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Since Tesa published the Product Troubleshooter FAQ, many list members have been asking this question. The purpose of this discussion is to provide some background information that may help you to make the choice, working with your personal physician/healthcare provider. Principles of drug action For those who want to bend their minds to the technicalities of the body's management of drugs, click here for a 'starter' link. But be warned, this is a seriously addictive journey, with no end in sight for those who have embarked on it. And for those who want more: Summary of Interactions with Vitamins, Herbs, and Foods
On p.65 of the book, Dr St Amand states, "Any pure guaifenesin which has no added pseudoephedrine, dexromethorphan, or any of the other compounds that may cause side effects is recommended." and "Guaifenesin is available in 200 mg
tablets over the counter, but I do not recommend self-treatment." What do some of these terms I've been reading about mean? To help you understand the information that will be discussed here, it may be useful to understand some of the terms that will be used: Absorption - In layperson's terms, when we take a pill, this is the action of our digestive systems (mostly our intestines) that moves a substance we have ingested out of our digestive tract into our bloodstream. To be effective at reversing fibromyalgia, the guaifenesin in a pill must be absorbed before it can enter our bloodstreams and be transported to our kidneys, the site of it's action. Absorption into the bloodstream can also occur through the skin, in which case our digestive systems are not involved. Active ingredient - The drug of interest when you take a pill, put on a skin patch, or rub a cream or gel into the skin -- in our case, guaifenesin. This is the substance contained in a capsule/tablet/syrup/cream/gel that has the effect(s) we're looking for when we take it. Additives (inactive ingredients) - These are the other chemical compounds that are added to a capsule/tablet/syrup for various purposes. Additives will be discussed in some detail below. Dissolution - This term refers to the extent to which a tablet (or any substance we ingest) dissolves in our intestinal tracts. A tablet of guai has to dissolve before the guai can be absorbed. Half-life - The half-life of an active ingredient is the length of time it takes for the ingredient in our bloodstream to be reduced by one-half of the original amount that was administered. It can be used to calculate how much of the ingredient is still in the bloodstream after a period of time. For example, the amount of a drug remaining in our bloodstream 1 hour after an injection of 100mg of the drug, if it had a T1/2 (the abbreviation for half-life) of 1 hour, would be reduced to 50mg. After 2 hours, the amount remaining would be 25mg, and, after three hours, only 12.5mg would still be in our bloodstream. The half-life of guai is 1 hour. Long-acting (LA) - In our case, this refers to the characteristics of a tablet that are designed to delay the release of the guaifenesin into your system for a period of time. Although we use the term, "LA guai," it is somewhat inaccurate, because it sounds like we are talking about the drug, guaifenesin, itself. But we're not. Guaifenesin always has a half-life of 1 hour. Rather, when we say, "LA guai," we're actually talking about how the guaifenesin tablets are constructed so that only a little guai is released into your system at a time, over a period of time (12 hours in most cases). A more accurate term for these tablets is "sustained or extended release." "LA" refers to a dosage form, not the drug itself. Long-acting drugs usually have active metabolites (break-down products). Quick-acting (QA) - Again, this term refers to how a dose of guai is delivered to your system, not to the guai, itself. In one sense, all guai is "quick-acting," because it has a relatively short half-life, compared to other drugs. But we use the term, "QA guai," to refer to forms of taking it that do not substantially delay the release of the guai over time because of how they are constructed. What are the different
ways to take guai? With the exception of tablets that are specifically constructed not to dissolve right away (LA guai), all of these guai-delivery methods release the full dose of guai in a relatively short time after taking the dose. For example, when we swallow a gel cap, our digestive systems first have to dissolve the gel cap and then absorb the guai powder that was contained inside it. With syrup, our digestive systems don't have to first dissolve a gel cap before the guai is available to be absorbed, so the guai may hit our bloodstreams sooner than with gel caps. But, there could possibly be inactive ingredients in the syrup that could somewhat delay absorption of the guai for some people. With QA tablets, our digestive systems have to first break down the tablet before the guai is available for absorption, so it might take a little longer for the guai to be released and absorbed than with a gel cap or syrup. With guai cream or gel, the digestive tract is avoided altogether and the guai goes directly into our bloodstream. With LA tablets, it SHOULD take a long time before the entire tablet dissolves and the full dose of guai has been released for absorption. The LA tablets are designed so that they dissolve slowly and release only a little guai at a time. Are there different types
of guai? Is absorption important? What can affect
