Supplement Guide Volume 1 – Ephedrine, Epinephrine and Clenbuterol Researched and Composed By Joe “Yu Yevon” King Abstract
Competitive athletes are always seeking an advantage over their opponents. In the bodybuilding community, this means getting more defined and leaner before an upcoming bodybuilding exposition. As a result, fat burners have become more and more popular within the athletic and, particularly, the bodybuilding community. It is the effort of this author to discuss the facts behind the most common fat burner – ephedrine – and two other widely used thermogenic agents – epinephrine and clenbuterol - to allow athletes to make an educated decision when considering the use of fat burning supplements to enhance athletic performance.
Disclaimer:
No specific products are mentioned in this article; it rests upon the athlete to read the labels of fat burning supplements for their ingredients to determine their effectiveness and the safety of the product.
Ephedrine
Ephedrine is considered to still be a relatively new supplement, although it has been used in Chinese medicine for thousands of years. Bodybuilders find this supplement appealing because of its fat burning properties, especially when combined with aspirin and caffeine. Often referred to as an ECA stack, these three compounds have quickly become the most popular fat burners on the market despite the apparent lack of scientific data to back up the various claims.
Ephedrine is a naturally occurring sympathomimetic amine, which is found in plants of the genus Ephedra, including the herb ma huang. Ephedrine is structurally similar to the hormones adrenaline and amphetamines, and has similar metabolic pathways. Ephedrine works by stimulating beta adrenoreceptors (ephedrine is classified as a beta agonist) through the release of excitatory chemicals called catecholamines. The catecholamines act on cellular receptors found in numerous body tissues and are responsible for stimulating lipolysis, dilating bronchioles, decreasing appetite, and increasing heart rate and alertness. However, ephedrine is non-selective in which beta receptors it stimulates. Ephedrine interacts with several types of beta receptors (the exact amount is unknown, as more beta receptors are being discovered). In low doses, ephedrine can mimic adrenaline and methanphetamines, yet it can also raise blood pressure, increase heart rate, and in some cases lead to stroke. More of the side effects will be discussed later.
Bodybuilders supplement with ephedrine for two primary reasons – thermogenesis and an increase in strength. Ephedrine has been found to speed up the rate at which stored triglycerides is converted into adenosine triphosphate (ATP) through a process known as lipolysis.
Ephedrine also acts by stimulating norepinephrine, a neurotransmitter that acts to vasoconstrict arteries and blood vessels. In the lungs, norepinephrine opens bronchial passages allowing for more air to flow in. This is why ephedrine can be found in some allergy and asthma medications. In the heart, an increase in the flow of epinephrine causes a rapid heart beat and elevated blood pressure, which may create a feeling of increased energy. The release of norepinephrine also increases thermogenesis, the body’s ability to warm itself.
E/C/A
The exact mechanism of action is still somewhat unclear; however, evidence suggests that ephedrine, when combined with caffeine and aspirin, elevates the body’s production of norepinepherine (noradrenaline) which, in turn, stimulates beta-3 receptors, thus increasing the rate of thermogenesis. Ephedrine may also stimulate the two thyroid hormones T3 and T4.
Aside from ephedrine’s thermogenic effects, it is also reported to spare muscle tissue during a low calorie diet. However, there is very little scientific evidence to confirm this; the majority of evidence is purely anecdotal.
Ephedrine can be found in many different products in several different forms. The most commercially used source for ephedrine is from ma huang and has been used clinically for nasal congestion and chronically low energy levels. It is important to realize that not all ma huang sources are equal. The ephedrine concentration varies greatly between the various species of ma huang and is even dependent on the geographical area in which it is grown. Even further, there may be wide variation within the same species of plant. Thus, it is near impossible to tell exactly how much ephedrine is being ingested by the consumer upon purchase of the product.
Most manufacturers attempt to only use the high concentration sources of ephedrine and use the “L” form. Like amino acids and other substances with biochemical properties, ephedrine exists in various forms known as isomers, which are labeled according to their structure or rotation around the central axis. When only two isomers exist they are usually mirror images of one another and rotate clockwise (L) or counter clockwise (D).
Manufacturers also like to label ephedrine products as being “natural” since the ephedrine is derived from the natural herb ma huang. However, this is entirely misleading and, in many cases, false. The majority of ephedrine products have been “fortified” or “spiked” with additional ephedrine and norephedrine from sources other than that of the herb.
The most widely used form of ephedrine, even though most consumers are totally unaware of it, is pseudoephedrine. Pseudoephedrine is occasionally included in cold medications to prevent drowsiness and is an effective decongestant. Dosages of Ephedrine
Although there will be individual differences, the manufacturer recommended dosage for ephedrine and caffeine is typically 20 to 50 milligrams and 100 to 200 milligrams respectively. Aspirin is usually taken in dosages of 300 milligrams. Common supplementation requires 2 to 3 doses daily, including 30-45 minutes prior to exercise.
Side Effects
The side effects of ephedrine are glaring and are a great cause for concern; so much, in fact, that this author does not recommend consuming any product containing ephedrine.
Some individuals may experience allergic reactions to the drug, which has been shown to be fatal. Other individuals, teenagers included, who have underlying cardiovascular disease, may experience potentially fatal results from supplementation. Another cause for concern is the interaction with other drugs. Even caffeine and aspirin (ironically, the two substances it is taken with the most) can produce a myriad of side effects which may be life-threatening. The most common of these side effects is a substantial increase in blood pressure. Other side effects include tremors, headaches, rapid dehydration, gastrointestinal distress, heart attack, stroke, heart rate irregularities, nervousness, nerve damage, seizures, anxiety, psychosis, respiratory depression and death. Medical Research Pertaining to Ephedrine
A plethora of medical research is available outlining the dangers of ephedrine. The response from the medical community is overwhelming in the fact that ephedrine is dangerous for use in athletics. The following is just a small sampling of the research that has been conducted in recent years pertaining to ephedrine.
Johnson, Kent D. 2001: ephedra and Ma Huang Consumption: Do the Benefits Outweigh the Risks? Strength and Conditioning Journal: Vol. 23, No. 5, pp. 32–37.
“For most consumers, dietary supplements are generally safe. However, products containing ephedrine, pseudoephedrine, or Ma Huang (sinica ephedra) may be an exception.
“Ma Huang, ephedrine, and pseudoephedrine fall into a generation of drugs called sympathomimetics. These drugs have an adrenergic impact, mimicking the effects of sympathetic nervous system stimulation, such as those following the injection of epinephrine (32). Ma Huang is the herbal form of ephedrine; it is extracted from dried stems of the ephedra plant species and is marketed in weight-loss and energizing products.
“Ephedrine dilates the bronchial muscles, contracts the nasal mucosa, and raises the blood pressure.
