By Ritchi Morris, Ph.D., H.M.D., D.N., R.H.
Professional Member AANC
There is a plethora of clinical and research data substantiating the extraordinary therapeutic efficacy of D-L Phenylalanine (DLPA).
In this day and age the incidence of severe acute and chronic pain has been burgeoning progressively. This trend has spanned a multi-million dollar industry of pain control surgical procedures and chemical pain suppressors. Unfortunately, these approaches have not been without debilitating side effects of their own. This experience has motivated health professionals, pain treatment clinics, homeopaths, and naturopaths to seek more natural, less damaging alternatives.
Mother Nature has provided such an alternative:
DL-phenylalanine. Recent empirical studies have documented the efficacy of utilizing this essential amino acid for the control of such chronic and/or acute pain syndromes as lower lumbar back pain, joint pains resulting from rheumatoid arthritis, osteoarthritis, and other usage stresses; migraines; severe premenstrual spasms; neuritis; neuralgia; and postoperative conditions.
Thus, scientific research has demonstrated that relief from the above pain syndromes is available without the necessity of taking any radical measures, simply by supplementing one’s present diet with this spectacular combined form of phenylalanine.
What are amino acids?
One of the most important "essential" amino acids is phenylalanine. Amino acids form the very foundation upon which all the other parts of our bodies rest. For without these "building blocks" the other vital substances (e.g. protein) cannot be processed. These organic acids contain amines that are connected together in specific chains to form polypeptides and proteins. But even amino acids are accountable to a more basic substance: DNA (deoxyribonucleic acid.) DNA contains the "biological blueprints" that delineate the specific ways that the body is built and repaired.
These blueprints specify the variety of ways the body can interact with the environment.
The "messenger service" for the DNA is RNA (ribonucleic acid) which carries out instructions for the formation of polypeptides and proteins. Here the essential amino acids are constructed into chains in order to implement the chemical messages in our blood/body system. There are 26 common amino acids and eight "essential" ones. These eight are called "essential" because they cannot be synthesized by our bodies and, therefore, we must ingest them either nutritionally or via supplementation.
There are three forms of phenylalanine: L; D; and DL. The L form is the most commonly occurring type. The brain utilizes this substance as a precursor to produce norepinephrine (NE). It helps one’s brain restore the depleted stores of NE. For it is well known that stress and overwork tax one’s "brain-well" of NE levels thus leaving one feeling mentally "drained." With the conversion of phenylalanine and another amino acid (tyrosine), vital to this process, the brain’s well of NE can be refilled. As Durk Pearson/Sandy Shaw explain, "You can literally refill the storage pouches on your nerves by using - phenylalanine. Large amounts of vitamin C and B6 are required for the conversion of phenylalanine and tyrosine to NE.(1)
The D-Form derives its name from the fact that the NH2 particle occurs to the right of the carbon particle in this phenyl molecule. Hence, the D stands for "dextro" or right-handed seat, rendering this molecule a mirror-image of the L Form.
The most abundant sources for the D-Form are bacteria and plant tissue. Eventually, this D-Form becomes an L-Form as the human system converts it slowly before it can be assimilated and utilized for its identified bodily functions. (2)
The third or DL-Form is obviously a combination of the two forms above. Not until very recently has much been known or investigated about the D-L Phenylalanine form. However, since phenylalanine exists in all protein that we consume, our metabolic and digestive systems are designed organically to absorb and utilize this form and its by-products without difficulty just as easily as they absorb the separate L- and D- forms.
Until recently, the only major avenue explored for DLPA has been that of weight control. It seems that research by Nobel prize winner Rosalyn Yalow (3) yielded the fact that there is a brain hormone, cholecystokinin (C.C.K.) which seems to control satiation. It was further discovered by Dr. J. Gibbs (4) that this "saity signal" can be modulated by the L- and DL-Forms. Fortunately, with the furor over weight problems and fad dieting in this hemisphere, a dearth of experimentation occurred. From this, the role of DLPA in retarding the breakdown of endorphins and enkephalines (the brain’s natural pain killers and anesthetics) was unearthed.
Furthermore, research has shown that the nutritional value of DLPA rivals that of the L- and D-Forms. In this sense, the toxicity is very low - comparable to that of the complex carbohydrates (sugars occurring in raw fruits and vegetables.) Indeed, Rose, et al. demonstrated that DLPA can be substituted in the human diet for the L-Form without any adverse effects on health. Parenthetically, Rose (5) determined that the daily requirements for each are the same - 2.2 gm./day. Also, it has been shown that DLPA is very non-acidic. For example, it is approximately 1/10th as acidic as ascorbic acid (Vitamin C.)
