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Le PEA, the universal natural painkiller

palmitoylethanolamide Better known as PEA, palmitoylethanolamide is a natural and powerful active principle discovered in 1957. Since then, it has consistently been the subject of new scientific papers, and with good cause, since this molecule plays a key role in the body’s inflammation and pain processes. PEA offers anti-inflammatory properties and significant analgesic power. Extensively-studied, this natural compound has considerable therapeutic potential. Read on to find out more about PEA’s efficacy in this new article for Nutranews.

PEA’s powerful pain-killing activity

Inflammation- and pain-regulating effects
In humans as in other living beings, PEA plays a role in several biological functions. In the human body, it is primarily known for its painkilling and anti-inflammatory activity. Research has shown that this compound is able to bind to specific receptors, activated by peroxisome proliferator-activated receptor alpha (PPAR-alpha), which are involved in the regulation of pain and inflammation genes. In binding to these receptors, PEA thus modulates pain and inflammatory responses.

Effects on the perception of pain
As well as helping to regulate pain, PEA also appears to have other pain-relieving effects. In particular, it seems to act on CB1 and CB2 cannabinoid receptors which are involved in the immune response and perception of pain. PEA also appears to have an effect on TRPV1 receptors which play a role in nociception, the sensory process responsible for the most common types of pain – acute or nociceptive pain.

A natural compound with significant therapeutic potential

Therapeutic potential of PEA
As a result of its analgesic potency, PEA is often described as a natural, universal painkiller, able to combat both acute and chronic pain. It offers relief from pain of inflammatory and neuropathic origin, as well as that caused by a combination of the two1,2,3..

Benefits of PEA supplementation
PEA is a fatty acid amide which can be synthesised from phospholipids. While it can be produced within the body, PEA can also be hydrolysed by certain enzymes but this hydrolysis greatly reduces its activity. That is why scientists are investigating the benefits of supplementing with PEA. Their research has demonstrated benefits against dental, lumbar and pelvic pain as well as that associated with compression of the sciatic nerve, arthritis, carpal tunnel syndrome, glaucoma, diabetic neuropathy and multiple sclerosis1,2,3,4.. According to recent studies, it could also be useful in treating inflammatory diseases such as uveitis and ulcerative colitis5..

Recognised efficacy of PEA supplementation
Large-scale study on PEA’s painkilling effect
To confirm the benefits of supplementing with PEA, a large-scale study was conducted among a group of people suffering from sciatic pain⁴. Aged between 19 and 72, the 636 male and female volunteers were divided into three groups:
    - the first, a control group, received a placebo;
    - the second was given 300mg/day of PEA ;
    - the third received 600mg/day of PEA.
The three-week study highlighted significant differences between the control group and the two supplemented groups. Using a questionnaire, as well as clinical and laboratory tests, the researchers observed differences, in particular, in perception of pain and quality of life, with both PEA-supplemented groups displaying a decrease in pain perception. Improvements in quality of life were also reported by participants. These improvements were dose-dependent – in those given the 600mg dose of PEA, a reduction in pain of almost 50% was observed. This exceptional finding thus confirms the efficacy of PEA as a painkiller.

Promising results in relation to chronic inflammation of the colon
In addition to its pain-relief effects, PEA is also attracting scientific interest for its anti-inflammatory activity. One study, published in the prestigious journal Gut, investigated PEA’s effects against certain forms of chronic colon inflammation such as ulcerative colitis and haemorrhagic rectocolitis5. Efficacy was evaluated in mouse models with induced colitis, in colon tissue taken from patients with ulcerative colitis and in cultures of enteric glial cells which are involved in the inflammatory process. Using a number of different analyses, researchers reported significant and consistently positive results: an improvement in symptoms of ulcerative colitis and a decrease in pro-inflammatory markers. To expand their understanding of PEA’s anti-inflammatory action, the study’s authors also compared their results with those obtained using PEA combined with antagonists of PPAR-alpha receptors. In this case, no improvement was observed, confirming that it was PEA’s mechanism of action which was responsible for the improvements. In binding to PPAR-alpha receptors, the compound has a role in regulating inflammation, thus helping to combat pain and inflammatory diseases.

Extensively-studied, PEA appears to be a powerful, natural painkiller and anti-inflammatory. With recognised efficacy, PEA supplementation offers significant therapeutic potential for relieving both acute and chronic pain, be it inflammatory, neuropathic or a combination of the two. PEA’s benefits are now available as a nutritional supplement in capsule form from the SuperSmart catalogue: Natural Pain Relief.

> Sources :
1. JM Hesselink et TA Hekker, Therapeutic utility of palmitoylethanolamide in the treatment of neuropathic pain associated with various pathological conditions: a case series, J Pain Res. 2012;5:437-42.
2. M Alhouayek et GG Muccioli, Harnessing the anti-inflammatory potential of palmitoylethanolamide, Drug Discov Today. Octobre 2014;19(10):1632-9.
3. JM Hesselink et al., Palmitoylethanolamide, a Natural Retinoprotectant: Its Putative Relevance for the Treatment of Glaucoma and Diabetic Retinopathy, J Ophthalmol. 2015;2015:430596.
4. JM Hesselink et DJ Kopsky, Palmitoylethanolamide, a neutraceutical, in nerve compression syndromes: efficacy and safety in sciatic pain and carpal tunnel syndrome, J Pain Res. 2015; 8:729-734.
5. G Esposito et al., Palmitoylethanolamide improves colon inflammation through an enteric glia/toll like receptor 4-dependent PPAR-α activation, Gut. 2014 Aug;63(8):1300-12.
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P.E.A., an all-round, natural analgesic

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