Compounding news: PEA and other options in the treatment of pain
Recently codeine has been up scheduled away from “pharmacist only” to “prescription only”, which has given us an opportunity in the pharmacy to have conversations with our patients about more appropriate methods of pain management. Many of the options available to us are natural medicines, so I thought I would share them with you. We can compound these for your patients where a suitable pain relieving solution is not available in the ready-made market.
PEA is a natural compound which is synthesised in human, animal and plant cells. It is a fatty acid derivative with protective, anti inflammatory and restorative effects on the neuroglia, the cells that protect and support the nerve cells. It is produced endogenously from the lipid bilayer of cell membranes in humans in response to cellular injury and inflammation, and is also isolated from soy beans and egg yolks. It is available on the market in Europe for the treatment of neuropathic pain, and in Australia as a compounded supplement.
There has been much research done with (PEA), especially in neuropathic pain, inflammation and nerve compression syndromes. There is growing evidence to show that neuro inflammation has a role to play in chronic pain, mediated through mast cell activation and infiltration of immune cells and inflammatory mediators. PEA has been shown to stabilise the mast cells, thus reducing inflammation. It also reduces expression of pro inflammatory proteins, has neuroprotective effects and binds to cannabinoid like receptors.
Many clinical trials have shown it to be effective in the treatment of pain, such as neuropathic pain, sciatica, carpal tunnel syndrome, gut pain and arthritis. One trial in arthritis showed a greater response in terms of pain relief and mobility with PEA compared to the non-steroidal anti-inflammatory drug ibuprofen. No significant adverse events have been reported in clinical trials, and it is safe to be combined with prescription medicines for pain relief.
If you would like to read more about palmitolyethanolamide, see this article from the Journal of Pain Research from 2012. It is a case series with 7 clinical examples of its use in different patients with pain caused by various conditions including cancer, failed back surgery and diabetic neuropathy. This review article, published in 2012 gives a good summary of the role of the glial cells in pain, how PEA works and the clinical data.
The recommended dose range is 300mg to 600mg twice daily.
Magnesium binds to the NMDA receptor and stabilises it, reducing nerve membrane depolarisation and secondary messenger release. This explains its benefit in neuropathic and chronic pain.
It reverses the depleted cellular magnesium levels in patients with fibromyalgia. It is critical for energy production and regulating vasodilation, so helps to reduce pain score in patients with fibromyalgia.
Tension headaches are linked to magnesium deficiency, muscular tightness and tenderness in 70% of patients, and can be treated effectively with magnesium supplementation. Magnesium is well known as a preventative therapy in the management of migraines.
Magnesium glycinate is available as a compounded product in Australia. By attaching the magnesium molecule to a glycine molecule, it is absorbed via active transport mechanisms in the gut rather than through mineral absorption channels. This means better systemic absorption and therefore less gastrointestinal side effects. There is also the added therapeutic benefit of the glycine, which has a calming effect due to its action as an inhibitory neurotransmitter.
Capsaicin and menthol
Capsaicin activates pain receptors, increasing the release of substance P. The depletion of substance P over time results in pain desensitisation and has been shown to be effective in the treatment of neuropathic pain.
The initial burning sensation of capsaicin may be alleviated by pre-treatment with menthol, from peppermint oil. Extracted pure menthol has been shown to block pain receptors and to have a mild opioid effect, this reducing the discomfort associated with the use of capsaicin cream.
Essential oil blends
Essential oil blend of black pepper, marjoram, peppermint, lavender has been used in a placebo controlled clinical trial and shown to significantly reduce neck pain. (Ou, M. et al, J. Altern Complement Med, 2014). We can compound this for your patients in a plant oil based cream or liniment.
Please contact me if you would like any more information or if you have any questions.