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COX-2 Inhibitor

Many of the arthritis drugs reviewed in these web pages are referred to as "COX 2 Inhibitors."

To understand this term, start with my essay on "pain" where I comment that pain is usually associated with inflammation. This has been so universally considered true, that any remedy which reduces inflammation is expected to reduce pain.  So, an "anti-pain" medication is generally, in truth, an "anti-inflammation" medicine.

The question about how to stop pain is really the question of how to reduce or eliminate inflammation.

I've chosen one article on the Cox-2 Inhibitor to give you background.  My own fair comments are interspersed within the article, in blue type.

Source

Welcome to Dr. Nelson's

Cox-2 Inhibitor Page

First posted July 24, 2001 Last updated April 18, 2002

You are here because you want to know more about non-steroidal antiinflammatory drugs (NSAID's) and COX-2 inhibitors.

A common class of medications used in the treatment of arthritis and post-operative pain are called non-steroidal anti-inflammatory drugs, or NSAID's.

This name comes from non-steroidal (that it, they are not steroids), and anti-inflammatory (because they fight inflammation, a complex biochemical process that results in the swollen, tender joints of arthritis). These drugs block the action of an enzyme called cyclo-oxygenase. (See the section below for an explanation.) The chief side effect of NSAID's is stomach irritation, which can be anything from simple inflammation to life-threatening stomach bleeding. Although it is rarely serious, it can be. According to an 1998 article in the American Journal of Medicine, over 100,000 patients are hospitalized for the effects of NSAIDs and 16,500 die each year. This is serious stuff.

Here's a Simple Explanation of COX-2 Inhibitors

Philosophical Background (skip this section if you want to keep it simple)

Evolution proceeds by modifying the structure and use of an existing structure, not by creating new structures de novo. Bird wings, for example, came from quadruped forelimbs, which in turn came from the pectoral fins of lobe-finned fishes. Evolution not only proceeds by changes in the structure and use of existing structures, but from the changes in the structure and use of existing chemical processes. It should come, then, as no surprise that the chemical cyclo-oxygenase, an enzyme involved in the process of pain, is an enzyme that has existed for a very long time and therefore also has been adapted for use in many different chemical pathways.

Karl Note:  Like many medical doctors this one appears to NOT believe in God, or in God's creation of life. The Darwinian Theory of Evolution has long been disproved. Those doctors who believe in this type of stuff are usually very much oriented to chemicals being the source of life. They think that since that is true, chemicals must be the remedy for disease. Such doctors hardly ever accept alternative remedies. This does not mean that his technical data is false, just that he looks at chemicals for solutions.  I do not!

Pictorial Explanation of COX-2 Inhibitors

Basically, our body is a big chemical factory, with Chemical A making Chemical B and so on, until it produces the final product, D. Each step is facilitated by an enzyme, represented here by the arrow. For example, in the stomach, Chemical A makes Chemical B, etc, which leads to D, which is stomach mucous, the lining of the stomach and the way that the stomach protects itself from its own acid. Without this protective lining, the stomach just digests a hole in itself, creating a stomach ulcer, and bleeding. The bleeding can be serious enough to kill you.

Karl Note: Chemicals can never be adequate to explain the function of "life."  Life does NOT depend on the interaction of chemicals.  However, this statement does not preclude the physical science accuracy of the above.  The above describes effects, not causes.  Dr. Nelson's data is probably OK as far as it goes, but he suffers from being inside the Allopathic box, and cannot think outside that box!

Here's another example: In your joints, you may have Chemical Z going to Chemical Y by an enzyme, and then to Chemical X by another enzyme, etc. Chemical V is a substance called prostaglandin E2, which is the substance that causes the joint pain of arthritis. Aspirin, Motrin, and other anti-inflammatory medications block the production of prostaglandin E2, by blocking one of the enzymes (shown here by the arrows) that make it.

Karl Note: There is completely omitted here any possible cause of the above. The above may be an accurate scientific representation of the action of enzymes, for instance, but most doctors shy away from naming the original cause of this type of sequence of actions.  Any drug which is administered in denial of true causation can never be the best remedy.  Only on this web site, and for the first time in "health technology" is there a true theoretical description of what PAIN is.  The most important theoretical presentation on this web is Karl Loren's breakthrough description of exactly what PAIN really is.

It just so happens that the middle enzyme in both these processes is the same enzyme, and it is called Cyclo-oxygenase. Even the researchers got tired of calling it that, so they called it COX for short. It turns out that when your anti-inflammatory medicine blocks the sequence of chemical reactions that results in V (joint pain), it also blocks D (stomach lining). That is why NSAID's cause stomach ulcers!

