by Bryan Haycock - Ephedrine stimulates lipolysis by increasing noradrenaline (NA) release from sympathetic nerve terminals. This increase in noradrenaline activates adrenergic receptors which increases cAMP levels in fat cells and muscle cells. This has the effect of increasing lipolysis in fat cells and increasing protein synthesis in muscle tissue. Negative feedback mechanisms are activated as well, and involve the production of phosphodiesterases, adenosine, and prostaglandins. Caffeine has the ability to inhibit phosphodiesterase activity and interfere with the adenosine receptor. This combined with its ability to prevent some NA re-uptake12 increase the effectiveness of ephedrine in a synergistic fashion. Aspirin has been shown to increase the effectiveness of ephedrine in some individuals presumably by its actions as a prostaglandin inhibitor.

Maximum effectiveness is achieved when taking 20 mg ephedrine with 200 mg caffeine and 300 mg aspirin three times a day about one half hour before meals. Common side effects are associated with its sympathetic activity namely, anorexia, initial rise in blood pressure, initial tachycardia, slowed GI motility (constipation), insomnia, agitation, anxiety, nervousness and depression- like withdrawal symptoms. Most all of these symptoms exhibit tachyphylaxis after about 4-6 weeks. Thermogenic activity seems to last upwards of 20 weeks due to its low desensitization properties and beta-3 affinity. About 75% of ephedrine’s effects on weight loss in the obese are due to appetite control.

Anyone considering taking ephedrine, caffeine and aspirin should educated themselves first about the potential side effects. Individuals with pre-existing high blood pressure should not use sympathomimetics such as ephedrine. When taking herbal forms of ephedrine, be sure you understand just how much is in each serving. Be aware that herbal preparations are standardized but you still can not be sure exactly how much you are taking with each capsule.

Ephedrine hydrochloride is commercially available from a limited number of companies with some restrictions. You can buy ephedrine here.

The Difference Between Ephedrine and Ephedra

Todd A Harrison, Buchanan Ingersoll to Kim Stratford, President of American Council on Regulatory Compliance

Executive Summary. This responds to your request for an explanation of the differences between over-the-counter ("OTC") bronchodilator/expectorant drug products containing ephedrine hcl and dietary supplements that contain ephedra, ephedrine alkaloids, or ephedrine. As explained below, the differences are substantial and FDA's decision to prohibit the sale of dietary supplements containing ephedrine has absolutely no impact on a company's ability to market and sell OTC drug products containing ephedrine hcl. The most noticeable difference between the two products is that ephedrine hcl drug products contain "Drug Facts" boxes and ephedra/ephedrine dietary supplement products contain "Supplement Facts" boxes. Only those products that contain "Supplement Facts" boxes will be affected by FDA's proposal to prohibit the sale of ephedra/ephedrine dietary supplements.

Discussion. The Federal Food, Drug and Cosmetic Act ("FFDCA") and U.S. Food and Drug Administration ("FDA") regulations treat dietary supplements and OTC drug products differently.

Dietary supplement products are not formally recognized as safe and effective by the Agency.

Over-the-counter ("OTC") drug products may only be marketed if the FDA has recognized the products as safe and effective.

"Ephedra" is the commonly used name for a dietary supplement containing ephedrine alkaloids or naturally occurring ephedrine. It is sold either as a raw botanical or as an extract from botanical sources, and it also is sometimes known by other names, such as Ma Huang and Chinese Ephedra. The raw botanical or extract naturally contains the following alkaloids (among others): ephedrine, pseudoephedrine, norpseudoephedrine, norephedrine, methylephedrine, and methylpseudoephedrine. Because ephedra is sold as a "dietary supplement," it was marketed without FDA's concurrence or approval and could not be removed from the market until such time that FDA found that it posed a significant or unreasonable risk of harm.

In contrast, OTC drug products that contain ephedrine hcl are specifically marketed pursuant to FDA's "Final Monograph for Cold, Cough, Allergy, Bronchodilator, and Antiasthmatic Drug Products for Over-the-Counter Human Use" ("final monograph"). The final monograph identifies certain ingredients that FDA has determined are "generally recognized as safe and effective" for particular uses and sets forth specific rules regarding labels that, when complied with, permit a company to market one of those ingredients. The inclusion of ephedrine hcl in the final monograph represents a finding by FDA that ephedrine is generally recognized as safe and effective when labeled in accordance with the monograph. Moreover, ephedrine hcl has never been eligible to be marketed as a dietary supplement, nor could any claims regarding weight control or energy have been made for products containing ephedrine hcl. To do so, would have caused the product to be considered an unapproved new drug, by the agency.

FDA has announced its attention [sic] to prohibit the sale of ephedra dietary supplements - not ephedrine hcl OTC drug products.

FDA has announced its intention to prohibit the sale of dietary supplement products that contain ephedra, ephedrine alkaloids, and ephedrine because of perceived concerns over their safety. This announcement was based on FDA's analysis of perceived risks associated with ephedra products, including (1) a study by the RAND Corporation allegedly suggesting health risks associated with ephedra; (2) the available evidence suggests that there is a "significant or unreasonable risk of illness or injury" associated with consumption of ephedra; (3) a new warning label would not mitigate that risk.

More importantly, this action pertains only to dietary supplements that contain ephedra, ephedrine alkaloids, or ephedrine. This decision does not reflect, in any way, FDA's view of the safety of ephedrine hcl bronchodilator drug products. Indeed, the FDA's decision does not affect the regulatory status of OTC bronchodilator products containing  ephedrine hcl in the United States and the ability to market these products in the United States.

Conclusion. Because ephedra dietary supplements and ephedrine hcl OTC drug products are subject to entirely separate legal and regulatory regimes, FDA's decision to ban ephedra dietary supplements has absolutely no impact on the status of OTC ephedrine hcl drug products, and companies are free to market and distribute OTC ephedrine hcl drug products.

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Publication Date: November 10, 2005