The Search for the Killer Painkiller

NY Times ^ | February 15, 2005 | ANDREW POLLACK

[neverdem]

Despite all the advances of modern medicine, the main drugs used to fight pain today are essentially the same as those used in ancient times.

Hippocrates wrote about the pain-soothing effects of willow bark and leaves as early as 400 B.C. Opium was cultivated long before that. Aspirin and morphine, based on the active ingredients in these traditional remedies, were isolated in the 1800's and helped form the foundation of the modern pharmaceutical industry.

But scientists are now trying to find new ways of fighting pain. The effort has been given new impetus by the recent withdrawal of Vioxx and the questions surrounding the safety of similar pills like Celebrex and Bextra. Those concerns come on top of the problems of abuse of narcotic painkillers like OxyContin. "There's a huge void, and no one is filling it," said Remi Barbier, chief executive of Pain Therapeutics, a company in South San Francisco, Calif.

But Dr. Barbier's company and dozens of others are trying. And some new treatments may come from things in nature that soothe or sting, like marijuana, hot chili peppers, nicotine and deadly toxins of snails and fish.

While the withdrawal of Vioxx leaves more room for newcomers, it also makes their challenge harder. Not only have opioids and aspirin been hard to beat, but the Food and Drug Administration is now expected to demand more evidence that drugs are safe before approving them.

But what scientists have going for them now is a more detailed, though still not complete, understanding of the molecular mechanisms by which pain is perceived. The goal is to create drugs that block specific parts of the mechanism while avoiding the side effects that have plagued opioids and anti-inflammatory drugs like aspirin.

Tens of millions of Americans suffer from chronic pain, according to various surveys, and millions more suffer acute pain from an illness or injury each year. Specialists say pain has received inadequate attention and treatment.

"Pain has historically been viewed as a symptom of other things that are more important," said Dr. Russell Portenoy, chairman of pain management and palliative care at Beth Israel Medical Center in New York. But now, he said, there is a growing realization that "chronic pain is itself an illness, and it's a complex illness."

Normal pain - from touching a hot stove, for example - is a beneficial warning system. After an injury nerves can become extra sensitive to pain. A warm shower can be painful on a sunburned back. That, too, is protective, said Dr. Clifford J. Woolf, a professor of anesthesia research at Harvard and Massachusetts General Hospital. The sensitivity forces a person to protect an injured area so it can heal.

But in some cases this nerve hypersensitivity continues well after the stimulus is gone, like an alarm frozen in the "on" position. The pain takes on a life of its own.

"Persistent pain is not just long-term acute pain," said Dr. Allan I. Basbaum, a professor of anatomy at the University of California, San Francisco and editor of the journal Pain. "The nervous system has changed."

Doctors classify pain into various categories, but there are two main types of persistent pain. One, sometimes called nociceptive pain, results from damage to tissues, as from arthritis or a burn. The other, called neuropathic pain, results from damage to the nerves themselves and is often set off by diseases like diabetes or shingles.

Opioids, like morphine or OxyContin, are used for more severe tissue-type pain. But the drugs have side effects, including constipation and a slowdown in breathing. Users can become tolerant, meaning that they need increasingly higher doses, or they become addicted to the drugs.

Aspirin and similar drugs like naproxen (sold under names like Aleve and Naprosyn) and ibuprofen (Advil and Motrin) are called nonsteroidal anti-inflammatory drugs or Nsaid's and are used for less serious pain. They block certain chemicals that contribute to inflammation, but they can also cause stomach ulcers and bleeding.

Vioxx, Celebrex and Bextra are newer types of Nsaid's called cox-2 inhibitors, which were intended to cause fewer gastrointestinal problems. But Vioxx was found to raise the risk of heart attacks and stroke, and there is concern the other cox-2 inhibitors may do so as well.

Nsaids don't work for neuropathic pain, specialists say, and there is disagreement on how effective opioids are. Doctors often use epilepsy drugs like Pfizer's Neurontin, which calm overexcited nerves that can cause seizures. Certain antidepressants are also used, most recently Eli Lilly's Cymbalta, which is also approved as a treatment for diabetic neuropathic pain.

Some efforts to develop better pain relievers focus on variations of the existing treatments.

For example, DOV Pharmaceutical, based in Hackensack, N.J., is in the final stages of testing a drug, bicifadine, for lower back pain. Like some antidepressants, it helps prolong the action of two brain chemicals, serotonin and norepinephrine.

