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| ====== Introduction ====== | ====== Introduction ====== | ||
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| - | Fat loss supplements are products, most commonly taken orally, designed to burn fat by speeding up your body’s metabolism to aid in the ultimate goal of improving the health of people consuming them.<sup>[1]</sup>. The most common ingredients found in weight loss supplements include: bitter orange, caffeine, calcium, green coffee bean extract, green tea extract, guar gum, pyruvate, raspberry ketones, and white kidney beans.<sup>[2]</sup> | + | Fat loss supplements are products, most commonly taken orally, designed to burn fat by speeding up the body’s metabolism to aid in the ultimate goal of improving the health of the person consuming them.<sup>[1]</sup>. The most common ingredients found in weight loss supplements include: bitter orange, caffeine, calcium, ephedrine, green coffee bean extract, green tea extract, guar gum, pyruvate, raspberry ketones, and white kidney beans.<sup>[2]</sup> |
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| ===== Prevalence in the 21st Century ===== | ===== Prevalence in the 21st Century ===== | ||
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| - | Weight loss supplements is a go to as obesity rates continue to follow an increasing trend worldwide, with predictions stating that by 2025 about 1/5 adults will be obese.<sup>[3]</sup> Since the number of obese and overweight Canadians has increased, the market for weight loss products has also increased as more Canadians are turning to these health products. These health products can be purchased at pharmacies, health food stores, grocery stores, and online.<sup>[4]</sup> | + | Weight loss supplements are go to as obesity rates continue to follow an increasing trend worldwide, with predictions stating that by 2025 about 1/5 adults will be obese.<sup>[3]</sup> Since the number of obese and overweight Canadians have increased, the market for weight loss products has also increased as more Canadians are turning to these health products. These health products can be purchased at pharmacies, health food stores, grocery stores, and online.<sup>[4]</sup> |
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| ===== What is the market for these products? ===== | ===== What is the market for these products? ===== | ||
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| - | By 2019, it is expected that the global weight-loss markets will exceed $206 billion. In Canada the weight loss market provides a revenue of $235 million with an annual growth rate of 2.0%. Although the rates of obesity have had a long-term increase, the weight-loss markets in comparison have not increased as dramatically.<sup>[5]</sup> According to a survey conducted by the Heart and Stroke Foundation in 2010, when comparing to other age groups, young Canadians are the age group to spend the most on losing weight. In that survey, it was found that about 34% of young Canadians would spend over $500 on weight-loss supplements.<sup>[6]</sup> | + | By 2019, it is expected that the global weight loss markets will exceed $206 billion. In Canada the weight loss market provides a revenue of $235 million with an annual growth rate of 2.0%. Although the rates of obesity have had a long-term increase, the weight-loss markets in comparison have not increased as dramatically.<sup>[5]</sup> According to a survey conducted by the Heart and Stroke Foundation in 2010, when comparing to other age groups, young Canadians are the age group to spend the most on losing weight. In that survey, it was found that about 34% of young Canadians would spend over $500 on weight loss supplements.<sup>[6]</sup> |
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| ===== Are there risks associated with the products? ===== | ===== Are there risks associated with the products? ===== | ||
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| There are associated risks with using such products and these vary based on: the ingredients that the product is composed of, whether the product should be used in combination with other products, and also the age and health status of the person.<sup>[4]</sup> | There are associated risks with using such products and these vary based on: the ingredients that the product is composed of, whether the product should be used in combination with other products, and also the age and health status of the person.<sup>[4]</sup> | ||
| - | Weight-loss supplements can be harmful as they can pose various side effects but also it is most likely that the ingredients within the supplements can interact with one another and with other medications a person may be taking. It is often the case that ingredients are tested individually but not in combination to see their combined effects on the person.<sup>[2]</sup> | + | Weight loss supplements can be harmful as they can pose various side effects but also it is most likely that the ingredients within the supplements can interact with one another and with other medications a person may be taking. It is often the case that ingredients are tested individually but not in combination to see their combined effects on the person.<sup>[2]</sup> |
