General Properties:
Phenylalanine is a natural, essential Amino Acid with remarkable pain-relieving and anti-depressant properties when consumed as a supplement to the diet. It is safe, non-toxic, non-addicting, and the body does NOT build a tolerance to it. The following report describes some of the known information on this unique supplement. References are included and an additional general reference list is included at the end of this report.

Phenylalanine/DLPA-Recommended Dosage:
For pain relief: initially, consume two to three grams per day for severe pain. When pain subsides, reduce dosage to 500 milligrams per day or stop taking until pain begins to return.

For anti-depression: initially, consume one to one and one-half grams per day. When depression is alleviated, reduce dosage to 500 milligrams per day to maintain state. Alternately, slower results are obtained by taking 500 milligrams per day initially.

It is best to take phenylalanine products just prior to meals and on an empty stomach in order to maximize the absorption and increase the effects. If possible, take just before going to bed or just after waking up. Some reports suggest taking later in the day could lead to insomnia. Other reports suggest that taking phenylalanine just prior to going to bed will help you wake up quickly, fresh and cheerful.

Safety:
PRECAUTIONS: individuals with PKU disease (phenylketouria) should not consume phenylalanine because their bodies do not have the enzyme necessary to metabolize phenylalanine. If you have this inherited disease you know about it because there are some foods (high in phenylalanine) that you cannot eat.

Also, in rare cases blood pressure is affected and is dose dependent (the higher the dose the greater the increase in blood pressure in some individuals). If you suffer from or are prone to having high blood pressure you may want to begin slowly. In this case you should first take a small dose of about 100 milligrams phenylalanine, measuring blood pressure at intervals while gradually increasing dosage and monitoring blood pressure each day. For similar reasons, do not take blood pressure elevating drugs, such as MAO (monamine oxidase) inhibitors.

Phenylalanine is non-toxic and has no side effects in metabolically normal people. However, sensitivities and excess dosages can cause headaches, insomnia, and/or irritability. Reducing dosage will eliminate these effects.

The body does not build up any tolerance to phenylalanine so that increased doses are not needed to achieve the desired effect. It is not physiologically or psychologically addicting.

The U.S. Food and Drug Administration has placed phenylalanine on its GRAS (generally recognized as safe) list, largely due to it vast usage and because of the availability of scientific literature showing the safety and non-toxic nature of PA.

Actual Uses:
The most notable and documented uses are against pain and depression.

Phenylalanine is used to help alleviate chronic pain such as occurs with arthritis, dental surgery, premenstrual cramps, lower back pain, migraine headaches, joint pains, whiplash, postoperative pain, cancer, neuralgia, and other long-term pain and constant irritating discomfort. Phenylalanine is a natural anti-inflammatory and its pain relieving properties, especially for arthritis, are probably partially due to its anti-inflammatory properties and reduced swelling. As an anti-inflammatory agent, phenylalanine takes longer to work in the body than synthetic pain-killers. Depending upon the individual and the severity of the pain, it may take from two days to three weeks to have an effect on the chronic pain. However, once taken effect, the dosage may be reduced to a maintenance dose. Often, depending upon the condition and cause of the pain, maintenance dose may not be needed as the pain may not return.

The pain-relieving effects of phenylalanine are increased if the patient takes the usual over-the-counter pain remedies, such as aspirin, acetaminophen, or ibuprofen. The different effects of the two types of pain-killing agents do not interfere with each other, rather, they work in combination with each other and enhance the ability of each to control pain.

Phenylalanine is used to help fight depression brought on by feelings of helplessness and a wide variety of depressions, including the depressive phase of manic-depressive illness and endogenous, schizophrenic, and post-amphetamine depression. Depending upon dosage and type of depression, effects may take from 2 days to 2 weeks to be noticeable. Generally, depression is alleviated within a few days when the higher doses are taken initially (1000 to 1500 mg per day), whereas initially taking the lower dose (500 mg per day) show effects within a couple weeks.

Additional less documented and as yet unsubstantiated uses have been for improving memory, increasing mental alertness, promoting "sexual interest", and the suppression of appetite. Considering the various effects produced during depression, and the ability of phenylalanine as an anti-depressant, these uses may be more of a consequence of the depressive state that has been modified.