Pain Therapeutics is in the final stages of testing a combination of an opioid with a small amount of a drug that counteracts the opioid's effect. The theory is that this will stop the buildup of tolerance, allowing opioids to be used more effectively.

NicOx, a French company, is testing a drug that breaks down in the body into naproxen and a chemical that releases nitric oxide. Nitric oxide plays many roles in the body, including dilating blood vessels and spurring mucus formation in the gastrointestinal tract. Some early trials suggest, though not definitively, that the drug may have lower gastrointestinal and cardiovascular risks than other Nsaid's.

But experts say there is also a need for totally new categories of pain relievers, ones that work in entirely different ways.

One such drug, called Prialt, was approved by the F.D.A. in December. It is a synthetic version of a toxin that a South Pacific marine snail uses to paralyze its prey. The drug impedes the transmission of pain signals through the nerves by blocking channels through which calcium ions flow into nerve cells.

"This is really the first new analgesic in two decades," said Lars Ekman, head of research and development at Elan, the Irish company that developed the drug. He said the drug was nonaddictive and 1,000 times as potent as morphine.

Potent, yes, but also problematic. To minimize side effects as diverse as heart rhythm disturbances and hallucinations, the drug must be injected directly into the fluid surrounding the spinal cord with a catheter and implanted pump. That will limit its use, as will the F.D.A. approval, which is only for severe pain that is not responsive to other analgesics.

Neuromed Technologies of Vancouver, British Columbia, says it has a calcium channel blocker that is safe enough to be taken orally. But the drug is only in the first stage of clinical trials, so there is no real proof yet that it is safe and effective.

Another approach is to block sodium channels. This is how local anesthetics like those given by dentists work. Wex Pharmaceuticals of Vancouver is testing tiny amounts of a toxin from the fugu, or puffer fish, a dangerous delicacy in Japan.

Chili peppers are less deadly, but their main ingredient, capsaicin, can cause intense pain when put in the mouth or rubbed on skin. Exposure desensitizes and temporarily damages the pain sensors.

Some over-the-counter pain ointments contain capsaicin. NeurogesX of San Carlos, Calif., is developing a patch containing highly concentrated capsaicin to be put on the skin for an hour in a doctor's office. A local anesthetic would be used to blunt the pain of the treatment itself. But after the patch is removed, pain in that area is diminished for weeks, the company's studies have shown. AlgoRx of Secaucus, N.J., is developing a capsaicin formulation that can be injected into joints or spread on surfaces exposed during surgery.

A different approach would be to block the sensors on nerve cells activated by capsaicin, called the TRPV1 or VR-1. That would theoretically provide pain relief without the initial pain. The drug giant Merck and tiny Neurogen of Branford, Conn., are working together on drugs to block this receptor, as are other companies like Amgen and GlaxoSmithKline.

Derivatives of marijuana are also being looked at. "Certainly with marijuana there's thousands of years of human experience that in addition to the psychoactive effects there are also medicinal effects," said Dr. James E. Shipley, senior vice president for clinical development and medical affairs at Indevus Pharmaceuticals in Lexington, Mass. "The problem heretofore is that you can't have one without the other."

Indevus is testing a drug based on a chemical, tetrahydrocannabinol-11-oic acid, that THC, the main ingredient in marijuana, turns into in the body. In healthy volunteers, Dr. Shipley said, the drug caused no psychoactive effects. But there has been only one small trial showing that the drug provided better pain relief than a placebo.

GW Pharmaceuticals, a British company, is further ahead. It says it is close to getting approval from Canada to sell a mouth spray derived from marijuana as a treatment for neuropathic pain in patients with multiple sclerosis. Nicotine, the poisonous substance in tobacco, also has soothing effects. Companies like Abbott Laboratories and Targacept, which was once part of cigarette maker R. J. Reynolds, are in early testing of drugs designed to bind to some of the same receptors in the body as nicotine but not be addictive.

Rinat Neuroscience of Palo Alto, Calif., and Genentech are working together on an antibody that blocks nerve growth factor, a protein made by the body that stimulates the growth of nerve cells.

Genentech initially tested the growth factor to see if it would reverse nerve damage from diabetes. But patients getting the drug experienced severe pain. It turns out that nerve growth factor has a second role: it is released after an injury and helps activate the pain pathway. So the companies figure that blocking it will stop pain.