absorption? Ansel, Popovich, & Allen (1995), on p. 75 of 'Pharmaceutical Dosage Forms and Drug Delivery Systems' (published by Williams & Wilkins: Media, PA) state, "The variables that can contribute to the differences between products are many. For instance in the manufacture of a tablet, different materials or amounts of such formulative components as fillers, disintegrating agents, binders, lubricants, colorants, flavorants and coatings may be used... The tablets may vary in shape, size, and hardness, depending upon the punches and dies elected for use by the manufacturer and the compression forces utilized in the process. During packaging, shipping and storage the integrity of the tablets may be altered by physical impact, or changes in conditions of humidity, temperature, or through interactions with the components of the container. Each of the factors noted may have an effect on the rates of tablet disintegration, drug dissolution, and consequently on the rate and extent of drug absorption." What additives are
typically used in manufacturing tablets and capsules? Tablet antiadherents - These are substances, such as magnesium stearate or talc, that prevent the ingredients of a tablet from sticking to the machines used to make them. Tablet binders - These are substances, such as methylcellulose or povidone, that are used to "glue" the ingredients in a tablet together. (In LA guai tablets, methycellulose is most often used to "hold" the guai powder so that it is released very slowly.) Tablet or capsule fillers - These are substances, such as lactose, cellulose or dibasic calcium phosphate, that are used to increase the bulk (amount) of the ingredients or to change the compression characteristics of the ingredients used to manufacture a tablet or capsule. Tablet coating agents - These include substances used to coat a tablet so that it is resistant to heat, humidity, or air, so that the tablets don't break down when they are exposed to the environment. Other coatings, such as sugar, may be used to improve the taste of a tablet. Or, enteric coatings may be used that prevent the tablet from breaking down until it reaches your intestines (will pass through your stomach) to help with gastrointestinal upsets. Tablet excipient - Dibasic calcium phosphate is often used in making guai tablets to help compress the powder ingredients into a tablet form. Tablet disintegrants - Used to promote the breaking up of a tablet into smaller particles that are more readily dissolved. Disintegrants include alginic acid, carboxymethylcellulose calcium, and starches. Tablet and capsule glidants - These help improve the "flow" characteristics of a powder mixture, and include colloidal silica, cornstarch or talc. Tablet lubricants - These are used to reduce friction when making a tablet, and include calcium stearate, mineral oil or stearic acid. Flavors and colors - These include natural and artificial flavors, and dyes. Are different additives
used in LA vs. QA guai tablets and capsules? Quick-acting guai capsules and tablets do not include the delaying additives that are used to construct the LA pills. This means that when you take a 600mg QA tablet in the morning, for example, and your digestive tract is working normally, the full 600mg dose of guai will be released into your digestive tract as soon as the capsule or tablet dissolves, and all of the guai in the tablet or capsule will enter your bloodstream in a much shorter period of time. Other than the delaying additives, however, LA and QA tablets may include many of the same additives needed to manufacture the tablets. Binders, antiadherents, excipients, and fillers, for example, may be used in manufacturing both LA and QA tablets. Dyes and flavors may also be used in tablets or syrup. Guaifenesin powder in gel caps usually does not include any additives. What differences between
people affect how well guai is absorbed? What about the dyes in my
guai tablets? Why are cycling symptoms
sometimes more intense when taking QA guai than LA guai? Another reason may be that some people are better able to dissolve QA tablets or capsules than LA tablets because their digestive tracts have a difficult time breaking down the LA tablets due to the additives, or because the LA tablets they were taking were very tightly compressed, or some other factor. Or, there may be something about the additives that interferes with absorption for a particular individual. The combination of removing any barriers to absorption and the difference in the rate at which guai is released into your system with QA guai, together, may mean that your kidneys are receiving A LOT more guai than they were before. If you were having absorption problems with your LA guai and don't with the QA guai, the actual amount of guai hitting your system from a 600mg QA dose could be even greater than 12 times the guai you were receiving from the 600mg LA pill! What are the advantages of
taking LA guai? A second important advantage of LA guai is that you may avoid the "rollercoaster effect" that some people experience in their cycling symptoms when taking QA guai. Because the full dose of QA guai hits your system at once, and then the amount of guai in your bloodstream decreases at a relatively rapid rate over the next few hours, you may have a couple of hours of feeling awful after taking your dose, and then a couple of hours of feeling nothing until your next dose. Also, if you are someone who does better when maintaining a constant level of guai in your system, you may find that you begin feeling worse and worse the longer it has been since taking your last QA dose. These kinds of ups and downs are avoided with the steady stream of guai that LA tablets deliver. What are the advantages of
