In one form or another, the herb ephedra has been used in supplements for more than 3,000 years. Practitioners of traditional Chinese medicine (TCM) have valued ephedra, or ma huang, for its powers as a general restorative, an asthma remedy, and a dilator of the bronchial passages to ease breathing. A North America variant, known as Mormon tea, was used by the settlers of the southwestern United States in the 1800s to the same effect.
Ephedrine, the active component of ephedra, was first discovered in 1885. Further research in the 1930s led to the synthesis of ephedrine, as well as the invention of the class of synthetic drugs known as amphetamines, which possess similar decongestant powers and stimulant effects on the central nervous system. The use of these types of drugs was not regulated in many parts of the world until the 1980s, during a time when ephedrine was used extensively as a performance-enhancing stimulant by athletes and as a weight loss tool by the general population.
Research in three different forums resulted in the regulation of the use of ephedrine. The World Anti-Doping Agency (WADA), a successor organization to the different agencies of the International Olympic Committee that had attempted to regulate drug use in sport through the 1990s, conducted extensive research into the performance-enhancing qualities of ephedrine. WADA regulations prohibit the use of ephedrine by athletes in amounts greater than 10 mcg per ml in any international sports competition over which it has authority. The United States Food and Drug Agency (FDA), which is responsible for the regulation of all dietary supplements manufactured, imported to, or sold in the United States, determined that a significant health risk existed for the public through the consumption of ephedra supplements. Consequently, in 2004, all ephedra supplements were banned in the United States. The U.S. prohibition was made against the backdrop of the sudden death by cardiac arrest of Baltimore Orioles pitcher Steve Bechler, who was believed to have been taking ephedra supplements at the time of his death. Related research carried out in England and other European laboratories stimulated similar regulatory restrictions on ephedra throughout the European Community.
Ephedra-free supplements were developed to fill this regulatory void. Manufacturers have sought to replace the proven stimulant effect of ephedrine with a number of compounds, including caffeine, Citrus aurantium, ginseng, and synthetic compounds.
Caffeine is a well-known stimulant, although it has a lesser impact on the central nervous system than ephedrine. Supplements commonly include caffeine-rich substances such as black tea, cola nut extract, or guarana (a root obtained in the Amazon basin). Citrus aurantium (commonly called bitter orange) is a compound similar in composition to ephedrine; the active component is synephrine, a stimulant. While a legal component of supplements distributed and sold for general health and purported weight loss qualities (often referenced as having "fat-burning" properties, or thermogenesis), synephrine is listed as a WADA-prohibited substance. The risks associated with bitter orange/synephrine use regarding the effect upon the user's heart rate are not demonstrably different that those established through ephedrine research. Ginseng and willow bark are herbs reputed to have aspirin-like effects on athletic performance, working as an anti-inflammatory in the musculoskeletal system. Engineered compounds such as DMAE (2-dimethylaminoethanol) are reputed to provide memory-enhancing and increased energy performance powers. As of 2006, long-term research on the effects of DMAE is not yet available.
By the scientific standards of objective testing over time, using large population samples, the period between the identification of difficulties with ephedra use and the introduction of ephedra-free supplements is a short one. It may be that so long as any stimulant that mirrors the properties of human adrenaline is used, issues will arise regarding the safety of the use of such compounds in relation to the heart and the central nervous system. The practitioners of traditional Chinese medicines valued ephedra not as a sport supplement, but as a general restorative and balm to the health of a person. If ephedra were accepted simply for those general health qualities, the bans on its use in competitive sport would be rendered separate.
Ephedra and its replacement, Citrus aurantium, do not have a long life within the biology of the body; they are both readily processed, broken down, and excreted, as each is water soluble.