The purpose of D-L Phenylalanine
Finally, in the last decade, specific values for DLPA have been identified. After years of private research, perhaps the foremost authority on DLPA, Dr. Seymour Ehrenpreis, presented his findings to the Second World Congress on Pain.(6) Dr. Ehrenpreis et al. declared that, at least good, if not excellent relief from pain was observed in every patient using DLPA.
Further documentation of the powerful analgesic capabilities of DLPA were furnished by a 1979 study at the University of Chicago again conducted by Dr. Ehrenpreis (13) In treating various arthritic conditions with average doses of 375 mg. daily, highly significant results were obtained; better than 75 percent of the chronic pain patients experienced good to complete relief within a period of one week to one month. It was also discovered that the DL-Form actually supplants completely the L-Form in the body and nourishes it better than does the L-Form.
We have enjoyed marked success with many patients who had already sought most every medical treatment known - to no avail. The most extreme case of this where I succeeded has been with a 37-year old Viet Nam vet who had been suffering for eight years with crippling pain in his back, neck and extremities. He had sought help from hospitals and doctors (veterans and civilian) and clinics specializing in joint diseases here and in other countries.
The most essential feature of DLPA (aside from its pain- relieving qualities, of course) is that DLPA accomplishes the same as or even better amount of pain-relief than these synthetic invasions of the body, but via natural, non-invasive means.
The function of D-L Phenylalanine
All forms of phenylalanine are intimately associated with several different brain functions. One major link is with the pain relief systems of human (and in mammals in general.) Empirical research has identified such a self-contained system complete with signal activators, response hormones and neuronal sensation relief. When signals of pain (e.g. injury, duress, chronic) from a particular sector of the body reach the brain, the dorphin hormones are released and directed to the given point of trauma.
It appears that man-made pain killers such as morphine, Demerol and Codeine mimic this endorphin substance in that a loss of pain sensation results from saturation with it. The anesthetic power of this endorphine system extends into the realm of chronic pain as well. Further research in the late 1970’s by the Ehrenpreis group demonstrated that inflammatory conditions such as rheumatoid arthritis, osteoarthritis, neuralgia and/or degenerative conditions such as spinal disc damage, body joints, and postoperative pain could be effectively relieved by treatment with endorphine substance. (14)
However, this natural substance pain-relief system does not function without some complications. It has been determined that certain enzymes in the body serve to destroy the endorphins before they reach the particular traumatized areas. It seems that MAO-based enzymes such as carboxypeptidase "A" and "enkephalinase" tend to void the action of endorphins upon contact "pac-man" style. This quandary was averted initially by injecting these endorphins. However, this presented several serious side effects (to be discussed below.)
Recent efforts to solve this dilemma fostered experimentation with various substances known to negate or neutralize MAO and other such enzymes. It was discovered that combining the L- and D-Form of phenylalanine brought about the desired effects upon these enzymes. In effect, the DLPA acts like a downfield blocker in football. It places a "bodyblock" on these enzymes which impedes their contact with the passing endorphins, thereby enabling the endorphins to reach their designated areas of trauma.
The latest interest of the Ehrenpreis Croup (15) demonstrated that the blood of chronic pain sufferers displayed significantly lower degrees of endorphin activity. This was also true for their cerebrospinal fluid levels. Administration of DLPA to these subjects resulted in a rapid normalization of these levels. Herein seems to lie the crux of DLPA’s amazing analgesic power on sources of chronic pain.
DLPA seems to focus on chronic pain only. Studies demonstrate that DLPA does not interfere with or mask the triggering system in the brain for acute, short-term pain (e.g.: lacerations, broken bones, sprains, etc.) while dissolving chronic pain so well. Therefore, DLPA displays a selectivity for the nagging, long-term pains while functioning in tandem with the body’s short-term acute pain system. Furthermore, DLPA plays the crucial role of protecting the brain’s own natural analgesic hormone-endorphin - thus enabling the endorphins to complete their analgesic mission and do so more effectively for a much longer period than that of the pharmaceuticals.
What are the "appropriate" dosages?
It must be emphasized that the "appropriate" dosages for each individual is contingent upon a constellation of factors: body weight; height; duration; frequency of occurrences of the pain syndrome; metabolic type; and age. Also, there are mental and emotional factors that must be considered. For instance, whenever an individual experiences pain, especially of a chronic nature, a "negative feedback cycle" tends to develop. That is, the individual begins to experience anticipatory anxieties or becomes "fear-conditioned" with the onset of the particular pain symptoms or even the mere hint of them. Thus, it is difficult to calculate just what percentage of pain is truly physical and which is mental (expectations) after one has endured chronic, recurrent pain for a while. Hence, I always recommend the "cross-ties" approach at this point: consulting a medical doctor (ortho, neuro, osteo) a homeopath, and a chiropractor in order to cross-reference their diagnoses and recommendations and sift out the common denominators. But, most importantly, one must not delay in seeking these examinations if one has reached this point without relief from consuming DLPA.
