Supplement Performance - Ephedrine, Caffeine and the Combo

Effects on Muscular Endurance

Ephedrine is classified as a sympathomimetic drug and central nervous

system stimulant. Its ability to act as a sympathetic agonist and increase

thermogenesis (fat burning) has led to its use in weight loss/fat loss.1 Ephedrine

has also been coupled with both caffeine and aspirin to further enhance its

effectiveness (i.e., ECA). Ephedrine stimulates release of norepinephrine, which

stimulates the synthesis of prostaglandins by the activated tissues.1 Aspirin

inhibits the synthesis of prostaglandins and serves as a prostaglandin blocker,

and thereby may prevent inhibition of norepinepherine release.1 Further, as a

central nervous system stimulant, it’s used to reduce fatigue and increase

alertness.

In most dietary supplements, ephedrine appears as an extract from one

of two herbs: ephedra or Ma Huang. Ephedra species have a long tradition of

use (more than 5,000 years) for respiratory ailments.2 Unlike other herbs, active

ingredients are well characterized and consist of ephedrine and related

alkaloids (mostly ephedrine, pseudoephedrine, and norpseudoephedrine).2

Recently, another herb, Sida cordifolia, was said to contain ephedrine alkaloids,

but firm data on amounts are lacking, even from the supplier.2

It should be noted that the U.S. Olympic Committee (USOC) and the

International Olympic Committee (IOC) prohibit use of ephedrine during

competition. The ephedrines can be easily detected, like amphetamines, by

extracting the urine with diethyl ether at pH 13 and by gas chromatography of

the extract using a nitrogen-selective detector. However, IOC-accredited

laboratories are advised to ignore small concentrations of ephedrines provided

the pH and specific gravity of the urine is within normal limits.3

Latest Bell Study

There is growing body of evidence that combined ephedrine and caffeine

ingestion improves performance.4,5,6,7,8 The latest paper was recently published

by Dr. Douglas Bell and colleagues.9 The purpose of this study was to

investigate the effects of ingesting caffeine, ephedrine and their combination on

muscular endurance using a double-blind, repeated measures design. Ninety

minutes after ingesting either caffeine (four milligrams per kilogram body weight

[mg/kg]), ephedrine (0.8 mg/kg), a combination of caffeine ephedrine, or a

placebo, 13 male subjects performed a weight training circuit consisting of three

supersets. Each superset consisted of the leg press followed by the bench

press; two minutes of rest between supersets.

The trials involving ephedrine ingestion, when compared with the nonephedrine

trials (caffeine and placebo), showed ephedrine caused significant

increases in the mean number of repetitions completed for both the leg-press

and bench-press exercises, but only during the first supersets. Results indicated

that the total weight lifted during all three sets was greater for the trials involving

ephedrine ingestion.

The performance enhancement was attributed primarily to the effects of

ephedrine; there was no evidence of an additive or synergistic interaction

between the caffeine and ephedrine. This finding contrasts with earlier research

into the effects of caffeine ephedrine on cycle ergometer exercise time to

exhaustion at 80 percent maximal aerobic power9 in which the caffeine and

ephedrine did appear to interact additively.12

The magnitude of the effect during the first set is highly significant for this

type of exercise, considering it was induced only 90 minutes after ingesting

caffeine ephedrine. The 16 percent improvement in bench-press performance

would otherwise be expected to require from four to about 12 weeks of strength

training. However, as Dr. Bell and colleagues pointed out, these results should

be considered in light of evidence suggesting a learning effect throughout the

experiment. Nevertheless, results strongly support the conclusion that there

was an ergogenic effect of the caffeine ephedrine on this type of exercise.

The trials involving ephedrine ingestion caused significant increases in

systolic blood pressure compared with non-ephedrine trials. However, the

treatment did not affect diastolic blood pressure. Two subjects displayed

extremely high hypertensive responses to the caffeine ephedrine treatment.

The subjects were otherwise normotensive, but had pre-exercise blood

pressures of 204/90 and 214/112, respectively, 90 minutes after ingesting

caffeine ephedrine.

What About Side Effects?