| There is also the possibility of fraudulent and adulterated products in which some prescription drug ingredients and substances may be included in the supplements but not be listed on the product label thus putting the consumer at risk.<sup>[2]</sup> | There is also the possibility of fraudulent and adulterated products in which some prescription drug ingredients and substances may be included in the supplements but not be listed on the product label thus putting the consumer at risk.<sup>[2]</sup> | ||
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| ===== Are they regulated? ===== | ===== Are they regulated? ===== | ||
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| - | In terms of regulation of these weight-loss supplements the Food and Drug Administration (FDA) does not test or approve them but instead lets manufacturers decide whether they are safe. If it is found that a supplement is unsafe the FDA will then remove it from the market.<sup>[2]</sup> | + | In terms of regulation of these weight loss supplements the Food and Drug Administration (FDA) does not test or approve them but instead lets manufacturers decide whether they are safe. If it is found that a supplement is unsafe the FDA will then remove it from the market.<sup>[2]</sup> |
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| ===== Additional Information ===== | ===== Additional Information ===== | ||
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| The use of supplements may give the user hope that they are attaining their goal and may choose to reward that with culinary pleasure. They may depend on the supplements entering a cycle of excessive supplement use and poor diet.<sup>[9]</sup> | The use of supplements may give the user hope that they are attaining their goal and may choose to reward that with culinary pleasure. They may depend on the supplements entering a cycle of excessive supplement use and poor diet.<sup>[9]</sup> | ||
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| ====== Caffeine ====== | ====== Caffeine ====== | ||
| Caffeine is viewed as the World’s most popular drug. | Caffeine is viewed as the World’s most popular drug. | ||
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| - | <box width classes round white centre| **Chemical Structure of Caffiene**> {{:caffeine-chemical-structure.jpg|Chemical structure of Caffeine}}</box| Figure 3: Caffeine and adenosine have similar molecular structure allowing them to form an antagonistic relationship. When caffeine binds to adenosine receptors, adenosine is not able to bind, and the adenosine receptors are antagonized[[https://caffeineandyou.wordpress.com/in-the-body/|.> | + | <box width classes round white centre| **Chemical Structure of Caffiene**> {{:caffeine-chemical-structure.jpg|Chemical structure of Caffeine}}</box| Figure 1: The molecule of caffeine. Caffeine is an alkaloid meaning it contains mostly nitrogen atoms. The formula is C8H10N4O2.> |
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| ===== What is it? ===== | ===== What is it? ===== | ||
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| - | It is consumed in coffee, tea, energy drinks, pill form, cold medications and many other products.<sup>[10]</sup> It is a powerful stimulant that is found in coffee beans or synthesized in a laboratory. Individual’s use caffeine to enhance their endurance and physical strength, and it has also been proven to assist in weight loss.<sup>[11]</sup> Nootropic drugs, are identified as those that are used to enhance memory of other cognitive functions. Caffeine is classified as a Nootropic as another one of its effects on the human body is sensitizing neurons and providing mental stimulation.<sup>[12]</sup> An individual that is consistently consuming caffeine will develop a tolerance to its effects.<sup>[13]</sup> When this occurs often the only benefit the consumer will experience is the anti-sleep effect. If the user were to take a break from caffeine the sensitivity to caffeine will increase again.<sup>[11]</sup> | + | Caffeine is consumed in coffee, tea, energy drinks, pill form, cold medications and many other products.<sup>[10]</sup> It is a powerful stimulant that is found in coffee beans or synthesized in a laboratory. Individual’s use caffeine to enhance their endurance and physical strength, and it has also been proven to assist in weight loss.<sup>[11]</sup> Nootropic drugs, are identified as those that are used to enhance memory or other cognitive functions. Caffeine is classified as a Nootropic as another one of its effects on the human body is sensitizing neurons and providing mental stimulation.<sup>[12]</sup> An individual that is consistently consuming caffeine will develop a tolerance to its effects.<sup>[13]</sup> When this occurs often the only benefit the consumer will experience is the anti-sleep effect. If the user were to take a break from caffeine the sensitivity to caffeine will increase again.<sup>[11]</sup> |
