Painkiller addiction, a world-wide problem: what are safer natural alternatives to opioids?

Painkiller addiction, a world-wide problem: what are safer natural alternatives to opioids?

One of the sad results of the past two years during which hospitals were very busy treating COVID-patients was that others had to wait much longer for much-needed operations. A not so obvious side-effect has been that people who were in pain due to the much longer delays, were prescribed strong pain-killers.
At this very moment, a shocking amount of half a million Dutch citizens are being prescribed oxycodone, which is the same type of opioids that has caused a vast amount of people all over the world and more specifically in the USA to become addicted.

The opioid epidemic is raging out of control in the USA and other Western countries. Meanwhile the discussion of natural alternatives is almost non-existent. As if nature doesn't provide any pain relief.

The reality is that many pharmaceutical pain drugs have been developed as synthetic analogues of natural herbs that reduce pain. Aspirin was synthesized as an analogue of an active ingredient t in willow bark and meadowsweet herb .
Since then, pharmaceutical medical researchers have synthesized analogues for a larger amount of natural substances to provide patentable pain relief. One of the most famous of these is oxycodone, but other familiar opioid pain relievers are hydrocodone, tramadol, morphine, codeine, heroin and fentanyl.

The dark history of oxycodone

Oxycodone is an opiate synthesized from the opioid paramorphine. Oxycontin is a form of oxycodone, oxycodone hydrochloride.

Oxycodone was synthesized in Germany in 1916 in an attempt to improve upon extracted opioids such as morphine and heroin.
Both morphine and heroin are extracted from the opium poppy plant.
Morphine was isolated from opium in 1805 by a German pharmacist. In 1898, Bayer introduced a new pharmaceutical under the trademarked brand name of heroin. Heroin is up to 3 times more potent than morphine.

Oxycodone was first sold in 1939 by Merck, while oxycodone was most famously used by Hitler who received frequent injections.
In 1995, Purdue Pharma received approval for OxyContin. It quickly became an extremely popular drug to help patients with severe pain.
It also quickly became a recreational drug as it also allowed the user to get high.
By 2016, Oxycontin and other synthetic opioids such as Fentanyl were responsible for over 20 000 deaths in the US according to the CDC.

The dark history of fentanyl

Fentanyl is both incredibly powerful and addictive. It is also deadly dangerous. Estimates are that fentanyl can be more than a thousand times stronger than morphine and heroin.

Fentanyl is considered an essential pain medication. Yet, it comes with severe side-effects such as breathing problems, low blood pressure and above all, addiction.
The addictiveness of fentanyl has become its greatest problem. It is so addictive that tens of thousands of people throughout the USA are dying from addiction to fentanyl or heroin that is laced with fentanyl.
Because fentanyl is so strong, heroin suppliers are now lacing heroin with fentanyl, which is producing a wild-fire effect throughout the country as heroin addicts are increasingly dying from heroin laced with fentanyl purchased on the street.

Signs of an opioid overdose

It’s important to be able to recognize the signs of an overdose, and to know when it’s time to call for help.
Common signs that a person is suffering from a drug or opioid overdose:
  • pale face
  • cold or clammy skin
  • limp body
  • blue or purple fingernails or lips
  • vomiting or making gurgling noises
  • unable to speak
  • shallow breathing or heartbeat that slows or stops

In case you are interested, you may want to watch one of several documentaries on fentalyl abuse. Or read a book. One that the Dutch professor on clinical pharmacology, recommended is called 'The Empire of Pain' which documents the vile history of how Purdue Pharma made people addicted to Oxycontin. It should also be available as an audiobook. The first episode (or several) is available free of charge at YouTube

Is opium a natural substance?

Indeed, opium is a natural substance as long as it is produced from poppy flowers, more specifically Papaver somniferum. Even poppy seeds, commonly eaten in bread and pastry also contains trace amounts of opiates. But poppy seeds won't get you high or addicted.
It is only when the sap from seed pods is concentrated and the opiates such as morphine are extracted, that people who use it, can become addicted.

Long before heroin and morphine were distributed by drug companies, natural opium was utilized by herbalists as a therapeutic medication. This came in the form of a tincture called laudanum, utilized as an analgesic but also as a treatment for colic, lung infections, anxiety and insomnia. Laudanum tincture only contained about 1% morphine.

As time went on, the distribution of pharmaceutical grade opium extracts became widespread and the world was inundated with these addictive forms. Then even more addictive highly concentrated synthetic versions were introduced.
Yet, those early natural forms are greatly overshadowed by today's synthetic opiates such as oxycodone and fentanyl which are about a hundred thousand times more addictive than laudanum.

What are natural alternatives to opioids?