Experts like Dr. Basbaum and Dr. Woolf, who consult for various pharmaceutical companies, say that controlling pain may require a combination of drugs hitting different mechanisms, just as cancer is treated with combinations. Ultimately, they say, the goal will be to tailor drug therapy to each patient based on the mechanisms underlying that person's pain.

New drugs are not expected to reach the market for a few years, and many may fail or have unacceptable side effects. Still, the void left by Vioxx has buoyed companies like NicOx, which two years ago faced a bleak future when a big drug company it was working with decided not to pursue its drug.

"You're standing on a rock surrounded by water," said Vaughn Kailian, a director of NicOx, "and just when you think you're going to vanish under the waves, the water recedes and you're standing on a mountain."

[neverdem]

Susan Farley for The New York Times

Joan Klopfer, 54 | Bronx, nurse
I used to be a nurse at Sloan-Kettering Cancer Center. In late 1997, I was lifting a heavy patient in the I.C.U. when I felt pain shooting down both my legs.

I knew right away I was in trouble. I had two herniated disks as a result and had to undergo spinal fusion. I woke up in the recovery room in the most excruciating pain you could imagine. It was worse than natural childbirth. They gave me morphine, which wasn't really enough.

I went home with a prescription for Percocet. It would offer me some relief for maybe an hour, then this awful pain would start again. Eventually, they put me on OxyContin, and I would take oxycodone as a "rescue dose" whenever I experienced terrible breakthrough pain.

Now, seven years later, I'm in constant pain, and this is as good as it's going to be. I'm permanently disabled. I probably will never work again.

My life is altered tremendously as a result of the pain.

Marty Katz for The New York Times
Farrell Fitch, 59 | Chevy Chase, Md., agency worker
I have nerve damage on the left side of my face, a result of shingles. At first, I thought I'd be fine and could get through it. But I couldn't. It feels like a branding iron pressed against my head.

What's discouraging is that you lose faith in the medicine. It takes the edge off the pain, but can never really take it away.

My doctor started me on hydrocodone and an antidepressant. After about two years, I wasn't getting any better so I tried other things. I tried acupuncture, massage therapy, even Chinese herbs. Eventually, I went to a pain specialist and one of the first things he had me do was to try methadone. It was a catastrophe. It just made me incredibly sick.

I got better when I combined Neurontin and Vicodin; something just clicked. Three years later, I had another crushing episode. I had to stop working and go on disability.

The pain is a large part of my life now. I struggle with it.

Frances Roberts for The New York Times

Steve Feldman, 52 | Manhattan, advertising
I was diagnosed with Lyme disease about seven years ago, and a side effect of it is arthritis. It's affected my hips, my hands and my fingers. The only time it bothers me is when the Lyme disease kicks in, which inflames everything.

When it first started, I asked my doctor what I could take besides aspirin or Motrin. All those things really have no effect on it at all.

We tried one of the arthritis medications, Vioxx, and the sides effects were awful. I suffered nausea and stomach pains and stopped taking it.

Then my doctor suggested some nutritional alternatives that had worked for some of his other patients. I said, "Sure, anything to get rid of the aches."

So I started taking glucosamine, fish oils and a product that's an oil made from macadamia nuts. I actually started feeling the aches going away after a couple weeks.

My doctor also said don't stagnate. In other words, walk. Use the joints. That helps me because it gets the muscles and the tendons around the joints used to working.

[neverdem]

FReepmail me if you want on or off my health and science ping list.

[zencat]

I'm with you. Have abnormal large congenital cysts in my C-T region and many more in the L region. Several of the cysts are over 1cm in the T region and cause unimaginable pain and numbness down my arms. Have a pretty good doc that cool with narcotics, but most people can't understand that it's just not "back pain". Duh! You've freaking cysts around the nerve root push on the nerve itself. It doesn't only hurt at times, just an indescribable feelings of numbness, pain. It's still not all about the narcotics, but does help the same way antibiotics help strep throat or pneumonia.

