Daily Issues | Featured Article | Pain Relief
The Checkered History of Over-the-Counter Pain Relievers

In ancient times, pain relief was often the province of mystical healers who communed with the gods. Early civilizations relied on a combination of herbal remedies and magical rituals to cure what ailed them.
For example, many native cultures tried to draw pain out of the body by sucking on specially made pipes that were placed against the skin. The Incas used to chew the leaves of the coca plant while they worked, giving them almost superhuman stamina and tolerance for pain. In ancient Egypt, healers would pull electric eels from the Nile and place them over a patient’s wounds. Even Hippocrates, the father of Western medicine, got in on the act. He used to prescribe willow leaves to take the edge off.
These methods probably sound a bit crazy. Are they? Perhaps. But no more so than mindlessly popping a pill that kills 16,500 people each year and puts another 76,000 in the hospital.1,2
Pain happens. It’s an unfortunate fact of life. For as long as there have been people, there has been pain. And for as long as there has been pain, people have tried to ease it however they could. Relieving pain is an old pursuit.
It’s also a cash cow. True to form, Big Pharma has been on the scene for years. But their quest to turn (your) pain into (their) gold has led to a series of over-the-counter (OTC) drugs that often do as much harm as good.
Fortunately, there is hope. Years of research have taught us a lot about how the body processes pain — and how to block it. These findings have given us new insight into ancient methods that we used to dismiss without a second thought. In fact, the wisdom of the ancients may soon lead to safer natural alternatives to OTC drugs.
In this article I will survey the problems with the most common OTC pain relievers. Then I will tell you about several of these alternative remedies.
It’s funny. For all of our modern technology, it’s only by looking backward that we are finally moving forward.
The Painful Legacy of NSAIDs
Nonsteroidal anti-inflammatory drugs (NSAIDs) have become a staple of the modern American medicine cabinet. It’s almost a reflex. If you’re hurting, you reach for the nearest NSAID. Pop a pill and forget it. You probably never give it a second thought.
NSAIDs do a little bit of everything. They break fevers. They prevent clots. They stop swelling and inflammation. Oh, yeah — they relieve pain, too.
The most common NSAIDs are acetylsalicylic acid, ibuprofen, and naproxen. Acetylsalicylic acid is commonly sold as Aspirin. It was the first NSAID discovered, and it is one of the most widely used medications in the world. An estimated 40,000 tons of it are consumed every year.3
Ibuprofen is the generic version of several brand names. You buy it as Advil, Motrin, and Nurofen, among others.
Similarly, naproxen is the generic name of drugs like Aleve and Midol.
All of the NSAIDs work in basically the same way. They inhibit the cyclooxygenase (COX) enzymes, which control inflammatory reactions. No COX, no inflammation. It’s as simple as that.
The problem is selectivity. Nothing can affect as many different processes in your body as NSAIDs do without having side effects.
And the NSAIDs definitely have side effects. They can cause severe gastrointestinal (GI) problems, including ulcers and bleeding. They can give you kidney problems. And aside from low-dose aspirin, they dramatically increase your risk of heart attack and stroke. (Taking one baby aspirin per day may reduce your risk of heart attack.)
Neither children nor pregnant women should take NSAIDs. You also shouldn’t take NSAIDs if you’re taking any of the following drugs:
- ACE Inhibitors (used to lower blood pressure and treat congestive heart failure).
- Probenecid (used to treat gout).
- Lithium (used to treat psychiatric conditions and headaches).
- Warfarin (used to prevent blood clots).
- Methotrexate (used to treat cancer and autoimmune disease, including rheumatoid arthritis).
Hospitals give out NSAIDs like candy. And yet, NSAIDs bring 76,000 people a year to the hospital in the first place. Moreover — stop me if I’ve said this before — 16,500 people die from taking NSAIDs every year.
Well, I guess that’s one way to relieve pain.
You’ve Tried Everything for Your Back Pain. Now What?
Doctors, physical therapists, chiropractors, and other back care specialists mean well, but let’s face it… their options for treating you are limited.
Drugs, surgery, and therapy. That’s all they’ve got.
Here’s the problem: all three treatment options are based on the same limited thinking about back pain. And that thinking misses the real cause of your pain.
If it didn’t, wouldn’t your pain be gone for good?
Most likely your pain — whether it be back pain, sciatica, or pain from a herniated disc — is caused by something totally different.
And that “something else” is what’s keeping you in pain, despite your doctor’s or therapist’s best efforts.
