Herbs: The Future Of Pain Relief

Words: Dr Rajgopal NIDAMBOOR

Pain is relative. It is also specific. Pain can emanate from previous illness and trauma, or from underlying causes, such as arthritis. In certain cases, there is no obvious cause of pain — or, one may erroneously attribute pain to a recent activity rather than a serious causal effect. Besides, it is not uncommon for people to assume aches as being caused, for example, by a recent sports activity, or hard work. In addition, most people would not know that aches might be symptomatic of a heart ailment, or a sign of stomach cancer. 

You get the clue. Most individuals bogged down by pain reach, by way of reflex, for a bottle of pain-killers, or soothing balm — to control, or get over, pain. It works. But, when the pain begins to stay, or leaves its ‘visiting card’ in their body, or joints, they sense there is something wrong. They visit a physician, or therapist — to find out what’s gone ‘wrong.’ The rest, as the cliché goes, is elementary, nay ‘alimentary.’ They are put on medication, most often a NSAID [non-steroidal anti-inflammatory drug] — for pain relief. Soon enough, they get over their pain syndrome, and also forget about it. They are lucky.

However, in many instances, the pain only expands in its intensity and, over a period of time, it becomes firmly established. When this happens, they are at their wit’s end — not because the NSAID medication they had begun to take dutifully has given them relief, but because it has slowly led to some unpleasant side-effects — in certain cases, sombre side-effects.

It’s, therefore, not without reason that research is at its wits’ end — and, for long deliberated on a tangibly acceptable line of treatment, with less side-effects. In the course of time, like most scientific endeavours, this sustained work has paid dividends — a group of novel medications that they not only provide better pain relief, but are also relatively free of side-effects.

Their identity — herbal COX-2 inhibitors.

Cox-1 & Cox-2

There are essentially two types of enzymes involved in prostaglandins production: cyclooxygenase COX-1 and COX-2. Prostaglandins are substances responsible for pain as well as other body functions, which also include protection of the stomach lining. COX-2, in essence, plays a key role in the creation of prostaglandins involved in pain and inflammation.

COX-2 inhibitors hamper the activity of specific COX enzymes, which release prostaglandins. On the other hand, COX-1 produces prostaglandins that protect the digestive system from its own erosive acids. So, it is important that the enzyme is best left to itself, and not interfered with.

COX is an enzyme naturally present in our body. COX-1 enzymes are produced abundantly throughout the body. These enzymes are involved in the regulation of day-to-day cellular and metabolic activities — maintaining stomach lining stability, regulating blood flow within the kidneys, and balancing platelet function. COX-1 should be present in the body always; also, it would not be the right thing for us to impede it. COX-2 enzymes, like COX-1 enzymes, are essential for inducing pain. But, unlike the COX-1 enzyme, COX-2 enzyme is present in our body within a restricted area. Also, factors such as diet, stress, and injury can affect its formation. So, when COX-2 is produced on a constant basis, persistent pain follows. The implication: obstructing COX-2 is a choice we’d rely upon for joint and muscular pain relief and management, among other things.

COX-1 enzyme produces prostaglandins that help maintain the capability of the gastroduodenal mucosa, while COX-2 enzymes form prostaglandins at sites of tissue inflammation, or injury, that trigger pain and swelling. You get the point — aspirin and the other NSAIDs inhibit both COX-1 and COX-2. They often cause gastrointestinal bleeding and ulcers. On the other hand, herbal COX-2 inhibitors ‘selectively’ inhibit COX-2, while sparing COX-1. Hence, they cause relatively less gastrointestinal side-effects.

NSAIDs

Prostaglandins are natural chemicals — they are key elements involved in inflammation. They perform a variety of functions within the body, including the control of inflammation and blood vessel permeability, regulation of hormones, stomach acid secretion, body temperature, and smooth muscle contraction. The enzyme responsible for prostaglandins synthesis is, as already cited, COX. This is precisely the link vis-à-vis the COX enzyme’s significance.

To go back to NSAIDs — NSAIDs reduce inflammation by thwarting the body’s production of prostaglandins. In the process, they also disturb the production of certain prostaglandins that play a critical role in protecting the stomach from acidic effects as well as maintaining the natural, healthy condition of the belly lining. Any ‘disturbed’ effect can lead to gastric ulcers and bleeding. 

NSAIDs are commonly prescribed medications for inflammatory symptoms, or arthritis, a major joint disorder. Common side-effects of NSAIDs include — abdominal pain, diarrhoea, bloating, heartburn, and dyspepsia. Long-term NSAID usage can lead to ulceration of the stomach and duodenum, in 15 per cent of patients; though many patients are asymptomatic, or not aware of their ulcers, they are at risk, no less, of developing serious ulcer complications, including bleeding, or perforation of the stomach.

