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How to

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Mayleena Holm

on 16 February 2015

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Effectiveness of Herbal/Botanical Medicine in Pain Relief
Not all herbs of the same species or plant have the same quality or quantity of biochemically active compounds within them.

Many factors such as genetics, growing conditions, harvesting, drying, packaging and storage influence why there can potentially be such dramatic differences in the composition of two individual plants.
Direct Pain Relief
Directly alleviating pain by acting on sensory neurons or the central nervous system.
The pain relieving properties differ depending on the method of use of the herb (orally or topically).
Some herbs may relieve a significant amount of pain relief when taken alone, while others need to be used in conjunction with other herbs or drugs for effective pain relief.
Anti-inflammatory effects
Anti-inflammatories block cox enzymes from making prostaglandins, reducing swelling and redness, in turn reducing the pain that the swelling causes.
Side effects
Due to all the inconsistencies and the lack of research into herbal medicines they can have some adverse effects. Which are more pronounced in pregnant women, breastfeeding women, children and the elderly. Since all herbal medicines are not regulated by the FDA or the MHRA, there may be other components in them other than the main therapeutic ingredient which could cause other side effects.
Willow Bark
Where does it come from?
Indigenous to southern China.
Rhizome of plant Zingiber officinale.

What is it used for?
Rheumatoid arthritis, osteoarthritis, joint and muscle pain, dental pain, menstrual cramps.

How does it work?
Main Active Ingredients: Gingerols (markedly 6 gingerol, C17H26O4), Shogaols, Zingerone, Sesquiterpenes (hydrocarbon typically found in essential oil), Salicylates
Over 400 biochemically active ingredients, of which phenylpropanoids are used by the plant for protection against bacteria, fungi, and harmful microbes.

Mechanisms of action:
- Most are similar to NSAID inhibiting enzymes associated with pro-inflammatory responses and pain
- Inhibition of inducible nitric oxide synthase.
- Inhibition of lipoxygenase.
- Suppression of inflammatory prostaglandin and leukotriene synthesis.
- Also inhibits enzyme necessary for leukotriene biosynthesis, arachidonate 5 lipoxygenase.
- Inhibits cyclooxygenase 2 expression (in inflammatory reactions causes more prostaglandins to be produced).
- Interference in cytokine signaling.
- Similar to capsaicin, gingerol component acts on TRPV 1 vanilloid (heat and pain) receptors in sensory nerve endings.
- Influence Calcium levels borth extracellular and intracellular that regulate the TRPV receptor.
- Antioxidants bind free radicals causing tissue damage.
- Inhibit production of pro-inflammatory cytokine from LPS stimulated peritoneal macrophages.
- Salicylates converted into salicylic acid in the body, inhibits nerve cells from producing pro-inflammatory prostaglandins.

Where does it come from?
Unopened pink flower buds of the evergreen clove tree, can be used in the forms of essential oil, dried flower buds, leaves and stem.

What is it used for?
It is mostly used for relieving pain from toothache. It also has a local anesthetic effect and temporarily numbs and relieves the pain.

How does it work?
Active ingredient: Eugenol has antioxidant, anti-septic, local anesthetic, anti-inflammatory, rubefacient (warming and soothing), carminative and anti-flatulent properties.
Other main constituents: Beta-caryophyllene showed anti-inflammatory activity in several animal models, including carrageenan- and PGE-induced hind paw oedema.

Clove is also a direct pain reliever as eugenol is also believed to depress the sensory receptors involved in pain perception and inhibits the conduction of action potential in sciatic nerves.

Where does it come from?
Bark from several species of willow trees.

What is it used for?
There is much less evidence that Willow Bark is effective for anything other than lower back pain. However, it has been used for other things, such as gout, muscle pain, menstrual pain, and headaches.

How does it work?
Active Ingredients: Salicin, flavinoid, catechol.
Salicin acts like aspirin, but does not damage the GI tract as much as aspirin does.
All these compounds in willow bark contribute to the anti-inflammatory effects of willow bark.
Where does it come from?
Plant of the ginger family. It is the main spice in curry, gives it the recognisable bright yellow colour.
Part of Siddha medicine, originating to more than 1000 years ago.
One of the most studied natural herbs.