[John Valentine]

The authors failed to mention this one, perhaps the most promising of new therapies for neuropathic pain:

ACV1

Metabolic's novel compound ACV1, was discovered by Associate Professor Bruce Livett and fellow scientists associated with the University of Melbourne. ACV1 is a peptide compound discovered in the venom of the Australian marine cone snail, Conus Victoriae, which has been found to have profound analgesic properties. Owing to the success and advanced stage of efficacy testing already performed on the compound, Metabolic will accelerate the commencement of a pre-clinical toxicity program. Metabolic has acquired from the inventors the exclusive worldwide license to commercialise ACV1, in return for milestone and royalty payments.

Cone snails have evolved a rich cocktail of peptides in their venom, which together act by a variety of mechanisms in the nervous system to quickly immobilize or kill their prey. The potential of cone snail venoms as a source of new therapies has been recognised for many years, and the first such compound to be commercialised is the analgesic Ziconotide being developed by Elan Pharmaceuticals. Ziconotide acts by blocking a component of the central nervous system called the N-type calcium channel and must be injected into the spine (directly into the central nervous system) so as to avoid adverse reductions in blood pressure which would otherwise occur. ACV1 acts by an entirely novel mechanism, specifically blocking a subtype of a broad class of receptors in the peripheral nervous system called neuronal nicotinic acetylcholine receptors (nAChR). Unlike other cone snail venoms, ACV1 is effective and without apparent adverse effects when administered by convenient routes such as subcutaneous injection, providing substantial pain relief in models of nerve pain. Nerve (neuropathic) pain is the category of pain having the greatest need for improved drugs. An additional unique feature is that ACV1 also appears from the animal data to accelerate the functional recovery of injured nerves.

More here: http://www.metabolic.com.au/

[corkoman]

Very good article. The withdrawal of Vioxx and Celeb are forcing all new drugs to be compared with the opiodes. Other than the dependancy issue and constipation they are remarkably well-tolerated for chronic use over decades. Being compared to opiates is unfair - with their high safety profile any new drug is going to have to jump through hoops of fire to get approved.

Pain is nature's fire alarm but the Maker didnt give us a very good way to turn that alarm klaxon off.

[St.Mark]

Sciatica, pain down my right leg all the times. Some days are worse than others. Right now I am on Vicoden but my tolerance for the drug has gone up and so has the pain. It hurts so bad sometimes I cry and I am a 50 year old man that never cried a day in his adult life.

[xJones]

I took my cousin to a chronic pain care center. She has very bad daily migraine headaches and she'd done all the pain meds plus alternative meds, herbals, and acupuncture.

While I waited for her, I talked to the other people and everyone else was there for chronic back pain. I don't what they got, but my cousin had cortisone shots to both sides of her neck. It only eases things for about 3 months. Any migraine help would be appreciated.

[afnamvet]

Having just been released from the hospital for a partial bowel obstruction (Crohn's disease), I can attest to the effectiveness of morphine. 2-4mg every four hours for level 7-8 pain. I don't recall the alternative pain med name that was available.

[Goodgirlinred]

I just want my Viox back until they come up with something just as good to replace it. I had forgotten how bad the pain was until I had to go off of it and it got out of my system. Now I have to take OTC Ibuprophen in high doses and experience stomach upset. :(

[steve86]

Have your tried acupuncture? It stopped my mother's sciatica in its tracks, instantly, after several unproductive visits to conventional physicians. And my wife had the experience of sinus clearing while actually receiving the acupuncture.

I am 50 also and went through the crying thing in the 90s. Embarrassing when you know the neighbors can hear it. My pain left on its own -- so might yours.

[steve86]

Maybe some acupuncturists are better than others.

[John Valentine]

ACV1 is targeted at precisely your type of pain. See above.

Problem is, it's four years away from the market.

[unixfox]

Oh man how I feel your pain! I have sciatica as well and it has to be the worst pain you can get. My leg has gone so numb that I couldn't walk.

I cannot tolerate codeine or any derivative thereof. I have learned to actually pop my back to alleviate the pressure. The problem with painkillers is that they only trick your brain into thinking the pain is gone. When what they should really do is attack the affected area.

[Graybeard58]

Having just been released from the hospital for a partial bowel obstruction

My colon ruptured and the pain was intense. Two years after that surgery, scar tissue obstructed my bowels. THAT pain made the original pain seem like a picnic.

On vacation, lying on a couch in a motel lobby waiting for an ambulance to come through a snow storm. A cop got there before the ambulance and I layed there wondering if I could get his gun some how and end that pain.

I am 59 years old and that was the first and only time I had ever given a thought to suicide.