A huge population of patients with pain syndromes takes NSAIDs regularly: approximately 35 million Americans alone, for example, according to reports, are currently on NSAID treatment. At the same time, some estimates suggest that the annual risk of serious complications is 2-4 per cent with continual NSAID treatment. The risk increases substantially in elderly patients — especially those suffering from rheumatoid arthritis, patients taking blood-thinning medications [e.g., heparin], or prednisone, a cortisone medication, and those with a prior history of bleeding ulcers and/or affected by heart disease. It is also reported that nearly 2,500 people die, in the UK, from stomach bleeding, each year — a well-known side-effect of NSAIDs, like aspirin and ibuprofen.

Herbal Ammo

Scientists have [re]discovered many traditional herbs that can safely inhibit the COX-2 enzyme. These herbs are ginger, turmeric, holy basil, green tea, rosemary, skullcap, oregano, Chinese goldthread, and so on.

To begin with, let’s explore what herbal COX-2 inhibitors hold for us — a mirror to the future of pain relief — gently, and purposefully, and without the ‘troubled’ side-effect profile of conventional, or synthetic, COX-2 medications. So, get ready to doff your hat to herbal coxibs — the safe and sure alternative mode to pain relief and for physical, physiological, and emotional wellness.

Our body has two inflammatory pathways, both evolving from arachidonic acid, the inflammatory precursor. So, it is obvious that blocking one pathway while sparing the other isn’t good medicine. Research also reports that an herbal inhibitor of 5-LOX has proved to be valuable in the treatment of arthritis. The medication [5-Loxin] is derived from Boswellia serrata, a tree native to India, whose aromatic gum resins have been used in Ayurveda to treat arthritis, since ages. As a matter of fact, laboratory analysis of the gummy resin from Boswellia serrata shows one component — ß-boswellic acid — that acts as a specific inhibitor of 5-LOX. With its isolation, it is now possible to derive the benefits of 5-LOX inhibition without resorting to the use of large amounts of ‘ordinary’ Boswellia serrata extracts for treatment.

When research synthesised COX-2 inhibitors, a hugely beneficial, and grossly unexpected, side-benefit also resulted from their efforts — the motivation to find herbs and plant compounds to synthetically copy, or mimic, the former. In so doing, it identified several traditional herbs that contain natural and safe COX-2 inhibitors. You know their identity.

So, from one, it is two today — the creation of synthetic COX-2 prescription drugs has led to the [re]discovery of herbal alternatives that are naturally available and, what’s more, without prescription. Also, all of this with their natural ease of use, economics of scale, and relatively fewer, or minimal, or negligible side-effects in comparison to conventional coxib medications.

Gastric Safety

Conventional COX-2 inhibitors, research acknowledges, have a lower potential to cause stomach ulcers; but, one cannot rule out the possibility of ulcers in certain patients. This is not all. As a safety measure, labels for cox medications, celecoxib and rofecoxib, for instance, clearly advise patients to be vigilant for heart concerns, gastric ulceration and bleeding that can occur without warning, and report them to their physician. In addition, conventional COX-2 inhibitors can also increase blood pressure, cause leg swelling and alter, or aggravate, kidney function, like their older ‘cousins’ — traditional NSAIDs — in certain patients. What’s more — as with new drugs — previously undetermined risks may emerge down the line with conventional coxibs. It is, therefore, imperative that further research is needed to determine if conventional coxibs are reliable enough to replace traditional NSAIDs as first-line agents.

It is a well-known fact that, for ages, natural remedies such as white willow bark [Salix alba] and myrtle [Myrtus communis] have provided pain relief for millions of users. Willow bark, an ancient remedy, which is used to treat fevers and arthritic complaints, has often been referred to as ‘nature’s aspirin.’ Salicin is its active ingredient. Several human studies have evaluated and confirmed the remedy’s ability to rapidly relieve pain and, in the process, reduce inflammation.

Myrtle has also, for long, been used as a stimulant, astringent, emetic, anti-spasmodic, expectorant, diaphoretic, and tonic. It finds reference in ancient Egyptian and Greek manuscripts. Evidence also supports the fact that it was prescribed by Hippocrates, father of modern medicine, to combat pain and fevers. What was not known for centuries was the exact mechanism of its action. Salicin, studies now report, does not lead to stomach upset, or gastric bleeding, as aspirin does. It lowers your body’s levels of prostaglandins and has been known to have long-lasting effects. It has a noticeable action on acute and chronic pain, including back and neck pain, muscle and menstrual cramps. A large number of arthritis sufferers have experienced reduced swelling and inflammation — and, eventually increased mobility — in the back, knees, hips, and other joints, with its use.

Dr RAJGOPAL NIDAMBOOR, PhD, is a wellness physician-writer-editor, independent researcher, critic, columnist, author and publisher. His published work includes hundreds of newspaper, magazine, web articles, essays, meditations, columns, and critiques on a host of subjects, eight books on natural health, two coffee table tomes and an encyclopaedic treatise on Indian philosophy. He is Chief Wellness Officer, Docco360 — a mobile health application/platform connecting patients with Ayurveda, homeopathic and Unani physicians, and nutrition therapists, among others, from the comfort of their home — and, Editor-in-Chief, ThinkWellness360.

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