“Adverse reactions to ephedrine include nervousness, restlessness, trouble sleeping, irregular heartbeat, difficult or painful urination, dizziness or light-headedness, headache, loss of appetite, nausea or vomiting, trembling, troubled breathing, unusual increase in sweating, unusual paleness, feeling of warmth, weakness and heart disease.
“Ephedrine has been a banned substance in both the Olympic Games and virtually all amateur competitions for many years. Recently, however, the NCAA became more concerned about ephedrine use in its member institutions because of a recent increase in positive ephedrine drug tests. In the December 1999 issue of the NCAA News, an increase in positive tests from ephedrine use by student athletes was reported (26). According to this article, the increase in positive tests is probably due to the increased consumption of "natural" products containing ephedrine-like diet aides, herbal products (Ma Huang), or energizing bars used to boost an athlete's energy levels
“Dietary supplements are not closely regulated by the Food and Drug Administration (FDA). In 1994, Congress passed the Dietary Supplement Health and Education Act (DSHEA), which defined dietary supplements as being distinct from drugs or food additives (21, 23). This act allowed lenient labeling requirements for dietary supplements. The manufacturers of these products do not need to provide the detailed nutritional information required by the FDA for foods and over the counter drugs. The DSHEA cleared the way for companies to market products that do not meet the strict, established definitions of a food or drug (21). As a result, manufacturers of ephedrine-containing supplements (such as Ma Huang) are not required to label the precise amount of ephedra in that product. Without this knowledge, the consumer may unknowingly face potential danger from overdose. In addition, many of these products are labeled as natural, which leaves the consumer with the false impression that they are inherently safe.
“The herbal form of ephedrine is Ma Huang. Remember that ephedrine consumed in the “natural,” herbal form has the same effect as that taken from prescription or from over the counter medicine. In fact, ephedra-laden supplements may actually be more dangerous. Several studies have looked at the concentration of ephedra in Ma Huang, the most common herbal form found in dietary supplements. Gurley et al. (21) examined the ephedra concentration in 9 commercially available supplements containing Ma Huang. The authors used a liquid chromatographic method for determining ephedra concentration in their laboratory preparations, and they demonstrated a tremendous variability in ephedra concentration for the 9 samples. For each of the 9 commercially available samples that were tested, the range of ephedra concentration was 1.08–13.54 mg. Only 3 of the products listed ephedra content on the label, and 1 particular sample exhibited lot to lot variations in ephedra of 137%. As demonstrated by this study, it becomes difficult to determine the exact amount of ephedra being consumed from supplements containing Ma Huang.
“Taking dietary supplements containing ephedrine should only be done after serious contemplation. In fact, the FDA is currently examining the effects of ephedrine consumption in these types of products. Between 1993 and 1997, the FDA examined notices of 34 deaths and about 800 medical and psychiatric complications directly linked to Ma Huang (15, 22). Several medical reports and case studies have recently been published documenting problems related to ephedrine consumption. Jacobs and Hirsch (22) reported 2 patients who experienced physical and psychiatric consequences when using Ma Huang–laden supplements. One patient reported suicidal and depression tendencies after taking Ma Huang regularly for 2 years to enhance his workout performance. The other patient experienced episodes of acute psychosis and paranoid-type behavior while performing his duty on board ship in the military service. This patient reported consuming Ma Huang–containing supplements to improve his fitness level for several months prior to exhibiting the psychological phenomenon. Both patients' conditions resolved after treatment and discontinued administration of the Ma Huang.
“Other documented reports have connected Ma Huang to physically related medical problems. Powell et al. (28) published a report on a patient who suffered from nephrolithiasis after taking an energy supplement containing Ma Huang for about 10 months. This particular patient presented for medical treatment with acute renal failure and complete mid ureteral obstruction caused by a kidney stone. Once the kidney stone was harvested, laboratory analysis confirmed that the stone was an ephedrine-based metabolite and had a similar profile as 200 other stones analyzed by this particular laboratory. To help further determine the composition of the stones, 8 samples were selected from this original group of 200 and further analyzed by gas chromatography/mass spectrometry. The authors confirmed that ephedrine, norephedrine, and pseudoephedrine were the primary elements forming the kidney stones.
“Blau (11) reported the case of a 24-year-old man with left abdominal pain. The patient was admitted to the hospital while experiencing a ureteral obstruction. A medical history revealed that this patient took an average of 40–120 over the counter ephedrine tablets per day (25 mg of ephedrine per tablet) for several years. While in the hospital, this patient passed a stone and the specimen analysis revealed ephedrine. Since ephedrine excretion is primarily accomplished by the kidney (70–80% excreted unchanged in the urine), ephedrine abuse can drastically increase renal load (7, 11). In another case of ephedrine abuse, Nadir et al. (25) reported a case study from a patient with severe, acute hepatitis due to Ma Huang consumption. Other reported and published complications include hypertension, dysrhythmias, myocardial infarction, myocarditis, seizures, and stroke (28, 36).
“From 1993–1997, the FDA received numerous reports of medical and psychiatric complications directly related to Ma Huang consumption (15, 22). Because of these complaints, the FDA promoted a proposal to establish guidelines that would help regulate the concentration of ephedrine permitted for sale in Ma Huang–containing dietary supplements. The guidelines included recommendations to (a) prohibit supplements containing 8 mg or more of ephedrine per serving; (b) require labels warning not to exceed 24 mg of consumption in a 24-hour period; (c) require labels warning against using ephedrine for longer than a 7-day period; and (d) prohibit combining ephedrine with other stimulants, such as caffeine (15). After review by the House Committee on Science and the Government Accounting Office (GAO), the FDA chose to withdraw its proposal and decided to continue collecting data and case reports from the public (17). Also, the Department of Health and Safety hosted a public meeting in early August 2000 to hear public comments concerning dietary supplements and ephedrine consumption (16).
“It is clear that the debate on the effectiveness and safety of over the counter drugs and dietary supplements containing ephedrine will continue. However, the research supports at least 3 conclusions. First, there seems to be enough laboratory evidence to question the effectiveness of ephedrine as an ergogenic aid. Second, reported weight-loss products containing ephedrine may be effective in weight management strategies for obese patients, but there is little, if any, evidence supporting their effectiveness in non-obese or lean populations. And finally, ephedrine consumption on a regular, extended basis may be a health hazard in certain individuals who are hypersensitive to the drug's effects or when potential interactions may occur with similarly acting over the counter or prescription medicines.
“Before using any dietary supplements containing ephedrine, pseudoephedrine, or Ma Huang, it is judicious to have a complete physical exam and consult with a physician or other health care provider concerning potential health risks or drug and prescription interactions. As exercise and fitness professionals, it is our professional responsibility to educate our clientele about the potential risks and benefits concerning these products and attempt to help these individuals establish the safest and healthiest lifestyle possible.”
