Lynne Noble
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A potted history of analgesics and the r ...

A potted history of analgesics and the role of nutritional medicine in overcoming the prob

Nov 23, 2022

A potted history of analgesics and the role of nutritional medicine in overcoming the problem of synthetic drugs.

Pain can be divided into   four types under the headings, acute, chronic, neuropathic and nociceptive pain. Acute pain is short lived and alerts us to the fact that something is wrong due to, for example, injury or infection. Nociceptive pain is characterised by a sharp, throbbing or aching sensation and is generally the result of an external injury. Chronic and neuropathic pain are what we generally experience in our day to day lives, especially as we age. Chronic pain is referred to as such when the acute pain experienced initially continues for longer than six weeks.   The   history of pain and its response is an interesting one. Ibuprofen and paracetamol are relatively new kids on the block so how was pain relief effected without the sledgehammer of morphine and its derivatives?

In 1887, phenacetin was introduced to the UK.  Phenacetin had pain-relieving and antipyretic (fever reducing) effects. It was added to many medications at the time and used extensively.  However, phenacetin was found to be carcinogenic as well as implicated in kidney damage. Phenacetin was initially withdrawn from use in Canada in 1978, the UK in 1980 and finally the US in 1983.  

Aspirin was introduced to the UK in 1899.  It does not naturally occur in nature but scientists at Bayer created acetylsalicylic acid with the brand name of Aspirin. With the advent of analgesics such as paracetamol - which was introduced in 1956 – and ibuprofen – which was introduced in 1961, Aspirin   lost its popularity other than its benefits as an anti-clotting agent.  

One of the problems with Aspirin was that its reputation as a preventative medicine for heart attacks was in doubt.  A double blind study overseen by Elwood found that heart attack survivors were likely to go on to have a further heart attack. A similar study   conducted by the American epidemiologist   Hershel Jick found that although aspirin did appear to prevent heart attacks, the attacks that did occur were more deadly.  Fewer aspirin takers reached hospital but this may be because the patients had died before they could be taken to hospital.

The findings informed the American Heart Association and the American College of Cardiology to change the guidelines for who should be taking aspirin.  Thus, individuals over the age of 70 years were recommended not to take aspirin routinely if they had an increased risk of bleeding and who did not have existing heart disease. 

Paracetamol, introduced   in   1956,  is touted as a safe drug.    However, the side effects which are not generally common knowledge include   thrombocytopenia, a condition where there is an abnormally low number of platelet cell. In addition, a condition known as leukopenia (low number of white blood cells), kidney and liver damage can   occur if too much is taken.  It would be too much to expect – given the genetic differences of individuals – that   the recommended maximum dose   may be too high for some people.  Overdose can be fatal in some cases.    Further, long term use for chronic pain is often recommended. However, damage may be subclinical and potentially irreversible before it is revealed. Nevertheless, paracetamol is available over the counter - in paediatric form - under the brand name Calpol.

Ibuprofen was introduced in 1961.  Its anti-inflammatory properties are not as pronounced as other NSAID’s like Indomethacin, but it does have effective analgesic and temperature lowering properties.

 Ibuprofen was intended to be a safer alternative to aspirin although the gastric side effects of vomiting, nausea and gastric bleeding, found in aspirin, are also characteristic of ibuprofen.  Black faeces, indicating blood in the poo  -or indeed vomiting  ‘coffee grounds’ - is evidence of the more severe effects of ibuprofen.  Swollen ankles after taking Ibuprofen indicate kidney damage.

The NHS website urges individuals to call 999 or go to A&E if:

·         You have severe chest pain or stomach pain – these can be signs of a hole in your stomach or gut

·         You have difficulty breathing, or asthma symptoms that become worse

·         You get a severe headache, a high temperature or stiff neck and a dislike of bright lights, I these can be signs or inflammation of the protective membranes that surround the brain and spinal cord

·         You have blurred vision or you see or hear things that are not real (hallucinations)

              (NHS website)

If, as it appears, our ‘safe’ pain relieving meds are not as safe as we would like to believe then   we have to ask the question ‘Are there natural alternatives which would deliver equally effective benefits but without the side effects?’

 I believe so.  Further, they do not require a GP prescription and, as they come without the side effects of synthetic drugs, they are safer.  We shall look at some of these naturally occurring analgesics below.

 Thiamine as an analgesic

Fibromyalgia syndrome (FMS)is a good   example of how thiamine can respond to intractable pain. Studies show that immune system cells known as microglia become activated in this   condition. Active microglia fuel chronic neuroinflammation.  Research showed that Individuals who took between 600mg to 1800mg of thiamine had a   50%-80% reduction in pain and fatigue.  However, other   participants   didn’t benefit until they reached   a daily intake of 1500mg-1800mg of thiamine.

The reason for this discrepancy has been ascribed to    factors   such as intracellular defects or enzyme abnormalities which necessitate the need for much higher doses In order to overcome these barriers.

