Allopurinol is the most common pharmaceutical used to manage gout and it has been approved for use in the USA since 1966. Allopurinol does not end a gout attack and in fact it will usually make it worse if started during a flare.
Often confused as a gout treatment, allopurinol is designed to be used for prevention of future gout attacks and does this by lowering the amount of uric acid in the blood stream. This is accomplished by three different methods which I explain below.
The Basics: Uric Acid
Gout is specifically caused by having an excess of uric acid in addition to an overall condition of acidosis, which means your body is too acidic in general. The more uric acid you have circulating in your blood, the greater the chance of getting a gout attack. The excess occurs when there is either too much uric acid being made, or not enough is being eliminated (in urine), or both.
Uric acid is not necessarily a bad thing. When it becomes excessive, it is the cause of the pain of a gout attack. In fact, in its normal role, uric acid it is beneficial, because it facilitates many essential functions in the body to keep it healthy and running smoothly. Also, uric acid is a major antioxidant. Medical science estimates that half of the total antioxidant action in the body is provided by uric acid.
Possibly the most important role of uric acid has to do with cellular regeneration. The two proteins that make up uric acid also make up half of the cell’s genetic material in DNA and RNA. These two proteins are called xanthine and hypoxanthine.
Here is the important part: Cells in the body are constantly dying and regenerating. When the cells die and are broken down, xanthine and hypoxanthine are released from the DNA/RNA, and then join back together to form uric acid.
When new cells are being born they require the same proteins, xanthine and hypoxanthine, as building blocks – these proteins come from uric acid. The body breaks down uric acid to provide the xanthine and hypoxanthine needed to build new cells.
Cells breakdown and free their xanthine and hypoxanthine, which then combine into uric acid, which is used as an antioxidant. Uric acid then gets broken down to free xanthine and hypoxanthine, which is then used as building blocks for the DNA and RNA in new cells.
This is how the body makes sure there is enough protein available to build new cells, and also how it makes sure there is enough uric acid to perform the function of an antioxidant (to protect the body by neutralizing dangerous free radicles).
Uric Acid Chemistry
There is a chemical that allows xanthine and hypoxanthine to join together to form uric acid. This is an enzyme called xanthine oxidase (XO). When the body needs to slow down the production of uric acid, it can slow down the production of XO.
The following is an explanation of how this works:
- Hypoxanthine is what is called an “XO-inhibitor”. When the body “sees” an excess of hypoxanthine, it wants to get rid of the excess. And the body can eliminate hypoxanthine (and also xanthine) easier than it can eliminate uric acid. In order to eliminate hypoxanthine more quickly, the body slows down production of XO, which slows down production of uric acid, which speeds up elimination of the excess hypoxanthine.
This whole process is called a “negative feedback loop” in pharma-talk.
Fool Me Once
Allopurinol is an “analog” of hypoxanthine. An analog is a molecule with all the same atoms as another molecule but arranged differently. In the body, analogs are often “seen” to be the same as the authentic molecule, and can easily be changed into each other’s form.
When you begin taking allopurinol, it provides an excess of the xanthine and hypoxanthine, which leads to excess production of uric acid. This is how allopurinol can worsen an attack, if started during an attack.
Fool Me Twice
Once the body “sees” the increase in xanthine and hypoxanthine, it suppresses the production of XO, which decreases production of uric acid. Remember that the body can eliminate xanthines and hypoxanthines easier than it can uric acid. The net result is that uric acid levels in the blood go down. This means you have less chance of having another gout attack.
This is one of the ways that allopurinol helps prevent gout flares. It acts as a primary xanthine oxidase inhibitor. It “fools” the body into reacting to what it thinks is too much xanthine and hypoxanthine.
More DNA and RNA Please
A second way that allopurinol helps prevent gout flares is by “driving” or “forcing” xanthines and hypoxanthines to combine into new DNA/RNA production…that way some of them become unavailable to make uric acid. This effectively lowers uric acid blood levels because there is less material available to make uric acid…hence fewer gout attacks.
Use It or Lose It
A third way that allopurinol helps prevent gout flares is by increasing the excretion of uric acid. Science has identified several places inside the kidneys where uric acid gets moved into the stream of urine to be eliminated.
And since allopurinol is very closely related to the chemical structure of uric acid, when you start taking allopurinol the body gets a “message” that there is an excess of uric acid which it needs to be rid of. This is a signal to the kidneys to increase the rate of elimination .
Thus allopurinol increases excretion of uric acid, and also increases excretion of xanthines and hypoxanthines. The result is that lower levels of building blocks (xanthine and hypoxanthine) and also lower levels of “end product” (uric acid) end up in the blood stream to cause a gout attack.
- Brand names of generic allopurinol include Zyloprim, Zyloric, Zyrik, Progout, Alloril, Milurit, Allosig, Allohexal and Aluron.
- When starting allopurinol, lower doses should be initiated and increased over time, so as to not trigger a gout attack or make a current attack worse.
- Dosing often will start at 100mg a day for one week, then go to 200mg a day for another week, ending up at the maximum maintenance dose of 300mg a day.
- The lowest possible dose to prevent an attack should generally be used, which will vary from person to person.
- Allopurinol is in the pregnancy category “C”. Although it has been shown to rarely have effects on a developing mammal fetus, it should be avoided in pregnant women or those who are trying to become pregnant.
- Allopurinol and coffee share similar chemical properties. See my article on Coffee and Gout for more info.
- Allopurinol is sometimes used for conditions other than gout, such as uric acid kidney stones, Tumor Lysis Syndrome and an inherited genetic condition called Lesch-Nyhan Syndrome.
Side Effects of Allopurinol
According to Drugs.com, noticeable side effects of allopurinol are uncommon, but as with all pharmaceuticals there are “unseen” side effects. The noticeable ones include skin rash, diarrhea, nausea, drowsiness and itching.
The unseen side effects include increases of overall acidity in the body, which puts extra burden on your kidneys, liver and other organs. Although allopurinol has been used relatively safely for over fifty years, these unseen side effects do take a toll on your overall health, and so The Gout Killer recommends that you AVOID all pharmaceuticals as much as possible, while being monitored by your health care practitioner of course.
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Hey Bert, I’d have to say at 5, it’s getting a lot better, and I’d have to say on it’s way out after using your methods. I love reading about all the knowledge you know; it’s pretty much changed my mind frame about things. I don’t get gout all the time, it comes now and then, but your book is awesome! I’m a big fan! Your The Man! ~ Nifae
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Obviously, preventing the horrific pain of gout is top priority, but the use of any type of pharmaceuticals should be a last resort. Until all avenues of natural, holistic, and lifestyle changes have been made, the potential risks of using a man-made artificial drug should not be taken lightly.
If your gout could be controlled by all-natural lifestyle changes, would you subject your body to the burden of daily use of pharmaceutical drugs like allopurinol?
I urge you to adopt a “whatever-it-takes” attitude about the changes needed to free yourself from gout for good. If you’re serious about improving your health, not only will gout become a thing of the past but you will feel better and be healthier in every other way too.
Personally, I have made a number of simple and affordable lifestyle changes, and as a result I have not had a single gout attack in many years. You can do this too! I talk all about the lifestyle changes that worked for me in my video-based program, Kill Your Gout FOR GOOD.
☆ Remember! Allopurinol Is Just One Method Of Many For Managing Gout.
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