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Topic starter
04/09/2018 4:43 am
DL-phenylalanine markedly potentiates opiate analgesia - an example of nutrient/pharmaceutical up-regulation of the endogenous analgesia system
by
Russell AL, McCarty MF.
Brampton Pain Clinic,
Bramalea, Ontario, Canada.
Med Hypotheses 2000 Oct;55(4):283-8
ABSTRACT
In the author's clinical experience, concurrent treatment with DL-phenylalanine (DLPA) often appears to potentiate pain relief and also ease depression in patients receiving opiates for chronic non-malignant pain. An analysis of this phenomenon suggests that it may be mediated, at least in part, by up-regulation of the 'endogenous analgesia system' (EAS), a neural pathway that projects caudally from medullary nuclei to the dorsal horn of the spinal column; when stimulated by chronic pain or therapeutic measures such as opiates or acupuncture, the EAS suppresses activation of second-order pain-receptive neurons in the dorsal horn, and thereby alleviates pain. Since serotonin and enkephalins are key neurotransmitters in the EAS, it is reasonable to predict that measures which promote serotonin activity (such as 5-hydroxytryptophan and serotonin-reuptake inhibitors) as well as enkephalin activity (such as D-phenylalanine, an enkephalinase inhibitor) should potentiate EAS-mediated analgesia - a view consistent with much previous medical research. Comprehensive support of the EAS with well-tolerated nutrients and pharmaceuticals may amplify the analgesic efficacy of chronic opiate therapy, while enabling dosage reductions that minimize opiate side-effects. Analogously, this approach may complement the efficacy of acupuncture and other analgesic measures that activate the EAS.
04/09/2018 5:38 am
This interests me as I like to use Ultram (tramadol) for its mood enhancing (opiate ) effects..150mg puts me in a wonderful state of mind..especially after not sleeping well or a bout of depression..
The problem lies after using it for 2-3 days where a crash causes heavy muscular fatigue for a day or two..nothing a good sleep can't remedy..I'd be willing to try DLPA to see if I could decrease the dosage, maybe to 100mg spread out over the day..
04/09/2018 6:11 am
interesting.
jhb
Topic starter
04/09/2018 6:48 am
I have been considering using D-L-phen in conjunction with selegiline as D-phen also partially converts into PEA and selegiline, being an MAO-b inhibitor, slows the break down of PEA.
"D-phenylalanine, which does not normally occur in the body or in food, is metabolized to phenylethylamine (PEA), an amphetamine like compound that occurs normally in the human brain and has been shown to have mood-elevating effects. Decreased urinary levels of PEA (suggesting a deficiency) have been found in some depressed patients. Although PEA can be synthesized from L-phenylalanine, a large proportion of this amino acid is preferentially converted to L-tyrosine. D-phenylalanine is therefore the preferred substrate for increasing the synthesis of PEA--although L-phenylalanine would also have a mild antidepressant effect because of its conversion to L-tyrosine and its partial conversion to PEA. Because D-phenylalanine is not widely available, the mixture D,L-phenylalanine is often used when an antidepressant effect is desired"
L-deprenyl plus L-phenylalanine
in the treatment of depression
by
Birkmayer W, Riederer P, Linauer W, Knoll J
J Neural Transm 1984; 59(1):81-7
ABSTRACT
The antidepressive efficacy of 1-deprenyl (5-10 mg daily) plus 1-phenylalanine (250 mg/day) has been evaluated in 155 unipolar depressed patients. Both oral and intravenous administration showed beneficial effects in 90% of outpatients and 80.5% of inpatients. It is concluded that this combined treatment has a potent antidepressive action based on the accumulation of 1-phenylethylamine in the brain.
Topic starter
04/09/2018 7:23 am
After reading this study, one may well be able to reduce tramadol dose by the addition of both DL-phenylalanine and 5-Htp...
A risk-benefit assessment of tramadol
in the management of pain
by
Radbruch L, Grond S, Lehmann KA
Department of Anaesthesiology,
University of Cologne, Germany.