Legal Implications
In 1997, 60 million Americans spent $3.24 billion on herbs for reasons such as migraines, hypertension, depression, weight loss, and sexual stamina. An estimated 15 million adults are at risk for potential herb-drug interactions.
Ephedrine is now illegal in a growing number of countries including Australia, Canada and some European countries. Ephedrine is also illegal in a growing number of states such as New York, Ohio and California. The reason for the ban is due to the hundreds of ephedrine related deaths worldwide. It is the opinion of this author that the movement for the ban of ephedrine is a positive step that will educate consumers and save lives. While the FDA (Food and Drug Administration) does not directly regulate ephedrine, it urged the United States Congress to consider a national ban on the drug primarily because of its use by teenagers to be an alternative to ecstasy. Ephedrine is also banned in the International Olympic Committee, the NFL and the NCAA.
A law known as the Dietary Supplements Health and Education Act or "DSHEA," prevents the FDA from regulating these products. Prior to the DSHEA, dietary supplements were in regulatory limbo. The FDA claimed it had the power to regulate them and tried to make the manufacturers and suppliers prove their safety claims for their products.
The DSHEA reduced the FDA's and federal control over these products, compared with food and drugs, which are subjected to strict regulation and compliance monitoring by the FDA. Under the DSHEA, dietary supplements like ephedrine are loosely defined as products intended to supplement the diet. These supplements contain herbs, minerals, amino acids, vitamins and combinations of these things. The supplement industry can sell any product that meets that definition in stores and its supplier can make claims about its alleged healthful qualities. Thermogenesis – Beta Agonists
In recent years, a class of drugs known as thermogenic agents has been introduced to the athletic community. In order to understand the essence of thermogenic agents, the process of thermogenesis must first be understood.
Thermogenesis is the biochemical term applied to the physiological state where the body converts excess calories into heat rather than storing them in adipose tissue. Therefore, thermogenic agents work to increase thermogenesis and stimulate adipose tissue to release stored triglycerides into the blood stream, making them available for b-oxidation. Thermogenic agents belong to the class of drugs known as stimulants. These drugs include caffeine, ephedrine, clenbuterol, epinephrine and cocaine.
For further reading on thermogenesis, read Thermoregulation: Physiological Responses and Adaptations to Exercise in Hot and Cold Environments. For further reading on fat metabolism, read Metabolic Primer Part II – A Comprehensive Discussion on Fat Metabolism and Essential Fatty Acids - An In Depth Analysis.
Epinephrine is also known as adrenaline. Epinephrine is a hormone secreted by the adrenal medulla of the adrenal glands. As epinephrine is a highly complex hormone, full investigation of its actions go further than the purposes of this investigation. Therefore, only epinephrine’s thermogenic effects will be discussed.
Adrenal Medulla
The adrenal glands are two endocrine glands in one and are located above the kidneys. The adrenal glands prepare the body to fight stress.
The adrenal complex houses both adrenal glands, the outer being the adrenal cortex, the inner being the adrenal medulla.
The adrenal medulla is a part of the sympathetic nervous system and is essentially a modified sympathetic ganglion. The activation of the sympathetic nervous system is directly linked to the hormones produced by the adrenal medulla.
Chromaffin cells (secretory cells of the adrenal medulla) contain vesicles filled with epinephrine (E) and norepinepherine (NE). Collectively, these two hormones are referred to as catecholamines and are synthesized from the amino acid tyrosine. The chemical process looks like this:
Endorphin is also secreted by the adrenal medulla. Endorphin has an anti-stress analgesic effect, meaning it can ease the feeling of pain.
The adrenal cortex is the source of corticosteroid hormones. The adrenal cortex can be broken up into three zones, and each zone secretes a different hormone.
ZONE 1 – The outer zone, zona glomerulosa, secretes aldosterone. Aldosterone is a mineralocorticoid and is involved in the regulation of sodium and potassium, blood pressure, and blood volume.
ZONE 2 – The middle zone, zona fasciculata, secretes glucocorticoid hormones, primarily cortisol. Cortisol regulates the metabolism of glucose. We’ll be discussing cortisol in depth in a later issue.
ZONE 3 – The inner zone, zona reticularis, secretes sex steroids such as androgens (chiefly de-hydro-epi-androsterone – DHEA) and small amounts of estrogen and progesterone.
Epinephrine has special properties that allow it to act as both a hormone and a neurotransmitter, which allows the endocrine system and nervous system to work synergistically as the body’s primary control and communications network. When the adrenal medulla is stimulated by the sympathetic nervous system, approximately 80% of its secretion is epinephrine and 20% is norepinephrine. Plasma norepinephrine levels increase markedly at work rates above 50% VO2max. But the epinephrine level does not increase significantly until the exercise intensity exceeds 60% to 70% of VO2max. This is the primary reason High Intensity Interval Training (HIIT) is so effective.
Epinephrine is most famous for producing the “fight or flight” effect. This is the autonomic-nervous system response, which enables the body to cope with a potentially dangerous situation. Dependant on the fight or flight actions, the body’s nervous system activates into overdrive and stimulates massive amounts of adrenaline, which is then quickly transported through the blood. Epinephrine, in turn, produces physiological effects, which are experienced within microseconds of its secretion. These effects include increased heart rate, sweating and feelings of tension. Adrenaline also stimulates thermogenesis by mobilizing fat stores from adipose tissue, which is designed to provide an adequate supply of available energy in case it is needed.
It is no mystery that epinephrine is released during exercise, and it is suggested that exercise-related fat loss is highly dependent on adrenaline. To date, there are two observed mechanisms of action for epinephrine to initiate thermogenesis. It can be a slow and controlled process involving systemic release, or it can take the form of direct innervation of the fat cells by the sympathetic nervous system.
Epinephrine binds to specific receptors on fat cells which produce metabolites called cyclic AMP (cAMP).
Cyclic AMP (cAMP)
Through mediation of G proteins, the binding of catecholamines and peptide hormones such as glucagon and gonadotropins results in the activation of the membrane enzyme adenylate (adenylyl) cyclase. This membrane enzyme converts adenosine triphosphate (ATP) into cAMP.
cAMP binds to a protein kinase, which in turn activates otherwise inactive enzymes by phosphorylating them (causing them to combine with phosphoric acid). The phosphorylated proteins then initiate the physiologic events associated with the actions of said hormones.
