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Notice: This information is presented for educational purposes only. Consult a doctor or other health professional for proper medical care.
What is Ephedra?
Ephedra, also known as Ma Huang, is a traditional Chinese herb which has been used in various applications for over 5,000 years. It is important to note that while there are approximately 40 different species of ephedra, when one refers to ephedra it is almost always in reference to those species which contain ephedrine group alkaloids (not all species do!).
Species with ephedrine group alkaloids (and those most often used in diet products) include: Ephedra sinica, Ephera equisentia and Ephera intermedia (1).
What are ephedrine group alkaloids?
Ephedrine group alkaloids comprise the primary, active element of the above noted species of ephedra (note: alkaloids are simply chemical compounds or constituents formed in a plant's normal metabolic processes). Within the ephedrine group alkaloids, the individual alkaloid ephedrine (note: this is ephedrine – the individual alkaloid ephedrine IS pure ephedrine) and the individual alkaloid pseudoephedrine (less potent than ephedrine) are the two most prevalent alkaloids – the ephedrine alkaloid is the most dominant with respect to quantity (up to 90%) (2) and with respect to potency (effect/activity).
Other alkaloids are generally present in very small or trace amounts (3) and generally have the effect of slightly slowing the absorption of ephedrine in the digestive tract, among other effects.
Related information…
Ephedrine group alkaloids are most prevalent in the ephedra herb's woody stems (also referred to as the ‘aerial parts' or ‘aboveground parts' of the plant). Hence, products which contain ephedrine group alkaloids are prepared from an extract sourced from the stem of ephedra. Notably, the concentration of ephedrine group alkaloids varies by species of ephedra as well as time of year (2). Because of this variability it is important to standardize extracts so that the quantity of ephedrine group alkaloids can be determined.
In short, standardization is a process by which the concentration of certain chemicals is measured. In the context of an ephedra extract, generally, standardization is conducted with respect to the quantity of ephedrine group alkaloids. Standardization may also be conducted for the individual ephedrine alkaloid. In either instance (or others) it is important to remember that it is the PRESENCE of a certain chemical or chemicals, not the ABSENSE, which is being standardized/measured.
The importance of understanding this distinction is that a product with ephedrine group alkaloids may contain not only the ephedrine alkaloid, but also other alkaloids as well (most likely pseudoephedrine). Although the research is not definitive, it appears very unlikely that a product with naturally derived ephedrine would exclusively contain ephedrine.
What is Ephedrine?
In short, ephedrine is a potent CNS (central nervous system) stimulant. As discussed above, ephedrine is a naturally occurring alkaloid. However, as with many of today's drugs which began as chemicals found in plants, such as aspirin which was originally derived from the bark of willow trees, ephedrine is also synthetically produced in laboratories.
Ephedrine produced in this manner is known as “synthetic ephedrine” as it is synthesized and not naturally occurring - for this reason, this type of ephedrine is also classified a drug. Although chemically this ephedrine is same as the individual ephedrine alkaloid, it is most often marketed in the hydrochloride (HCl) form. As with many drugs, conversion into hydrochloride form allows for more rapid absorption.
Thus, ephedrine HCl's active element is pure ephedrine. For this reason (i.e it's pure ephedrine) as well as the fact that it's in hydrochloride form, absorption is more rapid.
Ephedrine HCl v. Ephedrine Group Alkaloids - what's the difference?:
The primary differences between ephedrine HCl (synthetic) and ephedrine group alkaloids (naturally occurring) are: source and composition.
Regarding source differences, ephedrine HCl is synthesized in a laboratory whereas ephedrine group alkaloids are naturally occurring in certain species of the herb/plant ephedra. Regarding composition differences, ephedrine HCl is pure ephedrine (in hydrochloride form) whereas ephedrine group alkaloids contain the individual ephedrine alkaloid as well as other alkaloids (as noted above). The active ephedrine itself is chemically identical in either form.
As well, another difference is that the absorption rate of ephedrine HCl is slightly faster relative naturally occurring ephedrine. Importantly, because ephedrine HCl is synthesized (not naturally occurring) FDA has classified it as a drug.