What is it used for?
Very large dosages needed. Dosages not typically used in cooking.
It is used in menstrual pain, heartburn, osteoarthritis, jaundice and topically.

How does it work?
Active Ingredient: Curcumin
Effects are caused by hydroxyl and phenol groups in molecules. It can modulate immune system, through inactivation of transcription factor NF-kappaB, which in turn, downregulates the various proinflammatory cytokines (TNF, IL-1, IL-2, IL-6, IL-8, IL-12 and chemokines) and inhibits prostaglandin.
At lower doses, it can enhance antibody responses.
It also has slight antibacterial properties. It has shown an inhibition of growth of P. aeruginosa, which is resistant to most commonly used antibiotics.
Also has shown to exhibit activities similar to tumor necrosis factor blockers.
Different species and strains of the same herb may vary naturally in the amount of each biochemically active compounds within them.
- i.e. The amount of . [6][8] and [10]-gingerols and [6]-shogaol present in ginger purchased from in various grocery stores and health food shops varied from zero to several milligrams of compound per gram.
copyright: geneticsawareness.org
copyright: flickr.com
Growing Conditions:
- The lighting, soil conditions, weather conditions, pesticides and chemicals, presence of parasites, fungi, bacteria, viruses and other pathogens all influence the total health of the individual plant/herb and in turn impact the potency or strength, and amount produced of the biochemically active compounds.
- i.e. Leaf plucking or trimming the herbs/plants while alive has been shown to increase the amount of biochemically active compounds found in various plants, since the plant’s response is that of being under attack, thus producing more molecules which protect it naturally.
copyright: wikipedia.com
- The time at which a plant is harvested impacts the potency of the herbs. Concentrations of biochemically active compounds varies a great deal during the plant's life cycle. Immature plants, or plants that are aged past a certain time frame might not have optimal concentrations of biochemically active compounds.
copyright: flickr.com
- The process of drying herbs may alter the amount of biochemically active compounds. Storage may also alter the quality of the herb. Each time the herb is smelt, it loses some aromatic oil containing biochemically active molecules to the air, surroundings, and smell receptors within the person’s nose. Light, exposure to oxygen, and heat induce chemical changes in the herb causing them to lose potency (biochemically active compounds) and go “stale” in flavor.

- Proper storage of dried/bulk herbs in a airtight dark glass container extends shelf life and prevents oxidation. Adding the herbs to an alcohol tincture or glycerin extract helps extend storage life though may negatively interact with some of the biochemically active compounds. Antioxidants may be added to dried, powdered, bulk herbs and herbal capsules to help prevent chemical changes and preserve the herbs for longer.
copyright: wikipedia.com

Standardised herbs
- Processing may interfere with how much of each molecular component is left, but should have a standard amount of specific components labeled on the herb product. Potency of the molecular compounds often decreases the longer they are stored on the shelf.
What is herbal medicine?
"Herbal remedies are medicines made up of
plants, trees or fungi
." (NHS, 2014)
Where does it come from?
A woody, perennial herb with needle like leaves. Usually used in terms of essential oil or vapor bath

What is it used for?
Widely used to treat muscle pain, arthritis and improve circulation. It can also help relieve pain from sprains and joint aches due to its anti-inflammatory properties.

How does it work?
It stimulated blood circulation, which can relieve pain and also aids in coagulation of wounds for faster healing.
Rosmarinic acid is responsible for the anti-inflammatory property of rosemary. It works by inhibiting lipoxygenase and cyclooxygenases and the expression of inflammatory cytokines.
20 healthy male individuals were involved in an experiment to test the use of curcumin in relief of DOMS (delayed onset muscle soreness). The study was not in a large scale, but significant results were found.
Half the subjects were given 200mg of curcumin twice a day. The other half were given a placebo.
The supplements were given 48 hours before they were made to run downhill, and continued to be given 24 hours after running.
Using magnetic resonance imaging (MRI), laboratory analysis and histological analysis, the muscle damage was measured.

The results:
The subjects that were given curcumin reported less pain in the anterior thighs. The MRI also showed less muscle damage for this group, and less inflammation, even though the histological markers showed no differences.

