Ephedrine

There are great health and social pressures in our society to be thin. Experts agree that combining a healthy diet with regular exercise is the best way to lose weight. However, hundreds of different nutritional supplements are readily available on the market claiming to enhance physical performance and help with weight loss. These products are readily purchased by consumers looking for fast results without much concern or knowledge of the possible side effects or dangers. Short or long term exposure to xenobiotics found in these supplements can result in complex interactions with other components of the diet. Unfortunately, many herbal supplements can be marketed without extensive scientific testing and without a real understanding of how it might impact health status. One such substance is ephedrine.

This paper aims to present the most up to date research on how ephedrine interacts in the body to produce its effects. This includes risks, benefits and toxicities associated with its use. Comparisons of different lab studies will show how the efficacy of ephedrine for weight loss treatments can be exaggerated depending on the study protocol.

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 б and в-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 в1 receptors in the heart, the heart rate is increased leading to an increase in cardiac output. When в3 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. A common performance supplement is Extreme Ripped Force which contains 25 mg of ephedrine which is 3 times above the allowed FDA limit (Kapner 2003). A common diet pill is Metabolife 356® which is said to boost energy levels enabling you to exercise longer which will aid in weight loss. The product contains high levels of caffeine as well as ephedrine. Caffeine has been shown to increase the effect of ephedrine on weight loss (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. Toxicity associated with CNS stimulation is psychosis. For example, Steve Bechler, a 23-year-old Baltimore Orioles pitcher died from multiple organ failure after taking an ephedrine base supplement (Kapner 2003). Since his death, a lot more attention has been focused on the side effects of ephedrine. Some countries and states have even banned the drug due to the serious adverse effects it has on the body (Kapner 2003). Another case involved a 21 year old college student who while running an agility test collapsed and died. The student had taken hydroxycut and ripped fuel (which contain ephedrine) for the first time to increase his athletic performance. His autopsy showed no coronary artery damage and the diagnosis was acute arrhythmia caused by ephedrine (Federal Drug and Administration 2003).

Ephedrine can be administered in different ways, depending on the reason for taking it. Oral preparations of ephedrine (for medical use) are available as 25mg capsules and ephedrine can also be administered as a parenteral injection at a concentration of 50mg/mL. Nasal sprays (0.25%) are also available (Katzung, 2004). In an emergency situation involving severe trauma, ephedrine would be injected intra-venously for faster results to increase heart rate and maintain blood pressure. Ephedrine is readily absorbed from the gastro-intestinal tract (GIT) because of its lipid solubility. It crosses the wall of the small intestine where it enters the hepatic portal system and heads for the liver. Although ephedrine is metabolized in the liver, the majority of it (60-97%) is excreted unchanged in the urine. Ephedrine that is not excreted leaves the liver through the hepatic vein and enters the