[St.Mark]

Bear Wash- I hope it does leave like what happened to you. The Doc's say surgery is my only option besides drugs. The success rate stinks with back surgery. I have to apologize for the whining it's hurting bad tonight and I know I won't be able to sleep. Enough said, thanks for listening and understanding, sometimes a man can feel so damn alone with a problem.

[St.Mark]

I wish there was a cure too Unixfox I REALLY do!

[afnamvet]

I am 59 years old and that was the first and only time I had ever given a thought to suicide.

I'm 57 and have had those thoughts countless times. March 15th is the surgery date for either bowel resection (will be my 6th surgery) or multiple stricture plasty. Quality of life isn't too promising but who knows until after this is over. Good health to you and yours.

Roger

[neverdem]

Triptan nonresponder studies: implications for clinical practice.

Birth contol pills can cause migraines. Good luck

[not_apathetic_anymore]

bookmark

[KingNo155]

Did she see a good dentist? I only ask because my brother suffered from migraines for years and Doctors and dentists could not find any reason. To cut it short... he went to a new dentist who found a hairline crack inside his tooth next to the nerve, the tooth was removed and now he no longer has migraines.

[Wycowboy]

I've had migraines all my life. The new Triptan drugs were a Godsend for me, I never leave home without my Zomig. Another good one is the medicine that is delivered by means of a nasal inhaler. I forget the name of it, something like Dihydroergotomine. Prayer sometimes works too. Good luck.

[newzhawk]

I have spinal arthritis and 2 bad disks- I am on ultram and baclofen- started going to an accupuncturist with herbs and the needles- have been able to do more than I have in years- more energy and less attacks of pain and spasms. Have been taking lots of fish oils, glucosamine, lyprinol oil instead of the celebrex - some days I wish I could go back to one vicodin a day and do things I used to like tennis,working out etc but the Dr's are scared to death to order anything- and I would hate to have them cut me off once I got used to them- as they are prone to do. The pain clinics around here do a lot of nerve blocks and transmitter implants....Try an antidepressant for help with the pain despair-ps I am a nurse - ruined my back lifting people in ICU for 15 years

[Rennes Templar]

I'm a chiropractor. Have you seen one? I have relieved many bad cases of sciatica permanently. Go see an S.O.T. chiropractor. There is no reason to live in pain, unless you have severe nerve damage, which is rare.

[tiki]

Just anecdotal but my niece had horrible migraines and Feverfew worked. You take it just like aspirin, when the pain starts, unlike most herbal remedies which you usually have to take for months to see any improvement. It's cheap and if it worked it would be great.

[rdcorso]

I learned a good bit of advice right before I was supposed to start Vioxx that caused me not to take it.The article I read said you should never take a new medication that hasn't been on the market for less than seven years unless it's a life or death decision.The reason for this is the researches are just getting the information of the long term side affects at the six or seven year mark.I would also stay away from the drugs that the companies can't explain how they work.There are quite a few like that on the market and I think Celebrex is one of them.

[steve86]

Sounds encouraging. I took fish oil for a long time, recently gave it up because I tired of the after-taste, now have switched to flax seed oil with its healthful fatty acids (Omega-3 and Omega-6). And I was prescribed fluoxetine for pain-based depression as well.

Regarding choosing an acupuncturist, people often get referred through word-of-mouth and that is at it should be. I would much rather hear a personal recommendation than look up an ad in the yellow pages. We are lucky in my small town to have an M.D. Internist who is also certified in Traditional Chinese Medicine (he is from Taiwan). This way you get the western and eastern approaches in one package. State laws vary as far as certification for acupuncturists.

BTW, my family recently had some experience with the ICU staff. We all had to compliment them as some of the most professional individuals we had ever observed.

[MikeHu]

About two years ago, I thought I'd never walk again.

When I was a child, doctors told me I had arthritis and would be crippled by the time I was an adult. Then, they said, "Doctors could operate." "And then I'd be all right?" I asked hopefully. "No, but then they can operate," the doctor replied cynically.

So I started exercising with light weights because I noticed increasing the circulation in that way relieved the pain. After a year of doing that, somebody asked if I ever considered entering a bodybuilding competition "because you're the most muscular guy around." Doctors who saw me said I was probably the healthiest guy they had personally seen -- but once a year I'd come down with severe back pains for about two months and for another two months, I'd have a bad case of bronchitis.