In a study on mice, doses which were calculated on 250mg per kilogram of body weight found a remarkable analgesic effect in a dose dependent form.

The trio of BI, B6 and B12 vitamins has been found to inhibit pain sensing neurons in the spinal dorsal horn and thalamus where sensory   information from the site of injury or infection must pass.  It is the brain which interprets sensory information.   Thus pain is actually felt in the brain, not at the site of the injury as most people   tend to believe.

Other studies have shown that thiamine has significant analgesic effects on both inflammatory and neuropathic pain including diabetic neuropathy.

Further studies have shown that when an individual has thermal injuries such as scalds or burns, 2-4g of thiamine eases the pain significantly. Similar antinoiceptive effects have been found in PMS, neuritis. painful vertebral syndrome, amputation stumps and painful varicose ulcers.

The benefits of thiamine also extend to labour. Studies conducted in the Soviet Union and the West have found that 40-300g of thiamine produced some relief in 50% of 622 labours with 90% having shorter labours. 

Thiamine can be found in organ meats, wholemeal cereals, yeast extract, malted milk, peas and pork in good amounts. Thiamine is depleted rapidly with high carbohydrate diets, alcohol, tea, coffee and raw fish including shell fish.

 

The role of tryptophan in inflammation and analgesia

Tryptophan is an essential amino acid which is required for the synthesis of nicotinic acid. It is also the precursor of the neurotransmitter, serotonin which gives you the ‘feel good factor’ and provides restful deep sleep. It acts as a mood stabiliser calming   aggression so the more tryptophan   taken in     diet, the more relaxed an individual will feel. 

The uptake of tryptophan via  the blood brain barrier can be problematical. Firstly, tryptophan is a rather large molecule and cannot compete with the smaller amino acids crossing the blood brain barrier so tryptophan is often better taken –as a supplement - without any other competing proteins.

In order to assist tryptophan across the blood brain barrier, it may be taken with a little carbohydrate  - half a biscuit would be suitable - which acts as a carrier.  In addition, tryptophan needs vitamin C and vitamin B6 to accomplish the transport across the blood brain barrier.

Tryptophan metabolism controls excessive inflammation.  When inflammation occurs it activates tryptophan metabolism which triggers body wide intra and extra cellular changes that calm inflammation   and   effect an immunomodulatory effect.  Therefore, tryptophan therapy is useful for those with auto immune disease.

As tryptophan is adaptive in the way that it responds to inflammation, it could l be considered an anti-ageing amino acid as well as an effective analgesic and soporific

For pain relief try 500mg 3 X daily.

Good   sources of tryptophan are poultry - especially turkey breast- lentils, beans and tuna but there are many more sources   of this   valuable  amino acid.    

 

Vitamin C

Vitamin C has a powerful anti-inflammatory action and, as such, is able to alleviate pain with an inflammatory component. Vitamin C deficiency is high in specific groups of individuals.  These include those who have undergone surgery, have a chronic condition or have traumatic injury.

The symptoms of chronic regional pain syndrome decreases with high dose vitamin C.

Vitamin C can diminish acute herpetic and post herpetic neuralgia.  Studies have found that cancer related pain decreases significantly when high dose vitamin C is taken.

It is difficult to state a daily amount of vitamin C since there are so many factors involved. In this calculation.   Smoking, for example, uses up 30mg for each cigarette; stress and infection   contribute to vitamin C deficiency. Bowel tolerance will vary between individuals but should be used as a guide.

However, research   provides guidance of 3g daily of vitamin C for pain relief.  This may seem like an excessive amount when compared against the recommended daily allowance.   However,   the recommended dietary allowance for vitamin C,   was set at a specific amount to prevent scurvy. It was not intended to address pain which requires much higher therapeutic amounts. 

Vitamin C is found in   fresh fruit and vegetables.  As a water soluble vitamin, it is destroyed fairly rapidly by heat and also leaches into cooking water. Large   doses are better supplemented when needed for therapeutic dosing. During the 1940’s to the 1950’s rose hip syrup  - Delrosa - was given to school children daily, in order to avoid the problems caused by hypovitaminosis. 

 

 

 

Magnesium as an analgesic

 

The benefits of magnesium in relieving pain and inflammation are well- known.  Studies have found that at the cellular level, magnesium reduces inflammation. It was found that when an inflammatory condition   occurs then a magnesium deficiency is created.  Increasing magnesium intake decreases inflammation.

 

Magnesium is actively required by 700 enzyme systems in the body. There are a number of ways in which magnesium helps to reduce inflammation.  Magnesium has been found to be a natural calcium channel blocker.  This is important as excessive calcium is one of the most pro-inflammatory substances in the body. 

 

The ratio of calcium to magnesium is held to be in the ratio of 800:400mg but more recent studies have argued that the amount of magnesium should equal that of calcium intake.

 

Dr Joseph Mercola DO has been quoted as saying

 

‘We are all going to die at some point, but if you’re deficient in magnesium you may wind up dying sooner rather than later.’

