DLPA COMPLEX
Package of 60 Capsules
Lamberts
DLPA COMPLEX - Lamberts
Cod. inatural: lmb10305
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Package of 60 Capsules.
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DL-Phenylalanine (DLPA) the natural therapeutic and analgesic agent - LAMBERTS
Introduction:
What is the DLPA?
DLPA is a 50:
50 mixture of the two forms of essential amino acid phenylalanine. D indicates the dextro, meaning the right shape, the L indicates levo, or left shape. Each is the mirror image of the other. Thus, there are two stereoisomeric forms which are known, which means that a solution of D-phenylalanine will rotate polarized light to the right while a solution of L-phenylalanine will rotate towards the left. From all points of view, in aspects of their molecular structures, the two are identical. The 50:50 mixture of DLPA is called racemic because polarized light rotates, since the left and right rotations cancel each other.
In nature, the way of all the amino acids L is always the preferred amino acids and proteins of all foods are of the variety L. This preference is applicable to all types of proteins, animals, plants and microorganisms. However, Nature rarely produces an amino D. For example, one found in the structure of some antibiotics and are also in man-made drugs, having been found application in medicinal drugs produced by fermentation and chemical synthesis.
Although the two forms of phenylalanine appear identical in terms of its chemical constitution, differ considerably in their biological properties. As we will see now. L-phenylalanine (LPA) is a component of proteins and have other properties which are not related to them, but the D-phenylalanine (DPA) has no function in protein structures and exhibits properties that have nothing to do with the other form. DPA is not found in natural products, but can be synthesized in the laboratory.
The racemic mixture of DLPA is also produced by chemical methods. However, although it is selective nature as to produce and use only the L-form is easy to produce chemicals 50:50 mixture, as in chemical reactions appear equally likely to produce both L and D forms The task of producing synthetically pure DPA is a very complicated issue and so the DPA is about ten times more expensive than DLPA. However, the latter provides 50% DPA and DLPA doses then can be adjusted to provide the required intake of DPA.
There is no antagonism between the two forms of phenylalanine DLPA contained in (1) and while the LPA is mainly nutritional, DPA is purely therapeutic. The human body is able to convert about 0.5 g of DPA in LPA day, but has not found any evidence that the LPA can be retransformada in DPA (2). This fact was established experimentally by administering to young subjects diets containing no LPA, but with a content between 1.1 and 2.2 grams per day of DPA. These subjects fell into a negative nitrogen balance, indicating that the agency could not use the DPA as a component in the synthesis of proteins. When they returned to supplement with DLPA, passed all a positive nitrogen balance, indicating the absence of antagonism between the two forms.
How does DLPA?
A review of existing literature reveals that DLPA is mainly used as a painkiller. It has also been found useful in treating depression, alleviating the symptoms of arthritis and conditions of premenstrual syndrome. Among the less well-established therapies with DLPA include Parkinson's Disease, Multiple Sclerosis and Vitiligo.
The best aspect investigated in therapy with DLPA, is the role it plays as an analgesic, but to understand it in all its significance, it is necessary to first consider painkillers naturally produced by the body, called endorphins.
One of the most intriguing questions that has preoccupied humans for centuries, is why some people can tolerate pain better than others. In animals, as in humans, it is known that the reaction of "fight and flight" response to danger induces changes in the body that prepare the animal to resist or to get away from danger and one of these changes is to increase resistance to pain.
This increased resistance is motivated by increasing production inside the body's own natural painkillers called endorphins we. The fact that some people have a greater ability than others to produce these painkillers, means they can tolerate pain better. The discovery of endorphins in the early seventies, was the direct result of research conducted on how to morphine, which is the most powerful painkillers produced in nature, acts with pain-suppressing properties. Morphine is a component of opium, which is derived from the poppy bulbs and therefore is considered an opiate.
During these investigations it was found that an injection of morphine administered directly into the brain, generating a thousand fold higher analgesic activity than the same amount of morphine injected into a muscle.
This observation suggested that the brain must have specific receptors that were highly sensitive to morphine. This finding was unexpected, given that morphine is a substance foreign to the body, then had to be asked a question: "Why would such recipients developed brain?" The brain is the only organ that has this feature, and also other receptors have been found in areas of the spinal cord, which are related to the modulation of pain (3).