Then two years ago,it seemed the back pain wouldn't go away this time and I could barely walk ten feet in excruciating pain. I thought about getting an electric scooter with a seat. But just then, I noticed an article in the newspaper about a doctor who claimed he had found a surprisingly simple cure for fibromyalgia -- which seems to include 90% of the chronic symptoms most people complain about. The cure was guaifenesin.

I knew nothing about fibromyalgia but I was very familiar with guaifenesin because I took it to cure my bronchitis -- and noted back in the mid-80s that it made me feel good. I thought one should take it regularly as a health tonic like Geritol. Health professionals I suggested this to warned me against becoming addicted to cough medicine because shortly before this time,codeine was the main ingredient in cough medicines. Now, the new and improved wonder formula was guaifenesin. I thought it was so good I went and bought 1,000 shares of AH Robbins, the patent holder; they corroborated my suspicions that there were promising other as yet unspecified cures for guaifenesin. They did not materialize by the time of the stock market crash of 1987 and so I sold it and forgot about it.

So guaifenesin I knew something about and bought a few bottles before attending the lecture that weekend. I had been reluctant to continue taking the product except when I had bronchitis symptoms since the label warned against it -- as standard protocol. I learned at the lecture that there was no known negative side-effect with prolonged use. I searched the Internet to find what studies I could on guaifenesin and was impressed that there was no known negative side-effects but it seems, many positive ones.

Apparently guaifenesin does not only liquefy the mucus in the lungs when one has a respiratory inflammation but liquefies the mucus throughout one's body. The major lubricant in the body is mucus. As a joint moves, the cartilage releases mucus to provide lubrication for that movement.

As cells age, they tend to become less liquid and fluid, so as they congeal, they eventually cease functioning as cells, which requires the proper viscosity to continue optimal functioning. The pioneer of this cure is St. Amand. The cure is an underground sensation, spawning support groups around the world.

What convinced me was that a week into the regimen, I noticed my old high school football knee injury of thirty-five years disappeared completely and hasn't returned, nor have I had debilitating back pain or bronchitis since. The exciting concept here is that all the cells in the body may be breaking down due to the same universal cause rather than that only the heart, lungs, joints, digestive tract, etc. tissue are malfunctioning while all the others are perfectly all right. It may be that it is just noticed in one tissue or organ before the others -- but the whole body is disfunctioning in this way -- because the essential liquidity of the body is too thick to allow for proper cell functioning.

Most of those I've shared this cure with have noticed that there was a period of pain-free functioning that is pretty inobtrusive. And when they noticed painful episodes in their lives thereafter, they noted coincidentally, that they weren't using it. It is pretty similar chemically to aspirin; in fact, it was a rival to aspirin that lost out a hundred years ago -- but maybe should have been the path we went down. Rather than causing digestive upset, it seems to cure it -- along with many other chronic conditions.

[jamaly]

Bump for later.

[steve86]

That reads like an infomercial (understatement), but I can confirm that guaifenesin has been helpful in the case of my wife's fibromyalgia. It is also fairly inexpensive if you buy the generic #100 bottles (around 38 cents a tablet, I believe it is). These are the exact same physical tablets as the Guaifenesin Extended-Release 600 mg brand.

[steve86]

I meant same as the Mucinex brand.

[MikeHu]

There is a feeling among many that the quick-acting tablets are actually preferable because the patented process to make the tablets slow-release may render it indigestible with people who have digestive difficulties, as many who have FM do.

So the quick-acting tablets are available for around $10; one chiropractor even suggested that the reason the study failed to prove the guaifenesin cure was because they were using the extended release tablets, and he found in his own patients, many for whom extended release tablets did not work, quick-acting does. When a tablet is indigestible, it may cause digestive upset; that doesn't seem to be a problem with quick-acting tablets.

[neverdem]

Interesting comments, thank you.

[MikeHu]

Some things just make sense.

Usually when there is a breakthrough in understanding, insurmountable, ever-multiplying complexities give way to a universal, unifying simplicity.

That is the history of human understanding.

[lainde]

bttt

[MamaLucci]

I have read about the guaifenesin cure, and was very interested in reading
that a freeper has tried it with success. Please tell me, were you strict about avoiding products with salicylates?
What dosage worked for you?

[eno_]

I wonder if any Drug War (i.e. ONDCP) money was used to promote "new improved" painkillers?