For example: Both the pancreas hormone, glucagon and the adrenal medulla hormone, epinephrine use this mechanism to increase the release of glucose from the liver. This creates a cascade of events that is so cool I have to bold it for you! These events result in an amplification (or magnification) of the hormones signals and effects. Thus, a single hormone molecule can form thousands of cAMP molecules, which in turn produce millions of phosphorylated enzymes, and they in turn form billions of glucose molecules – all within several seconds!
At the adipose tissue cell, the production of cAMP activates hormone-sensitive lipase. Once activated, hormone-sensitive lipase breaks down triglycerides into free fatty acids and glycerol. The free fatty acids are carried to the skeletal muscles where they undergo b-oxidation.
Some athletes feel as though natural production and manipulation of adrenaline is not sufficient to give them desired results. Therefore, synthetic epinephrine is injected. Supposed advantages of epinephrine supplementation include increased energy (especially around the normally lethargic pre-contest diet), and increased fat burning. However, like caffeine, epinephrine’s life-span is short-lived in the bloodstream. This simply means that athletes experience a hard “crash” after its effects wear off.
Side Effects of Supplementation
Athletes who rely on epinephrine supplementation for increased fat burning and energy are also running the risk of developing potentially severe heart problems associated with increased heart rate and blood pressure. These effects have been observed in healthy individuals as well as athletes with a pre-existing heart problem. Another cause for concern is the biofeedback mechanism. Like anabolic steroids, natural epinephrine levels will shut down if exogenous sources are taken. As soon as the external source (in the form of a supplement) is stopped, the body is left with little or no circulating epinephrine. It is conceivable that the athlete can destroy the entire fabric of the endocrine system due to the decrease in production of this hormone, as it affects so many other endocrine hormones that are essential to life.
Legal Implications
Pure, synthetic epinephrine is classified as a prescription drug. Possession of the drug without proper documentation is a federal offense, and possession with intent to sell is a mandatory prison sentence. The use of epinephrine and related drugs are banned by the International Olympic Committee and most all other sports organizations, and athletes are routinely tested specifically for this drug.
Clenbuterol
At the 1992 Barcelona Olympic Games, two US athletes tested positive for clenbuterol and were forever banned from competition. This drug is so dangerous, and its effects so severe, it is absolutely frightening.
Clenbuterol (also known as Clenasma, Cesbron, Contrapasmina, Contrasmina, Novegam, Pharmachim, Spiropent (mite), Ventipulmin, Ventolase, Monores and Prontovent), stimulates beta andrenoreceptors, which are located in the heart, lungs and skeletal muscles. Clenbuterol itself can be divided into two classifications – agonists and antagonists. Beta-2 agonists are used as bronchodilators in the treatment of asthma (very low levels - .02 to .03 mg/day – are found in some asthma medications). Beta antagonists are used as antihypertensive drugs. Both classifications are chemical modifications of adrenaline (epinephrine) and noradrenaline (norepinephrine).
Asthma medications containing clenbuterol are non-existent in the United States, as it is obvious that the drug is just too dangerous for wide-spread asthma treatment. In fact, clenbuterol is banned for both animal and human use within the US. Clenbuterol is most commonly found in the form as a constituent of aerosol cans, but tablet and liquid forms also exist. Clenbuterol can still be found in countries such as Germany, Austria, Mexico, Spain and Italy. The US equivalent to clenbuterol is a drug called albuterol, which is also extremely dangerous.
The primary action of clenbuterol (as mentioned above) is to stimulate beta receptors. It relaxes smooth muscle tissue surrounding the bronchioles. Clenbuterol can also mimic adrenaline, displaying the same thermogenic effects. The secondary effects of clenbuterol were discovered by accident and were first deemed as side effects because the results were not expected. Animals given clenbuterol in clinical trials experienced an increase in skeletal muscle, a decrease in body fat and increased energy levels. The mechanism of action required to display the aforementioned effects are not well understood in the scientific community; however, it is believed that clenbuterol increases protein utilization and RNA accretion. It should also be noted that clenbuterol’s anabolic effects are not sufficient to be deemed comparable to anabolic steroids.
One study conducted by L. Bonaventure and colleagues found:
“Clenbuterol induces hypertrophy and a slow-to-fast phenotype change in skeletal muscle, but the signaling mechanisms remain unclear. We hypothesized that clenbuterol could act via local expression of insulin-like growth factor I (IGF-I).”
These data show that muscle hypertrophy induced by clenbuterol is associated with a local increase in muscle IGF-I content. They suggest that clenbuterol-induced muscle hypertrophy could be mediated by local production of IGF-I.
Insulin-like Growth Factor-1 (IGF-1) (from Metabolic Primer Part III)
Hormones such as growth hormone (GH), insulin, and insulin-like growth factors (IGFs) promote protein anabolism and growth. Hormones profoundly influence protein metabolism. Thus, GH and insulin increase the uptake of amino acids and protein synthesis in certain tissues such as muscle and bone. The effects of GH are mediated by the IGFs (somatostadins), which are usually secreted locally by surrounding tissues. IGFs are responsible for fetal growth. The absence of GH or IGFs leads to a cessation of growth and dwarfism. Bone and muscle growth is particularly severely affected while growth of heart, nerve, and brain tissue is spared. IGF-1 closely resembles the pancreatic hormone insulin; however, they have receptors of their own and promote cell proliferation and protein synthesis in their target cells. IGF-1 and GH interact at the epiphyseal plate and through the liver to promote bone growth.
With regard to body fat, it is believed that clenbuterol increases the rate of lipolysis (the process by which fatty acids are converted to acetyl CoA and then later to ATP). Other evidence suggests that clenbuterol increases the rate of brown-adipose tissue thermogenesis. Another important discovery is that clenbuterol’s effects are time related. Rats being fed clenbuterol showed weight gain and increased protein synthesis in as little as 4 days. Conversely, clenbuterol’s growth-promoting abilities seem to be limited as the rats showed reduced weight gain after 21 days. It has been suggested that such factors as receptor desensitization and interaction with other hormones may account for this.
Many athletes, especially bodybuilders, use this drug commonly. In fact, its use in the sport of bodybuilding on both the professional and amateur levels is so widespread it is recognized as commonplace. As clenbuterol has a half-life of about 50 hours, it is commonly used heavily all the way up to 48 hours before a drug tested competition. The 50-hour half-life of clenbuterol is somewhat misleading, however, due to the fact that clenbuterol undergoes biphasic elimination. Common dosages are around 50 to 100 micrograms/day. Other reports suggest that athletes cycle clenbuterol on a one- to two-week on/one- to two-week off pattern in doses up to 140 mcg/day.
It is important to note that once a bodybuilder ceases clenbuterol use, most, if not all, muscle gains made while on the drug are lost.