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| ===== Mechanism ===== | ===== Mechanism ===== | ||
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| - | {{:caffeine-works-coffee.jpg|}}| | + | {{:caffeine-works-coffee.jpg|}} |
| - | **Figure 4**: Caffeine and adenosine have similar molecular structure allowing them to form an antagonistic relationship. | + | **Figure 2**: Caffeine and adenosine have similar molecular structure allowing them to form an antagonistic relationship. |
| When caffeine binds to adenosine receptors, adenosine is not able to bind, and the adenosine receptors are antagonized. | When caffeine binds to adenosine receptors, adenosine is not able to bind, and the adenosine receptors are antagonized. | ||
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| The main mechanism of action of caffeine is antagonizing the adenosine receptors.<sup>[12]</sup> Adenosine is a purine hormone that is released locally and acts on various receptors that cause variation in cellular concentrations of cyclic AMP.<sup>[14]</sup> When adenosine acts upon its receptors it causes sedation and relaxation, by reducing the spontaneous firing of neurons in numerous parts of the brain.<sup>[12]</sup> The receptors of adenosine are located throughout the body in places including the brain, cardiovascular, respiratory, renal and gastrointestinal systems as well as in adipose tissue. The presynaptic activity of adenosine inhibits neuronal release of acetylcholine, norepinephrine, dopamine, gamma amino-butyric acid, and serotonin.<sup>[14]</sup> The inhibition of adenosine by caffeine results in the release of norepinephrine, dopamine and serotonin in the brain and increasing circulation of catecholamines.<sup>[12]</sup> | The main mechanism of action of caffeine is antagonizing the adenosine receptors.<sup>[12]</sup> Adenosine is a purine hormone that is released locally and acts on various receptors that cause variation in cellular concentrations of cyclic AMP.<sup>[14]</sup> When adenosine acts upon its receptors it causes sedation and relaxation, by reducing the spontaneous firing of neurons in numerous parts of the brain.<sup>[12]</sup> The receptors of adenosine are located throughout the body in places including the brain, cardiovascular, respiratory, renal and gastrointestinal systems as well as in adipose tissue. The presynaptic activity of adenosine inhibits neuronal release of acetylcholine, norepinephrine, dopamine, gamma amino-butyric acid, and serotonin.<sup>[14]</sup> The inhibition of adenosine by caffeine results in the release of norepinephrine, dopamine and serotonin in the brain and increasing circulation of catecholamines.<sup>[12]</sup> | ||
| - | When consuming a caffeinated beverage, the body will completely absorb all of the caffeine into the blood system, reaching a peak in the blood 30-60 minutes after consumption. Quickly after absorption caffeine will enter the brain.<sup>[14]</sup> In an average human the half-lives are 4-6hrs. This changes due to different factors including smoking, which causes short half-lives, and chronic diseases and pregnancy leading to longer half-lives.<sup>[14]</sup> | + | When consuming a caffeinated beverage, the body will completely absorb all of the caffeine into the blood system, reaching a peak in the blood 30-60 minutes after consumption. Quickly after absorption caffeine will enter the brain.<sup>[14]</sup> In an average human the half-lives are 4-6hrs. This changes due to different factors including smoking, which causes shorter half-lives, and chronic diseases and pregnancy leading to longer half-lives.<sup>[14]</sup> |
| The peak of caffeine in the blood 30-60 minutes after consumption correlates with a metabolic spike that can be seen in individuals to a varying degree.<sup>[14]</sup> This metabolic spike assists in the reduction of body weight when conjoined with a low-caloric administered diet. The increase in metabolic rate is dependent on the dosage of caffeine. The increased release of catecholamine when caffeine is present in the blood stream seems to have an effect on the increased metabolic rate. Both metabolic rate and the amount of catecholamine released increases linearly with increasing dosages of caffeine.<sup>[15]</sup> Caffeine is not an efficient long term fat loss method even though it possesses the mechanism to increase fat loss and metabolic rate. The reasoning for this is that with time one can become habituated to the effects of caffeine on the body, and specifically desensitized to this mechanism. The most efficient usage for caffeine as a fat loss supplement would be to take intermittently and paired with low-calorie diet.