Did you know that Rush Limbaugh was put on Vioxx while in rehab?

Bit of a tradeoff, eh?

[rdb3]

I am 59 years old and that was the first and only time I had ever given a thought to suicide.

---

I certainly empathize, Graybeard. Cluster headaches make me feel suicidal. Those are completely nonresponsive to pain medication. The only solution is to prevent them from starting. After they start, hold on for life for about 60-90 minutes.

[MikeHu]

There are some people who do not believe that the obsession with avoiding salicylates is an integral part of the guaifenesin cure. Dr. St. Amand may have gone overboard in using that as an explanation for why the Oregon study failed to show the effectiveness of the guaifenesin cure -- using time release guaifenesin tablets. As one chiropractor pointed out, and I noticed too when I started on slow-acting guai, the process of supercompacting the powder under pressure makes the tablets as hard as rocks and may be undigested by an impaired digestive system, as is common in many fibromyalgics. One will note that if one puts one of these highly-compressed tablets in water -- they will not dissolve, no matter how much time passes. So they will go through one's digestive as an irritant -- giving one no relief from irritable bowel syndrome. If that is a major marker, then not only would it not solve the problem but might even exacerbate the condition. Thus it was often noted, that many patients got worse before they got better. And so, they are warned they must be obsessive-compulsive about avoiding salicylates, which he asserts, is all plant products.

That's what causes a lot of people to be apprehensive about taking on the guaifenesin cure for fibroyalgics. One is the fear of getting worse rather than better, and two, the obsession over avoiding contact with all plant material requires a lifetime of dedication. The fact is, guaifenesin works, as anybody who's taken cough medicine knows -- along with aspirin when they have a respiratory inflammation. If it is liquifying the mucus in your respiratory tract, it is liquefying the mucus throughout your body.

It's a lot like blood thinners; it doesn't just work in the blood going to your head, or liver, or feet; it thins all the blood. Otherwise, you have an ad hoc explanation for the mucus in your lungs, in your digestive tract, in your joints, etc. The property of fluids is that they tend to equalize -- and that's what makes exchanges of fluids, gases, toxins and nutrients possible.

The doctor's cure is not the final word on this matter. If you search "guaifenesin," there are thousands of abstracts, generally narrowly focused but nobody connects all these studies into a comprehensive whole. However, each one notes very impressive properties -- one study notes that it is one of the most effective muscle relaxants. That's important because a explanation for FMS is that the cells are constantly firing -- or turned on and never gets to shut off or relax. That's the doctor's elaborate explanation on calcium regulation.

A lot of those associated with the doctor are pretty cultish in propagation of the guaifenesin cure. To these people Dr. St. Amand is a saint and his prescriptions and proscriptions must be followed to the letter, chapter and verse.

But there are a lot of others who have not been officially diagnosed "fibromyalgics." In my own case, doctors could never find anything wrong with me. That's a common experience with FMS -- that doctors often insisted it was "all in one's head." I don't go around diagnosing people as fibromayalgics but I run into a lot of people who tell me they have an arthritic knee, occasional backaches or common chronic ailments -- and I relate my experience and insight.

Lastly, I mentioned in a previous post that about 100 years ago, aspirin and guai were used as remedies for roughly the same afflictions -- and because of better marketing, aspirin became the remedy of choice for whatever ailed one. A lot of people can't tolerate aspirin and that causes its own problems -- but not in everyone! Some people can tolerate aspirin well; others cannot tolerate aspirin at all, regardless of whether they are on the guaifenesin cure or not. Rather than assuming one is aspirin intolerant, it's far better and simpler to assume one is not -- and then be more rigorous in avoiding the salicylates if one suspects he may be. Usually one knows by adulthood whether they tolerate aspirin well or not. That's why they created ibuprofen and then naproxen -- and those who couldn't tolerate those, the cox-inhibitors. But as any doctor would logically proceed, assume the simplest explanation first rather than the most complex and elaborate.

[MamaLucci]

Thanks so much for your informative reply. I just checked, and the Mucinex I bought IS the extended release. Does Mucinex make a fast acting tablet? If not, where can I find it?

[MikeHu]

"I assume that guaifenesin is a prescription drug and am wondering if her doctor, who is a general practioner is knowledgeble enough to prescribe it for her if she asked him to."