Also of importance is drug interactions. Athletes who use clenbuterol are also likely to be using other drugs and anabolic agents at or around the same time. Its true effectiveness in humans cannot be scientifically verified because of this. Further, clenbuterol’s use in athletics has only become prominent in the 1990s, therefore the athletes taking clenbuterol now are still known as “first-generation users.”
Side Effects
The lightest side effects experienced by clenbuterol users include nausea, headaches, and insomnia – the three often being interrelated. Another side effect commonly observed is tachycardia, or excessively rapid heart beat, which can easily be fatal. Bodybuilders are especially at risk for developing tachycardia close to a contest due to the use of diuretics, which flush water and electrolytes from the body. Electrolytes are electrically charged ions and are integral parts of the cardiac and nervous systems. Clenbuterol speeds up the excretion of these minerals.
Although not conclusive, it is widely accepted that IFBB pro bodybuilder Mohammed Benaziza died from clenbuterol use.
More side effects have been observed, such as tremors, seizures, cardiac arrest, hemorrhaging, and extreme nervousness, paranoia and dementia. In many animal studies, clenbuterol has been shown to cause myocardial hypertrophy – an enlarging of the cardiac tissues of the heart – that causes vascular obstruction leading to death.
A recent study conducted by J. Burniston et al. concluded:
“These data show significant myocyte-specific necrosis in the heart and skeletal muscle of the rat. Such irreversible damage in the heart suggests that clenbuterol may be damaging to long-term health.”
Conclusions and Recommendations
In an earlier publication of the Journal of Hyperplasia Research, this author stated, “Warriors of the iron know these (bodily) systems well. We know their structure, their actions, and their importance. We are in complete control of our internal systems. We have the power to manipulate them to induce growth of massive proportions. We have the power, the will, the knowledge to control these systems, to maximize their efficiency, and to blast our bodies into pure, unhindered hyperplasia. This, fellow warriors, is the system behind bodybuilding.” To add to this, not only should athletes and bodybuilders be aware of the systems to be able to induce muscle growth, athletes should also be aware of how to keep these systems working properly and safe from damage. Therefore, it is essential that athletes understand the substances and drugs they are putting into their body to keep these systems functioning properly and optimally. It is the professional recommendation of this author that none of the substances discussed in the current investigation (ephedrine, epinephrine, and clenbuterol) should ever be used by an athlete wishing to maintain a safe and healthy lifestyle.
Researched and Composed by Joe “Yu Yevon” King Abstract
As a continuation to Supplement Guide Volume 1 – Ephedrine, Epinephrine, and Clenbuterol, this article will focus on other popular fat burning supplements, their mechanisms of action, dosages, side effects and recent research concerning the compounds. It is essential for all athletes to understand every facet of the compounds they are considering using. This way the athlete will be informed on what is occurring on a physiological level, which will allow the athlete to make an informed decision when choosing a fat burning or performance enhancing supplement.
Disclaimer: No specific products are mentioned in this article, it rests upon the athlete to read the labels of fat burning supplements for their ingredients to determine their effectiveness and the safety of the product.
Recommended reading in conjunction with this article for full comprehension of topics discussed:
Endocrine Insanity Part III
Energetic Transference Occurring in the Biosphere Part II: Anaerobic Energy Pathways
Thermoregulation: Physiological Responses and Adaptations to Exercise in Hot and Cold Environments
13 Weeks to Hardcore Fat Burning – The Diet
A comprehensive discussion on B-Complex & its relation to peak performance Hydroxy Citric Acid (HCA)
HCA was first introduced as a diet aid to treat clinical obesity; however, the bodybuilding community is experimenting with this compound for use in pre-contest preparation. HCA is obtained from the rinds of the Garcinia fruit found in southern Asia. HCA is unique from other appetite suppressors as it does not directly effect the central nervous system and works to prevent the conversion of carbohydrates into adipose tissue.
When carbohydrates are ingested, the liver converts much of it into blood glucose (As well as muscle and liver glycogen). The glucose is then facilitated into cells by insulin (for more on insulin, read Endocrine Insanity Part III). When necessary, the body converts the stored glycogen back into glucose and can further be broken down into smaller subunits in the Kreb’s Cycle, also known as the Citric Acid Cycle (for more on the Kreb’s Cycle, read Energetic Transference Occurring in the Biosphere Part II: Anaerobic Energy Pathways). If excess glucose is available and is not needed by the body, it will be converted into fat via lypogenesis. The final step of glycolysis (the breakdown of glucose) takes place in the mitochondrial matrix. Citrate is produced and is then transferred outside of the mitochondrial matrix and into the cytoplasm to be broken down even further. It is at this stage where HCA comes into play.
In order for the citrate to be broken down, the enzyme ATP citrate lipase must be present. If HCA is present as well, it will block the activity of the enzyme, thus altering the body’s fat metabolism in several ways.
1. The pathway for glycogen production becomes more accessible.
2. The body will begin to metabolize more stored fat as energy due to the decrease in fat production.
3. Pyruvate, the substance that enters the mitochondrial matrix to be converted into citrate, will be either completely metabolized in the Kreb’s Cycle or is recycled as lactate and phosphoenolpyruvate.
As a result, HCA will also indirectly suppress appetite because the body “thinks” there are plenty of substrates available.
It is important to understand that HCA is still a relatively new supplement and its effectiveness is still somewhat unclear. More research must be conducted to confirm or deny its effects. Dosages
It is recommended that HCA be taken 30 to 60 minutes before meals. The recommended dosage is 1000 milligrams (1 gram) 2 to 3 times daily. Most over the counter products containing HCA only contain about 250 milligrams of the compound, but also include ephedrine. This creates a very poor situation for the athlete wanting to supplement with HCA. Ephedrine should be avoided at all times by any athlete, however HCA is primarily only found in products also containing ephedrine. It would be wise of supplement companies to develop supplements containing only HCA as the active ingredient. Side Effects
Given this products relatively short time on the market, it may be too soon to tell whether or not this compound is completely safe. Moreover, since it is commonly packaged with ephedrine, it is difficult to isolate the compound in anecdotal reports. However, few side effects have been reported in clinical trials. Some individuals may experience nausea, especially when taking the compound on an empty stomach. More alarming is the clinical tests conducted on animals. A major pharmaceutical company conducted preliminary research on HCA in an effort to market it as a weight loss supplement under their label. The project was abandoned due to adverse side effects observed in laboratory animals, including testicular atrophy and other toxicities. However, it is still unknown if these same effects are observed in human subjects.
Further, a California based supplement company has been ordered by the state to cease production and marketing of the product under the claim that it promotes weight loss until credible scientific evidence is presented to support their claims. Inosine
Inosine was first introduced in the mid 1980s. Inosine belongs to the family of nucleotide molecules called purines (non-protein nitrogen compounds). Together with pyrimidines, purines make up the nitrogen bases, which are the building blocks of DNA. The famous chemist, Dr. Liebig, isolated this compound in the 1840s and was originally thought to be another waste product of the body’s metabolism. It wasn’t until the 1970s when Japanese researchers found inosine plays a crucial role in lipolysis.