<sup>[15]</sup> | The peak of caffeine in the blood 30-60 minutes after consumption correlates with a metabolic spike that can be seen in individuals to a varying degree.<sup>[14]</sup> This metabolic spike assists in the reduction of body weight when conjoined with a low-caloric administered diet. The increase in metabolic rate is dependent on the dosage of caffeine. The increased release of catecholamine when caffeine is present in the blood stream seems to have an effect on the increased metabolic rate. Both metabolic rate and the amount of catecholamine released increases linearly with increasing dosages of caffeine.<sup>[15]</sup> Caffeine is not an efficient long term fat loss method even though it possesses the mechanism to increase fat loss and metabolic rate. The reasoning for this is that with time one can become habituated to the effects of caffeine on the body, and specifically desensitized to this mechanism. The most efficient usage for caffeine as a fat loss supplement would be to take intermittently and paired with low-calorie diet.<sup>[15]</sup> | ||
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| ===== Legal Status ===== | ===== Legal Status ===== | ||
| - | Caffeine is legal in every country in the world. There is recommended dosages to take to avoid various different health risks. Some of the major health concerns associated with caffeine include coronary heart disease, reproductive disorders and psychiatric disturbances.<sup>[12]</sup> The intake of greater than 250mg of caffeine can acutely raise blood pressure, correlating with coronary heart disease. Caffeine has also been suggested to have harmful effects on unborn infants. Concerning psychiatric disturbances, the excessive consumption of caffeine has been proven to produce nervousness, restlessness, anxiety and insomnia. Anxiety neurosis is often misdiagnosed instead of Caffeinism (5). Many coffee drinkers appear to be addicted to the caffeine. Those who have been addicted and are trying to cut back can develop caffeine withdrawal syndrome which is recognized as an official diagnosis in ICD-10.<sup>[17]</sup> | + | Caffeine is legal in every country in the world. There is recommended dosages to take to avoid various different health risks. Some of the major health concerns associated with caffeine include coronary heart disease, reproductive disorders and psychiatric disturbances.<sup>[12]</sup> The intake of greater than 250mg of caffeine can acutely raise blood pressure, correlating with coronary heart disease. Caffeine has also been suggested to have harmful effects on unborn infants. Concerning psychiatric disturbances, the excessive consumption of caffeine has been proven to produce nervousness, restlessness, anxiety and insomnia. Anxiety neurosis is often misdiagnosed instead of Caffeinism.<sup>[14]</sup> Many coffee drinkers appear to be addicted to the caffeine. Those who have been addicted and are trying to cut back can develop caffeine withdrawal syndrome which is recognized as an official diagnosis in ICD-10.<sup>[17]</sup> |
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| ====== Ephedrine ====== | ====== Ephedrine ====== | ||
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| Ephedrine is one of the four active components found in the herb Ephedra and belongs to a class of medications called sympathomimetics (adrenergic drugs). | Ephedrine is one of the four active components found in the herb Ephedra and belongs to a class of medications called sympathomimetics (adrenergic drugs). | ||
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| + | <box width classes round white centre| **Chemical Structure of Ephedrine and similar compounds**> {{:amphetamine-pic-48d11.png?600|Chemical structure of Ephedrine}}</box| Figure 3: Molecular structures of epinephrine and ephedrine and methamphetamine. The structural similarities of ephedrine to epinephrine allows it to act as a agonist to beta-adrenergic receptors, thus facilitating a stimulative response to the sympathetic nervous system.> | ||
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| ===== What is it? ===== | ===== What is it? ===== | ||
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| ===== Mechanism ===== | ===== Mechanism ===== | ||
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| The key within ephedrine’s mechanism of action lies with its similar molecular structure to adrenaline (epinephrine) as a sympathomimetic amine. Adrenaline is naturally produced by the body’s adrenal glands and binds to adrenergic receptors to stimulate the sympathetic nervous system in flight-or-flight response. This response includes increased blood flow to skeletal muscles, mobilizing energy, and increased heart output. | The key within ephedrine’s mechanism of action lies with its similar molecular structure to adrenaline (epinephrine) as a sympathomimetic amine. Adrenaline is naturally produced by the body’s adrenal glands and binds to adrenergic receptors to stimulate the sympathetic nervous system in flight-or-flight response. This response includes increased blood flow to skeletal muscles, mobilizing energy, and increased heart output. | ||