Guaifenesin used to be available both over-the-counter (fast-acting) and as a prescription (slow-acting, extended release) until the FDA decided there's no reason to keep it as a prescription medication since there's never been a problem with it.

Previously, whenever doctors prescribed guaifenesin, it had to be the extended release version because drug coverage would not cover over the counter medications -- but only prescribed drugs. Therefore there was this bias towards the extended release version -- for patients with drug coverage and quite a number of fibromyalgics were on permanent disability. So when the extended release no longer was a prescription drug, everybody had to buy their own -- whether extended or fast acting, the latter being considerably cheaper. At that point, there was tremendous confusion because although guaifenesin is really a cheap generic, the process for making it extended release is patented -- and not guaifenesin itself.

Immunesupport.com and http://www.guailife.com/ are the cheapest, easily available sources I know of without any complications of pretending to make it rocket science or in need of a presciption. If somebody can figure out how to order and have it shipped from Canada, in bulk (powder) form they are really cheap -- about 1,000 capsules worth for $10. They make a profit on selling the gelatin caps to put them in. Their sites are not user-friendly.

[MikeHu]

By the way, it's commonly known as Robitussin -- or any of those generic knockoffs, Tussin, Super-Tussin, etc. Buy the one without the other powerful active ingredients like pseudoepinephrine (PE), DM, CF. Those things are another story.

[MamaLucci]

Thanks for the link and all the great info. :)
FRegards.

[ExtremeUnction]

Seven years ago I had a sudden onset on chronic, debilitating neuropathic pain. This type of pain can best be described as, "sensitive to touch." That is, my back and shoulders were on fire, with unbelievable pin-prick/fire sensations. But if I took my shirts off,(no contact of skin to anything but air), the pain stops). My doctor put me on the anti-seizure drug, Neurontin. It worked, but at the doses required, it made me a zombie. My M.D. then switched me to 2 mg. of Clonazapam, once or twice a day, plus 100 mg of Tramadol, twice a day. The Clonazapam made me VERY sleepy at first, but I adapted to it. Today, I am pain free. I am down to just 2 mg. of Clonazapam, once a day. But if I miss a dose, look out! The neuropathic pain in my back and shoulders returns with a vengeance!!

Fellow Freepers. I once thought that pain was for sissies. But, in my case, my doctor said that my pain was likely caused by a back/nerve injury sustained long ago. If your doctor can't help you, go to another doctor. My doctor's philosophy is, no one should hurt in this day and age. I am pain free. I can barely remember my 2-3 years of terrible pain. But it can be fixed, You just have to search for the fix. Be aggressive. Complain. Do research. It's worth it..believe me.

[Judith Anne]

This is totally new to me--I know about guiafenisin and I know about aspirin--are you saying they aren't to be taken together?

In other words, could you explain a little further?

[MikeHu]

I'm not saying they shouldn't be taken together. According to the doctor who came up with the guaifenesin cure for fibromyalgia, he claimed that in the cases that it didn't work, it was because aspirin blocked its effects, and that aspirin blocks the effects of other medications too.

However, most of us have taken aspirin and guaifenesin for a cold with good results -- at least as a treatment for a cold. My contention is that it would then be highly unlikely that it would nullify that effect for the treatment of fibromyalgia -- and probably a more plausible explanation might be that those particular individuals could not tolerate aspirin well, as a more likely explanation than that it blocked all drugs in everyone.

If one has an intolerance or allergy to something, if he were to take it, it would override a medication until he stopped that exposure. One of the discoveries made over the last several years is that there is a greater intolerance to aspirin than had been thought initially when it was believed that nobody could possibly be allergic (intolerant) to aspirin. They used to say the same thing about milk -- as a perfect food for everyone.

That's what makes the guaifenesin cure as advocated by Dr. St. Amand problemmatical and more daunting for those considering it. The guaifenesin part is fairly straightforward and uncomplicated. But then he goes into a very tortuous explanation of why it might not work in some people -- rather than realizing that there's no cure that works for everybody unfailingly.

But if it works for you, that's all you need to know. If it doesn't, you have to continue your search.

[Judith Anne]

Thanks for the information on this thread. I appreciate it.

[Centurion2000]

bump

[andyandval]

look at this

[F16Fighter]

bump for later reading

[lonevoice]

Major ping to you, Pride. Please read all the posts from MikeHu beginning with #27.