Many addictions to opioids occur as a result of an initial prescription of oxycontin or fentanyl. Often for pain that is transitory in nature. This means that many addictions could be circumvented if natural alternatives were initially used to reduce pain. Or at least natural alternatives were used along with non-opioid pain-killers such as NSAIDs.

It is important to understand the cause of the pain and use therapies that help the body heal the cause of pain. This can be done with herbs, acupuncture, massage as well as meditation and yoga exercise.

For those who have experienced a dependence to painkillers, rebuilding life after opioid addiction can be difficult considering everything to overcome such as trauma, social situations and emotions.

Learning to incorporate some of the following activities will provide long-lasting pain relief while enhancing overall quality of life.

Endorphins are the body’s naturally occurring opioids that are released from the brain and central nervous system under certain conditions. The following activities help the pituitary gland secrete natural endorphins and relax the body.

a. exercise to reduce pain: running is one of the best natural methods for promoting the release of endorphins. Joggers call this feeling a “runners high” caused by the body’s natural painkilling endorphins produced while running.
But running isn’t the only exercise that works. Walking or any type of exercise for as little as 20 minutes a day will release endorphins that naturally relieve pain in the body.

b. Meditation has been scientifically proven to have powerful healing effects on the mind and body.
c. Yoga is complementary to meditation. Yoga triggers the body’s endorphin system as well as strengthening the body’s response to stress and discomfort.
c. Acupuncture is an ancient Chinese pain therapy which is gaining popularity as it can even relieve severe pain. The benefits of acupuncture are achieved by clearing blockages in the body and releasing endorphins to defeat pain.
d. Massage also can reduce pain, though it depends on the type and region of pain. But even massage that focuses on the body as a whole can reduce pain. The best results were seen with lower back pain.

e. Mindfulness helps the mind relax and return or remain the present moment. By relaxing the mind and staying focused on the current task at hand, the entire body enters a state of calm thereby reducing tension and minimizing any associated pain.
f. Epsom magnesium salt bath can help relax the body and allows it to absorb magnesium. Both Epsom salts and magnesium supplements relax the body and can even be used during surgery to reduce pain and relax muscles.
g. Neurofeedback or self-regulation of brain waves helps improve the mind’s focus. Neurofeedback rewards the brain for desirable behaviour, and over time, helps a person remain in an optimal state to overcome stress, depression, headaches, and other sources that stimulate pain in the body.

Herbs that help manage pain

Many herbs stimulate the body's own healing mechanism, allowing the body to heal more quickly.
Most herbal medicine used as painkillers also simultaneously reduce inflammation, because this mostly goes together.
Herbal medicines used for pain can inhibit pain enzymes such as cyclooxygenase (COX) and lipoxygenase (LOX).
Other herbs stimulate the production of gamma-aminobutyric acid (GABA) neurotransmitters within the nerves or simply bind with GABA-receptors. These all have the effect of reducing pain.

A third way in which herbs combat pain is by reducing 'substance P', a neuropeptide, which is part of the inflammatory pain cycle.

Here follows a list of the most popular natural pain-reducing herbs

Willow bark (Salix alba)
Willow bark contains natural salicins. As mentioned above, the isolation of salicins from meadowsweet and willow bark lead to the development of aspirin.
Willlow bark has been used for thousands of years to help with different types of pain. Research has shown that natural salicin inhibits both COX-1 and COX-2 enzymes. Using willow bark instead of aspirin avoids some of the side-effects seen with aspirin such as damaging the gastrointestinal tract and has a broader mechanism of action.

Meadowsweet (Spiraea ulmaria)
Meadowsweet contains many of the same salicins as willow bark. It was meadowsweet that provided the basis for the 1830 analogue that led to the famous aspirin by Bayer.

Ginger (Zingiber officinalis)
Ginger contains many pain-reducing constituents. Ginger even exceeds some NSAIDs for reducing arthritic pain and menstruation pain.

Essential oils
Essential oils of lavender, clary sage, and rose as well as thyme can help relieve pain.
Devil's claw (Harpagophytum procumbens)
The root of devil's claw can relieve pain associated with headache, backache, menstruation and joint pain. It can also reduce inflammation.

Myrrh or guggul (Commiphora mukul)
This ancient herb commonly known as myrrh, but is called guggul in ayurvedic medicine has been used for up to 5000 years for a variety of inflammatory and pain conditions, above all to relieve joint pain.

Nettles (Urtica urens)
Nettles have been used to help relieve inflammation and joint pain as well as arthritic pain and rheumatism.

Frankincense (Boswellia serrata)
Frankincense or boswellia is an ancient remedy used for a variety of aches and pains, above all for nerve and joint pain.

