Medicine for Africa - Medical Information Service

SPARTAME

Definition:

Aspartame – APM – is marketed in the USA under the brandnames of NutraSweet® and Equal®, and outside of the US as Equal® and Canderel®.

Today, aspartame is used in more than 5,000 dry and liquid food products, including tabletop sweeteners, diabetic food products, soft drinks, especially ‘diet sodas’, candy, chocolate and sugar-free chewing gums, cocoa mixes, instant tea and coffee products, breath mints, as well as some cereals, instant breakfasts, yogurts, juice beverages, milk drinks and shake mixes, gelatin and frozen desserts, as well as wine coolers, among many other products.  They are also often used as filling substance for drugs, both over-the-counter and prescription drugs, vitamins and herb supplements.

Aspartame is an artificial sweetener that is about 180 to 200 times sweeter than naturally grown sugar. It is produced in the laboratory and consists of three major substances:

Aspartic acid, an amino acid – 40% of aspartame;
Phenylalanine, an essential amino acid – 50% of aspartame;
Methanol, a wood alcohol – 10% of aspartame.

Aspartic Acid:
Also called asparaginic acid, is a non-essential amino acid, i.e. the body itself can produce the amino acid from food sources such as sugar cane and molasses.  Its main functions are as a neurotransmitter in the brain, allowing for an easy transfer of information from one nerve cell (neuron) to another. While this is an important function of this ‘excitatory’ amino acid, excessive amounts of aspartic acid can result in just the opposite effect, by producing s0-called ‘free radicals’ which can cause more or less severe damage to the same brain cells and even kill them, thus, it is also called an excitotoxin.
Free radicals, in general, play an important role in biology, especially for the purpose of killing invading bacteria by certain leukocytes (so-called neutrophil granulocytes), and in certain cell signaling processes. Superoxide and hydroxyl radicals are the most important oxygen based, and probably best known, radicals. However, just as many of these radicals are able to kill intracellular invaders, they are also implicated in undesired side effects resulting in sometimes serious cell damage. Thus, actions and/or reaction of free radicals are also implicated in the development of certain cancers, as they may induce unwanted cell mutations.  Furthermore, atherosclerosis, Parkinson’s disease, senile and drug-induced hearing problems, schizophrenia and Alzheimer’s disease are just some of the potential negative results of too many unwanted free radicals within the blood stream.
Aspartic acid also has a cumulative harmful effect on both the endocrine and the reproductive system; rising levels increase the level of norepinephrine (noradrenaline), a so-called ‘stress hormone’ that, in excess, can cause agitation, anxiety and even mania. And animal studies have shown that aspartic acid can also surpass the placental barrier and reach the fetus. As humans are about five times more sensitive to the effects of aspartic acid than rodents, the chances that this excitotoxin can also breach the human placental barrier during pregnancy and reach the growing and fragile system of an unborn child appear to be likely.
     
Phenylalanine:
This is an essential amino acid, which means that the body cannot produce this acid de novo and therefore requires its outside supply through the intake of foods, such as meat, eggs, milk and bananas.  Phenylalanine is naturally produced by plants and many microorganisms, and is one of the twenty amino acids that are used to make up proteins that are coded for by the human DNA (deoxyribonucleic acid).
Phenylalanine can turn neurotoxic, if present in excess, or if the body cannot metabolize this amino acid appropriately, resulting in a build up of phenylalanine in blood and tissues. If this failure to metabolize the amino acid is genetically based, the disease is called ‘phenylketonuria’ (PKU), and people with this disorder have to abstain from any ingestion of phenylalanine containing products or foods.  If phenylalanine and/or its metabolized products are present in excess, be it because of PKU or because of excessive intake, they will be able to compete in the brain with physiological neurotransmitters such as serotonin, decreasing its levels, and thus making depression more likely, and potentially, more serious.  Furthermore, continuously increasing levels of phenylalanine in the brain can worsen schizophrenia, and make the occurrence of seizures more likely.  On the other hand, decreased levels of serotonin can also lead to increased craving of carbohydrates by the individual, thus contradicting APM’s basic idea of decreasing the calorie intake by replacing sugar with APM.  
If phenylalanine is ingested in its natural form and protein-bound via naturally occurring food products, it is usually accompanied by the ingestion of another amino acid – tyrosine, which slows down the absorption of phenylalanine, and thus keeps its blood levels ‘in check’.

Unfortunately, aspartame contains both aspartic acid and phenylalanine in their free form, not bound to or accompanied by any other amino acid or protein, resulting in an expedited and almost uninhibited uptake of these products into the blood stream.  