 

Research has shown that magnesium can be effective in both muscle and nerve pain In addition,     magnesium has  muscle relaxing properties. It is these characteristics which are harnessed in the Epsom salt type bath crystals. Moreover, a study on rats which appeared in the Journal of Physiology confirmed that magnesium decreases nerve pain.

 

N-methyl-D-aspartate (NMDA) is a pain carrying neurotransmitter. When this neurotransmitter is stimulated it is a major mechanism of pain.   However, drugs such as Amantadine and Ketamine  - which  help decrease and balance this neurotransmitter - have significant side effects.  For example, some of the side effects of Amantadine are listed as being

·          Depression, anxiety and irritability

·         Hallucinations and confusion

·         Anorexia

·         Dry mouth

·         Constipation

·         Somnolence

·         agitation

 

among  others.

 

Magnesium is superior in that it  has been found to calm down NMDA without the side effects that most   prescription drugs have.

 

The authors of the above study have argued that magnesium deficiency can be a major amplifier of pain and have highlighted that most people are magnesium deficient.

 

The only contraindication to supplementing with magnesium is for those who have kidney disease. 

 

Magnesium supplementation for migraine

 

Magnesium oxide is often used to prevent migraine at a dose of 500mg daily. Evidence for magnesium’s effectiveness is in patients who have had aura with their migraines. It is thought that magnesium may prevent waves of brain signalling.  These waves –cortical spreading depression – initiate the visual and sensory changes associated with aura.

 

Magnesium also decreases the release of substance P and glutamate – both pain carrying transmitters -  in addition to   preventing  vasoconstriction of   blood vessels in the brain  caused by the neurotransmitter serotonin.

 

Substance P is released from the ends of specific sensory nerves and is found in the central and peripheral nervous system.  It is associated with inflammatory processes and pain.

 

Neuronal substance P is stored in vesicles and released when it comes into contact with

·         leukotrienes

·         prostaglandins

·         histamine

Ginger blocks both the production of prostaglandins and leukotrienes. In cell based studies capsaicin (found in peppers) and curcumin both blocked the production of leukotrienes.

 

The inflammatory processes   associated with Substance P  related  pain can be addressed by common foods as we will see.

 

Glutamate is neurotoxic and has to be remain within neurons. It’s concentration in cells is much larger than the small amount released when nerve transmission is crucial.  If too much is released, pumps in the membrane suck the excess back.

 

When damaged cells release   glutamate the neuron isn’t killed instantly.  The cell becomes excited.  As a result its pores are opened too much.  This allows excessive quantities of salt and calcium into the cell.

 

Sodium causes cell swelling which presses on adjacent blood vessels. This can ultimately lead to cell death and the subsequent   release of further glutamate from damaged cells.

 

Calcium is more    lethal   than sodium. Calcium rushes into open pores in the cell wall. As it does so it destroys the neuron’s vital structures resulting in cell death.  Dead cells will continue to spew out glutamate destroying areas of brain that it comes into contact with. This onslaught will continue   until the glutamate pumps are able to overcome the extra cellular glutamate and return it to the   cell.

 

Alpha-Lipoic Acid – found in spinach, broccoli and liver helps glutamate transport proteins which aid the  removal excess extracellular glutamate.  [1]

 

The flavonoid agipenin which is found in parsley, celery, thyme, cloves, lemon balm and chamomile,   inhibits glutamate. In culture it was found to be neuroprotective against glutamate- induced neurotoxicity in cerebellar and corticol neurons[2]. An antagonistic effect of apigenin on NMDA, the pain carrier, was found.

 

GABA is a neurotransmitter which has calming and pain relieving properties.  Rosmarinic acid, which is found in oregano, lemon balm, sage, marjoram and rosemary, increases GABA levels by inhibiting an enzyme which converts GABA to L-glutamate.  Thiamine is required for the synthesis of GABA.

 

The olive leaf contains oleuropein which prevents against damage from bacteria and insects. It helps to relieve intestinal spasms so is useful for pain from irritable bowel syndrome.

 

 Studies show that oleuropein dissolves the outer lining of micro-organisms thus destroying them. It is also an antioxidant and therefore has anti-inflammatory properties.  It has been shown to inhibit cancerous cells in the breast, bladder and brain.

 

A study published in the Pakistan Journal of Biological Sciences found that a salve made of ginger, cinnamon and sesame oil was just as effective as the over counter medication creams containing salicylate which is a topical analgesic.  

 

These natural products can be found in the pantries of most people’s houses. They are effective analgesics and anti-inflammatory agents without the side effects of synthetic drugs.   The good news is that these are only a minute part of the nutritional substances that can be found in the kitchen if only people understood how to use their properties.

 

In future articles I will be adding more amazing   nutritional medicines to the collection of natural products which aid healing and wholeness.

 

Lynne Noble copyright 23/11/22

 

 

 

 

 

 


[1]  http://www.jpands.org/vol9no2/blaylock.pdf

[2] https://www.ncbi.nlm.nih.gov/pubmed/15464088

 

 

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