using QA guai? Using QA guai to do a blocking test is also good, because if you aren't blocking, the increased cycling symptoms from raising your dose for the blocking test will last for a much shorter period of time than if you raise your dose by taking additional LA guai. Your response will be much more obvious regarding whether you are or are not blocked. And, if you are someone who might have a digestive tract problem of some sort, the reduced or eliminated additives in QA guai may allow you to absorb the guai much better, so that your progress on the protocol is enhanced. Further, if you end up being one of the fortunate ones who need a lower dose of QA guai than LA guai, QA guai may end up being less expensive to take. Of course, that depends on your insurance coverage, where you buy your guai, and so on. But how do I handle the
more intense cycling symptoms if I take QA guai? The first method is to take smaller doses more frequently over the course of the day. If you want to take a 600mg/day dose, you might need to take 200mg three times a day, rather than 300mg twice a day. The second method is to take your doses with food. The food may slow down the rate at which your digestive tract dissolves the tablets. Third, (careful here) you many need to reduce your daily dose from what it was with LA tablets. If you are dissolving/absorbing the QA guai better than the LA guai, you may be able to reduce your dose and still end up with MORE guai in your system than you were getting with the LA tablets. If you are just starting out on the protocol and are using QA guai, it may be wiser to start out at 400mg/day or less, rather than 600mg/day with LA guai, and then titrate up from there to find the dose at which you are "significantly but tolerably worse." If you are switching from LA guai to QA guai, and feel that you need to reduce your dose, it is very important that you are mapped regularly for at least 3 months following the dose reduction to make sure you haven't gone below your cycling dose. Why have some people
reported that their maps show significantly more deposits after switching from
LA to QA guai? First, if you weren't absorbing the guai contained in your LA tablets very well, but do absorb the guai in a QA form more effectively and have stayed on the same daily dose, it's very possible that you are flooding your bloodstream with phosphates, because your dose on the QA guai is actually now too high. When this occurs, we know that our bodies will temporarily store the phosphates in various sites (often your neck and upper back) until your kidneys can clear them out of your bloodstream. If you continue taking the same dose of QA guai over time, the number of temporary deposits will continue to increase, until your map once again looks like you are a Dalmatian. This result can be very upsetting, because it looks like you are going backwards and you will likely be feeling terrible. Reducing your QA dose will stop the phosphate flooding and give the temporary storage sites an opportunity to clear. The big problem with this process is the pain involved!! The phosphates hurt when they come out of your tissues the first time, hurt when they go back into temporary storage, and then hurt again when they are pulled out. The second possible reason, of course, is that if you have reduced your dose when switching, you may have gone too low and are, in fact, re-depositing phosphates in areas you previously cleared. The third possible reason is that you might be inadvertently blocking on something you've introduced into your life since making the switch and haven't discovered it yet! If I have switched to QA
guai and my map starts showing more deposits, what can I do? One of the ways in which you can distinguish between a too-high dose, a too-low dose, and blocking is by considering the rate at which your maps have changed. If you have been taking a too-high dose and are flooding your system with phosphates, you should see many new deposits in a very short time, i.e., on your next map. If your dose is too low, or you are blocking, the re-depositing seems to be slower. Your first map after switching may show no change from your last map, then the next one three months later may start showing some new deposits, and then there will be a noticeable difference after six months that is your clue. Most people don't want to wait this long, however, and do a blocking test, try raising their doses or switch brands of guai if they become concerned. Prepared by Val
Barnes based on pharmaceutical textbooks provided by Tom Slaughter of Mulberry
Pharmacy, information available on Dr. Greg Penniston's website and discussions
with him, information provided by Dr. Paul St. Amand in his book and in the
Guai-Support archives, comments from Dr. Tom Savino, and research literature
available on the web. Reviewed for pharmaceutical accuracy by Tom Slaughter and
Val's local pharmacist prior to publication on the website.. |
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Parting the Fog: The Personal Side of Fibromyalgia/Chronic Fatigue Syndrome By Sue Jones, a GG Member Parting the Fog" is a candid, first person account of what it is like to walk in the shoes of someone suffering from fibromyalgia/chronic fatigue syndrome. It relays the seriousness of this condition in an easy-to-read manner, while employing humor and focusing on hope.
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