These centers opiate receptors in the brain are not only related to pain relief and others have been discovered in the brain region known as "limbic system". The entire system consists of a set of brain structures that have long believed is related to the regulation of emotional states. The fact that these areas are also in abundance opioid receptors, probably explains the feeling of euphoria experienced by taking morphine. This property is distinct from the analgesic effect of morphine, but also appears to be articulated through it and other opiates (ie, endorphins). Thus, the ability to produce euphoria, which is easier in some individuals than in others, could also be explained by its efficiency in their own production of endorphins.
How DLPA intervenes in the production of endorphins
The expression Endorphin is the contraction of two words endogenous morphine because, although not morphine itself occurs within the brain, other morphine-like substances with similar properties do occur there.
Following the discovery of opiate receptors, a career started investigations in order to determine natural endorphins or opiates existed and were isolated and identified a number of compounds related to these products. The first discovered by Hughes group at the University of Aberdeen (4), were named methionine-enkephalin and leucine-enkephalin, differing from one another by the presence of the normal amino acid. Both are peptides, i.e., structures of various amino acids combined with each other.
Other compounds that were discovered later, include the beta-endorphin, alpha-endorphin, dynorphin, and others. One of these, beta-lipotropin, contains 91 amino acids, including methionine appears built-enkephalin. The beta-lipotropin as no opioid activity by itself, but acts as a precursor of active endorphins mentioned before, each of which constituy a separate section within the chain of lipoproteins.
From these findings, and the appearance of these natural opiates, modern nomenclature now identified three distinct families of peptides, which are enkephalins, endorphins and dynorphins.
One might think that these substances are the natural response against chronic pain. However, their therapeutic use raises different problems. All are peptides and thus protein digestive enzymes in the digestive tract, the break in individual amino acids and its activity is lost.
Therefore, the oral therapy is useless. Actually it should be injected directly into the brain or spinal cord to place them correctly and at the same time, avoid the digestive system. However, this method is impractical for long-term therapy, besides being very costly from an economic standpoint.
However, clinical studies have been conducted that indicate a great effectiveness in injected endorphins (5,6,7), so that it is already known that this pathway may result. However, despite its efficacy, the injected activity of endorphins is not durable because, like many naturally occurring agents, are rapidly broken by enzymatic action. The naturally occurring endorphins are subject to the same treatment. Any agent who was able to slow this breakdown would allow natural endorphins or injected maintain its activity for a longer time period. This inhibition of enzymes is the basis on which the DLPA operate and DPA.
There are a number of enzymes involved in the degradation of endorphins and enkephalins produced by nervous tissue and in vitro experiments have indicated that DPA very significantly inhibits enzymes that destroy the enkephalins. The magnitude of the inhibition varies depending on the source of opioids, according to whether the hypothalamus, the striate cortex or spinal cord nervous system of mice (8). Confirmation of these findings in intact mice has been reported by Balagot and his group (9). They found that when mice injected with DPA were compared with those who had not been, the levels of methionine-enkephalin in three regions of the nervous system is maintained for at least 6 days in the mice treated with DPA. Having established that the DPA effectively inhibits breakdown of endorphins and enkephalins in intact animals, we proceeded with the tests on humans.
Human trials with DPA and DLPA
(I) Pain Relief
In one of the first investigations (10) on the relief of chronic pain with endorphins, 32 patients with chronic pain were taken far endorphin levels in the spinal fluid. All patients were given a placebo and then were told that it was a new drug that would provide pain relief. Fourteen of these patients reported after they had experienced in their pain relief and, in the same group, all increased endorphins in the spinal fluid, although they had been treated with a sugar pill harmless. Therefore it can be assumed that the mere suggestion that a painkiller had been enough to stimulate production in these patients extra pain-killing endorphins. This indicates that the placebo effect in reducing pain is strong and you have to give him an edge in any study about pain relief.
Experimental evidence on pain relief using DPA have yielded equivocal results. There has been significant pain relief in a study in which 43 patients, especially with osteoarthritis were administered 250 mg of DPA, three to four times daily for 4-5 weeks. The improvement was not apparent until the last two weeks of therapy and so obviously DPA levels were up in the body to achieve these effects. The effectiveness of DPA increased with the decrease in severity of pain in this study (9). This report suffered criticism, according to which the statistical analysis of the data using a binomial distribution of probabilities revealed that the effect of the DPA is negligible (11). However, this study did suggest that a longer therapy have more significant beneficial effects produced.