It was concluded that curcumin had an effect for reducing pain and preventing delayed onset muscle soreness.
Prevention of DOMS
Post-operative Pain in Mice
Incisions were made on the hindpaw of mice to test the effect of curcumin in relieving post-operative pain.
The sensitivity to touch and heat, as well as the temperature and effects towards oedema were measured.
The gait of the mice were compared using multiparameter digital gait analysis. Pain after incision was assessed with conditioned place preference (CCP).
Some of the mice were given 50mg/kg of curcumin.

The results:
Curcumin reduced sensitivity to both touch and heat, reduced inflammation and oedema. Mice treated with curcumin had no affirmation of ongoing pain, where as mice without curcumin treatment had evidence of pain 48 hours after the incision. The mice treated with curcumin also had a more normal gait than the other group of mice.

Curcumin is a possible candidate for the prevention of pain after surgery.
What is pain?
"Pain is an unpleasant sensory and emotional experience associated with actual or potential tissue damage, or described in terms of such damage" (Journal of Hospice and Palliative Nursing. 2003)
Treatment of Lower Back Pain
210 patients reporting lower back pain with a score of more than 5 (out of 10) were randomly given 120mg of willow bark extract (a low dosage), 240mg of salicin (a high dosage), or a placebo. The trial lasted 4 weeks, and 191 subjects completed the study.
The number of people pain free for at least 5 days in the final week were counted.

The results:
39% of high dosage patients, 21% of low dosage patients, and 6% of the placebo group were pain free at the end of the trial.
Reduction in pain was obvious in the high dosage patients even after only a week of the trial.

Willow bark could potentially be an effective treatment for lower back pain.
50 mice were injected with 0.05mL of fresh lambda carrageenan to induce inflammation of their hind paws. Saline (control group) or different concentrations of clove essential oil were then injected. Anti-inflammatory effects were measured by measuring the change in foot volume before and 3 hour after saline or clove essential oil injection.

The result:
Anti-oedema effect of clove essential oil is significant with effect greatest at concentration of 0.05mL/kg. It was shown in the experiment that clove contain anti-inflammatory activity in addition to its antibacterial and analgesic actions.

Anti-oedema effect
Single dose of TNBS was intrarectal administrated to anaesthetized mice to induce colitis. Development of colitis was assessed everyday by body weight. Mice were either fed with diet mixed with different concentration of rosemary oil (experimental group) or soy oil (control group). Mice were then killed 3 days after TNBS administration and the mucosal damage to colon was assessed using colon macroscopic scoring system.

The result:
It was found that rosemary can suppress inflammation of colon at high concentration of 5000ppm while lower concentrations of 1250ppm has minimal effect. It can be concluded that rosemary contains properties of anti-inflammatory with concentration playing a key point to efficiency.

Alleviating colitis
Where does it come from?
Cayenne, peppers and paprika

How is it used?
Orally and Topically

What is it used for?
Short-term pain relief, especially against muscle soreness and spasms in extremities and back.
Used successfully in controlling:
Postherpetic neuralgia, diabetes and neuropathic pain
Pain in osteoarthritis
Cluster headaches

How does it work?
The herb acts selectively on primary sensory neurons with nociceptive function, causing neurogenic inflammation.
1st exposure: intensely activates neurons
After 1st exposure: neurons become insensitive to all further stimulation (including stimulation from capsaicin)
Induce depletion of substance P and other neuropeptides from sensory nerve terminals.

Effective as a topical pain relief medication.
Compared with NSAIDs, analgesic effects are not as significant.

© HealthyHobbit

Where does it come from?
Extract from the secondary root of the plant. Found in the Kalahari sands of southern Africa

How is it used?

What is it used for?
Lower back pain, osteoarthritis and disorders of the musculo-skeletal system
Traditionally used for fever, pain, arthritis, malaria, diabetes, labor and convulsions

How does it work?
Significant analgesic effects have been seen in experiments against thermally and chemically induced nociceptive pain stimuli in mice. The opioidergic systems seems to be involved in the antinociceptive effect. The significant increase in the content of nitrites/nitrates was also significantly attenuated in experiments on mice.

There have been numerous studies and clinical trials outlining the effectiveness of Devil’s claw on alleviating pain associated with osteoarthritis. The effectiveness of pain relief is comparable to that of the usage of NSAIDs.

Where does it come from?
Flowers and Leaves of the plant, which is native to Europe.