All available studies and clinical reports reveal that approximately 85 to 100 percent of the individuals who utilize a DLPA regime properly achieve the relief desired. However, DLPA is not a miracle cure and not every case can be helped. Relief is usually forthcoming within the first week. In most cases, the dosage can be reduced progressively by 500 mg./day every three days until the minimum appropriate dosage for the given individual is established. Once this level is found, it should be taken throughout the day - not in one mega dose.
A last benefit of the use of DLPA is that it can be taken concomitantly with any other prescription pain relievers. It has been demonstrated that such common chemical analgesics like Motrin, Butasolidan, Nalfon and Indocin function quite compatibly with DLPA. Indeed, the majority of clinical reports reveal a much more effective net effect when both are used together than when either is taken alone. Moreover, when DLPA is taken along with aspirin-based formulas
(approximately 3-6 tablets a day) this seems to be the most effective regimen.
As with all substances, there are cautions for the use of DLPA. Host importantly, the proper dosage must be followed strictly. All recent studies confirm that the most effective results are gained by such careful adherence. Secondly, DLPA is not to be taken by pregnant persons or those who are allergic to it (phenylketonurics). Thirdly, people with circulatory problems or hypertension should be careful to take DLPA after meals only. Lastly, this is not a miracle cure and professional help should be sought if no relief is attained as outlined above.
DLPA - Administration & Dosage Schedule
- Form Capsule or tablet
- Strengths 350 or 500 mg
- Initial Dosage Up to 2,000 mg/day
- Phase 1 First 2 weeks
- Phase 2 3,500 mg/day - Weeks 3-6
- Phase 3 (if necessary) 4,500 mg/day - Weeks 7-10
- Ideal level for maintenance: Reduce by 500 mg/day until the discomfort slightly disappears
- Consumption Rate 2-3 times throughout the day. Never in one large dose!
- Consumption Method 15 minutes before or 1 hour after meals and at bedtime on an empty stomach!
- Cautions Stop at 4,500 mg - more is not better
- Always take amino acids on an empty stomach to maximize absorption
If no noticeable relief is detected within 3-4 weeks, continue to increase dosage to a maximum of 4,500 mg/day but, after 2 weeks at this level, consult a healing arts professional.
- Pearson, D. and Shaw, S. Life Extensions–A Practical Scientific Approach. Warner Books, N.Y.C., N.Y., pp. 185-186.
- Ibid. Pearson and Shaw, p. 130.
- Nutrition News, "DLPA in the Nutritional Control of Arthritis and Chronic Pain," Pomona, Cal., 1983.
- Yalow, R. "Nobelist Ties Gut Hormone to Appetite Control by Brain Medical World News, Feb. 5, 1979, p. 18.
- Smith, Gibbs, Young, "Cholecystokinin and Intestinal Satiety in the Rat," Fed. Proc. 33(5): May, 1974, pp. 11-46-49.
- Pert, C. "Oplole Antagonist Counters Obesity," Science News, Feb. 14, 1981.
- Atone, I., "Clonidine HCL Reduces Heroin Withdrawal Symptoms," J. Amer. Med. Assoc., 243(3): Jan. 25, 1980, p. 343.
- Rose, W.C., "Amino Acid Requirements of Man," Nutrition Reviews, Vol. 34(10), 1967, pp. 307-309.
- Ehrenpreis, S., Balagot, R.C., Myles, S. Advocate, C. and Comaty, J.E:, "Further Studies on the Analgesic Activity of D-Phenylalanine in Mice and Humans," Procedures of the International Narcotic Research Club Convention, E. Leong Way (ed.) 1979, pp. 379-382.
- Budd, K. "Use of D-Phenylalanine, and Enkephalinase Inhibitor in the of Intractable Pain," Advances in Pain Research and Therapy J.J. Bonica et al. (ed.), Vol. 5, Raven Press, N.Y., 1983,289-293.
- Bagalot,R.C. et al. Advances in Pain Research and Therapy, J.J. Bonics, et al. (edits). Vol. 5, Raven Press, N.Y., 1983.
- 12K Myles, S.B. , et al. , "Naloxone Reversible Analgesia in Mice Pr~ducedby D-Phenylalanine and Hydrocinnamic Acid, Inhibitors of Carboxypeptidose A." In Advances in Pain Research and Therapy. J.J. Bonica, et al. (edits). Vol. 5, Raven Press, N.Y., 1983, pp. 479-488.
- Op. Clt., Ehrenpreis, et al., 1979, pp. 379-382.
- Ibid, Ehrenpreis, et al:,1978, 1979.
- Ibid, Ehrenpreis, et al:,1978, 1979.
Article Categories: Health Conditions & Chronic Disease