In a double-blind crossover study, conducted on 21 patients with chronic pain, seven noted more than 50% pain relief after 2 weeks of treatment with administration of 250 mg three times a day DPA. For all patients had stopped the medication to which they were subjected, while taking DPA and not noticed any pain relief administrárseles placebo. Of the remaining 14 patients, one experienced improvements, both the DPA and placebo, while the other 13 showed no improvement, nor the DPA or the placebo. With this level of dosage, side effects of DPA and placebo were the same (12), suggesting that the amounts administered were perfectly safe.
A similar dose (250 mg or 750 mg of DPA DLPA three times daily, 15-30 minutes before meals), administered another test done on 10 patients with benign chronic pain, provide relief from substantial and total, usually within a period of 2-3 days. This action is extremely fast for the DPA and could reflect the conditions in which patients were treated, among whom were the post-surgical minor aches, back pain, osteoarthritis, cervical contracture, rheumatoid arthritis, and attacks myofasciitis migraine (13). Balagot patients (9) were subjected to two weeks of therapy with DPA before experiencing pain relief, but it is a well known phenomenon that the response to an analgesic anyone can vary considerably from one individual to another.
Not all the DPA investigations have yielded beneficial effects on pain relief. Walsh and his group (14), who have expressed criticism of the results of Balagot (9) conducted a double-blind pilot study on 30 patients with chronic pain who were not relieved with analgesics different therapies. These patients received either DPA 250 mg four times daily, or placebo (lactose) for 4 weeks, before crossing over a period identical with another treatment. Pain was quantified using a visual analogue scale of pain and a cold pressure test. The results suggest that the DPA was no better than placebo in relieving pain in these patients. Inconsistent results were also obtained in both normal and hypertensive patients suffering from headaches, treated with the same conventional dose of DPA (15). Two other enkephalinase inhibitors alleviated pain syndromes of migraine and other headache dolore in the same investigation.
Although the tests are few in number, there is also experimental evidence that the DPA can enhance an acupuncture-induced analgesia. There are individuals who respond while others do not respond to acupuncture when it is applied to relieve pain. Managing DPA both patient groups before acupuncture treatment, it was found that this amino acid produced increases in pain threshold and greater persistence of analgesic in patients who responded to acupuncture. In the group of non-responders, half of them also showed increases of these criteria after treatment with DPA. In patients treated with placebo acupuncture before these criteria were not potentiated (16). Similar results were observed in animals subjected to acupuncture.
(II) Depression
Depression is described as a mental state characterized by excessive sadness but whose activity can be agitated and restless or slow and delayed. The general behavior is governed by beliefs pessimistic or hopeless, with derangement of sleep, appetite and concentration. Endogenous depression is having a state of depression caused by influences arising within the body or derived from it. Symptoms of depression include early morning, irregular sleep settings and lack of initiative, with feelings of hopelessness and helplessness. Therapy is usually strong antidepressant drugs. The first indications that DLPA could play a role in alleviating the symptoms of endogenous depression Yaryura the reported Dr. Tobias, that their patients treated with DPA (250 mg twice daily) or DLPA (750 mg twice daily), administered for several weeks. Ten patients showed a substantial reduction in symptoms after 5 days and in the other five patients this amino acid enhanced the therapeutic effects of the drugs were prescribed (18).
A study in another medical center indicated that 17 out of 23 patients treated with DPA or DLPA were relieved of their symptoms of endogenous depression despite the fact that conventional drugs had not previously avail. They all returned to a normal state of complete euthymia, after 13 days (19). These findings were confirmed in an open, more complete, on 20 patients with different types of depression (20). After treatment with DLPA (75 to 200 mg a day before meals) 80 percent of these patients showed reduced symptoms and moderate total. In another double-blind pilot study, these same researchers administered the DLPA dose of 150-200 mg to 14 depressed patients, and treated with 150-200 mg of imipramine (a well known antidepressant drug) to another 13 patients were then switched to the other therapy. Both treatments alleviated depression in equal measure to all patients (21).