According to Dr. Bell and colleagues, “Our research should not be

construed as advocacy for athletes or recreational fitness enthusiasts to use

ephedrine or other ephedra alkaloid-containing (ECA) products. We

acknowledge that there are serious risks such that demonstrated by the

hypertensive responses observed in subjects in this study… It should be noted,

however, that there is little, if any, scientific evidence that documents the

associated health risks of acute or chronic use of C-E [caffeine ephedrine] in

prospectively designed studies.”

For example, Dr. Boozer and colleagues at the New York Obesity

Research Center recently published a paper examining long-term safety and

efficacy for weight loss of an herbal Ma Huang and kola nut supplement.10

Authors concluded that in a six-month placebo-controlled trial, herbal

ephedrine/caffeine (90/192 mg/day) promoted body weight and body fat

reduction and improved blood lipids without significant adverse effects.

However, it should be noted that weight loss trials frequently involve medical

screening to detect pre-existing conditions, such as heart disease, that may

predispose subjects to an increased risk of adverse effects. Whether persons

taking ephedrine or ephedra without such medical screening have a similar risk

of adverse events is unknown.11

Between June 1, 1997 and March 31, 1999, the FDA received 140

reports of adverse events allegedly associated with the use of ephedrinecontaining

dietary supplements that contain, or were suspected of containing,

ephedrine alkaloids.14 After review, FDA analysts felt there was a clear

connection to ephedrine alkaloids in 60 of the cases, approximately one-third of

which involved the cardiovascular system.

However, according to Dr. Steven Karch, “The AERs [Adverse Event

Reports] I have reviewed in this statement do not show that ephedra, when

consumed in appropriate amounts, is causally related to the adverse events...

FDA's literature review consists of many references that are either irrelevant or

inappropriate to an analysis of the safety of ephedra products. Thus, the

literature review's relevance in an analysis of the safety of ephedra products is

questionable... In sum, my review of the above information leads me to a very

different conclusion than that reached by FDA and its consultants‚ that ephedra

products may be safely consumed when taken in accordance with the current

national standards as reflected in the American Herbal Products Association

trade recommendation for ephedra products.”14

Recently, JAMA meta-analysis concluded that ephedrine and ephedracontaining

dietary supplements have modest short-term benefits with respect to

weight loss and harms in terms of a two- to three-fold increase in psychiatric

symptoms, autonomic symptoms, upper gastrointestinal symptoms and heart

palpitations.

Since dietary supplements are not regulated for quality control the same

way traditional pharmaceuticals are, the amount of active ingredients in

ephedra-containing herbal products can vary tremendously. For example, Dr.

White and colleagues determined the variability of ephedrine and

pseudoephedrine among capsules from the same lot of Ma Huang.13 Although

the label claimed each capsule contained 375 milligrams of Ma Huang per

capsule, the amount varied from 368 to 411 milligrams.

Bottom Line

Ephedrine ingestion, either alone or in combination with caffeine, could

lead to a significant increase in the number of repetitions that could be

performed and the total amount of weight that could be lifted during weight

training. However, ephedrine/ephedra is not for everyone and must be used

responsibly. It is very important that you read product labels, warnings and

cautions, and follow the directions.

SIDEBAR

Ephedra Products: Serving Limits, Warnings, Precautions

• Do not take more than 25 milligrams of ephedrine alkaloids per serving

and not more than 100 milligrams per day.

• Consult a health care professional before consuming an ephedracontaining

dietary supplement if you have heart disease, thyroid disease,

diabetes, high blood pressure, depression or other psychiatric condition,

glaucoma, difficulty in urinating, prostate enlargement, seizure disorder;

or if you are using a monoamine oxidase inhibitor (MAoI) or any other

prescription drug; or if you are using an over-the-counter drug containing

ephedrine, pseudoephedrine or phenylpropanolamine (ingredients found

in certain allergy, asthma, cough/cold and weight control products).

• Do not use ephedra products if you’re under the age of 18. Do not use

ephedra products if you are pregnant or nursing.

• Discontinue use and call a health care professional immediately if you

experience rapid heartbeat, dizziness, severe headache, shortness of

breath, or other similar symptoms.

• Exceeding the recommended serving will not improve results and may

result in serious adverse health effects.