So why hasn’t your doctor told you about this “something else”? Simply put, it’s just not part of the medical school curriculum or the “established medical thinking” about back pain. And… frankly, it may not be in their best interests…
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The Surprising Truth About Tylenol
Tylenol is the trade name of acetaminophen (a.k.a. paracetomol). It relieves pain and breaks fevers without the same risks as NSAIDs. In particular, Tylenol does not cause GI symptoms.
For that reason it is marketed as a safer alternative to NSAIDs. Safe enough, your doctor claims, for children and pregnant women.
And yet, acetaminophen toxicity is the leading cause of acute liver failure in the Western world. Tylenol accounts for more overdoses in the U.S., the U.K., Australia, and New Zealand than any other drug.
That’s right. Not heroin. Not cocaine. Not LSD.
Tylenol.
The real problem is that many common OTC cold and flu medications have the same active ingredient. Many people take several different drugs when they’re sick. The combination can be deadly.
When it comes to Tylenol, there can definitely be too much of a good thing.
COX-2 Inhibitors Don’t Live Up to Hype
When their profits were threatened by the specter of serious side effects, Big Pharma rushed to come up with a new and improved pain reliever. COX-2 selective inhibitors were heralded as the magic bullet. Whereas NSAIDs inhibit all COX enzymes, the new drugs targeted just COX-2 to provide side effect-free pain relief. No more complications, Big Pharma said. We promise.
The three most common versions were:
- Celebrex (celecoxib).
- Vioxx (rofecoxib).
- Bextra (valdecoxib).
COX-2 inhibitors do avoid many of the side effects of traditional NSAIDs. However, they also significantly increase your risk of heart attack, edema, thrombosis, and stroke. The risk is so substantial that Vioxx was pulled off the market in 2004. Celebrex is also named in over 31,000 ongoing lawsuits.
Sounds like Big Pharma’s “smart bomb” wasn’t quite as smart as they thought.
Back to Basics
So what’s the moral of the story? Is pain relief a tradeoff that only brings comfort at the cost of dangerous side effects?
Not at all. We’ve just run into trouble by trying to manipulate nature instead of working with it. Most modern drugs are simply quicker-acting versions of ancient remedies.
For example, opioid drugs like morphine are based on the same chemistry as coca leaves. The Egyptians’ use of electric eels was the forerunner of a modern technique known as transcutaneous electrical nerve stimulation (TENS), which applies an electrical current to the skin to relieve pain. Some have argued that the use of “healing pipes” led to acupressure, acupuncture, and massage.
And the willow leaves? They contain the chemical that was used to develop Aspirin.
We haven’t invented anything new to relieve pain. We’ve just made the relief faster — and more dangerous.
I’m not advocating that you go grab a mouthful of leaves the next time you have a headache. But I am suggesting that natural alternatives can provide safe, effective pain relief. Here are a few to consider:
- Curcumin. This is the natural pigment that gives the Indian spice turmeric its yellow color. Researchers at Cornell showed that curcumin is a safe, natural COX-2 inhibitor — Celebrex without the side effects.4
- Thunder God Vine. Extracts of this plant have long been used in traditional Chinese medicine to treat rheumatoid arthritis. Studies have shown that Thunder God Vine also inhibits COX-2 and reduces production of inflammatory proteins.5
- Omega-3 Essential Fatty Acids. Add another item to the long list of reasons that fish oil is good for you. A study at Cardiff University in Wales showed that omega-3s can not only inhibit COX-2, but also slow the rate of joint degradation that causes arthritic pain.6
- Resveratrol. This compound from grape skins is also common in traditional Chinese herbal medicine. Researchers at Cornell and at Barcelona University in Spain showed that resveratrol inhibits COX-2 in animal models.7,8
- Flavonoids/Phenolics. Researchers at Tsukuba University in Japan showed that some of these plant-derived chemicals selectively inhibit COX-2. However, more research is needed, as not all flavonoids have this effect.9
- Hops extract. A 2008 study in the journal Phytochemistry showed that the alpha acids in hops inhibit COX-2. Over a 6-week trial, patients taking 1000 mg per day reported 54% improvement in symptoms of knee osteoarthritis.10
Given my background in modern medicine, it is always surprising to me that “low-tech” treatment options like these can be just as, if not more, effective than their most sophisticated modern counterparts. And yet, it really shouldn’t be. After all, people survived for centuries without Big Pharma’s help. Pain isn’t new. It makes sense that the ancients would have figured out what to do about it.