In the most important test of this type, conducted on 400 patients, including 370 who had suffered from endogenous depression, were administered to 200 mg of DLPA a day. Physical and psychiatric assessments were performed every seven and five days respectively. After 15 days of treatment, 73 percent did not have any symptoms of depression and 23 percent had relief from most symptoms. After sixty days of therapy, 80 percent had symptoms disappeared and another 15 percent had experienced more relief. Only 4 to 5 percent failed the response (22).
We have seen above, in one of the tests that DLPA was at least as active as the drug imipramine (21). Another group of researchers confirmed these findings in tests on 60 patients (22) in a double-blind control. Patients were divided into two groups for 15 days and one group received 200 mg of DLPA and the other received 200 mg of imipramine. Over the next five days both groups received a placebo and, within 10 days following each of the groups returned to their original medication. The evaluation of the responses indicated that the percentage of patients showing improvement was as follows, with the figure for DLPA first 15 days - 83% and 57%; period of 5 days of placebo - 12% and 9 % after 30 days and 73% -83%. These figures include total and partial responses to therapy. L-Phenylalanine also plays a role in alleviating the symptoms of depression, but is primarily effective in bipolar depression (23).
(III) Rheumatoid Arthritis
The use of DLPA as an analgesic in osteoarthritis has already been mentioned here, but this amino acid also appears to have anti-inflammatory properties as in this condition. There is one case report of a 47 year old with a history of 18 years of AR, presenting a marked inflammation and swelling of the back of your hands until the knuckles concealment. After seven days of treatment with 750 mg of DLPA three times a day, 15-30 minutes before each meal, the pain was gone and the swelling had reduced to make visible the knuckles. Furthermore, the flexibility of the joints so had improved substantially. This therapy may require a period of not less than three weeks for improvement to make an appearance but if after this time there is no response, the dose may be doubled DLPA for another 3 weeks (24).
(IV) Parkinson's disease and Multiple Sclerosis
At least one report indicating that DLPA may prove beneficial in the treatment of patients with Parkinson's Disease. Fifteen patients received 250 mg twice daily DLPA 30, minutes before meals. After 4 weeks, repeated neurological, significant improvements were observed in terms of stiffness, gait difficulties, irregularities in the speech and mental depression. However, no improvement in tremor (25) associated with this condition.
The transcutaneous electrical nerve stimulation (TENS) is a recognized treatment for multiple sclerosis and other neurological disorders. In a double-blind pilot study, this technique was combined with oral therapy DPA. A total of 50 patients (12 men and 38 women) received double therapy and 49 of them improved in certain aspects of their status. Thus, it was found better bladder control, greater mobility and less depression in which showed a response. No explanation was given about these improvements and why DLPA could enhance TENS therapy, but the effects were real (26).
(V) Vitiligo
This is a state in which some of the skin plates lacking the natural pigment called melanin. It is not considered to constitute a state belonging to the medical pathology but rather a cosmetic problem, but may result in psychological stress in affected persons. Phenylalanine at doses of 50 mg per kilogram of body weight orally, followed by 30-45 minutes of exposure to ultraviolet light. It has been argued that a short exposure restores pigmentation in the affected areas (27). In addition, patients who have responded to this therapy have acquired the ability to tolerate the sun on vitiligo lesions. The answer is usually slow, but may be needed about 32 treatments lasting four months to achieve improvement.
It is perfectly clear DLPA function in this treatment but something can be inferred, since this amino acid is a precursor of L-tyrosine, which in turn is the starting material in the production of melanin.
(VI) Premenstrual Syndrome
Among the many symptoms that are PMS, those described as acute abdominal contractions and unrest exactly match the typical symptoms of withdrawal from a narcotic. These observations led to the intriguing suggestion that perhaps the premenstrual syndrome may be the result of a temporary disruption of domestic production of opiates endorphins. There is biochemical evidence that any connection is based on the fact that endorphins maintain an interaction with a number of female hormones (28). Other research has found that brain endorphin levels fluctuate significantly throughout the course of the menstrual cycle (29). These results confirm previous reports in the sense that there is a link between PMS and endorphins (30) and the possible relationship between withdrawal or imbalance of endorphin in specific menstrual syndromes and postnatal depression (31 ).