Inosine has been shown to maintain ATP levels in bone marrow while enhancing cardiovascular function. The exact mechanism of action, however, is still somewhat unknown. Inosine has been observed to increase blood flow to the heart and increase the contraction strength of the ventricles in some studies. It is believed that inosine can readily diffuse through cell membranes and trigger the release of oxygen from red blood cells and increase their oxygen-binding capacity, meaning more oxygen is extracted from the lungs and is made available for cellular respiration. Therefore, inosine has been used in clinical settings for years to treat heart and kidney disease.
Inosine may also affect lipogenesis under certain unique conditions, such as when the body’s ATP and O2 stores are abnormally low. In these conditions, inosine may help to maintain normal metabolic reactions through the triggering of key enzymes.
In athletics, inosine was first used by Soviet athletes long before it was introduced to the west. Many anecdotal reports suggest that an “energy kick” similar to that of ephedrine is experienced about 30 minutes after ingesting the compound. As of late, it is unclear as to whether this is a placebo effect or if there is a biochemical explanation for this phenomenon. At this juncture, it would be premature to suggest that the reported “energy kick” is anything other than a placebo effect.
Some investigations suggest that inosine may not enhance performance at all and, in fact, will actually decrease performance. A study conducted by Old Dominion University revealed no ergogenic effect of inosine on aerobic endurance. Nine highly-trained runners consumed either a placebo or 6 grams of inosine prior to several performance tests, including a peak oxygen uptake test and a 3-mile run on a treadmill conducted to simulate maximum effort. Although there were no differences in the 3-mile run performance between groups, peak oxygen uptake, or a variety of hematological and psychological variables, time to exhaustion during the peak oxygen uptake test was longer in the placebo condition. It is speculated that inosine may impair the ability of fast-twitch muscle fibers to function optimally in very high-intensity exercise.
Recent research at Ball State University revealed similar findings. Starling and colleagues investigated the effect of 5,000 milligrams of inosine daily for five days on the performance of competitive male cyclists on three tests: a Wingate bike test, a 30-minute self-paced cycling performance test, and a supramaximal cycling sprint to fatigue. No significant difference was found between groups with the exception of impaired performance observed in the supramaximal test following inosine supplementation.
McNaughton and colleagues conducted a double-blind, placebo, cross-over study using inosine supplementation on trained cyclists. The subjects consumed 10 grams of inosine daily for 10 days, with a 6-week washout period between trials. Subjects were tested at baseline, after 5 days, and after 10 days on three cycling-performance tests designed to measure different energy pathways. The first test included five repetitions of a 6-second sprint; the second test was a 30-second sprint; and the last test was a 20 minute time trial. Inosine supplementation had no effect on any test.
Dosages
In clinical treatment settings, inosine is given via a intramuscular injection in standard dosages of 250 milligrams 2 to 3 times daily. Recently, oral tablets and liquids have been produced; however, no studies evaluating their effectiveness have been conducted (despite what supplement companies advertise). Oral dosages range from 800 to 4000 milliliters a day. However, as a general rule, the proper dosage is about 8 to 10 milligrams per kilogram of bodyweight.
Many supplement manufacturers attempt to fool the consumer by combining inosine with other compounds. This effectively renders inosine useless. The only active form of inosine is its pure nucleotide form. Other forms such as inosine-5-monophosphate have been shown to be inactive in medical studies. Many other versions are also available and placed into popular fat burning supplements. Anything other than pure inosine is virtually useless.
Athletes find inosine most useful when taken 30 minutes prior to activity; however, medical research indicates that inosine is metabolized extremely quickly. In fact, some studies suggest that inosine is almost completely metabolized within seconds of coming in contact with the bloodstream. More research needs to be conducted, but if the current literature is correct (and this author believes they are well on the right track), then inosine may be completely useless for athletes.
Side Effects
Due to its rapid degradation, few side effects have been reported in the last 20 years of its use by athletes. However, as stated above, it may also be totally ineffective. However, those who suffer from gout should not take inosine. Gout is a form of arthritis, which develops when too much uric acid is produced, or when the kidneys fail to remove enough uric acid. Gout is specifically caused when uric acid combines with sodium to form sharp crystals called sodium urate salt, which then settles in the body’s soft tissues causing pain and inflammation. Uric acid is one of the metabolic products of purines and supplementation of inosine will further aggravate this condition. Another side effect of elevated uric acid levels are kidney stones. Evidence suggests that individuals who develop kidney stones are at a greater risk of obtaining kidney disease. Therefore, individuals with any type of renal disease must completely refrain from ingesting inosine.
Choline
Choline has been used by athletes for years, most commonly in a stack with inositol. Like many other compounds peddled by manufacturers, there is little scientific research dedicated to choline and its benefits for athletes.
Choline is a member of a class of biocompounds known as phosphoglycerides and is a member of the B-complex group of vitamins. For more on B-complex vitamins, read A comprehensive discussion on B-Complex & its relation to peak performance. Among choline’s apparent functions are the building of cell membranes, fat mobilization, decrease in cholesterol levels (via increasing cholesterol utilization), assisting the liver to metabolize triglycerides and the manufacture of phospholipids. Choline may also assist in the preservation of the tissues of the liver and kidneys by combining with free form fatty acids and phosphoric acid to form lecithin.
Another possible role of choline is to boost the integrity of myelin sheaths – insulation covering the body’s nerves. Without myelin sheaths, nerve impulses would “short circuit,” leading to a myriad of physiological dysfunctions, the most well known being multiple sclerosis. Choline, when combined with vitamin B5, works to produce the neurotransmitter acetylcholine, which plays an integral role in muscle contraction and cognitive functions such as alertness and memory. The research linking choline and memory has been pioneered by Dr. Richard Passwater, who noted in his book The New Supernutrition that college-age students supplementing with choline had significantly higher abilities to recall word sequences. However, it still remains unclear whether choline actually directly enhances memory or whether the increased alertness allows for better memorization. As suggested earlier, these results can be exemplified when choline is combined with vitamin B5 (pantothenic acid). Venom describes vitamin B5 in the aforementioned article:
“Pantothenic acid is derived from the Greek word pántothen, meaning "from all quarters," and as its name depicts, it is found present in virtually all plants and animal foods, hence, deficiency is not likely. It is part of the chemical makeup of Coenzyme A. It is also known in other forms -Calcium Pantothenate, Pantothenate, and Panthenol [74,63].
