Palmitoylethanolamide

What is N-Palmitoylethanolamide?

N-Palmitoylethanolamide, is relatively new to most customers, and is sold first as a medicine in Netherlands under the trademark of PEAPURE for the treatment of Nerve Pain or Migraine. However, n-palmitoylethanolamide is now popularly marketed in the United States and Europe as a dietary supplement ingredient in the formulas of sports nutrition for joint support, pain release, etc.

According to Wikipedia, N-Palmitoylethanolamide (PEA), an endocannabinoid, belongs to a family of endogenous (body-own) lipid amides. It is secreted by human adipocytes and possesses anti-inflammatory, analgesic, possibly vasomodulation properties, a significant antiepileptic effect and may be used in treatment of anxiety disorders and anti-depression.

Since 2012 it is also available in the USA and it is shipped to the the USA via the Netherlands. Meanwhile there are many hundreds of satisfied US citizens using this natural painkiller.

Development of N-Palmitoylethanolamide

Since 2008, N-Palmitoylethanolamide has been marketed as a food for special medical purposes in Italy and Spain, under the brand name Normast (Epitech Srl). Recently, a food-supplement named PeaPure was introduced (JP Russell Science Ltd.). In the USA, N-Palmitoylethanolamide is under evaluation as a nutraceutical for inflammatory bowel syndrome (proposed brand name Recoclix, CM&D Pharma Ltd.; Nestlé).

Since 2014 there is also available a new N-Palmitoylethanolamide cream, to enhance the effects of N-Palmitoylethanolamide(PEA) also via the thin nerves in the skin.

ORIGIN AND OCCURRENCE OF N-Palmitoylethanolamide

PEA, also called palmitoylethanolamide or palmidrol by some authors, is a naturally occurring C16:0 fatty acid derivative where the carboxylate function is amidated by the primary amine of ethanolamine. Its chemical name is N-(2-hydroxyethyl)hexadecanamide. PEA was first synthesized by refluxing ethanolamine with palmitic acid giving white crystals melting at 98-99°C.
The evidence that PEA is a natural compound came from Kuehl et al. who isolated PEA from soybean lecithin, egg yolk and peanut meal. In 1965 Bachur and co-workers

Mechanism of action of N-Palmitoylethanolamide

How does N-Palmitoylethanolamide work? Nobel laureate professor Rita Levi-Montalcini discovered the mechanism of PEA related to its inhibitory effects on activated mast cells, a kind of inflammation cells inducing inflammation and pain. She also explained that PEA counteracts NGF, a pro-inflammatory growth factor.

Mast cells play a key role in inflammatory reactions triggered by tissue injury or immune activation. The endogenous molecule capable of modulating inappropriate mast cell activity discussed was N-(2-Hydroxyethyl)hexadecanamide (palmitoylethanolamide).

N-Palmitoylethanolamide and anti-inflammation

The anti-inflammatory effect of PEA is partly linked to its modulation of mast cells degranulation, as has been shown via histological analysis and by the inhibition of the release of several pro-inflammatory enzymes such as iNOS, chymase and metalloproteinase MMP-9), as well as mediators such as nitric oxide and TNF-α.

Palmitoylethanolamide kills pain via natural descending neuronal pathways
Palmitoylethanolamide is a natural painkiller. There are many mechanisms via which PEA excerts its analgesic actions. One mechanism becoming more in the forus of neurobiology is via the inhibition of the spinal system through various brain area’s:
Increased levels palmitoylethanolamide (PEA), increased in three brain areas of the descending antinociceptive system, i.e. the dorsal raphe (DR), the periaqueductal gray (PAG) and rostral ventromedial medulla (RVM) , as well as in the spinal cord (SC) following chronic constriction injury (CCI) of the sciatic nerve in the rat. This is nature’s own way to counteract pain.

PEA, operating at both spinal and supra-spinal levels thus becomes up-regulated during neuropathic pain and therefore many pharmaceutical companies are looking for new substances with the possibility to patent, that inhibit PEA inactivation and might be therefore useful in the treatment of neuropathic pain. Fort the time being these inhibitors suffer from a great many side effects, and simple supplementation of pure PEA therefore seems the golden standard.

Benefits of taking N-Palmitoylethanolamide supplements
N-Palmitoylethanolamide has been shown to have anti-inflammatory, anti-nociceptive, neuroprotective, and anticonvulsant properties. And many sports nutrition supplements are starting to use it in formulas of joint supports, brain health, together with natural products like Cissus Quadrangularis, SAMe, MSM, glucosamine, chondroitin,etc.
Chronic Pain
A Wikipedia article suggests PEA may be most effective in chronic pain disorders such as peripheral neuropathy, chronic regional pain syndrome (CRPS), sciatica, and nerve entrapment. A recent study suggests it could be helpful in Fibromyalgia.
For many weightlifters and bodybuilders this is their joints. Tendons and ligaments bear the brunt of punishing weight-lifting sessions, commonly becoming inflamed and sore.

The connective tissue just can’t keep up with the heavier and heavier weights lifted week after week.
Niggling pains become chronic injuries, often requiring a forced rest, a change of routine or the permanent dropping of some exercises altogether.

Hesselink reports that clinical trials involving over 6,000 people have established PEA’s effectiveness in treating chronic pain and inflammation. Animal models suggest PEA is able to prevent or inhibit two key processes in production of chronic nerve pain: nerve sprouting and dorsal root ganglia activation. cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS). Why is PEA not better known in the West? PEA appears to been used in Italy and Spain for quite some time. Interest picked up in the Netherlands and Germany when a Netherlands distributor came on the scene. It’s hardly known in the U.S., although Palmitoylethanolamide For Pain reports that “many people” on the West coast of the U.S. as well as Australia and Canada are using it.

Side effects of N-Palmitoylethanolamide
Since N-Palmitoylethanolamide is an endogenous fatty acid, and there is no any troublesome adverse effects and easy to use to reduce pain, even together with other drugs. There are no known significant adverse effects about N-Palmitoylethanolamide have been reported.
N-Palmitoylethanolamide dosage
N-Palmitoylethanolamide is available as capsules of 400 mg (step in dose: take 1200 mg daily).
Where to buy N-Palmitoylethanolamide?
Bulk N-Palmitoylethanolamide is under mass production from Herb Nutritionals Co., Ltd. All information regarding specifications, certificate of analysis (COA), MSDS, and pricing for N-Palmitoylethanolamide is available. Our aim is to offer the best quality PEA ingredient for sports nutrition industry.