What is the legal status of ephedrine – is ephedrine legal?
Yes, generally speaking, ephedrine is legal. However, it is important to distinguish between synthetic ephedrine (e.g. ephedrine HCl) and ephedrine from naturally occurring ephedrine group alkaloids when discussing the legal status of ephedrine.
Regarding naturally occurring ephedrine:
On April 13, 2005, a federal court in Salt Lake City [U.S. District Court for the District of Utah, Central Division] issued its decision on a legal challenge to FDA's 2004 Final Rule banning all ephedrine-alkaloid dietary supplements. Judge Tena Campbell's decision made two key points:
1. It held that the analysis used by FDA was incorrect and improper. FDA's analysis weighed risks against benefits. The Dietary Supplement Health and Education Act (DSHEA), however, requires a straightforward risk assessment.
The court held that requiring supplement companies to demonstrate a benefit as a pre-condition to marketing violated DSHEA by shifting the burden from FDA to industry.
2. It held that FDA didn't have adequate scientific evidence to find that a daily dose of 10 mg. or less of ephedrine alkaloids presented a "significant or unreasonable risk of illness or injury" [under 21 U.S.C. § 342(f)(1)(A)].
The court effectively held that it's improper to ban all ephedra supplements because FDA lacks data to determine what dosage might be safe.
The case isn't necessarily over yet. FDA may appeal, and the 10th Circuit Court of Appeals might reverse the district court's ruling. Meanwhile, FDA may seek to block renewed ephedra sales while the matter is pending (4).
However, at this time it is legal to buy/sell ephedrine alkaloid products with a daily dose of 10mg or less. But, while US federal courts have validated the legality certain states (i.e. California, Illinois, New York and Texas) restrictions still stand.
Regarding synthetic ephedrine (e.g. ephedrine HCl):
Yes, generally speaking synthetic ephedrine is also legal. However, because synthetic ephedrine is classified as a drug, certain additional restrictions do apply.
FDA's ban with respect to synthetic ephedrine applied to the use of this substance for diet/energy/fat loss on the basis that synthetic ephedrine is classified as a drug which has not been approved for such uses.
As with any drug it must be approved by FDA for specific uses. To date, synthetic ephedrine has only been approved for use in treating allergies, asthma, nasal congestion, and related upper respiratory symptoms, but not for weight loss or to enhance athletic performance. It is unlikely that anyone or any company will seek to secure FDA approval for the use of synthetic ephedrine for weight loss due to the expense involved and lack of barriers to competition.
In addition, the drug, or synthetic form, ephedrine is regulated by DEA (as with any drug). Largely out of concerns pursuant to the illegal manufacture of methamphetamine products, DEA has imposed certain quantity limits and other restrictions on the sale of synthetic ephedrine.
Products containing only synthetic ephedrine are HIGHLY regulated by DEA, however, products which combine synthetic ephedrine with another substance (e.g. guaifenesin) are less strictly controlled. Examples of less-controlled products would include VasoPro and Bronch-Eze, which combine ephedrine HCl and guaifenesin.
In short, although the ephedrine in products such as VasoPro and Bronch-Eze is the same ephedrine earlier used in now banned diet/energy products, ephedrine itself was never banned by FDA. Moreover, its use offered with these products is as a bronchodilator (an approved use).
Notice: This information is presented for educational purposes only. Consult a doctor or other health professional for proper medical care.
(1) “Ephedra and Ephedrine Alkaloids for Weight Loss and Athletic Performance” National Institute of Health, Office of Dietary Supplements.
(2) Dentali, Steven J., Ph.D., “Ephedra's Alkaloids Provide its Kick,” Nutrition Science News , October, 1999
(3) White LM, Gardner SF, Gurley BJ, Marx MA, Wang PL , Estes M. Pharmacokinetics and cardiovascular effects of ma-huang (Ephedra sinica) in normotensive adults. J Clin Pharmacol. 1997; 37 :116–122.
(4) Thiessen, Mark, “Judge Rules Against FDA Ban on Ephedra,” Associated Press, April, 2005, Available: http://www.washingtonpost.com/wp-dyn/articles/A53586-2005Apr14.html |
