Guaifenesin is a substance that helps loosen and liquefy mucus, and as such is a common component of many nonprescription cold and cough remedies. It is derived from a tree bark extract called guaiacum, historically appreciated for its expectorant qualities in the Caribbean region and adopted by European explorers in the 1500’s.
Some 400 years later, in 1952, guaiacum was approved for use as an expectorant by the Food and Drug Administration. And 20 years ago the extract was synthesized, pressed into tablets, and named guaifenesin.
How Guaifenesin Works
Guaifenesin works by drawing water into the bronchi – the air passages branching into our lungs. The released water both thins the mucus and lubricates the airway, facilitating the removal of cold, flu and allergy-associated mucus from the chest by coughing, and making it easier to breathe.
Guaifenesin is also considered helpful for thinning postnasal drainage from the sinuses and reducing nasal congestion,(1) and so may relieve sinus pressure/ headache. As Dr. Sarah Myhill comments, “Whoever designed the human body needs a black mark for putting in sinuses! They are cavities in the bones of the face with only one entry and exit hole which is easily blocked by catarrh or swollen mucus membranes.” When this occurs, less oxygen can enter the sinuses, promoting bacterial overgrowth and causing sinusitis.
Here again, guaifenesin can help to relieve congestion by increasing the clearance of secretions, helping with the mucus membrane’s natural job of washing away invading viruses, bacteria, pollen and other potential allergens – “the first level of immune defense.”
Guai also enjoys a popular reputation as ‘the opera singer’s friend.’ Terming it their ‘wonder drug,’ singers have traditionally used guaifenesin to improve the state of their vocal folds in extremes of humidity (very dry or very humid), after flying long distances, and during mild allergies, for its ability to promote ‘secondary mucosal secretion’ – the thinner, lubricating mucus that occurs on the vocal folds naturally when they are healthy and well hydrated.
Patients with chronic obstructive pulmonary disease (COPD) may find guaifenesin’s thinning and lubricating action helpful at times when they experience particular difficulty coughing up the thick or sticky mucus that can block their damaged airways.
Similarly, guaifenesin can assist by thinning ‘sticky’ mucus to help expel inhaled particles that can exacerbate asthma symptoms.
Importantly, whether used to ease the congestion of colds, flu, or rhinosinusitis, or to support healthy vocal folds, guaifenesin works best if one drinks plenty of water, as extra fluids increase the flow of water and mucus.
As with many complex herbal compounds used in traditional medicine, exactly how guaifenesin encourages healthy mucus flow is not yet completely understood. But based on its long history - if taken as instructed on the package or as suggested by a pharmacist or healthcare provider - guai has at most minor side effects and is generally considered safe for use even by youngsters over 12 years of age.*
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The Guifenesin Protocol for Fibromyalgia Patients
Guaifenesin is also used in the very popular Guaifenesin Protocol for symptoms of Fibromyalgia, conceived by R. Paul St. Amand, MD, Assistant Clinical Professor of Medicine in Endocrinology at UCLA.
Though highly demanding and still considered experimental, the Protocol has been adopted by many FM patients, owing to widespread anecdotal descriptions of quality-of-life benefits. Nevertheless, note that Guaifenesin has not been approved by the FDA for this application and should be used as such only with the approval and supervision of a medical doctor familiar with the patient and Protocol.
The Protocol’s Underlying Theory
Dr. St. Amand explains this in his book written with Claudia Marek, What Your Doctor May Not Tell You About Fibromyalgia, and their article on Fibromyalgia symptoms, diagnosis, and the Guaifenesin Protocol. The theory is that:
• Excess inorganic phosphate compounds accumulate within the cells of some people rather than being excreted normally, possibly owing to a genetic defect involving a missing enzyme or kidney dysfunction.
• It is known that excess phosphate in the cells’ mitochondria impedes their formation of adenosine triphosphate (ATP), the body’s energy source - and that muscle pain after exercise is linked with an inorganic phosphate increase. Also, researchers have reported a 20 percent average reduction in the level of ATP in muscle biopsies taken from people with FM, notes self-described Guaifenesin Protocol beneficiary Devin Starlanyl in her book, Fibromyalgia and Chronic Myofascial Pain: A Survival Manual.