How Phenylalanine Works:
Against pain: phenylalanine is capable of increasing the endorphin and enkalphalin levels in the blood. Endorphins are the natural morphine-like pain-killing substances that are produced by the brain in response to pain. Phenylalanine inhibits (slows down) the enzymes that break down the endorphins, thereby allowing them to remain longer and in greater supply than would normally be the case.

Against depression: phenylalanine is the precursor to the neurotransmitters dopamine, norepinephrine (noradrenaline), and epinephrine (adrenaline). The decrease in the brain levels of these neurotransmitters have been linked to certain forms of depression. Supplementation with phenylalanine elevates the production of these neurotransmitters in the brain and helps alleviate depression.

Phenylalanine requires vitamin C and vitamin B6 to be converted into norepinephrine. Supplementation with these vitamins may be necessary for complete effectiveness if the consumer is deficient in these and possibly other vitamins.

Storage:
Storage is similar to the storage of any drug products. Store supplements made with phenylalanine away from direct sunlight and keep bottle closed when not in use. Store at room temperature.

Chemistry:
Phenylalanine is an amino acid found in relatively large amounts in meat, milk, cheese, and some high protein foods. When food is consumed, the digestive system breaks down protein into amino acids which become building blocks for cellular functioning. Then the cells uses these amino acids to rebuild bodily proteins such as enzymes, hormones, and peptides. Proteins are large molecules that are composed of multiple small amino acid molecules linked end to end. There are twenty different amino acids that are used in the biosynthesis of proteins. The order and composition of amino acid sequences determines which protein is produced from the unlimited possibilities available.

Phenylalanine is one of ten essential amino acids required in the diet (the others are arginine, histidine, isoleucine, leucine, lysine, methionine, threonine, tryptophan, and valine). These are essential because the body is not capable of producing these amino acids out of other amino acids. Tyrosine is not an essential amino acid (its production comes from phenylalanine).

Phenylalanine is metabolized within the body to tyrosine, another amino acid, which is converted into neurotransmitters such as L-dopamine, norepinephrine (noradrenaline), and epinephrine (adrenaline). These neurotransmitters are also physiologically active hormones called catecholamines, that possess various regulating functions in many metabolic pathways. As major chemical communication signals within our nervous system, these neurotransmitters regulate our mood, attitude, state of mind, and general nervousness conditions.

The phenylalanine molecule exits in two forms (called isomers) that are mirror images of each other, like left and right-handed gloves, termed L-phenylalanine and D-phenylalanine. The L- and D- refers to the terms levorotatory and dextrorotatory, respectively, and refers to the direction that light is bent (refracted) when traveling through a pure isomer. Though structurally basically the same, each of these "isomers" have slightly different properties. The levorotatory forms of amino acids exist naturally in food and provide the nutritive value of protein. The dextrorotatory forms of amino acids also provide nutrition but are metabolized through different pathways. Each of the pure isomers can be converted easily into a 50/50 mixture of each isomer, since thermodynamics dictate that the mixture result from equilibrium.

It is theorized that the D-isomer of phenylalanine is the isomer responsible for reducing pain and that the L-isomer of phenylalanine is the isomer effective for depression. However, other literature sources show that both these effects are the result of consuming the D-isomer of phenylalanine alone. Either way, it is evident that only supplementation will work since food alone will not produce the desired effects.

In practice, supplements contain both the L- and D- isomers of phenylalanine and is called D,L-phenylalanine (DLPA), a 50/50 mixture of each isomer. The resulting material does not reflect light in either direction. DLPA is considered the best way to take phenylalanine because it provides nutritive value and can work to relieve pain and depression. The D,L mixture is also much less expensive than either pure isomer would be by itself. For general use, the costs to separate the isomers is prohibitive and consumption of the pure optical isomers offers no benefit over taking the mixture.

A Few Words on Pain:
Pain is how our bodies communicate to us that something is wrong. It is there for us to respond to, usually quickly, and make the most appropriate response. There exists two main types of pain, the chronic and the acute. Chronic pain is long-lasting, usually difficult to determine and halt, and returns easily if medication does work. Acute pain is short-acting, usually simpler to determine and halt, and commonly does not return when remedied.

Pain-relievers are essential but many of the prescription pain drugs can become addicting or abused. In addition, while under the effects, new trauma resulting in pain may be unnoticed or neglected. The consumer must be made aware that pain has a purpose, especially acute pain, and to properly regulate their reliance and consumption of pain medication.