How is it used?
Orally and made into a oil to use topically.

What is it used for?
Used for depression and anxiety with great effect. Additionally, research has suggested it is also effective for pain relief of burns and bruises, as well as use after surgery.

How does it work
Depression: the plant contains hyperforin, which is a chemical messenger acting on the nervous system controlling mood. An increase in hyperforin has been shown to increase happiness.


More research is needed to understand the effectiveness of St John's wort in its effectiveness on direct reduction pain. However, the research that has been undertaken has shown that it is mildly effective in relieving physical pain. With psychological pain on the other hand it has been shown to be of great effect and may be a alternative to antidepressants in some medical forms of depression.

Important to note its side effects:
Increases light sensitivity thus increases sunburn risk.
Has many drug interactions causing either the drugs not to work or potentially lethal interactions. Due to these reasons the herb is banned for use in Japan and Canada

Where does it come from?
There are 4 main types of lavender. The plant's fragrant flowers and stems are used.

How is it used?
Orally, topically and within oil.

What is it used for?
It is antimicrobial agent in nature with a pleasant fragrance additionally it is has a carminative actions (relieving flatulence). Additionally, it has a direct effect on the CNS to reduce firing and induce sleep.

How does it work?

The neurological effects of lavender vary with a combination of: Psychological effects of odour and inhaled volatile compounds, as well as acting directly via the limbic system – especially amygdala & hippocampus causing depression of CNS signals, thus this has been associated with reduction in pain.

Interestingly, when used topically such as during massage, linalool & linalyl acetate are rapidly absorbed through the skin. These molecules are known to have the following effects Linalyl acetate – narcotic action and Linalool – sedative thus sleep inducing.

Studies are inconsistent and more research is needed. However, for direct pain relief lavender is known to be a effective supplement although this is mostly through psychological benefit rather than physical.

Heavy metals
Drug interactions
Herbal medicine is being used in modern day in conjunction with conventional medicine, as well as an alternative to modern medicine. The use of herbal medicine to treat pain is on the rise as many people can not afford to pay for conventional medicine or wish to choose a more natural course of treatment.
Different types of pain
Neuropathic - Pain caused from nerve damage
Nociceptive - Pain caused by stimulation of receptors
Pain relief may be direct, affecting the sensory nerves themselves, or in-direct as a result of the medicine's anti-inflammatory properties reducing the inflammation causing the sensory nerves to fire.
Herbal medicine must be treated with caution as certain herbs may cause harmful side effects if used incorrectly.
Herbs may not all be identical, the potency of the same herbal species may vary incredibly creating Inconsistencies.
Herbal medicine can be effective in alleviating pain, but more research needs to be done to prove it.
It can be very variable depending on multiple factors, including preparation, genetics, dosage, etc.
Possible drug interactions may impede overall treatment progress.
Less chance of addiction
Generally cheaper than pharmaceuticals and can be used for management of chronic diseases.
Can be a preventive measure
Alternative option if pharmaceutical drugs are not effective/suitable for long time use/too expensive
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Devil's Claw
St John's Wort

Where does it come from?
Common crop grown in the Pacific islands for its roots and leaves.

How is it used?
Orally in ceremonial drinks and chewing of leaves and roots.

What is it used for?
Chewing small amount of the leaf or root causes the mouth and throat to go numb, providing pain relief to sore throats, canker sores, sore gums, and toothaches. Consuming small doses also relaxes muscles, induces sleepiness or feeling of well-being.

Surface anesthesia similar to cocaine in duration and strength, subcutaneous injects reportedly caused anesthesia for hours up to days.

Historically used as a sedative or anti-anxiety.

How does it work?
Its major components for pain relief are Kava lactones, Dihydrokavain , Dihydromethysticin and kawai.
Kava lactones absorbed in the stomach enterocytes into the bloodstream, travel to the brain and act as a nervous system depressant producing symptoms similar to drunkenness.

Analgesic effects are obtained from non-opiate pathways.

Theory that psychotropic effects are due to inhibition of 3H noradrenaline.

Research has shown evidence that the plant is very effective in reducing pain and has a direct effect on the pain pathways.
Kava Kava
- Randomised placebo controlled cross over 29 people with osteoarthritic pain took ginger or ibuprofen for 6 months, those taking ginger reported more pain relief than the ibuprofen group and the placebo group.