| - | Ephedrine’s structure allows it to bind to adrenergic receptors. The bulk of its effect comes from the pre-synaptic neuron being unable to distinguish between real adrenaline from ephedrine. Specifically, it directly agonizes all three subsets of β-adrenergic receptors in brown adipose tissue while sparing activation from the α-adrenergic receptors. When stimulated, the β-class of adrenergic receptors simulate lipolysis – the breakdown of fats by hydrolysis to release fatty acids. | + | Ephedrine’s structure allows it to bind to adrenergic receptors. The bulk of its effect comes from the pre-synaptic neuron being unable to distinguish between real adrenaline from ephedrine. Specifically, it directly agonizes all three subsets of β-adrenergic receptors in brown adipose tissue while sparing activation from the α-adrenergic receptors. When stimulated, the β-class of adrenergic receptors simulate lipolysis – the breakdown of fats by hydrolysis to release fatty acids. Associated with the increased fat oxidation, ephedrine is also able increase metabolic rate through increasing resting energy expenditure (REE) independent of exercise. This is in contrast to caffeine, which requires exercise to induce its fat-burning effects. |
| - | Associated with the increased fat oxidation, ephedrine is also able increase metabolic rate through increasing resting energy expenditure (REE) independent of exercise. This is in contrast to caffeine, which requires exercise to induce its fat-burning effects. | + | |
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| + | {{:metabolism1.jpg?400|Lipolysis pathway}} | ||
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| + | **Figure 4**: Illustration of the lipolysis pathway by which ephedrine stimulates when binding with beta-adrenergic receptors in adipocytes. | ||
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| + | When accumulates in the the blood, it takes the place of epinephrine to cause the breakdown of triglycerides to free fatty acids and glycerol. | ||
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| ===== Clinical Data ===== | ===== Clinical Data ===== | ||
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| - | <box width classes round white centre| **Raspberry Ketone**> {{:raspberry_ketone_-_chemical_makeup.png?300|This is the molecular formula for Raspberry Ketone}}</box| Figure 4: Chemical Structure of Raspberry Ketone> | + | <box width classes round white centre| **Raspberry Ketone**> {{:raspberry_ketone_-_chemical_makeup.png?300|This is the molecular formula for Raspberry Ketone}}</box| Figure 5: Chemical Structure of Raspberry Ketone> |
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| - | **Figure 5**: Showing the results of the test subjects that were on a high-fat diet | + | **Figure 6**: Showing the results of the test subjects that were on a high-fat diet |
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| Using rodents as the test subject, they were fed a high-fat diet (HFD) that included a 0.5, 1, 2% of raspberry ketone (RK) for 10 weeks. Another experiment conducted alongside the previous one was done by feeding rodents a HFD for 6 weeks and then the last 5 weeks a HFD however with %1 RK. The results showed that RK did indeed prevent the HFD-induced elevations in body weight, as well as decreased the weight of the liver and triacylglycerol. Red raspberry ketone was seen to increase norepinephrine-induced lipolysis through the translocation of hormone-sensitive lipase coming from the cytosol to lipid droplets in the fat cells. Additionally, it stimulated the metabolism of adipose tissues (white and brown) as well as inhibiting small intestinal absorption through suppressing pancreatic lipase activity.<sup>[27]</sup> | Using rodents as the test subject, they were fed a high-fat diet (HFD) that included a 0.5, 1, 2% of raspberry ketone (RK) for 10 weeks. Another experiment conducted alongside the previous one was done by feeding rodents a HFD for 6 weeks and then the last 5 weeks a HFD however with %1 RK. The results showed that RK did indeed prevent the HFD-induced elevations in body weight, as well as decreased the weight of the liver and triacylglycerol. Red raspberry ketone was seen to increase norepinephrine-induced lipolysis through the translocation of hormone-sensitive lipase coming from the cytosol to lipid droplets in the fat cells. Additionally, it stimulated the metabolism of adipose tissues (white and brown) as well as inhibiting small intestinal absorption through suppressing pancreatic lipase activity.<sup>[27]</sup> | ||