Based on this and other evidence, it is likely that the complex of symptoms of premenstrual syndrome is at least partly due to a temporary interruption of an endorphin. This would explain the much earlier observations that the lowering of the threshold of pain is one of the three main symptoms of premenstrual syndrome (32). Our current understanding of the function of maintaining in DLPA opioid activity of endorphins may explain the action of this amino acid in alleviating some of the symptoms of premenstrual syndrome. We have seen that DLPA can help in relieving depression and endogenous type this is one of the most common symptoms of PMS.
There are many specific tests performed to determine the action of DLPA in the treatment of premenstrual syndrome that have been reported in the medical literature, but Dr. Arnold Fox, in his book DLPA (published by Long Shadow Books, USA) recommended following regime: DLPA 375 mg with breakfast and lunch. If this dose is not effective, can be increased to 375 mg DLPA with each of the three meals. The amino acid is administered 4-7 days before menstruation and treatment is stopped when menstruation stops. DLPA is compatible with all other treatments of premenstrual syndrome.
How Safe Is DLPA?
Although DPA is an amino acid, it is not in feed protein content and, as unnatural stereoisomer of the native L-phenylalanine (LPA), must be considered as a foreign substance to the organism. Therefore, it is important to determine if its intake is safe. Most of our knowledge about the potential side effects of the DPA (either pure or 50% in the DLPA) comes from clinical trials and experiments on patients.
Clinical Trials:
D-phenylalanine administered orally as D-isomer or racemic component (50% DPA) to depressed patients in doses varying from 50 to 500 mg / day for 15 days to 6 months, has been associated with effects passenger side or low entity, such as dizziness and headache, and in 1 patient, insomnia with doses above 300 mg / day (19,20,21,25). Phenylalanine concentrations in plasma have been reported in these investigations. Beckmann and his group (19) have reported that there had been no change in blood or urine biochemical, and no changes were observed in blood pressure, pulse and body temperature with the administration of D-phenylalanine.
In an open trial without placebo, oral administration of D-phenylalanine in divided doses for a total of 750 to 1,000 mg / day for 4 to 5 weeks to 78 patients with chronic pain, was found to be associated with side effects in 22 cases (28 percent) among whom were: somnolence in 7, nausea in 4, increased frequency of bowel movements in 4, 3 headaches, irritability exaggerated 2, sweats in 1, and an allergic rash in 1 (9). Three tests double blind placebo control and cross-oral administration of D-phenylalanine included some mention of side effects. In the first, two of 22 adult patients with severe pain who were administered 750 mg / day of D-phenylalanine in divided doses for 3 weeks experienced vomiting and temporary light, nausea and drowsiness. Two additional patients experienced these side effects with both D-phenylalanine as placebo (12). No changes hematological, hepatic or neurological effects in 30 patients treated with 1,000 mg / day of D-phenylalanine in divided doses for 4 weeks to treat her chronic pain (14). A light sedation with fatigue occurred in an unspecified number of patients, but no abnormal laboratory findings reported physical or when doses above 600 mg / day were administered to 19 adult patients with disorders of attention deficit (39) .
Urinary excretion of phenyl-ethyl-amine was not increased with a single infusion of 100, 300, or 600 mg of DL-phenylalanine in 6 healthy adult volunteers (34). Similar results were observed in 22 hyperactive children 6 to 12 years of age, who were orally administered D-phenylalanine (20 mg / kg of body weight per day, or 600 mg / day per 30 kg body weight) for 2 weeks (35). No side effects were reported in the latest study was double-blind placebo-cross.
Security level in human intake:
In these limited research on human beings, D-phenylalanine doses ranging from 50 to 1000 mg / day for up to 6 months duration have been associated with the presence of side effects. In the absence of a systematic evaluation of the effects of the administration of D-phenylalanine is not possible to estimate a maximum level of safety for oral ingestion of D-phenylalanine.
Dr. Len Mervyn
Clinical Biochemist great reputation both for his work on vitamin B12 essential, for the discovery of ubiquinone or Coenzyme Q10. Standard has written extensively in the field of nutritional supplementation. Is Lamberts Healthcare Consultant Ltd., a member of the Royal Society of Chemistry and a member of the Academy of Sciences in New York.
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