Methanol:
Methanol, also known as wood alcohol, comprises 10% of APM. Methanol is a well known lethal poison that is liberated from APM at temperature ranges exceeding 86ºF (approximately 30ºC) – a temperature that is below the normal body temperature and that can easily be present during storage or transport.  Methanol can almost equally easily be absorbed by the body by way of ingestion or inhalation.
According to the US Environmental Protection Agency (EPA), methanol is considered a ‘cumulative poison due to the low rate of excretion once it is absorbed by the human body’ – thus, even minute or small amounts of methanol, ingested over time via aspartame-containing food products, will build up inside the body and result in subsequent toxic disorders (see Symptoms).  While the EPA usually keeps a tight control on the methanol exposure to humans, allowing only minute amounts to be present in food products or via other environmental exposures, the level that the FDA allowed to be present in APM is seven times the amount the EPA allows for any other usage or user.
Also, similar to the above mentioned differences between bound and unbound amino acids, if methanol is present in natural foods such as fruits, it is bound to pectin and has ethanol as co-factor, to limit and counterbalance some of methanol’s negative effects.  APM does not provide any of these control substances – releasing methanol with its full destructive potential into the consumer of aspartame enriched food products.
Thus, the methanol that is absorbed from APM will be converted in the liver to formaldehyde – another well known neurotoxin and carcinogen that also interferes with the physiological (normal) DNA replication.  As formaldehyde is metabolized (broken down), another cumulative poison is being produced – formic acid (the poison of fire ants).  Formic acid is highly toxic to human cells, as it accumulates in the brain and spinal fluid, as well as in kidneys and other organs.  Although the amounts of formic acid that result from the methanol portion of APM are minute, no conclusive studies have been performed to-date, in order to determine the extent of danger to any consumer which may be the result of the intake of APM.
 

            Historic Review

Aspartame was an ‘accidental’ discovery in the mid 1960s by a scientist at a pharmaceutical company, GD Searle Company, while searching for a new drug to treat gastric ulcers.

The product he developed – L-aspartame-L-phenylalanine methyl ester – Aspartame (APM) proved to be almost 200 times sweeter than sugar, while having no calories at all, making it a potential highly valuable product for health-conscious consumers.

Some early trials performed by researchers in university settings revealed the occurrence of brain cancers and severe brain damage in monkeys and mice, while company own research showed the product to be safe for consumption. In 1973, the company applied for FDA (Food & Drug Administration) approval, which was denied for eight years, due to persistent concerns regarding APM’s toxicity, brought to the table by several well known scientists and consumer groups, pointing to the seriousness of the central nervous system (CNS) damage and carcinogenic potential of APM, as shown in animal tests.

In 1979, the FDA established a ‘Public Board of Inquiry’ (PBOI), in order to review a number of objections that were voiced by prominent scientists against the approval of aspartame.  At the same time, aspartame received approval in France, primarily for the use in pharmaceutical products, and started to be marketed under the name Canderel®.

Finally, in 1981, the negative tide for the company turned positive when Ronald Reagan became President.  The President’s transition team included the then CEO of GD Searle, who became the new Secretary of Defense – his name was Donald Rumsfeld.  The transition team nominated a new FDA Commissioner, who, soon after taking on his new job, overruled the PBOI findings, and gave initial approval for aspartame in July 1981 for its use in dry products.  In October of 1981, it was approved as a tabletop sweetener, and for many other usages, and in July 1983, it was also approved as sweetener in carbonated beverages and other liquids.

The FDA Commissioner resigned in September 1983 under a cloud of controversy regarding the acceptance of inappropriate gifts and unauthorized industry-provided trips. Soon thereafter, he became a senior scientific consultant with a long-term contract at a company that was closely associated with the manufacturer of APM.

Aspartame, a product that was once labeled by the Pentagon as a biochemical warfare agent, has become a safe everyday food additive for consumers worldwide.

Symptoms:

The first major report of side effects was reported by the CDC (Center for Disease Control) in 1984, and 10 years later, more than 75% of all complaints listed in the US adverse-reaction monitoring system of the US Department of Health and Human services, involved aspartame.  By 1995, the list of over 10,000 consumer complaints included four deaths and more than 90 rather unique symptoms, most of them associated with impaired neurological functions. In addition, according to reports by many physicians in practice, aspartame-containing dry and/or liquid consumer products may cause symptoms that can mimic all the following diseases and disease processes such as [listed alphabetically]:

• Abdominal pains and cramps;
• Aggressive behavior, excitability and hyperactivity;
• Alzheimer’s disease;
• Arthritis;
• Asthmatic reactions;
• Attention deficit disorders (such as ADD or ADHD);
• Balance problems – walking instability;
• Cancers – renal/bladder/urinary, schwannomas [neural], and others;
• Cardiac arrest;
• Chronic fatigue syndrome;
• Circulatory disturbances;
• Convulsions and seizures;
• Diabetes and diabetic disorders;
• Diarrhea;
• Disorientation;
• Dizziness;
• Eye problems;
• Fatigue and general weakness;
• Fibromyalgia;
• Hair loss;
• Headaches, especially migraine like headaches and cluster headaches;
• Hypothyroidism;
• Impotence;
• Instability of glucose levels – erratic up/down swings of the glucose level; 
• Itching and skin irritations;
• Joint and musculoskeletal pains;
• Leukemia;
• Liver impairment;
• Lower abdominal cramps and pains;
• Lupus;
• Lyme disease;
• Lymphomas;
• Memory loss and loss of depth perception;
• Menstrual pains;
• Mood changes, including suicidal tendencies;
• Multiple chemical sensitivity;
• Multiple sclerosis – MS;
• Muscle weakness;
• Nausea and vomiting;
• Numbness of extremities, sometimes extreme;
• Panic disorders and other psychological disorders;
• Parkinson’s disease;
• Skin rash;
• Tinnitus;
• Tremors;
• Urinary discomforts;
• Vertigo;
• Vision changes, including deteriorating vision; and finally also, opposite to the products inherent promises –
• Weight gains.

Considering, that even according to the FDA’s own admission, less than 1% of those experiencing any problems, actually report them, there were probably more than one million people who potentially may have experienced adverse effects from taking aspartame in one way or another.  

While nobody says that aspartame is the cause of many of the above listed physiological diseases, the toxic ingredients of aspartame seem to not only worsen symptoms in patients who actually suffer from these diseases, but the toxins of aspartame also result in symptoms that are often misdiagnosed as one of these serious disorders, often resulting in an unnecessary overtreatment of the patient.  Thus, it has become more important for the physician – family practitioner or general physician – who sees the patient first, to include detailed questions regarding the patient’s nutritional habits when taking the patient’s past medical history.
                  
Patients with an erroneous diagnosis of multiple sclerosis, Parkinson’s disease, or Chronic Fatigue Syndrome, may be put on drug regimens of potentially harmful drugs, while simply not ingesting or stopping to eat and/or drink aspartame-containing products could have treated them more effectively.  The question of whether the economic benefit of the use of aspartame can justify the potentially enormous expenses derived from unnecessary medical and drug therapy costs, appears difficult to answer in favor of aspartame.

Phenylalanine: While phenylalanine (50% of aspartame) is sometimes used for the treatment of depression, excessive amounts of phenylalanine can accumulate in the brain and cause the level of serotonin (a neural transmitter and mood regulator) to decrease, making depression more likely, and if present, more serious. Additionally, the accumulation of phenylalanine can worsen schizophrenia and make individuals more susceptible to experiencing seizures.  Also, as mentioned above, the decrease of serotonin levels can result in the craving of carbohydrate rich foods, which may explain aspartame’s ineffectiveness as an aid in dieting/for dieters.  Thus, if somebody consumes an aspartame-containing beverage together with a carbohydrate-rich, protein-poor meal (e.g. dessert food), the phenylalanine effects on the brain will double! 

ADD – Attention Deficit Disorder, and ADHD – Attention Deficit Hyperactivity Disorder, have both been reported by news programs to be on a steep increase in young children in the USA.  Both disorders are behavioral and emotional type disorders, and can be triggered by too much phenylalanine in one’s daily diet.  Considering that the average daily food and drink intake of American children consists typically of cookies or other sweet baked products, (diet) sodas, chewing gum, etc., the amount of aspartame-derived phenylalanine and other damaging byproducts may indeed be significant.

Diketopiperazine – DKP – a breakdown product of phenylalanine that forms after prolonged periods of storage of aspartame-containing liquids, is known to produce brain tumors, uterine polyps and changes in blood cholesterol levels in animal experiments.

Methanol: Known side effects of e.g. a minor methanol intoxication (10% of aspartame) include:

• Vision disorders, including blurry vision, retinal damage and even blindness;
• Headaches;
• Tinnitus;
• Dizziness and weakness;
• Nausea, chills and gastrointestinal disturbances;
• Vertigo;
• Memory lapses
• Numbness, neuritis, and shooting pains in all extremities, and
• Various behavioral disturbances.

Obviously, some of the methanol-related side effects are very similar to the ones, listed above for aspartame in general.  In high concentrations, methanol is known to be a lethal poison.  
In 1978, the journal ‘Medical World News’ reported that aspartame contains methanol at levels that are 1,000 times greater than in most other foods under the control of the FDA.

Formaldehyde, a breakdown product of methanol is a known neurotoxin and a known carcinogen. It causes interferences with DNA replication, resulting in birth defects; it can cause retinal damage and has been documented to cause squamous-cell carcinoma (a form of skin cancer) in animals.  In humans, even low levels of formaldehyde can result in headaches, fatigue, dizziness, chest tightness, nausea, loss of concentration and seizures.