“Digestion This vitamin occurs mainly as coenzyme A. It is primarily absorbed in the small intestine via passive diffusion. Transportation in the heart, muscles, and liver cells is done by a sodium active transport. Within the central nervous system, adipose, and renal uptake, facilitative diffusion is used [74,42,12].
“Function Synthesis of CoA is dependant on Pantothenic acid. As discussed throughout this article, CoA is used in many reactions. Such as the kreb cycle, and production of energy from carbohydrates, proteins, and lipids. It also assists metabolism of certain drugs, skin, and steroids. Studies have show than Vitamin b5 may accelerate the normal healing process after surgery [78,76,75]. Here is one study by Taherzadeh MJ [73] “Physiological effects of deficiency of pantothenate, a necessary precursor in the synthesis of coenzyme A, were studied… the time required for complete conversion of the glucose decreased by 40%. Acetate addition affected the acetate and glycerol yields in a similar way in pantothenate-rich medium”
“Deficiency Deficiency usually occurs with people who are severally malnutritioned, along with alcoholics, diabetics, and certain bowel diseases. Side effects are vomiting, fatigue, weakness, and a burning feet syndrome, characterized by abnormal skin sensations [33,7,6,69].
“Recommendation The DRI recommends 5 mg a day for adults. For certain conditions such as pregnancy, 7 mg’s a day is recommended. Concerning side effects, intakes of 100 mg a day for Vitamin b 5 may increase niacin excretion. 10 g a day (besides niacin excretion) has exhibited no side effects. 20 g a day may cause some intestinal distress, and diarrhea. Pantothenic acid can be found in egg yokes, legumes, whole grains, mushrooms, broccoli, avocados, and several plants and meats [113,77,69,7,6].”
Dosages
The body synthesizes limited amounts of choline, therefore supplementation may be necessary. However, it is important to note that only moderate success has been observed from choline supplementation as opposed to the amazing and far-fetched claims that manufacturers give the compound.
Choline is best utilized when consumed in dosages of about 3000 milligrams a day when taken with 1000 milligrams of vitamin B5.
Side Effects
As choline is not a very active compound, and is essential for the body anyway, few side effects have been reported by researchers. Some clinical evidence recommends that people inflicted with depression, especially manic depressives, should not supplement with choline, as it may intensify their depressive episodes. It is unclear if choline will cause a relatively healthy person to develop depression.
Dr. Franco Columbu, legendary bodybuilder, comments on choline in his book The Bodybuilder’s Nutrition Book:
“As a bodybuilder, I have focused particular attention on vitamins playing a significant role in the metabolism of nutrients needed for building muscle and gaining definition. Choline is one of these.”
Inositol
Inositol is known as one of the original fat burning compounds and is still found in many fat burning products today. A deficiency of this naturally occurring compound may lead to an accumulation of fat inside the liver, as it aids the liver in metabolizing fat. In addition to this, inositol acts as a messenger, transmitting various hormonal signals within cells. When hormones bind to cell walls, inositol is involved in the extensive messenger relay that helps inform the cell what to do. This is an essential part of hormone recognition and action. However, supplementation of inositol may not enhance its effects, nor will it significantly promote weight loss. Although no recent studies suggest supplementation with inositol is harmful, there are no apparent benefits from its use.
Carnitine
Carnitine was first discovered in the early 1900s by Russian scientists. After over 90 years of research, carnitine has still not been definitively classified. Most biochemists include carnitine as a trimethylated amino acid; others, however, claim carnitine as an “accessory nutrient.” A few scientists still, suggest that carnitine is actually a stable member of the B-complex vitamin group. Whatever the classification, carnitine is water-soluble and synthesized in the liver, which requires the presence of other nutrients including vitamin C, B6, B3 and iron.
Carnitine’s primary mechanism of action is to stimulate the transport of long chain fatty acids across the inner membranes of mitochondria. It does this via the activation of an enzyme called carnitine acyltransferase (CAT1) which transfers one group of the fatty acid molecule (the fatty acyl group) to the hydroxyl group of the carnitine molecule. The resultant product is called O-acyl carnitine ester and is able to pass across the inner mitochondrial membrane. Here it is cleaved by another carnitine acyltransferase (CAT 2). The end result is ATP and is used as an immediate fuel source. Another effect of carnitine is to enhance the intake of oxygen into cells. The result is a greater availability of oxygen for the cells in times of stress, as in during workouts.
Carnitine is found naturally in meats (especially beef) and is also synthesized within the body from the amino acids lysine and methionine. Carnitine exists in two basic forms, “L” and “D” (left and right handed isomers, which rotate clockwise or counterclockwise). The body cannot use the “D” form of the molecule. Not only is the “D” form not utilized, but it may actually inhibit the effectiveness of the “L” form. Thus, it is essential that the “D” form of the molecule is not consumed.
90% of carnitine in the body is located in skeletal muscle where it is a part of the enzyme carnitine palmitoyl transferase, which is important in the transport of fatty acids into the mitochondria for oxidation. There is some evidence available which states that since carnitine facilitates the oxidation of pyruvate, it will also enhance the utilization of glucose and reduce the production of lactic acid during exercise while simultaneously increasing blood flow both during exercise and during rest, which will enhance the delivery of both oxygen and energy substrates to the muscle. However, in some studies, carnitine has been reported to expediate the oxidation of branched-chain amino acids, leading to premature fatigue.
Dosages
Manufacturers commonly package carnitine in 250 milligram tablets. However, it is important to note that on average, only 67% of the tablet is actually carnitine, with the rest being the tartate part of the compound. This author recommends taking 1000 milligrams of carnitine both before and after a workout to observe the greatest effects.
“New” Carnitine - ALCAR
Aside from the “L” form and the less common “D” form, there is a new manufactured form of carnitine on the market, known as Acetyl-L-Carnitine (ALCAR). It is also important to note that there is an additional form of carnitine – L-propionylcarnitine. It is suggested that ALCAR is more bioavailable than L-carnitine alone. It may be more beneficial to supplement with ALCAR than standard L-carnitine. The acytylization of carnitine occurs in the brain, liver and kidneys. ALCAR also plays a variety of roles in the body, including increasing acetylcholine production and stimulation of protein and membrane phospholipid synthesis.
Additionally, carnitine is a potent antioxidant (especially in combination with ALA) and has been used in clinical settings to help treat heart disease, Parkinson’s disease and even Alzheimer’s disease. One reason for this is due to carnitine’s ability to prevent oxidation and inflammation. Carnitine has also been found to reduce lipid peroxidation prevents or reverses many age-related increases in markers of oxidative and inflammatory events in the cortex, reduces damage to nucleic acids (DNA/RNA) and proteins, and also increases the levels of other antioxidants in the brain. Carnitine may also prevents mitochondrial decay, and restore the activity of many key enzymes that decline with age such as carnitine acetyltranferase, mitochondrial complexes III and IV, sodium potassium adenosine triphosphatase, and glutathione-S-transferase. Carnitine supplementation is also accompanied by many structural changes in the brain in both the young and the old. It stimulates nerve growth factor (NGF) binding, and rodent studies indicate significantly more regenerative elements and reduced degenerative elements.