[email protected]
Drug Saf 1996 Jul; 15(1):8-29
ABSTRACT
Tramadol is a cyclohexanol derivative with mu-agonist activity. It has been used as an analgesic for postoperative or chronic pain since the late 1970s, and became one of the most popular analgesics of its class in Germany. International interest has been renewed during the past few years, when it was discovered that tramadol not only acts on opioid receptors, but also inhibits serotonin (5-hydroxytryptamine; 5-HT) and noradrenaline (norepinephrine) reuptake. This review aims to provide a risk-benefit assessment of tramadol in the management of acute and chronic pain syndromes. Tramadol has been used intraoperatively as part of balanced anaesthesia. Such use is under discussion, however, as it was associated with a high incidence of intraoperative recall and dreaming, and postoperative respiratory depression has been described after intraoperative administration of high doses. Postoperatively, intravenous and intramuscular tramadol has been used with good efficacy. Analgesic doses were comparable with pethidine (meperidine) and 10 times higher than morphine. Nausea and vomiting were the most frequently reported adverse effects. In controlled studies, haemodynamic and respiratory parameters were only minimally impaired. The risk of severe respiratory depression in typical dosages is negligible in comparison with other opioids used for postoperative pain management. Tramadol has been used with good results for the management of labour pain without respiratory depression of the neonate. It was also effective for the treatment of pain from myocardial ischaemia, ureteric colic and acute trauma. Good results have been published for cancer pain management with tramadol in several studies. The potential for abuse or addiction seems to be minimal, and serious complications have not been reported. For patients with severe pain, the efficacy of morphine is superior, and most patients with adequate analgesia from tramadol had to be changed to a more potent opioid after a few weeks due to increased nociceptive input during tumour progression. Tramadol can be recommended as a safe and efficient drug for step II according to the World Health Organization guidelines for cancer pain management.
Topic starter
04/09/2018 8:08 am
I have also been lucky enough to have had some opium which I had tinctured. I found it most useful at the end of stressful week at a minor dose (1 drop) I would never taken it for more than 2 days and I had no desire to habituate the use of the tincture either, which surprises me, as I have quite an appetite for pleasure. My girlfriend also found it very useful for period pains, again she may have taken a dose once a month.
04/09/2018 8:53 am
Thanks Psimonkey..
I've seen these studies before and was always aware of DL-phen as a mood enhancer through PEA..the problem is it hasn't worked for me..I've high dosed l-phen with better results, but as stated, through a different conversion of l-tyrosine..not always the best mood enhancer..I'm gonna try the dl with the tramadol..I'm looking forward to trying selegiline as there introducing a patch sometime soon..(Esram?)..word has it that its much smoother than the liguid or tabs without the jitters..If you like an opium effect, I highly reccommend tramadol..Its a wonder drug for me as it works within an hour and really brightens my day..Its good for about 3-4 days then needs to be stopped or tolerance develops..its also habit forming..don't believe the hype.. AND there available overseas..
Miggy
Topic starter
04/09/2018 9:39 am
Thanks for that Miggy, I will look into it for sure.
EMSAM (R) info
Bristol-Myers Squibb and Somerset Pharmaceuticals Enter Into Agreement to Distribute and Commercialize EMSAM, Investigational Transdermal Treatment for Major Depressive Disorder
NEW YORK and TAMPA, Fla., December 22, 2004 /PRNewswire-FirstCall/ -- Bristol-Myers Squibb Company
BMY and Somerset Pharmaceuticals, Inc., a joint venture between Mylan Laboratories Inc. and Watson Pharmaceuticals, Inc., today announced they have entered into an agreement for the commercialization and distribution of Somerset's EMSAM(R) (selegiline transdermal system), an investigational monoamine oxidase inhibitor administered as a transdermal patch for the acute and maintenance treatment of patients with major depressive disorder. Somerset received an "Approvable" letter from the U.S. Food and Drug Administration (FDA) for EMSAM(R) in February, 2004, and if approved by the FDA, EMSAM(R) would be the first transdermal treatment for major depressive disorder.
Under the terms of the agreement, Bristol-Myers Squibb receives exclusive distribution rights to commercialize EMSAM(R), if approved, in the U.S. and Canada, with an opportunity to negotiate, within a specified time frame, rights in any or all of the rest of the world. Financial terms were not disclosed, however, Somerset will receive an upfront payment and a further payment following regulatory approval in the U.S. In addition to the upfront payment, Somerset will receive milestone payments based on achievement of certain sales levels, as well as the reimbursement of certain development costs incurred over the term of the agreement. Somerset will supply product to Bristol-Myers Squibb and receive royalties on Bristol-Myers Squibb sales of EMSAM(R).