 
Diagnosis:

‘Diagnosing’ side effects of food additives is usually performed by performing animal trials, sometimes followed by human trials. Different from the admission requests for pharmaceutical drugs, which need to be tested via 3-phase trials, food products and/or food additives require much less stringent approval conditions.  Furthermore, while all pharmaceutical companies also perform so-called Phase IV research ('post marketing surveillance trials’), aimed at evaluating the effectiveness and safety of a new drug, after it has been approved by the FDA and has been marketed to consumers.  These ‘pharmacovigilance’ trials have recently resulted in important findings, such as unacceptable adverse reactions in drugs like cerivastatin (Baycol® or Lipobay®), or rofecoxib (Vioxx®).  There is no equivalent research phase to ‘Phase IV’ performed for approved food additives, no matter how controversial their initial approval process may have been.

A recently performed, extensive research study, performed by an independent center in Italy – the Cesare Maltoni Cancer Research Center of the European Ramazzini Foundation – resulted not only in ‘grave’ conclusions regarding the negative potentials of aspartame, it also enlightened some of the major flaws of earlier (industry-) performed trials.  The conclusion they arrived at, was that APM is a multi-potential carcinogenic compound with its carcinogenic effect becoming evident with a daily consumption of merely 20 mg/kg body weight (bw), which is half the limit of the current ‘Acceptable Daily Intake’ (ADI) recommendations for humans according to European standards (40 mg/kg bw), and even less than half the ADI in the USA (50 mg/kg bw). 
    
Thus, it appears evident that the only way to ‘diagnose’ the bad to poor effects of a new food additive – in spite of early supportive trials – should consist of ‘field-oriented’ or ‘market-based’ continuous research efforts, confirming a new food additive’s effectiveness, or alerting its potential adverse reactions in a time period that can be kept as short as possible, regarding the immense task to be tackled.

 
Treatment:

The best Therapy and Prevention is to stay away from ingesting aspartame containing food products or beverages.

While it may take the body a few weeks to completely rid itself from the breakdown products of aspartame, individual symptoms should improve noticeably within just a few days to one-to-two weeks after stopping any aspartame intake.

As mentioned above, aspartame is not the causative agent of physiological diseases such as multiple sclerosis (MS), Parkinson’s or others; however, the consumption of aspartame has shown a worsening of typical symptoms in those patients.  Furthermore, aspartame has often been the cause of an erroneous diagnosis of those illnesses and others, because the effects of its breakdown products presented themselves with symptoms similar MS, Parkinson’s, and others.

On the other hand, it is well known that psychosomatic disorders, such as the so-called Attention Deficit Disorder (ADD) or Attention Deficit Hyperactivity Disorder (ADHD) can be greatly improved by changing dietary habits in general – and cutting out phenylalanine may, indeed, have a profound impact on these disorders.

 
Discussion:

Aspartame, as most, if not all, so-called ‘food additives’ of whatever kind, are not life-saving drugs.  Considering the innumerable ‘diet products’ that promise more than even their instruction sheets do, it seems even more important that the consumer can rely on the government’s regulatory agencies to ‘separate the wheat from the chaff’.

And this is where the major problem in the crusade of the aspartame approval story seems to lie.  In a capitalistically oriented society, it is to be expected that companies (public or private) are eager to sell their new discoveries, often without sufficient research, as to whether their new invention/discovery will indeed be a positive adjunct for mankind.  That is where the government is supposed to step in, and to take its share of responsibility – to make sure that new products/inventions, introduced to the public, will not be harmful to the community, but rather hold what they promise to deliver.  In the case of aspartame – it has become obvious that politics, not science, allowed this dangerous chemical compound to reach the public consumer, resulting in the needless suffering of probably millions of ‘government-trusting’ people.  Thus, if the public in a country like the USA, that takes pride in its efficient and stringent regulation procedures, falls victim to seemingly corrupt and ‘blind’ or incompetent regulatory organizations, questions arise as to the need of the existence of those institutions in the first place. 

Unquestionably, the US-FDA and similar governmental regulatory bodies worldwide are of great value to protect the public from unscrupulous marketers of any kind of products.  However, while especially the pharmaceutical industry has taken rather stringent measurements to regulate itself, there still seems to be a major need to instigate and realize similar efforts in certain governmental agencies.  

In summary, considering that aspartame is not a ‘life-saving’ drug, not even an effective ‘diet aid’, as it claims to be, it most likely should be taken out of the current food chain.  This article is not aimed at instigating or promoting actions that should be taken by responsible representatives of appropriate governmental agencies that have been created to protect the public from undue harm. However, it seems that the multitude of adverse reports that surfaced over more than two decades, should justify the need of a reasonable if not thorough reevaluation of aspartame.  The unknowing and trusting consumer deserves this.   

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