Turmeric (Curcuma longa)
Turmeric has been used medicinally for thousands of years, to reduce inflammation and pain. It reduces both LOX and COX-type enzymes as well as infection and speeds up wound healing.
Turmeric reduces arthritis and menstruation pain.

Feverfew (Tanacetum parthenium)
Herbalists have used feverfew for headaches and other types of pain for centuries. Feverfew inhibits COX-2 enzymes thanks to the active ingredients parthenolide and melatonin.

Skullcap (Scutellaria baicalensis)
Skullcap significantly reduces inflammation and pain related to inflammatory conditions by inhibiting the COX2-enyme.

Hops (Humulus lupulus)
Hops helps relieve nerve pain and anxiety related conditions. The main active ingredient humulone inhibits the COX2-enzyme.

Ashwagandha (Withania somnifera)
Ashwagandha can reduce inflammation and anxiety related to nerve pain. The mechanism in which ashwagandha works is by binding with the GABA receptors.

California Poppy (Eschscholzia californica)
Despite the name and similarity, the California poppy is unrelated to opium poppies. It does however have an analgesic and relaxing effect. It works by binding with the benzodiazepine and GABA receptors.

Kava (Piper methysticum)
Kava has been used for thousands of years by inhabitants of the Pacific islands for headaches and muscle pain. It has a sedative effect and provides muscle relaxation by binding to GABA receptors.

Arnica cream
An excellent herbal rub to use after intense sports, an acute injury, or even post-surgery, arnica is a well-known natural pain killer among athletes and yogis. It is derived from the arnica flower, and has anti-inflammatory properties, although the true nature of its healing action is still unknown.

CBD cream
Topical CBD cream may help with a variety of pain sensations, including arthritis-related pain and swelling, nerve pain and jaw pain.

Foods that can help to reduce pain

Capsaicin (Capsicin)
Capsaicin as found in hot chilli peppers, temporarily desensitizes nerve receptors. It can also be applied as a cream on the nose to decrease migraine and headaches

Gamma Linoleic acid (GLA)
GLA can be found in numerous seed oils. People who consume these essential fatty acids are able to reduce nerve pain associated with diabetes.

Due to the presence of compounds called anthocyanins—the same phytonutrients that give cherries their rich ruby red hue, cherries can diminish pain by blocking inflammation and inhibiting pain enzymes, just like aspirin, and other NSAIDs. Cherries are said to have the highest anti-inflammatory content of any food, making them great for remedying issues such as arthritis.

Peppermint (Mentha piperita)
Peppermint is most often used as a natural remedy for toothaches, discomfort from bloating and gas, joint conditions, skin irritations, headaches and muscle pain.

This natural pain-reducer comes from the enzymes present in pineapple stems. Bromelain reduces levels of prostaglandins, which are hormones that induce inflammation. Bromelain may benefit people with arthritis and conditions marked by musculoskeletal tension in addition to those suffering trauma-related inflammation. The enzyme also promotes healing in muscles and connective tissues.

Having a bout of ulceritis? Ulcers usually result from a pathogen called H. pylori which attacks the lining of the stomach and small intestines, but cranberry juice can kill it – reducing pain. Instead of turning to antibiotics, destroy the bacteria causing your ulcers and urinary tract infections with cranberries.

Finally there's another substance which for some reason is not well known at all, PEA on which we want to focus in this blog article.

The role of PEA in the endocannabinoid system

Let's first explain what PEA and endocannabinoid system means.
PEA (N-palmitoylethanolamide) is an endogenous fatty acid, synthesized and metabolized by cells that binds to cell receptors. PEA influences a multitude of physiological functions and has potent anti-inflammatory and pain-relieving properties.

Endocannabinoid system is a lipid communication network that has critical physiological functions and serves a vital purpose for our health and well-being through signaling processes, homeostasis and hormone regulation.

Lipids and the endocannabinoid system

In 1929, scientists George Oswald Burr and his wife, Mildred Burr, discovered that omega 6 fatty acids were essential for health. This kicked off science’s interest into lipids, and by the 1960s a new age of lipid research had begun.

Edward Dennis of University of California at San Diego wrote:
Lipids are in many ways the most important of the biomolecules because they are the ultimate controllers and regulators of our bodily processes; they are key to signaling events in cells. Further, imbalances in lipids are implicated in many illnesses, such as heart disease, stroke, arthritis, diabetes and Alzheimer disease. If we are going to solve these diseases, we must know what the lipids are and what they do.”

The endocannabinoid system (ECS) is a lipid communication network with important physiological functions in all animal life. The complex biochemical array of pathways involved in the synthesis, release, transport, and degradation of endocannabinoids by the body is also known as the endocannabinoidome. This lipid signaling network is a key modulator of physiological functions in many of the other networks and signaling systems including; the nervous system, the endocrine network, the immune system, the gastrointestinal tract, and the reproductive system, as well as others.