Our dependence on modern pharmaceuticals is contrived. The next time you reach for an OTC pain reliever, think about what you’re really putting into your body. I’m not going to say that you should never take one. But do give it a second thought.
And maybe give one of these natural alternatives a try. You, too, might be surprised.
To Your Health,
Michael Noltemeyer
Managing Editor
Total Health Breakthroughs
References:
- Warner TD and Mitchell JA. “Cyclooxygenase-3 (COX-3): filling in the gaps toward a COX continuum?” Proc Natl Acad Sci USA, 99.21 (2002):13371–3.
- Tamblyn R, et al. “Unnecessary Prescribing of NSAIDs and the Management of NSAID-Related Gastropathy in Medical Practice.” Annals of Internal Medicine, 127 (1997):429-438.
- Singh G and Triadafilopoulos G. “Epidemiology of NSAID induced gastrointestinal complications.” J Rheumatol, 26S (1999):18–24.
- Zhang F, et al. “Curcumin inhibits cyclooxygenase-2 transcription in bile acid- and phorbol ester-treated human gastrointestinal epithelial cells.” Carcinogenesis, 20.3 (1999):445-51.
- Maekawa K, et al. “The molecular mechanism of inhibition of interleukin-1beta-induced cyclooxygenase-2 expression in human synovial cells by Tripterygium wilfordii Hook F extract.” Inflamm Res, 48.11 (1999):575-81.
- Curtis CL, et al. “n-3 fatty acids specifically modulate catabolic factors involved in articular cartilage degradation.” J Biol Chem, 275.2 (2000):721-4.
- Subbaramaiah K, et al. “Resveratrol inhibits cyclooxygenase-2 transcription and activity in phorbol ester-treated human mammary epithelial cells.” J Biol Chem, 273.34 (1998):21875-82.
- Martinez J and Moreno JJ. “Effect of resveratrol, a natural polyphenolic compound, on reactive oxygen species and prostaglandin production.” Biochem Pharmacol, 59.7 (2000):865-70.
- Mutoh M, et al. “Suppression of cyclooxygenase-2 promoter-dependent transcriptional activity in colon cancer cells by chemopreventive agents with a resorcin-type structure.” Carcinogenesis, 21.5 (2000):959-63.
- Hall AJ, et al. “Safety, efficacy and anti-inflammatory activity of rho iso-alpha-acids from hops.” Phytochemistry, 69.7 (2008):1534-47.
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Thanks for all the information. We need to know what is really healthy advice now especially since there is so much misleading information with so many side effects being advertised.
Information is good but want a permanent Cure .
I enjoy your newsletter and learn much from it, but I wish you would be more careful with your grammar. I’m specifically referring to the following sentence: “As someone trained in modern medicine, it’s always surprising to me that “low-tech” treatment options like these can be just as, if not more, effective than their most sophisticated modern counterparts.”
‘It’ is trained in modern medicine? “As someone trained in modern medicine, I’m always surprised…” would be not only better grammar, but clearer and more effective.
Dear Janet,
You’re absolutely right. I suppose that’s what I get for writing on deadline while serving as my own copy editor. I’d like to think that I would have caught the mistake in someone else’s work, or in my own given more time for review, but that still doesn’t excuse my oversight. Thank you for pointing it out. I take great pride in using correct grammar, and so I deeply regret the error and promise to do better in future issues. I will work hard to make sure that this was the last grammatical error you’ll ever see from me.
Ashamedly,
Michael
Mike,
I just signed up, via ETR. I downloaded the Anti-Aging link to share with my folks, but lost it, when a seperate download brought in a Virus. Can it be accessed again, please? Thank you.
I’ve been as natural as possible my entire adult life. What I would love to see is an objective head to head comparison of supplements: natural ingredients vs.manmade /efficacy/dose/price ratio, as if you were the Consumers Reports of Vitamins and Supplements. Daunting, I realize, but, hey, I’d love to help you do it…
Does anyone do it?
Dear Rick,
Thanks for signing up! I’m glad you’re enjoying our content, though I was sorry to hear about your computer problem. We have a Support Desk to handle all customer service issues like this one; you can contact them at http://www.supportatetr.com.
As for your suggestion… I do not know of any publication that currently does something like that, but I think it’s a great idea. We will definitely look into it for future issues of THB.
Thanks for writing, and please let us know if there’s anything else you’d like to read about.
Best,
Michael