Ephedrine comes from the plant ephedra. It has been grown throughout northern Asia for thousands of years (Ephedrine Legal Advice 2004). Other common names for the drug include ephedra or Ma Huang. Three common active components of the drug include ephedrine, pseudoepherdine and phenylpropanolamine. The most potent of the three is ephedrine (Ephedrine Legal Advice 2004). The active ingredient in the plant ephedra is an alkaloid. The effects of alkaloids are similar to amphetamines.
The potency of ephedrine is directly related to the concentration of alkaloids present in the drug (Ephedrine Legal Advice 2004). The drug is a sympathomimetic agent and thus mimics the effects of the sympathetic nervous system. It activates ? and ?-receptors throughout the body. Since ephedrine is lipid soluble, it is able to cross the blood brain barrier and activate the central nervous system (Federal Drug and Administration 2003). The action on the central nervous system is to increase the release of norepinephrine and dopamine.
The rise in norepinephrine and dopamine heightens alertness and decreases fatigue (Federal Drug and Administration 2003). When ephedrine activates ?1 receptors in the heart, the heart rate is increased leading to an increase in cardiac output. When ?3 receptors in brown fat are activated by ephedrine, fat cells are broken down and metabolized (lipolysis). At the peripheral level, ephedrine acts as a vasoconstrictor, increasing the peripheral blood pressure.
However, at the respiratory level in the bronchioles of the lungs, the drug acts as a vasodilator dilating smooth muscles and opening up the airways. Ephedrine is also a potent antihistamine and blocks the effects of histamine (Federal Drug and Administration 2003). Due to the wide range of effects that ephedrine has on the body, it is used for many different therapies. The drug has been used for five thousand years in Asia as a decongestant for cold like symptoms (Ephedrine Legal Advice 2004). Today, it is used in many cold remedies such as Advil Cold and Sinus, Benylin and many others.
The antihistaminic effect of the drug decreases the runny nose, sneezing and congestion associated with the common cold (American Academy of Otolaryngology ?Head and Neck Surgery 2002). Its ability to act as a vasodilator on the airways makes it an effective treatment for asthma patients (Federal Drug and Administration 2003). It is also used to treat shock and hypotension because of its ability to increase blood pressure (Federal Drug and Administration 2003). Recently however, it has been used in many weight loss and performance enhancing supplements.
It is thought to increase weight loss by increasing the rate of metabolism of fats in the body. In performance enhancing supplements, it decreases fatigue, which enables the body to exercise for an extended period of time at an increased intensity (Federal Drug and Administration 2003). Supplements that ephedrine is commonly found in are energy drinks, diet pills and muscle enlargers. (Astrup et al 1992). Although desired results are seen for many athletes and dieters taking ephedrine, there are also many adverse effects associated with the drug.
Some of the adverse side effects include headaches, insomnia, nerve damage, heart palpitations, hyperactivity, shortness of breath, dizziness and high blood pressure. Ephedrine can induce toxicity in the body if taken at high enough levels. The results of ephedrine toxicity include arrythmias, myocardial infarctions, stroke, cardiac arrest and death (Federal Drug and Administration 2003). Ephedrine can be administered in different ways, depending on the reason for taking it. The reason ephedrine is used by athletes to improve their athletic performance comes from its ability to stimulate ?1 receptors in the heart.
This in turn releases additional norepinephrine from the sympathetic nerve terminals. The increase in norepinephrine causes greater contraction of heart muscles and therefore leads to a higher heart rate and increased cardiac output (Blechman et al. , 2004). The increased blood flow to muscle tissues allow the muscles to work harder for a longer period of time. This is ideal for athletes who are competing in tryouts for a sports team or just trying to increase the intensity of their own training program.
However, the dangerous side effects that can occur result from the same mechanism. Dramatically increased heart rate can lead to an irregular heart beat (arrythmia) and can quickly lead to death. It should be mentioned that ephedrine is the first herbal supplement to be taken off of the market by the FDA. Under the Dietary Supplement Health and Education Act (DSHEA) of 1994, the FDA may remove a dietary supplement from the market if it presents a significant or unreasonable risk of illness or injury when used according to its labeling or under ordinary conditions of use.
For the many deaths that have been linked to ephedrine use, it is extremely difficult to conclude that the product was not taken at too high a dose level or that interactions with other nutrients may have caused the problem. Therefore, removing a supplement from the market is not an easy process. There is currently a great deal of controversy over whether ephedrine should be available to the general public or not. Many believe that the supplement should still be available but that the terms of regulation should be more clearly stated and there should be an insert that comes along with the supplement like other medications do.
Many believe if the fine print was read correctly there may not be as many adverse effects. There is always a risk involved with consuming new dietary supplements. Although some weight loss studies have shown positive results relating to ephedrine use, the serious side effects of the drug far outweigh the slight benefits. Anyone doing a proper background check should realize that ephedrine can be a very dangerous product and consideration should even be taken when using it for medicinal purposes.