- Double blind study of people taking 1 gram ginger powder for 3 days from the beginning of menstruation experienced pain relief equivalent to the groups taking ibuprofen and mefenamic acid to relieve dysmenorrhea.

- Double blind crossover study people took 2 gram ginger before 30 minutes of cycling experienced no significant quadriceps muscle pain reduction compared to the placebo group.

- Rats with severe chronic adjuvant arthritis were orally given 33mg/kg of ginger oil for 26 days were observed to have a significant reduction of paw and joint swelling.
The way in which herbal medicines act has not yet been fully understood, and therefore the exact drug interactions are not completely known. However, there are some pharmacokinetic herb-drug and additive pharmacodynamic interactions that have been found.
Herbs that have hydrocolloidal carbohydrate components such as gums and mucilage are soluble in water but poorly absorbed, e.g. psyllium, rhubarb, flax-seed, marshmallow, and aloe.
These compounds are prone to bind to other drugs, especially when taken as whole or powdered forms. Psyllium (high in mucilage) inhibits the absorption of lithium. Aloe and rhubarb may cause diarrhea, which reduces the action of drugs that have a narrow effective dose range (eg, digoxin, warfarin).
In order to prevent a herb from binding with drugs, the drug should be taken 2 hours after or 1 hour prior to the herbal products.

Herbs such as meadowsweet and black willow, which contain pain-reducing salicylates, may displace highly protein-bound drugs such as warfarin, hence increasing the adverse effects of the drugs. These should therefore not be taken together.
Kava Kava acts as a dopamine antagonist and can increase tremor and make medications less effective in patients with Parkinson disease.
Certain herbs alter the metabolism of some drugs by either inhibiting or slowing down the metabolism, or speeding up the metabolism so much that the drug increases to levels where it becomes toxic.
Licorice decreases the metabolism of corticosteroids, causing adverse and toxic effects from their buildup.
St John’s wort can induce hepatic microsomal enzymes in the cytochrome P-450 system. Therefore it increases the drugs metabolized in this system (e.g. protease inhibitors, digoxin and theophylline, and cyclosporine). The drugs are thus rendered less effective, so it is not recommended that they are used concurrently.
As the herbal medicines have not been refined or tested as vigorously as modern medicines they may have residual heavy metals in their composition. Also, in unlicensed herbal medications heavy metals and their salts may be added, as they are not regulated by the FDA. This is one of the major issues internationally. The main heavy metals found are mercury, lead and arsenic and their respective salts. The presence of these may lead to heavy metal poisoning. Surveys carried out in the United States (2004) have shown that 20% of all Ayurvedic medicines in the Boston area contained potentially harmful levels of lead, mercury and arsenic.
Inorganic mercuric salts can cause:
Severe nausea
Bloody diarrhoea
Abdominal pain
Kidney damage and/or failure
Possible other effects to the nervous system
Arsenic salts can cause:
Various skin disorders
Severe nausea and vomiting
Haemorrhagic gastroenteritis
Cardiac arrythmias
Neuropathy of the peripheral nerves
Lead may potentially cause:
Abdominal pain
Kidney damage
Deterioration of mental control
Lack of coordination
Neuropathy of the peripheral nerves.
In 2004 reports from the United States and Hong Kong pointed towards a number of patients suffered lead poisoning after using a variety of unnamed Ayurvedic medicines.
Pharmacodynamic interaction is additive activity. E.g. valerian increases the hypnotic activity of benzodiazepines, and ginger, ginkgo and possibly by many other herbs increasing the anticoagulant action of warfarin. It is best that these products are not taken concurrently.
Ginger is an inhibitor of thromboxane synthetase and thus prolongs/alters bleeding time when taken with anticoagulants e.g. warfarin.
Kava Kava also has an additive effect, it potentiates alcohol, tranquilizers, and antidepressants, and may cause liver toxicity.
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Some medications both modern and herbal can be addictive especially opioids and cannbanoids. Opioids are derived from the poppy, which is a flower. Opioids bind to dopamine receptors in the brain stimulating the release of endorphins giving an analgesia sensation, as well as a general sensation of enjoyment. The patients get addicted to this "good feeling".
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