Karl Note:  The absence of true causation is deceptive.  It seems "rationale" to say what the doctor says.  What is missing, as always, are the associated factors that may truly identify causation.  This doctor, like almost all others, has fallen without even knowing it into the clutches of chemical medicine. That, too, has an origin and is fully explained HERE where you learn of the impact of Dr. Wundt and behavioral psychology on medicine and education.. 

Then someone discovered that the two COX enzymes were not the same, that there was a very small difference between them. They called one COX 1 and the other COX 2. Someone else then discovered that they could create a NSAID that blocked COX 2 (so you wouldn't get joint pain) but it would not block COX 1 (and wouldn't get a stomach ulcer). Wasn't that a neat trick?

For a more complex discussion of COX-2 inhibitors, click here.

There are now two COX 2 inhibitors on the market, Celebrex (pronounced sell'-uh-brex) and Vioxx. They are not any more effective than Motrin (Ibuprofen), but they are safer. The medicines are a lot more expensive (about $100 per month!), so many insurance companies try to limit the patients who have access to these medications.
 

The indication for the use of a COX-2 inhibitor over a regular NSAID are not clear. Remember the article I quoted above, which stated that over 100,000 patients are hospitalized for the effects of NSAIDs and 16,500 die each year. My own thought is that each patient should know about COX-2 inhibitors and make their own choice. Anyone who is healthy and taking NSAID's for a short time (less than a month) probably need not worry. Patients who are over 40 and will be on long-term anti-inflammatory medication might want to consider them, but in general may not need to spend the money for a COX-2 inhibitor. Patients who are over 65, and especially if they are facing other serious illnesses, should probably be taking a COX-2 inhibitor. Again, there are no clear indications. My medical philosophy is that I give you information, help you to understand the issues, and in the end you control your own healthcare. Look at the Celebrex and Vioxx websites, think about it, and discuss it with me next time you are in. The American College of Gasteroenterology has written some information about ulcers, but they have not taken into account the new COX-2 inhibitors.

Recent press releases related to the COX-2 Inhibitors, click here.

Source

Dr. Nelson's Cox-2 Inhibitor Page

First posted July 24, 2001 Las updated February 15, 2003

You are here because you want more complex information about COX-2 inhibitors.

More Complex Explanation of COX-2 Inhibitors

Many, and perhaps most, cells of the body have the cyclo-oxygenase enzyme in them. Given the importance of the pain signal to the survival of the organism, the cyclo-oxygenase pathway leading to prostaglandin E2 most likely evolved very early in the history of life. If this is true, then it probably also has been around long enough to have been incorporated into many other biological processes, and this is exactly what medical research has found. COX is used by the stomach to create the mucous which lines the stomach and prevents it from digesting itself, by platelets in the process of clotting, in the kidney to perform normal function, etc. This explains why, when you take aspirin or Motrin, you bleed more easily (we use this to our advantage in preventing heart attacks and stroke), develop stomach ulcers, etc. This COX enzyme is a normal constituent of the cell and therefore is called a constituitive enzyme.

The COX enzyme that is involved in pain, arthritis, and inflammation in general, is not normally present, but is induced on demand by the cell. This is called an inducible enxyme.

It was discovered that these two COX enzymes are not identical; they are very similar, but not identical. They were therefore given different names: the constituitive enzyme is called COX-1 and the inducible enzyme is called COX-2.

After a lot of work, it was discovered how to block COX-2 but not COX-1. This allows the body to continue with its normal processes (we are not blocking the constituitive enzyme) while decreasing pain and inflammation (we are blocking the inducible enxyme).

There has been some questions about whether or not COX-2 inhibitors will influence fracture healing, since inflammation is a necessary first step in bone healing. You can read more here. There is also question about COX-2 inhibitors and fusion. You can read more here.

This information may help you to decide if you want to spend the money for the COX-2 inhibitors, which cost more than regular NSAID's.

RESEARCHERS SHOW COX-2 INHIBITORS INTERFERE WITH BONE GROWTH, HEALING

You can reach Karl Loren at www.PainStudy.com by mail at 1831 N. Bel Aire Drive, Burbank, CA 91504.  Within the US and Canada, use the toll free number:  (800) 523-4521, the local number:  (818) 558-1799, the FAX:  (818) 558-7299, eMail to karl@painstudy.com

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