• When excess phosphate builds up in the cells, excess calcium – the main buffer for phosphate – builds up too. Excess calcium in the cells tends to stiffen the body’s tissues.
• A method of palpating muscles, tendons, and ligaments that Dr. St. Amand has described allows a physician to “map” or assess the extent of lesions in the tissues of FM patients, thought to be “contracted cells forming a spastic area caused by an excess of calcium.”
• A carefully planned, monitored regime of guaifenesin extract supplementation may help the body eliminate the excess calcium and phosphate compounds, supporting improvement of FM symptoms over time in some individuals.
Dr. St. Amand has reported increases of 60% in phosphate excretion and 30% in calcium excretion.
What the Guaifenesin Protocol Involves
Basically, it includes:
1. Adjusting or “titrating” the guaifenesin dosage to the individual’s needs, based on response over time.
2. Strict avoidance of the salicylates in aspirin and other similar pain-relief products, plus a long list of personal care products including plant derivatives such as aloe or mint that are applied to and absorbed through the skin; and many plant extracts taken by mouth. These can completely block the action of the guaifenesin. Salicylate-containing foods are not a problem, as the digestive process neutralizes their effect.
3. And strict adherence to a low carbohydrate diet, if the individual is hypoglycemic.
The Protocol also commonly delivers a significant physical impact in the early weeks, including a worsening of the individual’s worst FM symptoms, and frequently headaches, burning on urination, and/or strong-smelling perspiration and urine. These are not considered side effects, but rather “the signs and symptoms of the toxins and wastes being released by the guaifenesin” - and therefore an indication that the Protocol is working.
So far the Guaifenesin Protocol has not been demonstrated effective in a controlled clinical trial, or approved by the FDA for support of Fibromyalgia symptoms. An early one-year trial completed at the University of Oregon in June 1995 by Dr. Robert Bennett concluded that “patients in the placebo group compared with patients in the guaifenesin group appeared to improve equally - a finding that suggested a placebo effect,” says Dr. St. Amand. But “it is our belief that this study was flawed, due to our own lack of knowledge,” he explains.
Though Dr. Bennett’s patients were warned to avoid aspirin and aspirin-containing compounds, it wasn’t until after the study was completed that Dr. St. Amand came to understand the immense number of personal products and ingested plant extracts that, even in minute quantities, could reverse patients’ progress.
Also, in reviewing the patients’ wellness questionnaires, he noted that the study had not screened for hypoglycemic individuals, who therefore were not treated with the necessary diet.
As a result, he contends, “the study was doomed for lack of knowledge of these pitfalls.”
The Status of Research
Currently, one of the stated goals of Dr. St. Amand’s not-for-profit Fibromyalgia Treatment Center is to provide supporting research for the Guaifenesin Protocol.
He is now engaged in a multi-year investigation with The City of Hope that involves a cohort of his FM patients (an "Immunological and Genetic Analysis of Autoinflammatory Genes in Fibromyalgia"). By mid-2008 the research had identified abnormal elevations in a cluster of inflammatory cytokines that appear highly predictive of Fibromyalgia, two of which drop to normal in patients taking guaifenesin.(2) And in November 2008 Dr. St. Amand issued a call to patients he has diagnosed with FM, to widen the sample of DNA used in the investigation.
In the meantime, the scores of physicians who employ the Guaifenesin Protocol – as well as many of the individuals, like Devin Starlanyl, who have adopted it – provide personal testimonials indicating that this regimen supported significant improvements in their Fibromyalgia symptoms.
1. See "Guaifenesin & Sinusitis," by Jule Klotter, Townsend Letter for Doctors and Patients, Nov 2005.
2. See "Dr. St. Amand Comments on First Report from City of Hope Fibromyalgia Research."
* Note: As with all decisions involving your healthcare plan or health support regimen, it is very important to research and discuss guaifenesin and any potential side effects in collaboration with your professional healthcare team, to ensure it is considered in light of your personal health status and all other herbs, supplements, and prescription medications you currently take. This information has not been evaluated by the FDA and is not intended to prevent, diagnose, treat, or cure any illness, condition or disease.