Endocannabinoids, the products of the ECS, are directly released from membranes, which distinguishes them from other transmitter molecules, such as dopamine or hormones. Moreover, unlike the neurotransmitters or hormones, which are synthesized in one place but act globally in the body, the endocannabinoids are synthesized locally and act locally.

PEA – the rising star of the ECS

One endocannabinoid in particular has been studied in considerable detail, N-palmitoylethanolamide or PEA. The origins of PEA started in 1939 when clinician and researcher Coburn was looking into how to prevent the incidence of rheumatic fever in poor children living in New York.
He stumbled upon egg yolk as a key ingredient that prevented and/or reduced rheumatic fever. In 1957 scientists at Merck Sharp and Dome identified PEA as the molecule that provided this protection against streptococcal infection and rheumatic fever.

However, it wasn’t until 1993 that the mechanism of action of PEA was determined through the work of Rita Levi-Montalcini an Italian scientist who back in 1954 had discovered the nerve growth factor (NGF).

Levi-Montalcini’s discovery was that nerve growth factor activated specific immune cells called mast cells that further caused inflammation and allergic reactions. Almost forty years later, she discovered how a naturally produced fatty acid amide called PEA stopped the activation of mast cells, thereby preventing inflammation and allergies.

Furthermore, Levi-Montalcini discovered that PEA was produced locally by cells under threat from noxious and injurious external triggers, like UV-A, various toxins, allergens, infectious agents as well as other inflammatory agents. The local production of PEA thereby reduced their threat. PEA was not only produced locally but also acted locally. It seemed like PEA was called into action whenever there was demand, when the body needed protection not only against outside triggers but also when the body was under threat from within, for example against ageing or whenever the immune system was overactive as in various autoimmune disorders, which occurs when the body stops recognizing friend from foe, and starts acting against itself. Mast cells seem to be key components of the inflammatory response.

Levi-Montalcini succinctly pointed out the interaction between PEA and the mast cell:
…Unregulated mast-cell activation constitutes a considerable risk to the health of the organism, and it is not unreasonable to expect that nature should have devised a means for the host to defend itself against such damage. It has recently been proposed that saturated N-acylethanolamine like palmitoylethanolamide (PEA), which accumulate in tissues following injury and which down modulate mast cell activation, exert a local, and anti-injury function via mast cells. Palmitoylethanolamide is orally active in reducing tissue inflammation and mast cells.”

Once the mechanism of action of PEA was identified, there was a flurry of research on PEA, and new and interesting health benefits were soon discovered. As early as 1980, it was learned that PEA had a tendency to accumulate in the damaged heart muscle due to ischemia or deprivation of oxygen, and this might be of physiological importance because of its anti-inflammatory properties. It was suggested that these fatty molecules played a protective role, and that their presence, “may signify a response of myocardial tissue to injury directed at minimizing damage and promoting survival”.

Recent studies have shown that PEA protects various tissues, including the colon, kidney and particularly the nervous tissue. It shows potential benefits in spinal cord injury as well as other conditions like shock, stroke, MS and Alzheimer’s.

Currently there are number of animal and human studies on the application of PEA in the following conditions:
  • endometriosis
  • benign prostatic hyperplasia (BPH)
  • burning mouth syndrome
  • inflammatory bowel disease and syndrome (IBD/IBS)
  • depression
  • autism
  • transient brain injury
  • arthritis
  • pain originating from various types
  • coronary heart disease
  • chronic kidney disease
  • atopic dermatitis and eczema
  • vulvodynia
  • cannabis dependence
  • migraine
  • infectious diseases
In conclusion, PEA is an endogenously, and locally produced anti-injury molecule, the sole function of which is to offer immediate protection through down modulating disease processes and acting against noxious stimuli in various systems of the body. The medical potential of this fascinating and undervalued molecule that comes to the body’s rescue when the need arises is worthy of wider attention in the context of ongoing research into the endocannabinoid system.

The intelligent approach to pain

Not all pain is the same. Different types of pain have different causes. We can also approach pain differently in a spiritual and mental way.

Nearly all of the herbs listed above have different active ingredients that influence the body in different ways. Some of the herbs encourage the healing process and at the same time reduce inflammation and pain sensation.
Some herbs have sedative effects and stimulate the neurotransmitters that balance and reduce the effects of pain.
By contrast, most pharmaceuticals only contain one primary active ingredient. Whole herbs can offer a more intelligent approach as most have far fewer side effects.

By using other approaches such as meditation, yoga, and other forms of meditative exercise, the body can relax and learn to tolerate pain more easily.