Dexfenfluramine (Ponderal)
This fat burning agent is a modified form of the drug fenfluramine. This amphetamine derivative is unique as it may not be as addictive as other amphetamines. Manufacturers also claim that, unlike other amphetamines, it does not adversely affect the CNS, however medical science suggests otherwise. The drug is a very popular fat burner in Europe, but has been banned by the FDA for use in the United States. It is also banned in Canada. The driving reason behind its ban is its fatal effects and the onset of heart defects primarily observed in women.
Dexfenfluramine acts as an appetite suppressor by reducing natural levels of the neurotransmitter serotonin. Dexfenfluramine also has thermogenic properties and in this regard it has been compared to ephedrine and other beta agonists. Closely related to its thermogenic properties is dexfenfluramine’s effect on blood lipids. The drug has been found to lower circulation of both high and low density lipoprotein levels by inhibiting specific catecholamines such as epinephrine and norepinephrine. Dexfenfluramine has also been found to reduce insulin resistance.
Side Effects
The most frequently reported side effects are dry mouth, increased urination, diarrhea and drowsiness. Dexfenfluramine has much more serious adverse effects, which include sometimes being able to mimic the effects of antihypertensive and hypoglycemic drugs, which can easily be fatal in healthy athletes. If any decreases in exercise tolerance are observed, then medical attention must be sought immediately. Other side effects include pulmonary hypertension (which can easily lead to a heart attack or stroke) and depression.
Beta-3-Adrenergic Agonists (B3AA)
B3AAs are the compounds that researchers are investigating today, specifically to treat obesity. Researchers have uncovered a receptor that promotes the oxidation of adipose deposits when stimulated. Pending further research, B3AAs may hold the key to the next generation of fat loss supplements.
There are two basic types of adipose tissue found in mammals – white (WAT) and brown (BAT). WAT plays a major role in the storage of triglycerides for energy while BAT is the major site of energy dissipation in the form of heat, or thermogenesis. Brown fat and its relation to thermogenesis was discussed briefly in Thermoregulation: Physiological Responses and Adaptations to Exercise in Hot and Cold Environments:
“Brown fat can aid in increasing internal temperature, as it produces a large amount of heat during ß-oxidation. In brown fat, mitochondria density is high and oxidizes the fat in such a way as to produce a great deal more heat than ATP. Brown fat is predominantly found in younger animals and humans, but some adults may keep brown fat after adolescence.”
BAT accomplishes its thermogenic abilities through the use of a series of receptors called Beta (ß) = adrenoreceptors. There are at least three types of ß receptors, ß1, ß2 and ß3. ß1 and ß2 receptors are present in the heart, lung and blood vessels. However, it is the ß3 receptors that will be discussed within the context of this topic. The ß3 receptor was discovered in 1984 when studies on BAT suggested that an atypical adrenoreceptor was present in brown adipose tissue. Studies suggest that stimulation of ß3 receptors may be the key in combating obesity.
Once ß3 receptors were found and classified, their role in lipolysis was investigated. Japanese researchers were on the forefront of the research in the early 1990s. Their work with rats concluded that chronic treatment with the ß3 agonist arotinolol increased BAT-tissue content of DNA and total protein, both of which will increase the capacity of BAT thermogenesis.
Potential Causes for Concern
Use of B3AAs in athletics has thusfar been very limited, as it is still in the preliminary stages of research. However, it is important to note that B3AAs are closely tied to the well-known ß2 agonist – clenbuterol.
Thiomucase
Unlike most fat burners, thiomucase is not an oral supplement, rather it is applied as a cream (this is the most common version, although oral and injectable versions are available, they are very rarely used). Thiomucase is called a “spot reducer” by manufacturers. It is important to note that there is no such thing as spot reducing, therefore the use of this supplement is completely ineffective as the entire premise for it is based on myth. It is said that thiomucase will not stimulate the utilization of fat in the area over which it is applied, rather it will release the fluid contained within the adipose tissue, thereby shrinking the fat cell.
Thiomucase is a popular supplement that can only be obtained online within the United States, as the FDA has not approved the drug. It is available in Europe, however, with France being the largest supplier. This author strongly cautions against obtaining this drug within the United States, as it is classified as an illegal substance and individuals caught with the drug have and will be charged with drug smuggling. It is ironic that such harsh penalties can be given to an individual in possession of a drug that does not even work.
The Best Fat Burner Ever Found – GLV (Green Leafy Vegetables)
The best fat burner available today is GLV. Adam Knowlden discusses this miracle supplement:
“My favorite fat burner is GLV. Short for Green Leafy Vegetables, a potent fat burner. Try stacking, Asparagus, Broccoli, Brussel Sprouts, Cabbage, Green Beans, Lettuce, and Zucchini!
“Not only is the price of this stack economical, but a steady diet of GLV's will increase your insulin sensitivity, destroy cancer and all types of diseases, and increase your body building lifestyle in inumerable ways!”
The president of ABCbodybuilding.com and the Journal of Hyperplasia Research, Jacob Wilson, agrees:
“It has been proven that a diet moderate in highly fibrous carbs can increase insulin sensitivity in the muscle cells. Which is why we will stick with foods such as oatmeal, and fibrous green vegetables. The reason for this, is that your body will not overproduce insulin in response to these slow burning carbohydrates. Remember, the less fiber and the more processed the food you eat is, the more likely you are to cause an overproduction of insulin, because of how quickly the food is digested. If you continually do this, your muscle cells will become more and more resistant to the effects of insulin. However, the opposite also holds true. Your cells will become more and more sensitive when exposed to slower burning carbs.” For more on Jacob Wilson’s rationale, read 13 Weeks to Hardcore Fat Burning – The Diet.
Conclusion
Fat burning supplements are the most highly sought after supplements on the market today. Athletes, particularly wrestlers and bodybuilders (but not excluding most other sports), desperately seek to find a quick and easy way to decrease fat deposits while maintaining or increasing muscle mass simultaneously. However, most athletes fail to realize that supplements are just that – supplemental. Supplements should never take the place of a solid diet and workout plan. If the diet is not in order, then no supplement will yield the desired results. It is unfortunate that many athletes choose to risk their overall health and well-being to achieve a “quick fix” from a supplement. This will only lead down a path of destruction, both physically and mentally.
