Benowitz NL. Adverse cardiovascular and central nervous system events associated with dietary supplements containing ephedra alkaloids. N Engl J Med. 343:1833-8, 2000.
3 Public Citizen Health Research Group. Petition to the Food and Drug Administration (FDA) requesting the ban of production and sale of dietary supplements containing ephedrine alkaloids. (HRG Publication #1590). http://www.citizen.org/publications/release.cfm?ID=7053
4 Bell DG, McLellan TM, Sabiston CM. Effect of ingesting caffeine and ephedrine on 10-km run performance. Med Sci Sports Exerc. 34:344-9, 2002.
5 Bell DG, Jacobs I, Ellerington K. Effect of caffeine and ephedrine ingestion on anaerobic exercise performance. Med Sci Sports Exerc. 33:1399-403, 2001.
6 Astrup A, Breum L, Toubro S, Hein P, Quaade F. The effect and safety of an ephedrine/caffeine compound compared to ephedrine,caffeine and placebo in obese subjects on an energy restricted diet. A double blind trial. Int J Obes Relat Metab Disord. 16(4):269-77, 1992.
7 Astrup A, Buemann B, Christensen NJ, Toubro S, Thorbek G, Victor OJ, Quaade F. The effect of ephedrine/caffeine mixture on energy expenditure and body composition in obese women. Metabolism. 41:686-8, 1992.
8 Food and Drug Administration. FDA News: Statement from FDA Deputy Commissioner Crawford regarding Metabolife. August 15, 2002. http://www.fda.gov/bbs/topics/NEWS/2002/NEW00828.html
9 Food and Drug Administration. FDA News: Secretary Thompson urges strong warning labels for ephedra. October 8, 2002. http://www.fda.gov/bbs/topics/NEWS/2002/NEW00844.html