However, even without drugs, through the use of our own defensive pain mechanisms, during stress we can become oblivious to pain, but only temporarily. Take for example, a soldier who is wounded and continues to perform heroically without notice of pain or peril until, perhaps when the battle is over, he faints from shock at having lost an arm or leg. An example of intense acute pain that the body has chosen to ignore, using its endorphins, for a short period of time.

Phenylalanine can only work to relieve chronic pain. Thus, acute pain is still felt and acute injury is less likely to be furthered by inaction. Considering its ability and effectiveness, along with its safety and how it works within the body, phenylalanine is the safest pain-reliever available. With all the research that has been tried with new drugs to mimic phenylalanine's ability to enhance the body's natural endorphins, not one product has been discovered. Phenylalanine remains the safest and best all around pain fighter there is.

A Few Words on Depression:
Depression is serious illness and may be brought on by a multitude of factors, including chemical and physical impairment and disease. Always consider getting professional help for serious depression. It has been theorized that depression often results from the feeling of helplessness. This feeling has also been associated with a depletion of norepinephrine in the brain. Death from helplessness has been observed in animals and people. Results from some animal studies has led scientists to conclude that biochemical imbalances exist during these states and that they can be altered through supplementation with DLPA.

Studies are usually done on rats since they are plentiful, closely mimic brain biochemistry of humans, and because people are more tolerant of their being testing and destroyed for scientific purposes.

A study performed by Dr. J. M. Weiss showed the possible correlation between depression and norepinephrine depletion. He placed rats into very cold water for six minutes and tested their ability to escape shock in a box where all they needed to do was to leap over a low barrier. The rats were unable to jump over the barrier to a shock-free portion of the box because they had the feeling of helplessness brought on by the cold water. Dr. Weiss discovered that when these rats norepinephrine levels were measured, they were depleted. When rats were placed in warm water and similar tested, the rats were able to jump the barrier (no feeling of helplessness) and he found normal levels of norepinephrine in their brains. He verified his findings by artificially depleting the norepinephrine levels of rats and found that they had the same test results with the shock box.

Another study determined that wild rats survived 60 hours when forced to swim until exhaustion set in and they drowned. However, when wild rats were first restrained until they stopped squirming (essentially "they gave up") and then placed in water, the rats swam frantically for about 30 minutes before drowning. Some even died while being restrained. The feeling of helplessness was achieved by the restrained rats and they were less capable of surviving further stress. When rats were allowed to "escape" while being restrained and then placed in water, no feeling of helplessness existed and they could survive about 60 hours just like the unrestrained rats. These rats had lost their feeling of helplessness and regained their survivalist instinct.

Studies have also shown in humans that a helplessness attitude caused by stress contributes to poor health. Of 51 women having pap-smear cancer checkups and had suspicious cervical cells, 18 had suffered significant personal losses within the previous six months. Of these 18 women, 11 developed cancer, while only 8 of the other 33 patients developed cancer.

It has also been shown that poor health and a poor attitude contribute to increasingly poor health. This is why it is so important to keep a positive mental attitude during times of stress and illness. Attitude is everything when it comes to fighting disease and depression. Depression does not cause disease, it merely decreases effectiveness of the bodies own defenses in fighting disease.

Helplessness explains the feeling that often arrives soon after the elderly are placed in nursing homes. Elderly are more likely to be prone to disease states when they have let their advancing age and changing living conditions and capabilities affect the way they look at life. It is difficult for the elderly to remain composed and keep the right attitude when the living environment changes quickly.

Helplessness makes one feel as though they have absolutely no control over their own life. This manifests itself because of stressful circumstances relating to such things as health, family, finances, employment, and age.

For at least one year following any major accident, illness, or stress one should be careful and aware that their bodies are in a state that affects their health. They should do everything possible to keep a good positive attitude during this time because they are prone to disease. Since there is such a correlation between mental attitude and health, it would be best to keep a positive attitude all the time to keep the immune system at its peak. However, this is not always possible and certainly not practical. All one can do is try and maintain a peace of mind, eat and supplement their diet properly, be aware of stress thresholds, and take additional nutrients, such as DLPA, during times of stress.

If norepinephrine depletion is responsible for creating feelings of helplessness, then phenylalanine or tyrosine should be very effective at restoring levels of norepinephrine. This has been found to be true in clinical studies. However, supplementing with tyrosine is not as safe as with phenylalanine due to sometimes causing erratic decreases in blood pressure.