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| Another significant study that involved numerous animals (rats, guinea pigs, and rabbits). The ingredient (raspberry ketone) was readily absorbed into the experiments gastrointestinal tract with an approximate dosage of 1 mmol/kg. It was seen that most of the ingested dosage was excreted out within the first 24 hours. The results of another study showed that there was a lower weight gain in male rats in a 90-day study, with the consumption of 280mg/kg of the substance. The European Food Safety Authority (EFSA) showed no observed adverse effect level (NOAEL) with the dosage being set at roughly 100mg/kg. When the dosage increased to roughly 275mg and 700mg/kg there were higher enzyme activity levels recorded, specifically with alanine aminotransferase and aspartate aminotransferase. However, the study has several setbacks one specifically pertaining to that only 12% of the supplement used in question had raspberry ketone and the 88% remaining was unknown.<sup>[28]</sup> | Another significant study that involved numerous animals (rats, guinea pigs, and rabbits). The ingredient (raspberry ketone) was readily absorbed into the experiments gastrointestinal tract with an approximate dosage of 1 mmol/kg. It was seen that most of the ingested dosage was excreted out within the first 24 hours. The results of another study showed that there was a lower weight gain in male rats in a 90-day study, with the consumption of 280mg/kg of the substance. The European Food Safety Authority (EFSA) showed no observed adverse effect level (NOAEL) with the dosage being set at roughly 100mg/kg. When the dosage increased to roughly 275mg and 700mg/kg there were higher enzyme activity levels recorded, specifically with alanine aminotransferase and aspartate aminotransferase. However, the study has several setbacks one specifically pertaining to that only 12% of the supplement used in question had raspberry ketone and the 88% remaining was unknown.<sup>[28]</sup> | ||
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| ===== Legal Status ===== | ===== Legal Status ===== | ||
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| Raspberry ketone as previously stated is marketed as a natural ingredient, but there are other countries that agree. Within Denmark, food supplements are regarded as novel food, which essentially means that it is ‘original’. A loop hole some companies use is they advertise their product that contains raspberry ketone towards the Danish or UK consumer. The average/recommended dosage of the ingredient has been highly contested with most reputable sources saying 100 to 1400mg/day while a person not on food supplements may just consume a few mg/day (1.8-3.8mg/day). This is approximately a 26 to 368 times higher difference.<sup>[28]</sup> | Raspberry ketone as previously stated is marketed as a natural ingredient, but there are other countries that agree. Within Denmark, food supplements are regarded as novel food, which essentially means that it is ‘original’. A loop hole some companies use is they advertise their product that contains raspberry ketone towards the Danish or UK consumer. The average/recommended dosage of the ingredient has been highly contested with most reputable sources saying 100 to 1400mg/day while a person not on food supplements may just consume a few mg/day (1.8-3.8mg/day). This is approximately a 26 to 368 times higher difference.<sup>[28]</sup> | ||
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| + | ====== Conclusion ====== | ||
| + | When selecting and determining the efficacy of fat loss supplements it is important to examine the various ingredients listed on the label. The supplement industry is a for-profit business and oftentimes, there may be unsubstantiated and exaggerated claims of weight loss and it is therefore more crucial to look at relevant scientific studies to validate such statements. Furthermore, it is also imperative to critically analyze the studies that were performed and determine whether it the results can be applicable to human dosages. For example, studies done on raspberry ketones may show some promise in rodents, but has no evidence of efficacy in humans. Moreover, when converting rodent to human dosage, the required supplementation becomes astronomically high. Other critical variables regarding dietary supplements also include safety and toxicity. It is strongly advised for individuals looking at fat loss supplements to do their own extensive research on individual compounds and risks involved. | ||
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| ====== References ====== | ====== References ====== | ||
| [1] Williamson, J. (n.d.). What Is a Fat Burner? Retrieved from http://www.healthguidance.org/entry/14407/1/What-Is-a-Fat-Burner.html | [1] Williamson, J. (n.d.). What Is a Fat Burner? Retrieved from http://www.healthguidance.org/entry/14407/1/What-Is-a-Fat-Burner.html | ||
