EphedrineEssay Preview: EphedrineReport this essayThere 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
livers of rats, who generally use a diet of non-alcoholic fatty foods (PUFAs) consisting of fruit and vegetables. At a minimum, these rats take 2 to 4 g of ephedrine, typically in breakfast and on the basis of their diet.
Ephedrine is metabolized in the liver, which causes a loss of blood flow. If there is no blood flow problem during the delivery of ephedrine, only the liver may excrete it (for reasons of digestion). The systemic effects of ephedrine may be temporary but may last many years if the liver does not respond.
In cases of diarrhea or ulcerative colitis (UTI), it is suggested that ephedrine may act as a slow de-lipidase which prevents the liver from passing the lipoprotein. These findings are consistent with the use of high doses (>20 or >2000 mg/kg) of ileal ephedrine or ketoacidol (KE/OH), ileal ephedrine, or ketoacidol in combination with non-steroidal anti-inflammatory drugs (NSAIDs) such as ibuprofen, aspirin, and fluoxetine. The doses listed do not appear to be appropriate doses because there is evidence that only low and moderate amounts can decrease the toxicity of ephedrine. The toxicity of ileal ephedrine and ketoacidol is also seen in patients with osteopenia, high triglycerides or anorexia nervosa, and in chronic renal failure (e.g., diabetes).
A number of studies have shown that the use of ephedrine is protective against ulcers or cancer. The presence of cancer in children shows that this is not true. In an observational study, ephedrine was used for the treatment of malignancies for 12 weeks with or without cancer, although this study was limited by very small follow-up intervals and was not representative of the wider population. Ephedrine, when given for therapeutic reasons, had a dose of 10 mg/kg per day (see below), which included doses that appeared reasonably safe and were well tolerated by children. The number of patients treated with an investigational compound in this group increased from 1 in 4 in 2000 to 4 in 7 in 2012 as a result of the increased treatment success rate.
Evidence of its therapeutic benefit for adult patients is scarce. A study of children in a prospective cohort study in the United States showed no significant evidence that ephedrine is effective in treating pediatric cancers.
There is evidence of benefits in children through a number of small doses, ranging from 2 and 3mg/kg to 7 and 10 mcg/kg (Mellor 2001; McLeod and Wills 1975; Rook 1978). Ephedrine has been tested as a possible treatment for many of these pediatric diseases, including myelomas and myoclonus in children but not adults. In addition, no effective treatment for these diseases has been found to be available (Schmidt et al., 2005; Sabet et al., 2005). Ephedrine is available not without its side effects ranging from muscle loss, weakness, and constipation.
It is not clear how best to use ephedrine in treating ulcerative colitis (UTI). Studies by Schoon-Nielsen et al., 2005 showed that intravenous use