"This agreement with Somerset Pharmaceuticals marks a continued step forward in our efforts to deliver new and effective treatments to people with psychiatric disorders," said Anthony Hooper, president, U.S. Pharmaceuticals, Bristol-Myers Squibb. "This collaboration exemplifies our new corporate strategy which focuses our efforts on 10 disease areas, including affective disorders such as major depressive disorder. We look forward to partnering with Somerset in a venture that could provide an alternative for physicians treating patients with this disorder."
"We are excited to announce that we have partnered on EMSAM(R) with Bristol-Myers Squibb, which has a strong record in neuroscience," said Mel Sharoky, M.D., Somerset's president and chief executive officer. "Together with our partner, we look forward to working with FDA on EMSAM(R) because there is a need for additional treatment options for major depressive disorder. The EMSAM clinical program, to date, has involved more than 2,000 patients with major depressive disorder."
Approximately 19 million adults in the U.S., or close to 10 percent of the American population, suffer from major depressive disorder. Depression costs U.S. employers about $31 billion a year in productivity, not including disability-leave payments.
About Bristol-Myers Squibb
Bristol-Myers Squibb is a global pharmaceutical and related healthcare products company whose mission is to extend and enhance human life. Visit Bristol-Myers Squibb on the World Wide Web.
About Somerset Pharmaceuticals, Inc.
Somerset Pharmaceuticals, Inc. is a joint venture between Mylan Laboratories Inc. and Watson Pharmaceuticals, Inc. .
For more information about Somerset.
About Mylan Laboratories Inc.
Mylan Laboratories Inc. is a leading pharmaceutical company with four subsidiaries, Mylan Pharmaceuticals Inc., Mylan Technologies Inc., UDL Laboratories Inc. and Mylan Bertek Pharmaceuticals Inc., that develop, license, manufacture, market and distribute an extensive line of generic and proprietary products.
For more information about Mylan.
About Watson Pharmaceuticals, Inc.
Watson Pharmaceuticals, Inc., headquartered in Corona, CA, is a leading specialty pharmaceutical company that develops, manufactures, markets, sells and distributes brand and generic pharmaceutical products. Watson pursues a growth strategy combining internal product development, strategic alliances and collaborations and synergistic acquisitions of products and businesses.
For press releases and other company information, visit Watson Pharmaceuticals' Web site.
Forward-looking statement
The parties caution that this press release may contain forward-looking statements, which are made pursuant to the safe harbor provisions of the Private Securities Litigation Reform Act of 1995. Actual future results may differ materially from those expressed or implied by such forward-looking statements due to such factors including, but not limited to, changing market conditions, the availability and cost of raw materials, the impact of competitive products and pricing, the timely development, FDA approval, and market acceptance of Somerset's and its competitors' products, the outcome of litigation and other risks detailed from time to time in the Securities and Exchange Commission filings of Mylan Laboratories Inc., Watson Pharmaceuticals, Inc. and Bristol-Myers Squibb Company. Except as required by law, the parties undertake no obligation to update these statements for revisions or changes after the date of this release.
Mylan Laboratories Inc.; Watson Pharmaceuticals, Inc.
CONTACT: Media - Robert Hutchison, +1-609-252-3901, [email protected], or Investors - John Elicker, +1-212-546-3775, [email protected] , both of Bristol-Myers Squibb; Media & Investors -Melissa Goodhead, +1-813-288-0040, ext. 276, [email protected] , of Somerset; Media & Investors - Patty Eisenhaur, +1-951-493-5611, [email protected], of Watson; Media - Heather Bresch,+1-724-514-1800, [email protected] , or Investors - Kris King,+1-724-514-1800, [email protected] , both of Mylan
Ticker Symbol: (NYSE:BMY),(NYSE:MYL),(NYSE:MYL),(NYSE:WPI),(NYSE:
WPI)
Have you looked into Rasagiline, it appears to have almost all of the benefits and none of the "jitters" that can sometimes be present
I found another link that interested me, may be you too.